Comparative Pharmacology
Head-to-head clinical analysis: EMTRIVA versus LAMIVUDINE AND ZIDOVUDINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRIVA versus LAMIVUDINE AND ZIDOVUDINE.
EMTRIVA vs LAMIVUDINE AND ZIDOVUDINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Lamivudine is a nucleoside reverse transcriptase inhibitor (NRTI) that inhibits HIV reverse transcriptase via DNA chain termination after intracellular phosphorylation to lamivudine triphosphate. Zidovudine is also an NRTI that inhibits HIV reverse transcriptase after phosphorylation to zidovudine triphosphate, causing chain termination. Both drugs act synergistically.
Emtricitabine 200 mg orally once daily.
One tablet (lamivudine 150 mg / zidovudine 300 mg) orally twice daily.
None Documented
None Documented
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)
Lamivudine: 5-7 hours (mean 5.5 h); Zidovudine: 0.5-3 hours (mean ~1 h). In renal impairment, half-life of both prolonged; terminal phase reflects slow elimination from intracellular active triphosphates.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Lamivudine: ~70% unchanged in urine via active tubular secretion; Zidovudine: ~75% as metabolites (primarily 5'-glucuronide, G-ZDV) and ~15% unchanged in urine via glomerular filtration and tubular secretion.
Category C
Category A/B
Antiretroviral, NRTI
NRTI