Document Detail

Variability in the metabolism of proguanil to the active metabolite cycloguanil in healthy Kenyan adults.
MedLine Citation:
PMID:  2091335     Owner:  NLM     Status:  MEDLINE    
Extensive metabolizers (EM) and poor metabolizers (PM) of the malaria chemoprophylactic drug proguanil have been identified by measuring the proguanil/cycloguanil ratio in urine following a single dose of the pro-drug. The pharmacokinetic characteristics of proguanil were similar in 8 EM and 8 PM subjects, but there were significant differences between the 2 groups with respect to cycloguanil pharmacokinetics. In none of the PM subjects could cycloguanil be detected in whole blood samples at any time after proguanil dosage. Plasma cycloguanil was measureable in only 2 of 8 PM subjects, despite an analytical sensitivity in the high-performance liquid chromatographic assay of 1 ng/ml cycloguanil. A comparatively high proportion of Black Kenyan adults appear to metabolize proguanil poorly, possibly because they lack the specific mixed function oxidase which will accept proguanil as substrate.
W M Watkins; E K Mberu; C G Nevill; S A Ward; A M Breckenridge; D K Koech
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Transactions of the Royal Society of Tropical Medicine and Hygiene     Volume:  84     ISSN:  0035-9203     ISO Abbreviation:  Trans. R. Soc. Trop. Med. Hyg.     Publication Date:    1990 Jul-Aug
Date Detail:
Created Date:  1991-06-03     Completed Date:  1991-06-03     Revised Date:  2009-09-29    
Medline Journal Info:
Nlm Unique ID:  7506129     Medline TA:  Trans R Soc Trop Med Hyg     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  492-5     Citation Subset:  IM    
Kenya Medical Research Institute, Nairobi.
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MeSH Terms
Chloroguanide / blood,  pharmacokinetics*,  urine
Malaria / prevention & control
Plasmodium falciparum
Prodrugs / pharmacokinetics*
Triazines / blood,  pharmacokinetics*,  urine
Grant Support
//Wellcome Trust
Reg. No./Substance:
0/Prodrugs; 0/Triazines; 500-92-5/Chloroguanide; 516-21-2/cycloguanil

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