Publication: Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine.
Accepted Date
2010-10-11
Issued Date
2010-10-11
Copyright Date
2010
Resource Type
Language
eng
ISSN
1475-2875 (electronic)
Rights
Mahidol University
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BioMed Central
Bibliographic Citation
Ali S, Najmi MH, Tarning J, Lindegardh N. Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine. Malar J. 2010 Oct 11;9:275.
Suggested Citation
Ali, Shabana, Najmi, Muzammil H., Tarning, Joel, Lindegardh, Niklas Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine.. Ali S, Najmi MH, Tarning J, Lindegardh N. Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine. Malar J. 2010 Oct 11;9:275.. doi:10.1186/1475-2875-9-275. Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/781
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Title
Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine.
Corresponding Author(s)
Abstract
BACKGROUND: Artemether-lumefantrine is one of the most widely used anti-malarial
drug combinations in the world with excellent tolerability and cure rates in
adult and paediatric patients with uncomplicated falciparum malaria. The aim of
this study was to evaluate the pharmacokinetics of artemether and its active
metabolite, dihydroartemisinin, in healthy Pakistani volunteers.
METHODS: Twelve healthy male Pakistani subjects, aged 20 to 50, were recruited
into the study. A fixed oral combination of artemether-lumefantrine (80-480 mg)
was given as a single oral dose. Frequent blood samples were collected and
artemether and dihydroartemisinin were quantified in human plasma using
solid-phase extraction and liquid chromatography coupled with tandem mass
spectrometry. Drug concentration-time data were evaluated with non-compartmental
analysis.
RESULTS: Observed maximum concentrations (mean ± SD) of artemether and
dihydroartemisinin were 184 ± 100 ng/mL and 126 ± 46 ng/mL, respectively. These
concentrations were reached at 1.56 ± 0.68 hr and 1.69 ± 0.59 hr, respectively,
after drug intake. The terminal elimination half-life of artemether and
dihydroartemisinin were 2.00 ± 0.71 hr and 1.80 ± 0.31 hr, respectively. Apparent
volume of distribution and oral clearance for artemether were estimated to 666 ±
220 L and 257 ± 140 L/hr. The same parameters were estimated to 702 ± 220 L and
269 ± 57 L/hr for dihydroartemisinin.
CONCLUSIONS: The overall pharmacokinetic properties of artemether and
dihydroartemisinin in healthy Pakistani subjects are comparable to healthy
subjects and patients from other populations.