HINGAMYN (Chingaminum; synonym: Artrochin, Chloroquini Diphosphas, Delagil, Nivachine, Resochin, etc.; GFH, joint venture. B) — antimalarial and antiamoebic means. 4 (1-Metil-4-dietilaminobutil-amino) - a 7-hlorkhinolyna diphosphate; C18H26C1N3 * 2H3P04:
Inodorous crystal powder, white or white with a subtle creamy shade, or almost inodorous, bitter taste. Let's easily dissolve in water, we will dissolve in 95% alcohol, chloroform, ether and benzene very little; g°pl 214,5 — 218 ° (with decomposition), a pier. weight (weight) 515,9. Water solutions (pH 3,5 — 4,5) will sterilize at t ° 115 ° within 30 min.
Chingaminum exerts destructive influence on sexless erythrocyte forms of plasmodiums of malaria of all types, but does not affect their fabric and sexual forms, i.e. is antimalarial drug of preferential gematoshizotropny action (see. Antimalarial means). Also fabric forms of a dysenteric amoeba are sensitive to Chingaminum (see the Amebiasis). Mechanisms of antiprotozoan action of Chingaminum are a little studied. It is established that it oppresses nek-ry types of an intracellular metabolism (hl. obr. amino acids) at protozoa. It can be caused by the fact that Chingaminum breaks metabolism of nucleic acids by formation of complexes with them.
Except antiprotozoan action, nek-ry other properties are inherent in Chingaminum. So, it possesses immunodepressive and antiinflammatory effect, a cut most clearly is shown at its use in therapy of rheumatic diseases, collagenic diseases and some other systemic lesions of connecting fabric. The immunodepressive effect of Chingaminum consists in weakening of hl. obr. allergic reactions of the slowed-down type (see the Allergy).
It exerts considerably less expressed impact on allergic reactions of immediate type. The antiinflammatory effect of Chingaminum is characterized by preferential influence of drug on a proliferative phase of an inflammation. It affects an acute exudative inflammation rather poorly and only at prolonged use. Assume that the mechanism of an immunodepressive effect of Chingaminum is caused by generally oppressing influence of this drug on development of lymphoid cells. Besides, Chingaminum slows down reaction antigen — an antibody (see Antigen — an antibody reaction) and reduces the level of the circulating immunoglobulins. Antiinflammatory properties of drug connect with its stabilizing influence on membranes of lysosomes, decrease in power ensuring process of an inflammation owing to oppression of formation of ATP, braking of activity of the nek-ry enzymes (hyaluronidase, a collagenase, etc.) participating in genesis of separate manifestations of an inflammation. Antipro-liferativny the effect, obviously, is caused by the oppressing influence of Chingaminum on development of fibroblasts, and also on processes of synthesis and maturing of collagen.
Chingaminum is well soaked up in blood at different ways of introduction. In blood it for 50 — 60% contacts albumine of plasma. It is deposited preferential in parenchymatous bodies, partially — in skin, hair, cartilaginous and synovial tissue. Besides, it intensively communicates melanin and therefore in high concentration collects in an iris and a retina of an eye. Metabolism of Chingaminum happens hl. obr. in a liver with formation of N-dietilkhlorokhina, to-ry then is oxidized in a 4-amino-7-hlorkhino-lean. Chingaminum and its metabolites are allocated with kidneys and through went. - kish. path. Elimination half-life 2V2 — 5 days. Removal of Chingaminum from an organism amplifies under the influence of ammonium of chloride and donators of sulphhydryl groups, napr, Unithiolum (see).
As antiprotozoan means Chingaminum is applied to treatment and individual chemoprophylaxis of malaria (see), and also an abenteric amebiasis (see). The clinic of internal diseases uses it for treatment of rheumatism, a pseudorheumatism, a system lupus erythematosus, a scleroderma, an amyloidosis of kidneys, a glomerulonephritis, hron. hepatitis, recurrent and hron. forms of infectious and allergic myocarditis. Besides, Chingaminum renders to lay down. effect at Shegren's syndrome (see Shegren a syndrome), a sar-koidoza (see), a periodic disease (see). In nek-ry cases use
518 QUINHYDRONE ELECTRODE
of Chingaminum promote recovery of a sinoatrial rate at premature ventricular contraction and a paroxysmal form me r tsa those l no y and ritmiya.
For treatment of malaria Chingaminum is appointed inside after food the adult on 2 — 2,5 g to a course of treatment. At the same time in the first day appoint 1 g of drug in one step (at tropical malaria sometimes in addition enter 0,5 more g in 6 — 8 hours). To the 2nd and 3rd day appoint 0,5 g in one step. The highest doses for adults inside: one-time 0,5 g, daily 1,5 g. To children Chingaminum is appointed according to the following scheme: aged till 1 year in the first day — 0,05 g, for
the 2nd and 3rd day — 0,025 g; at the age of 1 — 6 years respectively 0,125 and 0,05 g; at the age of 6 — 10 years — 0,25 and 0,125 g; at the age of 10 — 15 years — 0,5 — 0,25 g. At tropical malaria in case of need treatment is carried out within 5 days. At the malignant course of malaria (coma, algidny, fulminant forms), and also at vomiting and a diarrhea Chingaminum is entered intramusculary or intravenously (kapelno) in the form of 5% of solution the adult on 10 ml. The daily dose for adults shall not exceed 30 ml of 5% of solution. To children Chingaminum is entered parenterally in a daily dose at the rate of 8,3 mg of drug of a pas of 1 kg of body weight.
For individual chemoprophylaxis of malaria it is possible to appoint Chingaminum inside the adult on 0,25 g 2 — 3 times a week, and at high risk of infection with tropical malaria — on 0,5 g 2 times a week or on 0,25 g every other day during the entire period of stay in the endemic area, or a season of transfer of the causative agent of malaria. With the same purpose to children aged till 1 year appoint 0,025 g of drug; at the age of 1 — 6 years — on 0,05 g; 6 — 10 years — on 0,125 g; 10 — 15 years — on 0,25 g 2 times a week.
At an abenteric amebiasis Chingaminum is appointed inside the adult in the first two days on 0,5 g by 2 times a day, then during 2 — 3 weeks on 0,5 g a day (in 1 — 2 reception). At infiltrative forms of amoebic abtsess of a liver, lungs and a brain Chingaminum is appointed on 0,25 g by 2 times a day during 2 — 3 weeks. Along with it enter intramusculary emetine a hydrochloride (see Emetin) on 1 ml of 1% of solution of 1 times a day within a week.
At general diseases of connecting fabric (collagenic diseases, etc.) Chingaminum is appointed inside the adult on 0,25 — 0,5 g a day long courses. As antiarrhythmic means it is accepted inside on 0,25 g by 2 — 3 times a day, gradually reducing a dose to 0,25 g of 1 times a day.
Side effect of Chingaminum is observed, as a rule, only at prolonged use of drug and shown by nausea, vomiting, a loss of appetite, dizzinesses, a headache, weight loss, canities, dermatitis, a leukopenia, a sonitus. Typical manifestation of side effect of Chingaminum are vision disorders (disorders of accommodation, decrease in visual acuity, feeling of flashing in eyes, a retinopathy). In high doses it can cause damages of a liver and dystrophic changes of a myocardium. At bystry intravenous administration development of a collapse is possible.
Chingaminum is contraindicated at a serious illness of heart, diffusion damage of kidneys, decrease in functions of a liver, defeats of an eyeground, organic diseases of c. N of page, psychoses.
Treatment by Chingaminum it is necessary to carry out iod by control of a picture of blood, functions of a liver, kidneys and sight.
Forms of release: powder; tablets on 0,25 g; 5% solution in ampoules on
5 ml. Storage: powder — in well corked container protecting from effect of light; tablets and ampoules — in the place protected from light.
Bibliography: Clinical pharmacology, under the editorship of V. V. Zakusov, page 551, M., 1978; M and sh to about in with to and y M. D. Pharmaceuticals, p. 2, page 332, M., 1984; N the expert about N about in and V. A., etc. Pharmacotherapy in rheumatology, page 99, M., 1976.
V. K. Muratov.