Pharmacology · Cholinesterase inhibitors
Galantamine !
A reversible cholinesterase inhibitor for mild to moderate Alzheimer dementia, with side effects like those of donepezil.
Updated 2026-11-01
The figure shows (-)-galantamine bound at the bottom of the gorge of human acetylcholinesterase, next to the catalytic site.
Mechanism of action
Galantamine is a reversible, competitive inhibitor of acetylcholinesterase that enters the brain. By slowing the breakdown of acetylcholine released by the surviving cholinergic neurons, it can improve memory and daily function for a time in Alzheimer disease.
- Enters the brain
- Competes with acetylcholine at the enzyme's active site
- Acetylcholine lasts longer at synapses
- Cognitive symptoms improve modestly
Pharmacokinetics
- Metabolism
- In the liver by CYP2D6 and CYP3A4; inhibitors of these enzymes raise its levels modestly
- Elimination
- Several metabolic routes plus the kidney, which removes part of it unchanged
- Half-life
- Terminal half-life about 7 hours
Indications
- Mild to moderate dementia of the Alzheimer type Alzheimer disease →
Adverse effects
Common
- Nausea, vomiting, diarrhoea and loss of appetite
- Weight loss
- Dizziness and headache
Contraindications
- Hypersensitivity to galantamine or its excipients
- Severe liver impairment (use not recommended)
Key interactions
- CYP2D6 inhibitors (fluoxetine, paroxetine, quinidine)
- Slower clearance and higher galantamine levels
- Anticholinergic drugs
- Opposite effects
- Succinylcholine
- Exaggerated muscle relaxation in anaesthesia
What is monitored
- Heart rate and fainting
- Weight and hydration
- Skin: any rash
- Breathing in people with severe asthma or COPD
Administration and safety
- Taken with meals, with good fluid intake
- Doses are increased gradually; after a break of more than three days, treatment restarts at the lowest dose
Nursing care
- Teach caregivers to stop and report at the first skin rash
- Check pulse and ask about fainting
- Encourage fluids to prevent dehydration
Pregnancy and breastfeeding
No adequate data in pregnancy; it is used mainly in older adults.
Test yourself
Think of the answer, then tap the question to see it.
Which serious skin reactions are listed for galantamine?
Stevens-Johnson syndrome and acute generalized exanthematous pustulosis; the drug is stopped at the first rash unless clearly unrelated.
Which liver enzymes metabolize galantamine?
CYP2D6 and CYP3A4.
Is galantamine a reversible or a carbamylating inhibitor?
Reversible and competitive, like donepezil; rivastigmine is the carbamylating one.
Related drugs
Related conditions
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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - GALANTAMINE tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); Galantamine: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); RCSB PDB - 4EY6: Crystal Structure of Recombinant Human Acetylcholinesterase in Complex with (-)-galantamine (RCSB Protein Data Bank, 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 21 (McGraw Hill, 2023).
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Representative model, for educational purposes only.