Comparative Pharmacology
Head-to-head clinical analysis: EMTRICITABINE versus TENOFOVIR LAMIVUDINE EFAVIRENZ.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRICITABINE versus TENOFOVIR LAMIVUDINE EFAVIRENZ.
EMTRICITABINE vs Tenofovir-Lamivudine-Efavirenz
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.
Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor that inhibits HIV-1 reverse transcriptase by competing with the natural substrate deoxyadenosine 5'-triphosphate and by incorporation into DNA causing chain termination. Lamivudine is a nucleoside reverse transcriptase inhibitor that inhibits HIV-1 reverse transcriptase via incorporation into viral DNA. Efavirenz is a non-nucleoside reverse transcriptase inhibitor that binds reversibly to HIV-1 reverse transcriptase at a non-substrate binding site, causing conformational change and enzyme inhibition.
200 mg orally once daily, typically in combination with other antiretroviral agents.
One tablet (300 mg tenofovir disoproxil fumarate, 300 mg lamivudine, 600 mg efavirenz) orally once daily on an empty stomach, preferably at bedtime.
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).
Tenofovir: 17 hours (prolonged in renal impairment); Lamivudine: 5-7 hours (intracellular triphosphate 17-19 hours); Efavirenz: 52-76 hours (single dose), 40-55 hours (multiple doses).
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).
Tenofovir: 70-80% renal (glomerular filtration and tubular secretion); Lamivudine: 70% renal (glomerular filtration and tubular secretion); Efavirenz: 14-34% renal, 16-61% fecal (as unchanged drug and metabolites).
Category C
Category A/B
Antiretroviral, NRTI
NRTI
"The risk or severity of adverse effects can be increased when Valganciclovir is combined with Emtricitabine."