Urinary excretion of mefloquine and some of its metabolites in African volunteers at steady state. 1987

D E Schwartz, and G Eckert, and J M Ekue
Biological Pharmaceutical Research Department, F. Hoffmann-La Roche & Co. Ltd., Basel, Switzerland.

Because of the extremely long terminal elimination half-life of mefloquine it is practically impossible to measure quantitatively its urinary excretion after a single dose. Indeed, a correct estimation would require collection of urine over a period of several months. This difficulty was overcome by measuring excretion in the course of a multiple-dose study when steady-state conditions had been reached. Six male African volunteers were given at an interval of 1 week 250 mg mefloquine base in the form of its hydrochloride. Urine was quantitatively collected from each subject during the 11th week and analyzed for unchanged drug and its alcohol and acid metabolites. Excretion of the unchanged drug and of its acid metabolite amounted respectively to 9% (5.2-13.1%) and 4.2% (2.9-6.2%) of the weekly dose. Concentrations of the alcohol metabolite were too low to be measured.

UI MeSH Term Description Entries
D008297 Male Males
D008657 Metabolic Clearance Rate Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site. Total Body Clearance Rate,Clearance Rate, Metabolic,Clearance Rates, Metabolic,Metabolic Clearance Rates,Rate, Metabolic Clearance,Rates, Metabolic Clearance
D011804 Quinolines
D005919 Glomerular Filtration Rate The volume of water filtered out of plasma through glomerular capillary walls into Bowman's capsules per unit of time. It is considered to be equivalent to INULIN clearance. Filtration Rate, Glomerular,Filtration Rates, Glomerular,Glomerular Filtration Rates,Rate, Glomerular Filtration,Rates, Glomerular Filtration
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000293 Adolescent A person 13 to 18 years of age. Adolescence,Youth,Adolescents,Adolescents, Female,Adolescents, Male,Teenagers,Teens,Adolescent, Female,Adolescent, Male,Female Adolescent,Female Adolescents,Male Adolescent,Male Adolescents,Teen,Teenager,Youths
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D001711 Biotransformation The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
D015767 Mefloquine A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects. Lariam,Mefloquine Hydrochloride,Mephloquine,Ro-21-5998-001,WR-142,490,WR-177,602,Ro 21 5998 001,Ro215998001,WR 142,490,WR 177,602,WR142,490,WR177,602

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