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Central Acetylcholinesterase Inhibitor
Aka: Central Acetylcholinesterase Inhibitor, Acetylcholinesterase Inhibitor, Cholinesterase Inhibitor, Anticholinesterase
- See Also
- Dementia
- Dementia Management
- Memantine (Namenda, an NMDA Receptor Blocker)
- Preparations
- Aricept (Donepezil)
- Rivastigmine (Exelon)
- Galantamine (Reminyl)
- Mechanism
- Decreased cerebral Cholinergic activity in Alzheimer Disease, Lewy Body Dementia, Vascular Dementia
- Cholinergic inhibitors reversibly bind cholinesterase at Synapse between CNS Neurons
- Results in decreased acetylcholine degradation, and hence increased Cholinergic activity
- Efficacy
- Minimal clinical benefit, despite Statistically Significant improvement in cognitive function in trials
- Improve neuropsychiatric scores 7 points
- Seven point improvement equals ~1 year of decline
- Benefits may persist for 1-2 years
- Rogers (1998) Arch Intern Med 158:1021-31 [PubMed]
- Meta-analysis shows marginal benefit to risk ratio
- Where NNT is Number Needed to Treat
- NNT for global improvement: 10
- NNT for cognitive improvement: 12
- NNT for significant side effects to stop med: 16
- Lanctot (2003) CMAJ 169:557-64 [PubMed]
- Adverse Effects
- No hepatotoxicity with newer agents (contrast with Tacrine, Cognex - the initial agent in class)
- Cardiovascular effects
- Atrioventricular Block
- Gastrointestinal effects
- Decreased appetite and Anorexia
- Diarrhea
- Nausea or Vomiting
- Weight loss
- Neurologic effects
- Dizziness
- Headache
- References
- Epperly (2017) Am Fam Physician 95(12): 771-8 [PubMed]