Comparative Pharmacology
Head-to-head clinical analysis: EMTRIVA versus TENOFOVIR LAMIVUDINE EFAVIRENZ.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRIVA versus TENOFOVIR LAMIVUDINE EFAVIRENZ.
EMTRIVA vs Tenofovir-Lamivudine-Efavirenz
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.
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.
Emtricitabine 200 mg orally once daily.
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
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)
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 excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
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