GALANTAMINE

brands

Class

• Neuroscience-based Nomenclature: acetylcholine multimodal; enzyme inhibitor; receptor PAM (ACh-MM)
• Cholinesterase inhibitor (acetylcholinesterase inhibitor); also an allosteric nicotinic cholinergic modulator; cognitive enhancer

GALANTAMINE commonly prescribed for

(Bold for FDA approved)

How GALANTAMINE works

• Reversibly and competitively inhibits centrally active acetylcholinesterase, making more acetylcholine available

• Increased availability of acetylcholine compensates in part for degenerating cholinergic neurons in neocortex that regulate memory

• Modulates nicotinic receptors, which enhances actions of acetylcholine

• Nicotinic modulation may also enhance the actions of other neurotransmitters by increasing the release of dopamine, norepinephrine, serotonin, GABA, and glutamate

• Does not inhibit butyrylcholinesterase

• May release growth factors or interfere with amyloid deposition

How long until GALANTAMINE works

• May take up to 6 weeks before any improvement in baseline memory or behavior is evident

• May take months before any stabilization in degenerative course is evident

Notable Side Effects

• Nausea, diarrhea, vomiting, appetite loss, increased gastric acid secretion, weight loss

• Headache, dizziness

• Fatigue, depression

Life Threatening Side Effects

• Rare seizures

• Rare syncope

weight gain

unusual

sedation

unusual

What to do about GALANTAMINE side effects

• Wait

• Wait

• Wait

• Use slower dose titration

• Consider lowering dose, switching to a different agent, or adding an appropriate augmenting agent

usual dosage range

• 16–24 mg/day

Dosage Forms

• Tablet 4 mg, 8 mg, 12 mg

• Extended-release capsule 8 mg, 16 mg, 24 mg

• Liquid 4 mg/mL – 100 mL bottle

long term use

• Drug may lose effectiveness in slowing degenerative course of Alzheimer disease after 6 months

• Can be effective in some patients for several years

habit forming

• No

Renal Impairment

• Should be used with caution

• Not recommended for use in patients with severe renal impairment

Hepatic Impairment

• Should be used with caution

• Reduction of clearance may increase with the degree of hepatic impairment

• Not recommended for use in patients with severe hepatic impairment

Cardiac Impairment

• Should be used with caution

• Syncopal episodes have been reported with the use of galantamine

Elderly

• Clearance is reduced in elderly patients

• Use of cholinesterase inhibitors may be associated with increased rates of syncope, bradycardia, pacemaker insertion, and hip fracture in older adults with dementia

Children and Adolescents

• Safety and efficacy have not been established

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Controlled studies have not been conducted in pregnant women

• Animal studies do not show adverse effects

• Not recommended for use in pregnant women or in women of childbearing potential

Breast Feeding

• Unknown if galantamine is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Recommended either to discontinue drug or bottle feed

• Galantamine is not recommended for use in nursing women