Comparative Pharmacology
Head-to-head clinical analysis: ABACAVIR DOLUTEGRAVIR AND LAMIVUDINE versus EMTRICITABINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ABACAVIR DOLUTEGRAVIR AND LAMIVUDINE versus EMTRICITABINE.
ABACAVIR, DOLUTEGRAVIR AND LAMIVUDINE vs EMTRICITABINE
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.
Nucleoside reverse transcriptase inhibitor; phosphorylated to emtricitabine triphosphate which competes with endogenous deoxycytidine triphosphate and incorporates into viral DNA causing chain termination.
One tablet (600 mg abacavir / 50 mg dolutegravir / 300 mg lamivudine) taken orally once daily.
200 mg orally once daily, typically 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).
Terminal elimination half-life is approximately 10 hours (range 8–12 hours) in adults with normal renal function; prolonged to >20 hours in severe renal impairment (CrCl <30 mL/min).
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: approximately 86% of the dose is excreted unchanged in urine via glomerular filtration and active tubular secretion. Biliary/fecal: minimal (<14% as unchanged drug and metabolites in feces).
Category A/B
Category C
NRTI
Antiretroviral, NRTI