A variety of anti-inflammatory drugs are prescribed to remove inflammation in damage foci. The drugs of this purpose are particularly important in diseases that are characterized by a chronic progressive inflammatory process, which can lead to disabilities.

Types of anti-inflammatory drugs

Anti-inflammatory agents - one of the main components of treatment:

• rheumatoid arthritis;
• osteoarthritis;
• osteochondrosis;
• gout;
• rheumatism;
• spinal hernia;
• neuralgia;
• kidney and bile colic;
• myositis;
• injuries and stretching;
• some hearty, gynecological diseases.

Anti-inflammatory drugs are prohibited or limited.

• ulcerative disease;
• blood clotting disorders;
• pregnancy and lactation period;
• allergies to these drugs;
• some kidney diseases;
• cardiovascular diseases;
• varicose disease;
• autoimmune pathology.

Non-steroidal anti-inflammatory means

Non-steroidal anti-inflammatory drugs for treatment are used in complex therapy With inflammation in bone, muscular and articular tissue. The peculiarity of these drugs in their nonspecifications - they remove the inflammatory process of any genesis in any localization. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most commonly used drugs in the world, as they act and as an anesthetic.

The first NSAID in the history of pharmaceuticals was aspirin, which was obtained from Willow's bark in the 18th century. Other, more, more than salicylic acid are produced modern drugs with similar action and, unfortunately, with similar side effects - negative effect on the health of the stomach and duodenal gut, liver I. blood system. To reduce the likelihood of negative consequences after taking non-steroidal anti-inflammatory drugs of this type, doctors are not recommended to exceed the allowed dosage.

NSAIDs of a new type based on other components have a more pronounced anti-inflammatory effect and prolonged action, but at the same time various complications cause different complications even with long-term reception. Such drugs include meloxico, pyroxics (derivatives of oxims), elementeton, diclofenac (phenyloxic acid derivatives), ibuprofen, ketotifen (propionic acid derivatives) and some others.

Steroid anti-inflammatory drugs

Medicines included in the group hormonal anti-inflammatory drugs are more potent than non-steroidal. These funds are based on adrenal hormone - cortisol. The mechanism of action of steroid drugs consists in local suppression of activities immune system. The side effects and contraindications of the drugs of this group are greater than that of the NSAID, and they prescribe them at:

• strong allergic reaction on the skin;
• rheumatoid arthritis;
• inflammation of vessels;
• hepatitis;
• mositis;
• shock states.

Steroid anti-inflammatory drugs are contraindicated with:

• pregnancy and breastfeeding;
• presence of bacterial or viral infection;
• the probability of bleeding;
• immunodeficiency;
• significant erosion of the joints;
• reception of diluting drugs of drugs;
• already made three injections of steroid drugs.

Combined anti-inflammatory drugs

Combined anti-inflammatory drugs are funds combining several components, thereby significantly enhanced the therapeutic effect of these medicines. Frequently used anti-inflammatory component combined drugs - diclofenac, and combine it with vitamins, paracetomol, lidocaine and other active substances.

Anti-inflammatory drugs - list

Competently choose anti-inflammatory drugs in each individual case only the doctor is capable of. Non-steroidal anti-inflammatory funds block the enzymes of the body responsible for the production of prostaglandins - substances, causing pain and inflammation. Apply different drugs of this group to enhance the action can not be caused by the strengthening of side effects. The use of steroid anti-inflammatory drugs without appointing a doctor can provoke hypertension, blood coagulation disorders, body masculinization in women, osteoporosis.

Anti-inflammatory tablets

Package and anti-inflammatory pills are the most purchased medicines. This form is convenient for use, so the most popular drugs are almost always produced in the form of tablets:

• - prescribed with strong pain in the muscles, joints, spine;
• Celecoxib is effective in arthrosis, osteochondrosis;
• - shown in arthritis, ostearrosis, spondyloarthritis;
• Ibuprofen is prescribed with an average painful syndrome with back pain, inflammation of the periosteum, fever.

Anti-inflammatory injections

Preparations in the form of injection provide their painkillers and anti-inflammatory effects much faster than pills. In addition, the injection can be made in close proximity to the focus of inflammation, which will significantly speed up the receipt of the drug into inflamed tissues. The most demanded anti-inflammatory drugs for joints, muscles, bone tissue:

• Ksefokam, Movied - Effective in Arthrosis, produced in the form of tablets;
• Diclofenac - recommended for osteochondroses, radiculitis, lumbago, bone inflammation, produced in the form of tablets;
• Nooofen, ketonal - effective in different inflammations, have few contraindications and side effects;
• Hydrocortisone, Kenalog, - Steroid preparations, are used as emergency assistance in strong inflammation and serious pain syndrome (opiates replace) are introduced directly into the inflamed focus.

Anti-inflammatory candles

The infection that penetrates the female reproductive organs and caused the milk, inflammation of the cervix or fibromus, requires applying anti-inflammatory vaginal candles, since the health of the woman and its offspring depends on the timeliness and quality of treatment. Rectal anti-inflammatory candles are used if necessary to cure focus of inflammation in the rectum and organs located nearby. In addition, treatment with the help of suppositories reduces the risk of side effects. List of anti-inflammatory candles:

• , Diclofenac, ibuprofen, paracetamol, Movied, Woltaren, Flamaks - are used to remove inflammatory processes in the rectum or vagina, as well as with cystitis, neuralgia, neuritis and if it is impossible to use anti-inflammatory funds in other forms;
• Longidase - Vaginal candles are used in the treatment of inflammation of the small pelvis organs;
• Floomizin, Terezhinin - are used for endometritis therapy, adnexitis;
• Ultrafrokt, proctusing - steroid preparation used with hemorrhoids, cracks, paraproitate;
• - Immunomodulatory and anti-inflammatory candles are used for inflammation of the rectum and after operations to accelerate healing.

Anti-inflammatory ointments

Ointment is an effective form of a drug for outdoor use, in some cases, ointments are used to introduce into the vagina or the rectum. Frequently used components of non-steroidal anti-inflammatory ointments - diclofenac, ibuprofen, ketoprofen. Anti-inflammatory ointments:

• Ortofen, Nurofen, Kathetonal, Meloxico - Nonteroidal preparations for the treatment of inflammation externally, bypassing the gastrointestinal tract.
• Sinalar, Moma, acreiderm - steroid anti-inflammatory ointments are prescribed by doctors in cases where local suppression of immunity is needed - with diseases of the skin, states of shock, hepatitis, allergies, muscle pathologies, joints, violations of vessels.

Anti-inflammatory cream

The list of non-steroidal anti-inflammatory drugs in the form of cream includes the names and many drugs manufactured in the form of ointments. Cream is a more convenient form for external application, and active substances are used the same for all anti-inflammatory preparations. Names of anti-inflammatory creams:

• Ketoprofen, arthrosylene, indochin, diclovitis - nonsteroidal creams are used to treat skin diseases, joints;
• Moma, acreiderm - steroid drugs are used to treat allergies, artirites.

Anti-inflammatory gels

The gel is another form of drugs for outdoor use, it is easily absorbed and leaves no fat film. List of anti-inflammatory drugs in the form of a gel:

• Sinalar, BEMATEYUZON - Steroid preparations for the treatment of skin diseases, allergies, accompanied by itching;
• Diclac gel, Voltaren, Fastum gel, Finalgel, Indusain - are used to treat pains and inflammation in muscles, joints.

Eye anti-inflammatory drops

Eye anti-inflammatory drops are used to treat ophthalmic diseases. They produce these anti-inflammatory drugs both with the content of steroids and without them. Many eye drops It can only be purchased after receiving the doctor's recipe, since only a qualified specialist can take into account all individual testimony and contraindications.

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Nonteroidal anti-inflammatory drugs are a group of medicines widely used in medical practice. Their popularity in the treatment various diseases due to pronounced ability to eliminate pain syndrome, temperature and foci of inflammation at high security for the body. The analgesic and anti-inflammatory activity of the NVPS is proved by numerous medical tests.

In efficiency, they are better "simple" painkillers, and some drugs are close to the analgesics central action and opioids.

Mechanisms Action NSAIDs

Main mechanism actions NSAIDscharacterizing their effectiveness and toxic action - this is inhibition of cyclooxygenase activity. It is an enzyme that regulates the conversion of arachidonic acid into prostaglandins, thromboxane and prostacycline. The anti-inflammatory effect of NSAIDs can also be determined by the slowdown in the peroxidation oxidation of fats, stabilizing the membrane by lysosomes, a decrease in the synthesis of ATP, the slowdown in the aggregation of neutrophils and the braking of the formation of a rheumatoid factor in people suffering rheumatoid arthritis.

Historical facts

The beginning of the use of nonsteroidal anti-inflammatory funds is 46-377. BC e. When hippocrates for pain relief and mitigating inflammation was taken bark. This fact was confirmed by Celsius in 30s. n. e. Further references to the properties of the cortex refer to 1763, and in 1827, when the chemicals managed to select the chemical substance from natural material, which turned out to be salicin - the predecessor of the NSAID.

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In 1869 received salicylic acid - A more effective substance that is derived from salicin. After the experiments carried out, it became clear that it could damage the gastric mucosa, and scientists began searching for new, more secure funds. In 1897, Bayer and Scientist Felix Hoffman, toxic salicylic K-Ta was converted to acetylsalicyl. The drug was called aspirin.

Aspirin was a long time was the only compound of the NSAID, but since 1950, the pharmacologists were obtained by new drugs of the NSAID Group, which became more efficient and secure relative to the previous ones.

Steroid and nonsteroid - differences

Unteroidal preparations are also used in medicine. Steroids are made on the basis of glucocorticoids - adrenal hormones. Non-steroidal anti-inflammatory agents have similar effectiveness, but their difference is that they do not have characteristic pronounced side effects in the form of hypertension, development sugar diabetesand do not cause an addictiveness of the body, requiring each time the dosage increases to achieve a similar effect.

What are the forms of release?

NSAIDs are manufactured both in the form of capsules and tablets for use and in the form of ointments, candles, gels and solutions for injection. Such a variety allows you to more effectively use therapeutic drug. The use of funds in the form of injections minimizes the negative effects of drugs on the gastrointestinal tract, but at the same time it is able to cause tissue necrosis.

For this reason, the injection of the NSAIDs is never applied for a long time.

Classification

To date, several dozen drugs are produced in the world, which include selective and non-selective NSAIDs, but only a part is registered in Russia. Their classification can be represented as follows:

By chemical structure:

• Salicylates - the oldest group, from which only aspirin (acetylsalicylic acid) is currently applied;
• Propionic acid derivatives - ketoprofen, ibuprofen, naproxen;
• Derivatives of acetic acid - diclofenac, indomethacin, acecloofenak, ketorolac;
• Pirazolidin - Felilbutazon, Analgin, sodium metamizole;
• Selective COF-2 inhibitors are considered the most safe means, of which only ropecoxib and celecoxib are used in Russia;
• Non-acidic - sulfonamids, alkanes;
• Other NSAIDs, to which the mefenamic acid, pyroxics, nimesulide, meloxicami belong.

Quite often, the list of non-steroidal anti-inflammatory drugs includes with an analgesic and antipyretic effect, but in fact the drug in this group is not included. Its anti-inflammatory activity is very weak, and its anesthetic and antipyretic effect is due to the blocking of COX-2 in the central nervous system.

By efficiency. The most pronounced action possesses the following painkillers: diclofenac, indomethacin, ketoprofen, ketorolac. The least expressed an anesthetic effect in ibuprofen. Maximum quickly remove inflammation of pyroxics, indomethacin, diclofenac, pyroxics. Quickly remove the temperature capable aspirin, fairing and nurofen.

Preparations of the new generation. Created to reduce side effects Drugs of this class on the body. Such drugs are Movied and Pyroquims, Naz, Arcocusia, which, in addition to selective action, have a prolonged period of removal (long output), thereby reinforcing therapeutic effect.

For the treatment of joints

Used as the basis of drug therapy, especially in the stage of exacerbation of the disease, quickly removing pain, swelling and inflammation. For this use:

• In the form of ointments. The effect of means is similar to preparations containing, but has a lower efficiency and a pronounced warming effect. Contraindicated in ulcers in the gastrointestinal tract, pregnancy and lactation, bronchial asthma. Price - 43-344 rub.
• - an analogue of diclofenac with antipyretic, anti-inflammatory and analgesic effect. It is used for inflammatory diseases of the OPA. Contraindicated in the "aspirin triade", hypersensitivity, erosion-peptic diseases and bleeding in the gastrointestinal tract, diseases of the liver and kidney, pregnancy, childhood, hypercalemia and after an aorticonophone shunting. Price - 134-581 rub.
• - It has a stereight effect, effectively removes pain and elevated temperature. Contraindicated in erosion-peptic diseases of the gastrointestinal tract, disorders of porphyrin metabolism, diseases of the liver and kidney, pregnancy and lactation, under 14 years of age and hypersensitivity. Price - 35-89 rubles.

For

The following non-steroidal anti-inflammatory means apply:

1. . It has pronounced anti-inflammatory, painkillers, and temperate antipyretic effect, successfully applied in the hernia of the spine. Contraindicated in ulcers and erosions in the gastrointestinal tract, pregnancy and lactation, allergies caused by the reception of the NSAIDs. Price - 14-75 rubles.
2. . The NSAIDs of the new generation is produced in the form of tablets, candles and a solution for injections, almost deprived of side effects. Price - 502-850 rubles.
3. . It has a strong anti-inflammatory, moderate painkillers and a weakly pronounced antipyretic effect. Contraindicated in ulcers and bleeding in the gastrointestinal tract, renal and liver failure, pregnancy and lactation, under 12 years of age and hypersensitivity. Price - 126-197 rubles.

With hernia spine

In the case of an intervertebral disk protrusion, apply the following drugs With hernia:

1. - effectively removes heat and pain, has an easy anti-inflammatory effect. Contraindicated with leukopenia, severe anemia, hepatic and renal failure and hypersensitivity to the medicine. Price - 345-520 rubles.
2. - It has pronounced analgesic, antipyretic and anti-inflammatory action, blocks an enzyme participating in inflammatory processes. Contraindicated with peptic ulcers, renal and liver failure, aspirin triad and hypersensitivity. Price - 502-850 rubles.
3. - The basic drug used for the diseases of the ODA has an anti-inflammatory, antipyretic and anesthetic effect in the hernia of the spine. Contraindicated in erosion lesions in the gastrointestinal tract, "aspirin triad", pregnancy, hepatic and renal failure, inhibition of blood formation, in childhood and with a hypersensitivity reaction. Price 121-247 rubles.

For

1. . Exhibits painkillers, anti-inflammatory, antipyretic properties that can remove a neuralgic attack, suppresses thrombocyte gluing. Contraindicated in ulcers in the gastrointestinal gastrointestinal disorders of the liver and kidneys, pregnancy, breastfeeding and in childhood, increased sensitivity. Price - 44-125 rubles.
2. Naz. The incoming nimesulide has an antipyretic, anti-inflammatory, anesthetic and antitrombocitan action. Contraindicated in acute ulcerative manifestations and bleeding in the gastrointestinal tract, severe violations of the liver and kidney, pregnancy and breastfeeding, under the age of 2 years and in the intolerance to the drug. Price - 173-424 rubles.
3. . It has pronounced painkillers, antipyretic, as well as a weak antispasmodic and anti-inflammatory effect. Contraindicated in hypersensitivity, inhibition of blood formation, hepatic or renal failure, aspirinic asthma, leukopenia, pregnancy and lactation, anemia. Price - 27-60 rubles.

With osteoarthritis

The following drugs are applied:

1. More often used in the form of ointments, gel or cream, has an painful and anti-inflammatory effect, removes the swelling associated with inflammation. Contraindicated in hypersensitivity, allergic Ranti, attacks of bronchorate, pregnancy and breastfeeding, skin integrity disorders in places of use, under the age of 14 and together with drugs including phenylbutasone. Price - 119-206 rubles.
2. , It is used as a preparation of a new generation during arthrosis. It has an analgesic, anti-inflammatory and antipyretic effect. Contraindicated in hypersensitivity, heart failure and arrhythmia, liver diseases and stomach ulcers, leukopenia and pregnancy. Price 220-475 rub.
3. . It has an analgesic, anti-inflammatory and antipyretic effect. Contraindicated in erosive-ulcerative lesions in the gastrointestinal tract, "aspirin" asthma, rhinestone, the urbivnica caused by the intake of NSAIDs, a pronounced violation of the work of the kidneys, pregnancy and lactation, hypersensitivity. Price - 120-345 rub.

For gout

The following NSAIDs are applied:

1. Manufactured in the form of tablets and ointments. The maximum effectiveness of the means is ensured after the simultaneous use of both forms of the drug. It is prohibited in hypersensitivity, ulcerative bleeding, inflammatory diseases in the gastrointestinal tract, hypercalemia, hepatic and renal failure, pregnancy and lactation. Price - 173-380 rubles.
2. Other NSAIDs -, ibuprofen.

Cheap drugs

1. Ibuprofen (analog). Price (Tablets) - 14-26 rubles.
2. Sodium (analogue of Tablets Voltairen). Price: Tablets - 14-35 rubles., Gel or ointment - 32-75 rubles.
3. Meloxico (analogue of Movals Tablets). Price - 31-84 rubles.
4. Acetylsalicylic acid (aspirin). Price - 7-17 rubles.
5. Analgin. Price - 27-60 rubles.

Criterias of choice

All NSAIDs - modern and efficient drugsBut when choosing a specific drug you need to know some features. So, if necessary, buying one of the three drugs - or, the seller in the pharmacy with a large share of probability will offer a more expensive option, despite their identity relatively active substance. A similar situation when choosing indomethacin, or metyindol.

In addition to the identical active substance, when choosing an analogue, it is necessary to pay attention to the accompanying components, since the components capable of calling can be included in the appropriate medication. allergic reaction. Also in the analogue of the drug there may be a different dosage of the active substance or a retarded form (continued).

All features of the drug are indicated in the instructions or on the package, and it is subject to careful study.

Application

Since non-steroidal anti-inflammatory tools are able to cause various side effects, before applying, it is necessary to adhere to the following rules:

1. Mandatory acquaintance and clear following the recommendations set out in the instructions.
2. Capsules or tablets adopted inwards are necessarily driving a glass of water, which will protect the stomach. The rule applies, among other things, the most modern means that are most secure.
3. After using the means inside, it is recommended not to take a shorter position for at least 3 minutes, so that under the action of gravity the capsule is better to go down the esophagus.
4. Simultaneous reception of drugs and alcohol-containing substances can provoke diseases of the stomach. At the time of the course of receiving NVPV, the alcohol is completely refused.
5. On the same day, two non-steroidal means are not recommended to receive, as this summarizes side effects, and the gain will not bring.
6. With the ineffectiveness of the drug, they definitely inform the doctor to determine the cause, dose adjustments and a more thorough selection of funds.

Indications for use

NSAIDs belong to the most frequently used drugs in medicine. So, they are prescribed 1/5 of the patients to eliminate pain and inflammation in diseases relating to the following areas:

1. Rheumatology.
2. Gynecology.
3. Traumatology.
4. Surgery.
5. Dentistry.
6. Neurology.
7. With eye diseases.

Anesthetics action npvp Especially efficient at:

1. Dysmenorhea.
2. Painful syndrome of various origin of the dental, head, muscular.
3. Migraine.
4. Kidney colic.

The ability to reduce the high temperature causes the use of drugs with "colds" diseases and in urgent situations when hyperthermia threatens human life. Then medications are administered parenterally as means of emergency therapy. NSAIDs are widely used to treat sports injuries and treat complications after chemotherapy sessions.

The ability of aspirin ignite the blood is used to prevent thrombosis.

NSAIDs are used in the treatment of various inflammation stages, accompanied by pain syndrome. These pathologies include the following diseases:

1. and pain.
2. Acute and migraine.
3. Pains accompanying menstruation.
4. Rheumatoid arthritis and.
5. Bone pain during metastases.
6. The pain accompanying Parkinson's disease.
7. Increase temperature (fever feeling).
8. Moderate pain after injury of soft tissues or inflammatory process.
9. Intestinal obstruction.
10. Renal colic.
11. Postoperative pain.

NSAIDs can be used to treat newborns who have no closure within 2 days after birth arterial flow.

Contraindications

1. Jazzen manifestations and presence of bleeding stomach.
2. Uncontrollable arterial hypertension.
3. Renal diseases.
4. Inflammation of the intestines.
5. Stroke, myocardial and transient infarction ischemic attack In the past, as well as cardiac ischemia (except aspirin).
6. Shuntovania coronary artery and stomach.
7. Thrombocytopenia.

special instructions

With long-term reception, the NSAIDs should control the condition of the blood and the functioning of the liver and kidney, which is especially relevant for patients over 65 years. With extreme caution, the means is used in patients suffering from elevated blood pressure, problems with the cardiovascular system, leading to a delay in the body of the fluid.

It follows the fate that this type of drugs can mask the symptoms of infectious diseases and affect the ability to concentrate attention.

What drugs are better suitable for children?

Npvp can be used in childhood For the treatment of inflammatory processes, accompanied by swelling, high temperature, inflammation of lymph nodes and painful sensations. The means should be applied with extreme caution, as they can cause irritation of the gastric mucosa, allergies, problems with breathing, vision and hearing, internal bleeding.

In the treatment of inflammatory diseases, children use a mefenamic acid and due to the absence of serious side effects, but at the same time they can provoke disorder of digestion or constipation. To eliminate foci of inflammation and temperature, use aspirin.

The prescription of drugs is made only by a doctor who carefully regulates the dosage to prevent possible side effects.

disadvantages

The main lack of nonsteroidal anti-inflammatory funds - this is toxicity for the gastrointestinal tract. Prostaglandins included in the E Group E play a major role in gastroduodenal protection. With a decrease in the concentration of prostaglandins in the mucous membrane of the stomach under the influence of drugs, this protection is broken, causing expansion, erosion and other lesions. Under the influence of NSAIDs in 30% of cases, the stomach ulcer develops. They destructively act on the mucous membrane of the 12-pans, increasing the risk of ulcers, perforations and bleeding in it.

Non-Steroid Anti-Local Preparations (NSAIDor NSAID)- A group of drugs possessing anesthetic, antipyretic and anti-inflammatory effects. Their action is based on blocking prostaglandin products, which are allocated in the place of any damage to the tissue. Currently, nonsteroidal antiber drugs are rightfully among the most sought-after medicinesused in clinical practice.

The most famous NSAID is aspirin (acetylsalicylic acid). By non-steroidal anti-inflammatory drugs also include diflunisal, lizinmonoatsetilsalitsilat, phenylbutazone, indomethacin, sulindac, etodolac, diclofenac, piroxicam, tenoxicam, lornoxicam, meloxicam, ibuprofen, naproxen, flurbiprofen, ketoprofen, tiaprofenic acid, nabumetone, nimesulide, celecoxib, rofecoxib, mesalazine and a lot others.

The main problem of using non-steroidal anticipal drugs is that being the most effective drugs in the treatment of many diseases, they act damagingly on the gastric mucosa and duodenal intestine, and as therapeutic, so the damaging effects of the NSAIDs are the consequences of the braking of the NSAP of the production of prostaglandins.

The main physiological functions of prostaglandins in the digestive tract are to stimulate the secretion of protective hydrocarbonates and mucus, activation of cell proliferation in normal regeneration processes and strengthening local blood flow in the mucous membrane. The anti-inflammatory and the analgesic effects of non-steroidal anticipal drugs are due to inhibiting cyclooxygenase enzyme (COW). There are two isoforms of COF: COF-1 and COF-2. The first of them is present in most tissues, including the gastrointestinal mucous membrane, controls the production of prostaglandins, regulating the integrity of the gastrointestinal mucosa, platelets and renal blood flow. COG-2 plays the role of a "structural" enzyme only in some organs (brain, kidney, bones, etc.) and is not normal in other tissues. Its expression is significantly increasing under the influence of "pro-inflammatory" incentives and, on the contrary, decreases under the action of endogenous substances with anti-inflammatory activity. It is believed that the anti-inflammatory action of the NSAID depends on the blocking of COF-2, and their side effects are associated with the suppression of COF-1 (Vasilyev Yu.V.).

Nonteroidal antiber drugs - the cause of gastrointestinal diseases

One of the most important problems of gastroenterology is the treatment and prevention of NSAID-gastropathins - diseases of the gastrointestinal tract associated with the method of non-steroidal anti-inflammatory preparations and acetylsalicylic acid. In the late 1970s, it was found that patients with rheumatic diseases receiving NSAIDs die from gastrointestinal bleeding and punching of ulcers more often than not accepting NSAIDs.

Despite significant progress in the field of studying the NSAIDs and the creation of more secure drugs, modern statistics testifies: the risk of gastrointestinal bleeding when taking the NSAID increases by 3-5 times, campaigns - in 6, the risk of death against complications associated with the damage to the gastrointestinal tract - 8 times. 40-50% of patients hospitalized with a diagnosis of acute gastrointestinal bleeding, it is due to the reception of this class of medicines. In the UK, up to 2000 patients die from such complications, in the United States, the NSAID is the cause of 100,000 hospitalization and 16,000 deaths per year.

In Moscow, 34.6% of hospitalization cases with a diagnosis of "acute gastrointestinal bleeding" are directly related to the reception of the NSAID. Bleeding and perforation of ulcers are the cause of the death of patients suffering from rheumatic diseases and taking NSAIDs, and amount to 13.8% among the direct causes of the death of patients with rheumatoid arthritis, ankylosing spondylitis and systemic red lupus (Burkov S.G.).

• all patients in need of constant reception of NSAIDs must be stratified depending on the risk of hemorrhagic complications.
• with a high risk of bleeding development, the translation of patients to selective COX-2 inhibitors is recommended in combination with a constant admission of proton pump inhibitors or misoprostol
• when developing bleeding, the reception of the NSAID should be terminated (replacing the drugs of other groups); It is recommended a combination of endoscopic and drug (proton pump inhibitors) hemostasis.

Professional medical articles concerning the problems of the damaging effects of nonsteroidal anticipable drugs on the mucous membrane of the gastrointestinal

• Abdulganiyev D.I., Belyanskaya AD, Nosov E.L. Communication of clinical manifestations of NSAID-Gastropathy in patients with rheumatoid arthritis with motor disorders of the upper sections of the tract // Scientific and practical rheumatology. 2011. No. 3. P. 25-28.


• Vasilyev Yu.V. Proton pump inhibitors in the therapy of the ulcer of the stomach and duodenum associated with non-steroidal anti-inflammatory drugs // Pharmatek. - 2005. - № 7. - with. 1-4.


• Nosov E.L. The use of nonsteroidal anti-inflammatory drugs and cyclooxygenase-2 inhibitors at the beginning of the XXI century // Russian Medical Journal. - 2003. - Volume 11. - № 7. - p. 375-378.


• Agapova N.G. About drug gastroduodenal ulcers // Masterstva LiKuvannya magazine. Ukraine. - 2007. - 2 (38).


• Burkov S.G. Modern approaches to acid-dependent disease therapy // RMW. - 2007. - Volume 15. - № 6.


• Guide to the use of non-steroidal anti-inflammatory drugs and official instructions of Actavis Ellzabeth LCC "Tablets of prolonged action Diclofenac Sodium" for US health professionals ( english, PDF): "Diclofenac Sodium Extended-Realeas Tablets".


• Official instruction Manufacturer of drugs Naproxen YEAR Genentech, Inc. For US patients (medical guide) "What is non-steroidal anti-inflammatory drugs? EC-Naprosyn (Naprosyn Naproxen Tablets), Naprosyn (Naproxen Tablets), Anaprox / Anaprox DS (Sodium Naproxen Tablets), Naprosyn (Naproxen Suspension) "(in English, PDF):" Medication Guide EC-Naprosyn ® (Naproxen Delayed -Release Tablets), Naprosyn ® (Naproxen Tablets), Anaprox ® / Anaprox ® DS (Naproxen Sodium Tablets), Naprosyn ® (NAPROXEN SUSPENSION).

On the site in the literature catalog, there is a section "NSAIDs and other drugs", containing articles on diseases of the GTS bodies caused by the reception of drugs and their treatment.

Application. Non-steroidal anti-inflammatory drug in anato-therapeutic-chemical classification (ATX)

Non-steroidal anti-inflammatory drugs are widely used in medicine for the treatment of various diseases and states and, therefore, they are represented in various sections of anatomy-therapeutic-chemical classification (ATX), in particular, in the section " Code M. Preparations for the treatment of diseases of the bone-muscular system »There are two subsections of various levels containing the following positions:

M01A Nonteroidal anti-inflammatory drugs:

M01AA Butylpiraizolidons

M01AA01 phenylbutazon
M01AA02 MOFEBUSAZON
M01AA03 Oxyfenbutaon
M01AA05 clofezon
M01AA06 Kebuson

Are the most common medicines and have long been applied in medicine. After all, pain and inflammatory process accompany the majority of diseases. And many patients are these drugs bring relief. But the use of them is associated with the risk of occurrence of side effects. And not all patients have the opportunity to use them without harm to health. Therefore, scientists create new medicines, trying to keep them high efficiency and did not have side effects. Such properties have non-steroidal anti-inflammatory drugs of a new generation.

The history of these drugs

In 1829, salicylic acid was obtained, and scientists began to investigate its action per person. New substances were synthesized and preparations that eliminate pain and inflammation appeared. And after the creation of Aspirin, they spoke about the emergence of a new group of drugs that do not have such negative actions as opiates, and more effective in the treatment of fever and pain. After that, the use of nonsteroidal anti-inflammatory drugs has become popular. This name is this group of drugs for the fact that there are no steroids in their composition, that is, hormones, and they do not have such strong side effects. But negative impact on the body still have. Therefore, for more than a hundred years, scientists are trying to create such a medicine that would act effectively and did not have side effects. And in recent years, nonsteroidal anti-inflammatory drugs of a new generation, which have such properties were obtained.

Principle of action of such drugs

Any inflammation B. human organism accompanied by pain, swelling and tissue hyperemia.

All these processes are monitored by special substances - prostaglandins. Non-steroidal anti-inflammatory drugs whose list is increasing, affect the form of these substances. Due to this, signs of inflammation are reduced, heat and swelling are undergoing, the pain ducks. Scientists have long found that the effectiveness of these drugs is associated with the fact that they affect the cyclooxygenase enzyme, with the help of which prostaglandins are formed. But recently it was discovered that it exists in several forms. And only one of them is a specific inflammation enzyme. Many NSAIDs have an action to another form, therefore, they cause side effects. And non-steroidal anti-inflammatory drugs of the new generation suppress enzymes that cause inflammation without acting on those that protect the gastric mucosa.

What diseases are NSAIDs apply?

Treatment of non-steroidal anti-inflammatory drugs is widespread as in medical institutionsand with self-relocating patients with pain symptoms. These medicines remove pain, reduce heat and swelling, reduce blood clotting. Effectively applying them in such cases:

For diseases of the joints, arthritis, bruises, tensile muscles and mosites (as an anti-inflammatory agent). Non-steroidal anti-inflammatory drugs with osteochondrosis are very effectively removed.

Often they are used as an antipyretic agent for colds and infectious diseases.

These drugs are most in demand as an anesthetizing with headaches, renal and hepatic colic, postoperative and premenstrual pains.

Side effects

Most often long use NSAIDs There are lesions of the gastrointestinal tract: nausea, vomiting, dyspeptic disorders, ulcers and gastric bleeding.

In addition, these drugs affect the activities of the kidneys, causing disorder of their functions, the increase in protein in the urine, the delay in urine outflows and other disorders.

Even non-steroidal anti-inflammatory drugs of the new generation are not disposed of negative effect on the cardiovascular system of the patient, they can cause pressure increase, rapid heartbeat and swelling.

Often after the use of these drugs happens headache, dizziness and drowsiness.

1. You can not make these drugs to take long courses in order not to strengthen side effects.

2. To start receiving a new drug is needed gradually, in small doses.

3. Put these drugs cost only water, and to reduce side effects you need to drink it no less than a glass.

4. You can not receive several NSAIDs at the same time. Therapeutic effect does not enhance this, but the negative impact will be higher.

5. Do not deal with self-medication, take drugs only by appointment of a doctor.

7. During treatment with these drugs, it is impossible to accept alcoholic beverages. In addition, the NSAIDs affect the effectiveness of some drugs, for example, reduce the effect of hypertensive drugs.

Forms of release NSAID

The most popular tableted forms of these drugs. But it is they who have the strongest negative effect on the stomach group.

To make the medicine immediately hit blood and begin to be impressed without the manifestation of side effects, it is administered intravenously or intramuscularly, which is probably not always.

Another form of use of these drugs is more accessible - rectal candles. Negative influence on the stomach is less, but they are contraindicated in the intestinal diseases.

With local inflammatory processes and diseases of the musculoskeletal system, it is best to use outdoor medicines. NSAIDs are produced in the form of ointments, solutions and creams that are effectively removing the fighting.

Classification NSAID

Most often, these medicines are divided into two groups in accordance in their chemical composition. Different drugs derived from acids and non-acidic. You can also classify the NSAID on impact efficiency. Some of them better remove inflammation, such as "Dicoofenak" drugs, "Ketoprofen" or "Movied". Others are more effective pleasing - means "ketonal" or "indomethacin". There are those most often used to reduce increased temperature - Medicines "Aspirin", "Nurofen" or "Naz". In a separate group, non-steroidal anti-inflammatory drugs of a new generation are also distinguished, they differ in greater efficiency and absence of side effects.

NSAIDs derived from acids

The largest list of non-steroidal anti-inflammatory drugs belongs to acids. In this group, there are several types of them:

Salicylates, the most common of which is aspirin preparation;

Pyrazolidin, for example, the means "analgin";

Those that contain in the composition of indoleutacetic acid - the drug "Indomethacin" or "etodolac";

Propionic acid derivatives, for example, tool "ibuprofen" or "ketoprofen";

Oxycams are new non-steroidal anti-inflammatory drugs, which include the "Pyroxiks" or "Meloxico" medicine;

The derivative of isonicotine acid includes only the Medizon medicine.

Non-acidic NSAIDs

The second group of these drugs make up non-acidic. These include:

Sulfonamids, for example, the drug "Nimesulid";

Koksibov derivatives - means of "Ropecoxib" and "Celecoxib";

Alcanons, for example, a Medication "Wheel".

The developing pharmaceutical industry creates all new drugs, but often they are the same in composition, as well as already known non-steroidal anti-inflammatory drugs.

List of the most effective NSAID

1. Means "Aspirin" - the oldest medical preparation, is still widely used in inflammatory processes and pain. Now it is produced under other names. This substance can be found in Bufferan medications, "Instrin", "Nandandol", "Uppsar Uppa", "Fortalgin C" and many others.

2. The drug "Diclofenak" was created in the 60s of the 20th century and is now very popular. Available under the names of "Voltaren", "Ortofen", "Diklak", "Claudifen" and others.

3. The drug "Ibuprofen" has proven itself as an effective painking and antipyretic agent, which is also easily transferred to patients. It is also known for the names of "long", "solpflex", "Nurofen", MiG 400 "and others.

4. Medication "Indomethacin" has the strongest anti-inflammatory effect. It is manufactured under the names of "Metindol", "Indusan" and others. These are the most common non-steroidal anti-inflammatory drugs for joints.

5. The "Ketoprofen" preparation is also quite popular in the treatment of diseases of the spine and joints. You can buy it under the name "Fastum". "Fold", "Kathetonal" and others.

NSAID new generation

Scientists constantly develop new drugs that would act more effectively and would have less side effects.

This requirements are answered by modern NSAIDs. They act selectively, only on those enzymes that manage the inflammation process. Therefore, they are less affected by gastrointestinal And the cartilaginous fabrics of patients do not destroy. It is possible to drink for a long time without fear of getting side effects. The benefits of these drugs also include a long period of their action, so that they can be taken less often - only 1 time per day. The disadvantages of these drugs can be attributed a fairly high price. Such modern NSAIDs is the drug "nimesulide", "Meloxicam", "Movalis", "Arrotozan", "Amelotex", "Naz" and others.

NSAIDs for diseases of the musculoskeletal system

Diseases of the joints and spine cause patients often unbearable suffering. In addition to strong pain, in this case there are edema, hyperemia and stiffness of movements. It is best to take NSAIDs, they are effective in the case of inflammatory processes by 100%. But since they do not treat, but only remove the symptoms, these drugs apply only at the beginning of the disease, to relieve pain.

The most effective in such cases external means. The best non-steroidal anti-inflammatory drugs during osteochondrosis is a diclofenac medication, better known to patients called "Voltaren", as well as "indomethacin" and "ketoprofen", which are used both in the form of ointments and orally. Well remove pain medication "Butadion", "naproxen" and "nimesulide". The most effective non-steroidal anti-inflammatory drugs during arthrosis are tablets, it is recommended to use medicines "meloxicams", "celecoxib" or "pyroxics". The choice of the drug should be individual, so the doctor should be engaged in the selection.

Non-steroidal anti-inflammatory

FUNDS

Historythe use of nonsteroidal anti-inflammatory agents for the treatment of a person has several millennia.

Celsius (1 century BC) described 4 classic signs of inflammation: hyperemia, temperature rise, pain, edema and used willow cortex extract to facilitate these symptoms.

The clinical efficacy of these natural medical devices is associated with the presence of salicylate in them. The chemical synthesis of salicylic acid was first spent in 1860 in Germany in Germany (at the request of a father suffering from heavy rheumatism) with a more acceptable taste than an extremely bitter extract of Willow Core. In 1899, Bayer began commercial production aspirin.

Over the past 35 years, more than 40 aspiropod-like drugs are synthesized. Since these drugs differ from glucocorticoids on chemical properties and mechanism of action, they received the common name "Non-Steroid Anti-inflammatory drugs".

CLASSIFICATION

1. Salicylic acid derivatives

Acetylsalicylic acid \u003d aspirin \u003d aspisol (injection form)

Salicylate sodium

Salicylamide

2. Pyrazolone derivatives

Amidopin \u003d pyramidon * analgin \u003d metamizole \u003d novagetol * butadion \u003d phenylbutazone balallgin *

3. Aniline derivatives (para-aminophenol)

Paracetamol \u003d Panadol \u003d\u003d Acetaminophen \u003d Efferganups

4. Propionic acid derivatives

Ibuprofen \u003d bruphen \u003d Dignoflex Naproxen \u003d Narosin \u003d Prosxen ketoprophne \u003d Profinid thiaprophone acid \u003d Surgam Flubiprofen

5. Anatralic acid derivatives

Methenic acid crowdenamic acid \u003d clogs

6. Phenyloxic acid derivatives

Diclofenac sodium \u003d Voltaren \u003d Ortofen

Diclofenak Restard

Alcloofenak

Arthrettek (Diclofenac + Mizoprostol)

7. Indoleux derivatives

Indomethacin \u003d methindol Sulindak \u003d clinyril ketorolac \u003d ketanes \u003d Toradol Tolm cellin \u003d TOLEKTIN

8. Oxycama

Pyroxikov \u003d remoxicams

Tenoxico \u003d Tetoldil \u003d Tylcotil

Meloxico \u003d Movied Selective COF-2 inhibitor

Nonarcotic analgesics

Preparations are not included in the group actually NSAVS Paracetamol AMIDOPINIIN ANALHIN

Barallgin Combined drug (contains analgin, spasmolitic and

ganglioblocator)

Non-steroidal anti-inflammatory means

Classification for action mechanism

1. Selective COF-1 inhibitors

Aspirin at low doses

2. Non-selective COF-1 inhibitors and COF-2

Aspirin in high doses

Butadion

Ibuprofen.

Ketoprofen.

Naproxen

Medehenamic acid

Diclofenak

Indomethacin

Sulindak and most NSPIDs

3. Selective COF-2 inhibitors

Meloxicami ranged

4. High-selective COF-2 inhibitors

MK-966 Zeanetoxit DUP 697 Floss NS-398

5. Selective COF-3 inhibitors (?)

Acetaminophen

Non-steroidal anti-inflammatory meansCharacteristic of drugs

Pharmacological effects

Anti-inflammatory

Arises in a few days.

The development of exudative and proliferative phases of inflammation is limited.

The maximum severity of the anti-inflammatory effect in pyrazolones (except for analgin and

amidopyrin)\u003e Salicylate\u003e Indole Ace derivatives\u003e Phenyluxus derivatives

acids\u003e Phenylpropionic acid derivatives.

ANALGESIC

Occurs through the clock ..

If the pain is associated with a weak inflammatory response - nonarcotic analgesics.

The pain mediated by inflammation affects the drugs with the most pronounced

anti-inflammatory action.

ANTIPYRETIC

In a few hours.

In the event that the patient does not tolerate the subfebrile temperature ( defensive reaction organism at the expense

increasing the activity of phagocytes and interferon products, increasing the release of lysosomal

enzymes) - derivatives of aniline, salicylic, phenyloxus acids.

In the case of hectic temperature - analgin, amidopin.

Antiagregant

The greatest activity in acetylsalicylic acid, irreversibly acetylating platelet cher.

SIDE EFFECTS

Damage to the mucous membrane of the gastrointestinal tract

The greatest danger is acetylsalicylic acid, indomethacin, butadiene.

Especially in patients belonging to the risk group (gastritis).

"Aspirin Asthma"

Edge, rhinitis, urticaria.

The smallest danger is paracetamol.

Delay of liquid and electrolytes (the result of blocking the COF in the kidney channels).

Already 4-5 days after the start of reception of drugs.

The most dangerous - butadiene, indomethacin.

Methemoglobinemia, hemolysis of erythrocytes

When using paracetamol in children (up to 1 year) or in people having genetic

predisposition.

Leukopenia, agranulocytosis

Pyrazolone group.

Hemorogic syndrome

More often when using acetylsalicylic acid.

Retinopathy and keratopathy

The result of indomethacin deposit in the retina and cornea.

Hallucinations

When using indomethacin in the liver, metabolites can form, similar to their own

chemical structure for serotonin, which leads to dizziness, sleep disorders, hallucinations.

Reia Syndrome

It is characterized by toxic encephalopathy, acute fatty dystrophy of the liver, brain, kidneys.

More often in young children.

Acetylsalicylic acid.

Selective cyclooxygenase-2 inhibitors (COF-2)

Despite the differences in the chemical structure, all NSAIDs (nonsteroidal anti-inflammatory funds) have common therapeutic effects;

suppress the development of edema, hyperemia, inflammation-related pain

reduce the severity of fever

expose analgesic activity side effects:

defeat GTC

violation of kidney function

Suppression of platelet aggregation * If the tissue is damaged by various factors include:

Cascade Arachidonic Acid Kininic System

local and systemic mechanisms of immunity chemotaxis and migration in leukocyte damage

and macrophadges

liberation of histamine and serotonin

In 1971, J. Vane, J. Smith and A.Willis have deciphered the main mechanism of the operation of the NSAID, which is associated with the inhibiting the synthesis of the COG (cyclooxygenase) - the key enzyme of the arachidonic acid metabolism. Arachidonic acid is predecessor of prostaglandins (GHG).

NSAIDcall a block or inhibition of the transition of cyclooxygenase (Latent PG-synthetase latent form) to an active enzyme. As a result, the formation of pro-inflammatory GHG types E and F is sharply reduced.

(Prostaglandins are detected in the focus of inflammation in various forms and take part in the development of vasodilation, hyperemia, fever).

COG - gem and glycoprotein, located in an endoplasmic network and a nuclear membrane of PG-forming cells. This enzyme catalyzes two independent reactions:

Cyclooxygenase

(consisting in the addition of oxygen molecules to arachidonic acid molecule with the formation of PGO2)

peroxidase

(leading to the conversion of Pgo2 to more stable PGN2)

Thus, COW is an enzyme playing a fundamental role in arachidonic acid metabolism, leading to the formation of GHG, thromboxane and prostacycline. In recent years, two main isoforms CHA:

- COF-1.

(providing synthesis of PG, regulatingphysiological activity of cells)

- COF-2.

(providing Synthesis of PG, involved in processesinflammation and cell proliferation)

COG - 1 Structural enzyme that is permanently present in most cells (with the exception of erythrocytes), regulates GHG products involved in ensuring the normal functional activity of cells.

COF - 2 is normal in most tissues (with the exception of the brain and the kidney cortical substance) only in trace amounts, however, the expression of COG-2 increases dramatically against the background of the development of inflammation.

* Suppression of platelet aggregation is considered as the therapeutic effect of low doses of aspirin,

used in the clinic for the prevention of thrombotic complications.

In 1994, J. Vane formulated a hypothesis according to which the anti-inflammatory effect of the NSAID is associated with their ability to inhibit COF-2, while the most common side effects (lesion of the gastrointestinal tract, kidney, disturbance of platelet aggregation) - with the suppression of the activity of COF-1

COF-1 and COG-2 are functioning as separate enzyme systems.

COG-1 is localized in an endoplasmic network, and COX-2 - both in the endoplasmic network and in a nuclear membrane, and COF-1 and COG-2, use various arachidonic acid pools that are mobilized under the influence of various incentives.

These crystallographic studies indicate certain differences in the structure of COF-1 and COF-2. It is believed that the presence of a small side chain of valine in COG-2 leads to the appearance of a new cavity (absent in COF-1), with which selective COF-2 inhibitors interact.

It is obvious that the specific COG-2 inhibitors may have certain advantages, but COF-1 probably takes part in the induction of COF-2 in the early phase of inflammation.

In recent years, the role of COW-2 in the regulation of physiological processes (embryogenesis, reproduction) and the pathogenesis of a wide range of pathological conditions emerging beyond inflammation are studied: some forms of CNS pathology (epilepsy, stroke), atherosclerotic damage to vessels, malignant neoplasms (adenomatosis, colon cancer intestine), osteoporosis, bronchial asthma.

Microglia cells performing the role of phagocytic cells in the CNS, with their pathological activation, the COX-2 is expressed. In this case, the inhibition of COG-2 causes the suppression of the apoptosis of neurons. This allows partially to explain the data of clinical studies that the NSAIDs slow down the development of alzheimer's symptoms.