Studies of the pharmacokinetic properties of nimorazole.
The pharmacokinetics of the hypoxic radio-sensitizer nimorazole were studied in 19 individuals after single oral doses of between 0.5-3.5 g. HPLC measurements showed, after a rapid absorption, a linear relationship between peak plasma concentration and given dose. Mean elimination half life was 3.1 h. A tendency to a dose-dependent variation in the apparent volume of distribution, total body clearance and elimination half life suggest non-linear pharmacokinetics of nimorazole. Tumour concentrations measured in 5 patients gave tumour/plasma ratios between 0.8-1.3. No toxicity was observed. The results indicate that nimorazole may have potential as a clinically useful hypoxic radiosensitizer.
D000328:Adult; D000368:Aged; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D005260:Female; D006207:Half-Life; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D008875:Middle Aged; D009369:Neoplasms / Q000378:metabolism; D009554:Nimorazole / Q000378:metabolism*; D009593:Nitroimidazoles / Q000378:metabolism*; D013997:Time Factors
D009593:Nitroimidazoles; D009554:Nimorazole