Global Research Journal of Pharmacy and Pharmacology

The pharmacokinetics of lumefantrine in adults on nevirapine-based antiretroviral therapy


Abstract

Accepted 23rd March, 2015

 

Pharmacokinetic parameters of lumefantrine in subjects treated for malaria and HIV-1 were obtained in two groups: antiretroviral therapy (ART) naive patients and those on nevirapine-based therapy. Both groups were on co-trimoxazole (TS) prophylaxis. Patients were enrolled prospectively. Both groups received artemether-lumefantrine (AL) combination twice daily for 3 days. Blood samples were collected just before the last dose and subsequently at 2, 4, 8, 24 and 120 h post dose. Concentrations of lumefantrine were determined by high performance liquid chromatography. Mean area under the plasma concentration-time curve (AUC0-∞ )  was 589 µg h/ml (552.4 - 627.4),  mean maximum concentration (Cmax) was 8.67 µg/ml (8.20 - 9.14), mean Day 7 concentration (Cday 7) was  0.99 µg/ml (0.94 - 1.04), mean elimination rate (K0) was  0.0214 µg/h  (0.0207- 0.0221), and mean half life was (T1/2) (h) 32.5 hrs (31.4 - 33.6) for subjects on nevirapine based ART and for  ART naive subjects were  375.2 (349.7- 400.7), 6.08 (5.57- 6.59), 0.64 (0.54 - 0.74), 0.0195 (0.0185 - 0.0205), 36.0 (34.1- 37.9) respectively. Time to maximum concentration (Tmax) was 4 h in both groups.  Nevirapine based ART significantly increases the exposure of lumefantrine but it is well tolerated.

 

Keywords: Pharmacokinetics, lumefantrine, nevirapine, HIV, Malaria.