Document Detail

Does gender, food or grapefruit juice alter the pharmacokinetics of primaquine in healthy subjects?
MedLine Citation:
PMID:  16722829     Owner:  NLM     Status:  MEDLINE    
AIMS: To evaluate the effects of gender, food and grapefruit juice on the pharmacokinetics of primaquine in healthy subjects.
METHODS: 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.
RESULTS: 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).
CONCLUSIONS: 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.
Bui Tri Cuong; Vu Quoc Binh; Bui Dai; Dinh Ngoc Duy; Claire M Lovell; Karl H Rieckmann; Michael D Edstein
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Publication Detail:
Type:  Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  British journal of clinical pharmacology     Volume:  61     ISSN:  0306-5251     ISO Abbreviation:  Br J Clin Pharmacol     Publication Date:  2006 Jun 
Date Detail:
Created Date:  2006-05-25     Completed Date:  2007-01-18     Revised Date:  2013-06-07    
Medline Journal Info:
Nlm Unique ID:  7503323     Medline TA:  Br J Clin Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  682-9     Citation Subset:  IM    
Department of Infectious Disease, Central Military Hospital, Hanoi, Vietnam.
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MeSH Terms
Antimalarials / pharmacokinetics*
Citrus paradisi*
Food-Drug Interactions
Primaquine / pharmacokinetics*
Sex Characteristics
Reg. No./Substance:
0/Antimalarials; 90-34-6/Primaquine

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