galantamine (Rx)

>10%

Nausea (20-25%)

Diarrhea (11-15%)

Vomiting (11-15%)

1-10%

Abdominal pain

Anorexia

Muscle cramp

Fatigue

Dizziness

Headache

Weight loss

Depression

Insomnia

UTI

Somnolence

Anemia

Syncope

Bradycardia

Other Information

Complete atrioventricular block

Contraindications

Hypersensitivity

Cautions

Moderate hepatic or renal impairment: max 8 mg q12hr (conventional) or 16 mg qDay (ER)

Not recommended in severe hepatic or renal impairment

Dose-related increase in risk of syncope reported

Renamed Razadyne from Reminyl in the US to avoid confusion with Amaryl

Serious skin reactions (Stevens-Johnson syndrome and acute generalized exanthematous pustulosis) reported; inform patients and caregivers that therapy should be discontinued at first appearance of skin rash, unless rash is clearly not drug-related; do not resume treatment and consider alternative therapy if signs or symptoms suggest a serious skin reaction

As a cholinesterase inhibitor, therapy is likely to exaggerate neuromuscular blocking effects of succinylcholine-type and similar neuromuscular blocking agents during anesthesia

All patients should be considered at risk for adverse effects on cardiac conduction, including bradycardia and AV block, due to vagotonic effects on sinoatrial and atrioventricular nodes; cholinesterase inhibitors have vagotonic effects on sinoatrial and atrioventricular nodes, leading to bradycardia and AV block; bradycardia and all types of heart block have been reported in patients both with and without known underlying cardiac conduction abnormalities

Cholinomimetics may be expected to increase gastric acid secretion due to increased cholinergic activity; monitor patients closely for symptoms of active or occult gastrointestinal bleeding, especially those with increased risk for developing ulcers, eg, those with a history of ulcer disease or patients using concurrent nonsteroidal anti-inflammatory drugs (NSAIDs)

Cholinomimetics may cause bladder outflow obstruction

Use caution when prescribing to patients with a history of severe asthma or obstructive pulmonary disease; monitor respiratory function closely for occurrence of respiratory adverse effects

Cholinesterase inhibitors are believed to have potential to cause generalized convulsions; seizure activity may also be a manifestation of Alzheimer’s disease; patients with Alzheimer’s disease should be monitored closely for seizures while receiving therapy

Due to pharmacological properties, therapy may cause nausea, vomiting, diarrhea, anorexia, and weight loss; monitor patient’s weight during therapy

Individuals with mild cognitive impairment demonstrate isolated memory impairment greater than expected for their age and education, but do not meet current diagnostic criteria for Alzheimer’s disease

Pregnancy

There are no adequate data on developmental risk associated with use in pregnant women

Animal data

• In studies conducted in animals, administration of galantamine during pregnancy resulted in developmental toxicity (increased incidence of morphological abnormalities and decreased growth in offspring) at doses similar to or greater than those used clinically

Lactation

There are no data on presence of ddrug in human milk, effects on breastfed infant, or on milk production

Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for drug and any potential adverse effects on breastfed infant from therapy or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Derived from daffodil bulbs

Increases acetylcholine from surviving presynaptic nerve terminals by modulating the nicotinic acetylcholine receptor. Glutamate and serotonin levels may increase

Pharmacokinetics

Half-Life: 7 hr

Peak Plasma Time: 1 hr

Bioavailability: 90%

Protein Bound: 18%

Vd: 175 L

Metabolism: CYP2D6 & CYP3A4

Excretion: Urine