Comparative Pharmacology
Head-to-head clinical analysis: EMTRIVA versus LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE NEVIRAPINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRIVA versus LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE NEVIRAPINE.
EMTRIVA vs LAMIVUDINE; TENOFOVIR DISOPROXIL FUMARATE; NEVIRAPINE
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 inhibits HIV-1 reverse transcriptase via DNA chain termination after intracellular phosphorylation to lamivudine triphosphate. Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor (NtRTI) that, after hydrolysis and phosphorylation, inhibits HIV-1 reverse transcriptase by competing with deoxyadenosine 5'-triphosphate and causing DNA chain termination. Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that directly binds to and inhibits HIV-1 reverse transcriptase, causing a conformational change and reducing enzyme activity.
Emtricitabine 200 mg orally once daily.
One tablet (300 mg lamivudine, 300 mg tenofovir disoproxil fumarate, 400 mg nevirapine) orally once daily. Nevirapine requires a 14-day lead-in dose of 200 mg once daily when initiating therapy.
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 in adults (extended to 20-30 hours in renal impairment). Tenofovir: 17-18 hours in adults (prolonged in renal impairment). Nevirapine: ~45 hours (single dose) to 25-30 hours (multiple doses due to autoinduction).
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Lamivudine: 70% renal (glomerular filtration and tubular secretion) as unchanged drug. Tenofovir: 70-80% renal (glomerular filtration and tubular secretion) as unchanged drug. Nevirapine: ~81% renal (metabolites, <5% unchanged), ~10% fecal.
Category C
Category A/B
Antiretroviral, NRTI
NRTI