Comparative Pharmacology
Head-to-head clinical analysis: ABACAVIR SULFATE LAMIVUDINE versus EMTRIVA.
Head-to-head clinical analysis: ABACAVIR SULFATE LAMIVUDINE versus EMTRIVA.
ABACAVIR SULFATE; LAMIVUDINE vs EMTRIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Abacavir is a nucleoside reverse transcriptase inhibitor (NRTI) that, after intracellular phosphorylation to carbovir triphosphate, competes with natural deoxyguanosine triphosphate for incorporation into viral DNA, causing chain termination. Lamivudine is an NRTI that, after phosphorylation to lamivudine triphosphate, inhibits HIV-1 reverse transcriptase via incorporation into viral DNA, resulting in chain termination.
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.
One tablet (abacavir 600 mg/lamivudine 300 mg) once daily, in combination with other antiretrovirals.
Emtricitabine 200 mg orally once daily.
None Documented
None Documented
Abacavir: 1.5 h; Lamivudine: 5-7 h (intracellular 10-15 h). Clinical context: Both support twice-daily dosing; lamivudine's longer intracellular half-life allows once-daily dosing.
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)
Renal: Abacavir ~83% (metabolites), Lamivudine ~70% (unchanged). Fecal: Abacavir ~16%, Lamivudine minimal. Biliary: negligible.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI