Comparative Pharmacology
Head-to-head clinical analysis: EMTRIVA versus LAMIVUDINE AND TENOFOVIR DISOPROXIL FUMARATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRIVA versus LAMIVUDINE AND TENOFOVIR DISOPROXIL FUMARATE.
EMTRIVA vs LAMIVUDINE AND TENOFOVIR DISOPROXIL FUMARATE
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 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.
Emtricitabine 200 mg orally once daily.
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
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 intracellular triphosphate 10.5-15.5 hours. Tenofovir: 17 hours (pro-drug) intracellular active diphosphate >60 hours. Once daily dosing maintains therapeutic concentrations.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Renal: Lamivudine ~70% unchanged; Tenofovir ~70-80% unchanged via glomerular filtration and active tubular secretion.
Category C
Category A/B
Antiretroviral, NRTI
NRTI