ABSORPTION, DISTRIBUTION, AND EXCRETION IN MICE OF THE ANTI-MALARIAL MEFLOQUINE, ERYTHRO-2,8-BIS(TRIFLUOROMETHYL)-ALPHA-(2-PIPERIDYL)-4-QUINOLINEMETHANOL HYDROCHLORIDE
Following oral administration of 14C-labeled mefloquine hydrochloride to female mice, the drug was well absorbed and distributed throughout the body. At 24 and 48 h after dosing, the majority of radiolabel remaining in the body was in the form of parent drug. The major route of radiolabel excretion was fecal after oral or i.p. administration, with approximately 20% in the urine by 240 h. The elimination t1/2 of unchanged drug after oral or i.p. dosing was 18.7 and 13.5 h, respectively, for urine and 14.5 and 15.4 h, respectively, for feces. The t1/2 of parent drug after oral administration was 17.0 h for plasma and 18.6 h for erythrocytes. The erythrocyte concentration of drug was approximately 5 times the plasma concentration.