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Pharmacology: Pharmacodynamics: Entecavir is intracellularly phosphorylated to guanosine triphosphate which competes with natural substrates to effectively inhibit hepatitis B viral polymerase and enzyme inhibition blocks reverse transcriptase activity thereby reducing viral DNA synthesis.
Pharmacokinetics: Absorption: Delayed with food; Cmax decreased 44-46% AUC decreased 18-20%.
Distribution: Extensive.
Protein binding: ~13%.
Metabolism: Minor hepatic glucoronide/sulfate conjugation.
Half-life elimination Terminal: ~5-6 days, accumulation ~24 hours.
Time to peak, plasma: 0.5-1.5 hours.
Excretion: Urine (60-73% as unchanged drug).
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