ANTIRHEUMATIC MEANS — the pharmaceuticals applied to pharmacotherapy of rheumatic diseases (rheumatism, a pseudorheumatism, collagenic diseases, arthroses, etc.).
There is no standard classification of P. of page. Because in a pathogeny of the majority of rheumatic diseases the leading role is played by processes of an inflammation and an allergy (autoallergy), as P. villages use the pharmaceuticals influencing these processes. Pages belong to such P. steroid and nonsteroid anti-inflammatory drugs (see), drugs gold (see), some immunodepressive substances (see), immunostimulators, D-penitspllamin and some derivatives of quinoline. Besides, pages carry the drugs operating to P. and on other pathogenetic mechanisms of a number of rheumatic diseases, napr, the drugs influencing metabolism of cartilaginous tissue, and also the means lowering contents uric to - you in an organism.
From number steroid anti-inflammatory drugs as P. pages apply hydrocortisone (see), Prednisonum (see), Prednisolonum (see), dexamethasone (see), Triamcinolonum (see) and other drugs of glucocorticoids, and from among non-steroidal anti-inflammatory drugs — salicylates, napr, acetylsalicylic acid (see), sodium salicylate (see), etc., derivatives indolacetic to - you, napr, indometacin (see), sulindak, derivatives fenilpropionovy to - you, napr, diclofenac-sodium (Voltarenum), derivatives anthranilic to - you (antranilata), napr, mefenamovy to - that, etc., derivatives pyrazol it, e.g. analginum (see), pyramidon (see), Butadionum (see), etc.
From group drugs of gold as P. villages use some of its organic compounds in the form of water solutions (sanokrizin, miokrizin, etc.) and the oil suspensions (Crysanolum, etc.) intended for parenteral administration.
From immunodepressive most as P. pages were widely used substances some cytostatic drugs: Azathioprinum, Cyclophosphanum (see), Chlorbutinum (see), methotrexate (see). Besides, possess antirheumatic action also anti-lymphocytic serum (see) and anti-lymphocytic globulin.
To number P. of the page operating with hl. obr. on metabolism of cartilaginous tissue, carry Rumalonum and arteparon which use for treatment of arthroses. The drugs influencing contents in an organism uric to - you, together with the nek-ry other means applied at gout usually allocate in special group antigouty means (see).
On character and the mechanism of action, and also by efficiency at various rheumatic diseases separate groups P. of page differ from each other. So, antirheumatic action of glucocorticoids is caused by hl. obr. the expressed antiinflammatory and immunodepressive properties of drugs of this group. Glucocorticoids are effective at rheumatism (see) irrespective of manifestations and localization of rheumatic process, pseudorheumatism (see), collagenic diseases and other rheumatic diseases of inflammatory and autoimmune genesis, and also at the secondary synovites developing against the background of dystrophic and exchange diseases of joints. Glucocorticoids are most effective when these diseases proceed with a high degree of activity.
Non-steroidal anti-inflammatory drugs have antirheumatic effect of hl. obr. as a result of suppression of processes of an inflammation in tissues of joints and internals. Besides, these drugs have analgetic properties: they weaken pains at various diseases of joints. In revmatol. to practice drugs of this group are used but to the same indications, as glucocorticoids. However on force of action non-steroidal anti-inflammatory drugs concede to glucocorticoids and therefore are most effective at the rheumatic diseases proceeding with rather low degree of activity. Non-steroidal anti-inflammatory drugs often combine with glucocorticoids (especially in the course of cancellation of the last) and other P. page, napr, with derivatives of quinoline, drugs of gold, etc. At the choice of drugs from group of non-steroidal anti-inflammatory drugs it must be kept in mind that they are various on force of antiinflammatory and analgetic action. The most active among them are sulindak, indometacin, Voltarenum, Naproxenum.
Drugs of gold differ in a narrow range of antirheumatic action. They render antiinflammatory effect concerning an active synovitis only at a pseudorheumatism and, on a nek-eye to data, at a juvenile pseudorheumatism, sarkoidozny arthritis and psoriasis arthritis. At extraarticular (system) manifestations of a pseudorheumatism drugs of gold are not shown, and at other rheumatic diseases are inefficient. The mechanism of effect of these drugs remains obscure. Assume that their effect at a pseudorheumatism can be caused by linkng of ions of gold with sulphhydryl groups of various proteins owing to what there is an inhibition of lizosomalny enzymes, disturbance of formation of a rhematoid factor, and also stabilization of collagen. Besides, drugs of gold slow down proliferation and transformation of lymphocytes and inhibit a complement, having at the expense of it a nek-swarm an immunodepressive effect.
D-Penicillaminum like drugs of gold possesses a narrow range of antirheumatic action and it is effective generally at a pseudorheumatism. According to some scientists, it is effective also at a scleroderma. At the diseases connected with histocompatibility antigens of HLA B27 (Bekhterev's disease, etc.), and other rheumatic diseases D-Penicillaminum neeffek tiven. About the mechanism of its antirheumatic action there is no conventional representation. Assumed that D-Penicillaminum has antirheumatic effect due to decrease in a copper content in an organism. However it is not established to correlation between to lay down. effect of drug and extent of decrease in a copper content under its influence. Ability of D-Penicillaminum to inactivate a rhematoid factor, obviously, has also no crucial importance in the mechanism of antirheumatic effect of this drug since it is effective not only at the arthritis proceeding with high credits of this factor but also at seronegative forms of a pseudorheumatism. It is not excluded that D-Penicillaminum has a nek-swarm an immunodepressive effect since, according to experimental data, it oppresses synthesis of immunoglobulins V-lymphocytes and suppresses transformation of lymphocytes in response to stimulation by antigenic and mitogenetic factors.
Applied in rheumatology immunodepressants (a methotrexate, Cyclophosphanum, etc.) have antirheumatic effect of hl. obr. due to suppression of processes of an allergy (autoallergy) by disturbance of proliferation of immunocompetent cells. Besides, these drugs thanks to the cytostatic properties can exert the oppressing impact on * a proliferative phase of an inflammation. As P. immunodepressants apply page generally at collagenic diseases and a pseudorheumatism, and sometimes — at rheumatism and psoriasis arthritis. It must be kept in mind that immunodepressants are shown only in cases of a heavy course of these diseases (e.g., at quickly progressing forms of collagenic diseases, lupoid nephrite, joint and visceral and septic forms of a pseudorheumatism with the expressed extraarticular manifestations, etc.), and also at inefficiency - other P. of page and need of replacement of glucocorticoids.
Derivatives of quinoline by the principle of action are close to immuno-depressants and exert the oppressing impact on processes of an immunogenesis (reduce the maintenance of a rhematoid factor and some other autoimmune components, slow down development and transformation of lymphocytes). It is possible also that their antirheumatic effect is partly caused by the stabilizing influence on lysosomes and oppression of synthesis and maturing of collagen. On antirheumatic activity derivatives of quinoline concede to immunodepressants, D-Penicillaminum and drugs of gold. Derivatives of quinoline are effective at rheumatism, collagenic diseases, a pseudorheumatism and some other rheumatic diseases. Usually derivatives of quinoline use in a combination with steroid and non-steroidal anti-inflammatory drugs.
Experience of use of an immunostimulator of levamisole in rheumatology is limited. There are data on efficiency of this drug at a pseudorheumatism, a syndrome of Reuters, a system lupus erythematosus and some other rheumatic diseases.
Drugs of gold, D-Penicillaminum, immunodepressants, derivatives of quinoline and levamisole differ from glucocorticoids and non-steroidal anti-inflammatory drugs in the following features of antirheumatic action: slow development to lay down. effect, more considerable suppression of displays of a disease, rather long (several weeks, months) preservation of improvement or remission after the termination of treatment. In this regard the specified drugs allocate in the special group designated as P. by page of long action (basic antirheumatic drugs, drugs of the second row). Such drugs in an initiation of treatment it is necessary to combine page (non-steroidal anti-inflammatory drugs or glucocorticoids) with high-speed P.
Usually P. pages appoint counting on their systemic action. At the same time for stopping of signs of an acute synovitis villages use some P. counting on local action and for this purpose enter vnutrisustavno. Apply some glucocorticoids to topical (intra joint) treatment (a hydrocortisone, Kenalogum, etc.), cytostatic substances (Cyclophosphanum, Thiophosphamidum), etc. With the same purpose sometimes use colloid solutions of radioactive gold or yttrium, and also Contrykal.
Side effect of P. of page of separate groups is shown unequally. So, glucocorticoids cause the phenomena of a hypercorticoidism, dispeptic disturbances, a hyperglycemia, ulcerogenic effect, etc. The irritation belongs to the heaviest side effects of non-steroidal anti-inflammatory drugs went. - kish. path and ulcerogenic effect. Drugs of gold can cause cytopenias, a nephropathy, neurotoxic effects, skin rashes, damages of mucous membranes (stomatitis, conjunctivitis), etc. Cytopenias, damages of kidneys, skin rashes, in rare instances heavy autoimmune syndromes are characteristic of side effect of D-Penicillaminum. Immunodepressants can cause oppression of a hemopoiesis, an exacerbation latentno of the proceeding infections, went. - kish. frustration, etc. At prolonged use of derivatives of quinoline dispeptic frustration, vision disorders, skin rashes are possible. Side effect of levamisole is shown by nausea, vomiting, a leukopenia, skin rashes, fever. Sometimes levamisole causes encephalopathy and an agranulocytosis.
Bibliography: Bibikova T. I. and Sigidin Ya. A. Treatment of rheumatism quinolinic drugs, M., 1974, bibliogr.; Clinical pharmacology, under the editorship of V. V. Zakusov, page 140, M., 1978; Muratov V. K. About the mechanism of action of antirheumatic means, Owls. medical, No. 9, page 57, 1972, bibliogr.; N the expert about N about in and V. A., etc. Pharmacotherapy in rheumatology, M., 1976; Ya. A Whitefishes dynes. Mechanisms of medical action of antirheumatic means, M., 1972, bibliogr.; Sigidin Ya. A., etc. Current trends in pharmacotherapy of a pseudorheumatism, Rubbed. arkh., t. 52, No. 1, page 78, 1980, bibliogr.; Trinus F. P., M about hort N. A. and Klebanov B. M. Non-steroidal anti-inflammatory drugs, Kiev, 1975, bibliogr.; Jasinowski M. Ya., etc. Salicylates, M., 1975, bibliogr.; In and at H. C. Use and abuse of corticosteroids in rheumatic diseases, Drugs, v. 19, p. 447, 1980; With r an i g G. L. a. Bucha-n a n W. W. Antirheumatic drugs, cli-nical pharmacology and therapeutic use, ibid., v. 20, p. 453; Reinicke C. u. T a n n e r E. Moderne Konzeptionen über den pharmakologischen Wirkungsmechanismus von Antirheumatika, Z. ges. inn. Med., Bd 29, S. 873, 1974.
Century of K. Muratov.