Comparative Pharmacology
Head-to-head clinical analysis: EMTRICITABINE versus LAMIVUDINE AND TENOFOVIR DISOPROXIL FUMARATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRICITABINE versus LAMIVUDINE AND TENOFOVIR DISOPROXIL FUMARATE.
EMTRICITABINE vs LAMIVUDINE AND TENOFOVIR DISOPROXIL FUMARATE
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 is phosphorylated to its active metabolite, lamivudine triphosphate, which inhibits HIV-1 reverse transcriptase by competing with natural substrate and causing chain termination. Tenofovir disoproxil fumarate is a nucleotide analogue, tenofovir, which after diphosphorylation inhibits HIV-1 reverse transcriptase and hepatitis B virus polymerase via DNA chain termination.
200 mg orally once daily, typically in combination with other antiretroviral agents.
One tablet orally once daily, each tablet containing lamivudine 300 mg and tenofovir disoproxil fumarate (equivalent to tenofovir disoproxil 245 mg or tenofovir 300 mg).
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 intracellular triphosphate 10.5-15.5 hours. Tenofovir: 17 hours (pro-drug) intracellular active diphosphate >60 hours. Once daily dosing maintains therapeutic concentrations.
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).
Renal: Lamivudine ~70% unchanged; Tenofovir ~70-80% unchanged via glomerular filtration and active 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."