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.
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).


METHODS
Open-label, crossover study.


METHODS
Two hospital-based clinical research units.


METHODS
Twelve men infected with human immunodeficiency virus-1.


METHODS
Steady-state pharmacokinetics of ABC, 3TC, and ZDV were assessed after dosing with ABC-COM and the triple combination tablet.


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 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.


CONCLUSIONS
Steady-state pharmacokinetics of ABC, 3TC, and ZDV were similar in patients who took them as ABC-COM or as a triple combination tablet.
Crémieux
A C
AC
Unité d'Investigation Clinique, H pital Bichat, Paris, France.
Katlama
C
C
Gillotin
C
C
Demarles
D
D
Yuen
G J
GJ
Raffi
F
F
D000328:Adult; D019540:Area Under Curve; D018592:Cross-Over Studies; D015224:Dideoxynucleosides / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D004338:Drug Combinations; D004359:Drug Therapy, Combination; D015658:HIV Infections / Q000097:blood / Q000188:drug therapy / Q000378:metabolism*; D015497:HIV-1; D006207:Half-Life; D006801:Humans; D019259:Lamivudine / Q000008:administration & dosage / Q000097:blood / Q000494:pharmacology*; D008297:Male; D008657:Metabolic Clearance Rate; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D013607:Tablets; D015215:Zidovudine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D000099227:Abacavir
D015224:Dideoxynucleosides; D004338:Drug Combinations; D019259:Lamivudine; D018894:Reverse Transcriptase Inhibitors; D013607:Tablets; D015215:Zidovudine; D000099227:Abacavir