Co-author, editor and medical expert – Petrashevich Anna Aleksandrovna.
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Last updated date: 08/26/2021
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How NSAIDs work When NSAIDs are needed When NSAIDs are contraindicated Non-steroidal anti-inflammatory drug Motrin®
NSAIDs (non-steroidal anti-inflammatory drugs) or NSAIDs (non-steroidal anti-inflammatory drugs) are one of the most popular drug groups in medicine. Their advantage is their complex action (antipyretic, anti-inflammatory and analgesic), as well as a wide range of indications for which they can be used. But what are these drugs, when can they be used and what is their analgesic effect based on?
How do NSAIDs work?
Non-steroidal anti-inflammatory drugs contain substances that cause anti-inflammatory, analgesic and antipyretic effects.
Pain, inflammation, increased body temperature are the result of a number of chemical reactions in the body that occur under the influence of some factor (infection, injury, dysfunction of internal organs, etc.). But if you exclude any link from this chain of reactions, it is interrupted - the mechanism for the formation of pain and inflammation is disrupted. This is precisely the principle of action of NSAIDs: they block the synthesis of prostaglandins - substances that play an important role in the development of inflammatory processes and pain.
It is this combination – anti-inflammatory, analgesic and antipyretic effects – that has made NSAIDs one of the most popular medications today. After all, many diseases are accompanied by fever, pain and inflammation. These agents are usually distributed depending on the severity of anti-inflammatory activity and the chemical structure of the active substance, duration of action and selectivity.
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SELECTIVE NON-STEROID ANTI-INFLAMMATORY DRUGS
Preferanskaya Nina Germanovna Associate Professor, Department of Pharmacology, Educational Department, Institute of Pharmacy and Translational Medicine, Multidisciplinary Center for Clinical and Medical Research, International School “Medicine of the Future”, First Moscow State Medical University. THEM. Sechenov (Sechenov University), Ph.D.
Recurrent pain leads to disability in up to 80% of patients. In patients over 50 years of age, in 17% of cases, pain syndrome is caused by chronic diseases in the lumbar region, including degenerative lesions of the intervertebral cartilaginous discs, in 57% of cases degenerative changes in the spine are detected, 28% suffer from osteoarthritis, 6% from spondylolisthesis (displacement of the vertebrae relative to each other ), 1% - rheumatoid arthritis.
Selective NSAIDs have pronounced anti-inflammatory, anti-edematous and analgesic (painkiller) effects.
The main indications for the use of selective NSAIDs are: osteoarthritis, rheumatoid arthritis, acute arthritis in non-rheumatic diseases, ankylosing spondylitis, acute and chronic pain in the lower back, exacerbation of chronic joint diseases, as well as diseases of extra-articular and soft tissues.
They are indispensable for various sprains, bruises, arthrosis, and are effective for chronic pain due to inflammation, pain in the postoperative period, cramping pain and those associated with dysmenorrhea.
Under conditions of development of the inflammatory process, the synthesis and enzymatic activity of cyclooxygenase-2 (COX-2) is induced. With the help of this enzyme, an excess amount of inflammatory mediators (histamine, kinins) is formed at the site of inflammation, which dilate blood vessels, increase the permeability of the vascular wall, and sensitize nociceptors to bradykinin and histamine. The main mechanism of action of selective NSAIDs is the selective inhibition of the COX-2 enzyme, which is an inducible (adaptive, regulated) enzyme.
At therapeutic doses, selective cyclooxygenase inhibitors predominantly inhibit the inflammation-induced COX-2 isoform and have virtually no effect on the other COX-1 isoform. COX-2 begins to function only during inflammation under the influence of immune mediators (cytokines). When inhibited, the synthesis of prostaglandins involved in inflammation, cell proliferation and destruction is suppressed. Prostaglandins and related biologically active compounds (eicosanoids) and other inflammatory mediators affect the hemodynamics of the kidneys, water-salt and fat metabolism, stimulate the movement of leukocytes to the area of inflammation and phagocytosis of foreign compounds, etc. Nerve cell receptors receive fewer irritating signals and pain subsides , decreases.
The main undesirable side effects when using selective NSAIDs are: dizziness, drowsiness, headache, fatigue, increased heart rate (tachycardia), slight shortness of breath, dry cough, indigestion, the appearance of protein in the urine, increased activity of liver enzymes and skin rash (spotted).
It is worth noting that these drugs exhibit less undesirable side effects from the gastrointestinal tract (vomiting, belching, diarrhea, bleeding, ulceration of the mucous membrane, ulcerogenic effect): the active substance is in a special shell - film-coated capsules or tablets are made from substances that do not dissolve in the acidic environment of the stomach. These coatings are enteric-soluble and begin to degrade only when they enter the intestines, which can significantly reduce the irritating effect of drugs on the gastric mucosa.
Due to the decrease in the activity of histamine and bradykinin, the manifestations of allergic reactions decrease. The drugs reduce the function of the urinary system to a lesser extent, which in turn reduces the occurrence of edema and increased blood pressure.
New generation drugs - highly selective NSAIDs - do not have a destructive effect on cartilage tissue and are chondroneutral. With their use, it was possible to minimize the effect on the blood coagulation system and platelet function.
As a result of the above, the tolerability of the use of selective NSAIDs improves and with their long-term use, unwanted side effects occur much less frequently. All this increases patient adherence to the use of selective NSAIDs, creates high compliance and the patient’s willingness to strictly follow the doctor’s recommendations.
Classification of non-steroidal selective agents of reversible action NSAIDs:
1. Highly selective reversible COX-2 inhibitors “ K oxybs”
- fluorinated derivative of benzenesulfonamide - Celecoxib (Celebrex);
- chlorinated pyridine derivative of phenylsulfone - Etoricoxib (Arcoxia).
2. Predominantly selective reversible COX-2 inhibitors “ Oxycams”
- thiazole derivative of benzothiazine carboxamide - Meloxicam (Movalis, Mirlox).
3. Selective reversible inhibitors of COX-2
- methanesulfonamide derivative: Nimesulide (Nise, Nimulid).
Celecoxib Celecoxib , substance) - TN "Celebrex" (caps. 100 mg, 200 mg), TN "Dilaxa" (caps. 200 mg), TN "Roukoxisib-Routek" (caps. 200 mg) - highly selective COX inhibitor 2, a fluorinated benzenesulfonamide derivative - effectively relieves pain in degenerative joint pathologies. The mechanism of analgesic action is based on inhibition of the synthesis and production of prostaglandins E1 and E2, which play an important role in the development of the inflammatory process, suppresses the exudative and proliferative phases of inflammation and increases the sensitivity of pain receptors. At therapeutic concentrations it does not inhibit COX-1. As a result of suppression of PGE2 synthesis, fluid retention is possible, because reabsorption of the thick ascending segment of the loop of Henley, as well as other distal parts of the nephron, increases. In addition, it is known that PGE2 can inhibit the reabsorption of water in the area of the collecting ducts, preventing the action of antidiuretic hormone. The drug does not inhibit the excretory capacity of the kidneys, even in patients with chronic renal failure. Celecoxib (until it is eliminated from the body) temporarily reduces the rate of sodium excretion. With long-term use in high doses, its selectivity decreases. Equilibrium concentration in blood plasma is achieved by the fifth day of taking the drug.
Important! The drug is contraindicated for use in children and adolescents under 18 years of age.
Particular caution should be exercised by people diagnosed with heart failure, since the drug increases the susceptibility to fluid retention.
Prescribe with caution during pregnancy and breastfeeding.
During treatment, you should refrain from activities that require increased attention and quick reaction, as accommodation disturbance may occur.
Etoricoxib (Table 60 mg, 90 mg, 120 mg) - Arcoxia TN (table 30 mg, 60 mg, 90 mg, 120 mg), Costarox TN (table 60 mg, 90 mg, 120 mg) - highly selective COX2 inhibitor, chlorinated pyridine derivative of phenylsulfone . NSAIDs inhibit the activity of COX-2 through a selective mechanism, interfering with the biosynthesis of prostaglandins and other inflammatory mediators. There is a decrease in the severity of symptoms of the inflammatory process, while the substance does not affect the functional activity of platelets and does not damage the mucous membrane of the digestive tract. The degree of inhibition of COX-2 is dose-dependent. The drug does not affect COX-1 if the daily dosage does not exceed 150 mg.
Patients with ailments of the musculoskeletal system use the drug to get rid of morning stiffness, there is an improvement in joint mobility, the intensity of inflammation decreases, and pain is well relieved. The therapeutic effect after administration occurs within half an hour. The active substance of the drug is perfectly absorbed into the bloodstream and is characterized by high bioavailability, which is 100%.
The drug has the ability to reduce the excitability of the thermoregulation center in the diencephalon and have an antipyretic effect.
After oral administration, the substance is quickly absorbed in the digestive tract and penetrates into the blood. After taking Etoricoxib, 120 mg, its maximum concentration in the blood is observed after 60 minutes. Eating reduces the maximum concentration by 35%, and the time to reach it increases to 2 hours.
Important! Metabolism occurs with the participation of microsomal liver enzymes and forms inactive metabolites. The drug overcomes the BBB and the placental barrier, which must be taken into account when prescribing to women during breastfeeding. It is not prescribed to patients with diseases of the cardiovascular system and urinary system, pregnant women and children under 12 years of age.
When are NSAIDs needed?
The range of indications for taking NSAIDs is quite wide. But, since these drugs have a pronounced analgesic effect, in modern medical practice it is the analgesic property of these drugs that has become most in demand. In each individual case, the choice of one or another NSAID remains with the doctor. It takes into account the nature of the pain and its cause, the severity of the pain syndrome, the state of the gastrointestinal tract, the characteristics of the person’s general health, his age and other circumstances that are important when prescribing a particular remedy.
Thus, for episodic and short-term pain, it is better to give preference to drugs with a short-term effect, which eliminate pain relatively quickly. At the same time, if attacks of pain continue for several hours in a row, preference is given to NSAIDs, which have a long duration of action (pain relief for up to 12 hours in a row after a single dose).
NSAIDs are used as an independent remedy for pain of traumatic origin, in the postoperative period, for menstrual, headache, muscle and joint pain.
As a symptomatic medicine as part of a complex treatment, NSAIDs are prescribed for a large number of diseases that are accompanied by pain and inflammation (rheumatism, arthritis, tonsillitis, ARVI, etc.).
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When NSAIDs are contraindicated
It should be understood that even the strongest NSAIDs are not a cure for the underlying disease (for example, if they are taken for headaches caused by hypertension). They help reduce the intensity of the inflammatory process, alleviate or completely eliminate pain for a certain time, but do not affect the pathological processes that caused the pain syndrome.
Each NSAID is accompanied by instructions that introduce the indications and contraindications for taking the drug, and also indicate the compatibility of various drug groups and possible side effects. It is very important to read this information carefully before you start taking any medicine, including NSAIDs. Pay special attention to the state of the gastrointestinal tract; in case of diseases of the digestive system, drugs in this group should be taken with caution and only after consultation with a doctor.
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Non-steroidal anti-inflammatory drug Motrin®
Motrin® is a modern drug from the group of non-steroidal anti-inflammatory drugs, which includes naproxen. This substance allows you to have a pronounced anti-inflammatory and analgesic effect, which lasts up to 12 hours in a row. Its effectiveness and high safety profile have been clinically proven, making Motrin® a recommended treatment for pain across a wide range of indications. The drug is intended for adults and children over 15 years of age. Before taking Motrin®, carefully read the instructions for the drug and consult your doctor.
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The information in this article is for reference only and does not replace professional advice from a doctor. To make a diagnosis and prescribe treatment, consult a qualified specialist.
Nonsteroidal anti-inflammatory drugs
Nonsteroidal anti-inflammatory drugs, or NSAIDs, are analgesics that exhibit three effects: analgesic, antipyretic and anti-inflammatory. At the same time, the notoriety about the bad effect of these drugs on the stomach literally haunts them.
We will understand the features of the principle of action, indications and, of course, the safety of NSAIDs in the second article in the series on analgesic drugs.
NSAIDs include:
- salicylates - acetylsalicylic acid;
- pyrazolones - analgin;
- derivatives of organic acids - ibuprofen, naproxen, ketoprofen, indomethacin, ketorolac, aceclofenac, diclofenac, piroxicam, meloxicam, mefenamic acid, etc.;
- coxibs - celecoxib, rofecoxib, parecoxib, etoricoxib.
Acetylsalicylic acid: an analgesic with experience
Few people know that the very first NSAID, acetylsalicylic acid, is of plant origin - its predecessor was obtained from meadowsweet, or meadowsweet. The drug was created by Bayer pharmacists at the end of the 19th century and named it after the Latin name for the meadowsweet Spiraea ulmaria aspirin.
The principle of action of aspirin, like all other NSAIDs, is to block the enzyme cyclooxygenase (COX). There are two types of COX in the body. The first, COX-1, is a necessary, “good” enzyme: it performs many important functions, including protecting the gastric mucosa. The second, COX-2, is responsible for the production of prostaglandins, triggering the mechanism of pain and inflammation.
Acetylsalicylic acid blocks both types of COX, with the first type of enzyme to a greater extent than the second. Therefore, the list of its side effects is considerable, and the leader in it is damage to the gastric mucosa, which can lead to the development of gastritis and even peptic ulcers. Aspirin is strictly contraindicated in children under 15 years of age due to the risk of developing Reye's syndrome - severe damage to the brain and liver.
Adults can take the drug as an antipyretic and mild pain reliever. However, in recent years, acetylsalicylic acid in this field has given way to safer NSAIDs and has become a cardiac drug due to its property of preventing platelet aggregation and thus “thinning” the blood.
Doubtful analgin?
Metamizole sodium, or analgin, is a fairly active pain reliever and a very weak anti-inflammatory drug. It is loyal to the stomach, directing all its negative influence on the blood. A serious side effect of analgin is the ability to change the blood picture and lead to the development of aplastic anemia, agranulocytosis and other hematological troubles.
In many countries of the world, including the USA, analgin is prohibited for sale. But in Germany, for example, it is widely used and is even considered the drug of choice for the treatment of postoperative pain. In Russia, they know, love and drink analgin, and, frankly, there is nothing wrong with it - the main thing is not to consume it regularly (that is, day after day) and not to exceed the recommended doses.
Diclofenac associates
The group of acid derivatives amazes even specialists with their choice, but each drug included in it still has its own “face”. Derivatives of organic acids are distinguished by pronounced anti-inflammatory properties, often overshadowing the analgesic and antipyretic effect. The exception is ibuprofen, which is still most often used to combat pain and fever, rather than inflammation.
Indomethacin and diclofenac are considered one of the most powerful anti-inflammatory drugs in this subgroup. The first has an adverse effect on the stomach and blood, and is rarely used today. Diclofenac is much safer, which, coupled with high activity and cost-effectiveness, ensures extremely high popularity in rheumatic diseases.
However, in terms of analgesic effect, diclofenac is significantly inferior to many drugs, in particular naproxen, which is successfully used to combat various types of intense pain, including dental, headache, periodic, etc. Naproxen is sold without a prescription and is in demand as quite safe, an affordable and yet powerful analgesic.
Another NSAID used for pain relief is ketorolac, known by the trade name Ketanov. It is distinguished by its speed, strength and duration of analgesic action in combination with gastrointestinal side effects traditional for NSAIDs. Therefore, ketorolac is used only with a doctor’s prescription to relieve postoperative pain, pain due to cancer and in other difficult cases.
Mefenamic acid is much more innocent than ketorolac, but is not as effective. Its reputation as an effective antipyretic agent is somewhat exaggerated: the drug is slightly more active than acetylsalicylic acid.
And another representative of NSAIDs that cannot be ignored is meloxicam, which combines a rather gentle effect on the stomach with a powerful anti-inflammatory effect, due to which it is often used in rheumatology.
Coxibs: the last word in pharmacology
Coxibs are the youngest group of NSAIDs, the first representative of which, celecoxib, went on sale in the late 1990s. Coxibs have almost no effect on COX-1, and therefore have virtually no gastrointestinal side effects traditional for this group. They adequately fight pain and inflammation in arthritis and other rheumatoid diseases, but they did not live up to the initial expectations that specialists had when the first coxib appeared.
Drugs in this group are still not without side effects (in particular, experts are still discussing the possible effect of coxibs on increasing the risk of heart attack and stroke) and, moreover, have a rather high price, which can pull the rug out from under already unhealthy legs. The decision to prescribe them should only be made by a doctor, and self-medication with coxibs, as well as most other NSAIDs, should not be done.
To readers who are still tormented by the agony of choice, I would like to say: do not be tormented. Get rid of this stone on your soul by placing it on the shoulders of your doctor. Trust him with your pain and inflammation and don’t test your stomach trying to hit the roof and find the “best” NSAID from dozens of medications.
Marina Pozdeeva
Photo thinkstockphotos.com
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