EMETYN (Emetinum; synonym: Ipecine, Methylcephaelin) — an antiparasitic; the alkaloid which is contained in roots of a tropical shrubby plant of an ipecacuanha (Seryayonz ipecacuanha Willd) this. madder family (Rubiaceae).
AA. allocate from roots of an ipecacuanha (see) or receive in the polusinteti-chesky way from alkaloid of the tsefelin (see) which is contained in the same plant.
In the medical practician E. apply in the form of dihydrochloride (Emetini hydro-chloridum; synonym of Emetinum hydro-chloricum; GFH; joint venture. Б). Z-Etil-
2, 3, 4, 6, 7, 11-hexahydro-9, 10-dimetoksi-2-(1, 2, 3,
4-tetragidro-6, 7-dimetoksi-1-isoquinolylmethyl)-1 N-benzo [and] cinchona of a lysine dihydrochloride; G29H40N2O4 • 2 HC1 • 7 H20:
Inodorous white crystal powder, bitter taste. On light slightly turns yellow. Let's easily dissolve in water (1: 8), alcohol and chloroform. It is insoluble on air. Pier. the weight (weight) — 553,6 (anhydrous), 679,6 (water). Water solutions will sterilize at t ° 100 ° within 30 min.; pH of 1% of solution 4,5 — 6,0.
Has pernicious effect on activators of an amebiasis and balanthidiasis. It is effective also at nek-ry trematodoza, for example at shistosomatoza. The mechanism of its proti-voprotozoyny action is connected with the fact that E. breaks intracellular synthesis of protein at protozoa by inhibition of process of a translocation peptidil-transport-ache RNA between donorny and acceptor sites of ribosomes. Efficiency E. at shistosomatoza it is caused, obviously, the fact that E. inhibits cholinesterase of trematodes and thereof will paralyze their suckers. Due to strongly expressed local irritative effect of emetine on fabric at intake it causes reflex vomiting and a diarrhea, and at hit on mucous membranes of an eye — conjunctivitis. Expectorant and emetic effects of drugs of a root of an ipecacuanha are caused by availability of emetine in them.
In the medical practician E. enter parenterally since the expressed local irritative action on went. - kish. path E. limits its enteral use. After intramuscular introduction E. it is quickly soaked up in blood, out of an organism it is brought very slowly and deposited in nek-ry bodies. In the greatest concentration E. collects in a liver. In high concentration it is found also in lungs, kidneys, a spleen and a wall of intestines. Through a blood-brain barrier does not get. It is brought out of an organism preferential through kidneys. After single introduction it is found in urine within 40 — 60 days.
AA. apply generally at acute amoebic dysentery (in the presence in Calais of amoebas erythrophages and big fabric forms of amoebas) and nek-ry forms of an abenteric amebiasis (e.g., at amoebic hepatitises and abscesses of a liver). Efficiency E. at these forms of an amebiasis it is caused by ability of drug in a significant amount to be deposited in a liver. Besides, E. sometimes use for treatment of shistosomatoz.
In medical practice according to all indications apply emetine a hydrochloride, solutions to-rogo enter intramusculary or deeply under skin.
At an amebiasis the adult appoint on 1,5 ml 1% of solution of drug 2 times a day. Duration of a course of treatment at amoebic dysentery averages 4 — 6 days (as much as possible — no more than 8 days), and at an abenteric amebiasis — 7 — 8 days.
At amoebic dysentery treatment E. stop after subsiding of acute displays of a disease (the termination of ponos, emergence of the issued or semi-issued chair, disappearance of fabric forms of amoebas in Calais). After cancellation E. treatment is continued by contact amebo-tsidny drugs, napr, Chiniofonum (see), epteroseptoly (see), tetracyclines (see) or other antiamoebic means. At abenteric forms of an amebiasis E. usually appoint in combinations with Chingaminum (see) or metronidazole (see).
The highest doses for adults: one-time — 0,05 g (5 ml of 1% of solution), daily — 0,1 g (10 ml of 1% of solution). Dose E. on a course of treatment shall not exceed 0,1 g on 1 kg of body weight of the patient.
To children E. appoint in the following daily doses: from 6 months to 1 year — 0,005 g; from 1 to 2 years — 0,01 g; from 2 to 5 years — 0,02 g; from 5 to 9 years — 0,03 g; from 9 to 15 years — 0,04 g. To children up to 6 months E. do not appoint.
Side effect E. it is shown by nausea, vomiting, ponosa, abdominal pains, headaches. At cumulation of drug emergence of hypotension, heartaches, tachycardias, changes of an ECG is possible (inversion or flattening of a tooth of T in all assignments, lengthening of an interval of QT, a depression of a segment S T). AA. can also cause muscular weakness, a tremor, muscular pains, polyneurites.
At emergence of symptoms of intoxication E. cancel. For reduction of toxic effect of drug it is possible to use thiamin (see).
Contraindications to use of emetine are organic heart diseases, the central and peripheral nervous system, pregnancy, the expressed adynamy.
Form of release: powder, ampoules on 1 ml of 1% of solution. Storage: powder — in well corked container protecting from effect of light; ampoules — in the place protected from light.
See also Antiparasitics, Vomitives. Bibliography: Clinical pharmacology, under the editorship of V. V. Zakusov, page 554, M., 1978; Mashkovsky M. D. Pharmaceuticals, p. 2, page 350, M., 1984; The pharmacological basis of therapeutics, ed. by A. G. Gilman a. o., N. Y., 1980.
V. K. Muratov.