Орнидазол

Описание

Ornidazole is an orally bioavailable 5-nitroimidazole derivative with antibacterial and antiprotozoal activities. Ornidazole inhibits the growth of clinical isolates of B. fragilis (MICs = 0.5-5 μM) and various anaerobic bacteria when used at concentrations ranging from less than 0.1 to 3.2 μg/ml. It also inhibits the growth of Giardia isolates (IC₅₀s = 0.01-0.47 μg/ml). Oral administration of ornidazole reduces T. vaginalis and T. foetus infection in mice and E. histolytica infection in rats with curative dose (CD₅₀) values of 37, 3, and 10 mg/kg, respectively. Ornidazole (400 mg/kg per day) induces infertility in male rats within 7 days and inhibits spermatozoa binding to rat oocyte zona pellucida.

Химические свойства

Crystalline Solid

Использование

Ornidazole is a drug that cures some protozoan infections. It has been investigated for use in Crohn's disease after bowel resection. It is indicated in treatment of mixed amoebiasis, mixed amoebic dysentery, mixed giardiasis, trichomoniasis, bacterial vaginosis, Sexually transmitted diseases, infections of gynaecology, lower respiratory tract infections, ENT, surgical and dental infections.

Определение

ChEBI: A C-nitro compound that is 5-nitroimidazole in which the hydrogens at positions 1 and 2 are replaced by 3-chloro-2-hydroxypropyl and methyl groups, respectively. It is used in the treatment of susceptible protozoal infections and for the treatment of anaerobic bacterial infections.

Фармацевтические приложения

A 5-nitroimidazole available for oral administration, intravenous infusion and as a vaginal pessary. Its activity closely parallels that of metronidazole and tinidazole.
Peak plasma levels after a single 750 mg or 1.5 g oral dose reach 11 mg/L and 30 mg/L, respectively, within about 2 h. The half-life is 12–14 h. It is well absorbed from the vagina, with peak plasma concentrations of 5 mg/L being reached 12 h after the insertion of a 500 mg vaginal pessary. After a single 1 g intravenous infusion for colorectal surgery, serum levels reached about 24 mg/L after 15 min and about 6 mg/L after 24 h. It has wide tissue distribution, including CSF. Plasma protein binding is 10–15%.
It is metabolized in the liver, mainly to hydroxymethyl derivatives. The plasma clearance rate decreases in hepatic failure because of reduced liver metabolism and decreased biliary elimination. About 60% of an oral dose is recovered in the urine and 20% in the feces. The dosing interval should be doubled in patients with severe hepatic impairment, but it is unnecessary to reduce the dose in patients with impaired renal function. It is removed by hemodialysis.
Toxicity and side effects are similar to those of metronidazole and tinidazole and it has similar clinical uses. It has been shown to be effective for the prevention of recurrence of Crohn’s disease after ileocolonic resection.

Профиль безопасности

Poison by intravenous route. Moderately toxic by ingestion and intraperitoneal routes. Experimental reproductive effects. Mutation data reported. Whenheated to decomposition it emits very toxic fumes of Clí and NOx.