Comparative Pharmacology
Head-to-head clinical analysis: ATAZANAVIR SULFATE RITONAVIR LAMIVUDINE ZIDOVUDINE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ATAZANAVIR SULFATE RITONAVIR LAMIVUDINE ZIDOVUDINE versus EMTRIVA.
ATAZANAVIR SULFATE;RITONAVIR;LAMIVUDINE;ZIDOVUDINE vs EMTRIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Atazanavir is an HIV-1 protease inhibitor that inhibits viral polyprotein cleavage, resulting in immature non-infectious virions. Ritonavir is a potent CYP3A4 inhibitor that boosts atazanavir exposure. Lamivudine and Zidovudine are nucleoside reverse transcriptase inhibitors (NRTIs) that chain-terminate viral DNA synthesis.
Nucleoside reverse transcriptase inhibitor; emtricitabine is phosphorylated to emtricitabine 5'-triphosphate which competes with deoxycytidine 5'-triphosphate for incorporation into viral DNA, resulting in chain termination.
One tablet (atazanavir sulfate 300 mg / ritonavir 100 mg / lamivudine 300 mg / zidovudine 300 mg) orally once daily with food.
Emtricitabine 200 mg orally once daily.
None Documented
None Documented
Atazanavir: ~7 h (boosted with ritonavir, effective half-life ~8-12 h for once-daily dosing). Ritonavir: 3-5 h. Lamivudine: 5-7 h. Zidovudine: 0.5-3 h.
Terminal elimination half-life ~10 hours (mean 10 h, range 7-14 h) in adults; prolonged in renal impairment (up to 90 h in severe impairment)
Atazanavir: 79% fecal (unchanged), 13% renal (7% unchanged). Ritonavir: 86% fecal, 11% renal. Lamivudine: 70% renal (unchanged). Zidovudine: 60-80% renal (metabolite AZT glucuronide), ~19% unchanged.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI