Rivastigmine
Brand: Exelon (US/EU) / Rivamer (IN) / Rivastigmine (BD)
Neurological
Cholinesterase inhibitor (AChE + BuChE; pseudo-irreversible)
Pharmacokinetics
| Half-life | 1.5 hours |
| Tmax | 1 h |
| Bioavailability | 40 % (approx) |
| Protein Binding | 40 % |
| Volume of Distribution | 1.8 L/kg (approx) |
| Clearance Route | renal |
| Active Metabolites | yes |
| Notes | Not significantly metabolized by CYP; extensive hydrolysis by esterases to inactive metabolite; patch reduces peak-related GI adverse effects. Patch max 13.3 mg/24 h (separate from oral dosing). |
⚠️ Safety & Warnings
Severity: Moderate
Adverse Effects:
Nausea, vomiting, diarrhea, anorexia/weight loss, dizziness, bradycardia, syncope, tremor; patch: application-site reactions
Contraindications:
Hypersensitivity to rivastigmine or other carbamate derivatives; history of allergic contact dermatitis with rivastigmine patch
Precautions:
Caution in sick sinus syndrome/AV block, bradyarrhythmia, peptic ulcer disease/GI bleeding risk, asthma/COPD; monitor weight; titrate slowly. If therapy interrupted for several days, restart at lowest dose to reduce GI effects.