External anti-inflammatory. Non-steroidal drugs: types and characteristics, features of use

Non-steroidal anti-inflammatory drugs, which are briefly called NSAIDs or NSAIDs (means) are widely used throughout the world. In the United States, where statistics cover all branches of life, it was estimated that every year American doctors write more than 70 million prescriptions for NSAIDs. Americans drink, inject and smear on skin more than 30 billion doses of non-steroidal anti-inflammatory drugs per year. It is unlikely that our compatriots are lagging behind them.

Despite their popularity, most NSAIDs are distinguished by high safety and extremely low toxicity. Even when used in high doses, complications are extremely unlikely. What are these miraculous remedies?

Non-steroidal anti-inflammatory drugs are a large group of drugs that have three effects at once:

  • painkillers;
  • antipyretic;
  • anti-inflammatory.

The term "non-steroidal" distinguishes these drugs from steroids, i.e. hormonal drugs, which also have anti-inflammatory effects.

The property that favorably distinguishes NSAIDs from other analgesics is the absence of addiction with prolonged use.

Excursion into history

The "roots" of non-steroidal anti-inflammatory drugs go back to the distant past. Hippocrates, who lived in 460-377. BC, reported the use of willow bark for pain relief. A little later, in the 30s BC. Celsius confirmed his words and stated that willow bark perfectly softens the signs of inflammation.

The next mention of the analgesic cortex is found only in 1763. And only in 1827, chemists were able to isolate from the willow extract the very substance that became famous in the time of Hippocrates. The active ingredient in willow bark turned out to be the glycoside salicin, a precursor to non-steroidal anti-inflammatory drugs. From 1.5 kg of bark, scientists received 30 g of purified salicin.

In 1869, for the first time, a more effective derivative of salicin, salicylic acid, was obtained. It soon became clear that it damages the gastric mucosa, and scientists began an active search for new substances. In 1897, the German chemist Felix Hoffmann and the Bayer company ushered in a new era in pharmacology by converting the toxic salicylic acid into acetylsalicylic acid, which was named Aspirin.

For a long time, aspirin remained the first and only representative of the NSAID group. Since 1950, pharmacologists began to synthesize more and more new drugs, each of which was more effective and safer than the previous one.

How do NSAIDs work?

Non-steroidal anti-inflammatory drugs block the production of substances called prostaglandins. They are directly involved in the development of pain, inflammation, fever, muscle cramps. Most NSAIDs non-selectively (non-selectively) block two different enzymes that are required for prostaglandin production. They are called cyclooxygenase - COX-1 and COX-2.

The anti-inflammatory effect of non-steroidal anti-inflammatory drugs is largely due to:

  • a decrease in vascular permeability and an improvement in microcirculation in them;
  • a decrease in the release from cells of special substances that stimulate inflammation - inflammatory mediators.

In addition, NSAIDs block energy processes in the focus of inflammation, thereby depriving it of "fuel". Analgesic (pain-relieving) action develops as a result of a decrease in the inflammatory process.

Serious disadvantage

It's time to talk about one of the most serious disadvantages of non-steroidal anti-inflammatory drugs. The fact is that COX-1, in addition to participating in the production of harmful prostaglandins, also plays a positive role. It is involved in the synthesis of prostaglandin, which prevents the destruction of the gastric mucosa under the action of its own hydrochloric acid. When non-selective COX-1 and COX-2 inhibitors begin to work, they completely block prostaglandins - both "harmful" ones that cause inflammation and "beneficial" ones that protect the stomach. So non-steroidal anti-inflammatory drugs provoke the development of gastric ulcer and duodenum and internal bleeding.

But there are special drugs among the NSAID family. These are the most modern tablets that can selectively block COX-2. Cyclooxygenase type 2 is an enzyme that is involved only in inflammation and does not carry any additional load. Therefore, blocking it is not fraught with unpleasant consequences. Selective blockers COX-2s do not cause gastrointestinal problems and are safer than their predecessors.

Nonsteroidal anti-inflammatory drugs and fever

NSAIDs have a completely unique property that sets them apart from other drugs. They have an antipyretic effect and can be used to treat fever. To understand how they work in this capacity, you should remember why the body temperature rises.

Fever develops due to an increase in the level of prostaglandin E2, which changes the so-called firing rate of neurons (activity) within the hypothalamus. Namely, the hypothalamus - a small area in the diencephalon - controls thermoregulation.

Antipyretic non-steroidal anti-inflammatory drugs, also called antipyretics, inhibit the COX enzyme. This leads to inhibition of prostaglandin production, which as a result contributes to the inhibition of neuronal activity in the hypothalamus.

By the way, it was found that ibuprofen has the most pronounced antipyretic properties. It outperformed its closest competitor, paracetamol, in this respect.

Classification of non-steroidal anti-inflammatory drugs

And now let's try to figure out what kind of drugs belong to non-steroidal anti-inflammatory drugs.

Today, several dozen drugs of this group are known, but far from all of them are registered and used in Russia. We will consider only those medicines that can be bought in domestic pharmacies. NSAIDs are classified according to their chemical structure and mechanism of action. In order not to frighten the reader with complex terms, we present a simplified version of the classification, in which we present only the most famous names.

So, the entire list of non-steroidal anti-inflammatory drugs is divided into several subgroups.

Salicylates

The most experienced group, with which the history of NSAIDs began. The only salicylate that is still used today is acetylsalicylic acid, or aspirin.

Propionic acid derivatives

These include some of the most popular non-steroidal anti-inflammatory drugs, in particular drugs:

  • ibuprofen;
  • naproxen;
  • ketoprofen and some other medicines.

Acetic acid derivatives

Acetic acid derivatives are no less famous: indomethacin, ketorolac, diclofenac, aceclofenac and others.

Selective COX-2 inhibitors

The safest non-steroidal anti-inflammatory drugs include seven new drugs of the latest generation, but only two of them are registered in Russia. Remember their international names are celecoxib and rofecoxib.

Other non-steroidal anti-inflammatory

Separate subgroups include piroxicam, meloxicam, mefenamic acid, nimesulide.

Paracetamol has very weak anti-inflammatory activity. It mainly blocks COX-2 in the central nervous system and has an analgesic, as well as a moderate antipyretic effect.

When are NSAIDs used?

Typically, NSAIDs are used to treat acute or chronic inflammation accompanied by pain.

We list the diseases in which non-steroidal anti-inflammatory drugs are used:

  • arthrosis;
  • moderate pain due to inflammation or soft tissue injury;
  • osteochondrosis;
  • lower back pain;
  • headache;
  • acute gout;
  • dysmenorrhea (menstrual pain);
  • bone pain caused by metastases;
  • postoperative pain;
  • pain in Parkinson's disease;
  • fever (increased body temperature);
  • intestinal obstruction;
  • renal colic.

In addition, non-steroidal anti-inflammatory drugs are used to treat children whose ductus arteriosus does not close within 24 hours of birth.

This amazing aspirin!

Aspirin can be safely attributed to the drugs that surprised the whole world. The most common non-steroidal anti-inflammatory pills that have been used to reduce fever and treat migraine have shown an unusual side effect. It turned out that by blocking COX-1, aspirin at the same time inhibits the synthesis of thromboxane A2, a substance that increases blood clotting. Some scientists suggest that there are other mechanisms for the effect of aspirin on blood viscosity. However, for millions of patients hypertension, angina, ischemic disease heart and other cardiovascular diseases is not so significant. For them, it is much more important that aspirin in low doses helps prevent cardiovascular disasters - heart attack and stroke.

Most experts recommend taking low-dose cardiac aspirin to prevent myocardial infarction and stroke in men aged 45–79 and women aged 55–79. The dose of aspirin is usually prescribed by a doctor: as a rule, it ranges from 100 to 300 mg per day.

A few years ago, scientists discovered that aspirin reduces the overall risk of developing cancer and mortality from them. This effect is especially true for rectal cancer. American doctors recommend that their patients take aspirin specifically to prevent the development of colorectal cancer. According to them, the risk of developing side effects due to long-term treatment aspirin is still lower than oncological. By the way, let's take a closer look at the side effects of non-steroidal anti-inflammatory drugs.

Cardiac risks of non-steroidal anti-inflammatory drugs

Aspirin, with its antiplatelet effect, stands out from the orderly row of fellows in the group. The vast majority of non-steroidal anti-inflammatory drugs, including modern COX-2 inhibitors, increase the risk of myocardial infarction and stroke. Cardiologists warn that patients who have recently survived heart attack, it is necessary to refuse treatment with NSAIDs. According to statistics, the use of these drugs almost 10 times increases the likelihood of developing unstable angina. According to research data, naproxen is considered the least dangerous from this point of view.

On July 9, 2015, the FDA, the most authoritative American drug quality control organization, issued an official warning. It talks about an increased risk of stroke and heart attack in patients using non-steroidal anti-inflammatory drugs. Of course, aspirin is a happy exception to this axiom.

The effect of non-steroidal anti-inflammatory drugs on the stomach

Another known side effect of NSAIDs is gastrointestinal. We have already said that he has close ties with pharmacological action all non-selective inhibitors of COX-1 and COX-2. However, NSAIDs not only reduce prostaglandin levels and thereby deprive the gastric mucosa of protection. Drug molecules themselves behave aggressively towards the mucous membranes of the gastrointestinal tract.

Against the background of treatment with non-steroidal anti-inflammatory drugs, nausea, vomiting, dyspepsia, diarrhea, stomach ulcers, including those accompanied by bleeding, may occur. Gastrointestinal side effects of NSAIDs develop regardless of how the drug enters the body: oral in the form of tablets, injections in the form of injections or rectal suppositories.

The longer the treatment lasts and the higher the dosage of NSAIDs, the higher the risk of developing peptic ulcer. To minimize the likelihood of it occurring, it makes sense to take the lowest effective dose for the shortest period.

Recent studies show that more than 50% of people taking NSAIDs have mucosal small intestine still gets damaged.

Scientists note that drugs of the NSAID group affect the gastric mucosa in different ways. So, the most dangerous drugs for the stomach and intestines are indomethacin, ketoprofen and piroxicam. And among the most harmless in this regard are ibuprofen and diclofenac.

Separately, I would like to say about enteric coatings that cover non-steroidal anti-inflammatory tablets. Manufacturers claim that this coating helps to reduce or completely eliminate the risk of gastrointestinal complications of NSAIDs. However, research and clinical practice show that in fact such protection does not work. Much more effectively, the likelihood of damage to the gastric mucosa reduces the simultaneous use of drugs that block the production of hydrochloric acid. Inhibitors proton pump- omeprazole, lansoprazole, esomeprazole and others - are able to somewhat mitigate the damaging effect of drugs from the group of non-steroidal anti-inflammatory drugs.

Say a word about citramone ...

Citramon is the product of a brainstorming session of Soviet pharmacologists. In ancient times, when the assortment of our pharmacies did not number in the thousands of drugs, pharmacists came up with an excellent formula for analgesic-antipyretic. They combined "in one bottle" a complex of a non-steroidal anti-inflammatory drug, an antipyretic and seasoned the combination with caffeine.

The invention turned out to be very successful. Each active ingredient enhanced the effect of each other. Modern pharmacists have somewhat modified the traditional prescription, replacing the antipyretic phenacetin with safer paracetamol. In addition, cocoa and citric acid, which, in fact, gave the name to citramone, were removed from the old version of citramone. The preparation of the XXI century contains aspirin 0.24 g, paracetamol 0.18 g and caffeine 0.03 g. And despite a slightly modified composition, it still helps with pain.

However, despite the extremely affordable price and very high efficiency, Citramon has its own huge skeleton in the closet. Doctors have long found out and fully proved that it seriously damages the mucosa of the gastrointestinal tract. So seriously that the term "citramone ulcer" even appeared in the literature.

The reason for this overt aggression is simple: the damaging effect of Aspirin is enhanced by the activity of caffeine, which stimulates the production of hydrochloric acid. As a result, the gastric mucosa, already left without protection of prostaglandins, is exposed to the action of an additional amount of hydrochloric acid. Moreover, it is produced not only in response to food intake, as it should be, but also immediately after the absorption of Citramon into the blood.

We add that "citramone", or as they are sometimes called, "aspirin ulcers" are large. Sometimes they do not "grow" to gigantic, but they take in quantity, settling in whole groups in different parts of the stomach.

The moral of this digression is simple: don't go overboard with Citramon despite all its benefits. The consequences can be too severe.

NSAIDs and… sex

In 2005, in the piggy bank of unpleasant side effects of non-steroidal anti-inflammatory drugs arrived. Finnish scientists conducted a study that showed that long-term use of NSAIDs (over 3 months) increases the risk of erectile dysfunction. Recall that under this term, doctors mean erectile dysfunction, popularly called impotence. Then urologists and andrologists were consoled by the not very high quality of this experiment: the effect of drugs on sexual function was evaluated only on the basis of the man's personal feelings and was not verified by specialists.

However, in 2011, another study was published in the authoritative Journal of Urology. It also showed an association between treatment with non-steroidal anti-inflammatory drugs and erectile dysfunction. However, doctors argue that it is too early to draw final conclusions regarding the effect of NSAIDs on sexual function. In the meantime, scientists are looking for evidence, it is still better for men to refrain from long-term treatment with non-steroidal anti-inflammatory drugs.

Other side effects of NSAIDs

With the serious troubles that threaten treatment with non-steroidal anti-inflammatory drugs, we figured it out. Let's move on to less common adverse events.

Impaired kidney function

The use of NSAIDs is also associated with a relatively high level of renal side effects. Prostaglandins are involved in the expansion of blood vessels in the renal glomeruli, which allows you to maintain normal filtration in the kidneys. When the level of prostaglandins falls - and it is on this effect that the action of non-steroidal anti-inflammatory drugs is based - the work of the kidneys may be disturbed.

People with kidney disease are, of course, most at risk for kidney side effects.

photosensitivity

Quite often, long-term treatment with non-steroidal anti-inflammatory drugs is accompanied by increased photosensitivity. It is noted that piroxicam and diclofenac are more involved in this side effect.

People taking anti-inflammatory drugs may react to the sun's rays with skin redness, rashes, or other skin reactions.

Hypersensitivity reactions

Non-steroidal anti-inflammatory drugs are also "famous" for allergic reactions. They can manifest as a rash, photosensitivity, itching, Quincke's edema, and even anaphylactic shock. True, the latter effect is among the extremely rare and therefore should not frighten potential patients.

In addition, taking NSAIDs may be accompanied by headache, dizziness, drowsiness, bronchospasm. Rarely, ibuprofen causes irritable bowel syndrome.

Non-steroidal anti-inflammatory during pregnancy

Quite often, pregnant women face the issue of anesthesia. Can expectant mothers use NSAIDs? Unfortunately no.

Despite the fact that non-steroidal anti-inflammatory drugs do not have a teratogenic effect, that is, they do not cause gross malformations in a child, they can still do harm.

So, there is evidence that suggests a possible premature closure of the ductus arteriosus in the fetus if his mother took NSAIDs during pregnancy. In addition, some studies show an association between NSAID use and preterm birth.

Nevertheless, selected drugs are still used during pregnancy. For example, Aspirin is often given with heparin to women who have antiphospholipid antibodies during pregnancy. Recently, the old and rather rarely used Indomethacin has gained particular fame as a medicine for the treatment of pregnancy pathologies. It began to be used in obstetrics for polyhydramnios and threat premature birth. However, in France, the Ministry of Health issued an official order banning the use of non-steroidal anti-inflammatory drugs, including aspirin, after the sixth month of pregnancy.

NSAIDs: accept or refuse?

When do NSAIDs become a necessity, and when should they be abandoned outright? Let's look at all possible situations.

NSAIDs needed Take NSAIDs with caution Better to avoid NSAIDs
If you have osteoarthritis that is accompanied by pain, inflammation of the joints and impaired mobility that is not relieved by other drugs or paracetamol

If you have rheumatoid arthritis with severe pain and inflammation

If you have a moderate headache, joint or muscle injury (NSAIDs are prescribed only for a short time. It is possible to start pain relief with paracetamol)

If you have mild chronic pain, not related to osteoarthritis, for example, in the back.

If you often suffer from indigestion

If you are over 50 years of age or have a history of gastrointestinal disease and/or a family history of early heart disease

If you smoke, have high cholesterol or high arterial pressure or suffer from kidney disease

if you are taking steroids or blood thinners (clopidogrel, warfarin)

If you have been taking NSAIDs to relieve symptoms of osteoarthritis for many years, especially if you have had gastrointestinal diseases

if you have ever had a stomach ulcer or stomach bleeding

If you suffer from coronary artery disease or any other heart disease

If you suffer from severe hypertension

If you have chronic kidney disease

If you have ever had a myocardial infarction

If you are taking aspirin to prevent a heart attack or stroke

If you are pregnant (especially in the third trimester)

NSAIDs in faces

We already know the strengths and weaknesses of NSAIDs. And now let's figure out which anti-inflammatory drugs are best used for pain, which ones for inflammation, and which ones for fever and colds.

Acetylsalicylic acid

The first NSAID to be released, acetylsalicylic acid, is still widely used today. As a rule, it is used:

  • to lower body temperature.

    Please note that acetylsalicylic acid is not prescribed to children under the age of 15 years. This is due to the fact that with childhood fever against the background of viral diseases, the drug significantly increases the risk of developing Reye's syndrome - rare disease life threatening liver.

    Adult dosage acetylsalicylic acid as an antipyretic is 500 mg. Tablets are taken only when the temperature rises.

  • as an antiplatelet agent for the prevention of cardiovascular accidents. The dose of cardioaspirin can range from 75 mg to 300 mg per day.

In an antipyretic dosage, acetylsalicylic acid can be bought under the names Aspirin (manufacturer and trademark owner of the German corporation Bayer). Domestic enterprises produce very cheap pills, which are called - Acetylsalicylic acid. In addition, the French company Bristol Myers produces effervescent tablets Upsarin Upsa.

Cardioaspirin has many names and formulations, including Aspirin Cardio, Aspinat, Aspicor, CardiASK, Thrombo ACC, and others.


Ibuprofen

Ibuprofen combines relative safety and the ability to effectively reduce fever and pain, so preparations based on it are sold without a prescription. As an antipyretic, ibuprofen is also used for newborns. It has been proven to reduce fever better than other non-steroidal anti-inflammatory drugs.

In addition, ibuprofen is one of the most popular over-the-counter analgesics. As an anti-inflammatory drug, it is not prescribed so often, however, the drug is quite popular in rheumatology: it is used to treat rheumatoid arthritis, osteoarthritis and other joint diseases.

The most popular brand names for ibuprofen include Ibuprom, Nurofen, MIG 200 and MIG 400.


Naproxen

Naproxen is prohibited for use in children and adolescents under 16 years of age, as well as in adults suffering from severe heart failure. Most often, non-steroidal anti-inflammatory drugs naproxen are used as painkillers for headache, dental, periodic, joint and other types of pain.

In Russian pharmacies, naproxen is sold under the names Nalgezin, Naprobene, Pronaxen, Sanaprox and others.


Ketoprofen

Ketoprofen preparations are distinguished by anti-inflammatory activity. It is widely used to relieve pain and reduce inflammation in rheumatic diseases. Ketoprofen is available in the form of tablets, ointments, suppositories and injections. Popular drugs include the Ketonal line manufactured by the Slovak company Lek. German joint gel Fastum is also famous.


Indomethacin

One of the outdated non-steroidal anti-inflammatory drugs, Indomethacin is losing ground every day. It has modest analgesic properties and moderate anti-inflammatory activity. In recent years, the name "indomethacin" has been heard more and more often in obstetrics - its ability to relax the muscles of the uterus has been proven.

Ketorolac

A unique non-steroidal anti-inflammatory drug with a pronounced analgesic effect. The analgesic abilities of ketorolac are comparable to those of some weak narcotic analgesics. The negative side of the drug is its insecurity: it can cause stomach bleeding, provoke stomach ulcers, and liver failure. Therefore, you can use ketorolac for a limited period of time.

In pharmacies, Ketorolac is sold under the names Ketanov, Ketalgin, Ketorol, Toradol and others.


Diclofenac

Diclofenac is the most popular non-steroidal anti-inflammatory drug, the "gold standard" in the treatment of osteoarthritis, rheumatism and other joint pathologies. It has excellent anti-inflammatory and analgesic properties and is therefore widely used in rheumatology.

Diclofenac has many forms of release: tablets, capsules, ointments, gels, suppositories, ampoules. In addition, diclofenac patches have been developed to provide a long-lasting effect.

There are a lot of analogues of diclofenac, and we will list only the most famous of them:

  • Voltaren is the original drug of the Swiss company Novartis. Differs in high quality and the same high price;
  • Diklak - a line of German drugs from Heksal, combining both reasonable cost and decent quality;
  • Dicloberl made in Germany, Berlin Chemie company;
  • Naklofen - Slovak drugs from KRKA.

In addition, the domestic industry produces many inexpensive non-steroidal anti-inflammatory drugs with diclofenac in the form of tablets, ointments and injections.


Celecoxib

A modern non-steroidal inflammatory drug that selectively blocks COX-2. It has a high safety profile and pronounced anti-inflammatory activity. Applicable for rheumatoid arthritis and other joint diseases.

The original celecoxib is sold under the name Celebrex (Pfizer). In addition, pharmacies have more affordable Dilaxa, Coxib and Celecoxib.


Meloxicam

A popular NSAID used in rheumatology. It has a rather mild effect on the digestive tract, so it is often preferred for the treatment of patients with a history of diseases of the stomach or intestines.

Assign meloxicam in tablets or injections. Meloxicam preparations Melbek, Melox, Meloflam, Movalis, Exen-Sanovel and others.


Nimesulide

Most often, nimesulide is used as a mild analgesic, and sometimes as an antipyretic. Until recently, pharmacies sold a children's form of nimesulide, which was used to reduce fever, but today it is strictly prohibited for children under 12 years of age.

Trade names of nimesulide: Aponil, Nise, Nimesil (German original drug in the form of a powder for preparing a solution for internal use) and others.


Finally, we will devote a couple of lines to Mefenamic acid. It is sometimes used as an antipyretic, but it is significantly inferior in effectiveness to other non-steroidal anti-inflammatory drugs.

The world of NSAIDs is truly amazing in its diversity. And despite the side effects, these drugs are rightfully among the most important and necessary, which can neither be replaced nor bypassed. It remains only to give praise to the tireless pharmacists who continue to create new formulas, and to be treated with ever safer NSAIDs.

NSAIDs are widely used by physicians in the treatment of diseases that occur with inflammation, fever and pain. They are effective, but cause a number of side effects. Today there are many NSAIDs that are better tolerated by the body.

New generation non-steroidal anti-inflammatory drugs: what is it

NSAIDs are a category of drugs that affect the disease symptomatically. Used for chronic and acute pathologies. The action is based on a decrease in the production of cyclooxygenase enzymes that trigger inflammation, fever and pain. New generation drugs rarely cause side effects.

How they help

The principle of action is based on a decrease in the permeability of capillary and arterial walls, the production of inflammatory mediators. This leads to minimization of irritation of pain nerve receptors. A person has inflammation and pain. NSAIDs of a new generation affect the centers of thermoregulation of the brain, lowering body temperature.

Classification

New generation medicines are divided into:

  1. acids(pyrazolone, salicylates, derivatives of phenylacetic and isonicotinic acids, oxicams, propionic, anthranilic acids)
  2. Non-acid derivatives(sulfonamides).

According to the mechanism of action, NSAIDs are divided into:

  • Selective, suppressing COX-2.
  • Non-selective inhibitors of cyclooxygenase enzymes.
  • Selective, suppressing COX-1.

According to the effect of relieving inflammation, NSAIDs are divided into:

  1. Strong - Flurbiprofen, Indomethacin.
  2. Weak - Aspirin, Amidopyrine.

According to the strength of the analgesic effect, NSAIDs are classified into:

  • Strong - Ketoprofen, Ketorolac.
  • Weak - Aspirin, Naproxen.

Effective new generation NSAIDs

The pharmaceutical industry offers a wide range of NSAIDs in tablets, drops, suppositories, ointments, gels, injection solutions.

Sold in tablets. Main component - etoricoxib. Relieves pain and inflammation, fever. Suppresses the action of COX-2. It is forbidden to use Arcoxia in violation of hemostasis, stomach ulcers, pathologies of the heart, pregnancy, liver (kidney) dysfunction.

It is produced in the form of a gel, tablets, suppositories, injections. Rofecoxib has a medicinal effect. Acts as a COX-2 inhibitor. Relieves swelling, inflammation, itching, fever and pain. Well tolerated by most patients. It is forbidden to take with cancer, asthma, pregnancy. May provoke hallucinations, intestinal upset.

Produced in tablets and solution for injection. Contains lornoxicam. Suppresses the activity of cyclooxygenase enzymes, the release of free radicals. Does not affect the opioid receptors of the central nervous system, the respiratory system. It is forbidden to take with severe pathologies of the heart, liver dysfunction, dehydration. Frequent side effects - blurred vision, increased pressure.

Available in injection solution, tablets, suppositories, suspensions. Treats due to the presence of meloxicam. Effectively removes fever, inflammation and pain. Has a prolonged action. Does not affect the hemostasis system. It is forbidden for bleeding in the esophagus, kidney dysfunction. Sometimes causes migraine, colitis and gastropathy.

Sold in the form of tablets, gel, suspension. Suppresses COX-2, reduces the production of prostaglandins. It has a pronounced anti-febrile, analgesic and anti-inflammatory effect. It is forbidden for pregnant women and children. Of the side effects, it provokes hematuria, oliguria, dyspepsia.

Produced in the form of an ointment. Formulated with methyl salicylate & bee venom. Relieves inflammation and pain. It is used for myalgia, arthralgia, sprain, neuritis. It is forbidden for acute arthritis, skin pathologies. May cause local allergies.

Produced in the form of ointment and balm. Contains methyl salicylate and menthol. Expands blood vessels and removes irritation, relieves pain and spasm, restores mobility. It is forbidden for dermatological problems and pregnancy. May cause hives.

Produced in the form of an ointment. Based on nonivamide, camphor and dimethyl sulfoxide. Relieves irritation and pain, warms and improves blood circulation. Valid for 6 hours. Prohibited for use by children and pregnant women. Side effects include local allergic reactions.

Available in the form of cream and tablets. Contains meloxicam and pepper tincture. Has a warming effect. Effective for sprains, injuries, articular and vertebral pathologies. Used from 12 years of age. May cause itching and rash.

This is an ointment consisting of nicoboxyl and nonivamide. It contains nicoboxyl and nonivamide. It has an analgesic, vasodilating and hyperemic effect. Improves enzymatic reactions. Helps a few minutes after application.

Available in injection solution and capsules. Contains meloxicam. Helps with musculoskeletal pathologies. Not used for severe hepatic and kidney disease, gastric ulcer. May increase blood pressure and reduce visual acuity.

Produced in capsules. The composition contains tenoxicam. Eliminates pain in muscles, joints and spine. Removes stiffness after waking up. Normalizes the condition in a week of use. Not applicable for lactation, kidney dysfunction and pregnancy.

Available in the form of a gel, injection solution and tablets. Therapeutic action based on the presence of meloxicam in Amelotex. It is used for degenerative and dystrophic changes in the bones. Approved for use from 18 years old. May cause a local allergic reaction.

Produced in the form of a suspension, tablets and gel. Contains nimesulide. Relieves pain and inflammation in sprains, injuries, muscle and joint pathologies. Not used for epidermal, hepatic and renal diseases. Prohibited for pregnant and lactating women, children under 7 years of age.

Produced in the form of a gel, suspension, tablets. Contains nimesulide. Well tolerated, has minimal toxicity. Effective in pathologies of soft tissues and spine. Contraindicated in pregnant women, children, allergy sufferers.

Available in the form of capsules, gel, suspension. Therapeutic action is based on nimesulide. Used for a long course. Does not cause pronounced side effects. It is forbidden for damage to the dermis, hypersensitivity.

Sold in injections and tablets. Solution for injection into the muscle. Characterized by speed. Relieves inflammation, fever and pain. Used in the acute stage of the disease. It is forbidden for children, in the presence of serious problems with the kidneys, pregnant women.

Available in solution, suppositories, tablets. Contains meloxicam. It is used for degenerative changes in the bones. injected into the muscle. Contraindicated in inflammation of the intestines, insufficiency in the work of the heart, ulcerative bleeding.

It is sold in the form of eye drops. It contains bromfenac. Eye drops are used after surgery for cataract extraction. The effect persists for a day. The remedy is prohibited for pregnant women, persons under 18 years of age, with a tendency to bleeding.

Produced in injections, tablets, suppositories, gel. Active element - diclofenac sodium. It is a powerful analgesic and anti-inflammatory. Used for miosis inhibition, therapy cystic edema yellow spot. Prohibited in the elderly childhood, violation of hemostasis, pregnancy.

How to Protect Your Stomach When Taking Nonsteroidal Drugs

NSAIDs have a bad effect on the digestive tract, in particular on the stomach. To minimize the negative impact of the drug on the body, a person should undergo diagnostics and treatment before starting therapy.

It is better to choose a selective group of drugs. Non-selective anti-inflammatory nonsteroidal drugs apply up to five days. In the presence of erosive and ulcerative changes, people over the age of 60 should use NSAIDs simultaneously with Omeprazole.

Non-steroidal anti-inflammatory drugs- an extensive group of drugs in medicine, prescribed for the relief of pain, lowering the temperature in various diseases. Medicines have not only a pronounced therapeutic effect, but also certain contraindications, side effects.

Non-steroidal anti-inflammatory drugs have a number of contraindications

Classification of NSAIDs

In pharmacology, different signs are used to distribute non-steroidal anti-inflammatory drugs.

By chemical structure

According to the chemical structure and activity, drugs are divided into acidic and non-acidic drugs.

Groups of acid preparations:

  • oxicam - Meloxicam, Piroxicam;
  • preparations based on indoleacetic acid - Indomethacin, Sulindac;
  • drugs that contain propionic acid - Ketoprofen, Ibuprofen;
  • salicylates - Aspirin;
  • preparations based on phenylacetic acid - Diclofenac, Aceclofenac;
  • pyrazolone derivatives - Analgin, Phenylbutazone.

Aspirin belongs to the group of salicylates.

Non-acid agents include alkanones (Nabumeton), sulfonamides (Nimesulide), coxibs (Celecoxib, Rofecoxib).

All non-steroidal drugs have a similar mechanism of action, have a non-specific effect on inflammatory enzymes, therefore, they well eliminate pain of various origins, and cope well with fever during colds and flu. But for each drug, this or that action is somewhat more pronounced than for other drugs of the same group.

According to the principle of general action

According to the mechanism of action, NSAIDs are classified into selective and non-selective drugs.

non-selective NSAIDs

The body produces 2 types of cyclooxygenase enzymes. COX-1 appear only as a response to the inflammatory process, COX-2 protects the walls of the stomach from the influence of negative factors.

Non-selective NSAIDs inhibit the synthesis of COX-1 and COX-2, therefore, they have an extensive list of adverse reactions, this group includes most nonsteroidal drugs.

Indications - high fever, migraine, gynecological and dental diseases, biliary colic, chronic prostatitis. But most often, NSAIDs are prescribed to eliminate the manifestation of problems with joints, muscles - arthritis, arthrosis, myositis, bruises, sprains, fractures. The main contraindications are peptic ulcer, poor blood clotting, kidney and liver pathologies, asthma.

List of popular non-selective NSAIDs

Pharmaceutical companies are constantly trying to reduce the negative impact of NSAIDs on the gastrointestinal tract, so modern non-selective drugs are safe, have a long period of action, which allows you to take drugs once a day.

List of non-selective NSAIDs of the new generation:

  1. Movalis - effective remedy, on sale there are solutions for injections, pills, ointments, the medicine has a powerful antipyretic effect, quickly eliminates pain and signs of inflammation.
  2. Xefocam is one of the best means for the relief of an acute attack of pain, the action of the drug is similar to morphine, but refers to non-narcotic drugs. Available in tablets and powder.
  3. Nimesulide - tablets and gel with a pronounced anti-inflammatory effect, help well with back and joint pain, the medicine eliminates hyperemia, swelling, signs of the inflammatory process, improves mobility.
  4. Aertal - in terms of therapeutic effect, the drug is similar to Diclofenac, but has greater selectivity, is produced in tablets, powder for suspensions, in the form of a cream.
During long-term treatment with NSAIDs, it is necessary to regularly monitor the functioning of the liver, kidneys, and blood counts, this is especially true for elderly patients.

Movalis is an effective non-steroidal agent

selective NSAIDs

Most modern NSAIDs are selective inhibitors, blocking only the inflammatory enzyme, as practice shows, they have a more gentle effect on the gastrointestinal tract, so the risk of ulcers and bleeding is reduced, but the likelihood of blood clots increases. The disadvantage is the high cost.

Selective drugs are more effective than non-selective drugs, the therapeutic effect is observed within 20-30 minutes after taking the medicine, they are successfully practiced in severe joint diseases - infectious non-specific polyarthritis, rheumatoid spondylitis and arthritis, gout, osteoarthritis, osteochondrosis.

List of the best NSAIDs:

  1. Celebrex - capsules to eliminate fever, pain and inflammation, significantly reduce the risk of colon cancer. The medicine helps well with arthritis, osteochondrosis.
  2. Firocoxib is a highly selective drug in the form of tablets.
  3. Rofecoxib - the drug quickly copes with pain, swelling with bursitis, tendonitis, sprains, eliminates fever, headache and toothache of varying degrees of intensity. Produced in the form of tablets, suppositories, solution for injections, gel.

Celebrex is a selective drug

But even drugs that do not affect the stomach should not be taken in the presence of internal bleeding, perforation of the gastrointestinal mucosa, which occurred while taking NSAIDs. Potent medicines are also contraindicated in severe forms of dysfunction of the kidneys, liver, heart, hemocoagulation disorders, aspirin asthma.

NSAIDs are antiplatelet agents, they are prescribed for diseases of the heart and blood vessels - ischemia, angina pectoris, prevention of stroke, heart attack, hypertension.

Non-steroidal anti-inflammatory drugs during pregnancy

NSAIDs have teratogenic properties, can provoke a miscarriage, cause the development of severe pathologies in a newborn, so it is dangerous to take these drugs during pregnancy.

NSAIDs penetrate into breast milk in small quantities, but there is no reliable data on how safe these doses are for children, so doctors recommend refraining from taking these drugs during lactation, or drinking drugs with a short half-life after feeding.

What analgesics can be taken by lactating and pregnant women? Paracetamol, drugs based on ibuprofen can be drunk in the I, II trimester.

NSAIDs can prevent or delay the onset of ovulation, negatively affect human reproductive functions, but how great this risk is has not yet been clinically identified.

NSAIDs for children

Due to the large number of negative reactions, the destructive effect on the gastric mucosa, the ability to thin the blood, most NSAIDs are prohibited for the treatment of children.

Medicines based on nimesulide, ibuprofen and paracetamol, in the form of suppositories and suspensions, are considered safe for children. The main indications are fever, colds, headache, teething.

List of safe NSAIDs for children:

  1. Ibuprofen, Nurofen, Ibuklin, Ibufen - drugs help reduce fever, are effective painkillers, adverse reactions are rare, and are used in pediatrics for children older than 3 months.
  2. Paracetamol, Panadol, Efferalgan - can be given to children older than 2 months, but these medicines are not recommended to be given to a child in the presence of liver pathologies.
  3. Nimesulide, Nise, Nimesil - representatives of the latest generation of NSAIDs, have a long analgesic effect, are used to treat children over 12 years old.

Nimesulide can be given to children over 12 years of age

The most dangerous for children are derivatives of acetylsalicylic acid - Aspirin, Citramon, they should not be taken by patients under 16 years of age. These drugs can provoke the development of Reye's syndrome, the disease is accompanied by encephalopathy and depression of liver function.

How to protect the stomach when taking nonsteroidal drugs?

NSAIDs negatively affect the integrity of the gastric mucosa, which often causes the development of ulcers, erosions, gastritis, and internal bleeding. To avoid the occurrence of such dangerous complications, it is necessary to adhere to certain rules.

How to reduce the negative impact of NSAIDs:

  1. It is strictly forbidden to drink alcohol while taking nonsteroidal drugs, otherwise the risk of erosions and ulcers increases significantly.
  2. Tablets should not be taken on an empty stomach, you need to drink the medicine during meals, drink plenty of purified water or milk.
  3. Be sure to study the interaction of other medicines with NSAIDs in the instructions.
  4. During treatment, you must not only strictly observe the dosage, but also follow the regimen, try to take the medicine at the same time.
  5. To protect the stomach from the negative effects of NSAIDs, it is necessary to take proton pump inhibitors in parallel with them - Omeprazole, Pantoprazole.

Omeprazole helps to cope with the negative effects of NSAIDs

If you have to take non-steroidal anti-inflammatory drugs for a long time, you need to do a gastroscopy, get tested for the presence of Helicobacter pylori bacteria - this will help to avoid the development of severe stomach problems.

NSAIDs are the most popular group of medicines in the world, but they must be taken wisely, clearly follow the instructions. If the dosages are not observed, internal bleeding, ulcers may occur, with extreme caution, drugs are prescribed to pregnant lactating women, children, and the elderly.

Over the past 30 years, the number of NVPS has increased significantly and now this group has a large number medicines, differing in chemical structure, features of action and application (Table 1).

Table 1

CLASSIFICATION OF NSAIDs

(by chemical structure and activity)

I group - NSAIDs with pronounced anti-inflammatory activity

(Nasonov E.L.; 2003)

Salicylates

a) acetylated:

Acetylsalicylic acid (ASA) - (aspirin);

Lysine monoacetylsalicylate (aspizol, laspal);

b) non-acetylated:

sodium salicylate;

Choline salicylate (sachol);

Salicylamide;

Dolobid (diflunisal);

Disalcid;

Trilisat.

pyrazolidins

Azapropazone (Rhymox);

Clofezon;

Phenylbutazone (butadione);

Hydroxyphenylbutazone.

Derivatives of indoleacetic acid

Indomethacin (methindol);

Sulindak (clinoril);

Etodalac (lodin);

Derivatives of phenylacetic acid

Diclofenac sodium (ortofen, voltaren);

Diclofenac potassium (Voltaren - Rapid);

Fentiazak (donorest);

Lonasalac calcium (irriten).

Oxycams

Piroxicam (roxicam);

Tenoxicam (tenoctin);

Meloxicam (Movalis);

Lornoxicam (Xefocam)

Propionic acid derivatives

Ibuprofen (brufen, nurofen, solpaflex);

Naproxen (naprosin);

Naproxen sodium salt (apranax);

Ketoprofen (knavon, profenid, oruvel);

Flurbiprofen (flugalin);

Fenoprofen (fenoprone);

Fenbufen (lederlen);

Thiaprofenic acid (surgam)

Non-acid derivatives

Group II - NSAIDs with weak anti-inflammatory activity

Anthranilic acid derivatives (phenamates)

Mefenamic acid (pommed);

meclofenamic acid (meclomet);

Niflumic acid (donalgin, nifluril);

Morniflumat (nifluril);

Tolfenamic acid (clotam).

Pyrazolones

Metamizole (analgin);

Aminophenazone (amidopyrine);

Propyphenazone.

Para-aminophenol derivatives

Phenacetin;

Paracetamol.

Derivatives of heteroarylacetic acid

Ketorolac;

Tolmetin (tolectin).

Different

Proquoazone (Biarizon);

Benzydamine (tantum);

Nimesulide (mesulide);

Celebrex (celecoxib).

CLASSIFICATION OF NSAIDs

(by duration)

1. Short action (T1/2 = 2-8 hours):

ibuprofen; ketoprofen; indomethacin; fenoprofen;

Voltaren; fenamates;

Tolmetin;

2. Average duration of action (T1 / 2 \u003d 10-20 hours):

Naproxen;

Sulindak;

Diflunisal;

3. Long-acting (T1 / 2 = 24 hours or more):

Oxycams;

Phenylbutazone.

PHARMACODYNAMICS OF NSAIDs

From a clinical point of view, all NSAIDs have a number of common features:

1. Non-specificity of the anti-inflammatory effect, i.e. inhibitory effect on any inflammatory process, regardless of its etiological and nosological features.

2. A combination of anti-inflammatory, analgesic and antipyretic effects.

3. Relatively good tolerance (which is apparently associated with rapid excretion from the body).

4. Inhibitory effect on platelet aggregation.

5. Binding to serum albumins, with different drugs competing for binding sites. This is significant because, on the one hand, unbound drugs are quickly eliminated from the body and do not have additional effects, and on the other hand, drugs released from albumin can create an unusually high concentration and cause side effects.

The main nodal mechanisms are universal for most drugs, although their different chemical structure suggests a predominant effect on some specific processes. In addition, most of the mechanisms listed below are multi-component, i.e. within each of them, the same type of influence of different groups of drugs can be realized in different ways.

In the action of NSAIDs, the following key links are distinguished:

1. Prevention of damage to cellular structures, a decrease in capillary permeability, which most clearly limits the exudative manifestations of the inflammatory process (inhibition of lipid peroxidation, stabilization of lysosomal membranes, preventing the release of lysosomal hydrolases into the cytoplasm and into the extracellular space that can destroy proteoglycans, collagen, cartilage tissue).

2. Reducing the intensity of biological oxidation, phosphorylation and glycolysis. This leads to inhibition of the production of macroergs necessary for the biosynthesis of substances, the transport of fluid and metal ions through the cell membrane, and for many other processes that play an important role in the pathogenesis of inflammation (reducing the energy supply of the inflammatory reaction). In addition, the effect on tissue respiration and glycolysis changes plastic metabolism, since intermediate products of oxidation and glycolytic transformations of substrates serve as a building material for various synthetic reactions (for example, the biosynthesis of kinins, mucopolysaccharides, immunoglobulins).

3. Inhibition of synthesis or inactivation of inflammatory mediators (histamine, serotonin, bradykinin, lymphokines, prostaglandins, complement factors and other non-specific endogenous damaging factors).

4. Modification of the inflammation substrate, i.e. some change in the molecular configuration of tissue components, preventing them from reacting with damaging factors.

5. Cytostatic effect, leading to inhibition of the proliferative phase of inflammation and a decrease in the post-inflammatory phase of the sclerotic process.

6. Inhibition of rheumatoid factor production in patients with rheumatoid arthritis.

7. Violation of the conduction of pain impulses in the spinal cord (metamizole).

8. The inhibitory effect on hemocoagulation (primarily on the inhibition of platelet aggregation) is an additional, secondary factor in the anti-inflammatory effect: a decrease in the intensity of coagulation in the capillaries of inflamed areas prevents microcirculation disorders.

MECHANISMS OF ACTION OF NSAIDs

Undoubtedly, the most important mechanism of action of NSAIDs is the ability to inhibit COX - an enzyme that catalyzes the conversion of free polyunsaturated fatty acids (for example, arachidonic) into prostaglandins (PG), as well as other eicosanoids - thromboxanes (TrA2) and prostacyclin (PG-I2) (Fig. one). It is proved that prostaglandins have versatile biological activity:

METABOLISM OF ARACHIDIC ACID

PHOSPHOLIPASE A 2

ARACHIDONIC

COX-1, COX-2

LIPOXYGENASE

PROSTACYCLINE

LEUKOTRIENES

OTHER PROSTAGLANDINS

THROMBOXANE

Fig.1. Metabolism of arachidonic acid.

a) are mediators of the inflammatory response: they accumulate in the focus of inflammation and cause local vasodilation, edema, exudation, migration of leukocytes and other effects (mainly PG-E2 and PG-I2);

b) sensitize receptors to mediators of pain (histamine, bradykinin) and mechanical influences, lowering the threshold of sensitivity;

in) increase the sensitivity of the hypothalamic centers of thermoregulation to the action of endogenous pyrogens (interleukin-1, etc.) formed in the body under the influence of microbes, viruses, toxins (mainly PG-E2);

G) play an important physiological role in the protection of the mucous membrane of the gastrointestinal tract(increased secretion of mucus and alkali; preservation of the integrity of endothelial cells within the microvessels of the mucosa, contributing to the maintenance of blood flow in the mucosa; preservation of the integrity of granulocytes and, thus, the preservation of the structural integrity of the mucosa);

e) affect kidney function: cause vasodilation, maintain renal blood flow and glomerular filtration rate, increase renin release, sodium and water excretion, participate in potassium homeostasis.

There are at least two cyclooxygenase isoenzymes that are inhibited by NSAIDs (Fig. 2). The first isoenzyme, COX-1, controls the production of PGs that regulate the integrity of the gastrointestinal mucosa, platelet function, and renal blood flow, and the second isoenzyme, COX-2, is involved in the synthesis of PGs during inflammation. Moreover, COX-2 is absent under normal conditions, but is formed under the influence of some tissue factors that initiate an inflammatory reaction (cytokines and others). In this regard, it is assumed that the anti-inflammatory effect of NSAIDs is due to inhibition of COX-2, and their undesirable reactions - inhibition of COX-1.

Recently, additional studies of COX-2 have been carried out and it has been established that pro-inflammatory activity may be inherent in COX-2, and anti-inflammatory properties in the third isomer of COX-COX-3. Like other COX enzymes, COX-3 is also involved in the synthesis of prostaglandins and plays a role in the development of pain and fever. However, unlike COX-1 and COX-2, COX-3 is not involved in the development of inflammation. COX-3 activity is inhibited by paracetamol, which has little effect on COX-1 and COX-2. However, it should be noted that COX-3 was found in the tissues of experimental animals and the existence of this isoform of COX in the human body requires proof, as well as further study and evidence of the mechanism of action of paracetamol associated with the inhibition of COX-3.

The ratio of the activity of NSAIDs in terms of blocking COX-1 / COX-2 makes it possible to judge their potential toxicity. The smaller this value, the more selective the drug is for COX-2 and thus less toxic. For example, for meloxicam it is 0.33, diclofenac - 2.2, tenoxicam - 15, piroxicam - 33, indomethacin - 107.

The data indicate that NSAIDs not only inhibit cyclooxygenase metabolism, but also actively influence PG synthesis associated with Ca ++ mobilization in smooth muscles. Thus, butadione inhibits the conversion of cyclic endoperoxides into prostaglandins E2 and F2 λ , and fenamates can also block the reception of these substances in tissues.

An important role in the anti-inflammatory action of NSAIDs is played by their influence on the metabolism and bioeffects of kinins. In therapeutic doses, indomethacin, orthophene, naproxen, ibuprofen, acetylsalicylic acid (ASA) reduce the formation of bradykinin by 70-80%. This effect is based on the ability of NSAIDs to provide nonspecific inhibition of the interaction of kallikrein with high molecular weight kininogen. NSAIDs cause chemical modification of the components of the kininogenesis reaction, as a result of which, due to steric hindrance, the complementary interaction of protein molecules is disrupted and effective hydrolysis of high-molecular kininogen by kallikrein does not occur. A decrease in the formation of bradykinin leads to inhibition of the activation of λ-phosphorylase, which leads to a decrease in the synthesis of arachidonic acid and, as a result, the manifestation of the effects of its metabolic products.

Important is the ability of NSAIDs to block the interaction of bradykinin with tissue receptors, which leads to the restoration of disturbed microcirculation, a decrease in capillary hyperextension, a decrease in the release of the liquid part of the plasma, its proteins, pro-inflammatory factors and formed elements, which indirectly affects the development of other phases of the inflammatory process. Since the kallikrein-kinin system plays the most important role in the development of acute inflammatory reactions, the NSAIDs are most effective in early stages inflammation, in the presence of a pronounced exudative component.

Inhibition of the release of histamine and serotonin, blockade of tissue reactions to these biogenic amines, which play a significant role in the inflammatory process, have a certain significance in the mechanism of the anti-inflammatory action of NSAIDs. The intramolecular distance between the reaction centers in the molecule of antiphlogistics (compounds of the butadione type) approaches those in the molecule of inflammatory mediators (histamine, serotonin). This suggests the possibility of competitive interaction of the mentioned NSAIDs with receptors or enzyme systems involved in the processes of synthesis, release and transformation of these substances.

As mentioned above, NSAIDs have a membrane-stabilizing effect. By binding to the G-protein in the cell membrane, antiphlogistics affect the transmission of membrane signals through it, inhibit the transport of anions, and affect biological processes that depend on the overall mobility of membrane lipids. They realize their membrane-stabilizing effect by increasing the microviscosity of membranes. Penetrating through the cytoplasmic membrane into the cell, NSAIDs also affect the functional state of the membranes of cell structures, in particular lysosomes, and prevent the pro-inflammatory effect of hydrolases. Data were obtained on the quantitative and qualitative features of the affinity of individual drugs for the protein and lipid components of biological membranes, which can explain their membrane effect.

One of the mechanisms of damage to cell membranes is free radical oxidation. Free radicals generated during lipid peroxidation (LPO) play an important role in the development of inflammation. Therefore, the inhibition of NSAID peroxidation in membranes can be considered as a manifestation of their anti-inflammatory action. One of the main sources of free radical generation is the metabolism of arachidonic acid. Individual metabolites of its cascade cause the accumulation of polymorphonuclear neutrophils and macrophages in the focus of inflammation, the activation of which is also accompanied by the formation of free radicals. NSAIDs, by acting as scavengers for these compounds, offer a new approach to the prevention and treatment of tissue damage caused by free radicals.

In recent years, studies of the effect of NSAIDs on the cellular mechanisms of the inflammatory response have received significant development. NSAIDs reduce cell migration to the site of inflammation and reduce their phlogogenic activity, and the effect on polymorphonuclear neutrophils correlates with inhibition of the lipoxygenase pathway of arachidonic acid oxidation. This alternative pathway for the conversion of arachidonic acid leads to the formation of leukotrienes (LTs), which meet all the criteria for inflammatory mediators. Benoxaprofen has the ability to influence 5-lipoxygenase and block the synthesis of LT.

Less studied is the effect of NSAIDs on the cellular elements of the late stage of inflammation - mononuclear cells. Some NSAIDs reduce the migration of monocytes that produce free radicals and causing tissue destruction. Although the important role of cellular elements in the development of the inflammatory response and the therapeutic effect of anti-inflammatory drugs is undoubted, the mechanism of action of NSAIDs on the migration and function of these cells remains to be elucidated.

There is an assumption about the release of NSAIDs of natural anti-inflammatory substances from the complex with plasma proteins, which comes from the ability of these drugs to displace lysine from albumin.

MAIN EFFECTS OF NSAIDs

Anti-inflammatory effect

The severity of the anti-inflammatory properties of NSAIDs correlates with the degree of COX inhibition. The following order of activity was noted: meclofenamic acid, supprofen, indomethacin, diclofenac, mefenamic acid, flufenamic acid, naproxen, phenylbutazone, acetylsalicylic acid, ibuprofen.

NSAIDs suppress predominantly the exudation phase. The most powerful drugs (indomethacin, diclofenac, phenylbutazone) also act on the proliferation phase (reducing collagen synthesis and associated tissue sclerosis), but weaker than on the exudative phase. NSAIDs have practically no effect on the alteration phase. In terms of anti-inflammatory activity, NSAIDs are inferior to glucocorticoids., which, by inhibiting the enzyme phospholipase A2, inhibit the metabolism of phospholipids and disrupt the formation of both prostaglandins and leukotrienes, which are also the most important mediators of inflammation.

The distribution of NSAIDs according to the severity of anti-inflammatory activity is presented in table 1. Among the NSAIDs of the first group, indomethacin and diclofenac have the most powerful anti-inflammatory activity, and the least ibuprofen.

Analgesic effect

The mechanism of analgesic action consists of several components, each of which can have independent significance.

Some PGs (E2 λ and F2 λ) can increase the sensitivity of pain receptors to physical and chemical stimuli, for example, to the action of bradykinin, which in turn promotes the release of PGs from tissues. Thus, there is a mutual strengthening of the algogenic action. NSAIDs, blocking the synthesis of PG-E2 and PG-F2 λ , in combination with a direct anti-bradykinin action, prevent the manifestation of the algogenic effect.

Although NSAIDs do not act on pain receptors, by blocking exudation and stabilizing lysosome membranes, they indirectly reduce the number of receptors sensitive to chemical stimuli. A certain importance is attached to the influence of this group of drugs on the thalamic centers of pain sensitivity (local blocking of PG-E2, F2 λ in the CNS), which leads to inhibition of the conduction of pain impulses to the cortex. According to the analgesic activity of diclofenac, indomethacin in relation to inflamed tissues is not inferior to the activity of narcotic analgesics, in contrast to which, NSAIDs do not affect the ability of the central nervous system to sum up subthreshold irritations.

The analgesic effect of NSAIDs, to a greater extent, is manifested in pain of mild and moderate intensity, which are localized in the muscles, joints, tendons, nerve trunks, as well as in headache or toothache. With severe visceral pain associated with trauma, surgery, tumors, most NSAIDs are not very effective and are inferior in strength to narcotic analgesics. A number of controlled studies have shown a fairly high analgesic activity of diclofenac, keterolac, ketoprofen, metamizole in colic and postoperative pain. The effectiveness of NSAIDs in renal colic that occurs in patients urolithiasis, is largely associated with: inhibition of PG-E2 production in the kidneys, a decrease in renal blood flow and urine formation. This leads to a decrease in pressure in the renal pelvis and ureters above the site of obstruction and provides a long-term analgesic effect.

According to the new hypothesis, the therapeutic effect of NSAIDs can be partly explained by their stimulating effect on the production of endogenous regulatory peptides that have an analgesic effect (such as endorphins) and reduce the severity of inflammation.

The advantage of NSAIDs over narcotic analgesics is that they do not depress the respiratory center, do not cause euphoria and drug dependence, and for colic, the fact that they do not have a spasmodic effect is also important.

Comparison of selective analgesic activity, in relation to the degree of suppression of prostaglandin synthesis, showed that some NSAIDs with strong analgesic properties are weak inhibitors of prostaglandin synthesis, and vice versa, other NSAIDs that can actively inhibit prostaglandin synthesis have weak analgesic properties. Thus, there is a dissociation between the analgesic and anti-inflammatory activity of NSAIDs. This phenomenon is explained by the fact that the analgesic effect of some NSAIDs is associated not only with the suppression of central and peripheral prostaglandins, but also with the effect on the synthesis and activity of other neuroactive substances that play a key role in the perception of pain stimulation in the CNS.

The most well studied central analgesic action Ketoprofen, which is due to:

The ability to quickly penetrate the blood-brain barrier (BBB) ​​due to its exceptional fat solubility;

The ability to exert a central effect at the level of the posterior columns of the spinal cord by inhibiting the depolarization of neurons in the posterior columns;

The ability to selectively block NMDA receptors by suppressing the depolarization of ion channels, thus providing a direct and fast action to the transmission of pain. This mechanism is due to the ability of ketoprofen to stimulate the activity of the hepatic enzyme tryptophan-2,3-dioxygenase, which directly affects the formation of kynurenic acid, an antagonist of NMDA receptors in the central nervous system;

The ability to act on the heterotrimeric G-protein, changing its configuration through its competitive replacement in the areas of action. G-protein, located in the postsynaptic neuronal membrane, binds to various receptors, such as neurokinins (NK1, NK2, NK3) and glutamate receptors, which facilitate the passage of afferent pain signals across the membrane;

The ability to control the levels of certain neurotransmitters such as serotonin (through effects on G-protein and the serotonin precursor 5-hydroxytryptamine), to reduce the production of substance P.

Attempts to rank NSAIDs according to the severity of the analgesic effect have been carried out for a long time, however, due to the fact that the effects of many drugs are dose-dependent, and there is still no single standard for the possible assessment of their effectiveness in various clinical conditions, this question remains extremely difficult. One of the possible ways to solve it is to summarize the data of various publications indirectly related to each other for individual drugs. As a result of this study, a comparative characteristic of the analgesic effect of the most commonly used NSAIDs in the clinic was derived: ketorolac 30 mg > (ketoprofen 25 mg = ibuprofen 400 mg; flurbiprofen 50 mg) > (ASA 650 mg= paracetamol 650 mg = fenoprofen 200 mg = naproxen 250 mg = etodolac 200 mg = diclofenac 50 mg = mefenamic acid 500 mg) > nabumetone 1000 mg.

Based on the above data, a higher analgesic activity of propionic acid derivatives (ketoprofen, ibuprofen, flubiprofen) can be noted. The most powerful analgesic effect is shown by ketorolac (30 mg of ketorolac administered intramuscularly is equivalent to 12 mg of morphine).

Antipyretic effect

The starting link of the hyperthermic reaction is exogenous pyrogens (bacteria, viruses, toxins, allergens, medicines), which, when they enter the body, affect the thermal center of the hypothalamus through fever mediators. The first and most important is the endogenous pyrogen, a low molecular weight protein produced by leukocytes (monocytes, macrophages) after being activated by lymphokines. Endogenous pyrogen is specific for fever and acts on thermosensitive neurons in the preoptic region of the hypothalamus, where synthesis of PG-E1, E2 is induced with the participation of serotonin.

The second large group of fever mediators are non-specific, but very active neurotransmitters released in the brain and ensuring the activity of neurons in the nuclei of the hypothalamus and other structures that organize the processes of switching thermoregulation to a higher level. These include acetylcholine, serotonin, histamine, PG-E, and other neurotransmitters. PG-E, as a phosphodiesterase inhibitor, causes the accumulation of cAMP in thermosensitive cells, which contributes to an increased entry of Ca ++ into cells. This process leads to an increase in the sensitivity of cells to acetylcholine and an increase in their electrical activity. Excitation is transmitted to the nerve cells of the posterior hypothalamus, which leads, on the one hand, to an intensification of heat production, and, on the other hand, to peripheral vasoconstriction and a decrease in heat transfer, which generally leads to fever.

The essence of the antipyretic action of NSAIDs is reduced to inhibition of the transmission of excitation in the nuclei of the hypothalamus (which is established electrophysiologically and biochemically). Electrophysiologically showed a decrease in the flow of impulses from thermal receptors and, accordingly, a decrease in the "reference point" of this parameter. A pronounced inhibitory effect of salicylates on the postsynaptic potential in different parts of the brain was found. NSAIDs, inhibiting PG in the hypothalamus, reduce their effect on cAMP and block the entire cascade of reactions described above, which leads to an increase in heat transfer and a decrease in heat generation. Since PGs are not involved in maintaining normal body temperature, NSAIDs do not affect the value of normal temperature, which is how they differ from "hypothermic" drugs (chlorpromazine and others). The exceptions are amidopyrine and phenacetin, which have a hypothermogenic effect.

The inhibitory effect of NSAIDs on thermoregulation is also expressed in a decrease in the release of serotonin, adrenaline, and acetylcholine by the cells of the hypothalamus. The antipyretic effect of NSAIDs can be partially explained by their inhibitory effect on the synthesis in phagocytes, monocytes and reticulocytes of endogenous pyrogens and proteins with a molecular weight of 10-20 thousand.

There is an assumption that the antipyretic effect of some NSAIDs should be considered as the result of competitive antagonism of these drugs and PGs on the hypothalamic receptors.

Antiaggregatory effect

When using NSAIDs as antiplatelet agents, it should be borne in mind that different drugs may not have the same effect on aggregation, due to differences in the nature of COX inhibition. According to the mechanism of interaction with COX, 3 groups of NSAIDs are distinguished:

1. Drugs that cause slow and reversible competitive inhibition of the enzyme: indomethacin, voltaren.

2. Drugs causing slow and irreversible inhibition of the enzyme: salicylates.

3. Drugs that cause rapid reversible and competitive inhibition of the enzyme: brufen, naproxen, butadione.

These data, in addition to theoretical interest, are of great practical importance. It is known that after a single dose of ASA, a clinically significant decrease in platelet aggregation is observed for 48 hours or more. When using indomethacin, this process occurs in parallel with a decrease in the concentration of the drug in the blood. This is explained by the fact that ASA irreversibly inhibits the enzyme by its acetylation, and platelets, in contrast to endotheliocytes, being nuclear-free cells, lack the ability to synthesize proteins, including enzymes.

Thus, the synthesis of thromboxane A2 is restored only due to the appearance of new populations of platelets from the bone marrow (platelet lifespan is 7 days), while the initial level of prostacyclin is restored as new portions of COX are synthesized by existing endotheliocytes. As a result, ASA causes a shift in the balance between thromboxane A2 and prostacyclin in favor of the latter, which leads to a decrease in platelet aggregation.

It should be emphasized that only small doses of ASA (50 mg - 350 mg per day) "subtly", but clearly violate the parity of the effects of thromboxane A2 and prostacyclin. High doses of ASA "roughly", non-selectively inhibit the synthesis of both thromboxane A2 and prostacyclin, while increasing fibrinolysis and reducing the synthesis of fibrinogen and vitamin K - dependent coagulation factors in the liver. ASA does not affect the lifespan of platelets.

When using reversible COX inhibitors (all NSAIDs except salicylates), as their concentration in the blood decreases, the aggregation ability of circulating platelets is restored.

Along with the above properties, NSAIDs have a number of other effects.

Influence on the immune system. A number of NSAIDs (indomethacin, butadione, naproxen, ibuprofen) inhibit the transformation of lymphocytes (caused by various antigens), and therefore their immunosuppressive effect is manifested. Secondary immunosuppressive action is also determined by:

A decrease in capillary permeability, which makes it difficult for immunocompetent cells to contact the antigen, antibodies with the substrate;

Stabilization of lysosomal membranes in macrophages, which limits the breakdown of poorly soluble antigens necessary for the development of the next stages of the immune response.

Desensitizing action develops due to:

Reducing the content of PG-E2 and leukocytes in the focus of inflammation, which inhibits the chemotaxis of monocytes;

Inhibition of the formation of hydroheptanotrenic acid, which reduces the chemotaxis of T-lymphocytes, eosinophils and polymorphonuclear leukocytes in the focus of inflammation;

Inhibition of blast transformation of lymphocytes, which requires PG.


Anti-inflammatory drugs for joints are the main treatment for diseases of cartilage and connective tissue. They slow down the progression of the disease, help fight exacerbations, relieve painful symptoms. The scheme of taking the drug can be different - they are taken in courses, or as needed to alleviate the condition. Non-steroidal anti-inflammatory drugs (NSAIDs) are produced in various dosage forms - ointments and gels for local application, tablets and capsules, as well as injectable preparations for intraarticular administration.

Anti-inflammatory drugs (NSAIDs) - the principle of action

This group of drugs is very extensive, but they all have in common general principle actions. The essence of this process is that non-steroidal anti-inflammatory drugs for the treatment of joints interfere with the mechanism of the formation of the inflammatory process. The enzyme cyclooxygenase is responsible for the synthesis of so-called inflammatory mediators. It is she who is inhibited by drugs from the NSAID group, interrupting the chain of development of the inflammatory reaction. They prevent pain, fever and local swelling.

But there is another important feature action of non-steroidal anti-inflammatory drugs. There are two types of cyclooxygenase enzyme. One of them (COX-1) is involved in the synthesis of inflammatory mediators, and the second (COX-2) is involved in the synthesis of the protective layer of the stomach wall. NSAIDs act on both types of this enzyme, causing both of them to be inhibited. This explains the side effect common to these drugs, which consists in damage to the mucous membrane of the digestive organs.

According to their effect on COX-2 drugs are divided into selective and non-selective. The development of new NSAIDs aims to increase the selectivity of their effect on COX-1 and eliminate the effect on COX-2. Currently, a new generation of NSAIDs has been developed, which have almost complete selectivity.

The three main therapeutic effects of drugs in this group are anti-inflammatory, antipyretic and analgesic. In diseases of the joints, it is the anti-inflammatory effect that comes to the fore, and the analgesic effect is no less significant. The antipyretic effect is less important and practically does not manifest itself in the new generation of anti-inflammatory nonsteroidal drugs that are used to treat joint diseases.

Classification of anti-inflammatory drugs

Taking into account the features of the structure active ingredient All NSAIDs can be divided into several groups:

Non-selective NSAIDs (affect mainly COX-1)

These include the following tools:

  • Aspirin;
  • Ketoprofen;
Non-selective NSAIDs (equally affecting COX-1 and COX-2).
  • Lornoxicam;
  • Lorakam.
Selective NSAIDs (inhibit COX-2)
  • Celecoxib;
  • Meloxicam;
  • Nimesulide;
  • Rofecoxib.

Some of these drugs have a strong anti-inflammatory effect, others are more antipyretic (Aspirin, Ibuprofen) or analgesic (Ketorolac) effect.

Indications for the use of NSAIDs

knee arthritis is one of the causes

In diseases of the joints, nonsteroidal drugs are prescribed according to several schemes, depending on the dosage form and the stage of the disease. The list of diseases for which NSAIDs are prescribed is quite long - these are arthritis of various etiologies, including autoimmune, most arthrosis, the recovery period after injuries of the joints and muscular apparatus.

With an exacerbation chronic diseases joints, non-steroidal anti-inflammatory drugs are used in combination. They are prescribed in the form of a course of tablets and ointments, in a serious condition, the treatment is supplemented by intra-articular injections. Outside of exacerbation and in acute conditions, they are used as needed if symptoms of inflammation of the joints occur.

Side effects

Non-steroidal anti-inflammatory drugs have many side effects, so be sure to read the instructions before taking them. The most common side effects are:

  • provocation of a stomach or duodenal ulcer,
  • dyspepsia,
  • dysfunction nervous system,

They are especially pronounced in medicines in tablets, suppositories and solutions for intramuscular injections. Local funds(ointments and intra-articular injections) do not have such an effect.

Another common group of side effects is the effect on the hematopoietic system. NSAIDs have a blood-thinning effect, and this effect must be taken into account when taking these drugs so as not to harm your health. A more dangerous effect on the blood system is expressed in the inhibition of hematopoietic processes. It is manifested by a gradual decrease in the number of formed elements in the blood - first anemia develops, then - thrombocytopenia, subsequently - pancytopenia.

In addition, there are other side effects caused by the chemical characteristics of the drugs, they are indicated in the instructions for use. Due to the large number of side effects, you should consult your doctor before taking NSAIDs for the treatment of joints.

Contraindications

Contraindications to the use of NSAIDs in diseases of the joints stem from their side effects and relate primarily to tablet forms. They are not prescribed to patients during an exacerbation of diseases of the gastrointestinal tract, as well as to patients with diseases of the blood system - anemia of various origins, clotting disorders, leukemia and leukemia.

NSAIDs should not be administered simultaneously with drugs that reduce blood clotting (heparin), and it is also not recommended to take the same drug in different dosage forms - this leads to increased side effects. First of all, this applies to drugs containing ibuprofen and diclofenac.

In addition, it is possible to develop an allergic reaction to drugs of the NSAID group. Its intensity is not related to the dosage form, and appears with the same frequency when taking tablets, using ointments and injecting into the joints. Sometimes allergies can take very severe forms, for example, aspirin asthma - an asthmatic attack when using the drug. An allergic reaction to NSAIDs can be cross-reactive, so care should be taken when taking drugs.

Ointments with NSAIDs for joint diseases

Ointments are the most common dosage form used for joint pain. Their popularity is due to the fact that the effect of the ointment comes quickly enough, and the side effects are minimal. The ointment can be used to relieve acute pain and in recovery period after injury. But if a course of injections is prescribed, then the ointments are usually canceled.

The most popular drugs in the form of ointments are Diclofenac and preparations based on it (Voltaren), Dolobene, and others. Most of them can be bought at the pharmacy without a doctor's prescription. You can use such products for a long time without harm to health.

Non-steroidal anti-inflammatory drugs in tablets for diseases of the joints

NSAIDs in tablets are prescribed for joint damage, osteochondrosis, systemic connective tissue diseases with articular syndrome. They are used in courses, several times a year, prescribed in the acute period. But the main task of NSAID tablets is to prevent the exacerbation of diseases.

This dosage form is most effective for the treatment of diseases of the joints and spine, but has the greatest number of contraindications. In addition to the conditions listed above, tablets containing NSAIDs should not be used for liver diseases - fibrosis, cirrhosis, hepatitis, liver failure. In diseases of the kidneys, accompanied by a decrease in the filtration rate, a reduction in dosage or frequency of administration is required.

A complete list of anti-inflammatory drugs can be found on Wikipedia. Among the most famous of them is Diclofenac in tablets. Of more modern drugs new generation - Xefocam, Celecoxib and Movalis. New drugs are safer, but have another negative point - high cost. Tablets should be taken after meals or with meals.

NSAIDs in solutions for intra-articular injections

This dosage form is prescribed for severe course diseases and for the relief of severe exacerbations. It is used by courses that are held only in a medical institution. Intra-articular injections allow the most effective delivery of the active substance to the site of inflammation. But they require high qualifications from the doctor who conducts them, since they are associated with a risk of damage to the ligament of the joint.

Diclofenac, Movalis, Ksefokam and other drugs are available in injectable form. They are used to treat lesions of large joints, most often the knee, less often the elbow. Intra-articular injections are not prescribed for lesions of the joints of the hands and feet, as well as for diseases of the spine. This is due to the fact that the technical difficulties of administering the drug make this method of treatment almost impossible.

Intra-articular injections are considered a rather complex medical manipulation, and must be carried out in a treatment room, as they require sterility to avoid infection and highly qualified medical staff.

List of the best anti-inflammatory drugs

Let us consider in more detail the features of the use of the most popular drugs from the NSAID group.

(Voltaren, Naklofen, Olfen, Diklak, etc.)

Diclofenac and preparations based on it are produced in the form of tablets, capsules, ointments, gels, suppositories, injection solutions. These drugs exhibit a powerful anti-inflammatory effect, quickly relieve pain, lower the temperature and alleviate the patient's condition. A high concentration of the active ingredient in the blood is noted within 20 minutes after taking the drug.

Like most drugs from the NSAID group, they have a negative effect on the gastrointestinal tract, I have a fairly extensive list of contraindications and side effects, so they should be used only as directed by a doctor, in short courses. Standard daily dose Diclofenac in tablets for adult patients - 150 mg, it is divided into 2-3 doses. Local forms (ointments, gels) are applied to the affected area with a thin layer up to 3 times a day.

Indomethacin (Metindol)

It has the same therapeutic effect as Diclofenac. Available in the form of tablets, capsules, ointment, gel, rectal suppositories. But this drug has many more pronounced side effects, so it is now rarely used, giving preference to more modern drugs.

A drug from the group of oxycams, with a pronounced analgesic, anti-inflammatory and antipyretic effect. Available in the form of capsules, tablets, ointments, creams, suppositories. It is used to treat gout, arthritis, joint and muscle pain, as well as in preparation for the IVF procedure.

Like other NSAIDs, it has an extensive list of side effects associated with damage to the digestive tract, impaired hematopoiesis, and reactions from the nervous system. Therefore, the drug should be used only as directed by a doctor. The analgesic effect of taking Piroxicam tablets persists throughout the day. The standard dose of the drug for an adult is up to 40 mg per day.

Lornoxicam (Xefocam, Lorakam, Larfix)

The drug has a pronounced anti-inflammatory effect, quickly copes with excruciating pain syndrome. Does not show antipyretic action. The drug is used to treat postoperative pain, algomenorrhea, in the treatment of osteoarthritis and rheumatoid arthritis.

Available in the form of tablets and powder, intended for the preparation of a solution for injection. The recommended dose for oral administration is up to 4 tablets per day in 2 divided doses. For injection into a muscle or vein, a single dose of the drug is 8 mg, the solution is prepared immediately before administration.

When using the drug, the likelihood of complications in people with gastroenterological pathologies increases, therefore, the drug is not used for diseases of the gastrointestinal tract, as well as during pregnancy, lactation, pathologies of the heart, liver and in childhood.

Meloxicam (Movalix, Revmoxicam, Melox)

Drugs based on enolic acid belong to the class of selective COX-2 inhibitors. In this regard, they cause fewer side effects from the digestive system and do not provoke toxic injury kidneys and liver. Meloxicam tablets, rectal suppositories and injections in ampoules are produced.

Indications for the use of the drug are diseases of the joints of an inflammatory and degenerative nature with a pronounced pain syndrome - spondyloarthritis, osteoarthrosis and arthritis. As a rule, in the first days of treatment, the drug is used in the form of intramuscular injections, after the acute inflammatory process subsides, they switch to taking Meloxicam in tablet form (1 tablet twice a day).

Nimesulide (Nimesil, Nimesin, Remesulide)

The drug belongs to the group of highly selective COX-2 inhibitors, has a powerful anti-inflammatory effect, which is complemented by antipyretic and analgesic properties. Nimesulide is produced in the form of tablets, granules for suspension and in the form of a gel for topical use. A single dose of the drug in tablets is 100 mg, taken twice a day.

The gel is applied to the affected area several times a day (3-4), lightly rubbing. Suspension with a pleasant orange flavor can be prescribed to children from 12 years of age. The drug is intended for the treatment of post-traumatic and postoperative pain, degenerative joint lesions (accompanied by inflammation), bursitis, tendonitis.

In addition, Nimesulide is prescribed for atralgia, myalgia, painful periods, as well as for the relief of headache and toothache. The drug can have a toxic effect on the liver and kidneys, therefore, in diseases of these organs, the dose of the drug must be reduced.

Celecoxib (Revmroxib, Celebrex)

A drug from the coxibs group, used in the treatment of inflammatory diseases of the joints, acute pain syndrome, menstrual pains. Available in the form of capsules, which may contain 100 or 200 mg of the active substance. It shows a pronounced analgesic and anti-inflammatory effect, while, if not exceeding the therapeutic dose, it has practically no negative effect on the gastrointestinal mucosa.

The maximum allowable daily dose of the drug is 400 mg divided into 2 doses. With prolonged use of Celecoxib in high doses, side effects develop - ulceration of the mucous membrane, disorders of the hematopoietic system and other undesirable reactions from the nervous, cardiovascular and urinary system.

(Zerodol)

The action of the drug is similar to Diclofenac, it is available in the form of tablets containing 100 mg of the active substance. Adults are advised to take 1 tablet twice a day. The drug is intended for the treatment of gout, arthritis of various etiologies, osteoarthritis and spondylitis.

This medication is much less likely than other NSAIDs to provoke erosive lesions of the gastrointestinal tract, but its administration may be accompanied by a number of side effects from the digestive, nervous, hematopoietic, respiratory system. With extreme caution, the drug is prescribed for pathologies of the liver, kidneys, diabetes mellitus, ischemia, arterial hypertension and other conditions, a list of which is given in the instructions for the drug.

Rofecoxib

This modern facility from the category of highly selective COX-2 inhibitors, which have practically no negative effect on the gastrointestinal mucosa and kidneys. It is used as a strong analgesic and anti-inflammatory agent for most inflammatory and degenerative lesions of the musculoskeletal system. In addition, the medication is prescribed for migraine, neuralgia, lumbago, osteochondrosis, pain syndrome with muscle and ligament injuries.

This universal tool is often included in the scheme complex treatment thrombophlebitis, diseases of the genitourinary system, used in ophthalmology, in diseases of the ENT organs or in dental problems (stomatitis, pulpitis). With severe pain syndrome, you can take up to 4 tablets at a time. With caution, the drug is prescribed for bronchial asthma, on the early dates pregnancy, during lactation. This medication has much fewer contraindications and side effects than other anti-inflammatory drugs.

Combined NSAIDs

New generation anti-inflammatory drugs combine a combination of an active ingredient with vitamins or other active ingredients that enhance their therapeutic effect. We present to your attention a list of the most popular drugs of combined action:

  • Flamidez (diclofenac + paracetamol);
  • Neurodiclovit (diclofenac + vitamins B1, B6, B12);
  • Olfen-75 (diclofenac + lidocaine);
  • Diclocaine (lidocaine + diclofenac in low dosage);
  • Dolaren gel (diclofenac + flax oil + menthol + methyl salicylate);
  • Nimid Forte (nimesulide + tizanidine);
  • Alit (soluble tablets containing nimesulide and muscle relaxant dicycloverine);

This is not a complete list of combined anti-inflammatory drugs that are used to treat joints and degenerative lesions of the musculoskeletal system. For each patient, the doctor selects a treatment regimen individually, taking into account many factors. Drugs from the NSAID group have many contraindications and can cause a number of undesirable side reactions from various bodies and systems.

Therefore, you can not self-medicate! Only a specialist can recommend the best remedy, taking into account clinical picture diseases, severity of symptoms, comorbidities and determine the required dosage of the drug and the duration of the course of treatment. This will help to avoid unwanted complications, will alleviate the patient's condition and speed up recovery.

Who to contact?

Depending on the nature of the pathology, the following specialists can deal with the treatment of a patient with joint diseases: a neurologist, a general practitioner, an orthopedist or a rheumatologist. It is these doctors who have the right to prescribe drugs from the NSAID group for the treatment of specialized diseases.

If the intake of anti-inflammatory drugs has led to the occurrence of adverse reactions, such narrow specialists as a gastroenterologist, cardiologist, allergist, nephrologist can join the treatment of the patient. If the patient is forced to take NSAIDs for a long time, be sure to consult a nutritionist and choose the best diet that will protect the gastric mucosa from damage.