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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
Author(s) -
Crémieux AnneClaude,
Katlama Christine,
Gillotin Catherine,
Demarles Didier,
Yuen Geoffrey J.,
Raffi Francois
Publication year - 2001
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1592/phco.21.5.424.34497
Subject(s) - abacavir , pharmacokinetics , zidovudine , cmax , lamivudine , pharmacology , medicine , virology , human immunodeficiency virus (hiv) , virus , hepatitis b virus , viral disease
Study Objective. 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). Design. Open‐label, crossover study. Setting. Two hospital‐based clinical research units. Patients. Twelve men infected with human immunodeficiency virus‐1. Intervention. Steady‐state pharmacokinetics of ABC, 3TC, and ZDV were assessed after dosing with ABC‐COM and the triple combination tablet. Measurements and Main Results. 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 μg·hr/ml; GM maximum serum concentration (C max‐ss ), ABC 3.09 versus 3.19, 3TC 1.26 versus 1.40, and ZDV 1.19 versus 1.15 μg/ml; median time to C max‐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. Conclusion. Steady‐state pharmacokinetics of ABC, 3TC, and ZDV were similar in patients who took them as ABC‐COM or as a triple combination tablet.