Ниморазол

Описание

Nimorazole is 5-nitroimidazole with antimicrobial and radiosensitizing activities. It is active against T. vaginalis in a Coulter counter antimicrobial assay (EC₅₀ = 2.55 fmol/cell) and G. intestinalis (IC₅₀ = 0.393 μM). Nimorazole reduces the number of vaginal trichomonads in a mouse model of T. vaginalis intravaginal infection (ED₅₀ = 5.62 mg/kg). Under hypoxic conditions, nimorazole enhances radiation-induced SCC-7 tumor cell death in vitro and in vivo.

Использование

Nimorazole is an antimicrobial with activity against anaerobic bacteria and protozoa.

Фармацевтические приложения

An orally administered 5-nitroimidazole. It is slightly soluble in water at room temperature, soluble in alcohols, acetone and chloroform. The spectrum includes T. vaginalis, G. lamblia, E. histolytica, anaerobic bacteria and G. vaginalis. Activity against B. fragilis and Fusobacterium spp. is similar to or slightly less than that of metronidazole (mean MIC 0.25–1 mg/L).
A peak blood concentration of about 32 mg/L occurs within 2 h of a 500 mg oral dose. High concentrations are achieved in saliva and vaginal secretions. Excretion is principally via the urine where the drug appears as metabolites which display antimicrobial and antiprotozoal activity less than that of the parent drug.
It is generally well tolerated even at the high doses required in conjunction with radiotherapy for the treatment of head and neck tumors. Adverse effects are the same as those of metronidazole. Disulfiram-like reactions appear to be rare.
Clinical uses are similar to those of metronidazole. It is also used as a hypoxic radiosensitizer in the radiotherapy of head and neck tumors.