Trimethoprim/sulfamethoxazole does not affect the steady-state disposition of indinavir.
This study evaluates the safety and potential pharmacokinetic interaction between indinavir and trimethoprim/sulfamethoxazole (TMP/SMZ). In a randomized, three-period crossover fashion, 12 healthy adults received 1 week of indinavir sulfate 400 mg orally every 6 hours with placebo, TMP 160 mg/SMZ 800 mg orally every 12 hours with placebo, and indinavir sulfate with TMP/SMZ. Plasma indinavir, SMZ, and TMP concentrations were determined after the last dose of each treatment period. Concomitant administration resulted in a 17% decrease in geometric mean trough plasma indinavir concentrations (p = 0.032), an 18% increase in geometric mean AUC0-12 h and Cmax TMP values (p = 0.031 and 0.030, respectively), and a 5% increase in geometric mean AUC0-12 h SMZ values (p = 0.039). None of these effects was considered clinically significant. The combination of indinavir sulfate and TMP/SMZ is generally well tolerated, with no clinically significant pharmacokinetic interaction being noted.
Sturgill
M G
MG
College of Pharmacy, Rutgers, State University of New Jersey, Piscataway 08854-8020, USA.
Seibold
J R
JR
Boruchoff
S E
SE
Yeh
K C
KC
Haddix
H
H
Deutsch
P
P
D015746:Abdominal Pain / Q000139:chemically induced; D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000890:Anti-Infective Agents / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001663:Bilirubin / Q000097:blood; D018592:Cross-Over Studies; D003967:Diarrhea / Q000139:chemically induced; D004347:Drug Interactions; D005260:Female; D017320:HIV Protease Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics*; D006261:Headache / Q000139:chemically induced; D006801:Humans; D019469:Indinavir / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008875:Middle Aged; D015662:Trimethoprim, Sulfamethoxazole Drug Combination / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*
D000890:Anti-Infective Agents; D017320:HIV Protease Inhibitors; D019469:Indinavir; D015662:Trimethoprim, Sulfamethoxazole Drug Combination; D001663:Bilirubin