Galantamine increases the brain acetylcholine levels by inhibiting the enzyme acetylcholinesterase reversibly and competitively. It is used in disorders of memory impairment.

Indications of Galantamine:

• It is indicated for the treatment of mild-to-moderate dementia of Alzheimer's disease.

• Off Label Use of Galantamine in Adults:

  • Dementia associated with Parkinson's disease.
  • Lewy body dementia.
  • Severe dementia of Alzheimer's disease.

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Galantamine dosage in adults:

Galantamine treatment dose of mild-to-moderate Alzheimer dementia:

• Immediate-release tablet or solution:

  • Initial: 4 mg per oral twice daily for 4 weeks;
  • if tolerated, increase to 8 mg twice daily for ≥4 weeks;
  • if tolerated, increase to 12 mg twice daily.
  • Range: 16 to 24 mg daily in 2 divided doses.

• Extended-release capsule:

  • Initial: 8 mg per oral once daily for 4 weeks;
  • if tolerated, increase to 16 mg once daily for ≥4 weeks;
  • if tolerated, increase to 24 mg once daily.
  • Range: 16 to 24 mg once daily.

Note: The lowest dose should be resumed if therapy is interrupted for ≥3 days and gradually increased to the current dose.

Galantamine treatment dose of Severe Alzheimer dementia (off-label):

• Immediate-release tablet:

  • Initial: 4 mg per oral b.i.d daily for 4 weeks;
  • if tolerated, increase to 8 mg twice daily for ≥4 weeks;
  • if tolerated, increase to 12 mg twice daily.
  • May decrease to 8 mg twice daily if the target dose is not tolerated.
  • Range: 16 to 24 mg daily in 2 divided doses.

Galantamine treatment dose of Dementia associated with Parkinson disease and Lewy body dementia (off-label):

• Oral: American Psychiatric Association recommends dosing and titration similar to those for patients with Alzheimer's disease.

• Conversion from immediate release to the extended-release formulation:

  • The last immediate-release dose should b taken in the evening and the extended-release dose should be started the following morning for conversion from the immediate-release formulation to the extended-release formulation.
  • The same total daily dose should be used.
  • Conversion to galantamine from other cholinesterase inhibitors: Before switching to galantamine, patients experiencing poor tolerability with donepezil or rivastigmine should wait until side effects subside or allow a 7-day washout period.
  • Galantamine therapy can be started immediately in patients not having any side effects with donepezil or rivastigmine.

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Use in Children:

Not indicated [/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Dose in Pregnancy & lactation" collapse_text="Dose in Pregnancy & lactation" ]

Pregnancy Risk Factor C

• Studies on animal reproduction revealed negative outcomes.

Galantamine is used during lactation

• It is unknown if galantamine is excreted in breast milk.
• Galantamine should not be administered to nursing mothers without caution, as directed by the manufacturer.

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Galantamine dose adjustment in kidney disease:

• Mild impairment:

  • There are no dosage adjustments provided in the manufacturer’s labeling.

• Moderate impairment (CrCl 9 to 59 mL/minute):

  • Maximum dose: 16 mg/day.

• Severe impairment (CrCl <9 mL/minute):

  • Use is not recommended.

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Galantamine dose adjustment in liver disease:

• Mild impairment (Child-Pugh class A):

  • There are no dosage adjustments provided in the manufacturer’s labeling; however, single-dose galantamine pharmacokinetics were similar to those observed in healthy subjects.

• Moderate impairment (Child-Pugh class B):

  • Maximum dose: 16 mg/day.

• Severe impairment (Child-Pugh class C):

  • Use is not recommended.

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Common Side Effects of Galantamine:

• Gastrointestinal:

  • Nausea
  • Vomiting

Uncommon Side Effects of Galantamine:

• Cardiovascular:

  • Bradycardia
  • Syncope

• Central Nervous System:

  • Dizziness
  • Headache
  • Depression
  • Falling
  • Fatigue
  • Drowsiness
  • Lethargy
  • Malaise

• Endocrine & Metabolic:

  • Weight Loss

• Gastrointestinal:

  • Decreased Appetite
  • Diarrhea
  • Abdominal Pain
  • Abdominal Distress
  • Dyspepsia
  • anorexia

• Neuromuscular & Skeletal:

  • Tremor
  • Muscle Spasm

• Miscellaneous:

  • Laceration

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Contraindications to Galantamine:

Hypersensitivity to any drug or component of the formulation Hypersensitivity to other Tertiary Alkaloids

Warnings and precautions

• Depression in the CNS:

  • It can lead to CNS depression, which can impair physical and mental abilities.
  • When operating machinery or driving, be careful.

• Reactions to skin:

  • There are certain fatal dermatological reactions, including Stevens-Johnson Syndrome, erythema multife and acute generalized exanthematous pustulosis.
  • In such cases, therapy should be stopped.
  • If there are suspicions of drug-related rash, alternate therapy should be considered.

• Vagotonic effects

  • Cholinesterase inhibitors can help to prevent vagotonic effects that could lead to bradycardia, or heart block.
  • These conditions can be experienced without or with pre-existing heart disease.

• Weight loss

  • It can lead to weight loss. Regular bodyweight monitoring is important.

• Anomalies in cardiac conduction:

  • Patients suffering from conduction abnormalities, bradycardia or sick-sinus syndrome should be cautious.
  • According to Alzheimer's treatment guidelines, bradycardia is considered a relative contraindication to the use centrally-active Cholinesterase Inhibitors.

• Hepatic impairment

  • It is not recommended for severe hepatic impairment.
  • Moderate liver impairment calls for dose reduction

• Peptic ulcer disease:

  • It can increase gastric acid secretion so it should not be used in patients at high risk for ulcer disease (eg, prior history or use of NSAIDs).
  • You should monitor any bleeding symptoms.

• Renal impairment

  • It is not recommended for patients with severe renal impairment. Patients with moderate renal impairment should exercise caution.

• Respiratory disease

  • Patients with COPD or asthma should be cautious.

• Seizure disorder

  • Patients with seizure disorders should be cautious.

• Occlusion of the urinary tract:

  • This can cause or worsen bladder obstruction and exacerbate BPH.
  • In such situations, it is important to exercise caution.

Galantamine: Drug Interaction

Monitoring parameters:

Body weight Mental status [/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="How to administer?" collapse_text="How to administer?" ]

How to administer Galantamine?

Oral: The extended-release capsule should not be taken with breakfast, but should be taken orally with a solution or tablet. Dose of oral solution should be mixed with 3-4 ounces of non-alcoholic beverage. Mix well and consume immediately. You should resume the drug if the therapy has been stopped for more than 3 days. Then, gradually increase the dose. [/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Pharmacology & MOA" collapse_text="Pharmacology & MOA" ]

Mechanism of action of Galantamine:

Galantamine, a centrally-acting inhibitor of cholinesterase (competitive & reversible), is an example. It slows down acetylcholine degrading, thereby increasing cerebral cortex acetylcholine levels. It modulates nicotinic-acetylcholine receptors to increase acetylcholine levels from the surviving presynaptic terminals. It is possible that the levels of glutamate could be raised. Protein binding: 18% Metabolism:

• Hepatic metabolism primarily via CYP2D6 to O-desmethyl-galantamine and 3A4 to galantamine-N-oxide;
• the activity of galantamine metabolites is not considered to be clinically relevant.

Bioavailability: 90%. Half-life elimination:

• 7 hours.

Time to peak:

• Immediate-release: 1 hour (2.5 hours with food);
• Extended-release: 4.5-5 hours

Excretion:

• Urine (20%).

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International Brands of Galantamine:

• Razadyne
• Razadyne ER
• Auro-Galantamin ER
• Mar-Galantamin ER
• MYLAN-Galantamin ER
• PAT-Galantamin ER
• PMS-Galantamin ER
• Reminyl ER
• TEVA-Galantamin ER
• Antial
• Galagi 4
• Galagi 8
• Galamer
• Galantex XL
• Galantyl
• Galsya
• Gamine XR
• Gatamine
• Gazylan XL
• Luventa XL
• Nivalin
• Proneurax
• Remember
• Reminy ERl
• Reminyl
• Reminyl ER
• Reminyl LP
• Reminyl PRC
• Reminyl XL
• Tamirin SR

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Galantamine Brand Names in Pakistan:

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