Does gender, food or grapefruit juice alter the pharmacokinetics of primaquine in healthy subjects?
- 27 February 2006
- journal article
- research article
- Published by Wiley in British Journal of Clinical Pharmacology
- Vol. 61 (6), 682-689
- https://doi.org/10.1111/j.1365-2125.2006.02601.x
Abstract
To evaluate the effects of gender, food and grapefruit juice on the pharmacokinetics of primaquine in healthy subjects. In a randomized, two-phase cross-over study, 10 male and 10 female healthy Vietnamese subjects were administered 30 mg primaquine in the fasting state or with food, followed by administration of primaquine with grapefruit juice. The pharmacokinetics of primaquine were comparable between male and female subjects, with geometric mean ratios of Cmax = 0.89 [95% confidence interval (CI) 0.65, 1.22] and AUC = 0.80 (95% CI 0.56, 1.15). The mean CL/F of primaquine was slightly higher in males than in females [0.52 l h(-1) kg(-1)vs. 0.43 l h(-1) kg(-1), mean difference of 0.09 (95% CI -0.10, 0.28), P = 0.32]. When compared with fasting state values, food increased the geometric mean Cmax of primaquine by 26% (95% CI 12, 40) and the AUC by 14% (95% CI 3, 27). Similarly, grapefruit juice increased the geometric mean Cmax by 23% (95% CI 4, 45) and the AUC by 19% (95% CI 4, 37). The disposition of primaquine was comparable between genders, suggesting no need to modify the dose of primaquine for malaria treatment or prophylaxis. Food increased the oral bioavailability of primaquine, which may lead to higher antimalarial efficacy. Grapefruit juice increased the bioavailability of primaquine, with marked interindividual differences suggesting that people should not take primaquine with grapefruit juice.Keywords
This publication has 25 references indexed in Scilit:
- Can primaquine therapy for vivax malaria be improved?Trends in Parasitology, 2003
- How Important Are Gender Differences in Pharmacokinetics?Clinical Pharmacokinetics, 2002
- Grapefruit juice–drug interactionsBritish Journal of Clinical Pharmacology, 1998
- Drug Interactions with Grapefruit JuiceClinical Pharmacokinetics, 1997
- Examination of some factors responsible for a food‐induced increase in absorption of atovaquone.British Journal of Clinical Pharmacology, 1994
- Primaquine metabolism by human liver microsomes: effect of other antimalarial drugsBiochemical Pharmacology, 1992
- Effects of food on drug absorptionPharmacology & Therapeutics, 1989
- Atomic physicochemical parameters for three-dimensional-structure-directed quantitative structure-activity relationships. 2. Modeling dispersive and hydrophobic interactionsJournal of Chemical Information and Computer Sciences, 1987
- Pharmacokinetics of primaquine in man. I. Studies of the absolute bioavailability and effects of dose size.British Journal of Clinical Pharmacology, 1985
- Pharmacokinetics of primaquine in man: identification of the carboxylic acid derivative as a major plasma metabolite.British Journal of Clinical Pharmacology, 1984