Comparative Pharmacology
Head-to-head clinical analysis: ABACAVIR DOLUTEGRAVIR AND LAMIVUDINE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ABACAVIR DOLUTEGRAVIR AND LAMIVUDINE versus EMTRIVA.
ABACAVIR, DOLUTEGRAVIR AND LAMIVUDINE vs EMTRIVA
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; emtricitabine is phosphorylated to emtricitabine 5'-triphosphate which competes with deoxycytidine 5'-triphosphate for incorporation into viral DNA, resulting in chain termination.
One tablet (600 mg abacavir / 50 mg dolutegravir / 300 mg lamivudine) taken orally once daily.
Emtricitabine 200 mg orally once daily.
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 ~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 (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 excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI