Comparative Pharmacology
Head-to-head clinical analysis: ABACAVIR SULFATE AND LAMIVUDINE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ABACAVIR SULFATE AND LAMIVUDINE versus EMTRIVA.
ABACAVIR SULFATE AND LAMIVUDINE vs EMTRIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Abacavir is a carbocyclic synthetic nucleoside analog of guanosine; it is phosphorylated intracellularly to carbovir triphosphate, which inhibits HIV-1 reverse transcriptase by competing with the natural substrate dGTP and by incorporating into viral DNA, causing chain termination. Lamivudine is a synthetic nucleoside analogue of cytidine; it is phosphorylated intracellularly to lamivudine triphosphate, which inhibits HIV-1 reverse transcriptase via competitive inhibition and 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 (600 mg abacavir/300 mg lamivudine) once daily orally, or with food, in combination with other antiretroviral agents.
Emtricitabine 200 mg orally once daily.
None Documented
None Documented
Abacavir: ~1.5 h; Lamivudine: ~5-7 h (adults), prolongation in renal impairment.
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% as metabolites (<2% unchanged), lamivudine ~70% unchanged; biliary/fecal: minimal.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI