Absorption Readily absorbed from GI tract. C max for oseltamivir is 65.2 ng/mL. C max for metabolite is 348 ng/mL. AUC (0-12h) for oseltamivir is 112 ng•h/mL. AUC (0-12h) for metabolite is 2,719 ng•h/mL.
Distribution At least 75% of the dose reaches systemic circulation as oseltamivir carboxylate (bioavailability). The Vd is 23 to 26 L (metabolite); 3% is protein bound (metabolite); 42% is protein bound (parent drug).
Metabolism Converted to active oseltamivir carboxylate by esterases located predominantly in the liver.
Elimination The t ½ is 6 to 10 h for the metabolite. The t ½ for the parent drug is 1 to 3 h. More than 90% of oseltamivir is metabolized to oseltamivir carboxylate, which is entirely (more than 99%) eliminated by renal excretion. Less than 20% of the oral dose is eliminated through feces.
Special Populations Children Children 12 yr of age and younger clear the prodrug and active metabolite faster, resulting in a lower exposure for a given mg/kg dose.
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