The fate of metronidazole and tis implications in chemotherapy.
1. [14C]Metronidazole was rapidly absorbed from the gastro-intestinal tract of rats giving maximum blood levels of radioactivity, equivalent to 6-4 and 6-7 mug metronidazole per ml blood, 1 h after oral dosing. 2. There was rapid equilibration between blood and most tissues, although radioactivity was concentrated in the liver, kidney, gastro-intestinal tract and vaginal secretions. 3. The half-life of clearance of radioactivity from the majority of tissues was between 3 and 4 h, although it was longer in the skin (8 h) and gastro-intestinal tract (14 h). 4. Fourteen radioactive excretion products were detected in rat urine and all the major products were identified. These all contained a nitro group and represented 97 degrees of the total radioactivity excreted in urine. 5. Unchanged metronidazole was secreted throughout the entire length of the gastro-intestinal tract and into the vagina of rats. 6. A hypothesis has been proposed to explain the high clinical efficacy of metronidazole in treating trichomonal and amoebic infections.
D000284:Administration, Oral; D000818:Animals; D001345:Autoradiography; D001646:Bile / Q000378:metabolism; D001682:Biological Availability; D002849:Chromatography, Gas; D002855:Chromatography, Thin Layer; D004064:Digestive System / Q000378:metabolism; D004358:Drug Therapy; D005243:Feces / Q000378:metabolism; D005260:Female; D006900:Hydroxylation; D007275:Injections, Intravenous; D007408:Intestinal Absorption; D008795:Metronidazole / Q000097:blood / Q000378:metabolism* / Q000652:urine; D009928:Organ Specificity; D010084:Oxidation-Reduction; D051381:Rats; D014621:Vagina / Q000378:metabolism
D008795:Metronidazole