Rivastigmine is a carbamate acetylcholinesterase inhibitor with regional selectivity for the hippocampus and cortex. It is indicated for the treatment of mild to moderate dementia of the Alzheimer's type.
藥理
Rivastigmine appears to have greater central than peripheral activity, which may result in fewer peripheral adverse events. Donepezil and rivastigmine were found to be equally effective in providing cognitive improvement in patients with mild to moderate Alzheimer's disease.
藥動學
Absorption- Tmax, Transdermal: 8 to 16 hours. Distribution- Protein binding: 40%; Vd: 1.8 to 2.7 L/kg. Metabolism- extensive via cholinesterases. Excretion- Fecal: less than 1%; Renal: greater than 90% (changed); Dialyzable: No (hemodialysis); No (peritoneal dialysis); Hemofiltration: No. Elimination Half Life: 3 hours
禁忌症
Hypersensitivity to rivastigmine or carbamate derivatives
懷孕分類
B [FDA.AUS]
哺乳分類
Infant risk can not be ruled out.
副作用
Use of rivastigmine is associated with significant gastrointestinal effects including nausea, vomiting, anorexia, and weight loss. Other frequently occurring adverse effects include fatigue, asthenia, dizziness, headache, diarrhea, dyspepsia, insomnia and confusion.
劑量和給藥方法
(Mild, moderate, severe) Initial, 4.6 mg/24 hours patch topically once daily; after a minimum of 4 weeks and good tolerability, may titrate dose to 9.5 mg/24 hours patch topically once daily. (Mild to moderate) Maintenance, 9.5 mg/24 hours patch topically once daily; after a minimum of 4 weeks and good tolerability, may titrate to MAX of 13.3 mg/24 hours patch topically once daily when no longer receiving therapeutic benefit at lower dose. (Severe) Maintenance, 13.3 mg/24 hours patch topically once daily after minimum 4 weeks and good tolerability at lower dose of 9.5 mg/24 hours.