A comparison of the steady-state pharmacokinetics and safety of abacavir, lamivudine, and zidovudine taken as a triple combination tablet and as abacavir plus a lamivudine-zidovudine double combination tablet by HIV-1-infected adults

• Published in: Pharmacotherapy Vol. 21; no. 4; p. 424
• Main Authors: Crémieux, A C, Katlama, C, Gillotin, C, Demarles, D, Yuen, G J, Raffi, F
• Format: Journal Article
• Language: English
• Published: United States 01.04.2001
• Subjects: Adult; Area Under Curve; Cross-Over Studies; Dideoxynucleosides - administration & dosage; Dideoxynucleosides - blood; Dideoxynucleosides - pharmacokinetics; Drug Combinations; Drug Therapy, Combination; Half-Life; HIV Infections - blood; HIV Infections - drug therapy; HIV Infections - metabolism; HIV-1; Humans; Lamivudine - administration & dosage; Lamivudine - blood; Lamivudine - pharmacology; Male; Metabolic Clearance Rate; Reverse Transcriptase Inhibitors - administration & dosage; Reverse Transcriptase Inhibitors - blood; Reverse Transcriptase Inhibitors - pharmacokinetics; Tablets; Zidovudine - administration & dosage; Zidovudine - blood; Zidovudine - pharmacokinetics
• ISSN: 0277-0008
• DOI: 10.1592/phco.21.5.424.34497

To investigate the steady-state pharmacokinetics of a triple combination tablet containing abacavir (ABC) 300 mg, lamivudine (3TC) 150 mg, and zidovudine (ZDV) 300 mg taken twice/day, and those of ABC 300 mg twice/day plus a double combination tablet containing 3TC 150 mg and ZDV 300 mg twice/day (ABC-COM). Open-label, crossover study. Two hospital-based clinical research units. Twelve men infected with human immunodeficiency virus-1. Steady-state pharmacokinetics of ABC, 3TC, and ZDV were assessed after dosing with ABC-COM and the triple combination tablet. Steady-state pharmacokinetics of ABC, 3TC, and ZDV were similar for the triple combination tablet versus ABC-COM for the following: geometric mean (GM) area under the serum concentration-time curve, ABC 6.08 versus 5.87, 3TC 5.51 versus 5.53, and ZDV 1.38 versus 1.46 microg x hr/ml; GM maximum serum concentration (Cmax-ss), ABC 3.09 versus 3.19, 3TC 1.26 versus 1.40, and ZDV 1.19 versus 1.15 microg/ml; median time to Cmax-ss, ABC 0.75 versus 0.75, 3TC 1.50 versus 1.24, and ZDV 0.75 versus 0.75 hours; and GM oral clearance, ABC 51 versus 49, 3TC 27 versus 27, and ZDV 217 versus 206 L/hour. The GM half-lives of ABC and ZDV were similar for both treatments, 1.69 versus 1.58 and 2.30 versus 2.08 hours, respectively. Steady-state pharmacokinetics of ABC, 3TC, and ZDV were similar in patients who took them as ABC-COM or as a triple combination tablet.