Comparative Pharmacology
Head-to-head clinical analysis: ABACAVIR LAMIVUDINE versus ABACAVIR SULFATE AND LAMIVUDINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ABACAVIR LAMIVUDINE versus ABACAVIR SULFATE AND LAMIVUDINE.
ABACAVIR; LAMIVUDINE vs ABACAVIR SULFATE AND LAMIVUDINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Abacavir is a carbocyclic synthetic nucleoside analogue (guanosine analogue) that is phosphorylated intracellularly to carbovir triphosphate, which competes with deoxyguanosine triphosphate for incorporation into viral DNA by HIV reverse transcriptase, leading to chain termination. Lamivudine is a synthetic nucleoside analogue (cytosine analogue) that is phosphorylated intracellularly to lamivudine triphosphate, which competes with deoxycytidine triphosphate for incorporation into viral DNA by HIV reverse transcriptase, causing chain termination.
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.
One tablet (abacavir 600 mg/lamivudine 300 mg) orally once daily with or without food. Can be used in combination with other antiretrovirals.
One tablet (600 mg abacavir/300 mg lamivudine) once daily orally, or with food, in combination with other antiretroviral agents.
None Documented
None Documented
Abacavir: 1.5 hr (single dose) to 2 hr (steady state), clinically short requiring twice-daily dosing. Lamivudine: 5-7 hr (adults), extended in renal impairment (up to 20 hr with CrCl <50 mL/min).
Abacavir: ~1.5 h; Lamivudine: ~5-7 h (adults), prolongation in renal impairment.
Abacavir: 83% renal (1.2% unchanged, rest as metabolites), 16% fecal. Lamivudine: ~70% renal (mostly unchanged via tubular secretion), ~5% fecal.
Renal: abacavir ~83% as metabolites (<2% unchanged), lamivudine ~70% unchanged; biliary/fecal: minimal.
Category A/B
Category A/B
NRTI
NRTI