Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE versus EMTRIVA.
DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE vs EMTRIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Dolutegravir is an HIV integrase strand transfer inhibitor that blocks integration of HIV-1 DNA into host cell DNA. Abacavir and lamivudine are nucleoside reverse transcriptase inhibitors that inhibit HIV-1 reverse transcriptase via incorporation into viral DNA, 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 (dolutegravir 50 mg / abacavir 600 mg / lamivudine 300 mg) orally once daily.
Emtricitabine 200 mg orally once daily.
None Documented
None Documented
abacavir: 1.5 hr; lamivudine: 5-7 hr; dolutegravir: 14 hr. Twice-daily dosing for abacavir/lamivudine, once-daily for dolutegravir
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), 16% fecal; lamivudine: 70% renal (unchanged); dolutegravir: 64% fecal, 32% renal
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI