Comparative Pharmacology
Head-to-head clinical analysis: ABACAVIR LAMIVUDINE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ABACAVIR LAMIVUDINE versus EMTRIVA.
ABACAVIR; LAMIVUDINE vs EMTRIVA
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.
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) orally once daily with or without food. Can be used in combination with other antiretrovirals.
Emtricitabine 200 mg orally once daily.
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).
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)
Abacavir: 83% renal (1.2% unchanged, rest as metabolites), 16% fecal. Lamivudine: ~70% renal (mostly unchanged via tubular secretion), ~5% fecal.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI