Memantine hydrochloride is a low to moderate affinity, noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist which binds to NMDA receptor-operated cation channels. Memantine also blocks the 5-hydroxytryptamine-3 receptor (at a potency similar to the NMDA receptor) and nicotinic acetylcholine receptors (at one-sixth to one-tenth the potency). However, memantine has low to negligible affinity for gamma-aminobutyric acid, benzodiazepine, dopamine, adrenergic, histamine, and glycine receptors and for voltage-dependent calcium, sodium, or potassium channels.
藥動學
Bioavailability: approximately 100%; plasma protein binding: 45%; Excretion: 48-50% excreted unchanged in the urine; Elimination Half-life: 60-80 hrs
禁忌症
Hypersensitivity to the active substance or to any of the excipients.
Initial, 5 mg orally once daily; increase dose at minimum 1 week intervals in 5 mg increments to 10 mg/day (5 mg twice daily), 15 mg/day (5 mg and 10 mg in separate doses), and 20 mg/day (10 mg twice daily); target daily dose is 20 mg/day.
小兒調整劑量
腎功能調整劑量
(CrCl of 30 to 80 mL/min): No dosage adjustment necessary; (CrCl, 5 to 29 mL/min): Immediate-release, reduce dosage to 5 mg PO BID; extended-release, reduce dosage to 14 mg PO QD
肝功能調整劑量
Hepatic impairment, severe: Administer with caution