As an anti-inflammatory agent. Characteristics of individual drugs
Nonsteroidal anti-inflammatory drugs are used for various pathologies; they relieve pain, fever and inflammation in tissues. Most orthopedic problems cannot be solved without this group of medications, since patients are bothered by quite severe pain that interferes with the quality of life.
NSAIDs should be prescribed by a doctor, taking into account the indications and contraindications of a particular drug, especially if there is a need to take the drug for a long time. Despite their effectiveness, such drugs have severe side effects, the risk of which increases with long-term use of the drug.
Range of products
Non-steroidal anti-inflammatory drugs perfectly relieve pain syndromes, reduce high fever and inhibit the inflammatory process in body tissues. This effect is achieved by inhibiting enzymes that provoke the production of prostaglandins.
Prostaglandins are substances that are responsible for inflammatory processes in the body, in addition, they make a person more sensitive to pain. Thus, non-steroidal anti-inflammatory drugs dull pain and stop the development of the inflammatory process, this is a big advantage of the drug compared to analgesics that only relieve pain.
Classification
A couple of decades ago, only 7 groups of non-steroidal anti-inflammatory drugs were known, but nowadays there are already more than 15. NSAIDs are quite popular due to their complex action and good effect, so they have replaced opioid analgesics, which suppressed respiratory function, from the market.
There are two classifications of such drugs. They are divided into new and old, as well as acidic and non-acidic. Older drugs include Ibuprofen, Diclofenac, Voltaren, Nurofen, etc. New generation NSAID drugs are Nimesulide, etc.
Depending on whether NSAIDs are acids, they are divided into the following types:
- Preparations based on finylacetic acid. This acid is used in perfumery because it smells like honey. This substance is also part of amphetamine and is under control in the Russian Federation.
- Products made using anthranilic acid. This acid is used to make dyes and flavors.
- Pyrazolone preparations.
- Preparations made using isonicotinic acid.
- Propionic acid derivatives.
- Salicylates.
- Oxycams.
- Pyrazolidines.
New generation
It is no secret that old NSAIDs have a large number of side effects, while they do not have a strong enough anti-inflammatory effect. Conventionally, this can be explained in such a way that the drugs inhibit 2 types of enzymes COX-1 and COX-2, the first is responsible for protecting the body, and the second for the inflammatory process.
Thus, with long-term use of old-generation NSAIDs, patients experienced disturbances in the stomach, as its protective layer was destroyed. As a result, ulcers and other gastrointestinal problems appeared.
As it turned out, it is quite possible to reduce side effects, and at the same time increase the effectiveness of the drug, if you develop a drug that will suppress COX-2, practically without affecting the COX-1 enzymes. In recent years, new generation NSAID drugs have been developed that do just that. Below we look at the most popular new products.
This is one of the most popular non-steroidal anti-inflammatory drugs of the new generation. It is produced in Germany and Spain, and is available in the form of tablets, ointments, injections and suppositories. Movalis is a very good pain reliever, relieves high fever and inflammation, and has few contraindications.
Taken for inflammatory and degenerative diseases of the joints, in particular for various arthritis and arthrosis, for gout attacks, for ankylosing spondylitis, for severe pain in the joints. The big advantage of this drug is the ability to take it for a long time under the supervision of a doctor, which is exactly necessary for severe joint pathologies.
Movalis is very easy to use; you only need to take one tablet a day, as the drug lasts quite a long time. The cost of a package with 20 tablets of the product is approximately 600 rubles.
Nimesulide
Another popular new generation product is Nimesulide. It is actively used for various diseases, in particular for pathologies of the musculoskeletal system. The big advantage of this remedy is that it not only relieves inflammation, heat and pain, but also neutralizes enzymes that destroy cartilage tissue.
Nimesulide tablets are not expensive; for 20 pieces you will have to pay no more than 40 rubles. There are also analogues, for example Nise. This product can be purchased in the form of tablets, gel for external use, or powder for suspension. For 20 Nise tablets and 20 grams of gel you will have to pay about 200 rubles.
Xefocam
This drug is especially effective for severe pain; it is often prescribed for unspecified pain, as well as for joint pain, for example, gout, rheumatoid arthritis, severe stages of arthrosis and arthritis, and ankylosing spondylitis.
Interestingly, Xefocam is equated in action to Morphine, but it does not affect the central nervous system and is not addictive. The drug has side effects, so before use you need to consult a specialist who can calculate the minimum dosage, depending on the severity of the disease.
Ksefokam is produced in the form of tablets and solution for intravenous and intramuscular administration. The cost of tablets ranges from 300 to 500 rubles, depending on the required dosage, and 5 ampoules for injection will cost around 700 rubles.
Rofecoxib
This drug relieves pain, swelling, and inflammation. It is used mainly for orthopedic pathologies, in particular for osteochondrosis, arthritis, arthrosis, and also for toothaches. This product is sold under the name Denebol in the form of ointments and tablets.
Celecoxib
This drug is very effective for severe pain, and does not have any negative effect on the gastric mucosa, which is a big advantage of the drug. It is produced in the form of capsules of 100 and 200 mg. The cost of 10 capsules is 250 rubles.
Indications
NSAIDs are used for various inflammatory diseases, fever, pain of various etiologies. These drugs have an excellent antipyretic effect, and the effect lasts quite a long time, which makes the use of NSAIDs convenient in children. New generation drugs are indicated in the following cases:
- Arthritis, osteoarthritis, gout;
- Bekhterev's disease;
- Pain in various diseases of bones and joints;
- Osteochondrosis;
- Inflammation of soft tissues, synovitis, bursitis;
- Toothache;
- Pain after surgery;
- Fever.
Contraindications
New generation products have the following contraindications:
- Intolerance to the components of the drug;
- Stomach ulcers in the acute stage;
- Bleeding in the gastrointestinal tract;
- Reaction to acetylsalicylic acid (in particular rash, bronchospasm);
- Severe heart pathology;
- Severe kidney pathologies;
- Severe liver pathologies;
- Blood clotting disorder;
- Old age with long-term use;
- Alcoholism;
- Pregnancy and breastfeeding;
- Children's age up to 12 years.
During the treatment period, it is not recommended to drink alcohol or smoke, and it is also necessary to carry out treatment with caution if the patient is taking anticoagulants, glucocorticosteroids, sirotonin reuptake inhibitors, or antiplatelet agents.
Side effects
New generation non-steroidal anti-inflammatory drugs were developed specifically to reduce the impact on the mucous membranes of the gastrointestinal tract when taken. Therefore, these drugs do not have a destructive effect on the gastrointestinal tract, and on hyaline cartilage too. But still, with long-term use, some side effects may occur:
- Allergic reactions to the components of the drug;
- Fluid retention in the body, swelling;
- The appearance of protein in the urine;
- Increased activity of liver enzymes;
- Digestive problems;
- Headaches;
- General weakness and drowsiness;
- Dizziness;
- Increased blood pressure;
- Fatigue;
- The appearance of a dry cough;
- Dyspnea.
To avoid side effects, it is necessary to consult a doctor before taking the product and study the instructions for the drug. It is very important to use the product correctly and not to exceed the dosage, then the risk of side effects will be minimal.
What to replace
There are situations when pain takes you by surprise, and you don’t have the medicine prescribed by your doctor at hand. In this case, you can temporarily replace its intake with the help of various folk remedies: rubbing, ointments, compresses. But you should not abuse such methods and neglect basic treatment, as you can provoke a worsening of the condition.
To relieve body temperature above 38.5 degrees, rubbing is done. To do this, the patient must be undressed, and drafts in the room must be excluded. The body should be wiped with warm water and left to dry on the skin on its own, this way the body will cool down faster. Adults can be wiped at high temperatures with vodka diluted with water or add a little vinegar to the water. Children are wiped exclusively with water.
You can relieve pain due to joint pathologies using a rubbing mixture of iodine, analgin and vodka. To do this, grind 8 analgin tablets into powder, add 50 ml of alcohol and 50 ml of iodine, mix everything well. Rub the resulting pulp into the sore joint twice a day.
And comfrey.
About the products (video)
Osteoarthritis, rheumatoid arthritis and other diseases of the joints and spine that occur with pain and inflammation.
Peculiarities: all the drugs in this group act on a similar principle and cause three main effects: analgesic, anti-inflammatory and antipyretic.
These effects are expressed to varying degrees in different drugs, so some drugs are better suited for long-term treatment of joint diseases, while others are mainly used as painkillers and antipyretics.
Most common side effects: allergic reactions, nausea, abdominal pain, erosions and ulcers of the gastrointestinal mucosa.
Main contraindications: individual intolerance, exacerbation of gastric and duodenal ulcers.
Important information for the patient:
Drugs that have a pronounced analgesic effect and a significant number of side effects (diclofenac, ketorolac, nimesulide and others) can only be used as prescribed by a doctor.
Among nonsteroidal anti-inflammatory drugs, there is a group of so-called “selective” drugs that are less likely to have side effects from the gastrointestinal tract.
Even over-the-counter pain relief medications cannot be used long-term. If they are required frequently, several times a week, it is necessary to be examined by a doctor and treated according to the recommendations of a rheumatologist or neurologist.
In some cases, long-term use of drugs from this group requires additional use of proton pump inhibitors that protect the stomach.
| Trade name of the drug | Price range (Russia, rub.) | Features of the drug that are important for the patient to know about |
| Active ingredient: Diclofenac | ||
| Voltaren(Novartis) | A powerful pain reliever, mainly used for back and joint pain. It is not advisable to use it for a long time, as the drug has numerous side effects. May negatively affect liver function, causing headaches, dizziness and tinnitus. Contraindicated in aspirin-induced asthma, hematopoiesis and blood clotting disorders. Do not use during pregnancy, breastfeeding and children under 6 years of age. | |
| Diclofenac(different manufacturers) | ||
| Naklofen(KRKA) | ||
| Ortofen(different manufacturers) | ||
| Rapten rapid(Stada) | ||
| Active ingredient: Indomethacin | ||
| Indomethacin(different manufacturers) | 11,4-29,5 | Has a powerful anti-inflammatory and analgesic effect. However, it is considered quite outdated, as it leads in the likelihood of developing various side effects. It has many contraindications, including the third trimester of pregnancy, age up to 14 years. |
| Methindol retard(Polfa) | 68-131,5 | |
| Active ingredient: Diclofenac + paracetamol | ||
| Panoxen(Oxford Laboratories) | 59-69 | A powerful two-component pain reliever. Used to reduce severe pain and inflammation in arthritis, osteoarthritis, osteochondrosis, lumbago, dental and other diseases. Side effects are the same as diclofenac. Contraindications are inflammatory bowel diseases, severe liver, kidney and heart failure, the period after coronary artery bypass surgery, progressive kidney disease, active liver disease, pregnancy, breastfeeding, childhood. |
| Active ingredient: Tenoxicam | ||
| Texamen(Mustafa Nevzat Ilach Sanai) | 186-355 | It has a powerful analgesic and anti-inflammatory effect, the antipyretic effect is less pronounced. A distinctive feature of the drug is its long duration of action: more than a day. Indications are radicular syndrome with osteochondrosis, osteoarthritis with inflammation in the joints, neuralgia, muscle pain. Has a number of side effects. Contraindicated in case of bleeding from the gastrointestinal tract, pregnancy and during breastfeeding. |
| Active ingredient: Ketoprofen | ||
| Artrosilene(Dompe farmacheutichi) | 154-331 | A drug with a pronounced analgesic and anti-inflammatory effect. Does not have a negative effect on the condition of articular cartilage. Indications for use are symptomatic therapy of various arthritis, osteoarthritis, gout, headache, neuralgia, radiculitis, muscle pain, post-traumatic and postoperative pain, pain in cancer, painful periods. It causes many side effects and has many contraindications, including the third trimester of pregnancy and breastfeeding. In children, age restrictions depend on the trade name of the drug. |
| Quickcaps(Medana Pharma) | 161-274 | |
| Ketonal (Lec. d.d.) | 93-137 | |
| Ketonal duo(Lec. d. d.) | 211,9-295 | |
| Okie (Dompe farmacheutichi) | 170-319 | |
| Flamax(Sotex) | 86,7-165,8 | |
| Flamax forte(Sotex) | 105-156,28 | |
| Flexen(Italpharmaco) | 97-397 | |
| Active ingredient: Dexketoprofen | ||
| Dexalgin(Berlin-Chemie/Menarini) | 185-343 | A new powerful short-acting drug. The analgesic effect occurs 30 minutes after taking the drug and lasts from 4 to 6 hours. Indications for use are acute and chronic inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, spondyloarthritis, arthrosis, osteochondrosis), pain during menstruation, toothache. Side effects and contraindications are similar to those of other drugs. In general, with short-term use according to indications and in recommended doses, it is well tolerated. |
| Active ingredient: Ibuprofen | ||
| Ibuprofen(different manufacturers) | 5,5-15,9 | It is often used as an antipyretic drug and a means to relieve headaches. However, in large dosages it can also be used for diseases of the spine, joints and to relieve pain after bruises and other injuries. Possible side effects from the gastrointestinal tract, hematopoietic organs, as well as headache, dizziness, insomnia, increased blood pressure and a number of other undesirable reactions. Has many contraindications. Cannot be used in the third trimester of pregnancy and while breastfeeding; in the first and second trimester it should be used with caution, only on the recommendation of a doctor. cha. |
| Burana (Orion Corporation) | 46,3-98 | |
| Ibufen (Polfa, Medana Pharma) | 69-95,5 | |
| Moment (Berlin-Chemie/Menarini) | 71,6-99,83 | |
| Nurofen(Reckitt Benckiser) | 35,65-50 | |
| Nurofen Ultracap(Reckitt Benckiser) | 116-122,56 | |
| Nurofen Express(Reckitt Benckiser) | 102-124,4 | |
| Nurofen Express Neo(Reckitt Benckiser) | 65-84 | |
| Faspik(Zambon) | 80-115 | |
| Active ingredient: Ibuprofen + paracetamol | ||
| Ibuklin(Dr. Reddy's) | 78-234,5 | A combined drug containing two analgesic and antipyretic substances. It is more powerful than the same drugs taken separately. Can be used for pain in the joints and spine, injuries. However, it does not have a very pronounced anti-inflammatory effect, so it is not recommended for long-term treatment of rheumatic diseases. It has many side effects and contraindications. Do not use in children under 12 years of age, as well as in the third trimester of pregnancy and while breastfeeding. |
| Brustan(Runbaxy) | 60-121 | |
| Next(Pharmstandard) | 83-137 | |
| Active ingredient: Nimesulide | ||
| Nise(Dr. Reddy's) | 111-225 | A selective pain reliever mainly used for back and joint pain. May also relieve menstrual pain, headaches and toothaches. It has a selective effect, therefore it has less negative effects on the gastrointestinal tract. However, it has a number of contraindications and side effects. Contraindicated during pregnancy and breastfeeding; in children, age restrictions depend on the trade name of the drug. |
| Nimesulide(different manufacturers) | 65-79 | |
| Aponil(Medohemi) | 71-155,5 | |
| Nemulex(Sotex) | 125-512,17 | |
| Nimesil(Berlin-Chemie/Menarini) | 426,4-990 | |
| Nimika (IPKA) | 52,88-179,2 | |
| Nimulid(Panacea Biotek) | 195-332,5 | |
| Active ingredient: Naproxen | ||
| Nalgesin(KRKA) | 104-255 | A potent drug. It is used to treat arthritis, osteoarthritis, adnexitis, exacerbation of gout, neuralgia, radiculitis, pain in bones, tendons and muscles, headaches and toothaches, pain during cancer and after operations. It has quite a few contraindications and can cause a variety of side effects, so long-term treatment is only possible under the supervision of a doctor. |
| Naproxen(Pharmstandard) | 56,5-107 | |
| Naproxen-acri (Akrikhin) | 97,5-115,5 | |
| Active ingredient: Naproxen + esomeprazole | ||
| Vimovo(AstraZeneca) | 265-460 | A combination drug containing naproxen with analgesic and anti-inflammatory effects and the proton pump inhibitor esomeprazole. Formulated as sequential delivery tablets with immediate-release esomeprazole magnesium in the coating and enteric-coated sustained-release naproxen in the core. As a result, esomeprazole is released in the stomach before naproxen dissolves, thereby protecting the gastric mucosa from the possible negative effects of naproxen. Indicated for symptomatic relief in the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis in patients at risk of developing gastric and duodenal ulcers. Despite its good protective properties against the stomach, it can cause a number of other side effects. Contraindicated in severe liver, heart and kidney failure, gastrointestinal and other bleeding, cerebral hemorrhage and a number of other diseases and conditions. Not recommended in the third trimester of pregnancy, while breastfeeding and children under 18 years of age. |
| Active ingredient: Amtolmetin guacil | ||
| Nizilat(Dr. Reddy's) | 310-533 | A new non-steroidal anti-inflammatory drug with minimal negative effects on the gastric mucosa. Despite a number of possible side effects, it was generally well tolerated by patients (including long-term use for 6 months). It can be used both for rheumatic diseases (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout, etc.) and for the treatment of pain syndromes of other origins. It has quite a lot of contraindications. Not for use during pregnancy, breastfeeding and under 18 years of age. |
| Active ingredient: Ketorolac | ||
| Ketanov(Runbaxy) | 214-286,19 | One of the most potent analgesics. Due to the large number of contraindications and side effects, it should be used sporadically and only in cases of very severe pain. |
| Ketorol(Dr. Reddy's) | 12,78-64 | |
| Ketorolac(different manufacturers) | 12,1-17 | |
| Active ingredient: Lornoxicam | ||
| Xefocam(Nycomed) | 110-139 | It has a pronounced analgesic and anti-inflammatory effect. Indicated for short-term treatment of pain, including rheumatic diseases (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout, etc.). It has many side effects and contraindications. |
| Xefocam Rapid(Nycomed) | 192-376 | |
| Active ingredient: Aceclofenac | ||
| Aertal(Gedeon Richter) | 577-935 | Has good anti-inflammatory and analgesic effects. Helps significantly reduce the severity of pain, morning stiffness, swelling of joints, and does not have a negative effect on cartilage tissue. It is used to reduce inflammation and pain in lumbago, toothache, rheumatoid arthritis, osteoarthritis and a number of other rheumatological diseases. Causes many side effects. Contraindications are similar to those of Panoxen. Do not use during pregnancy, breastfeeding and children under 18 years of age. |
| Active ingredient: Celecoxib | ||
| Celebrex(Pfizer, Searle) | 365,4-529 | One of the most selective (selectively acting) drugs in this group, which has minimal negative effects on the gastrointestinal tract. Indications for use are the symptomatic treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis, back pain, bone and muscle pain, postoperative, menstrual and other types of pain. May cause swelling, dizziness, coughing, and a number of other side effects. It has many contraindications for use, including class II-IV heart failure, clinically significant coronary heart disease, peripheral arterial disease and severe cerebrovascular disease. Not for use during pregnancy, breastfeeding and under 18 years of age. |
| Active ingredient: Etoricoxib | ||
| Arcoxia(Merck Sharp & Dome) | 317-576 | A potent selective drug. According to the mechanism of action, side effects and contraindications, it is similar to celecoxib. Indications for use include osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and acute gouty arthritis. |
| Active ingredient: Meloxicam | ||
| Amelotex(Sotex) | 52-117 | A modern selective drug with a pronounced anti-inflammatory effect. Indications for use are pain and inflammatory syndrome in osteoarthritis, osteochondrosis, rheumatoid arthritis and ankylosing spondylitis. It is not usually used for antipyretic purposes or for the treatment of other types of pain. It can cause a variety of side effects, but the negative effect on the gastrointestinal tract is less than that of non-selective drugs in this group. It has many contraindications, including pregnancy, breastfeeding and children under 12 years of age. |
| Arthrozan(Pharmstandard) | 87,7-98,7 | |
| Bi-xicam(Veropharm) | 35-112 | |
| Meloxicam(different manufacturers) | 9,5-12,3 | |
| Mirlox(Polfa) | 47-104 | |
| Movalis(Boehringer Ingelheim) | 418-709 | |
| Movasin(Synthesis) | 73,1-165 | |
Remember, self-medication is life-threatening; consult a doctor for advice on the use of any medications.
Nonsteroidal anti-inflammatory drugs (NSAIDs) are drugs whose name indicates their composition, purpose and function.
Non-steroidal- do not contain the core, which is part of hormones and biologically active substances.
Anti-inflammatory- have a pronounced effect on inflammatory processes in a living organism, interrupting the chemical process of inflammation.
History of drugs from the NSAID group
The anti-inflammatory properties of willow have been known since the fifth century BC. In 1827, 30 grams of salicin were isolated from the bark of this plant. In 1869, based on salicin, the active substance, salicylic acid, was obtained.
The anti-inflammatory properties of salicylic acid have been known for a long time, but its pronounced ulcerogenic effect limited its use in medicine. The addition of an acetyl group to the molecule greatly reduced the risk of gastrointestinal ulcers.
The first medical drug from the NSAID group was synthesized in 1897 by Bayer. It was obtained by acetylation of salicylic acid. It received a patented name - “Aspirin”. Only the drug of this pharmacological company has the right to be called Aspirin.
Until 1950, aspirin remained the only nonsteroidal anti-inflammatory drug. Then, active work began to create more effective means.
However, the importance of acetylsalicylic acid in medicine is still great.
Mechanism of action of NSAIDs
The main point of application of NSAIDs are biologically active substances – prostaglandins. The first of them were found in the secretion of the prostate gland, hence their name. Two main types are more studied:
- Cyclooxygenase type 1 (COX-1), responsible for the synthesis of protective factors of the gastrointestinal tract and thrombus formation processes.
- Cyclooxygenase type 2 (COX-2), involved in the basic mechanisms of the inflammatory process.
By blocking enzymes, the effects of reducing pain, reducing inflammation and lowering body temperature are achieved.
There are drugs with selective and non-selective action. Selective agents block the COX-2 enzyme to a greater extent. Reduce inflammation without affecting processes in the digestive tract.
The action of cyclooxygenase of the second type is directed:
- to increase vascular permeability;
- release of inflammatory mediators in the damaged area;
- increased swelling in the area of inflammation;
- migration of phagocytes, mast cells, fibroblasts;
- an increase in the general temperature of the body, through thermoregulation centers in the central nervous system.
Inflammation
The process of inflammation is the body’s universal response to any damaging effect and has several stages:
- alteration stage develops in the first minutes of exposure to a damaging factor. The agents causing damage may be physical, chemical or biological. Biologically active substances are released from destroyed cells, triggering subsequent stages;
- exudation (impregnation), is characterized by the effect on mast cells of substances from dead cells. Activated basophils release histamine and serotonin into the site of damage, causing an increase in vascular permeability to the liquid part of the blood and macrophages. Swelling occurs and local temperature rises. Enzymes are released into the blood, attracting even more immunocompetent cells, triggering a cascade of biochemical and protective processes. The reaction becomes excessive. Pain occurs. It is at this stage that non-steroidal anti-inflammatory drugs are effective;
- proliferation stage, occurs at the moment of resolution of the second stage. The main cells are fibroblasts, which form a connective tissue matrix to restore the destroyed structure.
The stages do not have a clear time frame and are often included in combination. With a pronounced stage of exudation, occurring with a hyperergic component, the stage of proliferation is delayed. Prescribing NSAID drugs promotes speedy recovery and alleviates the general condition of the patient.
Main groups of non-steroidal anti-inflammatory drugs
There are many classifications. The most popular ones are based on the chemical structure and biological effects of substances.
Salicylates
The most studied substance is acetylsalicylic acid. The analgesic effect is very moderate. It is used as a drug to reduce temperature during febrile conditions and as a means of improving microcirculation in cardiology (in small doses it reduces blood viscosity by blocking type 1 cyclooxygenase).
Propionates
Salts of propionic acid have moderate analgesic and pronounced antipyretic effects. The best known is ibuprofen. Due to its low toxicity and high bioavailability, it is widely used in pediatric practice.
Acetates
Derivatives of acetic acid are well known and widely used in medicine. They have a pronounced anti-inflammatory effect and a strong analgesic effect. Due to the large effect on type 1 cyclooxygenase, they are used with caution in case of peptic ulcer and risk of bleeding. The most famous representatives: Diclofenac, Ketorolac, Indomethacin.
Selective COX-2 inhibitors
The most modern selective drugs today are considered Celecoxib and Rofecoxib. They are registered on the Russian market.
Other drugs
Paracetamol, nimesulide, meloxicam. They mainly act on COX-2. They have a pronounced analgesic and antipyretic effect of central action.
The most popular NSAID drugs and their costs
- Acetylsalicylic acid.
An effective and inexpensive drug. Available in dosages of 500 milligrams and 100 mg. The average price on the market is 8-10 rubles for 10 tablets. Included in the list of vital essentials.
- Ibuprofen.
Safe and inexpensive drug. The price depends on the form of release and the manufacturer. Has a pronounced antipyretic effect. Widely used in pediatrics.
400 milligram film-coated tablets, made in Russia, cost from 50-100 rubles for 30 tablets.
- Paracetamol.
A popular drug all over the world. Available in European countries without a doctor's prescription. The most popular forms are 500 milligram tablets and syrup.
Included in combination drugs as an analgesic and antipyretic component. It has a central mechanism of action, without affecting hematopoiesis and the gastrointestinal tract.
The price depends on the brand. Russian-made tablets cost about 10 rubles.
- Citramon P.
A combined drug containing anti-inflammatory and psychostimulating components. Caffeine increases the sensitivity of brain receptors tropic to paracetamol, enhancing the effect of the anti-inflammatory component.
Available in 500 milligram tablets. The average price is 10-20 rubles.
- Diclofenac.
It is available in various dosage forms, but is most in demand in the form of injections and local forms (ointments and patches).
The cost for a package of three ampoules is from 50 to 100 rubles.
- Nimesulide.
A selective drug that has a blocking effect on type 2 cyclooxygenase. Has a good analgesic and antipyretic effect. Widely used in dentistry and the postoperative period.
Available in the form of tablets, gels and suspensions. The average cost on the market is from 100-200 rubles for 20 tablets.
- Ketorolac.
A drug characterized by a pronounced analgesic effect, comparable to the effect of non-narcotic analgesics. It has a strong ulcerogenic effect on the mucous membrane of the gastrointestinal tract. Use with caution.
Must be released strictly according to a doctor's prescription. Release forms are varied. Tablets of 10 milligrams cost from one hundred rubles per pack.
Main indications for the use of NSAIDs
The most common reasons for taking this class of substances are diseases accompanied by inflammation, pain and fever. It should be remembered that drugs are rarely used for monotherapy. Treatment must be comprehensive.
Important. Use the information in this paragraph only if the emergency situation prevents you from contacting a qualified professional immediately. Please discuss all treatment issues with your doctor.
Arthrosis
A disease that causes changes in the anatomical structure of the articular surface. Active movements are extremely painful due to joint swelling and increased synovial fluid effusion.
In severe cases, treatment is reduced to joint replacement.
NSAIDs are indicated for moderate or moderate severity of the process. For pain, 100-200 milligrams of nimesulide are prescribed. No more than 500 mg per day. Taken in 2-3 doses. Drink with a small amount of water.
Rheumatoid arthritis
– inflammatory process of autoimmune etiology. Multiple inflammatory processes occur in various tissues. The joints and endocardial tissues are predominantly affected. NSAIDs are the drugs of choice in combination with steroid therapy. Endocardial damage always leads to the deposition of blood clots on the surface of the valves and chambers of the heart. Taking acetylsalicylic acid 500 milligrams per day reduces the risk of thrombosis by 5 times.
Pain due to soft tissue injuries
Associated with swelling at the point of application of the traumatic factor and surrounding tissues. As a result of exudation, small venous vessels and nerve endings are compressed.
Venous blood stagnates in the damaged organ, which further intensifies metabolic disorders. A vicious circle arises, worsening the conditions for regeneration.
For moderate pain syndrome, it is possible to use local forms of Diclofenac.
Apply to the area of bruise or sprain three times a day. The damaged organ needs rest and immobilization for several days.
Osteochondrosis
With this pathological process, compression of the spinal nerve roots occurs between the upper and lower vertebrae, forming the exit channels of the spinal nerves.
When the lumen of the canal decreases, the nerve roots innervating organs and muscles experience compression. This leads to the development of inflammatory processes and swelling of the nerves themselves, which further disrupts trophic processes.
To break the vicious circle, local ointments and gels containing Diclofenac are used in combination with injectable forms of the drug. Three milliliters of Diclofenac solution are injected intramuscularly once a day.
The course of treatment is at least 5 days. Considering the high ulcerogenicity of the drug, you should take proton pump blockers and antacids (Omeprazole 2 capsules twice a day and Almagel one or two scoops three times a day).
Pain in the lumbar region
With this localization, it is most often affected. The pain is quite intense. is formed from spinal roots emerging in the intervertebral foramina of the sacrum, emerging in a limited area into the shallow tissues of the gluteal region. This predisposes it to inflammation during hypothermia.
Ointments with NSAIDs containing Diclofenac or Nimesulide are used. In case of severe pain, the nerve exit site is blocked with an anesthetic drug. Local dry heat is used. It is important to avoid hypothermia.
Headache
Caused by various pathological processes. The most common cause is the brain. The brain itself does not have pain receptors. Pain sensations are transmitted from its membranes and receptors in the vessels.
Nonsteroidal anti-inflammatory drugs have a direct effect on prostaglandins, which regulate pain in the center of the thalamus. Pain causes vasospasm, metabolic processes decrease, and pain intensifies. NSAIDs, relieving pain, stop the spasm, interrupting the pathological process. The most effective drugs are Ibuprofen in a dose of 400 milligrams.
Migraine
It is caused by local spasm of blood vessels in the brain. More often the head hurts on one side. There are extensive neurological focal symptoms. Experience shows that non-steroidal analgesics in combination with antispasmodics are most effective.
Fifty percent Metamizole sodium solution (analgin) in the amount of two milliliters and two milliliters Drotaverine in one syringe intramuscularly or intravenously. After the injection, vomiting occurs. After some time, the pain is completely relieved.
Acute attack of gout
The disease is caused by a violation of uric acid metabolism. Its salts are deposited in various organs and tissues of the body, causing widespread pain. NSAIDs help stop. Ibuprofen preparations are used in a dosage of 400-800 milligrams.
Complex. Includes a diet low in purine and pyrimidine bases. In the acute period, animal products, broths, alcohol, coffee and chocolate are completely excluded.
Products of plant origin, except mushrooms, and large volumes of water (up to three to four liters per day) are indicated. If your condition improves, you can add low-fat cottage cheese to your food.
Dysmenorrhea
Painful periods or pain in the lower abdomen before them are common in women of fertile age. Caused by spasms in the smooth muscles of the uterus during rejection of the mucous membrane. The duration of pain and its intensity varies from person to person.
For relief, Ibuprofen preparations in a dose of 400-800 milligrams or selective NSAIDs (Nimesulide, Meloxicam) are suitable.
Treatment of painful menstruation may include the use of biphasic estrogen drugs that normalize the body's hormonal levels.
Fever
An increase in body temperature is a nonspecific pathological process that accompanies many painful conditions. Normal body temperature is between 35 and 37 degrees Celsius. With hyperthermia above 41 degrees, protein denaturation occurs and death can occur.
At normal body temperature, most biochemical processes in the body occur. The mechanisms of thermoregulation in higher organisms are of a neurohumoral nature. A small section of the hypothalamus, called the infundibulum, plays a major role in maintaining temperature homeostasis.
Anatomically, it connects the hypothalamus and thalamus at the junction of the optic nerves.
Substances called pyrogens are responsible for activating the hyperthermic reaction. One of the pyrogens is prostaglandin, produced by immune cells.
Its synthesis is regulated by cyclooxygenase. Nonsteroidal anti-inflammatory drugs can influence prostaglandin synthesis, indirectly reducing body temperature. Paracetamol acts on COX-1 in the center of thermoregulation, providing a rapid but short-lived antipyretic effect.
During fever, Ibuprofen exhibits the greatest antipyretic activity, acting indirectly. To reduce fever at home, a regimen with both drugs is justified.
500 milligrams Paracetamol and 800 milligrams Ibuprofen. The first quickly reduces the temperature to acceptable values, the second slowly and maintains the effect for a long time.
Teething fever in children
It is a consequence of the destruction of bone tissue during rapid tooth growth. Biologically active substances are released from the destroyed cells, which have a direct effect on the centers of the hypothalamus. Macrophages contribute to the inflammation process.
The most effective drug that eliminates inflammation and reduces temperature is Nimesulide at a dose of 25-30 milligrams, taken once or twice, completely stops the phenomena in 90-95 percent of cases.
Risks of using NSAIDs
Studies have shown that long-term use of non-selective drugs has a detrimental effect on the mucous membrane of the stomach and intestines. The ulcerogenic effect of acetylsalicylic acid has been confirmed. Long-term use of non-selective agents is recommended in conjunction with proton pump blockers (omeprazole).
Selective NSAIDs increase the risk of developing coronary heart disease tenfold even with long-term use. Aspirin is the only exception to this list. The antiplatelet properties of acetylsalicylic acid are used to prevent thrombosis, preventing blockage of great vessels.
Cardiologists warn that patients who have recently had a heart attack should avoid NSAID treatment. According to research data, Naproxen is considered the least dangerous from this point of view.
Studies have been published that long-term use of NSAIDs can cause erectile dysfunction. However, these studies were largely based on the feelings of the patients themselves. No objective data were provided on testosterone levels, seminal fluid examinations or physical examination methods.
Conclusion
A hundred years ago, the world's population was just over a billion people. Over the past twentieth century, humanity has made a huge breakthrough in all sectors of its activity. Medicine has become an evidence-based, effective and progressive science.
Today there are more than seven billion of us. The three main discoveries that influenced the survival of the human race are:
- vaccines;
- antibiotics;
- non-steroidal anti-inflammatory drugs.
There is something to think about and something to strive for.
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Nonsteroidal anti-inflammatory drugs (NSAIDs) are one of the main drugs used to treat inflammatory joint diseases.
They are prescribed in periodic courses for chronic processes, and, if necessary, for exacerbations of diseases and acute inflammatory processes. NSAIDs exist in various dosage forms - tablets, ointments, injection solutions. The choice of the necessary remedy, dosage and frequency of its use should be made by a doctor.
NSAIDs - what is this group of drugs?
The group of NSAIDs is quite extensive and includes drugs with different chemical structures. The name “non-steroidal” shows their difference from another large group of anti-inflammatory drugs – corticosteroid hormones.
The common properties of all drugs in this group are their three main effects - anti-inflammatory, analgesic, antipyretic.
This explains another name for this group - non-narcotic analgesics, as well as the enormous breadth of their use. These three effects are expressed differently in each drug, so they cannot be completely interchangeable. 
Unfortunately, all NSAID drugs have similar side effects. The most famous of them are the provocation of gastric ulcers, toxicity to the liver and inhibition of hematopoiesis. For this reason, you should not exceed the dosage indicated in the instructions, and also take these drugs if you suspect these diseases.
Abdominal pain cannot be treated with such medications - there is always a risk of worsening your condition. Various dosage forms of NSAIDs have been invented to improve their effectiveness in each specific situation and reduce potential health harm.
History of discovery and formation
The use of herbal remedies with anti-inflammatory, antipyretic and analgesic effects was described in the works of Hippocrates. But the first accurate description of the effect of NSAIDs dates back to the 18th century.
In 1763, the English physician and priest Edward Stone reported in a letter to the chairman of the Royal Society of London that an infusion of willow bark, growing in England, has antipyretic properties, described the recipe for its preparation and the method of use for febrile conditions.
Almost half a century later in France, I. Lear isolated a substance from willow bark that determined its medicinal properties. By analogy with 
From the Latin name for willow - salix, he called this substance salicin. This was the prototype of modern acetylsalicylic acid, which they learned to produce chemically in 1839.
The industrial production of NSAIDs began in 1888; the first drug to hit pharmacy shelves was acetylsalicylic acid under the trade name Aspirin, produced by Bayer, Germany. It still owns the rights to the Aspirin trademark, so other manufacturers produce acetylsalicylic acid under the international nonproprietary name or create their own (for example, Upsarin).
More recent developments have led to the emergence of a number of new drugs. Research continues to this day, and increasingly safe and effective means are being created. Oddly enough, the first hypothesis about the mechanism of action of NSAIDs was formulated only in the 20s of the 20th century. Previously, drugs were used empirically, their dosages were determined by the patient's well-being, and side effects were not well studied.
Pharmacological properties and mechanism of action
The mechanism of development of the inflammatory reaction in the body is quite complex and includes a chain of chemical reactions that trigger each other. One of the groups of substances involved in the development of inflammation is prostaglandins (they were first isolated from prostate tissue, hence the name). These substances have a dual function - they participate in the formation of protective factors in the gastric mucosa and in the inflammatory process.
Prostaglandin synthesis is carried out by two types of cyclooxygenase enzyme. COX-1 synthesizes “gastric” prostaglandins, and COX-2 synthesizes “inflammatory” ones, and is normally inactive. It is the activity of COX that NSAIDs interfere with. Their main effect - anti-inflammatory - is due to the inhibition of COX-2, and the side effect - disruption of the protective barrier of the stomach - is due to the inhibition of COX-1.
In addition, NSAIDs interfere quite strongly with cellular metabolism, which is responsible for their analgesic effect - they disrupt the conduction of nerve impulses. This is also the cause of lethargy, as a side effect of taking NSAIDs. There is evidence that these drugs stabilize lysosome membranes, slowing down the release of lytic enzymes.
Entering the human body, these drugs are absorbed mostly in the stomach, and in small quantities from the intestines.
Absorption varies; for new drugs, bioavailability can reach 96%. Enteric-coated drugs (Aspirin Cardio) are absorbed much less well. The presence of food does not affect the absorption of drugs, but since they increase acidity, it is advisable to take them after meals.
The metabolism of NSAIDs occurs in the liver, which is why they are toxic to this organ and cannot be used for various liver diseases. A small part of the incoming dose of the drug is excreted through the kidneys. Modern developments in the field of NSAIDs are aimed at reducing their effect on COX-1 and hepatotoxicity.
Indications for use - scope of application
The diseases and pathological conditions for which NSAIDs are prescribed are varied. Tablets are prescribed as an antipyretic for infectious and non-infectious diseases, as well as a remedy for headaches, dental, joint, menstrual and other types of pain (except for abdominal pain, if its cause is not clear). In children, suppositories containing NSAIDs are used to relieve fever. 
Intramuscular injections of NSAIDs are prescribed as an analgesic and antipyretic for severe patient conditions. They are necessarily part of the lytic mixture - a combination of drugs that can quickly bring down a dangerous temperature. Intra-articular injections treat severe joint damage caused by inflammatory diseases.
Ointments are used for local action on inflamed joints, as well as for diseases of the spine, muscle injuries to relieve pain, swelling and inflammation. Ointments can only be applied to healthy skin. For joint diseases, all three dosage forms can be combined.
The most famous drugs of the group
The very first NSAID to go on sale was acetylsalicylic acid under the brand name Aspirin. This name, despite being commercial, is strongly associated with the drug. It is prescribed to reduce fever, relieve headaches, 
small doses - to improve the rheological properties of blood. Rarely used for joint diseases.
Metamizole (Analgin) is no less popular than aspirin. Used to relieve pain of various origins, including joint pain. It is prohibited in many European countries, as it has a strong inhibitory effect on hematopoiesis.
– one of the popular drugs for the treatment of joints. Included in many ointments, available in and. It has a pronounced anti-inflammatory and analgesic effect, with almost no systemic effect.
Side effects
As with any other medication, there are numerous side effects when taking NSAIDs. The most famous among them is ulcerogenic, i.e. provoking ulcers. It is caused by inhibition of COX-1 and is almost completely absent in selective NSAIDs.
Acidic derivatives have an additional ulcerogenic effect by increasing the acidity of gastric juice. Most NSAIDs are contraindicated for gastritis with high acidity, gastric and duodenal ulcers, and GERD.
Another common effect is hepatotoxicity. It can manifest itself as pain and heaviness in the abdomen, digestive disorders, and sometimes short-term icteric syndrome, skin itching, and other manifestations of liver damage. For hepatitis, cirrhosis and 
liver failure, NSAIDs are contraindicated.
Inhibition of hematopoiesis, which, if the dosage is constantly exceeded, leads to the development of anemia, in some cases - pancytopenia (lack of all blood elements), impaired immunity, and bleeding. NSAIDs are not prescribed for severe bone marrow diseases and after bone marrow transplantation.
Effects associated with poor health - nausea, weakness, slow reaction, decreased attention, feeling tired, allergic reactions up to asthmatic attacks - occur individually.
Classification of NSAIDs
Today there are many drugs in the NSAID group, and their classification should help the doctor in choosing the most appropriate drug. This classification contains only international nonproprietary names.
Chemical structure
Based on their chemical structure, non-steroidal anti-inflammatory drugs are classified.
Acids (absorbed in the stomach, increase acidity):
- salicylates:
- pyrazolidines:
- indoleacetic acid derivatives:
- phenylacetic acid derivatives:
- oxicams:
- propionic acid derivatives:
Non-acidic derivatives (do not affect the acidity of gastric juice, are absorbed in the intestine):
- alkanones:
- sulfonamide derivatives:
By impact on COX-1 and COX-2
Non-selective - inhibit both types of enzyme, most of the NSAIDs belong to them.
Selective (coxibs) inhibit COX-2, do not affect COX-1:
- Celecoxib;
- Rofecoxib;
- Valdecoxib;
- Parecoxib;
- Lumiracoxib;
- Etoricoxib.
Selective and non-selective NSAIDs
Most NSAIDs are non-selective because they inhibit both types of COX. Selective NSAIDs are more modern drugs that act mainly on COX-2 and minimally affect COX-1. This reduces the risk of side effects.
However, complete selectivity of drug action has not yet been achieved, and there will always be a risk of side effects.
New generation drugs
The new generation includes not only selective, but also some non-selective NSAIDs, which have pronounced effectiveness, but are less toxic to the liver and hematopoietic system. 
New generation non-steroidal anti-inflammatory drugs:
- – has an extended period of validity;
- – has the strongest analgesic effect;
- – extended period of action and pronounced analgesic effect (comparable to morphine);
- Rofecoxib– the most selective drug, approved for patients with gastritis and peptic ulcer without exacerbation.
Non-steroidal anti-inflammatory ointments
The use of NSAID drugs in the form for local use (ointments and gels) has a number of advantages, primarily the absence of a systemic effect and a targeted effect on the site of inflammation. For diseases of the joints they are almost always prescribed. The most popular ointments:
- Indomethacin;
NSAIDs in tablets
The most common dosage form of NSAIDs is tablets. Used to treat various diseases, including articular ones.
Among the advantages, they can be prescribed to treat manifestations of a systemic process involving several joints. The disadvantages include pronounced side effects. The list of NSAID drugs in tablets is quite long, they include:
General application features
Nonsteroidal anti-inflammatory drugs for the treatment of joints are prescribed in courses or as needed, depending on the course of the disease.
The main feature of their use is that there is no need to take several drugs of this group in the same dosage form at the same time (especially tablets), since this increases the side effects, but the therapeutic effect remains the same.
It is permissible to use different dosage forms at the same time if necessary. It is important to remember that contraindications to taking NSAIDs are common to most drugs in the group.
NSAIDs remain the most important treatment for joints. They are difficult and sometimes almost impossible to replace by any other means. Modern pharmacology is developing new drugs from this group in order to reduce the risk of their side effects and increase the selectivity of action.
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Inflammatory reactions- these are universal protective-adaptive reactions to the influence of various exogenous and endogenous damaging factors (microorganisms, chemical agents, physical influences, etc.), playing an important role in the pathogenesis of most diseases of the maxillofacial area (periodontitis, alveolitis, periostitis, osteomyelitis, acute herpetic gingivostomatitis, etc.). This process is initiated and supported by endogenous biologically active substances (prostaglandins, thromboxane, prostacyclin, leukotrienes, histamine, interleukins (IL), NO, kinins), which are produced at the site of inflammation.
Despite the fact that inflammation is a protective reaction, excessive severity of this process can disrupt the functions of organs and tissues, which requires appropriate treatment. The specificity of the pharmacological regulation of this process depends on the characteristics of the etiology, pathogenesis and severity of individual phases of inflammation in a given patient, and the presence of concomitant pathology.
In dental practice, anti-inflammatory drugs of local and resorptive action are used (astringents, enzymes, vitamins, steroids and NSAIDs, dimexide, calcium salts, heparin ointment, etc.), which differ significantly in the mechanism of action, characteristics of the chemical structure, physicochemical properties, pharmacokinetics , pharmacodynamics, as well as on the effect on certain phases of inflammatory reactions. Despite the presence in the arsenal of a dentist of a large number of drugs of various directions of action, the main drugs used to obtain anti-inflammatory and analgesic effects are NSAIDs, the effect of which is manifested not only with resorptive action, but also with local application.
The use of enzymes in medicine (enzyme therapy) is based on their selective effect on certain tissues. Enzyme preparations cause hydrolysis of proteins, polynucleotides and mucopolysaccharides, resulting in the liquefaction of pus, mucus and other products of inflammatory origin. In dental practice, proteases, nucleases and lyases are most often used.
Non-steroidal anti-inflammatory drugs and non-narcotic analgesics
Index of drug descriptions
Acetylsalicylic acidBenzydamine
Diclofenac
Ibuprofen
Indomethacin
Ketoprofen
Ketorolac
Lornoxicam
Meloxicam
Metamizole sodium
Nimesulide
Paracetamol
Piroxicam
Phenylbutazone
Celecoxib
There is no INN
- Holisal
The range of NSAIDs currently used in medical practice is extremely wide: from traditional groups of salicylic acid derivatives (acetylsalicylic acid (aspirin) and pyrazolone (phenylbutazone (butadione)) to modern drugs derivatives of a number of organic acids: anthranilic acid - mefenamic acid and flufenamic acid; indoleacetic acid - indomethacin (methindol), phenylacetic - diclofenac (ortofen, voltaren, etc.), phenylpropionic - ibuprofen (brufen), propionic - ketoprofen (artrosilene, OKI, ketonal), naproxen (naprosyn), heteroarylacetic - ketorolac (ketalgin, ketanov, ketorol) and oxicam derivatives (piroxicam (piroxifer, hotemin), lornoxicam (xefocam), meloxicam (movalis).
NSAIDs have the same type of effects, but their severity varies significantly among drugs from different groups. Thus, paracetamol has a central analgesic and antipyretic effect, but its anti-inflammatory effect is not pronounced. In recent years, drugs with powerful analgesic potential have appeared, comparable in activity to tramadol (Tramal), such as ketorolac, ketoprofen and lornoxicam. Their high efficiency in severe pain syndrome of various localization allows for wider use of NSAIDs in the preoperative preparation of patients.
NSAIDs have also been created for topical use (based on ketoprofen, choline salicylate and phenylbutazone). Since the anti-inflammatory effect is associated with the blockade of cyclooxygenase (COX) COX-2, and many side effects are associated with the blockade of COX-1, NSAIDs have been created that primarily block COX-2 (meloxicam, nimesulide, celecoxib, etc.), which are better tolerated, especially patients at risk with a history of gastric and duodenal ulcers, bronchial asthma, kidney damage, and blood clotting disorders.
Mechanism of action and pharmacological effects
NSAIDs inhibit COX, a key enzyme in the metabolism of arachidonic acid, regulating its conversion to prostaglandins (PG), prostacyclin (PGI2) and thromboxane TxA2. PGs are involved in the processes of pain, inflammation and fever. By inhibiting their synthesis, NSAIDs reduce the sensitivity of pain receptors to bradykinin, reduce tissue swelling at the site of inflammation, thereby weakening the mechanical pressure on nociceptors.In recent years, it has been shown that the anti-inflammatory effect of these drugs is related to the prevention of activation of immunocompetent cells in the early stages of inflammation. NSAIDs increase the content of intracellular Ca2+ in T lymphocytes, which promotes their proliferation, the synthesis of interleukin-2 (IL-2) and the suppression of neutrophil activation. A relationship has been established between the severity of the inflammatory process in the tissues of the maxillofacial region and changes in the content of arachidonic acid, PG, especially PGE2 and PGF2a, lipid peroxidation products, IL-1β and cyclic nucleotides. The use of NSAIDs in these conditions reduces the severity of hyperergic inflammation, swelling, pain, and the degree of tissue destruction. NSAIDs act primarily on two phases of inflammation: the exudation phase and the proliferation phase.
The analgesic effect of NSAIDs is especially pronounced for inflammatory pain, which is due to a decrease in exudation, prevention of the development of hyperalgesia, and a decrease in the sensitivity of pain receptors to pain mediators. Analgesic activity is higher for NSAIDs whose solutions have a neutral pH. They accumulate less at the site of inflammation, penetrate the blood-brain barrier faster, and influence the thalamic centers of pain sensitivity, suppressing COX in the central nervous system. NSAIDs reduce the level of PG in brain structures involved in pain impulses, but do not affect the mental component of pain and its assessment.
The antipyretic effect of NSAIDs is mainly associated with an increase in heat transfer and appears only at elevated temperatures. This is due to inhibition of PGE1 synthesis in the central nervous system and inhibition of their activating effect on the thermoregulation center located in the hypothalamus.
Inhibition of platelet aggregation is due to blockade of COX and inhibition of thromboxane A2 synthesis. With long-term use of NSAIDs, a desensitizing effect develops, which is caused by a decrease in the formation of PGE2 in the inflammation site and leukocytes, inhibition of blast transformation of lymphocytes, and a decrease in the chemotactic activity of monocytes, T-lymphocytes, eosinophils, and polymorphonuclear neutrophils. PGs are involved not only in the implementation of inflammatory reactions. They are necessary for the normal course of physiological processes, perform a gastroprotective function, regulate renal blood flow, glomerular filtration, and platelet aggregation.
There are two isoforms of COX. COX-1 is an enzyme that is constantly present in most cells and is necessary for the formation of PGs that participate in the regulation of homeostasis and affect the trophism and functional activity of cells, and COX-2 is an enzyme that under normal conditions is found only in some organs (brain, kidneys, bones, reproductive system in women). The process of inflammation induces the production of COX-2. The blockade of COX-2 determines the presence of anti-inflammatory activity in drugs, and most of the side effects of NSAIDs are associated with the suppression of COX-1 activity.
Pharmacokinetics
Most NSAIDs are weak organic acids with a low pH. When taken orally, they have a high degree of absorption and bioavailability. NSAIDs bind well to plasma proteins (80-99%). With hypoalbuminemia, the concentration of free fractions of NSAIDs in the blood plasma increases, resulting in an increase in the activity and toxicity of the drug.NSAIDs have approximately the same volume of distribution. They are metabolized in the liver with the formation of inactive metabolites (with the exception of phenylbutazone), and are eliminated by the kidneys. NSAIDs are eliminated more quickly when the urine is alkaline. Some NSAIDs (indomethacin, ibuprofen, naproxen) are excreted 10-20% unchanged, and therefore their concentration in the blood may change in case of kidney disease. T1/2 varies significantly among different drugs in this group. Drugs with a short half-life (1-6 hours) include acetylsalicylic acid, diclofenac, ibuprofen, indomethacin, ketoprofen, etc., drugs with a long half-life (more than 6 hours) include naproxen, piroxicam, phenylbutazone, etc. The pharmacokinetics of NSAIDs may be affected by liver and kidney function, as well as the age of the patient.
Place in therapy
In dental practice, NSAIDs are widely used for inflammatory diseases of the maxillofacial region and oral mucosa, inflammatory swelling after injuries, operations, pain syndrome, arthrosis and arthritis of the temporomandibular joint, myofascial pain syndrome of the maxillofacial region, neuritis, neuralgia, postoperative pain, feverish conditions.Tolerability and side effects
NSAIDs are widely and uncontrolledly used as anti-inflammatory, analgesic and antipyretic drugs, but their potential toxicity is not always taken into account, especially in patients at risk with a history of diseases of the gastrointestinal tract, liver, kidneys, cardiovascular system, bronchial asthma and predisposed to allergic diseases. reactions.When using NSAIDs, especially a course, complications from many systems and organs are possible.
- From the gastrointestinal tract: stomatitis, nausea, vomiting, flatulence, pain in the epigastric region, constipation, diarrhea, ulcerogenic effect, gastrointestinal bleeding, gastroesophageal reflux, cholestasis, hepatitis, jaundice.
- From the central nervous system and sensory organs: headache, dizziness, irritability, increased fatigue, insomnia, tinnitus, decreased hearing acuity, sensory impairment, hallucinations, convulsions, retinopathy, keratopathy, optic neuritis.
- Hematological reactions: leukopenia, anemia, thrombocytopenia, agranulocytosis.
- From the urinary system: interstitial nephropathy,
- swelling.
- Allergic reactions: bronchospasm, urticaria, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), allergic purpura, Quincke's edema, anaphylactic shock.
- For the skin and subcutaneous fat: rash, bullous rashes, erythema multiforme, erythroderma (exfoliative dermatitis), alopecia, photosensitivity, toxicoderma.
Contraindications
- Hypersensitivity to drugs of this group.
- Course therapy with NSAIDs is contraindicated:
- with leukopenia;
- with severe damage to the kidneys and liver;
- in the first trimester of pregnancy;
- during lactation;
- children under 6 years of age (meloxicam - up to 15 years, ketorolac - up to 16 years).
Cautions
NSAIDs should be prescribed with caution to patients with bronchial asthma, arterial hypertension and heart failure. In elderly patients, low doses and short courses of NSAIDs are recommended.Interaction
When taken together with anticoagulants, antiplatelet agents and fibrinolytics, the risk of gastrointestinal bleeding increases. When combined with beta-blockers or angiotensin-converting enzyme (ACE) inhibitors, the antihypertensive effect may be reduced. NSAIDs increase the side effects of corticosteroids and estrogens. Deterioration of renal function can be observed when NSAIDs are combined with potassium-sparing diuretics (triamterene), ACE inhibitors, and cyclosporine. When paracetamol is combined with barbiturates, anticonvulsants and ethyl alcohol, the risk of hepatotoxicity increases. The use of paracetamol together with ethanol contributes to the development of acute pancreatitis.Examples of TN NSAIDs and non-narcotic analgesics registered in the Russian Federation
|
Synonyms |
|
|
Acetylsalicylic acid | |
|
Benzydamine |
Tantum verde |
|
Diclofenac |
Voltaren, Diclobene, Naklofen, Ortofen |
|
Ibuprofen |
Brufen, Nurofen |
|
Indomethacin |
Methindol |
|
Ketoprofen |
Artrosilene, Ketonal, OKI |
|
Ketorolac |
Ketalgin, Ketanov, Ketorol |
|
Lornoxicam |
Xefocam |
|
Meloxicam | |
|
Metamizole sodium |
Analgin |
|
Nimesulide |
Aulin, Nise, Nimesil, Novolid, Flolid |
|
Paracetamol |
Tylenol |
|
Piroxicam |
Piroxicam |
|
Phenylbutazone |
Butadion |
|
Celecoxib |
Celebrex |
G.M. Barer, E.V. Zoryan
