Penicillin analogs. Antibiotics of the penicillin group: indications, instructions for use. Penicillin antibiotics Synthetic penicillin drug names

14.07.2020 Insulin


The first were the antibiotics penicillins, which saved many thousands of lives during the Second World War, and are relevant in modern medical practice. It was with them that the era of antibiotic therapy began and thanks to them all other antimicrobial drugs were obtained.

This section provides a complete list of currently relevant antimicrobial drugs. In addition to the characteristics of the main connections, all trade names and analogues.


Main name Antimicrobial activity Analogs
Benzylpenicillin potassium and sodium salts They mainly affect gram-positive microorganisms. Currently, most strains have developed resistance, but spirochetes are still sensitive to the substance. Gramox-D, Ospin, Star-Pen, Ospamox
Benzylpenicillin procaine It is indicated for the treatment of streptococcal and pneumococcal infections. Compared with potassium and sodium salts, it acts for a longer time, since it dissolves and is absorbed more slowly from the intramuscular depot. Benzylpenicillin-KMP (-G, -Teva, -G 3 mega)
Bicillins (1, 3 and 5) It is used for chronic rheumatism for prophylactic purposes, as well as for the treatment of infectious diseases of moderate and mild severity caused by streptococci. Benzicillin-1, Moldamin, Extincillin, Retarpin
Phenoxymethylpenicillin It has a therapeutic effect similar to the previous groups, but does not break down in an acidic gastric environment. Available in pill form. V-Penicillin, Cliacyl, Ospin, Penicillin-Fau, Vepikombin, Megacillin Oral, Pen-os, Star-Pen
Oxacillin Active against staphylococci that produce penicillinase. It is characterized by low antimicrobial activity, it is completely ineffective against bacteria unstable to penicillin. Oxamp, Ampiox, Oxamp-Sodium, Oxamsar
Ampicillin Extended spectrum of antimicrobial activity. In addition to the main spectrum of inflammatory diseases of the gastrointestinal tract, it also treats those caused by Escherichia, Shigella, Salmonella. Ampicillin AMP-KID (-AMP-Forte, -Ferein, -AKOS, -trihydrate, -Inotek), Zetsil, Pentrixil, Penodil, Standacillin
Amoxicillin It is used to treat inflammation of the respiratory and urinary tract... After finding out the bacterial origin of the stomach ulcer, it is used for the eradication of Helicobacter Pylori. Flemoxin solutab, Hikontsil, Amosin, Ospamox, Ecobol
Carbenicillin The spectrum of antimicrobial action includes Pseudomonas aeruginosa and enterobacteria. The digestibility and bactericidal effect is higher than that of Carbenicillin. Securopen
Piperacillin Similar to the previous one, however, the level of toxicity is increased. Isipen, Pipracil, Picillin, Piprax
Amoxicillin / clavulanate Due to the inhibitor, the spectrum of antimicrobial activity is expanded in comparison with an unprotected agent. Augmentin, Flemoklav Solutab, Amoxiclav, Amklav, Amovikomb, Verklav, Ranklav, Arlet, Klamosar, Rapiklav
Ampicillin / sulbactam Sulacillin, Liboccil, Unazin, Sultasin
Ticarcillin / clavulanate The main indication for use is nosocomial infections. Hymentin
Piperacillin / tazobactam Tazocin

The information provided is for informational purposes only and is not a guide to action. All appointments are made exclusively by the doctor, and the therapy takes place under his supervision.

Despite the low toxicity of penicillins, their uncontrolled use leads to serious consequences: the formation of resistance in the pathogen and the transition of the disease into a chronic form that is difficult to cure. It is for this reason that most strains of pathogenic bacteria are resistant to first-generation ABP today.

Use for antibacterial therapy follows exactly the medication that was prescribed by a specialist. Independent attempts to find cheap analog and save money can worsen the condition.

For example, the dosage of an active substance in a generic can differ up or down, which will negatively affect the course of treatment.


When you have to replace a medicine due to an acute lack of finance, you need to ask a doctor about it, since only a specialist can choose the best option.

The drugs of the penicillin group belong to the so-called beta-lactams - chemical compounds that have a beta-lactam ring in their formula.

This structural component is of decisive importance in the treatment of bacterial infectious diseases: it prevents bacteria from producing a special biopolymer peptidoglycan, which is necessary for building the cell wall. As a result, the membrane cannot form and the microorganism dies. There is no destructive effect on human and animal cells for the reason that there is no peptidoglycan in them.

Medicines based on waste products of mold fungi are widely used in all areas of medicine due to the following properties:

  • High bioavailability - drugs are rapidly absorbed and distributed through tissues. The weakening of the blood-brain barrier with inflammation of the meninges of the brain also contributes to the penetration into the cerebrospinal fluid.
  • Broad spectrum of antimicrobial action. Unlike the first generation of chemicals, modern penicillins are effective against the vast majority of gram-negative and positive bacteria. They are also resistant to penicillinase and the acidic environment of the stomach.
  • The lowest toxicity among all ABP. They are allowed for use even during pregnancy, and the correct reception (as prescribed by the doctor and according to the instructions) almost completely eliminates the development of side effects.

In the process of research and experiments, many medications were obtained with different properties... For example, when belonging to a common series, penicillin and ampicillin are not the same thing. All penicillin antibiotics are well compatible with most other drugs. Concerning complex therapy with other types of antibacterial drugs, then combined use with bacteriostatics weakens the effectiveness of penicillins.


A careful study of the properties of the first antibiotic showed its imperfection. Despite a fairly wide spectrum of antimicrobial action and low toxicity, natural penicillin was found to be sensitive to a special destructive enzyme (penicillinase) produced by some bacteria. In addition, it completely lost its qualities in an acidic gastric environment, therefore it was used exclusively in the form of injections. In the search for more effective and stable compounds, various semi-synthetic drugs have been created.

Today, penicillin antibiotics, a complete list of which is given below, are divided into 4 main groups.

Produced by the molds Penicillium notatum and Penicillium chrysogenum, benzylpenicillin is an acid in molecular structure. For medical purposes, it chemically combines with sodium or potassium to form salts. The resulting compounds are used to prepare injection solutions that are rapidly absorbed.

The therapeutic effect is noted within 10-15 minutes after administration, however, it lasts no more than 4 hours, which requires frequent repeated injections into the muscle tissue (in special cases, sodium salt can be administered intravenously).

These drugs penetrate well into the lungs and mucous membranes, and to a lesser extent into the cerebrospinal and synovial fluids, myocardium and bones. However, with inflammation of the meninges (meningitis), the permeability of the blood-brain barrier increases, which allows for successful healing.

To prolong the effect of the drug, natural benzylpenicillin combines with novocaine and other substances. The resulting salts (novocaine, Bitsillin-1, 3 and 5) after intramuscular injection form a drug depot at the injection site, from where the active substance enters the bloodstream constantly and at a low speed. This property allows you to reduce the number of injections up to 2 times a day while maintaining therapeutic effect potassium and sodium salts.

These drugs are used for long-term antibiotic therapy of chronic rheumatism, syphilis, focal streptococcal infection.
Phenoxymethylpenicillin is another form of benzylpenicillin intended for the treatment of moderate infectious diseases. Differs from those described above in resistance to hydrochloric acid of gastric juice.

This quality allows the drug to be produced in the form of tablets for oral administration (4 to 6 times a day). Most pathogenic bacteria, except for spirochetes, are currently resistant to biosynthetic penicillins.


See also: Instructions for the use of penicillin in injections and tablets

Natural benzylpenicillin is inactive against staphylococcus strains that produce penicillinase (this enzyme destroys the beta-lactam ring of the active substance).

For a long time, penicillin was not used to treat staphylococcal infection, until in 1957 oxacillin was synthesized on its basis. It inhibits the activity of beta-lactamases of the pathogen, but is ineffective against diseases caused by strains sensitive to benzylpenicillin. This group also includes cloxacillin, dicloxacillin, methicillin and others that are almost never used in modern medical practice due to increased toxicity.

This includes two subgroups of antimicrobial agents intended for oral use and having a bactericidal effect against most pathogenic microorganisms (both gram + and gram-).

Compared to the previous groups, these compounds have two significant advantages. Firstly, they are active against a wider range of pathogens, and secondly, they are available in tablet form, which greatly facilitates the use. The disadvantages include sensitivity to beta-lactamase, that is, aminopenicillins (ampicillin and amoxicillin) are unsuitable for the treatment of staphylococcal infections.

However, in combination with oxacillin (Ampiox), they become resistant.

The drugs are well absorbed and act for a long time, which reduces the frequency of use to 2-3 times in 24 hours. The main indications for use are meningitis, sinusitis, otitis media, infectious diseases of the urinary and upper respiratory tract, enterocolitis and eradication of Helicobacter (the causative agent of stomach ulcers). A common side effect of aminopenicillins is the characteristic non-allergic rash that disappears immediately after withdrawal.

Constitute a separate penicillin series antibiotics, from the name of which the purpose becomes clear. Antibacterial activity is similar to aminopenicillins (with the exception of pseudomonas) and is pronounced against Pseudomonas aeruginosa.

According to the degree of efficiency, they are divided into:

  • Carboxypenicillins, the clinical significance of which has recently been decreasing. Carbenicillin, the first of this subgroup, is also effective against ampicillin-resistant proteus. Currently, almost all strains are resistant to carboxypenicillins.
  • Ureidopenicillins are more effective against Pseudomonas aeruginosa, and can also be prescribed for inflammation caused by Klebsiella. The most effective are Piperacillin and Azlocillin, of which only the latter remains relevant in medical practice.

To date, the vast majority of Pseudomonas aeruginosa strains are resistant to carboxypenicillins and ureidopenicillins. For this reason, their clinical significance is diminishing.


The ampicillin group of antibiotics, highly active against most pathogens, is destroyed by penicillinase-forming bacteria. Since the bactericidal effect of oxacillin resistant to them is significantly weaker than that of ampicillin and amoxicillin, combined medications were synthesized.

In combination with sulbactam, clavulanate and tazobactam, antibiotics obtain a second beta-lactam ring and, accordingly, immunity to beta-lactamases. In addition, inhibitors have their own antibacterial effect, enhancing the main active ingredient.

Inhibitor-protected drugs successfully treat severe nosocomial infections, strains of which are resistant to most drugs.

Read also: About modern classification antibiotics by parameter group

The broad spectrum of action and good patient tolerance made penicillin the optimal treatment for infectious diseases. At the dawn of the era of antimicrobial drugs, benzylpenicillin and its salts were the drugs of choice, but at the moment most pathogens are resistant to them. However, modern semi-synthetic penicillin antibiotics in tablets, injections and others dosage forms occupy one of the leading places in antibiotic therapy in various fields of medicine.

The discoverer also noted the special effectiveness of penicillin against pathogens of respiratory diseases, therefore, the drug is most widely used in this area. Almost all of them are harmful to bacteria that cause sinusitis, meningitis, bronchitis, pneumonia and other diseases of the lower and upper respiratory tract.

Inhibitor-protected agents treat even especially dangerous and persistent nosocomial infections.

Spirochetes are one of the few microorganisms that remain susceptible to benzylpenicillin and its derivatives. Benzylpenicillins are also effective against gonococci, which makes it possible to successfully treat syphilis and gonorrhea with minimal negative impact on the patient's body.

Intestinal inflammation caused by pathogenic microflora lends itself well to therapy with acid-resistant drugs.

Of particular importance are aminopenicillins, which are part of the complex eradication of Helicobacter.

In obstetric and gynecological practice, many penicillin preparations from the list are used both for the treatment of bacterial infections of the female reproductive system and for the prevention of infection in newborns.

Here, penicillin antibiotics also take their rightful place: eye drop, ointments and solutions for injections treat keratitis, abscesses, gonococcal conjunctivitis and other eye diseases.

Diseases of the urinary system, which are of bacterial origin, respond well to therapy only with inhibitor-protected drugs. The rest of the subgroups are ineffective, since the pathogen strains are highly resistant to them.

Penicillins are used in almost all areas of medicine for inflammation caused by pathogenic microorganisms, and not only for treatment. For example, in surgical practice, they are prescribed to prevent postoperative complications.

Treatment with antibacterial medications in general and penicillins in particular should be carried out only as directed by a doctor. Despite the minimal toxicity of the drug itself, its misuse seriously harms the body. In order for antibiotic therapy to lead to recovery, one should follow medical recommendations and know the characteristics of the drug.

The scope of application of penicillin and various drugs based on it in medicine is due to the activity of the substance against specific pathogens. Bacteriostatic and bactericidal effects are manifested in relation to:

  • Gram-positive bacteria - gonococci and meningococci;
  • Gram-negative - various staphylococci, streptococci and pneumococci, diphtheria, Pseudomonas aeruginosa and antiseptic bacilli, Proteus;
  • Actinomycetes and spirochetes.

Low toxicity and broad spectrum of action make antibiotics of the penicillin group the optimal treatment for angina, pneumonia (both focal and croupous), scarlet fever, diphtheria, meningitis, blood poisoning, septicemia, pleurisy, pyemia, osteomyelitis in acute and chronic forms, septic endocarditis, various purulent infections of the skin, mucous membranes and soft tissues, erysipelas, anthrax, gonorrhea, actinomycosis, syphilis, blennorrhea, as well as eye diseases and ENT diseases.

Strict contraindications include only individual intolerance to benzylpenicillin and other drugs in this group. Also, endolumbar (injection into the spinal cord) administration of drugs to patients with diagnosed epilepsy is not allowed.

During pregnancy, antibiotic therapy with penicillin drugs should be treated with extreme caution. Despite the fact that they have a minimal teratogenic effect, it is worth prescribing pills and injections only in case of urgent need, assessing the degree of risk to the fetus and the pregnant woman herself.

Since penicillin and its derivatives freely penetrate from the bloodstream into breast milk, it is advisable to refuse breastfeeding during therapy. The medicine can provoke a severe allergic reaction in a baby even at the first use. To prevent lactation from stopping, milk must be expressed regularly.

Among other antibacterial agents, penicillins stand out favorably with low toxicity.

TO undesirable consequences uses include:

  • Allergic reactions. Most often they are manifested by skin rash, itching, hives, fever and swelling. It is extremely rare in severe cases that anaphylactic shock is possible, requiring the immediate administration of an antidote (adrenaline).
  • Dysbacteriosis. Disruption of the balance of natural microflora leads to digestive disorders (flatulence, bloating, constipation, diarrhea, abdominal pain) and the development of candidiasis. In the latter case, the mucous membranes are affected. oral cavity(in children) or vagina.
  • Neurotoxic reactions. The negative effect of penicillin on the central nervous system manifested by increased reflex excitability, nausea and vomiting, convulsions, and sometimes coma.

Timely drug support for the body will help prevent the development of dysbiosis and avoid allergies. It is advisable to combine antibiotic therapy with the intake of pre- and probiotics, as well as desensitizers (if sensitivity is increased).

Children should be prescribed pills and injections with caution, taking into account the possible negative reaction, and carefully approach the choice of a particular drug.

In the first years of life, benzylpenicillin is used in cases of sepsis, pneumonia, meningitis, otitis media. For treatment respiratory infections, sore throats, bronchitis and sinusitis, the safest antibiotics from the list are selected: Amoxicillin, Augmentin, Amoxiclav.

A child's body is much more sensitive to drugs than an adult's. Therefore, you should carefully monitor the condition of the baby (penicillin is excreted slowly and, accumulating, can cause convulsions), and also take preventive measures... The latter include the use of pre- and probiotics to protect the intestinal microflora, diet and comprehensive strengthening of the immune system.

A bit of theory:

The discovery that made a real revolution in medicine at the beginning of the 20th century was made by accident. I must say that the antibacterial properties of molds were noticed by people in ancient times.

Alexander Fleming - the discoverer of penicillin

The Egyptians, for example, even 2500 years ago treated inflamed wounds with compresses from moldy bread, but scientists only took up the theoretical side of the issue in the 19th century. European and Russian researchers and doctors, studying antibiosis (the property of some microorganisms to destroy others), attempted to extract practical benefits from it.

It was succeeded by Alexander Fleming, a British microbiologist, who in 1928, on September 28, discovered mold in Petri dishes with colonies of staphylococcus aureus. Her spores, caught on crops through the negligence of the laboratory staff, germinated and destroyed the pathogenic bacteria. The concerned Fleming carefully studied this phenomenon and isolated a bactericidal substance called penicillin. For many years, the discoverer worked on obtaining a chemically pure stable compound suitable for treating people, but others invented it.

In 1941, Ernst Cheyne and Howard Florey were able to purify penicillin from impurities and conducted clinical trials with Fleming. The results were so successful that by the year 43, the United States had organized mass production of the drug, which had saved many hundreds of thousands of lives during the war. The merits of Fleming, Cheyne and Flory to humanity were appreciated in 1945: the discoverer and developers became Nobel Prize winners.

Subsequently, the original chemical product was constantly improved. This is how modern penicillins appeared, resistant to the acidic environment of the stomach, immune to penicillinase and more effective in general.

Read the fascinating article: The Inventor of Antibiotics or the Story of Human Rescue!

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Mushrooms are the kingdom of living organisms. Mushrooms are different: some of them get into our diet, some cause skin diseases, some are so poisonous that they can lead to death. But fungi of the genus Penicillium save millions of human lives from pathogenic bacteria.

Penicillin antibiotics based on this mold (mold is also a fungus) are still used in medicine.

In the 30s of the last century, Alexander Fleming conducted experiments with staphylococci. He studied bacterial infections. Having grown a group of these pathogens in a nutrient medium, the scientist noticed that there are areas in the dish around which there are no living bacteria. An investigation has shown that common green mold, which loves to settle on stale bread, is to blame for these stains. The mold was called Penicillium and, as it turned out, produced a substance that kills staphylococci.

Fleming studied the matter deeper and soon isolated pure penicillin, which became the world's first antibiotic... The principle of action of the drug is as follows: when a bacterial cell divides, each half restores its cell membrane with the help of a special chemical element, peptidoglycan. Penicillin blocks the formation of this element, and the bacterial cell is simply "absorbed" in the environment.

But difficulties soon arose. Bacterial cells have learned to resist the drug - they began to produce an enzyme called beta-lactamase, which breaks down beta-lactams (the basis of penicillin).

For the next 10 years, there was an invisible war between the pathogens that destroy penicillin and the scientists who modify this penicillin. So many modifications of penicillin were born, which now form the entire penicillin range of antibiotics.

The drug for any kind of application quickly spreads throughout the body, penetrating almost all of its parts. Exceptions: cerebrospinal fluid, prostate and the visual system. In these places, the concentration is very low, under normal conditions it does not exceed 1 percent. With inflammation, an increase of up to 5% is possible.

Antibiotics do not affect the cells of the human body, since the latter do not contain peptidoglycan.

The drug is quickly excreted from the body, after 1-3 hours most of it is excreted through the kidneys.

Watch a video on this topic

All drugs are divided into: natural (short and prolonged action) and semi-synthetic (antistaphylococcal, broad-spectrum drugs, antipseudomonal).

These drugs obtained directly from mold... At the moment, most of them are outdated, since pathogens have acquired immunity to them. In medicine, benzylpenicillin and Bicillin are most often used, which are effective against gram-positive bacteria and cocci, some anaerobic and spirochetes. All these antibiotics are used only in the form of injections into the muscles, since the acidic environment of the stomach quickly destroys them.

Benzylpenicillin in the form of sodium and potassium salts belongs to natural antibiotics short acting... Its effect wears off after 3-4 hours, so repeated injections must be done frequently.

Trying to eliminate this deficiency, pharmacists have created natural antibiotics of prolonged action: Bicillin and novocaine salt of benzylpenicillin. These drugs are called "depot forms", because after being injected into the muscle, they form a "depot" in it, from which the drug is slowly absorbed into the body.

Examples of drugs: benzylpenicillin salt (sodium, potassium or novocainic), Bitsillin-1, Bitsillin-3, Bitsillin-5.

Several decades after receiving penicillin pharmacists were able to isolate its main active ingredient, and the modification process began... After improvement, most drugs acquired resistance to the acidic environment of the stomach, and semi-synthetic penicillins began to be produced in tablets.

Isoxazolepenicillins are medicines that are effective against staphylococci. The latter have learned to produce an enzyme that destroys benzylpenicillin, and drugs from this group interfere with the production of the enzyme. But you have to pay for the improvement - drugs of this type are less absorbed into the body and have a smaller spectrum of action compared to natural penicillins. Examples of drugs: Oxacillin, Nafcillin.

Aminopenicillins are broad-spectrum drugs. They are inferior to benzylpenicillins in strength in the fight against gram-positive bacteria, but they capture a wider range of infections. Compared to other drugs, they stay in the body longer and better penetrate some of the body's barriers. Examples of drugs: Ampicillin, Amoxicillin. You can often find Ampiox - Ampicillin + Oxacillin.

Carboxypenicillins and ureidopenicillins - antibiotics effective against Pseudomonas aeruginosa... At the moment, they are practically not used, since infections quickly become resistant to them. Occasionally you can find them as part of a comprehensive treatment.

Examples of drugs: Ticarcillin, Piperacillin

Pills

Sumamed

Active substance: azithromycin.

Indications: respiratory tract infections.

Contraindications: intolerance, severe renal failure, childhood up to 6 months.

Price: 300-500 rubles.

Oxacillin

Active ingredient: oxacillin.

Indications: drug-sensitive infections.

Price: 30-60 rubles.

Amoxicillin Sandoz

Indications: respiratory tract infections (including tonsillitis, bronchitis), infections of the genitourinary system, skin infections, and other infections.

Contraindications: intolerance, children under 3 years of age.

Price: 150 rubles.

Ampicillin trihydrate

Indications: pneumonia, bronchitis, tonsillitis, other infections.

Contraindications: hypersensitivity, liver failure.

Price: 24 rubles.

Phenoxymethylpenicillin

Active ingredient: phenoxymethylpenicillin.

Indications: streptococcal diseases, infections of mild to moderate severity.

Price: 7 rubles.

Amoxiclav

Active ingredient: amoxicillin + clavulanic acid.

Indications: infections of the respiratory tract, urinary system, infections in gynecology, other infections sensitive to amoxicillin.

Contraindications: hypersensitivity, jaundice, mononucleosis and lymphocytic leukemia.

Price: 116 rubles.

Bitsillin-1

Active ingredient: benzathine benzylpenicillin.

Indications: acute tonsillitis, scarlet fever, wound infections, erysipelas, syphilis, leishmaniasis.

Contraindications: hypersensitivity.

Price: 15 rubles per injection.

Ospamox

Active ingredient: amoxicillin.

Indications: infections of the lower and upper respiratory tract, gastrointestinal tract, genitourinary system, gynecological and surgical infections.

Contraindications: hypersensitivity, severe gastrointestinal infections, lymphocytic leukemia, mononucleosis.

Price: 65 rubles.

Ampicillin

Active ingredient: ampicillin.

Indications: infections of the respiratory and urinary tract, gastrointestinal tract, meningitis, endocarditis, sepsis, whooping cough.

Contraindications: hypersensitivity, renal dysfunction, childhood, pregnancy.

Price: 163 rubles.

Benzylpenicillin

Indications: severe infections, congenital syphilis, abscesses, pneumonia, erysipelas, anthrax, tetanus.

Contraindications: intolerance.

Price: 2.8 rubles per injection.

Benzylpenicillin novocaine salt

Active ingredient: benzylpenicillin.

Indications: similar to benzylpenicillin.

Contraindications: intolerance.

Price: 43 rubles for 10 injections.

Amoxiclav, Ospamox, Oxacillin are suitable for the treatment of children. But before using the medicine, you must definitely consult with your doctor to adjust the dose.

Antibiotics of the penicillin group are prescribed for infections, the type of antibiotics is selected based on the type of infection. These can be various cocci, sticks, anaerobic bacteria, and so on.

Most often, antibiotics are used to treat infections of the respiratory tract and genitourinary system.

In the case of treating children, you need to follow the instructions of the doctor, who will prescribe the desired antibiotic and adjust the dose.

In case of pregnancy, antibiotics must be used with extreme caution, as they penetrate the fetus. During lactation, it is better to switch to mixtures, since the medicine also penetrates into the milk.

There are no special instructions for the elderly, although the doctor should take into account the condition of the patient's kidneys and liver when prescribing treatment.

The main and, often, the only contraindication is individual intolerance. It occurs frequently - in about 10% of patients. Additional contraindications depend on the specific antibiotic and are prescribed in the instructions for use.

In the event of side effects, you must immediately apply for medical help, cancel the drug and carry out symptomatic treatment.

Where does penicillin mold grow?

Almost everywhere. This mold includes dozens of subspecies, and each of them has its own habitat. The most notable representatives are penicillin mold, which grows on bread (it also infects apples, causing them to rot quickly) and mold used in the production of some cheeses.

How to replace penicillin antibiotics?

If the patient is allergic to penicillin, non-penicillin antibiotics can be used. Drug names: Cefadroxil, Cephalexin, Azithromycin. The most popular option is Erythromycin. But you need to know that Erythromycin often causes dysbiosis and indigestion.

Penicillin antibiotics are powerful against infections caused by various bacteria. There are quite a few types of them, and the treatment must be selected in accordance with the type of pathogen.

They seem harmless to the body due to the fact that the only contraindication is a hypersensitivity reaction, but improper treatment or self-medication can provoke resistance of the pathogen to an antibiotic, and another treatment, more dangerous and less effective, will have to be selected.

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Antibiotics owe their origin to the Scottish scientist Alexander Fleming. More precisely, his slovenliness. In September 1928, he returned to his laboratory from a long trip. During this time, an area with mold has grown in a Petri dish forgotten on the table, and a ring of dead microbes has formed around it. It was this phenomenon that the microbiologist noticed and began to investigate.

The mold in the test tube contained a substance that Fleming called penicillin. However, as many as 13 years passed before penicillin was obtained in its pure form, and its action was first tested on humans. The mass production of new drugs began in 1943, at a factory where whiskey was previously brewed.

Today there are about several thousand natural and synthetic substances with antimicrobial effect. However, the most popular of them are still drugs of the penicillin series.

Any pathogenic microorganism entering the blood or tissue begins to divide and grow. The effectiveness of penicillins is based on their ability to disrupt the formation of bacterial cell walls.

Antibiotics of the penicillin group block special enzymes that are responsible for the synthesis of a protective, peptidoglycan layer in the bacterial membrane. It is thanks to this layer that they remain insensitive to aggressive environmental influences.

The result of the impaired synthesis is the inability of the membrane to withstand the difference between external pressure and pressure inside the cell itself, due to which the microorganism swells and simply bursts.

Penicillins are antibiotics with a bacteriostatic effect, that is, they affect only active microorganisms that are in the stage of division and the formation of new cell membranes.

According to the chemical classification, antibiotics of the penicillin series are β-lactam antibiotics. In their structure, they contain a special beta-lactam ring, which determines their main action. To date, the list of such drugs is quite large.

The first, natural penicillin, despite all its effectiveness, had one significant drawback. He was not resistant to the enzyme penicillinase, which was produced by almost all microorganisms. Therefore, scientists have created semi-synthetic and synthetic analogs. Today, antibiotics of the penicillin group include three main types.

As many years ago, they are obtained using the molds Penicillium notatum and Penicillium chrysogenum. The main representatives of this group today are benzylpenicillin sodium or potassium salt, as well as their analogs Bicillins -1, 3 and 5, which are novocaine salt of penicillin. These drugs are not resistant to the aggressive environment of the stomach and therefore are used only in the form of injections.

Benzylpenicillins are characterized by a rapid onset of the therapeutic effect, which develops literally in 10-15 minutes. However, its duration is quite short, only 4 hours. Bitsillin can boast of greater stability, due to its connection with novocaine, its action lasts for 8 hours.

Another representative on the list of this group, phenoxymethylpenicillin, is resistant to an acidic environment, therefore it is available in tablets and suspensions that can be used by children. However, it also does not differ in the duration of action and can be prescribed from 4 to 6 times a day.

Natural penicillins are used very rarely today due to the fact that most pathological microorganisms have developed resistance to them.

This penicillin group of antibiotics was obtained using various chemical reactions, attaching additional radicals to the main molecule. The slightly altered chemical structure has endowed these substances with new properties, such as resistance to penicillinase and a broader spectrum of action.

Semi-synthetic penicillins include:

  • Antistaphylococcal drugs, such as Oxacillin obtained in 1957 and still used today, and cloxacillin, flucloxacillin, and dicloxacillin, which are not used due to their high toxicity.
  • Antipseudomonal, special group penicillins, which was created to fight infections caused by Pseudomonas aeruginosa. These include Carbenicillin, Piperacillin, and Azlocillin. Unfortunately, today these antibiotics are used very rarely, and due to the resistance of microorganisms that has arisen to them with new drugs, their list is not replenished.
  • Penicillin range of broad-spectrum antibiotics. This group acts on many microorganisms and at the same time is resistant to an acidic environment, which means that it is produced not only in injection solutions, but also in tablets and suspensions for children. This includes the most commonly used aminopenicillins, such as Ampicillin, Ampiox, and Amoxicillin. The drugs have long-term action and are usually applied 2-3 times a day.

Of the entire group of semi-synthetic drugs, it is penicillin antibiotics of a wide spectrum of action that are the most popular and are used both in inpatient and outpatient treatment.

Once upon a time, injections of penicillin could cure blood poisoning. Today, most antibiotics are ineffective even for simple infections. The reason for this is resistance, that is, resistance to drugs that microorganisms have acquired. One of its mechanisms is the destruction of antibiotics by the enzyme beta-lactamase.

In order to avoid this, scientists have created a combination of penicillins with special substances - beta-lactamase inhibitors, namely with clavulanic acid, sulbactam or tazobactam. Such antibiotics were called protected and today the list of this group is the most extensive.

In addition to the fact that inhibitors protect penicillins from the destructive action of beta-lactamases, they also have their own antimicrobial action. The most common of this group of antibiotics is Amoxiclav, which is a combination of amoxicillin and clavulanic acid, and Ampisid, a combination of ampicillin and sulbactam. Doctors and their analogues are prescribed - drugs Augmentin or Flemoklav. Protected antibiotics are used to treat children and adults, and they are also the drugs of first choice in the treatment of infections during pregnancy.

Antibiotics protected by beta-lactamase inhibitors are successfully used even for treatment severe infections resistant to most other drugs.

Statistics claim that antibiotics are in second place after pain relievers in terms of the prevalence of use. According to the analytical company DSM Group, 55.46 million packs were sold in one quarter of 2016 alone. Today pharmacies sell about 370 different brands of drugs, which are produced by 240 companies.

The entire list of antibiotics, including those of the penicillin series, refers to drugs of strict dispensing. Therefore, you need a doctor's prescription to purchase them.

An indication for the use of penicillins can be any infectious diseases that are sensitive to them. Usually doctors prescribe penicillin antibiotics:

  1. For diseases caused by gram-positive bacteria, such as meningococci, which can cause meningitis, and gonococci, which trigger the development of gonorrhea.
  2. With pathologies that are provoked by gram-negative bacteria, such as pneumococci, staphylococci or streptococci, which are often the causes of infections of the upper and lower respiratory tract, genitourinary system and many others.
  3. For infections caused by actinomycetes and spirochetes.

The low toxicity that the penicillin group has in comparison with other antibiotics makes them the most prescribed drugs for the treatment of tonsillitis, pneumonia, various infections of the skin and bone tissue, diseases of the eyes and ENT organs.

This group of antibiotics is relatively safe. In some cases, when the benefits of their use outweigh the risk, they are prescribed even during pregnancy. Especially when non-penicillin antibiotics are ineffective.

They are also used during lactation. However, doctors still advise to stop breastfeeding while taking antibiotics, since they can penetrate into milk and can cause allergies in the baby.

The only absolute contraindication to use penicillin drugs is an individual intolerance to both the main substance and auxiliary components. For example, benzylpenicillin novocaine salt is contraindicated for allergies to novocaine.

Antibiotics are quite aggressive drugs. Even though they have no effect on the cells of the human body, there can be unpleasant effects from their use.

Most often these are:

  1. Allergic reactions, manifested mainly in the form of itching, redness and rashes. Less often, edema may occur, the temperature rises. In some cases, anaphylactic shock may develop.
  2. Disruption of the balance of natural microflora, which provokes disorders, abdominal pain, bloating and nausea. In rare cases, candidiasis may develop.
  3. A negative effect on the nervous system, the signs of which are irritability, excitability, convulsions can rarely occur.

To date, of the entire variety of open antibiotics, only 5% are used. The reason for this lies in the development of resistance in microorganisms, which often arises from improper use of drugs. Antibiotic resistance is already killing 700,000 people every year.

In order for the antibiotic to be as effective as possible and not cause the development of resistance in the future, it must be drunk in the dosage prescribed by the doctor and always the full course!

If your doctor has prescribed penicillins or any other antibiotics for you, be sure to follow these rules:

  • Strictly observe the time and frequency of taking the drug. Try to drink the medicine at the same time, so you will ensure a constant concentration of the active substance in the blood.
  • If the dosage of penicillin is small and the drug needs to be drunk three times a day, then the time between doses should be 8 hours. If the dose prescribed by the doctor is calculated to be taken twice a day - up to 12 hours.
  • The course of taking the drug can range from 5 to 14 days and is determined by your diagnosis. Always completely drink the entire course prescribed by your doctor, even if the symptoms of the disease no longer bother you.
  • If you do not feel any improvement within 72 hours, be sure to tell your doctor about it. Perhaps the drug he chose was not effective enough.
  • Do not substitute one antibiotic for another yourself. Do not change dosage or dosage form. If the doctor has prescribed injections, then the pills in your case will not be effective enough.
  • Be sure to follow the instructions for admission. There are antibiotics that you need to drink with meals, there are those that you drink immediately after. Drink the drug only with plain, non-carbonated water.
  • For the duration of antibiotic treatment, give up alcohol, fatty, smoked and fried foods. Antibiotics are mainly excreted by the liver, so you should not additionally load it during this period.

If antibiotics-penicillins are prescribed to a child, then you should be especially careful about taking them. A child's body is much more sensitive to these drugs than an adult, so babies may experience allergies more often. Penicillins for children are produced, as a rule, in a special dosage form, in the form of suspensions, so you should not give the child pills. Drink antibiotics correctly and only as directed by your doctor when needed.

Penicillin antibiotics are several types of drugs that are divided into groups. In medicine, drugs are used to treat various diseases infectious and bacterial origin. The drugs have a minimal number of contraindications and are still used to treat various patients.

Once Alexander Fleming in his laboratory was engaged in the study of pathogens. He created a nutrient medium and grew staphylococcus. The scientist was not very clean, he simply put the beakers and cones in the sink and forgot to wash them.

When Fleming needed the dishes again, he found that they were covered with mold. The scientist decided to test the guess and examined one of the containers under a microscope. He noticed that where there is mold, there is no staphylococcus.

Alexander Fleming continued his research, he began to study the effect of mold on pathogenic microorganisms and found that the fungus destructively affects the membranes of bacteria and leads to their death. The public could not be skeptical about the research.

The discovery helped save many lives. Delivered humanity from those diseases that previously caused panic among the population. Naturally, modern medicines have a relative similarity with those drugs that were used at the end of the 19th century. But the essence of medicines, their effect has not changed so dramatically.

Penicillin antibiotics were able to revolutionize medicine. But the joy of the discovery did not last long. It turned out that pathogens, bacteria can mutate. They mutate and become insensitive to drugs. This has led to significant changes in antibiotics such as penicillin.

Scientists have been fighting against microorganisms and bacteria for almost the entire XX century, trying to create an ideal drug. The efforts were not in vain, but such improvements have led to the fact that antibiotics have changed significantly.

New generation drugs are more expensive, act faster, and have a number of contraindications. If we talk about those preparations that were obtained from mold, then they have a number of disadvantages:

  • Poorly absorbed. Gastric juice acts on the fungus in a special way, reduces its effectiveness, which undoubtedly affects the result of treatment.
  • Penicillin antibiotics are drugs of natural origin, for this reason they do not differ a wide range actions.
  • Medicines are quickly excreted from the body, approximately 3-4 hours after the injection.

Important: These medicines have practically no contraindications. It is not recommended to take them if there is an individual intolerance to antibiotics, as well as in the case of an allergic reaction.

Modern antibacterial agents differ significantly from the familiar to many penicillin. In addition to the fact that today it is easy to purchase medicines of this class in tablets, there are a great many varieties of them. To understand the drugs will help the classification, the generally accepted division into groups.

Antibiotics of the penicillin group are conventionally divided into:

  1. Natural.
  2. Semi-synthetic.

All medicines based on mold are antibiotics of natural origin. Today, such medicines are practically not used in medicine. The reason is that pathogenic microorganisms have acquired immunity to them. That is, the antibiotic does not act on the bacteria in the proper way; the desired result in the treatment can be achieved only with the introduction of a high dose of the drug. The funds in this group include: Benzylpenicillin and Bicillin.

The drugs are available in powder form for injection. They effectively act on: anaerobic microorganisms, gram-positive bacteria, cocci, etc. Since medicines are of natural origin, they cannot boast of a long-term effect, injections are often done every 3-4 hours. This makes it possible not to reduce the concentration of the antibacterial agent in the blood.

Penicillin antibiotics of semi-synthetic origin are the result of a modification of drugs made from mold. Medicines belonging to this group managed to give some properties, first of all, they became insensitive to acid-base environment. That made it possible to produce antibiotics in tablets.

And also medicines appeared that affected staphylococci. This class of drugs is different from natural antibiotics. But the improvements have had a significant impact on the quality of the drugs. They are poorly absorbed, do not have such a wide sector of action, and have contraindications.

Semi-synthetic drugs can be divided into:

  • Isoxazolepenicillins are a group of drugs that act on staphylococci, as an example, the names the following drugs: Oxacillin, Nafcillin.
  • Aminopenicillins - Several drugs belong to this group. They are distinguished by a wide sector of action, but in terms of strength they are significantly inferior to antibiotics of natural origin. But they can fight a large number of infections. Funds from this group remain in the blood longer. Such antibiotics are often used to treat various diseases, for example 2 very well-known drugs: Ampicillin and Amoxicillin.

Attention! The list of medicines is quite large, they have a number of indications and contraindications. For this reason, it is worth consulting a doctor before starting antibiotics.

Antibiotics belonging to the penicillin group are prescribed by a doctor. The drugs are recommended to be taken if you have:

  1. Diseases of an infectious or bacterial nature (pneumonia, meningitis, etc.).
  2. Respiratory tract infections.
  3. Diseases of the inflammatory and bacterial nature of the genitourinary system (pyelonephritis).
  4. Diseases of the skin of various origins (erysipelas, caused by staphylococcus).
  5. Intestinal infections and many other diseases of an infectious, bacterial or inflammatory nature.

Reference: Antibiotics are prescribed for extensive burns and deep wounds, gunshot or stab wounds.

In some cases, taking medication can help save a person's life. But you should not prescribe yourself such drugs on your own, as this can lead to the development of addiction.

What are the contraindications for drugs:

  • You should not take medication during pregnancy or lactation. The drugs can affect the growth and development of the child. They are able to change the quality of milk and its taste characteristics. There are a number of drugs that are conditionally approved for the treatment of pregnant women, but the doctor must prescribe such an antibiotic. Since only a doctor will be able to determine the acceptable dosage and duration of the course of treatment.
  • The use of antibiotics from the groups of natural and synthetic penicillins for treatment is not recommended for the treatment of children. Drugs of these classes can have a toxic effect on the child's body. For this reason, medications are prescribed with caution in determining the optimal dosage.
  • You should not use medicines without visible indications. Use drugs for a long period of time.

Direct contraindications for the use of antibiotics:

  1. Individual intolerance to drugs of this class.
  2. Propensity to allergic reactions of various kinds.

Attention! Long-term diarrhea and candidiasis are thought to be the main side effects of medication. They are associated with the fact that drugs have an effect not only on pathogens, but also on beneficial microflora.

The penicillin series of antibiotics is characterized by the presence of a small number of contraindications. For this reason, drugs in this class are prescribed very often. They help to quickly cope with the disease and return to a normal rhythm of life.

Medicines last generation differ in a wide range of actions. Such antibiotics do not have to be taken for a long time, they are well absorbed and, with adequate therapy, they can "put a person on his feet" in 3-5 days.

The question is which antibiotics are best? can be considered rhetorical. There are a number of drugs that doctors, for one reason or another, prescribe more often than others. In most cases, drug names are well known to the general public. But it is still worth studying the list of medicines:

  1. Sumamed is a drug used to treat infectious diseases of the upper respiratory tract. The active ingredient is erythromycin. The medication is not used to treat patients with acute or chronic renal failure, is not prescribed for children under 6 months of age. The main contraindication to the use of Sumamed should be considered individual antibiotic intolerance.
  2. Oxacillin - Available in powder form. The powder is diluted, and then the solution is used for intramuscular injections. The main indication for the use of the drug should be considered infections that are sensitive to this drug. Hypersensitivity should be considered a contraindication to the use of Oxacillin.
  3. Amoxicillin belongs to a number of synthetic antibiotics. The drug is quite famous, it is prescribed for angina, bronchitis and other respiratory tract infections. Amoxicillin can be taken for pyelonephritis (inflammation of the kidneys) and other diseases of the genitourinary system. The antibiotic is not prescribed for children under 3 years of age. Drug intolerance is also considered a direct contraindication.
  4. Ampicillin - the full name of the drug: Ampicillin trihydrate. An indication for the use of the drug should be considered infectious diseases of the respiratory tract (tonsillitis, bronchitis, pneumonia). The antibiotic is excreted from the body by the kidneys and liver, for this reason, Ampicillin is not prescribed for people with acute liver failure. Can be used to treat children.
  5. Amoxiclav is a drug that has a combined composition. It belongs to the latest generation of antibiotics. Amoxiclav is used to treat infectious diseases of the respiratory system, genitourinary system. It is also used in gynecology. A contraindication to the use of a medication should be considered hypersensitivity, jaundice, mononucleosis, etc.

List or list of penicillin antibiotics, which are available in powder form:

  1. Benzylpenicillin novocaine salt is an antibiotic of natural origin. Indications for the use of the drug can be considered serious infectious diseases, including congenital syphilis, abscesses different etiology, tetanus, anthrax and pneumonia. The drug has practically no contraindications, but in modern medicine it is used extremely rarely.
  2. Ampicillin - used to treat the following infectious diseases: sepsis (blood poisoning), whooping cough, endocarditis, meningitis, pneumonia, bronchitis. Ampicillin is not used to treat children, people with severe renal failure. Pregnancy can also be considered a direct contraindication to the use of this antibiotic.
  3. Ospamox is prescribed for the treatment of diseases of the genitourinary system, infections of a gynecological and other nature. It is prescribed in the postoperative period if there is a high risk of developing inflammatory process... An antibiotic is not prescribed for severe infectious diseases of the gastrointestinal tract, in the presence of an individual intolerance to the drug.

Important: A drug called an antibiotic must have an antibacterial effect on the body. All those medicines that affect viruses have nothing to do with antibiotics.

Sumamed - the cost varies from 300 to 500 rubles.

Amoxicillin tablets - the price is about 159 rubles. per packing.

Ampicillin trihydrate - the cost of tablets is 20-30 rubles.

Ampicillin in powder form for injection - 170 rubles

Oxacillin - the average price for the drug varies from 40 to 60 rubles.

Amoxiclav - the cost is 120 rubles.

Ospamox - the price varies from 65 to 100 rubles.

Benzylpenicillin novocaine salt - 50 rubles

Benzylpenicillin - 30 rubles


Antimicrobial drugs of the penicillin series are characterized by low toxicity, as well as a wide range of effects. They have an antibacterial effect on a large number of both gram-positive and gram-negative bacteria.

The influence of the penicillin series is determined by their ability to provoke the death of pathogenic microflora. Penicillin antibiotics have a bactericidal effect, coming into contact with bacterial enzymes, disrupting the synthesis of the bacterial wall.

The target for such antimicrobial agents is the multiplying bacterial cells. For humans, these drugs are safe, since the membranes of human cells do not have bacterial peptidoglycan.

Classification

There are two main groups of penicillins:

  • natural;
  • semi-synthetic.

A number of the penicillin series, which are obtained from the Penicillus micro-fungus, are not resistant to bacterial enzymes that have the ability to break down beta-lactam substances. Because of this, the spectrum of action of the natural penicillin series is reduced in comparison with the group of semisynthetic agents. What are the names of antibiotics for the penicillin series?

The spectrum of action of penicillins

Natural antimicrobial agents of this group show increased activity against the following bacteria:

  1. Staphylococcus.
  2. Streptococci.
  3. Pneumococcus.
  4. Listeria.
  5. Bacillus.
  6. Meningococcus.
  7. Gonococcus.
  8. Ducrea-Unna's wand.
  9. Clostridium.
  10. Fusobacteria.
  11. Actinomycetes.
  12. Leptospira.
  13. Borrelia.
  14. Pale spirochete.

The spectrum of influence of semi-synthetic penicillin antibiotics is somewhat wider than that of natural ones.

Antimicrobial drugs from this list are classified according to the spectrum of effects, as:

  • not active to Pseudomonas aeruginosa;
  • antipseudomonal medicines.

When are penicillins prescribed?

Antimicrobial agents of this group are used to eliminate:

  1. Pneumonia (acute pneumonia, usually of an infectious origin, which affects all elements of the structure of the organ).
  2. Bronchitis (damage to the respiratory system, in which the bronchi are involved in the inflammatory process).
  3. Otitis media (inflammation in different parts of the ear).
  4. Angina (an infectious and allergic process that affects the pharyngeal lymphoid ring).
  5. Tonsillopharyngitis (acute infection of the pharynx and palatine tonsils).
  6. Scarlet fever (an acute illness characterized by intoxication of the body, rashes all over the body, as well as fever and redness of the tongue).
  7. Cystitis (defeat Bladder).
  8. Pyelonephritis (nonspecific inflammation with damage to the tubular system of the kidney).
  9. Gonorrhea (a sexually transmitted disease that causes damage to the mucous membranes of organs).
  10. Syphilis (chronic damage to the skin, as well as mucous membranes, internal organs).
  11. Skin infections.
  12. Osteomyelitis (an infectious disease in which not only the bone and Bone marrow, but the whole body).
  13. Blenorrhea of ​​newborns (a disease characterized by purulent conjunctivitis, hyperemia of the eyelids and suppuration from them).
  14. Bacterial lesions of the mucous membranes, connective tissue.
  15. Leptospirosis (an acute infectious disease caused by bacteria of the genus Leptospira).
  16. Actinomycosis (a chronic disease from the group of mycoses, which is characterized by the formation of granulomatous foci).
  17. Meningitis (a disease that is caused by damage to the lining of the brain and spinal cord).

Aminopenicillins

Antibacterial agents from the list of aminopenicillins show increased effectiveness against a large number of infections that are provoked by enterobacteriaceae bacteria, as well as Helicobacter pylori and Haemophilus influenzae. Names of penicillin antibiotics, list of drugs:

  1. "Ampicillin".
  2. "Amoxicillin".
  3. "Flemoxin Solutab".
  4. Ospamox.
  5. "Amosin".
  6. Ecobol.

The action of antibacterial drugs from the list of ampicillins and amoxicillins, the effects of these medicines are similar.

Antimicrobial agents of the ampicillin series have a much less effect on pneumococci, but the activity of "Ampicillin" and its generics with the following names of drugs - antibiotics of the penicillin series "Ampicillin Akos", "Ampicillin trihydrate" is somewhat stronger in eliminating shigella.

The amoxicillin series is more effective against Pseudomonas aeruginosa, but some members of the group are eliminated by bacterial penicillinases.

List of names of penicillin antibiotics

The most effective drugs in the fight against ailments:

  1. Oxacillin.
  2. Dicloxacillin.
  3. "Nafcillin".
  4. "Methicillin".

The drugs show resistance to staphylococcal penicillinases, which eliminate other drugs in this series. The most popular is "Oxacillin".

Antipseudomonal penicillins

The preparations of this drug group have a broad spectrum of action, they are effective against Pseudomonas aeruginosa, which provokes cystitis, as well as tonsillitis and skin infections. What are the names of the drugs?

Penicillin antibiotics (names):

  1. "Carbetsin".
  2. "Piopen".
  3. "Tymentin".
  4. "Securopen".
  5. "Pitsillin".

Combined drugs

Inhibitor-protected penicillins include medicines that contain an antibiotic and a component that blocks the activity of bacterial beta-lactamases.

The inhibitors are:

  • clavulanic acid;
  • tazobactam;
  • sulbactam.

To eliminate respiratory as well genitourinary infections as a rule, the following names of penicillin antibiotics are used:

  1. Augmentin.
  2. "Amoxiclav".
  3. "Amoxil".
  4. "Unazine".

The drugs of combined effect include the antimicrobial drug Ampiox and its generic Ampiox sodium, which contains Ampicillin and Oxacillin.

"Ampiox" is produced in tablet form and in the form of powder for injections. The drug is used in the treatment of children and adult patients from sepsis, as well as septic endocarditis.

Medicines for adults

In the list of semi-synthetic drugs that are good for tonsillitis, as well as otitis media, pharyngitis, sinusitis and pneumonia, diseases of the genitourinary system, tablets and injections:

  1. "Hikontsil".
  2. Ospamox.
  3. "Amoxiclav".
  4. "Amoxicar".
  5. "Ampicillin".
  6. Augmentin.
  7. "Flemoxin Solutab".
  8. "Amoxiclav".
  9. "Piperacillin".
  10. "Ticarcillin".

Against prostatitis, such antimicrobial agents are not used, since they do not enter the prostate tissue. In case of allergic manifestations to penicillins, the patient may develop a nettle rash, anaphylaxis, and during therapy with cephalosporins.

"Ampicillin"

The drug inhibits the connection of bacterial cell walls, which is due to its antimicrobial effect. The drug affects coccal microorganisms and a large number of gram-negative bacteria. Under the influence of penicillinase "Ampicillin" is destroyed, therefore it is not effective against penicillinase-forming pathogens.

"Flemoxin Solutab"

People who are prone to drug allergies should have a sensitivity test before therapy. The medication is not prescribed for patients who have already had intense adverse reactions to penicillin.

Treatment must be completed. Interruption of therapy ahead of time can lead to the development of resistance of pathogens to the active substance and the transition of the disease to chronic stage.

"Amoxiclav"

The drug also includes amoxicillin, which is considered an antibiotic for penicillin, its molecule contains a beta-lactam ring. It is active against many bacteria, and also has a bactericidal effect by disrupting the synthesis of the cell wall. "Amoxiclav" is a new antibiotic of the penicillin series.

To preserve the activity of the antimicrobial agent in the preparation, clavulanic acid acts as the second active ingredient. This compound irreversibly neutralizes the β-lactamase enzyme, thereby making these pathogens sensitive to amoxicillin.

"Augmentin"

The drug has a prolonged effect, which is significantly different from other drugs based on amoxicillin. With this, the medication can be used to eliminate pneumonia, which is resistant to penicillins.

After getting inside active ingredients- amoxicillin and clavulanic acid - quickly dissolve and are absorbed into the stomach and intestines. The maximum pharmacological effect is manifested in that situation if the patient uses the drug before meals.

Penicillins for the treatment of children

Penicillin antibiotics are practically non-toxic, which is why they are usually recommended for children with infectious diseases. In most cases, preference is given to inhibitor-protected penicillins, which are intended for oral use.

The list of penicillin antimicrobial drugs intended for the treatment of children includes Amoxicillin and generics, Augmentin, Amoxiclav, and Flemoxin and Flemoklav Solutab. Medicines in the form of dispersible tablets are no less effective than injections and provoke less problems during treatment.

From birth, use for the treatment of children "Ospamox" and a number of its substitutes, which are produced in soluble tablets, as well as granules and powder for the manufacture of a suspension. The dosage is prescribed by the doctor, based on the age and body weight of the child.

In children, it is possible for the accumulation of penicillins in the body, which is provoked by anne of the urinary system or kidney damage. Increased content antimicrobial substance in the blood has a toxic effect on nerve cells, which is manifested by spasms. If such signs occur, therapy is stopped, and the penicillin antibiotic is replaced with a medication of another group.

"Ospamox"

The medication is produced in two dosage forms - tablets and granules. The dosage of the drug according to the instructions for use depends on the localization of the infectious process. Ospamox is a modern penicillin antibiotic for children.

Daily concentration is divided into several uses. Duration of therapy: until symptoms are eliminated plus five days. To make a suspension, a bottle with granules is filled with water, then shaken. The dosage of the medication for "Ospamox" will be as follows:

  • infants under one year old are prescribed a suspension at a concentration of 125 mg / 5 ml - 5 milliliters (1 spoon) twice a day;
  • babies from one to six years old - a suspension of 5 to 7.5 milliliters (1-1.5 tablespoons) twice a day;
  • children from six to ten years old - suspension from 7.5 to 10 ml twice a day;
  • patients from ten to fourteen years old are already prescribed a tablet form of the drug - 1 tablet of 500 milligrams twice a day;
  • adolescents - 1.5 tablets of 500 mg twice a day.

Contraindications and side effects

The restrictions for admission include allergy to antibiotics of the penicillin series. If rash occurs during therapy, itchy skin, it is necessary to stop using medications and consult a doctor.

Allergy can be manifested by Quincke's edema, anaphylaxis. The list of adverse reactions in penicillins is small. The main negative phenomenon is the suppression of beneficial intestinal microflora.

Diarrhea, thrush, skin rashes are the main negative reactions when using penicillins. Less commonly, the following effects appear:

  1. Nausea.
  2. Vomit.
  3. Migraine.
  4. Pseudomembranous colitis.
  5. Edema.

The use of benzylpenicillins, as well as carbenicillins, can provoke electrolyte imbalance with the development of hyperkalemia or hypernatremia, which increases the likelihood of a heart attack and an increase in blood pressure.

An extensive list of negative effects of "Oxacillin" and substitutes:

  1. The appearance of blood in the urine.
  2. Temperature.
  3. Vomiting urge.
  4. Nausea.

To prevent the appearance of negative effects, it is important to follow the instructions for use, as well as to use the drug in the dosage prescribed by the doctor.

Opinions

According to reviews, penicillin antibiotics have become a real salvation for many people. Thanks to them, you can cope with most diseases, for example: pneumonia, as well as tuberculosis, sepsis and other ailments.

But the therapy of pathological conditions with the use of antibiotics should be carried out only after the diagnosis is established and strictly according to the doctor's prescription. Of the most effective antimicrobial agents are isolated - "Amoxiclav", "Ampicillin", "Flemoxin Solutab".

In the reviews of medical specialists and people, as a rule, there are positive opinions about the drugs of these groups. It is noted that antimicrobial agents are effective in the treatment of respiratory diseases, and they are suitable for both adults and children. The responses mention the increased effectiveness of funds for sinusitis, otitis media, infections of the genital tract.

Penicillins (penicillina)- a group of antibiotics produced by many types of molds of the genus Penicillium, active against most gram-positive, as well as some gram-negative microorganisms (gonococci, meningococci and spirochetes). Penicillins belong to the so-called. beta-lactam antibiotics (beta-lactams).

Beta-lactams are a large group of antibiotics, which have in common the presence of a four-membered beta-lactam ring in the structure of the molecule. Beta-lactams include penicillins, cephalosporins, carbapenems, monobactams. Beta-lactams are the most numerous group used in clinical practice antimicrobial drugs, which occupies a leading place in the treatment of most infectious diseases.

Historical information. In 1928, the English scientist A. Fleming, who worked at St. Mary's Hospital in London, discovered the ability of the filamentous fungus of green mold (Penicillium notatum) cause the death of staphylococci in cell culture. The active substance of the fungus, which has antibacterial activity, was called penicillin by A. Fleming. In 1940, at Oxford, a group of researchers led by H.V. Flory and E.B. Cheyna isolated significant amounts of the first penicillin from culture Penicillium notatum. In 1942, the outstanding Russian researcher Z.V. Ermolyeva received penicillin from a mushroom Penicillium crustosum. Since 1949, virtually unlimited amounts of benzylpenicillin (penicillin G) have become available for clinical use.

The group of penicillins includes natural compounds produced by various types of mold. Penicillium, and a number of semi-synthetic. Penicillins (like other beta-lactams) have a bactericidal effect on microorganisms.

The most common properties of penicillins include: low toxicity, wide dosage range, cross-allergy between all penicillins and partly cephalosporins and carbapenems.

Antibacterial effect beta-lactams is associated with their specific ability to disrupt the synthesis of the bacterial cell wall.

The cell wall in bacteria has a rigid structure, it gives the microorganisms a shape and protects them from destruction. It is based on a heteropolymer - peptidoglycan, consisting of polysaccharides and polypeptides. Its cross-linked mesh structure lends strength to the cell wall. The composition of polysaccharides includes such amino sugars as N-acetylglucosamine, as well as N-acetylmuramic acid, which is only found in bacteria. Short peptide chains are associated with amino sugars, including some L- and D-amino acids. In gram-positive bacteria, the cell wall contains 50-100 layers of peptidoglycan, in gram-negative bacteria - 1-2 layers.

In the process of biosynthesis of peptidoglycan, about 30 bacterial enzymes are involved, this process consists of 3 stages. It is believed that penicillins disrupt the late stages of cell wall synthesis, preventing the formation of peptide bonds by inhibiting the enzyme transpeptidase. Transpeptidase is one of the penicillin-binding proteins with which beta-lactam antibiotics interact. Penicillin-binding proteins - enzymes that take part in the final stages of the formation of the bacterial cell wall, in addition to transpeptidases, include carboxypeptidases and endopeptidases. All bacteria have them (for example, Staphylococcus aureus there are 4 of them, Escherichia coli- 7). Penicillins bind to these proteins at different rates to form a covalent bond. In this case, the inactivation of penicillin-binding proteins occurs, the strength of the bacterial cell wall is disrupted and the cells undergo lysis.

Pharmacokinetics. When taken orally, penicillins are absorbed and distributed throughout the body. Penicillins penetrate well into tissues and body fluids (synovial, pleural, pericardial, bile), where they quickly reach therapeutic concentrations. The exception is the cerebrospinal fluid, the internal environment of the eye and the secretion of the prostate gland - here the concentration of penicillins is low. The concentration of penicillins in the cerebrospinal fluid can be different depending on the conditions: normally - less than 1% serum, with inflammation it can increase up to 5%. Therapeutic concentrations in the cerebrospinal fluid are created with meningitis and the administration of drugs in high doses. Penicillins are rapidly excreted from the body, mainly by the kidneys, by glomerular filtration and tubular secretion. Their half-life is short (30-90 minutes), the concentration in the urine is high.

There are several classifications Medicines belonging to the group of penicillins: by molecular structure, by source of production, by spectrum of activity, etc.

According to the classification presented by D.A. Kharkevich (2006), penicillins are subdivided as follows (the classification is based on a number of signs, including differences in the routes of production):

I. Preparations of penicillins obtained by biological synthesis (biosynthetic penicillins):

I.1. For parenteral administration (destroyed in the acidic environment of the stomach):

Short-acting:

benzylpenicillin (sodium salt),

benzylpenicillin (potassium salt);

Long-term action:

benzylpenicillin (novocaine salt),

Bitsillin-1,

Bicillin-5.

I.2.

phenoxymethylpenicillin (penicillin V).

II. Semi-synthetic penicillins

II.1. For parenteral and enteral administration (acid-resistant):

Penicillinase-resistant:

oxacillin (sodium salt),

nafcillin;

Broad spectrum of action:

ampicillin,

amoxicillin.

II.2. For parenteral administration (destroyed in the acidic environment of the stomach)

Broad spectrum of action, including Pseudomonas aeruginosa:

carbenicillin (disodium salt),

ticarcillin,

azlocillin.

II.3. For enteral administration (acid-fast):

carbenicillin (indanyl sodium),

carfecillin.

According to the classification of penicillins given by I.B. Mikhailov (2001), penicillins can be divided into 6 groups:

1. Natural penicillins (benzylpenicillins, bicillins, phenoxymethylpenicillin).

2. Isoxazolpenicillins (oxacillin, cloxacillin, flucloxacillin).

3. Amidinopenicillins (amdinocillin, pivamdinocillin, bacamdinocillin, acidocillin).

4. Aminopenicillins (ampicillin, amoxicillin, talampicillin, bacampicillin, pivampicillin).

5. Carboxypenicillins (carbenicillin, carphecillin, carindacillin, ticarcillin).

6. Ureidopenicillins (azlocillin, mezlocillin, piperacillin).

The source of production, the spectrum of action, as well as the combination with beta-lactamases were taken into account when creating the classification given in the Federal Guidelines (Formulary System), issue VIII.

1. Natural:

benzylpenicillin (penicillin G),

phenoxymethylpenicillin (penicillin V),

benzathine benzylpenicillin,

benzylpenicillin procaine,

benzathine phenoxymethylpenicillin.

2. Antistaphylococcal:

oxacillin.

3. Extended spectrum (aminopenicillins):

ampicillin,

amoxicillin.

4. Active in relation Pseudomonas aeruginosa:

Carboxypenicillins:

ticarcillin.

Ureidopenicillins:

azlocillin,

piperacillin.

5. Combined with beta-lactamase inhibitors (inhibitor-protected):

amoxicillin / clavulanate,

ampicillin / sulbactam,

ticarcillin / clavulanate.

Natural (natural) penicillins Are antibiotics of a narrow spectrum of action that affect gram-positive bacteria and cocci. Biosynthetic penicillins are obtained from the culture medium on which certain strains of molds are grown (Penicillium). There are several varieties of natural penicillins, one of the most active and persistent of them is benzylpenicillin. In medical practice, benzylpenicillin is used in the form of various salts - sodium, potassium and novocainic.

All natural penicillins have similar antimicrobial activity. Natural penicillins are destroyed by beta-lactamases, therefore they are ineffective for the treatment of staphylococcal infections, because in most cases, staphylococci produce beta-lactamases. They are effective mainly against gram-positive microorganisms (incl. Streptococcus spp., including Streptococcus pneumoniae, Enterococcus spp.), Bacillus spp., Listeria monocytogenes, Erysipelothrix rhusiopathiae, gram-negative cocci (Neisseria meningitidis, Neisseria gonorrhoeae), some anaerobes (Peptostreptococcus spp., Fusobacterium spp.), spirochete (Treponema spp., Borrelia spp., Leptospira spp.). Gram-negative organisms are usually resistant, with the exception of Haemophilus ducreyi and Pasteurella multocida. In relation to viruses (causative agents of influenza, poliomyelitis, smallpox, etc.), mycobacterium tuberculosis, the causative agent of amebiasis, rickettsia, and fungi, penicillins are ineffective.

Benzylpenicillin is active mainly against gram-positive cocci. The antibacterial action spectra of benzylpenicillin and phenoxymethylpenicillin are almost identical. However, benzylpenicillin is 5-10 times more active than phenoxymethylpenicillin against sensitive Neisseria spp. and some anaerobes. Phenoxymethylpenicillin is prescribed for infections medium severity. The activity of penicillin preparations is determined biologically by the antibacterial effect on a certain strain of Staphylococcus aureus. The unit of action (1 U) is taken to be the activity of 0.5988 μg of chemically pure crystalline sodium salt of benzylpenicillin.

Significant disadvantages of benzylpenicillin are its instability to beta-lactamases (with enzymatic cleavage of the beta-lactam ring by beta-lactamases (penicillinases) with the formation of penicillanic acid, the antibiotic loses its antimicrobial activity), insignificant absorption in the stomach (causes a relatively low need for injection routes of administration) in relation to the majority of gram-negative microorganisms.

Under normal conditions, benzylpenicillin preparations poorly penetrate into the cerebrospinal fluid, however, with inflammation of the meninges, permeability through the BBB increases.

Benzylpenicillin, used in the form of highly soluble sodium and potassium salts, acts for a short time - 3-4 hours, because quickly excreted from the body, and this requires frequent injections. In this regard, poorly soluble salts of benzylpenicillin (including novocaine salt) and benzathine benzylpenicillin have been proposed for use in medical practice.

Prolonged forms of benzylpenicillin, or depot-penicillins: Bicillin-1 (benzathine benzylpenicillin), as well as combined drugs based on them - Bicillin-3 (benzathine benzylpenicillin + benzylpenicillin sodium + benzylpenicillin novocaine salt + 5 benzylpenicillin benzathine benzathine benzathine ) are suspensions that can only be administered intramuscularly. They are slowly absorbed from the injection site, creating a depot in muscle tissue. This makes it possible to maintain the concentration of the antibiotic in the blood for a considerable time and thus reduce the frequency of administration of the drug.

All benzylpenicillin salts are used parenterally, because they are destroyed in the acidic environment of the stomach. Of natural penicillins, acid-stable properties, although in weak degree, only phenoxymethylpenicillin (penicillin V) possesses. Phenoxymethylpenicillin chemically differs from benzylpenicillin by the presence of a phenoxymethyl group instead of a benzyl group in the molecule.

Benzylpenicillin is used for streptococcal infections, including Streptococcus pneumoniae (community-acquired pneumonia, meningitis), Streptococcus pyogenes(streptococcal tonsillitis, impetigo, erysipelas, scarlet fever, endocarditis), with meningococcal infections. Benzylpenicillin is the antibiotic of choice in the treatment of diphtheria, gas gangrene, leptospirosis, and Lyme disease.

Bicillins are indicated, first of all, when it is necessary to maintain effective concentrations in the body for a long time. They are used for syphilis and other diseases caused by pale treponema (yaws), streptococcal infections (excluding infections caused by group B streptococci) - acute tonsillitis, scarlet fever, wound infections, erysipelas, rheumatism, leishmaniasis.

In 1957, 6-aminopenicillanic acid was isolated from natural penicillins, and on its basis the development of semi-synthetic preparations began.

6-Aminopenicillanic acid - the basis of the molecule of all penicillins ("penicillin core") - a complex heterocyclic compound, consisting of two rings: thiazolidine and beta-lactam. A side radical is associated with the beta-lactam ring, which determines the essential pharmacological properties the resulting drug molecule. In natural penicillins, the structure of the radical depends on the composition of the medium on which they grow Penicillium spp.

Semisynthetic penicillins are produced by chemical modification by attaching various radicals to the 6-aminopenicillanic acid molecule. Thus, penicillins were obtained with certain properties:

Penicillinase-resistant (beta-lactamase);

Acid-fast, effective when administered orally;

Possessing a wide range of actions.

Isoxazolepenicillins (isoxazolyl penicillins, penicillinase-stable, antistaphylococcal penicillins). Most staphylococci produce a specific enzyme beta-lactamase (penicillinase) and are resistant to benzylpenicillin (80-90% of strains are penicillinase-forming Staphylococcus aureus).

The main antistaphylococcal drug is oxacillin. The group of penicillinase-resistant drugs also includes cloxacillin, flucloxacillin, methicillin, nafcillin and dicloxacillin, which, due to high toxicity and / or low efficacy, have not found clinical use.

The spectrum of antibacterial action of oxacillin is similar to the spectrum of action of benzylpenicillin, but due to the resistance of oxacillin to penicillinase, it is active against penicillinase-forming staphylococci that are resistant to benzylpenicillin and phenoxymethylpenicillin, as well as resistant to other antibiotics.

By activity against gram-positive cocci (including staphylococci that do not produce beta-lactamase) isoxazolepenicillins, incl. oxacillin, are significantly inferior to natural penicillins, therefore, in diseases caused by microorganisms sensitive to benzylpenicillin, they are less effective than the latter. Oxacillin does not show activity against gram-negative bacteria (except Neisseria spp.), anaerobes. In this regard, drugs of this group are indicated only in cases where it is known that the infection is caused by penicillinase-forming strains of staphylococci.

The main pharmacokinetic differences between isoxazolepenicillins and benzylpenicillin are:

Fast, but not complete (30-50%) absorption from the gastrointestinal tract. These antibiotics can be used both parenterally (i / m, i / v) and orally, but 1-1.5 hours before meals, because they have low resistance to hydrochloric acid;

A high degree of binding to plasma albumin (90-95%) and the inability to remove isoxazolepenicillins from the body during hemodialysis;

Not only renal, but also hepatic excretion, no need to adjust the dosage regimen for mild renal failure.

The main clinical significance of oxacillin is the treatment of staphylococcal infections caused by penicillin-resistant strains Staphylococcus aureus(except for infections caused by methicillin-resistant Staphylococcus aureus, MRSA). It should be borne in mind that strains are common in hospitals Staphylococcus aureus resistant to oxacillin and methicillin (methicillin is the first penicillinase-resistant penicillin, discontinued). Nosocomial and community-acquired strains Staphylococcus aureus that are resistant to oxacillin / methicillin are usually multi-resistant - they are resistant to all other beta-lactams, and also often to macrolides, aminoglycosides, fluoroquinolones. The drugs of choice for MRSA infections are vancomycin or linezolid.

Nafcillin is slightly more active than oxacillin and other penicillin-resistant penicillins (but less active than benzylpenicillin). Nafcillin penetrates the BBB (its concentration in the cerebrospinal fluid is sufficient for the treatment of staphylococcal meningitis), is excreted mainly in the bile (the maximum concentration in bile is much higher than in serum), to a lesser extent - by the kidneys. Oral and parenteral administration is possible.

Amidinopenicillins - These are penicillins of a narrow spectrum of action, but with predominant activity against gram-negative enterobacteria. Amidinopenicillin preparations (amdinocillin, pivamdinocillin, bacamdinocillin, acidocillin) are not registered in Russia.

Extended-spectrum penicillins

According to the classification presented by D.A. Kharkevich, semisynthetic broad-spectrum antibiotics are divided into the following groups:

I. Drugs that do not affect Pseudomonas aeruginosa:

Aminopenicillins: ampicillin, amoxicillin.

II. Drugs active against Pseudomonas aeruginosa:

Carboxypenicillins: carbenicillin, ticarcillin, carphecillin;

Ureidopenicillins: piperacillin, azlocillin, mezlocillin.

Aminopenicillins - broad-spectrum antibiotics. All of them are destroyed by beta-lactamases of both gram-positive and gram-negative bacteria.

In medical practice, amoxicillin, ampicillin are widely used. Ampicillin is the ancestor of the aminopenicillin group. In relation to gram-positive bacteria, ampicillin, like all semisynthetic penicillins, is inferior in activity to benzylpenicillin, but superior to oxacillin.

Ampicillin and amoxicillin have similar spectra of action. Compared with natural penicillins, the antimicrobial spectrum of ampicillin and amoxicillin extends to sensitive strains of enterobacteria, Escherichia coli, Proteus mirabilis, Salmonella spp., Shigella spp., Haemophilus influenzae ; better than natural penicillins act on Listeria monocytogenes and sensitive enterococci.

Of all oral beta-lactams, amoxicillin has the greatest activity against Streptococcus pneumoniae, resistant to natural penicillins.

Ampicillin is not effective against penicillinase-forming strains Staphylococcus spp., all strains Pseudomonas aeruginosa, most strains Enterobacter spp., Proteus vulgaris(indole positive).

Combined drugs are available, for example Ampiox (ampicillin + oxacillin). The combination of ampicillin or benzylpenicillin with oxacillin is rational, because the spectrum of action with this combination becomes wider.

The difference between amoxicillin (which is one of the leading oral antibiotics) from ampicillin is its pharmacokinetic profile: when taken orally, amoxicillin is more rapidly and well absorbed in the intestine (75-90%) than ampicillin (35-50%), bioavailability does not depend on food intake ... Amoxicillin penetrates better into some tissues, incl. into the bronchopulmonary system, where its concentration is 2 times higher than the concentration in the blood.

The most significant differences in the pharmacokinetic parameters of aminopenicillins from benzylpenicillin:

Possibility of assignment inside;

Insignificant binding to plasma proteins - 80% of aminopenicillins remain in the blood in free form - and good penetration into tissues and body fluids (with meningitis, concentrations in the cerebrospinal fluid can be 70-95% of concentrations in the blood);

The multiplicity of prescribing combined drugs is 2-3 times a day.

The main indications for the appointment of aminopenicillins are infections of the upper respiratory tract and ENT organs, infections of the kidneys and urinary tract, infections of the gastrointestinal tract, eradication Helicobacter pylori (amoxicillin), meningitis.

A feature of the undesirable action of aminopenicillins is the development of an "ampicillin" rash, which is a maculopapular rash of a non-allergic nature, which quickly disappears when the drug is discontinued.

One of the contraindications to the appointment of aminopenicillins is infectious mononucleosis.

Antipseudomonal penicillins

These include carboxypenicillins (carbenicillin, ticarcillin) and ureidopenicillins (azlocillin, piperacillin).

Carboxypenicillins Are antibiotics that have a spectrum of antimicrobial action similar to aminopenicillins (with the exception of the effect on Pseudomonas aeruginosa). Carbenicillin - the first antipseudomonal penicillin, is inferior in activity to other antipseudomonal penicillins. Carboxypenicillins act on Pseudomonas aeruginosa (Pseudomonas aeruginosa) and indole-positive proteus species (Proteus spp.) resistant to ampicillin and other aminopenicillins. The clinical significance of carboxypenicillins is currently decreasing. Although they have a wide spectrum of action, they are inactive against most strains. Staphylococcus aureus, Enterococcus faecalis, Klebsiella spp., Listeria monocytogenes... Almost do not pass through the BBB. Multiplicity of appointment - 4 times a day. Secondary resistance of microorganisms develops rapidly.

Ureidopenicillins - these are also antipseudomonal antibiotics, their spectrum of action coincides with carboxypenicillins. The most active drug in this group is piperacillin. Of the drugs in this group, only azlocillin retains its importance in medical practice.

Ureidopenicillins are more active than carboxypenicillins in relation to Pseudomonas aeruginosa. They are also used in the treatment of infections caused by Klebsiella spp.

All antipseudomonal penicillins are destroyed by beta-lactamases.

Pharmacokinetic features of ureidopenicillins:

Administered only parenterally (intramuscular and intravenous);

Excretion involves not only the kidneys, but also the liver;

Frequency rate of application - 3 times a day;

Secondary resistance of bacteria develops rapidly.

Due to the emergence of strains with high resistance to antipseudomonal penicillins and the lack of advantages over other antibiotics, antipseudomonal penicillins have practically lost their value.

The main indications for these two groups of antipseudomonal penicillins are nosocomial infections caused by susceptible strains Pseudomonas aeruginosa, in combination with aminoglycosides and fluoroquinolones.

Penicillins and other beta-lactam antibiotics have high antimicrobial activity, but many of them can develop resistance of microorganisms.

This resistance is due to the ability of microorganisms to produce specific enzymes - beta-lactamases (penicillinases), which destroy (hydrolyze) the beta-lactam ring of penicillins, which deprives them of antibacterial activity and leads to the development of resistant strains of microorganisms.

Some semi-synthetic penicillins are resistant to beta-lactamases. In addition, to overcome acquired resistance, compounds have been developed that are capable of irreversibly inhibiting the activity of these enzymes, the so-called. beta-lactamase inhibitors. They are used to create inhibitor-protected penicillins.

Beta-lactamase inhibitors, like penicillins, are beta-lactam compounds, but they themselves have minimal antibacterial activity. These substances irreversibly bind to beta-lactamases and inactivate these enzymes, thereby protecting beta-lactam antibiotics from hydrolysis. Inhibitors of beta-lactamases are most active against beta-lactamases encoded by plasmid genes.

Inhibitor-protected penicillins are a combination of a penicillin antibiotic with a specific inhibitor of beta-lactamases (clavulanic acid, sulbactam, tazobactam). Beta-lactamase inhibitors are not used alone, but are used in combination with beta-lactams. This combination makes it possible to increase the resistance of the antibiotic and its activity against microorganisms that produce these enzymes (beta-lactamases): Staphylococcus aureus, Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, Escherichia coli, Klebsiella spp., Proteus spp., anaerobes, incl. Bacteroides fragilis... As a result, strains of microorganisms resistant to penicillins become sensitive to the combined drug. The spectrum of antibacterial activity of inhibitor-protected beta-lactams corresponds to the spectrum of penicillins contained in their composition, only the level of acquired resistance differs. Inhibitor-protected penicillins are used to treat infections of various localizations and for perioperative prophylaxis in abdominal surgery.

Inhibitor-protected penicillins include amoxicillin / clavulanate, ampicillin / sulbactam, amoxicillin / sulbactam, piperacillin / tazobactam, ticarcillin / clavulanate. Ticarcilin / clavulanate has antipseudomonal activity and is active against Stenotrophomonas maltophilia... Sulbactam has its own antibacterial activity against gram-negative cocci of the family Neisseriaceae and the family of non-fermenting bacteria Acinetobacter.

Indications for the use of penicillins

Penicillins are used for infections caused by pathogens that are sensitive to them. They are mainly used for upper respiratory tract infections, in the treatment of angina, scarlet fever, otitis media, sepsis, syphilis, gonorrhea, gastrointestinal tract infections, urinary tract infections, etc.

It is necessary to use penicillins only as directed and under the supervision of a physician. It must be remembered that the use of insufficient doses of penicillins (like other antibiotics) or stopping treatment too early can lead to the development of resistant strains of microorganisms (especially natural penicillins). If resistance develops, therapy with other antibiotics should be continued.

The use of penicillins in ophthalmology. In ophthalmology, penicillins are used topically in the form of instillations, subconjunctival and intravitreal injections. Penicillins do not pass well through the blood-ophthalmic barrier. Against the background of the inflammatory process, their penetration into the internal structures of the eye increases and the concentrations in them reach therapeutically significant ones. So, when instilled into the conjunctival sac, therapeutic concentrations of penicillins are determined in the corneal stroma; when applied topically, they practically do not penetrate into the moisture of the anterior chamber. With subconjunctival administration, drugs are determined in the cornea and moisture of the anterior chamber of the eye, in vitreous- concentrations below therapeutic.

Solutions for topical application prepare ex tempore. Penicillins are used for the treatment of gonococcal conjunctivitis (benzylpenicillin), keratitis (ampicillin, benzylpenicillin, oxacillin, piperacillin, etc.), canaliculitis, especially caused by actinomycetes (benzylpenicillin, phenoxymethylpenicillin / phylacillin) etc.) and other eye diseases. In addition, penicillins are used to prevent infectious complications in eyelid and orbital injuries, especially when a foreign body penetrates into the orbital tissue (ampicillin / clavulanate, ampicillin / sulbactam, etc.).

The use of penicillins in urological practice. In urological practice, inhibitor-protected drugs are widely used from antibiotics-penicillins (the use of natural penicillins, as well as the use of semi-synthetic penicillins as drugs of choice is considered not justified due to high level resistance of uropathogenic strains.

Side and toxic effect penicillins. Penicillins have the lowest toxicity among antibiotics and a wide range of therapeutic action (especially natural ones). Most of the serious side effects are related to hypersensitivity to them. Allergic reactions are observed in a significant number of patients (according to various sources, from 1 to 10%). Penicillins are more common than other drugs pharmacological groups are the cause of drug allergies. In patients with a history of allergic reactions to the administration of penicillins, with subsequent use, these reactions are noted in 10-15% of cases. Less than 1% of people who have not previously experienced such reactions develop an allergic reaction to penicillin when it is re-administered.

Penicillins can cause an allergic reaction in any dose and in any dosage form.

When using penicillins, both immediate and delayed allergic reactions are possible. It is believed that the allergic reaction to penicillins is mainly associated with an intermediate product of their metabolism - the penicilloin group. It is called a large antigenic determinant and is formed when the beta-lactam ring is broken. Small antigenic determinants of penicillins include, in particular, unchanged molecules of penicillins, benzylpenicilloate. They are formed in vivo, but are also determined in solutions of penicillins prepared for administration. It is believed that early allergic reactions to penicillins are mediated mainly by IgE antibodies to small antigenic determinants, delayed and late (urticaria) - usually IgE antibodies to large antigenic determinants.

Hypersensitivity reactions are caused by the formation of antibodies in the body and usually occur a few days after the start of penicillin use (the timing can range from a few minutes to several weeks). In some cases, allergic reactions are manifested in the form of a skin rash, dermatitis, fever. In more severe cases, these reactions are manifested by edema of the mucous membranes, arthritis, arthralgia, kidney damage, and other disorders. Anaphylactic shock, bronchospasm, abdominal pain, cerebral edema and other manifestations are possible.

A severe allergic reaction is an absolute contraindication to further administration of penicillins. The patient must be explained that even a small amount of penicillin ingested with food or during a skin test can be fatal for him.

Sometimes the only symptom of an allergic reaction to penicillins is fever (it is constant, remitting or intermittent in nature, sometimes accompanied by chills). Fever usually disappears within 1-1.5 days after drug withdrawal, but sometimes it can persist for several days.

All penicillins are characterized by cross-sensitization and cross-allergic reactions. Any preparations containing penicillin, including cosmetics and foods, may cause sensitization.

Penicillins can cause a variety of non-allergic side and toxic effects. These include: when taken orally - irritating effect, incl. glossitis, stomatitis, nausea, diarrhea; with i / m administration - pain, infiltration, aseptic muscle necrosis; with intravenous administration - phlebitis, thrombophlebitis.

An increase in reflex excitability of the central nervous system is possible. When using high doses, neurotoxic effects may occur: hallucinations, delirium, impaired blood pressure regulation, convulsions. Seizures are more likely in patients receiving high doses of penicillin and / or in patients with severely impaired liver function. Due to the risk of severe neurotoxic reactions, penicillins should not be administered endolumbar (with the exception of benzylpenicillin sodium salt, which is administered with extreme caution, for health reasons).

When treating with penicillins, it is possible to develop superinfection, candidiasis of the oral cavity, vagina, intestinal dysbiosis. Penicillins (usually ampicillin) can cause antibiotic-associated diarrhea.

The use of ampicillin leads to the appearance of "ampicillin" rash (in 5-10% of patients), accompanied by itching, fever. This side effect often occurs on the 5-10th day of the use of large doses of ampicillin in children with lymphadenopathy and viral infections or with concomitant use of allopurinol, as well as in almost all patients with infectious mononucleosis.

Specific adverse reactions when using bicillins are local infiltrates and vascular complications in the form of One's syndromes (ischemia and gangrene of the extremities when accidentally injected into an artery) or Nicolau (pulmonary and cerebral vascular embolism when injected into a vein).

When using oxacillin, hematuria, proteinuria, interstitial nephritis are possible. The use of antipseudomonal penicillins (carboxypenicillins, ureidopenicillins) may be accompanied by the appearance allergic reactions, symptoms of neurotoxicity, acute interstitial nephritis, dysbiosis, thrombocytopenia, neutropenia, leukopenia, eosinophilia. When using carbenicillin, it is possible hemorrhagic syndrome... Combination drugs containing clavulanic acid can cause acute liver damage.

Application during pregnancy. Penicillins cross the placenta. Although there are no adequate and well-controlled safety studies in humans, penicillins, incl. inhibitor-protected, are widely used in pregnant women, with no complications recorded.

In studies on laboratory animals with the introduction of penicillins in doses of 2-25 (for different penicillins) exceeding therapeutic, fertility disorders and effects on reproductive function were not found. No teratogenic, mutagenic, or embryotoxic properties have been identified when penicillins were administered to animals.

In accordance with the globally recognized FDA (Food and Drug Administration) recommendations that determine the possibility of using drugs during pregnancy, the drugs of the penicillin group in terms of their effect on the fetus belong to FDA category B (the study of animal reproduction did not reveal an adverse effect of drugs on the fetus, but adequate and there are no strictly controlled studies in pregnant women).

When prescribing penicillins during pregnancy, the gestational age should be taken into account (as with any other means). In the process of therapy, it is necessary to strictly monitor the condition of the mother and fetus.

Application during breastfeeding. Penicillins pass into breast milk. Although significant complications in humans have not been reported, the use of penicillins by nursing mothers can lead to sensitization of the child, changes in intestinal microflora, diarrhea, the development of candidiasis and the appearance of skin rashes in infants.

Pediatrics. When using penicillins in children, no specific pediatric problems have been reported, but it should be borne in mind that insufficiently developed renal function in newborns and children early age can lead to the accumulation of penicillins (in this regard, there is an increased risk of neurotoxic action with the development of seizures).

Geriatrics. No specific geriatric problems have been reported with penicillins. However, it should be borne in mind that the elderly are more likely to age-related renal impairment, and therefore dose adjustment may be required.

Dysfunction of the kidneys and liver. With renal / hepatic insufficiency, cumulation is possible. With moderate to severe impairment of renal and / or liver function, dose adjustment and an increase in the periods between antibiotic injections are required.

Interaction of penicillins with other drugs. Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect, bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) are antagonistic. Care must be taken when combining penicillins active against Pseudomonas aeruginosa (Pseudomonas aeruginosa), with anticoagulants and antiplatelet agents (potential risk of increased bleeding). It is not recommended to combine penicillins with thrombolytics. When combined with sulfonamides, the bactericidal effect may be weakened. Oral penicillins can reduce the effectiveness of oral contraceptives due to impaired enterohepatic estrogen circulation. Penicillins can slow down the excretion of methotrexate from the body (inhibit its tubular secretion). When ampicillin is combined with allopurinol, the likelihood of a skin rash increases. The use of high doses of benzylpenicillin potassium salt in combination with potassium-sparing diuretics, potassium preparations or ACE inhibitors increases the risk of hyperkalemia. Penicillins are pharmaceutically incompatible with aminoglycosides.

Due to the fact that with prolonged oral administration of antibiotics, the intestinal microflora, which produces vitamins B 1, B 6, B 12, PP, can be suppressed, it is advisable for patients to prescribe B vitamins to prevent hypovitaminosis.

In conclusion, it should be noted that penicillins are a large group of natural and semi-synthetic antibiotics that have a bactericidal effect. The antibacterial effect is associated with a violation of the synthesis of peptidoglycan of the cell wall. The effect is due to the inactivation of the enzyme transpeptidase, one of the penicillin-binding proteins located on the inner membrane of the bacterial cell wall, which takes part in the later stages of its synthesis. The differences between penicillins are associated with the peculiarities of their spectrum of action, pharmacokinetic properties and the spectrum of undesirable effects.

For several decades of successful use of penicillins, problems have arisen associated with their misuse. So, the prophylactic administration of penicillins at risk bacterial infection is often unreasonable. Incorrect treatment regimen - incorrect selection of the dose (too high or too low) and the frequency of administration can lead to the development of side effects, a decrease in effectiveness and the development of drug resistance.

So, at present, most strains Staphylococcus spp. resistant to natural penicillins. In recent years, the frequency of detection of resistant strains has increased. Neisseria gonorrhoeae.

The main mechanism of acquired resistance to penicillins is associated with the production of beta-lactamases. To overcome the acquired resistance, which is widespread among microorganisms, compounds have been developed that are capable of irreversibly suppressing the activity of these enzymes, the so-called. beta-lactamase inhibitors - clavulanic acid (clavulanate), sulbactam and tazobactam. They are used to create combined (inhibitor-protected) penicillins.

It should be remembered that the choice of one or another antibacterial drug, incl. penicillin, should be due, first of all, to the sensitivity of the pathogen that caused the disease to it, as well as the absence of contraindications to its appointment.

Today not a single medical institution can do without an antibiotic. Successful treatment of various diseases is possible only through the appointment of effective antibacterial therapy. The antibiotic today is represented by a wide range of various drugs aimed at the death of the pathogenic environment of a bacterial nature.

The first antibiotic created was penicillin, which defeated some epidemics and deadly diseases in the 20th century. Today, antibiotics of the penicillin group are rarely used in medical practice due to the high sensitivity of patients and the risk of developing allergies.

Antibiotic groups without penicillin

Antibiotic therapy without the use of penicillin components implies the appointment of alternative drugs of other pharmacological groups. Antibiotics without penicillin in a large assortment are produced for the treatment of various diseases in hospital and outpatient practice in children or adults.

Group of cephalosporins

Cephalosporins are antibiotics with a wide range of effects, which is due to the detrimental effect on many groups of microorganisms, strains and other pathogenic environments. The drugs of the cephalosporin group are available as intramuscular or intravenous injections. Antibiotics of this group are prescribed for the following conditions:

Famous cephalosporins include Ceforal, Suprax, Pancef. All antibiotics in this series have similar side effects, for example, dyspeptic disorders (upset stools, skin rashes, nausea). The main advantage of antibiotics is not only the detrimental effect on many strains, but also the possibility of treating children (including the neonatal period). Cephalosporin antibiotics are classified into the following groups:

1st generation

Cephalosporin antibiotics include Cefadroxil and Cephalexin, Cefazolin, Cefuroxime.

They are used for inflammatory diseases caused by many anaerobic bacteria, staphylococcal infection, streptococci and others.

Forms of drug release are varied: from tablets to solutions for parenteral administration.

2nd generation

Known drugs in this group: Cefuroxime (injections), Cefaclor, Cefuroxime axetila. The drugs are especially active against many gram-positive and gram-negative bacteria. The drugs are available both in the form of solutions and in tablet form.

III generation

Antibiotics of this series just belong to a wide spectrum of action. The drugs act on almost all microorganisms and are known under the following names:

  • Ceftriaxone;
  • Ceftazidime;
  • Cefoperazone;
  • Cefixime and Ceftibuten.

Forms of release - injections for intravenous or intramuscular administration. When the drug is administered, it is often mixed with saline or lidocaine solution to reduce pain. The drug and additional components are mixed in one syringe.

IV generation

The group is represented by only one drug - Cefepim. The pharmaceutical industry produces a drug in the form of a powder, which is diluted just before administration through the parenteral or intramuscular route.

The destructive effect of the antibiotic is to disrupt the synthesis of the body wall of the microbial unit at the cellular level. The main advantages include the possibility of treatment on an outpatient basis, ease of use, use in young children, minimal risks of development side effects and complications.

Macrolide group

Antibiotics from the macrolide group are drugs of a new generation, the structure of which is a full-fledged macrocyclic lactone ring. By the type of molecular atomic structure, this group received this name. Several types of macrolides are distinguished from the number of carbon atoms in the molecular composition:

  • 14, 15 membered;
  • 15-membered.

Macrolides are especially active against many gram-positive coccal bacteria, as well as pathogens acting at the cellular level (for example, mycoplasma, legionela, campylobacter). Macrolides have the lowest toxicity, are suitable for the treatment of inflammatory diseases of ENT organs (sinusitis, whooping cough, otitis media of various classification). The list of macrolide drugs is as follows:

Numerous medical studies have confirmed the low likelihood of side effects. The main disadvantage can be considered the rapid development of resistance of various groups of microorganisms, which explains the lack of therapeutic results in some patients.

Fluoroquinolone group

Antibiotics from the group of fluoroquinols do not contain penicillin and its components, but are used to treat the most acute and severe inflammatory diseases.

This includes purulent bilateral otitis media, severe bilateral pneumonia, pyelonephritis (including chronic forms), salmonellosis, cystitis, dysentery and others.

Fluoroquinols include the following drugs:

  • Ofloxacin;
  • Levofloxacin;
  • Ciprofloxacin.

The earliest developments of this group of antibiotics date back to the 20th century. The most famous fluoroquinols can belong to different generations and solve specific clinical problems.

1st generation

Known medicines from this group are Negram and Nevigramon. The basis of antibiotics is nalidixic acid. The drugs have a detrimental effect on the following types of bacteria:

  • proteas and klebsiella;
  • shigella and salmonella.

Antibiotics of this group are characterized by strong permeability, a sufficient number of negative consequences of admission. According to the results of clinical and laboratory studies, the antibiotic confirmed its absolute uselessness in the treatment of gram-positive cocci, some anaerobic microorganisms, Pseudomonas aeruginosa (including nosocomial type).

2nd generation

Second-generation antibiotics are derived from a combination of chlorine atoms and quinoline molecules. Hence the name - a group of fluoroquinolones. The list of antibiotics in this group is represented by the following drugs:


Second-generation antibiotics are prescribed for serious surgical situations and are used in patients of any age group. Here, the main factor is the risk of death, and not the appearance of any side effects.

III, IV generation

To the main pharmacological drugs 3 generations should include Levofloxacin (otherwise, Tavanik), used for chronic bronchitis, severe bronchial obstruction in other pathologies, anthrax, diseases of ENT organs.

Moxifloxacin (pharmacol. Avelox), known for its inhibitory effect on staphylococcal microorganisms, is reasonably considered to be the 4th generation. Avelox is the only drug that is effective against non-spore-forming anaerobic microorganisms.

Antibiotics of various groups have special instructions, indications, as well as contraindications for use. In connection with the uncontrolled use of antibiotics without penicillin and others, a law was passed on prescriptions from pharmacy chains.

Medicine of this kind is in great need because of the resistance of many pathogenic media to modern antibiotics. Penicillins have not been widely used in medical practice for more than 25 years, so it can be assumed that this group of drugs will effectively affect new types of bacterial microflora.

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The video tells about how to quickly cure a cold, flu or SARS. The opinion of an experienced doctor.



Antibiotics are substances that are produced by microorganisms or synthesized using medical technology from natural raw materials. These drugs are used to suppress the growth and development of colonies of pathogenic agents that have entered the human body.

Antibiotics of the penicillin group are the first drugs from this area that were used in clinical practice. And, despite the fact that almost 100 years have passed since their discovery, and the list of antimicrobial agents has been supplemented with medicines of the cephalosporin, fluoroquinol and other series, penicillin-type compounds are still the main antibacterial drugs for the relief of a huge list of infectious diseases.

A bit of history

The discovery of penicillin happened quite by accident: in 1928, scientist Alexander Fleming, who worked in one of the London hospitals, discovered a mold that grew on a nutrient medium, which was capable of destroying staphylococcal colonies.

The researcher named the active substance of the microscopic filamentous fungus Penicillium notatum penicillin. After 12 years, the first antibiotic was isolated in its pure form, and in 1942 the Soviet microbiologist Zinaida Ermolyeva received a drug from another type of fungus - Penicillium crustosum.

Since the second half of the 20th century, unlimited amounts of penicillin G (or benzylpenicillin) have become available to fight a wide variety of diseases.

Operating principle

The described active substance acts on pathogens bactericidal and bacteriostatic. The mechanism of the bactericidal scheme of the drugs included in the penicillin type (series) is associated with damage to the cell walls (violation of the integrity of the structure) of infectious agents, which leads to the death of microorganisms.

The bacteriostatic principle of action on pathogens is characterized by a temporary suppression of the ability of pathogens to reproduce.

The type of drug exposure is selected taking into account the severity of the development of the disease.

Most penicillins in small doses affect microbes bacteriostatically. With an increase in the amount of the drug involved, the effect changes to a bactericidal one. The specific dosage of the drug of the penicillin group can only be selected by a doctor; it is impossible to use antibiotics for treatment on your own.

Systematization of drugs

In addition to benzylpenicillin (and its various salts - sodium, potassium), natural penicillins also include:

  • Phenoxymethylpenicillin;
  • Benzathine benzylpenicillin.

The basic principles for the classification of semi-synthetic penicillin species are indicated below.

  • isoxazolyl-penicillins (Oxacillin, Nafcillin);
  • amino-penicillins (Amoxicillin, Ampicillin);
  • aminodi-penicillins (there are no medicines registered in the Russian Federation.);
  • carboxy-penicillins (carbenicillin);
  • ureido-penicillins (Piperacillin, Azlocillin);
  • inhibitor-protected penicillins (Piperacillin in combination with tazobactam, Ticarcillin in combination with clavulanate, Ampicillin in combination with sulbactam).

Brief description of natural medicines

Natural (natural) penicillins are drugs that have a narrow spectrum of effects on microorganisms. Due to long-term (and often uncontrolled) use of them for medical purposes, most pathogens have managed to acquire immunity to these types of antibiotics.

Today, the drugs Bicillin and Benzylpenicillin are most often used in the treatment of diseases, which are quite effective against some anaerobic agents, spirochetes, a number of cocci and gram-positive pathogens.

Gram-negative bacteria H. ducreyi, P. multocida, Neisseria spp., As well as listeria, a species of corynebacteria (in particular, C.diphtheriae), remain sensitive to natural antibiotics.

The method of using medicines to suppress the development of these pathogens is injection.

Natural penicillins, according to experts, have one major drawback: they are destroyed by beta-lactamases (enzymes produced by some microorganisms). That is why natural antibiotics belonging to the penicillin group are not used to treat ailments caused by staphylococcal infections.

Description of synthesized types of drugs

A number of semisynthetic drugs included in the penicillin antibiotic series and combined into the aminodipenicillin group are not registered in our country. Acidocillin, Amdinocillin, Bacamdinocillin are drugs with a narrow spectrum of action and are effective against gram-negative enterobacteriaceae.

The rest of the synthesized groups of drugs are widely used in medical institutions in Russia and require more detailed consideration.

Antistaphylococcal (penicillinase-stable) drugs

Another name for this group of antibiotics is isoxazolylpenicillins. Most often, the drug Oxacillin is used in therapy. The subspecies includes several more drugs (in particular, Nafcillin, Dicloxacillin, Methicillin), which are used extremely rarely due to their high toxicity.

In terms of the spectrum of action on pathogens, Oxacillin is similar to medicines included in the natural penicillin series, but slightly inferior to them in the level of activity (in particular, it is less effective against microbes sensitive to the effects of Benzylpenicillin).

The main difference between the drug and other penicillins is resistance to beta-lactamases, which are produced by staphylococci. The practical application of Oxycillin has been found in the fight against strains of this microorganism, which is the causative agent of community-acquired infections.

Aminopenicillins

This group of semi-synthetic penicillins is characterized by a wide range of effects on pathogens. The ancestor of aminopenicillins is the drug Ampicillin. On a number of parameters, it is superior to Oxycillin, but inferior to Benzylpenicillin.

Close in scope to this medication is the drug Amoxicillin.

Since these representatives of the group are susceptible to the destructive effects of beta-lactamases, medications protected from the action of enzymes of infectious agents by inhibitors (for example, Amoxicillin in combination with clavuanic acid, Ampicillin in combination with sulbactam) have been introduced into medical practice.

The expansion of the antimicrobial spectrum of inhibitor-protected aminopenicillins was due to the manifestation of their activity in relation to:

  • gram-negative bacteria (C.diversus, P.vulgaris, Klebsiella spp.);
  • gonococci;
  • staphylococci;
  • anaerobes of the species B.fragilis.

The growth and development of microorganisms, whose resistance to the penicillin type of antibiotics is not associated with the production of beta-lactamases, are not affected by inhibitor-protected aminopenicillins.

Ureidopenicillins and carboxypenicillins

Representatives of these groups are semi-synthetic antibiotics of the penicillin series that stop Pseudomonas aeruginosa; the list of these drugs is quite wide, but in modern medicine they are rarely used (pathogens lose sensitivity to them in a short time).

Carboxypenicillin medicines Carbenicillin, Tikarcillin (the latter is not registered in the Russian Federation) suppress the development of colonies of gram-positive bacteria and microorganisms of the family P. aeruginosa, Enterobacteriaceae.

Most effective remedy from the group of ureidopenicillins - Piperacillin; it is used in the fight against diseases caused by Klebsiella spp.

The described antibiotics, as well as natural penicillins, are susceptible to the negative influence of beta-lactamases. The solution to the problem was found in the synthesis of fundamentally new antimicrobial agents, in which, in addition to the already mentioned active substances, inhibitors were introduced.

Inhibitor-protected ureidopenicillins, carboxypenicillins have a wide range of effects on most known pathogens.

Pharmacokinetics

When taken orally, the antibiotic included in the penicillin series of drugs is quickly absorbed and, penetrating into the liquid media and tissues of the body, begins to affect the colonies of pathogens.

Medicines are characterized by the ability to concentrate in pleural, pericardial, synovial fluids and bile. They practically do not pass into the internal environment of the organs of vision and prostate, cerebrospinal fluid. They are found in minimal proportions in breast milk. In small quantities, they penetrate the placental barrier.

If necessary (for example, detection of meningitis in a patient), therapeutic concentrations in cerebrospinal fluid are achieved by introducing significant doses of drugs.

Some of the penicillins in tablet form are destroyed under the influence of gastrointestinal enzymes, and therefore it is used parenterally.

The main indicators of the process of transporting active substances from the digestive system into the blood of commonly used medicines (in tablets) are shown in the table.

Excretion of penicillins mainly (more than 60%) occurs with the help of the kidneys; some medications are excreted in the bile. Almost all drugs of the described group are removed during hemodialysis.

Contraindications

Despite the fact that most of the representatives of penicillins are characterized by high efficiency in the elimination of infectious agents, these drugs cannot be used to treat all patients without exception.

One of the disadvantages of this kind of medicines is the frequent occurrence of allergic reactions to them in patients (according to statistics, the percentage of skin rashes, edema and itching reaches 10 units).

If there is a history of a sick individual intolerance to penicillin, medical products of this group cannot be used in therapy.

Warnings

Penicillin antibiotics can cause toxic side effects of non-allergic etiology, in particular:

  • attacks of nausea and vomiting;
  • painful sensations in the abdomen;
  • diarrhea;
  • pseudomembranous colitis.

When using high doses of drugs, the manifestation of seizures, headache, hallucinations and fever is possible.

In addition, the use of drugs of the described series is often accompanied by the development of candidiasis, intestinal dysbiosis, the appearance of edema, and a violation of the blood pressure level.

It should be noted that penicillins are among the lowest toxic antibiotics, and the above side effect on the body manifests itself more often with independent uncontrolled use of medications (without first consulting a doctor).

Indications

Predominantly antibiotics of the penicillin group are used to eliminate the symptoms of infections upper paths, tonsillitis, otitis media, as well as in order to arrest the growth of colonies of infectious agents that cause inflammation of the urinary tract, the development of scarlet fever, syphilis and gonorrhea; for the prevention of rheumatism.

In addition, penicillin antibiotic therapy is used when making diagnoses such as:

  • erysipelas;
  • sepsis;
  • Lyme disease
  • meningitis;
  • tonsilopharyngitis;
  • leptospirosis;
  • actinomycosis

It should be remembered that the use of drugs of the penicillin group is allowed only as directed by a doctor. Self-medication can provoke the development of superinfection or the occurrence of severe complications of the disease.

Video

The video tells about how to quickly cure a cold, flu or SARS. The opinion of an experienced doctor.