Comparative Pharmacology
Head-to-head clinical analysis: EMTRIVA versus STAVUDINE LAMIVUDINE W NEVIRAPINE.
Head-to-head clinical analysis: EMTRIVA versus STAVUDINE LAMIVUDINE W NEVIRAPINE.
EMTRIVA vs STAVUDINE; LAMIVUDINE W/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.
Stavudine is a nucleoside reverse transcriptase inhibitor (NRTI) that inhibits HIV-1 reverse transcriptase by competing with the natural substrate thymidine triphosphate and by causing DNA chain termination after incorporation. Lamivudine is an NRTI that inhibits HIV-1 reverse transcriptase via similar mechanisms. Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds directly to reverse transcriptase and blocks RNA-dependent and DNA-dependent DNA polymerase activities.
Emtricitabine 200 mg orally once daily.
One tablet (stavudine 30 mg / lamivudine 150 mg / nevirapine 200 mg) orally 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)
Stavudine: 0.9–1.6 h (normal renal function), prolonged in renal impairment; lamivudine: 5–7 h (adults), 2–4 h (children); nevirapine: 25–30 h (terminal, after multiple doses), allowing once-daily dosing.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Stavudine: 50% excreted unchanged in urine via glomerular filtration and active tubular secretion; lamivudine: ~70% excreted unchanged in urine via active secretion; nevirapine: ~80% metabolized by liver, with <5% excreted unchanged in urine (metabolites eliminated renally and fecally).
Category C
Category A/B
Antiretroviral, NRTI
NRTI