Galantamine

Registered South African indications:

• Dementia associated with Alzheimer's disease

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Severe renal impairment
• Severe hepatic impairment

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment (CrCl ≥9ml/min)
• Moderate hepatic impairment
• Elderly (with low body weight and/or serious comorbidities)
• Porphyria
• Non-Alzheimer's type dementia or other types of memory impairment
• Cardiac disorders
• Risk factors for bradycardia
• Atrioventricular node block
• Sick sinus syndrome
• Cardiovascular diseases
• Supraventricular cardiac conduction disturbances
• Uncorrected electrolyte disturbance (e.g. hyperkalaemia, hypokalaemia)
• Immediate post myocardial infarction period
• New-onset atrial fibrillation
• Second degree (or higher) heart block
• Unstable angina pectoris
• Congestive cardiac failure, especially NYHA III-IV
• History of peptic ulcer disease or risk factors thereof
• Gastrointestinal obstruction
• Recent gastrointestinal surgery
• Epilepsy or history of seizures
• Cerebrovascular disease
• Severe asthma
• Obstructive pulmonary disease
• Active pulmonary infections (e.g. pneumonia)
• Urinary outflow obstruction
• Recent bladder surgery
• Pseudocholinesterase deficiency
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: prolonged release caps (PR cap)

Dementia of the Alzheimer type - mild to moderate

• Oral (PR cap): Initial: 8mg, dly; Treatment duration: ≥4 weeks; Maintenance: 16mg, dly; Treatment duration: ≥4 weeks; If response inadequate; Titrate to 24mg, dly

If there is no response to a daily dose of 24mg, this should be reduced to 16mg, dly

A diagnosis of Alzheimer's dementia should be made according to current guidelines by an experienced physician

Tolerance and dosing should be reassessed on a regular basis

Maintenance treatment can be continued for as long as therapeutic benefit and patient tolerance is favourable

Discontinue treatment if therapeutic benefit is no longer present or patient does not tolerate treatment

Galantamine prolonged release capsules should be administered once daily in the morning, preferably with food

Not indicated for use in children

Pregnancy

• Caution
• For galantamine no clinical data on exposed pregnancies are available. Studies in animals have shown reproductive toxicity. Caution should be exercised when prescribing to pregnant women

Breastfeeding

• Caution; not recommended
• It is not known whether galantamine is excreted in human breast milk and there are no studies in breastfeeding women. Therefore women on galantamine should not breastfeed

Fertility

• The effect of galantamine on human fertility has not been evaluated

Renal Impairment

• CrCl ≥9ml/min: Caution; no dose adjustment recommended
  For CrCl 9-59ml/min; Max: 16mg/24hrs is recommended
• CrCl <9ml/min: Contraindicated 

Hepatic Impairment

• Mild (Child-Pugh score 5-6): No dose adjustment recommended
• Moderate (Child-Pugh score 7-9): Caution; dose adjustment recommended
  Based on pharmacokinetic modelling, consider:
  Oral (PR cap): Initial: 8mg, 48hrly for 7 days; Maintenance: 8mg, dly for 28 days; Max: 16mg/24hrs
• Severe (Child-Pugh >9): Contraindicated

Elderly

• No dose adjustment recommended
  Caution in patients with low body weight and/or serious comorbidities

Porphyria Information

• Probably not porphyinogenic (PNP)
  Very common and common side effects that can be potentially porphyrinogenic through reduction in carbohydrate intake and that also can be confused with an acute porphyria attack are reduced appetite, anorexia, vomiting, nausea, abdominal pain, diarrhoea, dyspepsia, stomach and abdominal discomfort, fatigue and decreased weight

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Depression
• Visual hallucinations
• Auditory hallucinations
• Syncope
• Dizziness
• Tremor
• Headache
• Somnolence
• Lethargy
• Paraesthesia
• Hypersomnia  
• Seizures
• Fatigue
• Falling

Cardiovascular Disorders

• Bradycardia
• Supraventricular extrasystoles
• First degree atrioventricular block
• Complete atrioventricular block
• Sinus bradycardia
• Palpitations
• Hypertension
• Hypotension

Gastrointestinal Disorders

• Nausea and vomiting
• Abdominal pain
• Abdominal discomfort
• Diarrhoea
• Dyspepsia
• Retching

Hepatobiliary Disorders

• Hepatitis
• Increased hepatic enzymes

Endocrine and Metabolic Disorders

• Decreased weight
• Increased hepatic enzyme 
• Anorexia
• Dehydration
• Decreased appetite

Musculoskeletal Disorders

• Muscle spasms
• Muscular weakness

Skin and Subcutaneous Tissue Disorders

• Hyperhidrosis
• Stevens-Johnson syndrome
• Acute generalized exanthematous pustulosis
• Erythema multiforme
• Flushing
• Laceration

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity

Sensory Disorders

• Blurred vision
• Tinnitus
• Dysgeusia

• Non-steroidal anti-inflammatory drugs
• Cholinomimetic agents
• Ambenonium
• Donepezil
• Neostigmine
• Pyridostigmine
• Rivastigmine
• Pilocarpine (systemically administered)
• Anticholinergic agents
• Agents that increase the risk of torsades de pointes
• Anaesthesia
• Digoxin
• Beta-blockers
• Calcium-channel blockers
• Amiodarone
• CYP2D6 inhibitors
• Quinidine
• Paroxetine
• Fluoxetine
• CYP3A4 inhibitors
• Ketoconazole
• Erythromycin
• Ritonavir

• Weight
• Mental status

Galantamine, a tertiary alkaloid is a selective, competitive and reversible inhibitor of acetylcholinesterase. In addition, galantamine enhances the intrinsic action of acetylcholine on nicotinic receptors, probably through binding to an allosteric site of the receptor. As a consequence, an increased activity in the cholinergic system associated with improved cognitive function can be achieved in patients with dementia of the Alzheimer type.

Capsule 8mg

• Remcept xl (Actavis)
• Reminyl cr (Janssen) originator (Discontinued)

Capsule 16mg

• Remcept xl (Actavis)
• Reminyl cr (Janssen) originator (Discontinued)

Capsule 24mg

• Remcept xl (Actavis)
• Reminyl cr (Janssen) originator