Comparative Pharmacology
Head-to-head clinical analysis: ABACAVIR DOLUTEGRAVIR AND LAMIVUDINE versus ABACAVIR SULFATE AND LAMIVUDINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ABACAVIR DOLUTEGRAVIR AND LAMIVUDINE versus ABACAVIR SULFATE AND LAMIVUDINE.
ABACAVIR, DOLUTEGRAVIR AND LAMIVUDINE vs ABACAVIR SULFATE AND LAMIVUDINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Abacavir is a guanosine analogue reverse transcriptase inhibitor that is phosphorylated to carbovir triphosphate, which competitively inhibits HIV reverse transcriptase and causes DNA chain termination. Dolutegravir is an integrase strand transfer inhibitor that blocks the strand transfer step of HIV DNA integration into the host genome. Lamivudine is a cytidine analogue reverse transcriptase inhibitor that is phosphorylated to lamivudine triphosphate, which competitively inhibits HIV reverse transcriptase and causes DNA 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 (600 mg abacavir / 50 mg dolutegravir / 300 mg lamivudine) taken orally once daily.
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: 1.5-2 h. Dolutegravir: 14 h (range 11-18 h) supporting once-daily dosing. Lamivudine: 13-19 h (intracellular triphosphate t1/2 16-19 h in cells).
Abacavir: ~1.5 h; Lamivudine: ~5-7 h (adults), prolongation in renal impairment.
Abacavir: 83% renal (metabolites via alcohol dehydrogenase and glucuronidation), 16% fecal. Dolutegravir: <1% renal, 64% fecal (as unchanged drug), 35% urinary (metabolites, mainly glucuronide). Lamivudine: 70% renal (unchanged via tubular secretion and glomerular filtration), 5-10% fecal.
Renal: abacavir ~83% as metabolites (<2% unchanged), lamivudine ~70% unchanged; biliary/fecal: minimal.
Category A/B
Category A/B
NRTI
NRTI