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

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

Serious skin reactions may occur; discontinue at first appearance of skin rash

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

Active or occult gastrointestinal bleeding: monitor, especially those with an increased risk for developing ulcers

Cholinomimetics may cause bladder outflow obstruction

Monitor for respiratory adverse events in patients with a history of severe asthma or obstructive pulmonary 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