Today is our story about medicines. Rather, not about drugs in general, but about those of them that raise many questions and disputes. Of course, we will talk about antibiotics. And we will tell you about such a variety of them as 3 generation cephalosporins in tablets.

What are cephalosporins?

Cephalosporins belong to the group of semi-synthetic beta-lactam antibiotics derived from "cephalosporin C" produced by the fungus Cephalosporium Acremonium. Chemically, they are similar to penicillins. The bactericidal effect of beta-lactam antibiotics is based on the inhibition of the synthesis of the bacterial cell wall. They bind to specific proteins in the cell and result in an osmotically unstable cell membrane.

Traditionally, cephalosporins are classified by generation, from the first to the fifth, which correspond to the dates of release and, to some extent, their scope. However, it is more appropriate to distinguish between such drugs in accordance with their kinetic properties and spectrum of activity.

Oral cephalosporins, regardless of the generation they are from, have many similarities. Let's consider them.

Pharmacokinetics

While kinetic parameters such as uptake and plasma half-life differ slightly from one substance to another, all cephalosporins remain unchanged and are largely eliminated by the kidneys. Therefore, with severe renal failure it is recommended to reduce the dose of such drugs.

Indications for use

The basic indications are the same for all oral cephalosporins. In outpatient practice, they are mainly used in the treatment of infections. respiratory tract, including otitis media. Also, these drugs are used for genitourinary infections.

Of course, the resistance of existing pathogens to some antibiotics is important here. However, to date, there is no conclusive data showing that one of the oral cephalosporins is superior in practice to the other. In addition, all of their available forms are child-friendly.

Side effects

Generally, cephalosporins are relatively safe drugs. On average, only about 10% of patients treated with oral cephalosporins complained of adverse reactions... The most common ones are:

• gastrointestinal symptoms, especially diarrhea;
• nausea, vomiting, and various abdominal symptoms;
• cephalosporins can sporadically cause pseudomembranous enterocolitis;
• skin reactions such as rash, urticaria, itching occur in about 1% of patients;
• less commonly, side effects include neurological symptoms, in particular headache, changes in hematological parameters and a slight increase in transaminases.

Allergic reactions to oral cephalosporins are rare and only occur in people who are allergic to penicillin.

Like other antibiotics, 3rd and 4th generation oral cephalosporins tablets may reduce effectiveness oral contraceptives and vaccines. All oral cephalosporins can be prescribed to pregnant women when clearly needed.

On the one hand, third-generation cephalosporins are highly stable with respect to beta-lactamase. They have good activity against Escherichia coli. Also, pneumococci are usually sensitive to them. On the other hand, third-generation cephalosporins are often not effective enough against staphylococci, so they are not very suitable, for example, for the treatment of skin and soft tissue infections.

The list of 3rd generation cephalosporins in tablets includes the following effective drugs:

"Cefetamet"... This drug can be considered as a typical representative of the third generation cephalosporins. Indications for its use, like other cephalosporins, are respiratory and urinary tract infections.

"Cefix"... The tool has the same antibacterial spectrum actions like Cefetamet. The drug is indicated for respiratory diseases throat, nose, ear, infections urinary tract and acute uncomplicated gonorrhea. According to various studies, with its use, side effects are somewhat more common than with other oral cephalosporins, in particular, an increase in the incidence of diarrhea.

"Cefodox"... This drug has the same antimicrobial spectrum as other third-generation cephalosporins. Indications for its use are respiratory and urinary tract infections, as well as uncomplicated gonorrhea. It should be borne in mind that anti-inflammatory drugs interfere with the absorption of the drug.

Cephalosporins of the 4th and 5th generation appeared relatively recently. Distinctive feature beta-lactam antibiotics last generations is that they are introduced into the body bypassing the digestive tract, that is, parenterally. This eliminates their interaction with the intestinal microflora. That is why 5th generation cephalosporins in tablets are not currently produced.

The most widely used drugs of the latest generations are:

"Cefepim"- 4th generation cephalosporin for deep intramuscular use. In the event of a threat to life, the patient is given an intravenous infusion of the drug.

Zefter- bactericidal and water-soluble antibiotic of the 5th generation of the cephalosporin series. The drug is active against many antibiotic-resistant microorganisms penicillin... Contraindicated in persons under 18 years of age.

Oral cephalosporins from different generations are considered to be well tolerated and effective drugs. Wide antibacterial spectrum of action and low risks side effects allow them to be used in the treatment of various infections.

In the treatment of bacterial infection, antibiotics are the main means that can suppress the action of pathogenic flora and destroy the infection. Among the drugs of different groups, cephalosporins are distinguished by high activity and the most insignificant negative effects. Consider the advantages of drugs of the class of cephalosporins, areas of activity, instructions for use, changes in properties during the transition to the next generation.

Description of cephalosporins

The drugs in this group are beta-lactams and are of semi-synthetic origin. For the first time, the antibacterial action of Cephalosporium isolated from fungi was tested back in the 40s of the last century. The first antibiotic derived from Cephalosporium was synthesized in 1964. It was Cephalothin.

In 1971, Cefazolin was created, which has been actively used for almost 10 years. In 1977, the time of the second generation came, Cefuroxime and Ceftriaxone appeared.

Composition

Cephalosporins are bicyclic compounds in which two rings are combined:

• beta-lactam;
• dihydrothiazine.

The chemical base together is 7-aminocephalosporanic acid (7-ACA).

Release form: tablets, capsules, granules, injection

Most of the drugs in this group are used for injection into a vein or muscle, as they are poorly absorbed by the mucous membranes of the digestive tract. It is parenteral use that gives high bioavailability and provides a bactericidal effect.

A number of drugs can be used through the digestive tract. These drugs are available in capsule, tablet, and powder form for suspension. Among them are Cephalexin, Zinnat, Cefixim and others.

Receiving mechanism

7-ACK is produced from cephalosporin C using biotechnology. The acylation reaction (acyl substitution) at the amino group is used.

With a similar structure to penicillins, cephalosporins managed to create protection against the action of penicillinase, an enzyme that destroys beta-lactamase.

Specifications

Cephalosporins are widely used in the treatment of infectious infections of different localization due to:

• pronounced bactericidal effect;
• the minimum number of negative effects;
• easy portability.

Medicines are used in children with early age suitable for elderly patients.

Pharmacological properties

Cephalosporins block the synthesis of peptidoglycan, which forms the basis of the protective membrane of bacteria. Destroying the cell membrane, they lead to the death of micro-pathogens. The action of drugs in this group is possible only on developing organisms - during division and growth. The cells of the flora at rest do not react to the antibiotic.

With any method of administration, the active substance penetrates into all environments of the body in an amount sufficient for a therapeutic effect.

The substance is fixed in the lungs, synovial fluid, cerebrospinal fluid, pelvic organs, saliva and others.

Flora sensitivity to drugs

The creation of new generations of cephalosporins solved the main problem - ensuring action on new groups of micro-pathogens, that is, expanding the scope of use and effectiveness of drugs.

5 - high activity, 0 - inactive.

At the same time, the creation of new drugs led to the adaptation of the pathogenic flora to their action and the formation of resistance to drug effects in microbes.

In many pathogens, the permeability of the channels in the membranes decreases, due to this, the antibiotic cannot penetrate the bacteria, which significantly weakens its effectiveness.

Mutation selection

Microorganisms are able to quickly mutate, adjust their structures to changing conditions and remain viable.

Resistance against cephalosporins, in most cases, develops in a delayed manner, as for some antibiotics (aminoglycosides), or more rapidly.

Transmissibility

The pathogenic flora, in response to the action of antibiotics, is capable of producing beta-lactamases and releasing them into the intercellular space. Enzymes deactivate the drug. Cephalosporins are more resistant to β-lactamases than penicillins, but they also lose some of their properties.

Resistance

So far, it has not been possible to suppress the resistance of some groups of the bacterial flora. Even representatives of 4-5 generations are powerless against them:

• enterococci;
• klebsiella;
• shigella;
• Listeria monocytogenes;
• coli - intestinal and tuberculous;
• pseudomonad.

Meningococci and salmonella also show insignificant resistance.

1st generation cephalosporins

The first obtained antibiotic cephalothin has been known since 1964. Molds became the source for its manufacture; the manufacture of drugs is carried out by a semi-synthetic method with the use of acylation.

Zolin

The active ingredient is called cefazolin and is used in the formulation as a sodium salt. It has only forms for intramuscular and intravenous administration. It is a powder in a dilution bottle.

There are no oral forms due to poor absorption in the gastrointestinal tract. The dosage is 250 milligrams. Into a vein, a jet or drip is injected. Manufacturer - India.

Natsef

The drug is used parenterally. Has dosages of 500 and 1000 milligrams. Suitable for drip and jet injection.

White or light-colored powder in vials. Diluted with isotonic solution, lidocaine. It is used to treat children (except newborns).

ABOLmed, Russia.

Used parenterally for intramuscular administration requires deep insertion into the muscle. Treatment of children and elderly patients is allowed.

Available dosages are 0.5, 1 gram. The owner of the license is Austria.

This drug is used to treat many pathologies of the ENT organs - sinusitis of different localization, otitis media, tonsillitis.

It has oral forms - tablets (0.25 grams), capsules - 500 and 250 milligrams. The baby form is granules for dilution and suspension. Treatment of children under one year old is possible.

Produced in Russia, countries the former USSR and Serbia.

It is prepared in the form of a powder for dissolution and parenteral use. Produced by KRKA in Slovenia. The dosage is 1 gram. Not applicable for up to a month.

2nd generation cephalosporins

Medicines of this group of cephalosporins remain in demand. Significantly expanded the capabilities of the first generation, have a wider range of activities. Staphylococcus infection is well eliminated.

The Cypriot drug contains cefuroxime. The medicine is available in several dosages, tablets are not produced.

Cefoxitin sodium salt in vials (0.5 and 1 gram each). For injection only - intravenous and intramuscular. ABOLmed LLC, Russia.

The medicine is produced by companies in Russia and Italy for infusion use. Contains cefuroxime in an amount of 250-750 milligrams.

Cefuroxime axetil is in the form of tablets in dosages of 125 and 250 and granules for preparing a suspension for children. Use from 3 months is possible. The owner of the license is Glaxo Operations UK Limited (Great Britain).

In Italy, the preparation with sodium cefuroxime in the amount of 750 milligrams is produced under the trade name Super. For intramuscular and intravenous administration.

This type of cephalosporin cefaclor monohydrate has oral forms - capsules (0.5) and granules for suspension in two dosages, including for children. Country of origin - Germany.

Naphat cefamandola is a component of a drug for injection use produced by ABOLmed LLC, Russia. In vials of 10 milliliters 0.5 or 1 gram of 2nd generation cephalosporin.

The medicine is cefuroxime sodium. For infusion use only. Produced by ABOLmed LLC in three dosages.

Dosages - 250, 750, 1500 milligrams. It is located in vials, in which a solution for administration is obtained. The drug under this name is produced by several enterprises in Russia, Germany and Austria.

The drug Cefuroxime also has a tablet form.

Manufacturer - JSC Sintez, Russia. The active ingredient is cefuroxime. Release forms:

• bottle 10 milliliters - 750 milligrams;
• bottle of 20 milliliters - 1.5 grams.

Used for infusion.

3rd generation cephalosporins

Better penetrate cell walls, more resistant to enzymes produced by bacteria. Active against Streptococcus.

The medicine is a powder for reconstitution in vials, ceftriaxone sodium 1 gram. Hemofarm A.D., Serbia.

The parenteral agent contains ceftriaxone and sodium sulbactam. Country of origin - India.

Ceftazidime in vials, which are accompanied by a solvent (water) in ampoules. ABOLmed LLC, Russia. Use intramuscularly, intravenously.

The registration certificate for the drug belongs to the PFIZER company. The medicine contains ceftazidime and a beta-lactamase inhibitor (avibactam). It is used for infusion.

India produces cefixime for suspension dilution under the name Ixim Lupine. Conveniently dosed for adults and children. It is widely used in ENT practice.

India manufactures a medicine called Kefotex, which contains cefotaxime salt. Parenteral only.

Kefsepim

The best method of administration is by drip. It is also used as a jet into a vein and intramuscularly. There are no oral forms. India.

Manufactured in Great Britain. Packaged in vials for solution for injection.

Contains ceftriaxone. Dosages - 0.25, 1, 2 grams. Slovenia.

In Iran, ceftazidime is the active ingredient in Lorazidim. It is used intravenously and intramuscularly.

Indian preparation with ceftriaxone for injection.

Sulmagraph

Cefoperazone in combination with sulbactam. China.

Cefoperazone with sulbactam 1.5 grams each. China.

Sulperazon

Sulbactam + cefoperazone. Turkey.

Sulperacef

Cefoperazone and sulbactam. Has several dosages. ABOLmed, Russia.

Sulcef

Cefoperazone + Sulbactam - this is the composition of the medicine from Medokemi LTD from Cyprus. The antibiotic is used parenterally.

Suprax

Cefixime in oral form - capsules, granules for suspension. Jordan.

Talcef

Cefotaxime for parenteral administration. India.

Indian medicine with ceftriaxone.

Cebanex

Cefoperazone sodium is combined in the drug with sulbactam (1 + 1 gram). The Indian drug is used intramuscularly and intravenously.

Zedex

Ceftibuten in capsules and for diluting the suspension. Italy, Russia.

Ceperon J

Cefoperazone, India.

Cetax

Cefotaxime. India.

Cefabol

Cefotaxime, ABOLmed, Russia.

Cefaxone

Ceftriaxone, India.

Cefotaxime, India.

Cefbactam

Cefoperazone + Sulbactam in equal amounts (0.25, 0.5, 1 gram), SPC ELFA, Russia.

Cefzoxime J

Ceftizoxime, India.

Cefixime

A popular antibiotic for oral administration is tablets (200, 400 milligrams of cefixime), a suspension of 5 milliliters contains 100 milligrams of cefixime. India, Iran.

Cephobid

Cefoperazone, Pfizer, USA, Italy.

Cefoperazone, ABOLmed.

Cefoperazone - Vial

Cefoperazone, VIAL LLC, Russia.

Cefoperazone and Sulbactam Jodas

Indian medicine contains two substances that complement each other's action. It is produced in bottles containing an equal amount of substances (1 gram each).

Cefosin

Manufacturer - JSC Sintez. Contains sodium salt cefotaxime in an amount of 0.5 to 2 grams. Does not have oral forms.

Cefpar SV

Produced by OOO RUSYUROPHARM. As part of cefoperazone and sulbactam in an amount of 500 or 1000 milligrams. Used parenterally.

Cefroxime J

Cefuroxime, India.

Tsefson

Ceftriaxone, Turkey.

Ceftriabol

Ceftriaxone, ABOLmed.

Ceftriaxone, India.

Ceftrifin

Ceftriaxone. India.

Note: most of the drugs in this group of antibiotics are produced for parenteral use and do not have oral forms.

4th generation cephalosporins

Eliminate infection with gram-negative microorganisms more effectively. Resistant to chromosomal beta-lactamases.

Cefepime with L-Arginine. Bnfkbz.

Maxiceph

Cefepim. ABOLmed, Russia.

Cefaktiv

Cefpir with sodium carbonate. JSC Pharmasintez.

Cefepim. CJSC LEKKO, Russia.

Cefpirome

Cefpirome sulfate is manufactured by NoroBio Pharmaceutical (China). Has only parenteral form.

It is produced in the form of a powder, from which a solution for injection is prepared (0.5-1 grams). Applied to children from 2 months. Produced in India.

5th generation cephalosporins

Medicines of this group, along with all the best properties of cephalosporins, are active against Staphylococcus aureus (Staphylococcus aureus), which does not respond well to all antibiotics. Active against both types of beta-lactamases.

Zinforo

Ceftaroline fosamil. United Kingdom.

Ceftobiprol. Belgium.

Ceftobiprol

Active ingredient of the 5th generation, contained in Zefter.

Ceftaroline

Ceftaroline fosamil is an active substance that is part of Zinforo.

Ceftolosan

Ceftolosan / tazobactam. The drug with a combination of these substances is under the trade name Zerbaxa. Approved for use in 2018.

Indications for use

Since most drugs are administered parenterally, they are most often used in a hospital setting. Features of application by generation:

• During surgical treatment - for prophylaxis and after completion to avoid infection. For the treatment of skin lesions.
• Pneumonia. Often used outside the hospital. Pathology of ENT organs. Skin infections. In case of infection of the genitourinary organs in combination with other antibiotics. Joint and bone infections.
• Meningitis, gonorrhea, lesions nervous system, intestinal infections, inflammation of the lower respiratory and biliary tract. Salmonellosis.
• Pneumonia. Pelvic infections. Sepsis. Inflammation of the skin, bone structures, joints. Complicated pathologies of the urinary tract with infection by the bacterial community.
• Eliminate Staphylococcus aureus infection. Helps fight infections resistant to previous generations of cephalosporins and penicillins. Diabetic foot.

The sphere of activity of cephalosporins increases with the transition to more modern drugs... New generations of drugs are created taking into account the development of resistance and the ability of flora to permanent mutations.

Instructions for use and dosages

Most cephalosporins are used only parenterally.

When treating children

Dosages of drugs are selected by body weight. For each drug, for intramuscular and intravenous administration, there are dosing rules, in particular:

• Ceftriaxone - 40-100 milligrams per kilogram of body weight, 2-3 times;
• Cefazolin - 50-100 milligrams per kilogram, 2-3 times.

Oral forms are also dosed by body weight, for example:

• Cefaclor - 20-40 milligrams, divided into 3 doses;
• Cephalexin - 45 milligrams per kilogram, 3 times.

Most of the drugs are not used earlier than a month, for some there are other age restrictions (2-6 months). The course is 5-10 days.

Treatment for adults

Adult parenteral use of certain cephalosporins:

• Cefotaxime - 3-8 grams per day for 3 injections;
• Ceftazidime - 3-6 grams, 2 times;
• Cefoperazone + Sulbactam - 4-8 grams, 2 administrations.

Oral forms:

• Cefaclor - 0.25-0.5 grams each, three times;
• Cefuroxime - 0.25-0.5 grams, three times.

Take medicine with plenty of water.

For your information: because of the painfulness of administration, cephalosporins are often diluted with lidocaine or novocaine.

Pregnancy and lactation

Due to their low toxicity and lack of effect on the fetus, cephalosporins are used to treat pregnant women; drugs of 2-4 generations are usually chosen. During therapy breast-feeding should be interrupted.

Dosages are selected based on the condition. The lowest effective dose is used.

For patients with renal impairment

In renal failure, the number of applications can be reduced due to slower withdrawal. Control of creatinine clearance is carried out.

Contraindications

Fixed allergic manifestations to cephalosporins.

In case of overdose, the following deviations may develop:

• the most common are dyspeptic disorders, less often colitis;
• anemia;
• accession of other infections - candidiasis;
• changes in blood composition;
• skin manifestations.

In severe cases, anaphylactic shock is possible.

Undesirable consequences of using the drug

Despite the safety of cephalosporins, the body's reactions to its intake are possible:

• headache;
• dyspeptic manifestations;
• allergy;
• heart rhythm disturbances;
• dysfunction of the kidneys;
• pathology of hematopoiesis, violations of the composition of the blood.

The attachment of other infections is possible - fungal, viral.

What you need to pay attention to

Treatment with cephalosporins requires strict adherence to dosages and the prescribed time of use. If you skip it, you cannot double the amount of the drug. Even with obvious improvement, the course needs to be completed.

The suspension should not be stored longer than the prescribed period of use.

For digestive upsets, oral medications can be taken with meals. In most cases, it is allowed to take it regardless of food.

Interaction with other medications

The following types of mutual influence with cephalosporins have been identified:

1. Cross-allergy with the use of penicillins.
2. Decreased absorption during treatment with antacids. When taking oral forms - an interval of at least 2 hours.
3. Aminoglycosides and loop diuretics become more toxic. Control for renal dysfunction.
4. Cefoperazone preparations should not be taken with alcohol.

Joint reception with anticoagulants and antiplatelet agents can lead to bleeding.

Storage conditions and terms

List B. Store in a cool place (2-8 °, no more than 25 °). The drugs, for the most part, have a shelf life of 2-3 years.

Vacation conditions and cost

On prescription.

The cost of drugs depends on the manufacturer:

• Zinforo 600 milligrams, 20 vials - 19,000 rubles;
• Anaerocef - about 200 rubles;
• Vice-President - 130 rubles.

Domestic drugs are quite affordable.

Substitute antibiotics

Allergy to cephalosporins requires replacement of drugs with antibiotics from other groups. Among possible options- aminoglycosides, fluoroquinolones and macrolides. Depending on the localization of the inflammation, the specialized specialist selects the drug that is most suitable for the treatment of infection of this organ and the characteristics of the bacterial flora.

It is often suggested to use foreign-made cephalosporins of 4-5 generations, since their quality and efficiency are higher.

The drugs of the penicillin group are usually not substituted for drugs, since cases of cross-allergy are often observed.

Treatment with cephalosporins helps suppress bacterial infections different localization. The drugs differ from other antibiotics by good tolerance, a weak negative effect on the body. Medicines in this group have good responses from doctors and patients.

The absorption of cefaclor, cefixime and ceftibuten may be somewhat slowed down by the presence of food. Cefuroxime axetil is hydrolyzed during absorption to release the active cefuroxime, with food contributing to the process.

Parenteral cephalosporins are well absorbed when injected intramuscularly.

• Distribution

  Cephalosporins are distributed in many tissues, organs (except prostate) and secrets. High concentrations are noted in the lungs, kidneys, liver, muscles, skin, soft tissues, bones, synovial, pericardial, pleural and peritoneal fluids. In bile the most high levels create ceftriaxone and cefoperazone. Cephalosporins (mostly cefuroxime and ceftazidime) penetrate well into intraocular fluid but do not create therapeutic levels in rear camera eyes.

  The ability to overcome the blood-brain barrier and create therapeutic concentrations in the cerebrospinal fluid is most pronounced in the third generation cephalosporins - cefotaxime, ceftriaxone and ceftazidime, and in the fourth generation - cefepime.

  Second-generation cephalosporins (cefuroxime) moderately penetrate the blood-brain barrier only with inflammation of the meninges.

  Generation I cephalosporins poorly cross the blood-brain barrier.

• Metabolism

  Most cephalosporins are practically not metabolized. An exception is cefotaxime, which is biotransformed to form an active metabolite.

• Withdrawal

  The drugs are excreted mainly by the kidneys, while very high concentrations are created in the urine.

  Ceftriaxone and cefoperazone have a dual route of excretion - by the kidneys and the liver. The half-life of most cephalosporins varies within 1-2 hours. Cefixime, ceftibuten (3-4 hours) and ceftriaxone (up to 8.5 hours) have a longer half-life, which makes it possible to prescribe them once a day. In renal failure, cephalosporin dosing regimens (except for ceftriaxone and cefoperazone) require correction.

  • Generation I cephalosporins. All drugs in this group have a similar half-life (40-60 minutes), with the exception of cefazolin (about 2 hours), and are prescribed with an interval of 6 hours (cefazolin - 8 hours), are excreted mainly in the urine, penetrate well into tissues, but pass poorly through the blood-brain barrier (therefore, not used to treat meningitis).
  • Generation II cephalosporins. Drugs in this group have a similar half-life (50 - 80 minutes), except for cefotetan (about 4 hours), are excreted mainly by the kidneys, and are not metabolized in the body (except for cefoxitin). Cefuroxime axetil has a longer half-life and requires less frequent dosing (cefuroxime axetil - every 12 hours, cefaclor - every 8 hours), and therefore is currently considered the optimal drug among oral cephalosporins of the second generation.
  • Cephalosporins of the third generation have a similar half-life (1.2 - 2 hours), with the exception of ceftriaxone (about 8 hours), are excreted mainly by the kidneys (except: cefoperazone, which is excreted in significant quantities in the bile). III-generation drugs penetrate the blood-brain barrier and, as alternative agents, can be used to treat infections of the central nervous system caused by gram-negative bacteria.
  • Generation IV cephalosporins. Due to poor absorption in gastrointestinal tract 4th generation cephalosporins are used only parenterally. Their bioavailability after intramuscular administration is 90%, antibiotics are retained in therapeutic concentrations in the blood serum for 12 hours, which allows them to be administered 2 times a day.
  • Generation V cephalosporins. The binding of ceftobiprol to plasma proteins is 16% and does not depend on its concentration. Biotransformation from ceftobiprol medocaryl, which is a prodrug, into the active substance ceftobiprol occurs rapidly and is catalyzed by plasma esterases. Ceftobiprol undergoes minimal metabolism to a non-cyclic metabolite that is microbiologically inactive. The concentration of this metabolite is lower than the concentration of ceftobiprol itself. The drug is excreted mainly unchanged by renal excretion.

• Tab. Pharmacokinetics of cephalosporins

  A drug	Medium therapeutic doses	Half-life, h	Concentration in cerebrospinal fluid, mg / l	Plasma protein binding, %	Elimination route
  1st generation
  cefazolin	1 g every 8 hours	1,8		80	Kidney
  cephalothin	1-2 g every 4-6 hours	0,6		71	Kidney
  cephalexin	0.5 -1g every 6 hours	0,9		10	Kidney
  2nd generation
  cefamandole	1-2 g every 4-6 hours	0,8		75	Kidney
  cefaclor	0.25-0.5 g q 8 h	0,8		25	Kidney
  cefuroxime axetil	0.25-05 g q 12 h	1,3		35	Kidney
  III generation
  cefotaxime	2 g every 6-8 hours	1,0	5,6-44	35	Kidney
  ceftazidime	2 g every 8 hours	1,8	0,5-30	17	Kidney
  ceftriaxone	1-2 g every 12 hours	8,0	1,2-39	83-96	Kidneys-50% Bile-40%
  IV generation
  cefepime	0.5-1 g every 12 hours	2 hours	3,3-5,7	19%	Kidney

In the series from I to IV generations of cephalosporins, the spectrum of action expands and the level of antimicrobial activity against gram-negative bacteria increases, with a slight decrease in activity against gram-positive microorganisms.

Tab. Activity of cephalosporins against microorganisms and resistance to β-lactamases

Generation UPS	Sensitivity of microorganisms		Β-lactamase resistance
	gram-positive	gram negative	staphylococci	gram-positive bacteria
I	++++	+	++	-
II	+++	++	++	+/-
III	+	+++	+	+
IV	++	++++	++	++




Common to all cephalosporins is the lack of significant activity against enterococci, methicillin-resistant strains of S. aureus (MRSA) and L. monocytogenes. Coagulase-negative staphylococci (CNS) are less sensitive to cephalosporins than S. aureus.

• Generation I cephalosporins
  Tab. Antimicrobial activity of 1st generation cephalosporins
  

  	cephalothin	cefazolin	cefapirin	cephalexin
  St. aureus	+++	+++	+++	+++
  Streptococci	+++	+++	+++	+++
  Enterococci	-	-	-	-
  Haemophilus influenzae	-	-	-	-
  E.coli	++	+++	++	+++
  Klebsiella ssp.	++	+++	++	+++
  Serratia marcescens	-	-	-	-
  Proteus mirabilis	++	++	++	+++
  Pseudomonas aeruginosa	-	-	-	-
  Anaerobes
  Clostridii	++	++	++	-
  Bacteroides fragilis	-	-	-	-

  
  Note:
  +++ - very good
  ++ - good
  + - weak
  - - no action

  The spectrum of action of oral and parenteral 1st generation cephalosporins is the same, but the activity is slightly higher in parenteral medicines, among which cefazolin is the most active.

  Generation I cephalosporins are active mainly against gram-positive microorganisms. Antibiotics are active against Streptococcus spp. (S.pyogenes, S.pneumoniae) and methicillin-susceptible Staphylococcus spp. In terms of the level of antipneumococcal activity, I generation cephalosporins are inferior to aminopenicillins and most of the later cephalosporins.

  Certain strains of staphylococci, which are hyperproducers of β-lactamases, may exhibit moderate resistance to 1st generation cephalosporins.

  Inactive against enterococci and listeria.

  Generation I cephalosporins have a narrow spectrum of action and a low level of activity against gram-negative bacteria. Some gram-negative bacteria (E. coli, P. mirabilis) are naturally sensitive to 1st generation cephalosporins, but the acquired resistance to them is high. The drugs are effective against Neisseria spp., But their clinical relevance is limited. Activity against H. influenzae and M. catarrhalis is clinically insignificant. Natural activity against M. catarrhalis is quite high, however, they are sensitive to hydrolysis by β-lactamases, which are produced by almost 100% of the strains.

  Among the representatives of the Enterobacteriaceae family, E. coli, Shigella spp., Salmonella spp. Are susceptible. and P. mirabilis, while the activity against Salmonella and Shigella has no clinical significance. Among the strains of E. coli and P. mirabilis, causing community-acquired and especially nosocomial infections, acquired resistance is widespread due to the production of β-lactamases of a wide and extended spectrum of action.

  Other enterobacteriaceae, Pseudomonas spp. and non-fermenting bacteria are resistant.

  A number of anaerobes are sensitive; B.fragilis and related microorganisms are resistant.

• Generation II cephalosporins
  Tab. Antimicrobial activity of II generation cephalosporins

  	cefamandole	ceforanide	cefonicide	cefurok- Sim	cefock- sitin	cefotetam	cefme- tazol	cefaclor	cefuroxime axetil
  Gram-positive microorganisms
  St. aureus	+++	+++	+++	++	++	++	++	++	++
  Streptococci	+++	+++	+++	+++	+++	+++	+++	+++	+++
  Enterococci	-	-	-	-	-	-	-	-	-
  Gram-negative microorganisms
  Haemophilus influenzae	+	+	++	+++	+++	+++	+++	+++	+++
  E.coli	+++	+++	+++	+++	+++	+++	+++	+++	+++
  Klebsiella ssp.	+++	+++	+++	+++	+++	+++	+++	+++	+++
  Serratia marcescens	+	+	+	+	+	+	+	-	-
  Proteus mirabilis	+++	+++	+++	+++	+++	+++	+++	+++	+++
  Pseudomonas aeruginosa	-	-	-	-	-	-	-	-	-
  Anaerobes
  Clostridii	++	++	++	++	++	++	++	-	-
  Bacteroides fragilis	+	+	+	+	++	++	++	-	-

  
  Note:
  +++ - very good
  ++ - good
  + - weak
  - - no action

  There are certain differences between the two main representatives of this generation - cefuroxime and cefaclor. With a similar antimicrobial spectrum, cefuroxime is more active against Streptococcus spp. and Staphylococcus spp. Both drugs are inactive against enterococci, methicillin-resistant strains of S. aureus and listeria.

  Pneumococci show cross-resistance to second-generation cephalosporins and penicillins.

  The spectrum of action of second generation cephalosporins against gram-negative microorganisms is wider than that of representatives of the first generation. Both drugs are active against Neisseria spp., But only the activity of cefuroxime against gonococci is of clinical significance. Cefuroxime is more active against M. catarrhalis and Haemophilus spp., Since it is resistant to hydrolysis by their β-lactamases, while cefaclor is partially destroyed by these enzymes.

  E. coli, Shigella spp., Salmonella spp., P.mirabilis, Klebsiella spp., P.vulgaris, C.diversus are susceptible from the Enterobacteriaceae family. When the listed microorganisms produce broad-spectrum β-lactamases, they retain sensitivity to cefuroxime. Cefuroxime and cefaclor are degraded by extended-spectrum β-lactamases.

  Some strains of Enterobacter spp., C. freundii, Serratia spp., M. morganii, P. stuartii, P. rettgeri may show moderate sensitivity to cefuroxime in vitro, but clinical application this cephalosporin in infections caused by the listed microorganisms is inappropriate.

  Pseudomonas, other non-fermenting microorganisms, anaerobes of the B.fragilis group are resistant to II generation cephalosporins.

• Generation III cephalosporins
  Tab. Antimicrobial activity of 3rd generation cephalosporins
  

  	cefotaxime	ceftriaxone	cefoperazone	ceftazidime
  Gram-positive microorganisms
  St. aureus	++	++	+	+
  Streptococci	+++	+++	++	+
  Enterococci	-	-	-	-
  Gram-negative microorganisms
  Haemophilus influenzae	+++	+++	+++	+++
  E.coli	+++	+++	+++	+++
  Klebsiella ssp.	+++	+++	+++	+++
  Serratia marcescens	+++	+++	+++	+++
  Proteus mirabilis	+++	+++	+++	+++
  Pseudomonas aeruginosa	-	-	+	+++
  Anaerobes
  Clostridii	+	+	+	+
  Bacteroides fragilis	-	-	-	-

  
  Note:
  +++ - very good
  ++ - good
  + - weak
  - no action

  The basic third generation cephalosporins are cefotaxime and ceftriaxone, which are almost identical in their antimicrobial properties: they are highly active against Streptococcus spp., While a significant part of penicillin-resistant pneumococci and green streptococci remain sensitive to these drugs. Cefotaxime and ceftriaxone are active against S. aureus, except for methicillin-resistant strains of S. aureus, to a somewhat lesser extent against coagulase-negative staphylococci. Corinebacteria (other than C. jeikeium) are generally susceptible.

  Enterococci, methicillin-resistant strains of S. aureus, L. monocytogenes, B. antracis and B. cereus are resistant.

  Cefotaxime and ceftriaxone are highly active against meningococci, gonococci, H. influenzae and M. catarrhalis, including against strains with reduced sensitivity to penicillin, regardless of the resistance mechanism.

  Cefotaxime and ceftriaxone have high natural activity against almost all members of the Enterobacteriaceae family, including microorganisms producing broad-spectrum β-lactamases. Resistance of E. coli and Klebsiella spp. most often due to the production of extended-spectrum β-lactamases. Resistance of Enterobacter spp., C.freundii, Serratia spp., M. morganii, P.stuartii, P.rettgeri is usually associated with overproduction of chromosomal class C β-lactamases.

  Cefotaxime and ceftriaxone are sometimes active in vitro against certain strains of P. aeruginosa, other non-fermenting microorganisms, and B.fragilis, but they should never be used for associated infections.

  Ceftazidime and cefoperazone are similar in their main antimicrobial properties to cefotaxime and ceftriaxone. Their distinctive characteristics include the following:

  • Expressed (especially in ceftazidime) activity against P. aeruginosa and other non-fermenting microorganisms.
  • Significantly less activity against streptococci, especially S. pneumoniae.
  • High sensitivity to hydrolysis by extended spectrum β-lactamases.

  Cefixime and ceftibuten differ from cefotaxime and ceftriaxone in the following ways:

  • Lack of significant activity against Staphylococcus spp.
  • Ceftibuten is inactive against pneumococci and green streptococci.
  • Both drugs are inactive or inactive against Enterobacter spp., C. freundii, Serratia spp., M. morganii, P. stuartii, P. rettgeri.
  • Inhibitor-protected cephalosporins

    The only representative of this group of β-lactams is cefoperazone / sulbactam. Spectrum of action in comparison with cefoperazone combination drug expanded due to anaerobic microorganisms, the drug is also active against most strains of enterobacteriaceae producing β-lactamases of wide and extended spectra. The drug is highly active against Acinetobacter spp. due to the antibacterial activity of sulbactam.

• Generation IV cephalosporins

  The representative of the IV generation cephalosporins - cefepime in many respects is close to the III generation cephalosporins. Due to the peculiarities of the chemical structure, it has an increased ability to penetrate the outer membrane of gram-negative bacteria and a relative resistance to hydrolysis by chromosomal β-lactamases of class C. Therefore, along with the properties characteristic of basic III generation cephalosporins (cefotaxime, ceftriaxone), cefepime exhibits the following features:

  • High activity against P. aeruginosa and non-fermenting microorganisms.
  • Activity against microorganisms - hyperproducers of chromosomal β-lactamases of class C, such as: Enterobacter spp., C. freundii, Serratia spp., M. morganii, P. stuartii, P. rettgeri.
  • Higher resistance to hydrolysis by extended-spectrum β-lactamases (however, the clinical significance of this fact is completely unclear).

Indications for the appointment of cephalosporin antibiotics are determined, first of all, by their belonging to one generation or another.

• Generation I cephalosporins

  The main indications for the administration of 1st generation oral cephalosporins are:

  • Streptococcal or staphylococcal infections: these drugs are an alternative to natural penicillins and aminopenicillins in the treatment of infections of the upper respiratory tract, ENT organs,
  • The main remedies for the treatment of uncomplicated infections of the skin and soft tissues of the lungs and medium severity on an outpatient basis.
  • Acute purulent arthritis, the etiology of which is dominated by staphylococci.

  The injectable drug cefazolin is currently used mainly for preoperative prophylaxis in surgery, as well as for the treatment of skin and soft tissue infections.

  In the treatment of nosocomial infections (urinary tract infections, sepsis and pneumonia), I generation cephalosporins should only be used in combination with other antibacterial agents active against gram-negative microorganisms (aminoglycosides, fluoroquinolones).

• Generation II cephalosporins
  • Treatment of community-acquired pneumonia due to the pronounced activity of II generation drugs against H. influenzae and M. catarrhalis, including β-lactamase-producing strains, as well as Str. Pneumoniae. In the treatment of hospital pneumonia, II generation cephalosporins are used in combination with aminoglycosides.
  • Treatment of infections of the respiratory tract and ENT organs. Cefuroxime axetil and cefaclor are first-line agents in the treatment of various respiratory tract infections in outpatient practice: sinusitis, otitis media, exacerbation of chronic bronchitis. As an alternative agent, second-generation cephalosporins are used to treat tonsillitis / pharyngitis.
  • They are prescribed for infectious diseases of the skin and soft tissues.
  • They are used for acute and chronic uncomplicated urinary tract infections.
  • Cefuroxime is effective in the treatment of meningitis due to H. influenzae, N. meningitidis and Str. pneumoniae.
  • The injectable form of cefuroxime is used for preoperative prophylaxis in surgery.
  • Generation II cephalosporins (cefuroxime and cefamandol) are used to treat severe infections caused by H. influenzae - epiglottitis, sepsis after splenectomy, including in newborns and children of the first months (pneumonia, acute hematogenous osteomyelitis, arthritis).
  • Cephalosporins of this group with anti-anaerobic activity are used to treat mixed intra-abdominal and gynecological infections.
  • Cefuroxime can be used as the drug of choice for the prevention of postoperative infections in abdominal, cardiovascular and thoracic surgery, as well as in traumatology and orthopedics, and in most operations, a single dose of the drug is sufficient (1.5 g 30 minutes before anesthesia).
• Generation III cephalosporins
  • This group of drugs can be used in cases of severe community-acquired infection (with a high degree of probability associated with E. coli, Proteus mirabilis, K. pneumoniae, etc.).
  • Ceftriaxone and cefotaxime are effective in the treatment of nosocomial infections caused by microorganisms sensitive to them: pneumonia, wound infection, complicated urinary tract infections, severe infections of the skin, soft tissues, bones, joints. When conducting empirical therapy for severe nosocomial infection, the combined administration of cephalosporins and aminoglycosides is recommended.
  • Ceftriaxone and cefotaxime are the drugs of choice for the treatment of H. influenzae meningitis, Str. pneumoniae, N. Meningitidis, as well as meningitis caused by other gram-negative rods, with the exception of Ps. aeruginosa (drug of choice - ceftazidime) and Enterobacter spp. (the drug of choice is Biseptol).
  • Ceftazidime is the drug of choice for infections caused by Pseudomonas aeruginosa, as well as empiric therapy in situations with a high risk of Pseudomonas aeruginosa infection (in intensive care, oncology, hematological patients and patients with cystic fibrosis).
  • Generation III cephalosporins are also used in the treatment of a number of specific infectious diseases... A single administration of ceftriaxone is a highly effective method of treating chancroid.
  • Ceftriaxone, due to its high bactericidal activity against members of the Streptococcus family (excluding enterococci), is used as an alternative agent in the treatment of streptococcal endocarditis.
  • III generation cephalosporins are used to treat various severe infections, mainly hospital-acquired, caused by gram-negative microorganisms, including multidrug-resistant ones: pneumonia, pyelonephritis, osteomyelitis, infection abdominal cavity and small pelvis, wound and burn infection, sepsis.
  • The effectiveness of some drugs of this group (ceftazidime, ceftriaxone) has been shown in patients with immunodeficiency, agranulocytosis, including monotherapy.
  • Cefotaxime and ceftriaxone are first-line drugs in pediatric practice in the treatment of life-threatening infections in newborns caused by Streptococcus spp., S. pneumoniae, H. influenzae, Enterobacteriaceae (pneumonia, sepsis, meningitis).
  • Cefotaxime and ceftriaxone are used as alternatives for infections in adults with penicillin-resistant S. pneumoniae and N. gonorrhoeae.
• Generation IV cephalosporins

  Drugs of this generation are prescribed for the treatment of severe, mainly nosocomial, infections caused by multidrug-resistant microflora. This generation of cephalosporins is used in the following cases:

  • For respiratory tract infections: pneumonia, lung abscess, pleural empyema.
  • For complicated urinary tract infections.
  INN Lecform LS F (inside),% T 1/2 , h * Dosage regimen Features of drugs cephalexinTab. 0.25 g; 0.5 g; 1.0 g
  Caps. 0.25 g; 0.5 g
  Gran. d / suspension 0.125 g / 5 ml; 0.25 g / 5 ml in a bottle. 60 ml each
  Por. d / r-ra d / oral administration 0.125 g / 5 ml; 0.25 g / 5 ml; 0.5 g / 5 ml in a bottle. 95 1 Adults: 0.5-1.0 g every 6 hours;
  with streptococcal tonsillopharyngitis - 0.5 g every 12 hours for 10 days
  Children: 45 mg / kg / day in 3 divided doses;
  with streptococcal tonsillopharyngitis - 12.5-25 mg / kg every 12 hours for 10 daysGeneration I cephalosporin.
  Indications: tonsillopharyngitis, mild infections of the skin, soft tissues, bones and joints. cefuroxime axetilGran. d / suspension 0.125 g / 5 ml; 0.25 g / 5 ml in a bottle. or sachet
  Tab. 0.125 g; 0.25 g; 0.5 g50-70 (during meals)
  37 (fasting) 1,2-1,5 Adults: 0.25-0.5 g every 12 hours with meals;
  with streptococcal tonsillopharyngitis - 0.25 g every 12 hours with meals for 10 days
  Children: 30 mg / kg / day in 2 divided doses with meals;
  with otitis media - 40 mg / kg / day in 2 divided doses with meals;
  with streptococcal tonsillopharyngitis - 20 mg / kg / day in 2 divided doses with meals for 10 days
  Food increases bioavailability.
  Indications: infections of the respiratory tract, urinary tract, skin and soft tissues.
  Can be used for stepwise therapy after parenteral cefuroxime. cefaclorCaps. 0.25 g; 0.5 g
  Por. d / suspension 0.125 g / 5 ml; 0.25 g / 5 ml in a bottle.
  Susp. for oral administration 0.125 g / 5 ml in a bottle.
  Gran. 0.125 g; 0.25 g; 0.375 g in a bag.
  Tab. 0.5 g
  Tab. reg. release 0.375 g; 0.5 g; 0.75 g 95 0,5-1 Adults: 0.25-0.5 g every 8 hours (for streptococcal tonsillopharyngitis for 10 days)
  Children: 20-40 mg / kg / day
  2-3 doses (with streptococcal tonsillopharyngitis within 10 days)Generation II cephalosporin.
  Differences from cefuroxime axetil:
  - less resistant to β-lactamases;
  - less active against pneumococci,
  H.influenzae and
  M. catarrhalis cefiximeCaps. 0.1 g; 0.2 g; 0.4 g Suspension. for oral administration 0.1 g / 5 ml
  Por. d / suspension 0.1 g / 5 ml 40-50 3-4 Adults: 0.4 g / day
  1-2 receptions
  Children over 6 months: 8 mg / kg / day in 1-2 dosesGeneration III cephalosporin.
  Extended spectrum of activity against gram-negative bacteria.
  Indications: infections of the respiratory tract, urinary tract.
  Can be used for stepwise therapy after parenteral cephalosporins of the third generation.

  INN	Lecform LS	T ½, h *	Dosage regimen	Features of drugs
  cefazolin	Por. d / in. 0.125 g; 0.25 g; 0.5 g; 1.0 g; 2.0 g; 10.0 g per bottle.	1,5-2	I / v and i / m Adults: 2.0-6.0 g / day in 2-3 injections; for prophylaxis - 1.0-2.0 g 0.5-1 hours before the operation (if the operation is more than 3 hours: again after 4 hours) Children: 50-100 mg / kg / day in 2-3 introductions	Generation I cephalosporin. Primary activity against gram-positive cocci. Indications: perioperative prophylaxis in surgery, outpatient skin and soft tissue infections.
  cefuroxime	Por. d / in. 0.25 g; 0.75 g; 1.5 g per bottle.	1,5	I / v and i / m Adults: 2.25-4.5 g / day in 3 infusions; for prophylaxis - 1.5 g 0.5-1 hours before the operation (if the operation is more than 3 hours: again after 4 hours) Children: 50-100 mg / kg / day in 3-4 injections	Generation II cephalosporin. More active against pneumococci and gram-negative bacteria. Indications: community-acquired pneumonia, urinary tract, skin and soft tissue infections, perioperative prophylaxis.
  cefotaxime		1	I / v and i / m Adults: 3.0-8.0 g / day in 3-4 injections; with meningitis - 12-16 g / day in 4-6 injections; with uncomplicated gonorrhea - 0.5 g / m once. Children older than 1 month: 50-100 mg / kg / day in 2-3 injections; with meningitis - 0.2 g / kg / day in 4-6 injections. Can be used in children under 1 month of age.	High activity against streptococci and gram-negative microorganisms. Indications: severe community-acquired and nosocomial infections, meningitis, acute gonorrhea.
  ceftriaxone	Por. d / in. 0.25 g; 0.5 g; 1.0 g; 2.0 g per bottle.	6-8,5	I / v and i / m Adults: 1.0-2.0 g / day in one administration; with meningitis - 2.0-4.0 g / day in 2 injections; in acute gonorrhea - 0.25 g / m once Children: older than 1 month: 20-75 mg / kg / day in 1-2 injections; with meningitis - 100 mg / kg / day in 2 injections (but not more than 4.0 g / day); in acute otitis media - 50 mg / kg / m, 1-3 injections (but not more than 1.0 g per injection). Can be used in children under 1 month of age.	Basic cephalosporin III generation. Differences from cefotaxime: - long-term T ½; - excretion in urine and bile; - can cause pseudocholelithiasis.
  ceftazidime	Por. d / in. 0.25 g; 0.5 g; 1.0 g; 2.0 g per bottle.	1,5-2	I / v and i / m Adults: 3.0-6.0 g / day in 2-3 injections (with Pseudomonas aeruginosa infections - 3 times a day) Children: 30-100 mg / kg / day in 2-3 introductions; with meningitis - 0.2 g / kg / day in 3 injections	III generation cephalosporin, active against Pseudomonas aeruginosa. Less active against streptococci. Indications: infections in the detection or high probability of P. aeruginosa and other non-fermenting microorganisms; infections on the background of neutropenia.
  cefoperazone	Por. d / in. 1.0 g; 2.0 g per bottle.	1,5-2,5	I / v and i / m Adults: 4-12 g / day in 2 injections (with Pseudomonas aeruginosa every 6 hours) Children: 50-100 mg / kg / day in 2-3 injections	III generation cephalosporin is active against Pseudomonas aeruginosa. Differences from ceftazidime: - less active in P. aeruginosa; - excreted not only with urine, but also with bile; - worse penetrates the BBB; - can cause hypoprothrombinemia and disulfiram-like reaction.
  cefepime	Por. d / in. 0.5 g; 1.0 g; 2.0 g per bottle.	2	I / v and i / m Adults: 2.0-4.0 g / day in 2 administrations Children older than 2 months: 50 mg / kg / day in 3 injections; with cystic fibrosis - 0.15 g / kg / day in 3 administrations (but not more than 2.0 g / day)	Generation IV cephalosporin. High activity against enterobacteria, P. aeruginosa and other non-fermenting microorganisms. Activity against some strains resistant to III generation of cephalosporins. Higher resistance to extended-action β-lactamases. Indications: severe nosocomial infections caused by multidrug-resistant microflora; infections on the background of neutropenia.
  cefoperazone / sulbactam	Por. d / in. 2.0 g per bottle.	1,5-2,5/1	I / v and i / m Adults: 4.0-8.0 g / day in 2 introductions Children: 40-80 mg / day in 2-3 introductions	Inhibitor-protected cephalosporin. The ratio of the components is 1: 1. High activity against Enterobacteriaceae, Acinetobacter spp., B.fragilis. Indications: severe, mainly nosocomial, infections caused by multidrug-resistant and mixed (aerobic-anaerobic) microflora; infections against the background of neutropenia and other immunodeficiency conditions

  * With normal kidney function

Due to the fact that the majority antibacterial drugs can be purchased without a doctor's prescription, their uncontrolled use is increasing. This entails the development of resistance of microorganisms to drugs of this group and the ineffectiveness of standard therapy. Therefore, 4-generation cephalosporins have been developed that remain active against almost all bacteria resistant to antibiotics of the earlier versions.

1st and 4th generation cephalosporins

The main difference between the drugs in question and their predecessors is that 4th generation cephalosporins act on a larger number of microorganisms, both gram-positive and gram-negative. In addition, they are effective against cocci, rods and enterobacteria, completely resistant to 3 generation antibiotics.

Due to the listed features and advantages, cephalosporins of the described type are used in complex chemical therapy of acute and chronic inflammatory diseases of the skin, digestive, genitourinary system, pelvic organs, joints and bones.

Despite the relative safety of these antibiotics, they produce many side effects, among which allergic reactions, digestive disorders, and decreased activity are quite common. immune system... Therefore, 4th generation cephalosporins are rarely prescribed to women with hormonal disorders, including pregnant women, with dysbiosis, and autoimmune problems. Taking the described antibiotic agents can only aggravate the course of the disease.

List of 4th generation cephalosporins

To date, about 10 varieties of such drugs are known, but most of them are still in the research stage, and only 2 types are allowed for mass production: cefpirome and cefepime. These antibiotics are active active ingredients in many names of medicines.

The names of the 4th generation cephalosporins:

• Izodep;
• Kefsepim;
• Maxipim;
• Cefanorm;
• Ladef;
• Movizar;
• Cefepim;
• Maxiceph;
• Cefomax;
• We chain;
• Cefepim Alchem;
• Cefepim Jodas;
• Cefepim Ajio;
• Efipim.

It should be noted that antibiotics of the 4th generation cephalosporins are produced in ampoules with a solvent, which come with a powder for preparing a medicinal suspension. The fact is that the drugs act only when injected intramuscularly, being maximally absorbed into the blood and lymph. 4th generation cephalosporins are not available in tablets, because their molecular structure does not allow active substances to penetrate into the cellular structures of the intestinal mucosa and digestive tract, antibiotics are destroyed even when they enter the stomach due to high.

An important achievement in the production of the considered cephalosporins is that they can be stored for a long time even after dilution of the powder with a solvent. The resulting liquid sometimes darkens due to contact with air and ultraviolet radiation, but does not lose its therapeutic properties.

For a pronounced and stable result of treatment, it is important to follow the correct scheme - to inject the suspension every 12 hours (intramuscularly), preferably at the same specific time. You should also not exceed the recommended course duration, which usually ranges from 7 to 10 days. Otherwise, intoxication of the body with antibiotics, hepatological damage to the liver and kidney pathology is possible.

Content

Antibacterial drugs are divided into several groups according to the mechanism of action and active substance. One of them is the cephalosporins, which are classified by generation: from the first to the fifth. The third is more effective against gram-negative bacteria, including streptococci, gonococci, Pseudomonas aeruginosa, etc. This generation includes cephalosporins for both internal and parenteral use. They are chemically similar to penicillins and can replace them if you are allergic to such antibiotics.

Classification of cephalosporins

This concept describes a group of semi-synthetic beta-lactam antibiotics that are produced from "cephalosporin C". It is produced by the fungi Cephalosporium Acremonium. They secrete a special substance that inhibits the growth and reproduction of various gram-negative and gram-positive bacteria. Inside the cephalosporin molecule, there is a common core consisting of bicyclic compounds in the form of dihydrothiazine and beta-lactam rings. All cephalosporins for children and adults are divided into 5 generations, depending on the date of discovery and the spectrum of antimicrobial activity:

• First... The most common parenteral cephalosporin in this group is Cefazolin, oral - Cephalexin. Used when inflammatory processes skin and soft tissues, more often for the prevention of postoperative complications.
• Second... This includes the drugs Cefuroxime, Cefamandol, Cefaclor, Ceforanid. They have an increased activity against gram-positive bacteria compared to the 1st generation cephalosporins. Effective for pneumonia, combined with macrolides.
• Third... In this generation, the antibiotics Cefixime, Cefotaxime, Ceftriaxone, Ceftizoxime, Ceftibuten are allocated. Exhibit high efficiency in diseases caused by gram-negative bacteria. Used for infections of the lower respiratory tract, intestines, inflammation of the biliary tract, bacterial meningitis, gonorrhea.
• Fourth... Representatives of this generation are antibiotics Cefepim, Cefpir. May affect enterobacteriaceae that are resistant to 1st generation cephalosporins.
• Fifth... They have a spectrum of activity of 4th generation cephalosporin antibiotics. They act on flora resistant to penicillins and aminoglycosides. Effective in this group of antibiotics are Ceftobiprol, Zefter.

The bactericidal effect of such antibiotics is due to inhibition (inhibition) of the synthesis of peptidoglycan, which is the structural main wall of bacteria. Among the common features of cephalosporins, the following can be noted:

• good tolerance due to the minimum number of side effects compared to other antibiotics;
• high synergism with aminoglycosides (in combination with them, they show a greater effect than separately);
• manifestation of cross allergic reaction with other beta-lactam drugs;
• minimal impact on the intestinal microflora (on bifidobacteria and lactobacilli).

3rd generation cephalosporins

This group of cephalosporins, in contrast to the previous two generations, differs more a wide range actions. Another feature is a longer half-life, due to which the drug can be taken only once a day. The advantages include the ability of III generation cephalosporins to overcome the blood-brain barrier. Due to this, they are effective in treating bacterial and inflammatory lesions of the nervous system. The list of indications for the use of third-generation cephalosporins includes the following diseases:

• meningitis of a bacterial nature;
• intestinal infections;
• gonorrhea;
• cystitis, pyelonephritis, pyelitis;
• bronchitis, pneumonia and other lower respiratory tract infections;
• inflammation of the biliary tract;
• shigillosis;
• typhoid fever;
• cholera;
• otitis.

3rd generation cephalosporins in tablets

Oral antibiotics are easy to use and can be used to complex therapy at home infections of bacterial etiology. Oral cephalosporins are often prescribed in a stepwise therapy regimen. In this case, antibiotics are first administered parenterally, and then switched to forms that are taken orally. So, oral cephalosporins in tablets are represented by the following drugs:

• Cefodox;
• Pancef;
• Zedex;
• Suprax.

The active ingredient in this drug is cefixime trihydrate. The antibiotic is presented in the form of capsules with a dosage of 200 mg and 400 mg, a suspension with a dosage of 100 mg. The price of the first is 350 rubles, the second is 100-200 rubles. Cefixime is used for diseases of an infectious and inflammatory nature caused by pneumococci and streptococci pyrrolidonyl peptidase:

• acute bronchitis;
• acute intestinal infections;
• acute pneumonia;
• otitis media;
• relapses of chronic bronchitis;
• pharyngitis, sinusitis, tonsillitis;
• urinary tract infections without complications.

Cefixim capsules are taken with meals. They are allowed for patients over 12 years old. They are shown a dosage of 400 mg of Cefixime daily. Treatment is based on the infection and its severity. Children from six months to 12 years old are prescribed Cefixime in the form of a suspension: 8 mg / kg of body weight 1 time or 4 mg / kg 2 times a day. Regardless of the form of release, Cefix is ​​prohibited in case of allergy to antibiotics of the cephalosporin group. After taking the drug, the following side reactions may develop:

• diarrhea;
• flatulence;
• dyspepsia;
• nausea;
• stomach ache;
• rashes;
• hives;
• itching;
• headache;
• dizziness;
• leukopenia;
• thrombocytopenia.

Cefodox

The bactericidal effect of this antibiotic is due to cefpodoxime in the composition. Forms of issue of this drug- tablets and powder. Suspensions are prepared from the latter. Regardless of the release form, Cefodox is used to treat:

• pyelonephritis, mild or moderate cystitis;
• tonsillitis, pharyngitis, laryngitis, sinusitis, otitis media;
• pneumonia, bronchitis;
• urethritis, proctitis, gonococcal cervicitis;
• infectious lesions of the skin, joints, bone and soft tissues.

The use of Cefodox is not practiced in people who are hypersensitive to the composition of the drug. In tablet form, the antibiotic is not prescribed for children under 12 years of age, in the form of a suspension - at the age of 5 months, with galactose intolerance, malabsorption syndrome, lactase deficiency. The dosage of Cefodox is determined as follows:

• 200-400 mg per day - for patients over 12 years old (average dose);
• 200 mg - for infectious diseases of the respiratory and genitourinary systems;
• 400 mg - for bronchitis or pneumonia.

The course of therapy continues as prescribed by the doctor. Its average duration depends on the course of the disease and is established by a specialist. The price of the drug is about 350-400 rubles. The list of side effects of Cefodox includes the following symptoms:

• rash;
• itchy skin;
• headache;
• diarrhea;
• vomiting, nausea;
• eosinophilia;
• an increase in plasma creatinine and urea levels;
• violation of thrombocytopoiesis and leukocytopoiesis.

Panzef

This representative of the 3rd generation cephalosporins is based on cefexime. You can buy Pancef in the form of tablets and granules. They are indicated for the treatment of infectious diseases of various body systems:

• Urinary. Pancef is effective for gonococcal urethritis and cervicitis.
• Respiratory. This antibiotic is indicated for acute and chronic bronchitis, tracheitis, pneumonia.
• ENT organs. Pancef is prescribed for otitis media, pharyngitis, infectious sinusitis, tonsillitis.

Contraindications for this drug include sensitivity to penicillins and cephalosporins, elderly and up to six months of age. The dosage is determined taking into account the following principles:

• 8 mg / kg 1 time or 4 mg / kg 2 times a day - for patients over 12 years old;
• 400 mg - the maximum of the drug per day;
• 400 mg for 7-10 days, 1 time per day - with gonorrhea, proceeding without complications.

• 8 mg / kg 1 time or 4 mg / kg 2 times a day (6-12 ml of suspension) - for children 5-15 years old;
• 5 ml of suspension - for children 2–4 years old;
• 2.5-4 ml of suspension - for babies from 6 months to a year.

The cost of 6 Pancef tablets of 400 mg is 350 rubles, 5 ml of suspension is 550 rubles. Side effects of the drug appear more often from the digestive tract, but there are other reactions:

• anorexia;
• dysbiosis;
• dizziness;
• fever;
• flatulence;
• nausea;
• dysbiosis;
• vomit;
• jaundice;
• dry mouth;
• hyperbilirubinemia;
• glossitis;
• stomatitis;
• nephritis;
• hyperemia of the skin;
• eosinophilia;
• hives.

Cephalosporin 3rd generation Spectracef exists only in tablet form. Its active ingredient is cefditoren at a dosage of 200 mg or 400 mg. Microorganisms that cause such pathologies are sensitive to this substance:

• Upper respiratory tract diseases, including acute sinusitis and tonsillopharyngitis.
• Uncomplicated infections of subcutaneous fat and skin, including impetigo, abscess, folliculitis, infected wounds, furunculosis.
• Lower respiratory tract infections such as community-acquired pneumonia... This also includes periods of recurrence of chronic bronchitis.

You need to take Spectracef with a liquid, and preferably after a meal. The recommended dose is determined by the type of infection and its severity:

• 200 mg every 12 hours for 5 days - with exacerbation of bronchitis;
• 200 mg every 12 hours for 10 days - for skin infections, sinusitis, pharyngotonsillitis;
• 200 mg every 12 hours for 4-5 days - with community-acquired pneumonia.

Compared to other cephalosporins, Spectracef has a higher cost - 1300-1500 rubles. It is better to check the list of side effects in detailed instructions to the drug as they are numerous. Contraindications for Spectracef include:

• allergy to the constituent drugs and penicillins;
• children under 12 years old;
• hypersensitivity to the protein casein;
• liver failure;
• breast-feeding;
• pregnancy;
• being in a hospital on hemodialysis.

Zedex

One capsule of Cedex contains 400 mg of ceftibutene dihydrate, 1 g of this preparation in powder form contains 144 mg of this active ingredient... Their price varies from 500 to 650 rubles. The list of indications for both forms of drug release includes the following diseases:

• enteritis and gastroenteritis in children caused by Escherichia coli or strains of the genus Shigella and Salmonella;
• otitis media;
• pneumonia, bronchitis, scarlet fever, pharyngitis, acute sinusitis, tonsillitis;
• urinary tract infections.

Zedex is contraindicated in case of allergy to penicillins, intolerance to cephalosporins, severe renal failure and patients on hemodialysis. Age restrictions: suspension is allowed from 6 months, capsules - from 10 years. The dosage is determined as follows:

• 400 mg every day - for acute sinusitis and bronchitis;
• 200 mg every 12 hours for 10 days - with community-acquired pneumonia;
• 9 mg / kg suspension - for children from six months to 10 years.

Treatment lasts an average of 5-10 days. If Streptococcus pyogenes is affected, therapy should last for at least 10 days. List of possible adverse reactions:

• drowsiness;
• dyspepsia;
• anemia;
• eosinophilia;
• gastritis;
• headache;
• dizziness;
• convulsions;
• hives;
• nausea, vomiting;
• thrombocytosis;
• ketonuria;
• changes in taste;
• abdominal pain.

Suprax

Suprax is available in the form of dispersible tablets, i.e. water-soluble. Each contains 400 mg of cefixime. The cost of 7 tablets is about 800 rubles. List of indications for the use of Suprax:

• uncomplicated gonorrhea of ​​the urethra or cervix;
• shigellosis;
• angina is agranulocytic;
• acute bronchitis;
• urinary tract infections;
• pharyngitis of an acute course;
• otitis media, sinusitis, tonsillitis.

You can not use Suprax for colitis, kidney failure, pregnancy, colitis and in old age. You can take the drug regardless of food. Daily dose is calculated as follows:

• 400 mg for 1-2 doses - with a body weight of more than 50 kg;
• 200 mg at a time - with a weight of 25 to 50 kg.

With gonorrhea, treatment lasts 1 day, with mild infections of the genitourinary system - 3-7 days, with angina - 1-2 weeks. To prepare a suspension, one tablet must be crushed and poured with a small amount of water, and then shaken well. List side effects on Supraksa:

• nephritis;
• rash;
• hives;
• headache;
• constipation;
• vomit;
• itchy skin;
• nausea;
• pain in the epigastric region;
• bleeding;
• impaired renal function.

Powder

To prepare a solution for injection, third-generation cephalosporins are used in the form of a powder. When administered intramuscularly, drugs have more fast action and rarely cause side reactions, since they enter the body bypassing the digestive tract. Also, cephalosporin antibiotics in powder form are used for those who, by virtue of physiological characteristics cannot take pills. From this form of medicine, you can prepare a suspension that is easier to give to children.

The active ingredient of Fortum is ceftazidime at a dosage of 250, 500, 1000 or 200 mg. The drug is presented as a white powdery mass for the preparation of solutions for injections. The cost of 1 g is 450 rubles, 0.5 g - 180 rubles. The list of indications for the use of Fortuma includes infections:

• respiratory tract, including lesions on the background of cystic fibrosis;
• ENT organs;
• organs of the musculoskeletal system;
• subcutaneous tissue and skin;
• urinary tract;
• dialysis infections;
• in patients with suppressed immunity;
• meningitis, bacteremia, peritonitis, septicemia, infected burns.

Fortum is contraindicated in case of sensitization to ceftazidime, penicillins and antibiotics from the 3rd generation cephalosporin group. The drug is prescribed with caution to pregnant and lactating women, with renal failure and in combination with aminoglycosides. The daily dose is selected as follows:

• dosage per day should not be more than 6 g;
• adults are administered 1–6 g, divided into 2–3 doses;
• with reduced immunity and severe forms of infections, 2 g are administered 2-3 times or 3 g 2 times;
• in case of urinary tract damage, 0.5-1 g is injected 2 times.

Adverse reactions after the administration of Fortum can manifest themselves on the part of almost all systems and organs. More often, patients note:

• nausea;
• diarrhea;
• vomiting;
• candidiasis of the mucous membranes of the mouth and pharynx;
• abdominal pain;
• dizziness;
• fever;
• paresthesia;
• tremor;
• convulsions;
• Quincke's edema;
• neutropenia;
• thrombophlebitis;
• hives;
• itching, rash.

Tizim

This antibiotic is based on ceftazidime. One vial of Tizim contains 1 g of the indicated active ingredient. The price of the drug is 300–350 rubles. The list of diseases for which Tizim is effective includes the following pathologies:

• sepsis;
• cholangitis;
• peritonitis;
• infections of bones, skin, joints, soft tissues;
• pyelonephritis;
• infected burns and wounds;
• infections caused by hemodialysis and peritoneal dialysis.

The dosage is set for each patient individually, taking into account the localization and severity of the disease. The drug is administered intramuscularly or intravenously in the following dosages:

• 0.52 g every 8-12 hours - for adults;
• 30-50 mg per 1 kg of body weight 2-3 times a day - for children from 1 month to 12 years old;
• 30 mg / kg / day With an interval of 12 hours - for children up to 1 month.

It is allowed to enter no more than 6 g of Tizim per day. Contraindication to the use of this drug is high sensitivity to ceftazidime. Potential side effects include:

• nausea, vomiting;
• hepatitis;
• cholestatic jaundice;
• eosinophilia;
• diarrhea;
• hypoprothrombinemia;
• interstitial nephritis;
• candidiasis;
• phlebitis;
• soreness at the injection site.

Drug interactions

When using cephalosporins of 3 generations against the background of alcohol consumption, there is a high risk of developing a disulfiram-like effect. This deviation is similar to the state of the body in case of poisoning. ethyl alcohol... Against this background, the patient develops an aversion to alcohol. The effect persists for several days after the cephalosporins are discontinued. The danger in the possible development of hypoprothrombinemia is an increased tendency to bleeding. Interaction of cephalosporins with drugs:

• concomitant use of antacids reduces the effectiveness of antibiotic therapy;
• combination with loop diuretics is not allowed due to the risk of nephrotoxic effect;
• the combination with thrombolytics, anticoagulants and antiplatelet agents is also not recommended due to the increased likelihood of intestinal bleeding.

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