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 prescribed for the management of mild-to-moderate Alzheimer's disease dementia.

• 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 dosage is 4 mg twice daily for 4 weeks; if tolerated, 8 mg twice daily for 4 weeks; if tolerated, 12 mg twice daily.
  • 16 to 24 milligrammes each day, divided into two doses.

• Extended-release capsule:

  • Initial dosage is 8 mg orally once daily for 4 weeks. If tolerated, the dose is increased to 16 mg once daily for 4 weeks. If tolerated, the dosage is increased to 24 mg once daily.
  • 16 to 24 mg once daily is the range.

Note: If therapy is stopped for more than three days, the lowest dose should be started back up and progressively increased to the current level.

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

• Immediate-release tablet:

  • Initial dosage is 4 mg orally twice daily for 4 weeks; if tolerated, this dosage is increased to 8 mg twice daily for 4 weeks; if tolerated, this dosage is increased to 12 mg twice daily.
  • If the intended dose is not tolerated, it could be reduced to 8 mg twice daily.
  • 16 to 24 milligrammes each day, divided into two doses.

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

• Oral:Similar dosage and titration recommendations are made by the American Psychiatric Association for people who have Alzheimer's disease.

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

  • For conversion from the immediate-release formulation to the extended-release formulation, the final immediate-release dose should be taken in the evening, and the first extended-release dose should be started the next morning.
  • Use should be made of the same total daily dose.
  • Conversion from other cholinesterase inhibitors to galantamine: Patients who had trouble tolerating donepezil or rivastigmine should wait until their adverse effects subsided or give themselves a seven-day washout period before switching to galantamine.
  • Patients who are not experiencing any donepezil or rivastigmine adverse effects can begin galantamine medication right away.

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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:

  • The manufacturer's labelling does not mention dosage modifications.

• 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):

  • The manufacturer's labelling does not mention dosage changes, although the pharmacokinetics of a single dose of galantamine were comparable to those seen in healthy patients.

• 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.
  • Be cautious when operating machinery or when driving.

• Reactions to skin:

  • Acute generalised exanthematous pustulosis, Stevens-Johnson Syndrome, and erythema multife are a few deadly dermatological reactions.
  • 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 be taken orally with a solution or tablet rather than with breakfast. You should combine your oral solution dosage with 3–4 ounces of non-alcoholic liquid. Mix thoroughly, then consume right away. If the medication has been interrupted for longer than three days, you should restart the therapy. After that, gradually up the dose. [/bg collapse] [bg collapse icon="arrow" color="#f7f2f2" view="button-blue"] Pharmacology and MOA expands and collapses as needed.

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. To raise the amounts of acetylcholine from the remaining presynaptic terminals, it modifies nicotinic-acetylcholine receptors.

Protein binding: 18%

Metabolism:

• O-desmethyl-galantamine and galantamine-N-oxide are metabolised in the liver largely by CYP2D6 and 3A4, respectively; the therapeutic relevance of galantamine metabolite activity is not thought to exist.

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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