Description

Simple

A medication used to treat Alzheimer's Disease.

Clinical

A benzazepine derivative used to treat mild to moderate dementia associated with Alzheimer's Disease.

Overview

A benzazepine derived from norbelladine. It is found in galanthus and other amaryllidaceae. Galantamine is a cholinesterase inhibitor that has been used to reverse the muscular effects of gallamine triethiodide and tubocurarine, and has been studied as a treatment for Alzheimer's disease and other central nervous system disorders.

Pharmacology

Indication

For the treatment of mild to moderate dementia of the Alzheimer's type. Has also been investigated in patients with mild cognitive impairment who did not meet the diagnostic criteria for Alzheimer's disease.

Pharmacodynamic

Galantamine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. It is indicated for the treatment of mild to moderate dementia of the Alzheimer's type, but it is only a disease modifying agent that has little effect in altering the course of the underlying process of demen... Read more

Mechanism of action

Galantamine is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor. It is not structurally related to other acetylcholinesterase inhibitors. Galantamine's proposed mechanism of action involves the reversible inhibition of acetylcholinesterase, which prevents the hydr... Read more

Absorption

Information currently not available.

Protein binding

18%

Volume of distribution

175 L

Clearance

300 mL/min [After IV. or oral administration]

Half life

7 hours

Route of elimination

Galantamine is metabolized by hepatic cytochrome P450 enzymes, glucuronidated, and excreted unchanged in the urine.

Toxicity

LD50=75 mg/kg (rat)

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

  • Take with food.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Galantamine can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
4-Methoxyamphetamine
The metabolism of 4-Methoxyamphetamine can be decreased when combined with Galantamine.
5-methoxy-N,N-dimethyltryptamine
The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Galantamine.
Abacavir
Galantamine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The metabolism of Galantamine can be increased when combined with Abatacept.
Abexinostat
The risk or severity of QTc prolongation can be increased when Galantamine is combined with Abexinostat.
Abiraterone
The metabolism of Galantamine can be decreased when combined with Abiraterone.
Acarbose
Acarbose may decrease the excretion rate of Galantamine which could result in a higher serum level.
Acebutolol
The risk or severity of QTc prolongation can be increased when Galantamine is combined with Acebutolol.
Aceclofenac
Aceclofenac may decrease the excretion rate of Galantamine which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Galantamine which could result in a higher serum level.
Aceprometazine
The risk or severity of QTc prolongation can be increased when Galantamine is combined with Aceprometazine.
Acetaminophen
Acetaminophen may decrease the excretion rate of Galantamine which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Galantamine which could result in a lower serum level and potentially a reduction in efficacy.
Acetylcholine
The risk or severity of adverse effects can be increased when Galantamine is combined with Acetylcholine.
Acetyldigoxin
The risk or severity of QTc prolongation can be increased when Galantamine is combined with Acetyldigoxin.
Acetylsalicylic acid
Acetylsalicylic acid may decrease the excretion rate of Galantamine which could result in a higher serum level.
Aclidinium
The therapeutic efficacy of Aclidinium can be decreased when used in combination with Galantamine.
Acrivastine
Galantamine may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Galantamine which could result in a higher serum level.
6 References
  1. 1 . Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer's disease. Drugs. 2000 Nov;60(5):1095-122.PubMed: 11129124
  2. 2 . Greenblatt HM, Kryger G, Lewis T, Silman I, Sussman JL: Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution. FEBS Lett. 1999 Dec 17;463(3):321-6.PubMed: 10606746
  3. 3 . Woodruff-Pak DS, Vogel RW 3rd, Wenk GL: Galantamine: effect on nicotinic receptor binding, acetylcholinesterase inhibition, and learning. Proc Natl Acad Sci U S A. 2001 Feb 13;98(4):2089-94. Epub 2001 Feb 6.PubMed: 11172080
  4. 4 . Birks J: Cholinesterase inhibitors for Alzheimer's disease. Cochrane Database Syst Rev. 2006 Jan 25;(1):CD005593.PubMed: 16437532
  5. 5 . Lilienfeld S: Galantamine--a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer's disease. CNS Drug Rev. 2002 Summer;8(2):159-76.PubMed: 12177686
  6. 6 . Olin J, Schneider L: Galantamine for Alzheimer's disease. Cochrane Database Syst Rev. 2002;(3):CD001747.PubMed: 12137632