Comparative Pharmacology
Head-to-head clinical analysis: APTIVUS versus CRIXIVAN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APTIVUS versus CRIXIVAN.
APTIVUS vs CRIXIVAN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Tipranavir is a nonpeptidic HIV-1 protease inhibitor that binds to the active site of HIV-1 protease, thereby preventing the cleavage of viral polyprotein precursors into functional proteins, resulting in the production of immature, noninfectious viral particles.
Indinavir is a specific, potent, reversible inhibitor of HIV-1 protease. It binds to the active site of the viral protease, preventing the cleavage of viral polyprotein precursors into functional proteins, resulting in the formation of immature, non-infectious virions.
Oral: 500 mg twice daily with ritonavir 200 mg twice daily. Oral solution: 500 mg (1.25 mL) twice daily with ritonavir 200 mg twice daily. Must be taken with food.
800 mg orally every 8 hours on an empty stomach (1 hour before or 2 hours after meals) or with a light meal.
None Documented
None Documented
Terminal elimination half-life is 2.1 hours during multiple dosing with ritonavir (due to CYP3A inhibition), 5.5 hours when given alone.
Terminal elimination half-life is 1.8 to 2.5 hours in healthy adults; requires dosing every 8 hours.
Fecal (79.5% unchanged), renal (4.4% unchanged).
Primarily fecal (78-82%) with approximately 20% renal excretion of unchanged drug.
Category C
Category C
Antiretroviral
Antiretroviral