Abstract:
:Piperaquine (PQ) is an antimalarial drug whose high lipid solubility suggests that its absorption can be increased by a high-fat meal. We examined the pharmacokinetics of PQ phosphate (500 mg given orally) in the fasting state and after a high-fat meal in eight healthy Caucasian volunteers (randomized crossover). Plasma PQ concentration-time profiles were analyzed by using noncompartmental pharmacokinetic analysis. In the fed state, the geometric mean Cmax increased by 213%, from 21.0 to 65.8 microg/liter (P<0.001). The time of Cmax was not significantly different between the fasting and fed states. The geometric mean area under the concentration-time curve from zero onward (AUC0-infinity) increased by 98%, from 3,724 to 7,362 microg h/liter (P=0.006). The oral bioavailability of PQ relative to the fasting state was 121% greater after the high-fat meal (95% confidence interval, 26 to 216% increase; P=0.020). The side effects, postural blood pressure changes, electrocardiographic corrected QT interval, serum glucose, and other biochemical and hematological indices were similar in the fasting and fed states over 28 days of follow-up.
journal_name
Antimicrob Agents Chemotherjournal_title
Antimicrobial agents and chemotherapyauthors
Sim IK,Davis TM,Ilett KFdoi
10.1128/AAC.49.6.2407-2411.2005subject
Has Abstractpub_date
2005-06-01 00:00:00pages
2407-11issue
6eissn
0066-4804issn
1098-6596pii
49/6/2407journal_volume
49pub_type
临床试验,杂志文章,随机对照试验abstract::The pharmacogenetics of antimalarial agents are poorly known, although the application of pharmacogenetics might be critical in optimizing treatment. This population pharmacokinetic-pharmacogenetic study aimed at assessing the effects of single nucleotide polymorphisms (SNPs) in cytochrome P450 isoenzyme genes (CYP, n...
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journal_title:Antimicrobial agents and chemotherapy
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doi:
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journal_title:Antimicrobial agents and chemotherapy
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