Comparative Pharmacology
Head-to-head clinical analysis: EMTRICITABINE versus EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRICITABINE versus EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE.
EMTRICITABINE vs EMTRICITABINE 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.
Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) that is phosphorylated to emtricitabine triphosphate, which inhibits HIV reverse transcriptase by competing with natural substrate and causing chain termination. Tenofovir disoproxil fumarate is a prodrug of tenofovir, an acyclic nucleoside phosphonate diester analog of adenosine monophosphate; it inhibits HIV reverse transcriptase and hepatitis B virus polymerase by incorporating into DNA and causing chain termination after conversion to tenofovir diphosphate.
200 mg orally once daily, typically in combination with other antiretroviral agents.
One tablet (200 mg emtricitabine/300 mg tenofovir disoproxil fumarate) orally once 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).
Emtricitabine: Terminal elimination half-life is approximately 10 hours (range 8-14 hours) in patients with normal renal function; prolonged to >200 hours in severe renal impairment. Tenofovir: Terminal elimination half-life of tenofovir is approximately 17 hours (range 12-18 hours) in patients with normal renal function; prolonged in renal impairment. Clinically, the long half-life supports once-daily dosing.
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).
Emtricitabine: 86% excreted unchanged in urine via glomerular filtration and active tubular secretion; 14% metabolized to 3'-sulfoxide diastereomers and glucuronide conjugates, with <1% excreted in feces. Tenofovir disoproxil fumarate: Tenofovir is eliminated by a combination of glomerular filtration and active tubular secretion, with 70-80% of the dose recovered as unchanged tenofovir in urine within 72 hours; renal excretion is the primary route.
Category C
Category A/B
Antiretroviral, NRTI
NRTI
"The risk or severity of adverse effects can be increased when Valganciclovir is combined with Emtricitabine."