The pharmacokinetics of lamivudine in patients with impaired hepatic function

Abstract

Objective: This study was designed to evaluate the effect of hepatic impairment on the pharmacokinetics of lamivudine.

Methods: Sixteen patients not infected with hepatitis B virus or human immunodeficiency virus who had hepatic impairment due to liver cirrhosis were assigned to moderately or severely impaired groups by clinical signs/symptoms, ¹⁴C-aminopyrine metabolic activity and caffeine clearance and compared with eight healthy controls. Following a 300-mg dose of lamivudine, blood and urine samples were taken for drug assay.

Results: Lamivudine was well tolerated in patients with hepatic impairment. There were no statistical differences in overall lamivudine exposure (in terms of AUC or C_max) or other major pharmacokinetic parameters i.e. CL_R, t_max and t_1/2, between healthy control subjects and patients with moderate or severe hepatic impairment.

Conclusions: Hepatic impairment does not warrant dose modification of lamivudine based on this single-dose pharmacokinetic study.