EXELON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EXELON (EXELON).
Exelon (rivastigmine) is a reversible, non-competitive acetylcholinesterase and butyrylcholinesterase inhibitor, increasing acetylcholine levels in the brain.
| Metabolism | Primarily metabolized via esterase-mediated hydrolysis (not CYP450 enzymes) to the decarbamylated metabolite; undergoes minimal hepatic metabolism. |
| Excretion | Renal (97%) with unchanged drug <1%; biliary/fecal as metabolites. |
| Half-life | Terminal half-life: ~1.5 hours; clinical context: tid dosing recommended due to rapid elimination. |
| Protein binding | 40% bound, primarily to albumin. |
| Volume of Distribution | Vd ~1.1 L/kg; indicates extensive tissue distribution. |
| Bioavailability | Oral: 36-48% (first-pass effect); transdermal: 100% (avoidance of hepatic first-pass). |
| Onset of Action | Oral: 1-1.5 hours; transdermal: 4-6 hours (steady state achieved in 2-3 days). |
| Duration of Action | 10-12 hours (oral); 24 hours (transdermal, continuous release). |
| Action Class | Cholinesterase inhibitors - Alzheimer's disease |
| Brand Substitutes | Rivasmine 3mg Capsule, Rivadem 3mg Capsule, Rivasun 3mg Capsule, Ritas 3 Capsule, Rivagold 3mg Capsule, Rivasmine 6mg Capsule, Rivasun 6mg Capsule, Rivamer 6mg Capsule |
Initial: 1.5 mg orally twice daily; after 2 weeks increase to 3 mg twice daily; then after 2 weeks increase to 4.5 mg twice daily; then after 2 weeks increase to 6 mg twice daily (maximum). For transdermal patch: initial 4.6 mg/24 hr applied once daily; after 4 weeks increase to 9.5 mg/24 hr; may increase to 13.3 mg/24 hr after additional 4 weeks.
| Dosage form | FILM, EXTENDED RELEASE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. For severe renal impairment (CrCl <30 mL/min), use with caution; maximum oral dose 3 mg twice daily. Transdermal patch: maximum 4.6 mg/24 hr. |
| Liver impairment | Mild to moderate hepatic impairment (Child-Pugh A or B): use with caution; maximum oral dose 3 mg twice daily; transdermal maximum 4.6 mg/24 hr. Severe hepatic impairment (Child-Pugh C): not recommended. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment based on age alone; consider renal function and comorbidities. For patients with low body weight (<50 kg) or significant comorbid conditions, use lower end of dosing range and titrate slowly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for EXELON (EXELON).
| Breastfeeding | Excretion in human milk unknown; due to potential for serious adverse reactions, discontinue nursing or drug. |
| Teratogenic Risk | Pregnancy Category B. No evidence of teratogenicity in animal studies; no adequate human studies. Use only if benefit outweighs risk. |
| Fetal Monitoring | Monitor for cholinergic effects (bradycardia, hypotension, nausea, vomiting) and weight loss in mother; fetal monitoring for growth and heart rate if used in third trimester. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to rivastigmine or any component of the formulation","History of application site reactions with rivastigmine patch"]
| Precautions | ["Gastrointestinal adverse reactions including nausea, vomiting, diarrhea, anorexia, and weight loss","Increased risk of gastrointestinal bleeding, especially in patients with NSAIDs","Bradycardia and heart block","Extrapyramidal symptoms worsening in Parkinson's disease dementia","Seizures","Genitourinary effects (urinary obstruction)","Severe skin reactions (e.g., Stevens-Johnson syndrome)"] |
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| Fertility Effects | No human data on fertility; animal studies showed no impairment at therapeutic doses. |