Pharmacokinetics of primaquine in man: identification of the carboxylic acid derivative as a major plasma metabolite.

摘要: A method is described for the simultaneous determination of carboxylic acid and N-acetyl-derivatives primaquine, in plasma urine. After oral administration 45 mg to five healthy volunteers, absorption was rapid, with peak primaquine levels 153.3 +/- 23.5 ng/ml at 3 1 h, followed by an elimination half-life 7.1 1.6 systemic clearance 21.1 l/h, volume distribution 205 371 cumulative urinary excretion 1.3 0.9% dose. Primaquine underwent rapid conversion metabolite which achieved 1427 307 7 4 h. Levels this were sustained excess 1000 24 h study period, no carboxyprimaquine recovered N-acetyl not detected or Following [14C]-primaquine one subject, radioactivity rapidly exceeded concentrations. Plasma accounted mainly as . Though 64% dose over 143 [14C]-radioactivity urine, only 3.6% due primaquine. As neither nor N- acetylprimaquine remaining unidentified metabolites.