Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2018 Publisher: Creo Pharma Limited, Felsted Business Centre, Felsted, Essex, CM6 3LY
Pharmacotherapeutic group: Nitroimidazole derivatives
ATC Code: P01AB01
Metronidazole has antiprotozoan and antibacterial effects. It is effects against Trichomonas vaginalis, Gardnerella vaginalis and other protazoa including Entamoeba histolytica, Gardia lamblia and anaerobic bacteria.
Metronidazole is readily absorbed following administration by mouth and bioavailability is 90-100%. Peak plasma concentrations of approximately 5µg/ml and 10µg/ml are achieved an average of 1-2 hours after single doses of 250mg and 500mg respectively. Some accumulation and consequently higher concentrations occur when multiple doses are given. Absorption may be delayed, but is not reduced overall, by administration with food.
Metronidazole is widely distributed. It appears in most body tissues and fluids. It also crosses the placenta and rapidly enters foetal circulation. No more than 20% is bound to plasma proteins.
Metronidazole is metabolised in the liver by side-chain oxidation and glucuronide formation.
The plasma elimination half-life of metronidazole is about 6-9 hours; that of the hydroxy metabolite is slightly longer. The half-life of metronidazole is reported to be longer in neonates and in patients with severe liver disease.
The majority of a dose of metronidazole is excreted in the urine, mainly as metabolites; a small amount appears in the faeces.
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