Pj. Devries et al., THE PHARMACOKINETICS OF A SINGLE-DOSE OF ARTEMISININ IN SUBJECTS WITHLIVER-CIRRHOSIS, TM & IH. Tropical medicine & international health, 2(10), 1997, pp. 957-962
Artemisinin is mainly eliminated by hepatic transformation. To investi
gate whether the clearance of artemisinin in patients with liver cirrh
osis is different from healthy volunteers, a pharmacokinetic study was
performed in male Vietnamese patients with Child B cirrhosis of the l
iver who received 500 mg of artemisinin orally. The results were compa
red to those found in a previous study in healthy subjects. The mean (
+/- SD) area under the concentration time curve was 2365 (+/- 1761)h n
g/ml; the mean (+/- SD) clearance, 382 (+/- 303)L/h. The elimination h
alf life was 4 (+/- 13)h extimated by log-linear regression and 2.4 +/
- 0.9h estimated by non-linear regression using a one-compartment firs
t order elimination model. The mean (+/- SD) absorption time was 1.55
(+/- 0.8)h. These results were not different from the results of healt
hy subjects and show that liver disease has no effect on the availabil
ity and clearance of oral artemisinin, indicating that artemisinin has
an intermediate hepatic extraction ratio and that there is no signifi
cant first pass effect.