Comparative Pharmacology
Head-to-head clinical analysis: EMTRIVA versus LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE.
Head-to-head clinical analysis: EMTRIVA versus LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE.
EMTRIVA vs LAMIVUDINE; 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); tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor (NtRTI). Both inhibit HIV-1 reverse transcriptase and hepatitis B virus polymerase, causing chain termination of viral DNA.
Emtricitabine 200 mg orally once daily.
One tablet (300 mg tenofovir disoproxil fumarate and 300 mg lamivudine) orally once daily.
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 (healthy), up to 13.1 hours (moderate renal impairment). Tenofovir: 17-25 hours (HIV), 32-49 hours (hepatitis B), prolonged in renal impairment.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Lamivudine: predominantly renal (~70% unchanged). Tenofovir: renal (~70-80% unchanged via glomerular filtration and active tubular secretion).
Category C
Category A/B
Antiretroviral, NRTI
NRTI