Pharmacokinetic comparison of leucovorin and levoleucovorin

The pharmacokinetic values of d,l-leucovorin and l-leucovorin were compared in eight healthy volunteers following oral administration of 25 mg d,l-leucovorin and 12.5 mg l-leucovorin. Serum levels of l-5-formyltetrahydrofolate, l-5-methyltetrahydrofolate, and total reduced folates were measured by a...

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Bibliographic Details
Published in:European journal of clinical pharmacology 1993-07, Vol.44 (6), p.569-573
Main Authors: ZITTOUN, J, TONELLI, A. P, MARQUET, J, DE GIALLULY, E, HANCOCK, C, YACOBI, A, JOHNSON, J. B
Format: Article
Language:English
Subjects:
Adolescent
Adult
Biological and medical sciences
General and cellular metabolism. Vitamins
Humans
Leucovorin - administration & dosage
Leucovorin - pharmacokinetics
Male
Medical sciences
Middle Aged
Pharmacology. Drug treatments
Stereoisomerism
Tetrahydrofolates - pharmacokinetics
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Summary:The pharmacokinetic values of d,l-leucovorin and l-leucovorin were compared in eight healthy volunteers following oral administration of 25 mg d,l-leucovorin and 12.5 mg l-leucovorin. Serum levels of l-5-formyltetrahydrofolate, l-5-methyltetrahydrofolate, and total reduced folates were measured by an established microbiological method. Pharmacokinetic data for both preparations were consistent with those previously reported for d,l-leucovorin, with essentially complete first pass metabolism to l-5-methyltetrahydrofolate, the active metabolite. No differences were found between the two preparations in serum concentrations of active folate fractions, AUC, or Cmax, or in clearance and volume of distribution estimates. These data suggest that after administration of 25 mg of d,l-leucovorin, the d-diastereoisomer has no significant effect on the standard pharmacokinetic measurements of the active l-folates.
ISSN:0031-6970
1432-1041
DOI:10.1007/BF02440861