Comparative Pharmacology
Head-to-head clinical analysis: ABACAVIR DOLUTEGRAVIR AND LAMIVUDINE versus ABACAVIR SULFATE LAMIVUDINE AND ZIDOVUDINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ABACAVIR DOLUTEGRAVIR AND LAMIVUDINE versus ABACAVIR SULFATE LAMIVUDINE AND ZIDOVUDINE.
ABACAVIR, DOLUTEGRAVIR AND LAMIVUDINE vs ABACAVIR SULFATE, LAMIVUDINE AND ZIDOVUDINE
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 guanosine analogue that is phosphorylated to carbovir triphosphate, which inhibits HIV-1 reverse transcriptase by competing with natural substrate dGTP and causing chain termination. Lamivudine is a dideoxy-nucleoside cytidine analogue that is phosphorylated to lamivudine triphosphate, which inhibits HIV-1 reverse transcriptase via incorporation into viral DNA and chain termination. Zidovudine is a thymidine analogue that is phosphorylated to zidovudine triphosphate, which inhibits HIV-1 reverse transcriptase by competing with dTTP and causing chain termination. All three drugs are nucleoside reverse transcriptase inhibitors (NRTIs).
One tablet (600 mg abacavir / 50 mg dolutegravir / 300 mg lamivudine) taken orally once daily.
One tablet (abacavir 600 mg/lamivudine 300 mg/zidovudine 300 mg) twice daily or as a single tablet once daily (abacavir 600 mg/lamivudine 300 mg/zidovudine 300 mg) depending on formulation.
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; zidovudine: 0.5-3 h. Terminal half-lives: abacavir ~1.5 h, lamivudine ~13-19 h intracellularly (active triphosphate), zidovudine ~1 h (plasma) but intracellular triphosphate ~3-4 h. Clinical context: Twice-daily dosing due to prolonged intracellular half-life of active metabolites.
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 and metabolites: abacavir (83% as metabolites, 1% unchanged), lamivudine (70% unchanged), zidovudine (72-74% as metabolites, 14-18% unchanged). Biliary/fecal elimination is minor (<10% for each component).
Category A/B
Category A/B
NRTI
NRTI