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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
|
| pubmed:dateCreated |
1997-4-24
|
| pubmed:abstractText |
Mefloquine (MQ) is a chiral antimalarial agent effective against chloroquine-resistant Plasmodium falciparum. It is commercially available as a racemic mixture of the (+) and (-) enantiomers for oral administration. The pharmacokinetics of the (+) and (-) enantiomers of MQ were studied in eight healthy volunteers after administration of a first oral dose of 250 mg of racemic MQ and at steady state after 13 repeated doses of 250 mg given at 1-week intervals. Plasma samples were collected, and concentrations of each enantiomer were determined using a previously described achiral-chiral double column-switching liquid chromatographic method. At each time point, higher plasma concentrations values were found for the (-) enantiomer (p < 0.001). At steady state, Cmax values of (-)-MQ were higher than those of (+)-MQ (1.42 +/- 0.19 versus 0.26 +/- 0.05 mg/L; p < 0.001). Similarly, the plasma concentrations 7 days after the final dose were higher for (-)-MQ (1.01 +/- 0.26 versus 0.11 +/- 0.04 mg/L; p < 0.001). AUC values at steady state were also higher for (-)-MQ (197.3 +/- 36.7 versus 30.1 +/- 8.9 mg/L x h; p < 0.001). The terminal half-life values (T1/2beta) were longer for (-)-MQ (430.4 +/- 225.2 versus 172.8 +/- 56.5 h; p < 0.001). This study shows that the pharmacokinetics of MQ is highly stereoselective.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jun
|
| pubmed:issn |
0022-3549
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
83
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
824-7
|
| pubmed:dateRevised |
2004-11-17
|
| pubmed:meshHeading |
pubmed-meshheading:9120814-Adult,
pubmed-meshheading:9120814-Antimalarials,
pubmed-meshheading:9120814-Biological Availability,
pubmed-meshheading:9120814-European Continental Ancestry Group,
pubmed-meshheading:9120814-Female,
pubmed-meshheading:9120814-Humans,
pubmed-meshheading:9120814-Male,
pubmed-meshheading:9120814-Mefloquine,
pubmed-meshheading:9120814-Stereoisomerism
|
| pubmed:year |
1994
|
| pubmed:articleTitle |
Stereoselective pharmacokinetics of mefloquine in healthy Caucasians after multiple doses.
|
| pubmed:affiliation |
Hôpital Pitié Salpêtrière, Pharmacie, Pharmacocinétique, Paris, France.
|
| pubmed:publicationType |
Journal Article
|