Galantamine: Dose, Frequency, Indications, Interactions & more

Dosage and Frequency:

  • The typical starting dose of galantamine for treating Alzheimer’s disease is 4 mg twice daily.
  • After a minimum of 4 weeks, the dose may be increased to 8 mg twice daily based on tolerability.
  • Further dose escalation to 12 mg twice daily and then to a maximum of 16 to 24 mg per day, divided into two doses, can occur at intervals of at least 4 weeks.

Route of Administration (ROA):

  • Galantamine is administered orally as tablets, extended-release capsules, or oral solution.
  • It is recommended to be taken with food to reduce gastrointestinal side effects.

Mechanism of Action (MOA):

  • Galantamine is a reversible and competitive inhibitor of acetylcholinesterase, which increases the concentration of acetylcholine in the brain by slowing its breakdown.
  • It also allosterically modulates nicotinic acetylcholine receptors, which may further enhance cholinergic neurotransmission.

Pharmacokinetics (PK):

  • Galantamine is well absorbed after oral administration, with peak plasma concentrations reached within 1 hour.
  • It undergoes extensive hepatic metabolism primarily via the CYP2D6 and CYP3A4 pathways.
  • The elimination half-life is approximately 7 hours.

Pharmacodynamics (PD):

  • Galantamine enhances cholinergic function by inhibiting the breakdown of acetylcholine, which can improve cognitive function in Alzheimer’s disease.
  • It has been shown to improve cognitive performance and activities of daily living in patients with mild to moderate Alzheimer’s disease.

Pathophysiology:

  • Alzheimer’s disease is characterized by the accumulation of beta-amyloid plaques and neurofibrillary tangles in the brain, leading to progressive cognitive decline.
  • Cholinergic dysfunction is a hallmark feature of Alzheimer’s disease, contributing to cognitive impairment.

Indications:

  • Galantamine is indicated for the treatment of mild to moderate Alzheimer’s disease.
  • It is not recommended for use in patients with severe Alzheimer’s disease or in those with other types of dementia.

Contraindications:

  • Galantamine is contraindicated in patients with known hypersensitivity to the drug or any component of the formulation.

Drug Interactions:

  • Galantamine may interact with other drugs that inhibit or induce CYP2D6 or CYP3A4, potentially affecting its metabolism and efficacy.
  • Concurrent use of other cholinesterase inhibitors or anticholinergic medications may increase the risk of adverse effects.

Precautions:

  • Galantamine should be used with caution in patients with a history of asthma or obstructive pulmonary disease due to its cholinergic effects.
  • It should also be used cautiously in patients with bradycardia, sick sinus syndrome, or conduction abnormalities.
  • Galantamine may exacerbate or induce extrapyramidal symptoms in patients with Parkinson’s disease. Regular monitoring for signs of bradycardia, syncope, and other adverse effects is recommended.