List of anti-inflammatory drugs of the new generation. How to be guided in the choice of anti-inflammatory non-steroidal drugs of a new generation

Anti-inflammatory drugs I

drugs that suppress the inflammatory process by preventing the mobilization or transformation of arachidonic acid. To P. s. do not include drugs that can affect the inflammatory process through other mechanisms, in particular, "basic" antirheumatic drugs (gold salts, D-penicillamine, sulfasalazine), (colchicine), quinoline derivatives (chloroquine).

There are two main groups of P. with.: glucocorticosteroids and non-steroidal anti-inflammatory drugs.

Indication for the use of glucocorticosteroids as P. s. are predominantly pathoimmune. They are widely used in the acute phase of systemic diseases of the connective tissue (Connective tissue), arthritis, sarcoidosis, alveolitis, non-infectious inflammatory diseases of the skin.

Taking into account the influence of glucocorticosteroids on many functions of the body (see. Corticosteroid hormones) and the possible formation of a dependence on the course of a number of diseases (and others), the regularity of the use of these drugs (dangerous manifestations of withdrawal) to their appointment as P. s. treated with some caution and seek to reduce the duration of their continuous use. On the other hand, among all P. s. glucocorticosteroids have the most pronounced anti-inflammatory effect, so a direct indication for their use is an inflammatory process that is life-threatening or the patient's ability to work (in the central nervous system, in the conduction system of the heart, in the eyes, etc.).

Side effects of glucocorticosteroids depend on their daily dose, duration of use, route of administration (local, systemic), as well as on the properties of the drug itself (severity of mineralocorticoid activity, effects on, etc.). With their local application, a local decrease in resistance to infectious agents is possible with the development of local infectious complications. With the systemic use of glucocorticosteroids, Cushing's, steroid, steroid stomach, steroid, the development of osteoporosis, sodium and water retention, potassium loss, arterial, myocardial dystrophy, infectious complications (primarily tuberculosis), the development of psychosis, withdrawal syndrome in a number of diseases (sharp symptoms after discontinuation of treatment), insufficiency of adrenal function (after prolonged use of glucocorticosteroids).

Contraindications to the systemic use of glucocorticosteroids: tuberculosis and other infectious diseases, diabetes mellitus (including in the postmenopausal period), stomach and duodenal ulcers, arterial hypertension, a tendency to thrombosis, mental disorders,. When applied topically (, respiratory tract,), the main contraindication is the presence of an infectious process in the same area of \u200b\u200bthe body.

The main forms of release of glucocorticosteroids used as P. s. are given below.

Beclamethasone- dosed (beclomet-easyhaler) and dosed for inhalation in bronchial asthma (aldecin, beclazone, beclomet, beclocort, beclofort, becotide) or for intranasal use in allergic rhinitis (beconase, nasobek) at 0.05, 0.1 and 0, 25 mg in one dose. In bronchial asthma, the daily allowance ranges from 0.2-0.8 mg. To prevent the development of candidiasis of the oral cavity and upper respiratory tract, it is recommended that the oral cavity be given water after each inhalation of the drug. At the beginning of treatment, sometimes there is hoarseness, sore throat, which usually disappear within the first week.

Betamethasone(celeston) - tablets of 0.5 mg and solution in ampoules of 1 ml (4 mg) for intravenous, intraarticular, subconjunctival administration; depot-form ("diprospan") - solution in ampoules of 1 ml (2 mg betamethasone disodium phosphate and 5 mg slowly absorbed betamethasone dipropionate) for intramuscular and intraarticular administration.

For skin application - creams and in tubes under the names Betnovate (0.1%), Diprolen (0.05%), Kuterid (0.05%), Celestoderm (0.1%).

Budesonide(budesonide mite, budesonide forte, pulmicort) - dosed at 0.05 and 0.2 mg in one dose, as well as dosed powder of 0.2 mg(pulmicort turbuhaler) for inhalation in bronchial asthma (therapeutic dose 0.2-0.8 mg/day); 0.025% ointment ("apulein") for external use in atopic dermatitis, eczema, psoriasis (1-2 times a day is applied in a thin layer to the affected areas of the skin).

Hydrocortisone(solu-cortef, sopolkort N) - suspension for injections of 5 ml in vials (25 mg in 1 ml), as well as a solution for injection in ampoules of 1 ml (25 mg) and lyophilized powder for injection 100 mg with the supplied solvent. Used for intravenous, intramuscular and intraarticular administration (25 mg drug, in small - 5 mg). For external use, it is available in the form of 0.1% creams, ointments, lotions, emulsions (under the names "latikort", "locoid") and 1% ointment ("cortade").

When administered intra-articularly, the drug can cause the development of osteoporosis and the progression of degenerative changes in the joints. Therefore, it should not be used for secondary synovitis in patients with deforming arthrosis.

Desonide(prenacid) - 0.25% solution in vials of 10 ml(ophthalmic) and 0.25% eye ointment (10 G in a tube). A water-soluble, halogen-free glycocorticoid with a pronounced anti-inflammatory effect. It is indicated for iritis, iridocyclitis, episcleritis, conjunctivitis, scaly blepharitis, chemical damage to the cornea. Drops are used during the day (1-2 drops 3-4 times a day), at night - eye ointment.

Dexamethasone(decdan, dexabene, dexaven, dexazon, dexamed, dexon, detazone, fortecortin, fortecortin) - tablets of 0.5, 1.5 and 4 mg; solution in ampoules of 1 ml (4 mg), 2 ml(4 or 8 mg) and 5 ml (8 mg/ml) for intramuscular or intravenous (isotonic sodium chloride solution or 5% glucose solution) administration; 0.1% solution in bottles of 10 and 15 ml(eye drops) and 0.1% eye suspension in vials of 10 ml. Fluorine-containing synthetic glucocorticoid with a pronounced anti-inflammatory and anti-allergic effect. Parenteral use of the drug in systemic therapy should not be long (no more than a week). Inside appoint 4-8 mg 3-4 times a day.

Clobetasol(dermovate) - 0.05% cream and ointment in tubes. Used for psoriasis, eczema, discoid lupus erythematosus. It is applied in a thin layer to the affected areas of the skin 1-2 times a day until improvement occurs. Side effects: local skin.

Mazipredone- water-soluble synthetic derivative of prednisolone: solution for injection in ampoules of 1 ml(30 pcs.) for intravenous (slow) or intramuscular administration, as well as 0.25% emulsion ointment (deperzolon) for external use for dermatitis, eczema, diaper rash, lichen planus, discoid lupus, psoriasis, otitis externa. applied to the skin with a thin layer (on the soles and palms - under compression bandages) 2-3 times a day. Avoid getting ointment in the eyes! With prolonged use, systemic side effects are possible.

Methylprednisolone(medrol, metipred, solu-medrol, urbazon) - tablets of 4, 16, 32 and 100 mg; dry matter 250 mg and 1 G in ampoules with the attached solvent for intravenous administration; depot forms ("depo-medrol") - for injections in vials of 1, 2 and 5 ml (40 mg/ml), characterized by prolonged (up to 6-8 days) suppression of the activity of the hypothalamic-pituitary-adrenal system. They are mainly used for systemic therapy (, systemic connective tissue diseases, leukemia, various types of shock, adrenal insufficiency, etc.). Depo-Medrol can be administered intra-articularly (20-40 mg in large joints, 4-10 mg- in small ones). Side effects are systemic.

Methylprednisolone aceponate("advantan") - ointment 15 G in tubes. Used for various forms of eczema. applied to the affected areas of the skin 1 time per day. With prolonged use, erythema, skin atrophy, acne-like elements are possible.

Mometasone- metered aerosol (1 dose - 50 mcg) for intranasal use in allergic rhinitis (Nasonex drug); 0.1% cream, ointment (in tubes), lotion used for psoriasis, atopic and other dermatitis (Elokom drug).

Intranasally inhaled 2 doses each 1 time per day. Ointment and cream are applied in a thin layer to the affected areas of the skin 1 time per day; lotion is used for the hairy parts of the skin (a few drops are rubbed 1 time per day). With prolonged use, systemic side effects are possible.

Prednisone(apo-prednisone) - tablets of 5 and 50 mg. Clinical use is limited.

Prednisolone(decortin N, medopred, prednisol) - tablets of 5, 20, 30 and 50 mg; solution for injection in ampoules 1 ml containing 25 or 30 mg prednisolone or 30 mg mazipredone (see above); suspension for injection in ampoules 1 ml (25 mg); lyophilized powder in 5 ampoules ml (25 mg); eye suspension in vials of 10 ml (5 mg/ml); 0.5% ointment in tubes. For systemic therapy, it is used in the same cases as methylprednisolone, but in comparison with it, it exhibits a greater mineralocorticoid effect with a faster development of systemic side effects.

Triamcinolone(azmacort, berlicort, kenacort, kenalog, nazacort, polkortolone, triacort, tricort, fluorocort) - 4 tablets mg; metered aerosols for inhalation in bronchial asthma (1 dose - 0.1 mg) and for intranasal use in allergic rhinitis (1 dose - 55 mcg); solution and suspension for injection in vials and ampoules, 1 each ml(10 or 40 mg); 0.1% cream, 0.025% and 0.1% ointment for skin application (in tubes); 0.1% for topical use in dentistry (Kenalog Orabase). Used for systemic and local therapy; topical use in ophthalmology is prohibited. With intra-articular injection (in large joints 20-40 mg, in small joints - 4-10 mg) the duration of the therapeutic effect can reach 4 weeks. and more. Inside and on the skin, the drug is used 2-4 times a day.

flumethasone(lorinden) - 0.02% lotion. Glucocorticoid for external use. Included in the combined ointments. It is used for psoriasis, eczema, allergic dermatitis. It is applied in a thin layer to the affected areas of the skin 1-3 times a day. Avoid getting the drug in the eyes! With extensive skin lesions, it is used only for a short time.

Flunisolide(ingacort, sintaris) - metered aerosols for inhalation in bronchial asthma (1 dose - 250 mcg) and for intranasal use in allergic rhinitis (1 dose - 25 mcg). Appointed 2 times a day.

Fluocinolone(sinalar, sinaflan, flukort, flucinar) - 0.025% cream, ointment in tubes. It is used in the same way as flumethasone.

Fluticasone(cutiveit, flixonase, flixotide) - metered dose aerosol (1 dose - 125 or 250 mcg) and powder in rotadisks (doses: 50, 100, 250 and 500 mcg) for inhalation in bronchial asthma; dosed aqueous spray for intranasal use in allergic rhinitis. Apply 2 times a day.

Non-steroidal anti-inflammatory drugs(NSAIDs) - substances of various chemical structures that, in addition to anti-inflammatory, also, as a rule, have analgesic and antipyretic activity. The group of NSAIDs consists of derivatives of salicylic acid (acetylsalicylic acid, mesalazine), indole (indomethacin, sulindac), pyrazolone (phenylbutazone, clofezone), phenylacetic acid (diclofenac), propionic acid (ibuprofen, naproxen, flurbiprofen, ketoprofen), oxicam (meloxicam, piroxicam , tenoxicam) and other chemical groups (benzydamine, nabumetone, niflumic acid, etc.).

The mechanism of the anti-inflammatory action of NSAIDs is associated with their inhibition of the cyclooxygenase (COX) enzyme, which is responsible for the transformation of arachidonic acid into prostacyclin and thromboxane. There are two isoforms of cyclooxygenase. COX-1 - constitutional, "useful", involved in the formation of thromboxane A 2, prostaglandin E 2, prostacyclin. COX-2 is an "inducible" enzyme that catalyzes the synthesis of prostaglandins involved in the inflammatory process. Most NSAIDs equally inhibit COX-1 and COX-2, which leads, on the one hand, to the suppression of the inflammatory process, and on the other hand, to a decrease in the production of protective prostaglandins, which disrupts reparative processes in the stomach and underlies the development of gastropathy. That is, in the mechanism of the main action of NSAIDs, there is also a mechanism for the development of their main "side" actions, which are more correctly called undesirable for their intended use as P. s.

NSAIDs are used mainly in rheumatology. Indications for their use are other systemic diseases of the connective tissue: acute and chronic inflammatory diseases of the joints; secondary in degenerative joint diseases; microcrystalline (, chondrocalcinosis, hydroxyapatite); extra-articular rheumatism. As part of complex therapy, NSAIDs are also used for other inflammatory processes (adnexitis, prostatitis, cystitis, phlebitis, etc.), as well as for neuralgia, myalgia, injuries of the musculoskeletal system. The antiplatelet properties of acetylsalicylic acid (it irreversibly inhibits cyclooxygenase, in other drugs this effect is reversible within the half-life of the drug) led to its use in cardio- and angiology to prevent thrombosis.

A single dose of any NSAID gives only an analgesic effect. The anti-inflammatory effect of the drug appears after 7-10 days of regular use. Control over the anti-inflammatory effect is carried out according to clinical (reduction of swelling, pain severity) and laboratory data. If there is no effect within 10 days, the drug should be replaced with another from the NSAID group. With a local inflammatory process (, bursitis, enthesitis, moderately pronounced), treatment should be started with topical dosage forms (ointments, gels) and only if there is no effect, systemic therapy should be resorted to (orally, in suppositories, parenterally). Patients with acute arthritis (for example, gouty) - parenteral administration of drugs is indicated. In case of clinically pronounced chronic arthritis, systemic NSAID therapy should be immediately prescribed, with an empirical selection of an effective and well-tolerated drug.

All NSAIDs have a comparable anti-inflammatory effect, approximately equal to that of aspirin. Group differences relate mainly to adverse events not associated with the action of NSAIDs.

Side effects that are common to all NSAIDs include, first of all, the so-called NSAID gastropathy with a lesion predominantly of the antrum of the stomach (mucosal erythema, hemorrhages, erosion, ulcers); possibly gastric. Of the other gastrointestinal manifestations of side effects, constipation is also described. Inhibition of renal cyclooxygenase can be clinically manifested by fluid retention (sometimes with arterial hypertension and heart failure), the development of acute or progression of existing renal failure, hyperkalemia. By reducing platelet aggregation, NSAIDs can contribute to bleeding, including from ulcers of the gastrointestinal tract, and aggravate the course of NSAID gastropathy. Of the other manifestations of the side effects of NSAIDs, skin (itching,) were noted, from the side of the central nervous system. - (more often when using indomethacin), tinnitus, visual disturbances, sometimes (, confusion,), as well as side effects associated with individual hypersensitivity to the drug (, urticaria, Quincke's edema).

Contraindications to the use of NSAIDs: up to 1 year (for certain drugs - up to 12 years); "aspirin"; peptic ulcer of the stomach and 12 duodenal ulcer; renal or hepatic insufficiency, edema; increased, upcoming, individual intolerance to NSAIDs in history (asthma attacks, urticaria), last trimester of pregnancy, breastfeeding.

Individual NSAIDs are listed below.

Lysine acetylsalicylate(aspizol) - powder for injections of 0.9 G in vials with the supplied solvent. It is administered intramuscularly or intravenously, mainly with fever, at a dose of 0.5-1 G; daily dose - up to 2 G.

Acetylsalicylic acid(aspilight, aspirin, aspirin UPSA, acesal, acylpyrine, bufferin, magnil, novandol, plidol, salorin, sprit-lime, etc.) - tablets of 100, 300, 325 and 500 mg, "effervescent tablets" of 325 and 500 mg. As P. with. appoint 0.5-1 G 3-4 times a day (up to 3 G/day); for the prevention of thrombosis, incl. repeated myocardial infarction is used in a daily dose of 125-325 mg(preferably in 3 doses). In case of an overdose, dizziness occurs in the ears. In children, the use of aspirin can lead to the development of Reye's syndrome.

Benzydamine(tantum) - 50 tablets mg; 5% gel in a tube. Differs in good absorbability at dermal application; it is mainly used for phlebitis, thrombophlebitis, after operations on the veins of the extremities. Inside appoint 50 mg 4 times a day; the gel is applied to the skin of the affected area and gently rubbed until absorbed (2-3 times a day).

For use in dentistry (gingivitis, glossitis, stomatitis,) and for diseases of the upper respiratory tract (, laryngitis, tonsillitis), the drug "Tantum Verde" is produced - lozenges of 3 mg; 0.15% solution in vials of 120 ml and metered aerosol (1 dose - 255 mcg) for local use.

In gynecology, the preparation "tantum rose" is used - 0.1% solution for topical application, 140 ml in disposable syringes and dry matter for the preparation of a similar solution in sachets containing 0.5 G benzydamine hydrochloride and other ingredients (up to 9.4 G).

When ingested and the resorptive action of a topically applied drug, side effects are possible: dry mouth, nausea, swelling, sleep disturbances, hallucinations. Contraindications: age up to 12 years, pregnancy and lactation, increased to the drug.

diclofenac(veral, voltaren, votrex, diclogen, diclomax, naklof, naklofen, orthofen, rumafen, etc.) - tablets of 25 and 50 mg; retard tablets 75 and 100 mg; 50 each mg; capsules and retard capsules (75 and 100 mg); 2.5% injection solution in ampoules of 3 and 5 ml(75 and 125 mg); rectal at 25, 50 and 100 mg; 0.1% solution in vials of 5 ml- eye drops (drug "naklof"); 1% gel and 2% ointment in tubes. Inside, adults are prescribed 75-150 mg/ day in 3 doses (retard forms in 1-2 doses); intramuscularly - 75 each mg/ day (as an exception under 75 mg 2 times a day). In juvenile rheumatoid arthritis, the exact dose should not exceed 3 mg/kg. Gel and ointment (on the skin over the affected area) are used 3-4 times a day. The drug is well tolerated; side effects are rare.

ibuprofen(brufen, burana, ibusan, ipren, markofen, perofen, solpaflex, etc.) - tablets of 200, 400 and 600 mg; dragees 200 each mg; long-acting capsules 300 mg; 2% and 2% suspension in vials of 100 ml and suspension in vials of 60 and 120 ml (100 mg at 5 ml) for oral administration. The therapeutic dose in adults orally is 1200-1800 mg/ day (maximum - 2400 mg/ day) in 3-4 doses. The drug "Solpaflex" (prolonged action) is prescribed for 300-600 mg 2 times a day. (maximum daily dose 1200 mg). Overdose may cause liver dysfunction.

Indomethacin(indobene, indomine, metindol) - tablets and dragees 25 each mg; retard tablets 75 each mg; capsules of 25 and 50 mg; rectal suppositories 50 and 100 mg; solution for injection in ampoules of 1 and 2 ml(for 30 mg in 1 ml); 1% gel and 5% ointment for skin application in tubes. The therapeutic dose in adults inside is 75-150 mg/ day (in 3 doses), maximum - 200 mg/ day use 1 time per day. (for the night). In an acute attack of gout, it is recommended to take the drug at 50 mg every 3 h. In case of an overdose, a sharp headache and dizziness (sometimes combined with an increase), as well as nausea, disorientation, are possible. With prolonged use, retino- and due to the deposition of the drug in the retina and cornea are noted.

Ketoprofen(actron, ketonal, knavon, oruvel, prontoket spray) - 50 capsules mg, tablets of 100 mg and retard tablets of 150 and 200 mg; 5% solution (50 mg/ml) for oral administration (drops); injection solution (50 mg/ml) in ampoules of 2 ml; lyophilized dry matter for intramuscular injections and the same for intravenous administration, 100 mg in vials with the attached solvent; candles 100 mg; 5% cream and 2.5% gel in tubes; 5% solution (50 mg/ml) for external use, 50 ml in a spray bottle. Assign inside 50-100 mg 3 times a day; retard tablets - 200 mg 1 time per day during meals or 150 mg 2 times a day; candles, as well as cream and gel are used 2 times a day. (at night and in the morning). Intramuscularly injected 100 mg 1-2 times a day; intravenous administration is carried out only in a hospital (in the case when intramuscular injection is not possible), in a daily dose of 100-300 mg no more than 2 days. contract.

Clofezon(percluson) - an equimolecular compound of clofexamide and phenylbutozone in capsules, suppositories and in the form of an ointment. It acts longer than phenylbutazone; appointed by 200-400 mg 2-3 times a day. The drug should not be combined with other pyrazolone derivatives.

Mesalazine(5-AGA, salozinal, salofalk), 5-aminosalicylic acid - dragees and enteric-coated tablets of 0.25 and 0.5 G; rectal suppositories 0.25 and 0.5 G; suspension for use in enemas (4 G at 60 ml) in disposable containers. It is used for Crohn's disease, ulcerative colitis, irritable bowel syndrome, postoperative anastomosis, complicated hemorrhoids. In the phase of exacerbation of these diseases, 0.5-1 G 3-4 times a day, for maintenance therapy and prevention of exacerbations - 0.25 each G 3-4 times a day.

Meloxicam(movalis) - tablets of 7.5 mg; rectal suppositories 15 each mg. It inhibits mainly COX-2, therefore it has a less pronounced ulcerogenic effect than other NSAIDs. Therapeutic dose for secondary inflammation in patients with arthrosis - 7.5 mg/day; in rheumatoid arthritis use the maximum daily dose - 15 mg(in 2 doses).

Nabumeton(relafen) - tablets of 0.5 and 0.75 G. metabolized in the liver to form an active metabolite having a T 1 /2 of about 24 h. Highly effective in rheumatoid arthritis. Appointed 1 time per day. at dose 1 G, if necessary - up to 2 G/ day (in 2 doses). Side effects, except for those common to NSAIDs: the possibility of developing eosinophilic pneumonia, alveolitis, interstitial nephritis, nepheotic syndrome, hyperuricemia.

Naproxen(apo-naproxen, apranax, daprox, nalgesin, naprobene, naprosin, noritis, pronaxen) - tablets of 125, 250, 275, 375, 500 and 550 mg; oral suspension (25 mg/ml) in vials of 100 ml; rectal suppositories 250 and 500 mg. has a pronounced analgesic effect. Assign 250-550 mg 2 times a day; in an acute attack of gout, the first dose is 750 mg, then every 8 h by 250-500 mg within 2-3 days (until the attack stops), after which the dose is reduced.

Niflumic acid(donalgin) - capsules of 0.25 G. In case of exacerbation of rheumatic diseases, 0.25 G 3 times a day (maximum 1 G/ day), when improvement is achieved, the dose is reduced to 0.25-0.5 G/ day In an acute attack of gout, the first dose is 0.5 G, after 2 h - 0,25 G and after 2 more h - 0,25 G.

Piroxicam(apo-piroxicam, brexic-DT, moven, pirocam, remoxicam, roxicam, sanicam, felden, hotemin, erazone) - tablets and capsules of 10 and 20 mg; soluble tablets of 20 mg; 2% solution (20 mg/ml) for injection in ampoules of 1 and 2 ml; rectal suppositories 10 and 20 each mg; 1% cream, 1% and 2% gel in tubes (for skin application). After absorption, it penetrates well into the synovial fluid; T 1/2 from 30 to 86 h. Assign inside, intramuscularly and in suppositories 1 time per day. at a dose of 20-30 mg(maximum dose - 40 mg/day); in acute attack of gout on the first day 40 mg once, in the next 4-6 days - 20 mg 2 times a day. (for long-term treatment of gout, the drug is not recommended).

Sulindak(clinoril) - tablets 200 mg. Assign 2-3 times a day. The therapeutic dose is 400-600 mg/ day

Tenoxicam(tenicam, tenoctyl, tilkotil, tobitil) - tablets and capsules of 20 mg; rectal suppositories 10 each mg. It penetrates well into the synovial fluid; T 1/2 60-75 h. Appointed 1 time per day. an average of 20 mg. In an acute attack of gout in the first two days, the maximum daily dose is given - 40 mg. Special side effects: swelling around, visual disturbances; interstitial, glomerulonephritis, are likely.

Phenylbutazone(butadione) - tablets of 50 and 150 mg, dragee 200 mg; 20% injection solution (200 mg/ml) in ampoules of 3 ml; 5% ointment in tubes. Appointed orally at 150 mg 3-4 times a day. The ointment is applied in a thin layer (without rubbing) on the skin over the affected joint or other site of injury (for dermatitis, skin burns, insect bites, superficial thrombophlebitis, etc.) 2-3 times a day. With deep thrombophlebitis, the drug is not used. other NSAIDs are more likely to develop aplastic and agranulocytosis.

Flurbiprofen(flugalin) - tablets of 50 and 100 mg, capsules retard 200 each mg; rectal suppositories 100 each mg. The therapeutic dose is 150-200 mg/ day (in 3-4 doses), the maximum daily dose is 300 mg. Retard capsules are used 1 time per day.

II Anti-inflammatory drugs

The ability to weaken inflammatory processes has a different chemical structure. The most active in this regard are the hormones of the adrenal cortex and their synthetic substitutes - the so-called glucocorticoids (prednisolone, dexamethasone, etc.), which, in addition, have a strong antiallergic effect. In the course of treatment with glucocorticoids, their side effects are often manifested: metabolic disorders, sodium and water retention in the body and an increase in blood plasma volume, increased blood pressure, ulceration of the mucous membrane of the stomach and duodenum, suppression of immunity, etc. With prolonged use of glucocorticoids, the synthesis of natural hormones in the adrenal glands, as a result of which, when these drugs are stopped, signs of insufficient function of the adrenal cortex may develop. In this regard, treatment with glucocorticoids should be carried out under constant medical supervision, their use without a doctor's prescription is dangerous. are also part of a number of ointments and suspensions (for example, prednisolone ointment, ointments "Ftorocort", "Sinalar", "Locacorten", "Lorinden C", "Celestoderm V", etc.), used externally for inflammatory diseases of the skin and mucous membranes . You should also not use these dosage forms without a doctor's prescription, because. in this case, exacerbations of certain skin diseases and other serious complications may occur.

As P. with. some painkillers from among the so-called non-narcotic analgesics are used, for example, acetylsalicylic acid, analgin, amidopyrine, butadione, and drugs similar in properties to them (indomethacin, ibuprofen, ortofen, etc.). They are inferior to glucocorticoids in anti-inflammatory activity, but they also have a less pronounced side effect, which allows them to be widely used to treat inflammatory diseases of the joints, muscles and internal organs.

Also have a moderate anti-inflammatory effect (tannin, tanalbin, oak bark, romazulon, basic bismuth nitrate, dermatol, etc.), which are mainly used topically for inflammatory lesions of the skin and mucous membranes. Forming a protective film with the protein substances of tissues, they protect the mucous membranes and the affected surface from irritation and prevent the further development of the inflammatory process.

In inflammatory processes of the gastrointestinal tract, especially in children, they are prescribed, for example, mucus from starch, flax seeds, rice water, etc.; they do not have an anti-inflammatory effect, but only protect the surface of the mucous membrane from irritation. Enveloping agents are also used when prescribing drugs, which, in addition to the main one, also have an irritating effect.

The listed groups of drugs do not directly affect the cause of inflammation. In contrast, chemotherapeutic drugs - sulfanilamide drugs, etc. - have specific anti-inflammatory properties, which are determined mainly by their ability to suppress the vital activity of certain microorganisms, to prevent the development of inflammatory processes in infectious diseases. They are used in inflammatory processes of infectious origin only as prescribed by a doctor.

- lek. in va, overwhelming manifestations become inflamed. processes. Differences in chem. structure and mechanisms of action cause P.'s division with. on steroid and non-steroid drugs. Steroid P. with. according to chem. structure belong to 11.17 dihydroxysteroids. Along… … Chemical Encyclopedia

The human body, for all its perfection, is made carelessly. Viruses, microbes, inflammatory diseases try to put a person in a hospital bed for a long time.

The health of the future peanut depends on the state of the female reproductive system.

Even if the baby is not included in your plans yet, then monitoring the correct functioning of the genital organs is not only useful, but extremely important for any girl.

Not a single woman is immune from inflammatory diseases. Of course, the disease is easier to prevent than to cure. But if you are already ill, then you need to scrupulously follow all the doctor's prescriptions.

Anti-inflammatory drugs - general information

Anti-inflammatory drugs are substances that suppress the inflammatory process. From the point of view of biochemistry, these substances prevent the formation or transformation of arachidonic acid.

Classification of anti-inflammatory drugs:

glucocorticosteroids are natural or synthetic hormones of the adrenal cortex;
non-steroidal anti-inflammatory drugs;
antibiotics and antimycotics.

All anti-inflammatory drugs are available both in injectable forms and in the form of tablets, suppositories.

What is used in gynecology?

Glucocorticosteroids are prescribed only for hormonal disorders. As anti-inflammatory drugs, they are not used in gynecology. For the treatment of female diseases, drugs of the second and third groups are used.

Medicines are prescribed for colpitis of various origins, vaginal dysbacteriosis, inflammatory processes in the uterus, appendages, fallopian tubes.

The form of administration and dosage is prescribed exclusively by the attending physician based on the diagnosis and history of the patient. Do not self-medicate!

Anti-inflammatory suppositories

Suppositories are the most common type of drug administration in gynecology.

Consider the most popular drugs, we take the main active ingredient as the basis for the classification.

Broad-spectrum antibiotics:

hexicon;
betadine;
polygynax;
mycogynax;
terzhinan.

Candles with metronidazole:

ginalgin;
terzhinan;
metronidazole;
klion-d.

Antimycotics - antifungal drugs:

candida;
pimafucin;
clotrimazole;
nystatin.

Antifungal agents are usually prescribed simultaneously in the form of suppositories and tablets. Currently, in gynecology, they are trying to use multicomponent anti-inflammatory drugs. This increases the effectiveness of the treatment.

Non-steroidal anti-inflammatory drugs

Any gynecological diseases can be accompanied by pain. Non-steroidal anti-inflammatory drugs are prescribed for pain relief.

This group of medicinal substances blocks the synthesis of prostaglandins, normalizes capillary permeability and the blood circulation process in general.

In addition, all drugs in this group reduce body temperature, eliminate pain, relieve swelling. Anti-inflammatory drugs are prescribed for endometriosis, adhesions, urogenital infections.

Medicines of the NSAID group are also used in everyday gynecological practice. They are used for pain relief during the installation of intrauterine contraceptives, endometrial biopsy, medical procedures on the cervix.

What doctors prescribe to patients:

Preparations of phenylacetic acid - various diclofenac sodium, potassium in different forms;
Derivatives of propionic acids - nurofen, naproxen, ibuprofen, ketoprofen;
Indomethacin is a drug based on indolacetic acid;
Coxibs - celecoxib, roferocoxib, denebol;
Enolic acid preparations - meloxicam, rheumoxicam, movalis.

In pharmacies, NSAIDs are presented in various forms - tablets, suppositories, injections.

Medicines of this group have a lot of contraindications and side effects. The main side effect is an aggressive effect on the mucous membrane of the stomach and intestines. If a woman has a history of an ulcer or other erosive processes in the gastrointestinal tract, these substances should be prescribed with great care.

Antibiotics in gynecology

Antibiotics are substances derived from fungi mold and bacteria. They are able to suppress other microorganisms.

Each type of antibiotic has a specific antimicrobial spectrum of action. Although at present, doctors prefer broad-spectrum drugs. But in some cases, a narrowly targeted antibiotic may be required.

It should be understood that not every antibacterial drug is an antibiotic.

In gynecology, the means of this group treat inflammatory processes, erosion, colpitis of various etiologies, they are prescribed after surgery.

The main drugs in this group:

Penicillin - is indicated in the treatment of endometritis, inflammation of the appendages, perimetritis, parametritis, cervicitis, bartholinitis, gonorrhea. Medicines of the penicillin series do not act on the tubercle bacillus. Penicillin is a toxic drug, so it should be used only as directed by a doctor.
Streptomycin - used if penicillin treatment fails. The drug is used to treat tuberculosis of the uterus, is prescribed for cystitis in pregnant women.
Biomycin - prescribed for the treatment of gonorrhea.
II-IV generation cephalosporins are broad-spectrum antibiotics. Shown in the treatment of many diseases, including gynecological.

Important! All antibiotics have a lot of side effects. Therefore, self-medication is unacceptable!

Anti-Inflammatory Herbs

Herbal medicines are often included in the complex treatment of various diseases. Decoctions, herbal extracts are also used in gynecology.

The most commonly used chamomile, oak bark, sage, calendula. It is important to understand that herbs are medicines. They have indications, contraindications and side effects.

Many gynecological diseases are not treated with herbs. Therefore, you should not self-medicate, even with the help of herbs. First you need to contact a gynecologist, undergo an examination, take tests, and only after that the doctor can determine the course of treatment.

Conclusions on anti-inflammatory therapy

A lot of pathological changes occurring in the body accompany the pain syndrome. To combat such symptoms, NSAIDs, or remedies, have been developed. They perfectly anesthetize, relieve inflammation, reduce swelling. However, the drugs have a large number of side effects. This limits their use in some patients. Modern pharmacology has developed the latest generation of NSAIDs. Such drugs are much less likely to cause unpleasant reactions, but they remain effective drugs for pain.

Impact principle

What is the effect of NSAIDs on the body? They act on cyclooxygenase. COX has two isoforms. Each of them has its own functions. Such an enzyme (COX) causes a chemical reaction, as a result of which it passes into prostaglandins, thromboxanes and leukotrienes.

COX-1 is responsible for the production of prostaglandins. They protect the gastric mucosa from unpleasant effects, affect the functioning of platelets, and also affect changes in renal blood flow.

COX-2 is normally absent and is a specific inflammatory enzyme synthesized due to cytotoxins, as well as other mediators.

Such an action of NSAIDs as inhibition of COX-1 carries many side effects.

New developments

It is no secret that the drugs of the first generation of NSAIDs had an adverse effect on the gastric mucosa. Therefore, scientists have set themselves the goal of reducing undesirable effects. A new release form has been developed. In such preparations, the active substance was in a special shell. The capsule was made from substances that did not dissolve in the acidic environment of the stomach. They began to break down only when they entered the intestines. This allowed to reduce the irritating effect on the gastric mucosa. However, the unpleasant mechanism of damage to the walls of the digestive tract still remained.

This forced chemists to synthesize completely new substances. From previous drugs, they are fundamentally different mechanism of action. NSAIDs of the new generation are characterized by a selective effect on COX-2, as well as inhibition of prostaglandin production. This allows you to achieve all the necessary effects - analgesic, antipyretic, anti-inflammatory. At the same time, NSAIDs of the latest generation make it possible to minimize the effect on blood clotting, platelet function, and the gastric mucosa.

The anti-inflammatory effect is due to a decrease in the permeability of the walls of blood vessels, as well as a decrease in the production of various inflammatory mediators. Due to this effect, irritation of the nerve pain receptors is minimized. The influence on certain centers of thermoregulation located in the brain allows the latest generation of NSAIDs to perfectly lower the overall temperature.

Indications for use

The effects of NSAIDs are widely known. The effect of such drugs is aimed at preventing or reducing the inflammatory process. These drugs give an excellent antipyretic effect. Their effect on the body can be compared with the effect. In addition, they provide analgesic, anti-inflammatory effects. The use of NSAIDs reaches a wide scale in the clinical setting and in everyday life. Today it is one of the most popular medical drugs.

A positive impact is noted with the following factors:

Diseases of the musculoskeletal system. With various sprains, bruises, arthrosis, these drugs are simply irreplaceable. NSAIDs are used for osteochondrosis, inflammatory arthropathy, arthritis. The drug has an anti-inflammatory effect in myositis, herniated discs.
Strong pains. The drugs are quite successfully used for biliary colic, gynecological ailments. They eliminate headaches, even migraines, kidney discomfort. NSAIDs are successfully used for patients in the postoperative period.
Heat. The antipyretic effect allows the use of drugs for ailments of a diverse nature, both for adults and children. Such medicines are effective even in fever.
thrombus formation. NSAIDs are antiplatelet agents. This allows them to be used in ischemia. They are a preventive measure against heart attack and stroke.

Classification

About 25 years ago, only 8 groups of NSAIDs were developed. Today, this number has increased to 15. However, even doctors cannot name the exact number. Having appeared on the market, NSAIDs quickly gained wide popularity. Drugs have replaced opioid analgesics. Because they, unlike the latter, did not provoke respiratory depression.

The classification of NSAIDs implies a division into two groups:

Old drugs (first generation). This category includes well-known drugs: Citramon, Aspirin, Ibuprofen, Naproxen, Nurofen, Voltaren, Diklak, Diclofenac, Metindol, Movimed, Butadion .
New NSAIDs (second generation). Over the past 15-20 years, pharmacology has developed excellent drugs, such as Movalis, Nimesil, Nise, Celebrex, Arcoxia.

However, this is not the only classification of NSAIDs. New generation drugs are divided into non-acid derivatives and acids. Let's look at the last category first:

Salicylates. This group of NSAIDs contains drugs: Aspirin, Diflunisal, Lysine monoacetylsalicylate.
Pyrazolidins. Representatives of this category are drugs: Phenylbutazone, Azapropazone, Oxyphenbutazone.
Oxycams. These are the most innovative NSAIDs of the new generation. List of drugs: Piroxicam, Meloxicam, Lornoxicam, Tenoxicam. Medicines are not cheap, but their effect on the body lasts much longer than other NSAIDs.
Derivatives of phenylacetic acid. This group of NSAIDs contains funds: Diclofenac, Tolmetin, Indomethacin, Etodolac, Sulindac, Aceclofenac.
Anthranilic acid preparations. The main representative is the medicine "Mefenaminat".
Propionic acid agents. This category contains many excellent NSAIDs. List of drugs: Ibuprofen, Ketoprofen, Benoxaprofen, Fenbufen, Fenoprofen, Thiaprofenic acid, Naproxen, Flurbiprofen, Pirprofen, Nabumeton.
Derivatives of isonicotinic acid. The main medicine "Amizon".
Pyrazolone preparations. The well-known remedy "Analgin" belongs to this category.

Non-acid derivatives include sulfonamides. This group includes drugs: Rofecoxib, Celecoxib, Nimesulide.

Side effects

NSAIDs of the new generation, the list of which is given above, have an effective effect on the body. However, they practically do not affect the functioning of the gastrointestinal tract. These drugs are distinguished by another positive point: NSAIDs of the new generation do not have a devastating effect on cartilage tissue.

However, even such effective means can provoke a number of undesirable effects. They should be known, especially if the drug is used for a long time.

The main side effects can be:

dizziness;
drowsiness;
headache;
fatigue;
increased heart rate;
increase in pressure;
slight shortness of breath;
dry cough;
indigestion;
the appearance of protein in the urine;
increased activity of liver enzymes;
skin rash (spot);
fluid retention;
allergy.

At the same time, damage to the gastric mucosa is not observed when taking new NSAIDs. The drugs do not cause an exacerbation of the ulcer with the occurrence of bleeding.

Phenylacetic acid preparations, salicylates, pyrazolidones, oxicams, alkanones, propionic acid and sulfonamide drugs have the best anti-inflammatory properties.

From joint pain most effectively relieve medications "Indomethacin", "Diclofenac", "Ketoprofen", "Flurbiprofen". These are the best NSAIDs for osteochondrosis. The above drugs, with the exception of the drug "Ketoprofen", have a pronounced anti-inflammatory effect. This category includes the tool "Piroxicam".

Effective analgesics are Ketorolac, Ketoprofen, Indomethacin, Diclofenac.

Movalis has become the leader among the latest generation of NSAIDs. This tool is allowed to be used for a long period. Anti-inflammatory analogues of an effective drug are the drugs Movasin, Mirloks, Lem, Artrozan, Melox, Melbek, Mesipol and Amelotex.

The drug "Movalis"

This drug is available in the form of tablets, rectal suppositories and a solution for intramuscular injection. The agent belongs to the derivatives of enolic acid. The drug has excellent analgesic and antipyretic properties. It has been established that in almost any inflammatory process, this medicine brings a beneficial effect.

Indications for the use of the drug are osteoarthritis, ankylosing spondylitis, rheumatoid arthritis.

However, you should know that there are contraindications to taking the drug:

hypersensitivity to any of the components of the drug;
peptic ulcer in the acute stage;
severe renal failure;
ulcer bleeding;
severe liver failure;
pregnancy, child feeding;
severe heart failure.

The drug is not taken by children under 12 years of age.

Adult patients diagnosed with osteoarthritis are recommended to use 7.5 mg per day. If necessary, this dose can be increased by 2 times.

With rheumatoid arthritis and ankylosing spondylitis, the daily norm is 15 mg.

Patients who are prone to side effects should take the drug with extreme caution. People who have severe renal failure and who are on hemodialysis should take no more than 7.5 mg throughout the day.

The cost of the drug "Movalis" in tablets of 7.5 mg, No. 20, is 502 rubles.

The opinion of consumers about the drug

Reviews of many people who are prone to severe pain indicate that Movalis is the most suitable remedy for long-term use. It is well tolerated by patients. In addition, its long stay in the body makes it possible to take the medicine once. A very important factor, according to most consumers, is the protection of cartilage tissues, since the drug does not adversely affect them. This is very important for patients who apply arthrosis.

In addition, the medicine perfectly relieves various pains - toothache, headache. Patients pay particular attention to the impressive list of side effects. While taking NSAIDs, the treatment, despite the warning of the manufacturer, was not complicated by unpleasant consequences.

The drug "Celecoxib"

The action of this remedy is aimed at alleviating the patient's condition with osteochondrosis and arthrosis. The drug perfectly eliminates pain, effectively relieves the inflammatory process. No adverse effects on the digestive system have been identified.

The indications for use given in the instructions are:

osteoarthritis;
rheumatoid arthritis;
ankylosing spondylitis.

This drug has a number of contraindications. In addition, the medicine is not intended for children under 18 years of age. Particular caution must be observed in people who are diagnosed with heart failure, as the drug increases the susceptibility to fluid retention.

The cost of the drug varies, depending on the packaging, in the region of 500-800 rubles.

Consumer opinion

Quite conflicting reviews about this medicine. Some patients, thanks to this remedy, were able to overcome joint pain. Other patients claim that the drug did not help. Thus, this remedy is not always effective.

In addition, you should not take the drug yourself. In some European countries, this medicine is banned because it has a cardiotoxic effect, which is quite unfavorable for the heart.

The drug "Nimesulide"

This medicine has not only anti-inflammatory and anti-pain effects. The tool also has antioxidant properties, due to which the drug inhibits substances that destroy cartilage and collagen fibers.

The remedy is used for:

arthritis;
arthrosis;
osteoarthritis;
myalgia;
arthralgia;
bursitis;
fever
various pain syndromes.

In this case, the drug has an analgesic effect very quickly. As a rule, the patient feels relief within 20 minutes after taking the drug. That is why this remedy is very effective in acute paroxysmal pain.

Almost always, the medicine is well tolerated by patients. But sometimes side effects may occur, such as dizziness, drowsiness, headache, nausea, heartburn, hematuria, oliguria, urticaria.

The product is not approved for use by pregnant women and children under 12 years of age. With extreme caution should take the drug "Nimesulide" people who have arterial hypertension, impaired functioning of the kidneys, vision or heart.

The average price of a medicine is 76.9 rubles.

14221 0

Inflammatory reactions- these are universal protective and adaptive reactions to the impact of various exogenous and endogenous damaging factors (microorganisms, chemical agents, physical effects, etc.), which play an important role in the pathogenesis of most diseases of the maxillofacial region (periodontitis, alveolitis, periostitis, osteomyelitis, acute herpetic gingivostomatitis, etc.). This process is initiated and maintained by endogenous biologically active substances (prostaglandins, thromboxane, prostacyclin, leukotrienes, histamine, interleukins (IL), NO, kinins), which are produced in the focus of inflammation.

Despite the fact that inflammation is a protective reaction, the 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, 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, chemical structure, physicochemical properties, pharmacokinetics. , pharmacodynamics, as well as 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 a resorptive action, but also with topical 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 liquefaction of pus, mucus and other products of inflammatory origin. In dental practice, proteases, nucleases and lyases are most commonly used.

Non-steroidal anti-inflammatory drugs and non-narcotic analgesics

Index of drug descriptions

Acetylsalicylic acid
Benzydamine
diclofenac
ibuprofen
Indomethacin
Ketoprofen
Ketorolac
Lornoxicam
Meloxicam
Metamizole sodium
Nimesulide
Paracetamol
Piroxicam
Phenylbutazone
Celecoxib
INN is missing

Holisal

The widespread use of NSAIDs in dentistry is due to the spectrum of their pharmacological activity, which includes anti-inflammatory, analgesic, antipyretic, and antiplatelet effects. This allows the use of NSAIDs in the complex therapy of inflammatory processes in the maxillofacial area, for drug preparation of patients before performing traumatic interventions, as well as to reduce pain, swelling and inflammation after they are performed. The analgesic and anti-inflammatory activity of NSAIDs has been proven in numerous controlled trials that meet the standards of "evidence-based medicine".

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 derived from a number of organic acids: anthranilic acid - mefenamic acid and flufenamic acid; indolacetic - indomethacin (methindol), phenylacetic - diclofenac (ortofen, voltaren, etc.), phenylpropionic - ibuprofen (brufen), propionic - ketoprofen (artrosilene, OKI, ketonal), naproxen (naprosin), heteroaryl acetic - ketorolac (ketalgin, ketanov, ketorol) and oxicam derivatives (piroxicam (pyroxifer, hotemin), lornoxicam (xefocam), meloxicam (movalis).

NSAIDs have the same type of effects, but their severity in drugs of different groups varies significantly. So, paracetamol has a central analgesic and antipyretic effect, and 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 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 predominantly block COX-2 (meloxicam, nimesulide, celecoxib, etc.), which are better tolerated, especially risk group patients with a history of peptic ulcer of the stomach and duodenum, bronchial asthma, kidney damage, blood clotting disorders.

Mechanism of action and pharmacological effects

NSAIDs inhibit COX, a key enzyme in the metabolism of arachidonic acid, which regulates 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 in the focus of inflammation, thereby weakening the mechanical pressure on nociceptors.

In recent years, it has been shown that the prevention of activation of immunocompetent cells in the early stages of inflammation is important in the anti-inflammatory effect of these drugs. NSAIDs increase the content of intracellular Ca2+ in T-lymphocytes, which contributes to their proliferation, the synthesis of interleukin-2 (IL-2) and the suppression of neutrophil activation. A relationship was 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 under 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 in 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 in NSAIDs, solutions of which have a neutral pH. They accumulate less in the focus of inflammation, penetrate the BBB faster, affect the thalamic centers of pain sensitivity, suppressing COX in the central nervous system. NSAIDs reduce the level of PG in the brain structures involved in the conduction of 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 manifests itself only at elevated temperatures. This is due to inhibition of PGE1 synthesis in the CNS and inhibition of their activating effect on the thermoregulatory center located in the hypothalamus.

The inhibition of platelet aggregation is due to the blockade of COX and inhibition of the synthesis of thromboxane A2. With prolonged use of NSAIDs, a desensitizing effect develops, which is due to a decrease in the formation of PGE2 in the focus of inflammation and leukocytes, inhibition of blast transformation of lymphocytes, 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 PG involved in the regulation of homeostasis and affecting trophism and functional activity of cells, and COX-2 is an enzyme that is normally found only in some organs (brain, kidneys, bones, female reproductive system). 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, as a result of which the activity and toxicity of drugs increase.

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 more rapidly excreted in alkaline urine. Some NSAIDs (indomethacin, ibuprofen, naproxen) are excreted by 10-20% unchanged, and therefore, with kidney disease, their concentration in the blood may change. T1 / 2 in different drugs in this group varies significantly. To drugs with a short T1 / 2 (1-6 hours) include acetylsalicylic acid, diclofenac, ibuprofen, indomethacin, ketoprofen, etc., to drugs with a long T1 / 2 (more than 6 hours) - 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 edema after trauma, surgery, pain syndrome, arthrosis and arthritis of the temporomandibular joint, myofascial pain syndrome of the maxillofacial region, neuritis, neuralgia, postoperative pain, fever.

Tolerability and side effects

NSAIDs are widely and uncontrolledly used as anti-inflammatory, analgesic and antipyretic drugs, while 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 reactions.

When using NSAIDs, especially coursework, complications from many systems and organs are possible.

From the gastrointestinal tract: stomatitis, nausea, vomiting, flatulence, epigastric pain, constipation, diarrhea, ulcerogenic effect, gastrointestinal bleeding, gastroesophageal reflux, cholestasis, hepatitis, jaundice.
From the side of the central nervous system and sensory organs: headache, dizziness, irritability, fatigue, insomnia, tinnitus, hearing loss, impaired sensitivity, 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, angioedema, anaphylactic shock.
From the skin and subcutaneous fat: rash, bullous eruptions, erythema multiforme, erythroderma (exfoliative dermatitis), alopecia, photosensitivity, toxicoderma.

The most common complications associated with COX-1 inhibition (gastrointestinal lesions, impaired renal function and platelet aggregation, effects on the circulatory system).

Contraindications

Hypersensitivity to drugs of this group.
Course therapy of NSAIDs is contraindicated:

- with peptic ulcer of the stomach and duodenum;
- with leukopenia;
- with severe damage to the kidneys and liver;
- in the first trimester of pregnancy;
- during lactation;
- children under 6 years old (meloxicam - up to 15 years old, ketorolac - up to 16 years old).

Cautions

NSAIDs should be used with caution in patients with bronchial asthma, arterial hypertension and heart failure. Elderly patients are advised to prescribe low doses and short courses of NSAIDs.

Interaction

When taken together with anticoagulants, antiplatelet agents and fibrinolytics, the risk of gastrointestinal bleeding increases. When combined with β-blockers or angiotensin-converting enzyme (ACE) inhibitors, the antihypertensive effect may decrease. NSAIDs increase the side effects of corticosteroids and estrogens. Deterioration of kidney function can be observed when NSAIDs are combined with potassium-sparing diuretics (triamterene), ACE inhibitors, cyclosporine. The combination of paracetamol with barbiturates, anticonvulsants and ethyl alcohol increases the risk of a hepatotoxic state. The use of paracetamol in conjunction 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	Metindol
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

Content

Pain in the joints is excruciating and unbearable, it prevents a person from living normally. Many people have firsthand experience of how difficult it is to tolerate this phenomenon. If this problem has also affected you, then non-steroidal anti-inflammatory drugs for the treatment of joints will come to the rescue. You will soon find out which of them are really capable of relieving pain.

What are non-steroidal anti-inflammatory drugs

These drugs are abbreviated as NSAIDs. They begin the medical treatment of arthrosis. Anti-inflammatory drugs are called nonsteroidal because they do not contain hormones. They are safer for the body and give a minimum of side effects. There are selective agents that act directly on the focus of inflammation, and non-selective agents that also affect the organs of the gastrointestinal tract. The first one is preferable.

Treatment of joints NSAIDs

Means must be prescribed by a doctor, based on the intensity of pain and the manifestation of other symptoms. Diagnoses in which NSAIDs help:

infectious, aseptic, autoimmune, gouty or rheumatoid arthritis;
arthrosis, osteoarthritis, deforming osteoarthritis;
osteochondrosis;
rheumatic arthropathy: psoriasis, ankylosing spondylitis, Reiter's syndrome;
bone tumors, metastases;
pain after surgery, trauma.

Anti-inflammatory drugs for joints

The range includes pharmacological agents in the form of:

tablets;
intramuscular injections;
injections into the joint itself;
plasters;
candles;
creams, ointments.

In severe forms of joint diseases and a deterioration in the patient's well-being, the doctor, as a rule, prescribes stronger medicines. They help quickly. We are talking about injections in the joint. Such drugs do not spoil the gastrointestinal tract. In milder forms of the disease, the specialist prescribes pills, intramuscular injections. The use of creams and ointments is always recommended as an addition to the main therapy complex.

Tablets

There are such effective NVPS (means):

"Indomethacin" (another name is "Metindol"). Pills for joint pain relieve inflammation, have an antipyretic effect. The drug is drunk twice or thrice a day for 0.25-0.5 g.
"Etodolak" ("Etol Fort"). Produced in capsules. Anesthetizes quickly. Acts on inflammation. It should be taken one tablet 1-3 times after meals.
"Aceclofenac" ("Aertal", "Diclotol", "Zerodol"). diclofenac analogue. The drug is taken on a tablet twice a day. The drug often causes side effects: nausea, dizziness.
"Piroxicam" ("Fedin-20"). They have an antiplatelet effect, relieve pain, fever. The dosage and rules of admission are always determined by the doctor, based on the severity of the disease.
Meloxicam. Tablets are prescribed one or two per day after the disease passes from the acute stage to the next.

Ointments for the treatment of joints

Classification:

With ibuprofen ("Dolgit", "Nurofen"). An anti-inflammatory and analgesic ointment for joints with such a main component will help those with arthritis, trauma. Acts very quickly.
With diclofenac ("Voltaren", "Diklak", "Diclofenac", "Diklovit"). Such medicinal ointments warm up, relieve pain and block inflammatory processes. Quickly help those who have difficulty moving.
With ketoprofen ("Ketonal", "Fastum", "Ketoprofen Vramed"). Prevent the formation of blood clots. With too long use of ointments, a rash may appear on the body.
With indomethacin ("Indomethacin Sopharma", "Indovazin"). They act similarly to drugs based on ketoprofen, but less intensively. They warm well, help with rheumatoid arthritis, gout.
With piroxicam ("Finalgel"). They relieve painful symptoms, do not dry the skin.

injections

There are such NSAIDs for injection:

"Diclofenac". Relieves inflammation, pain, is prescribed for severe diseases. Intramuscularly injected 0.75 g of the drug once or twice a day.
"Tenoxicam" ("Teksamen L"). Soluble powder for injection. 2 ml per day is prescribed for mild pain syndrome. The dose is doubled and a five-day course is prescribed for gouty arthritis.
"Lornoxicam" ("Larfix", "Lorakam"). 8 mg of the drug is injected into a muscle or vein once or twice a day.

Anti-inflammatory non-steroidal drugs of a new generation

More modern, and therefore more effective means:

"Movalis" ("Mirloks", "Artrozan"). A very effective drug, produced in tablets, injection solution, suppositories. Virtually no side effects. For injections use 1-2 ml of solution per day. Tablets are taken at 7.5 mg once or twice a day.
"Celecoxib". Does not have a detrimental effect on the stomach. Take one or two tablets per day, but not more than 0.4 g of the drug per day.
Arcoxia. The drug is in tablets. The dosage is prescribed depending on the severity of the disease.
"Nimesulide". Available in tablets, sachets for dilution, in the form of a gel. The dose is determined by the doctor, as well as the rules of admission.