Comparative Pharmacology
Head-to-head clinical analysis: ABACAVIR SULFATE AND LAMIVUDINE versus EMTRICITABINE.
Head-to-head clinical analysis: ABACAVIR SULFATE AND LAMIVUDINE versus EMTRICITABINE.
ABACAVIR SULFATE AND LAMIVUDINE vs EMTRICITABINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Abacavir is a carbocyclic synthetic nucleoside analog of guanosine; it is phosphorylated intracellularly to carbovir triphosphate, which inhibits HIV-1 reverse transcriptase by competing with the natural substrate dGTP and by incorporating into viral DNA, causing chain termination. Lamivudine is a synthetic nucleoside analogue of cytidine; it is phosphorylated intracellularly to lamivudine triphosphate, which inhibits HIV-1 reverse transcriptase via competitive inhibition and 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/300 mg lamivudine) once daily orally, or with food, in combination with other antiretroviral agents.
200 mg orally once daily, typically in combination with other antiretroviral agents.
None Documented
None Documented
Clinical Note
moderateEmtricitabine + Ribavirin
"Emtricitabine may increase the hepatotoxic activities of Ribavirin."
Clinical Note
moderateLamivudine + Emtricitabine
"The risk or severity of adverse effects can be increased when Lamivudine is combined with Emtricitabine."
Clinical Note
moderateGanciclovir + Emtricitabine
"The risk or severity of adverse effects can be increased when Ganciclovir is combined with Emtricitabine."
Clinical Note
moderateValganciclovir + Emtricitabine
Abacavir: ~1.5 h; Lamivudine: ~5-7 h (adults), prolongation in renal impairment.
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).
Renal: abacavir ~83% as metabolites (<2% unchanged), lamivudine ~70% unchanged; biliary/fecal: minimal.
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
"The risk or severity of adverse effects can be increased when Valganciclovir is combined with Emtricitabine."