Pharmacology: Pharmacokinetics: Metronidazole is readily absorbed following administration by mouth and bioavailability approaches 100%. Peak plasma concentrations of approximately 5 and 10 μg per mL are within 1 to 2 hours after single doses of 250 and 500 respectively. Some accumulation and consequently higher concentrations occur when multiple doses are given. Absorption may be delayed, but is not reduced over all by administration with food.
Following the intravenous administration of metronidazole, peak-steady steady state plasma concentrations of about 25 μg per mL with trough concentrations of about 18 μg per mL have been reported in patients given a loading dose of 15 mg per kg body weight followed by 7.5 mg per kg every 6 hours. The bioavailability of Metronidazole from rectal suppositories is 60 to 80%; peak plasma concentrations are half those with equivalent oral doses and occur after about 5 to 12 hours. Absorption from vaginal pessaries has been reported to be poor.
Metronidazole is widely distributed. It appears in most body tissue and fluid bile, bone, breast milk, cerebral abscesses, saliva, seminal fluid and vaginal secretions and achieves concentrations similar to those in plasma. No more than 20% is bound to plasma proteins.
The elimination half-life of Metronidazole is about 8 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; that of hydroxy metabolite is prolonged patients with renal failure.
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