Makindo Medical Notes

⚠️ Excess acetylcholine can cause SLUDE syndrome (Salivation, Lacrimation, Urination, Defecation, Emesis). This reflects pathological overstimulation of the parasympathetic nervous system, such as in nerve gas exposure or overdose.

💊 About

• Always check the BNF or equivalent for prescribing advice.
• Acetylcholinesterase inhibitors are mainly used in dementia and neurological disorders.
• Similar mechanisms are seen in toxic exposures (e.g. organophosphates, nerve gases).

⚙️ Mode of Action

• Inhibit acetylcholinesterase, the enzyme responsible for breaking down acetylcholine (ACh).
• Increase both the level and duration of action of acetylcholine at synapses.
• Enhance cholinergic transmission, especially in the CNS and parasympathetic nervous system.

💊 Examples

• Donepezil (Aricept): tablets and oral dispersible tablets. Dosage: 5–10 mg daily.
• Galantamine (Reminyl XL): tablets, capsules, and liquid. Dosage: 8–24 mg once daily.
• Rivastigmine (Exelon): tablets and liquid (1.5–6 mg twice daily) or transdermal patches (4.6–9.5 mg once daily).

⚡ Clinical Side Effects

• Cholinergic overstimulation (muscarinic effects):
• Salivation, lacrimation, sweating.
• Urination, defecation, nausea, vomiting.
• Miosis (pupil constriction).
• Bradycardia, hypotension.
• Bronchospasm, increased bronchial secretions.
• These effects are mediated via muscarinic receptors.

📋 Indications / Dose

• Alzheimer’s disease (mild to moderate stages).
• Other dementias (e.g. Lewy body dementia, Parkinson’s disease dementia).

🔄 Interactions

• See BNF for full list.
• Potential interactions with anticholinergics (antagonistic effect).
• Risk of bradycardia with beta-blockers or digoxin.

⚠️ Cautions

• History of asthma, COPD, or bronchospasm.
• Peptic ulcer disease (↑ gastric acid secretion).
• Seizure disorders.
• Bradycardia or conduction abnormalities.

⛔ Contraindications

• Severe hepatic impairment (drug-specific).
• Uncontrolled cardiac conduction disorders (e.g. sick sinus syndrome, AV block).
• Known hypersensitivity to drug or excipients.

📚 References

• BNF – Acetylcholinesterase inhibitors
• NICE Dementia Guideline (NG97).
• UpToDate – “Cholinesterase inhibitors in dementia.”