METRONIDAZOLE (Metronidazolum; synonym: Klionum, orvagil, Trichopolum, flagyl, Clont, Efloran, Entizol, Flagyl, Metronidazole, Orvagil, Trichopol, Vagimid etc.) — antiprotozoan means. 1 (beta Hydroxyethyl) - a 2-methyl-5-nitroimidazole; With 6 H 9 O 3 N 3 :
White or slightly chartreuse crystal powder. We will dissolve in water a little, it is difficult — in alcohol.
The m has activity of hl. obr. concerning a number of protozoa — trichomonads, amoebas, lyambliya and balantidiya. From activators of other types koktsidiya and Bacteroides fragilis are sensitive to it. Has weak antikholinesterazny activity and has local irritative effect. At introduction inside it is quickly soaked up from went. - kish. a path also collects in blood in the maximum concentration in 2 — 3 hours. An elimination half-life — 6 — 8 hour. In blood M. there is a hl. obr. in the state connected with proteins. It is metabolized with formation of inactive products. Collects preferential in a liver, kidneys, a wall of intestines, lungs and a brain. M.'s removal and its metabolites comes from an organism hl. obr. with urine, partially with a stake, and at a lactation — and with breast milk; 15 — 58% of the accepted dose are allocated in not changed look. Gets through a placental barrier and it is found in fabrics of a fruit, however has no teratogenic effect.
As chemotherapeutic means of M. is applied to treatment of a trichomoniasis, an amebiasis, a lambliasis and a balanthidiasis.
Drug is appointed inside in time or after food. Tablets should be swallowed, without chewing.
Treatment acute and hron, an urogenital trichomoniasis at men and women is carried out, appointing M. courses of different duration (6 and 10 days). At a 6-day course M. appoint in the 1st day 0,5 g 2 times (with an interval of 12 hours), to the 2nd day — on 0,25 g 3 times (in 8 hours), in the next 4 days — on 0,25 g 2 times (in 12 hours). The general course dose for adults — 3,75 g. At a 10-day course M. appoint 0,25 g 2 times a day during all course. M.'s appointment to women intravaginalno in the form of candles or vaginal tablets significantly does not influence results of treatment. Sanitation at men comes usually in a day after an initiation of treatment, at women — in 1 — 2 day. For an exception of a possibility of reinfection it is reasonable to carry out simultaneous treatment of both sexual partners. If necessary courses of treatment of M. are repeated in 4 — 6 weeks.
For treatment of amoebic dysentery and an abenteric (fabric) amebiasis of M. appoint by the adult 0,25 g 2 — 3 times a day, to children from 2 to 5 years — on 0,25 g a day, from 5 to 10 years — on 0,375 g, from 10 to 15 years — on 0,5 g a day (in 1 — 2 reception). At amoebic abscesses the daily dose the adult is increased to 1 g. Duration of a course of treatment at an amebiasis usually 10 days. Improvement of the general state occurs on 2 — the 4th day; vegetative forms of amoebas disappear on 5 — the 6th day.
At a lambliasis metronidazole is appointed by the adult on 0,25 g by 2 times a day within 5 days. For children the dose of drug is reduced according to age (as at an amebiasis).
Along with antiprotozoan properties M. has also ability to cause disgust for alcohol in this connection it is used at treatment of alcoholism. At M.'s alcoholism appoint courses till 18 — 24 in the afternoon, in the 1st day — in a daily dose of 0,75 g, then the dose is daily increased by 0,25 — 0,5 g to a daily dose by 2,5 g. In 8 — 10 days the daily dose is gradually reduced to 0,75 pages. The daily dose is divided into 2 — 3 receptions.
The general course dose — 30 — 42 g. In the course of treatment daily on 1-3 times carry out alcoholic tests. Disgust for alcohol develops usually on 4 — the 8th day of treatment. Lack of effect to 8 — means to the 10th day that the patient is steady against M. V action such cases continuation of reception of M. is inexpedient. For the supporting treatment of alcoholics of M. appoint 1-1,5 g 2 — 3 times a day courses for 10 — 12 days. Breaks between courses of 20 days. As protrezvlyayushchy means at alcoholic intoxication of M. is appointed on 1 — 2,5 g by 2 — 3 bucketed times 1 hour (a daily dose of 4 — 6 g). Sobering up is followed by vomiting.
Side effect of drug is sometimes shown by loss of appetite, nausea, vomiting, diarrhea, a headache, drowsiness, serdtsebiyeniye, allergic reactions and oppression of a leukopoiesis. These phenomena pass upon termination of treatment or at drug withdrawal. At women at M.'s treatment development of a candidiasis of a vagina is possible, for prevention and treatment to-rogo it is necessary to appoint antifungal means, napr, nystatin (see), levorinum (see). At M.'s treatment cases of an asymptomatic current of an initial stage of syphilis without influence on the further course of a disease are described. In this regard at M.'s appointment it is recommended to exclude a disease of syphilis. As a contraindication to M.'s use serve diseases of the hemopoietic bodies, acute diseases of c. N of page and pregnancy. During treatment it is impossible to take alcoholic drinks.
Form of release: tablets on 0,25 g and 0,5 g; vaginal tablets and candles on 0,5 g. Keep in the place protected from light.
Bibliography: The pharmacological basis of therapeutics, ed. by L. S. Goodman a. A. Gilman, L., 1975.
H. A. Novitskaya.