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.

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.

Inhibition of plasma cholinesterase is observed for up to 10 hours. Absorption- time to peak concentration, approximately 1 hr; Bioavailability: about 36%; Effect of food: delays Tmax by 90 min, lowers Cmax by approximately 30% and increases AUC by approximately 30%. Distribution- Vd: 1.8 L/kg to 2.7 L/kg; Protein binding: 40%. Metabolism- Hepatic cholinesterase-mediated hydrolysis extensive; CYP450 minimally involved in metabolism. Excretion- Fecal: 0.4%; Renal: 97%; Dialyzable: no (hemodialysis), no (peritoneal dialysis). Elimination Half Life: about 1.5 hr.

Hypersensitivity to rivastigmine or carbamate derivatives

B [FDA.AUS]

Infant risk can not be ruled out.

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.

Adults: Initially 1.5mg PO BID then titrated to 6-12mg daily; do not exceed 12 mg/day