Comparative Pharmacology
Head-to-head clinical analysis: EMTRICITABINE versus LAMIVUDINE AND ZIDOVUDINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRICITABINE versus LAMIVUDINE AND ZIDOVUDINE.
EMTRICITABINE vs LAMIVUDINE AND ZIDOVUDINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Nucleoside reverse transcriptase inhibitor; phosphorylated to emtricitabine triphosphate which competes with endogenous deoxycytidine triphosphate and incorporates into viral DNA causing 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.
200 mg orally once daily, typically in combination with other antiretroviral agents.
One tablet (lamivudine 150 mg / zidovudine 300 mg) orally twice daily.
None Documented
None Documented
Clinical Note
moderateEmtricitabine + Ribavirin
"Emtricitabine may increase the hepatotoxic activities of Ribavirin."
Clinical Note
moderateLamivudine + Emtricitabine
"The risk or severity of adverse effects can be increased when Lamivudine is combined with Emtricitabine."
Clinical Note
moderateGanciclovir + Emtricitabine
"The risk or severity of adverse effects can be increased when Ganciclovir is combined with Emtricitabine."
Clinical Note
moderateValganciclovir + Emtricitabine
Terminal elimination half-life is approximately 10 hours (range 8–12 hours) in adults with normal renal function; prolonged to >20 hours in severe renal impairment (CrCl <30 mL/min).
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: approximately 86% of the dose is excreted unchanged in urine via glomerular filtration and active tubular secretion. Biliary/fecal: minimal (<14% as unchanged drug and metabolites in feces).
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
"The risk or severity of adverse effects can be increased when Valganciclovir is combined with Emtricitabine."