Comparative Pharmacology
Head-to-head clinical analysis: EMTRIVA versus LAMIVUDINE STAVUDINE.
Head-to-head clinical analysis: EMTRIVA versus LAMIVUDINE STAVUDINE.
EMTRIVA vs LAMIVUDINE; STAVUDINE
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. Stavudine is also an NRTI that inhibits HIV-1 reverse transcriptase after phosphorylation to stavudine triphosphate.
Emtricitabine 200 mg orally once daily.
Lamivudine 150 mg plus stavudine 30 mg orally twice daily. For patients weighing ≥60 kg, stavudine 40 mg twice 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 in adults; prolonged to 19-28 hours in severe renal impairment (CrCl <10 mL/min). Stavudine: 1.0-1.6 hours; prolonged to 7.4-8.2 hours in severe renal impairment.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Lamivudine: 70% renal excretion via glomerular filtration and active tubular secretion as unchanged drug; 5-10% fecal. Stavudine: 40% renal excretion via glomerular filtration and active tubular secretion; 34-39% unchanged in urine; fecal excretion minimal.
Category C
Category A/B
Antiretroviral, NRTI
NRTI