pharmacopeia
GET
/api/v1/drug/galantamine
2D structure
(1S,12S,14R)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraen-14-ol
SMILES CN1CC[C@@]23C=C[C@@H](C[C@@H]2OC4=C(C=CC(=C34)C1)OC)O
InChIKey ASUTZQLVASHGKV-JDFRZJQESA-N

Mechanism of action

Sourced from openFDA

Although the etiology of cognitive impairment in Alzheimer's disease (AD) is not fully understood, it has been reported that acetylcholine-producing neurons degenerate in the brains of patients with Alzheimer's disease. The degree of this cholinergic loss has been correlated with degree of cognitive impairment and density of amyloid plaques (a neuropathological hallmark of Alzheimer's disease).

Cholinesterase

Indications

Sourced from openFDA
  • Galantamine tablets are indicated for the treatment of mild to moderate dementia of the Alzheimer’s type.

Contraindications

Sourced from openFDA
  • Galantamine tablets are contraindicated in patients with known hypersensitivity to galantamine hydrobromide or to any excipients used in the formulation.contraindicated

Dosage & administration

Sourced from openFDA

Galantamine tablets: Recommended starting dosage is 4 mg twice daily; increase to initial maintenance dosage of 8 mg twice daily after a minimum of 4 weeks. Based on clinical benefit and tolerability, dosage may be increased to 12 mg twice daily after a minimum of 4 weeks at 8 mg twice daily. ( 2.2 ) Take with meals; ensure adequate fluid intake during treatment ( 2.2 ) Hepatic impairment: should not exceed 16 mg/day for moderate hepatic impairment; do not use in patients with severe hepatic impairment ( 2.3 ) Renal impairment: should not exceed 16 mg/day for creatinine clearance 9 to 59 mL/min; do not use in patients with creatinine clearance less than 9 mL/min ( 2.4 ) 2.2 Galantamine Immediate-Release Tablets The dosage of galantamine tablets shown to be effective in controlled clinical trials is 16 - 32 mg/day given as twice daily dosing. As the dosage of 32 mg/day is less well tolerated than lower dosages and does not provide increased effectiveness, the recommended dosage range is 16 - 24 mg/day given twice daily. The dosage of 24 mg/day did not provide a statistically significant greater clinical benefit than 16 mg/day. It is possible, however, that a daily dosage of 24 mg of galantamine tablets might provide additional benefit for some patients. The recommended starting dosage of galantamine tablets is 4 mg twice a day (8 mg/day). The dosage should be increased to the initial maintenance dosage of 8 mg twice a day (16 mg/day) after a minimum of 4 weeks.

Warnings & precautions

Sourced from openFDA

Serious skin reactions: discontinue at first appearance of skin rash ( 5.1 ) 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 ( 5.3 ) Active or occult gastrointestinal bleeding: monitor, especially those with an increased risk for developing ulcers ( 5.4 ) Cholinomimetics may cause bladder outflow obstruction ( 5.5 ) Monitor for respiratory adverse events in patients with a history of severe asthma or obstructive pulmonary disease ( 5.7 ) 5.1 Serious Skin Reactions Serious skin reactions (Stevens-Johnson syndrome and acute generalized exanthematous pustulosis) have been reported in patients receiving galantamine tablets. Inform patients and caregivers that the use of galantamine tablets should be discontinued at the first appearance of a skin rash, unless the rash is clearly not drug-related. If signs or symptoms suggest a serious skin reaction, use of this drug should not be resumed and alternative therapy should be considered. 5.2 Anesthesia Galantamine, as a cholinesterase inhibitor, is likely to exaggerate the neuromuscular blocking effects of succinylcholine-type and similar neuromuscular blocking agents during anesthesia. 5.3 Cardiovascular Conditions Because of their pharmacological action, cholinesterase inhibitors have vagotonic effects on the sinoatrial and atrioventricular nodes, leading to bradycardia and AV block.

Adverse reactions

Sourced from openFDA

Serious adverse reactions are discussed in more detail in the following sections of the labeling: Serious skin reactions [see Warnings and Precautions (5.1) ] Cardiovascular Conditions [see Warnings and Precautions (5.3) ] Gastrointestinal Conditions [see Warnings and Precautions (5.4) ] Genitourinary Conditions [see Warnings and Precautions (5.5) ] Neurological Conditions [see Warnings and Precautions (5.6) ] Pulmonary Conditions [see Warnings and Precautions (5.7) ] Deaths in subjects with mild cognitive impairment (MCI) [see Warnings and Precautions (5.8) ] The most common adverse reactions (≥ 5%) were nausea, vomiting, diarrhea, dizziness, headache, decreased appetite, and weight decreased ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Upsher-Smith Laboratorles, LLC at 1-855-899-9180 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The most common adverse reactions in galantamine-treated patients from double-blind clinical trials (≥ 5%) were nausea, vomiting, diarrhea, dizziness, headache, and decreased appetite. The most common adverse reactions associated with discontinuation (≥ 1%) in galantamine-treated patients from double-blind clinical trials were nausea (6.2%), vomiting (3.3%), decreased appetite (1.5%), and dizziness (1.3%).

Use in specific populations

Sourced from openFDA

Pregnancy: Based on animal data may cause fetal harm. ( 8.1 ) 8.1 Pregnancy Risk Summary There are no adequate data on the developmental risk associated with the use of galantamine tablets in pregnant women. 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 (see Data). In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. The background risk of major birth defects and miscarriage for the indicated population is unknown. Data Animal Data In rats, administration of galantamine (oral doses of 2, 8, or 16 mg/kg/day), from day 14 (females) or day 60 (males) prior to mating and continuing in females through the period of organogenesis, resulted in an increased incidence of fetal skeletal variations at the two highest doses, which were associated with maternal toxicity. The no-effect dose for embryo-fetal developmental toxicity in rats (2 mg/kg/day) is approximately equal to the maximum recommended human dose (MRHD) of 24 mg/day on a body surface area (mg/m 2 ) basis.

Pharmacokinetics

Sourced from openFDA
Metabolism
The pharmacokinetics of galantamine are linear over a dose range of 8-32 mg/day. Absorption and Distribution Galantamine is absorbed with time to peak concentration of about 1 hour.

Overdosage

Sourced from openFDA

Because strategies for the management of overdose are continually evolving, it is advisable to contact a poison control center to determine the latest recommendations for the management of an overdose of any drug. As in any case of overdose, general supportive measures should be utilized. Signs and symptoms of significant overdosing of galantamine are predicted to be similar to those of overdosing of other cholinomimetics. These effects generally involve the central nervous system, the parasympathetic nervous system, and the neuromuscular junction. In addition to muscle weakness or fasciculations, some or all of the following signs of cholinergic crisis may develop: severe nausea, vomiting, gastrointestinal cramping, salivation, lacrimation, urination, defecation, sweating, bradycardia, hypotension, respiratory depression, collapse and convulsions. Increasing muscle weakness is a possibility and may result in death if respiratory muscles are involved. Tertiary anticholinergics such as atropine may be used as an antidote for galantamine tablets overdosage. Intravenous atropine sulfate titrated to effect is recommended at an initial dose of 0.5 to 1.0 mg i.v.

Approval history

Sourced from openFDA
  • Jan 30, 2009ANDAANDA078185Hikma
  • Feb 6, 2009ANDAANDA077604Yabao Pharm
  • Feb 2, 2011ANDAANDA090178Sun Pharm
  • Mar 29, 2011ANDAANDA090957Aurobindo Pharma Ltd
  • Aug 5, 2016ANDAANDA204895Aurobindo Pharma

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
3,156 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fall80826%
  2. 2Cognitive Disorder65921%
  3. 3Constipation64821%
  4. 4Hypotension63020%
  5. 5Balance Disorder62720%
  6. 6Orthostatic Hypotension62320%
  7. 7Sedation58419%
  8. 8Depressed Level Of Consciousness55918%
  9. 9Pain55017%
  10. 10Creatinine Renal Clearance Decreased52917%
  11. 11Blood Calcium Decreased52817%
  12. 12Sedation Complication52517%
  13. 13Toxicity To Various Agents52517%
  14. 14Mobility Decreased52016%
  15. 15Drug Interaction2668.4%

Literature

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Recent PubMed references pinned to Galantamine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 118 ClinicalTrials.gov registrations naming Galantamine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Galantamine. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

  • CYP2D6CPIC C (provisional)ClinPGx 3FDA label: No Clinical PGx

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Galantamine work?
Although the etiology of cognitive impairment in Alzheimer's disease (AD) is not fully understood, it has been reported that acetylcholine-producing neurons degenerate in the brains of patients with Alzheimer's disease. The degree of this cholinergic loss has been correlated with degree of cognitive impairment and density of amyloid plaques (a neuropathological hallmark of Alzheimer's disease).
What is Galantamine used for?
According to FDA labeling, Galantamine carries indications including: Galantamine tablets are indicated for the treatment of mild to moderate dementia of the Alzheimer’s type.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Galantamine?
Galantamine is classified as Anticholinesterases, Cholinesterase Inhibitor, Cholinesterase Inhibitors, Increased Central Nervous System Acetylcholine Activity, Increased Glutamate Activity, Increased Serotonin Activity.
What are the brand names for Galantamine?
Galantamine is marketed under brand names including Razadyne.
What are the contraindications for Galantamine?
Galantamine labeling lists contraindications including: Galantamine tablets are contraindicated in patients with known hypersensitivity to galantamine hydrobromide or to any excipients used in the formulation.. Always consult the full prescribing information and a clinician.
Note. Data for galantamine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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