Comparative Pharmacology
Head-to-head clinical analysis: ABACAVIR DOLUTEGRAVIR AND LAMIVUDINE versus ABACAVIR SULFATE LAMIVUDINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ABACAVIR DOLUTEGRAVIR AND LAMIVUDINE versus ABACAVIR SULFATE LAMIVUDINE.
ABACAVIR, DOLUTEGRAVIR AND LAMIVUDINE vs ABACAVIR SULFATE; 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 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.
One tablet (600 mg abacavir / 50 mg dolutegravir / 300 mg lamivudine) taken orally once daily.
One tablet (abacavir 600 mg/lamivudine 300 mg) once daily, in combination with other antiretrovirals.
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 (intracellular 10-15 h). Clinical context: Both support twice-daily dosing; lamivudine's longer intracellular half-life allows once-daily dosing.
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% (metabolites), Lamivudine ~70% (unchanged). Fecal: Abacavir ~16%, Lamivudine minimal. Biliary: negligible.
Category A/B
Category A/B
NRTI
NRTI