Prolongation of the half-life to 1.3 hours in patients with moderate hepatic impairment and 2.4 hours in severely impaired patients. Initial distribution half-life is 4 to 11 minutes and the terminal half-life is 40 to 80 minutes. Elimination of radiolabeled drug is essentially complete within 72 hours, with 90% to 95% of the radioactivity appearing in urine and 5% to 10% in the feces.
Route of eliminationįlumazenil is completely (99%) metabolized.
Diazepam antidote flumazenil free#
The major metabolites of flumazenil identified in urine are the de-ethylated free acid and its glucuronide conjugate. Flumazenil is completely (99%) metabolized. Protein binding is reduced in patients with hepatic cirrhosis. Protein binding is approximately 50%, mostly (66%) to albumin.
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