PMID: 38081May 1, 1979

Biotransformation of mazindol. II. Absorption and excretion in the dog and man

Drug Metabolism and Disposition : the Biological Fate of Chemicals
H A Dugger, J G Heider


On administration of tritium-labeled mazindol (l) to man and the dog, absorption was slow but complete. Excretion was slow in both dog and man, but the dog did excrete the drug and/or metabolites faster than man. Blood levels of l in man after a single oral dose of a 2-mg tablet reached a peak value of 2.5 ng/ml, which remained essentially unchanged for at least 6 hr. After multiple doses of a 2-mg tablet t.i.d. for 4 days to subjects who had been receiving nonlabeled l, 2 mg t.i.d. for 6 months, the blood level reached a maximum concentration of 10.8 ng/ml, measured 2 hr after the last dose on day 4. This value is somewhat higher than predicted by the single-dose data, indicating that in man, mazindol does not induce its own metabolism.

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