Rasagiline

Registered South African indications:

• Idiopathic Parkinson's disease

Contraindications

Registered South African contraindications

• Hypersensitivity to rasagiline or to any of the excipients
• Concomitant treatment with other monoamine oxidase (MAO) inhibitors (including products without prescription e.g. St. John's Wort) or pethidine. At least 14 days must elapse between discontinuation of rasagiline and initiation of treatment with MAO inhibitors or pethidine
• Moderate or severe hepatic impairment (Child Pugh B and C)

Contraindications registered in other jurisdictions

• Hypersensitivity to rasagiline or to any of the excipients
• Concomitant treatment with other monoamine oxidase (MAO) inhibitors (including products without prescription e.g. St. John's Wort) or pethidine. At least 14 days must elapse between discontinuation of rasagiline and initiation of treatment with MAO inhibitors or pethidine
• Severe hepatic impairment 

Cautions

• Pregnancy
• Breastfeeding
• Mild hepatic impairment (South African recommendations)
• Mild to moderate hepatic impairment (Recommendations in other jurisdictions)
• Dyskinesia

Forms avail. in SA and covered in this monograph: tab

South African registered indications and dosages

Idiopathic Parkinson's disease
- Monotherapy (without levodopa)
- Adjunct therapy with levodopa in patients with end of dose fluctuations

• Oral (tab): 1mg, once daily taken with or without food

Not established for use in children below 18 years

Pregnancy

South African recommendations

• Caution
• Safety in pregnancy has not been demonstrated

Recommendations in other jurisdictions

• Caution; not recommended 
• There are no data from the use of rasagiline in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of rasagiline during pregnancy 

Breastfeeding

South African recommendations

• Caution
• It is not known whether rasagiline is excreted in human milk. Safety in lactation has not been demonstrated

Recommendations in other jurisdictions

• Caution
• Non-clinical data indicate that rasagiline inhibits prolactin secretion and thus, may inhibit lactation. It is not known whether rasagiline is excreted in human milk. Caution should be exercised when rasagiline is administered to a breastfeeding mother 

Fertility

Recommendations below are applicable to South Africa and other jurisdictions

• No human data on the effect of rasagiline on fertility are available. Non-clinical data indicate that rasagiline has no effect on fertility

Renal Impairment

Recommendations below are applicable to South Africa and other jurisdictions

• No dose adjustment recommended 

Hepatic Impairment

South African recommendations

• Mild: Caution; no dose adjustment recommended
  Caution should be used when initiating treatment with rasagiline in patients with mild hepatic insufficiency. In case patients progress from mild to moderate hepatic impairment, rasagiline should be stopped
• Moderate or severe (Child Pugh B and C): Contraindicated

Recommendations in other jurisdictions

• Mild: Caution; no dose adjustment 
  Caution should be used when initiating treatment with rasagiline in patients with mild hepatic impairment. In case patients progress from mild to moderate hepatic impairment rasagiline should be stopped 
• Moderate: Caution; not recommended 
  Rasagiline use in patients with moderate hepatic impairment should be avoided
• Severe: Contraindicated 

Elderly

Recommendations below are applicable to South Africa and other jurisdictions

• No dose adjustment recommended

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Hallucinations
• Abnormal dreams
• Confusion
• Dyskinesia
• Dystonia
• Balance disorder
• Cerebrovascular accident

Cardiovascular Disorders

• Angina pectoris
• Orthostatic hypotension

Gastrointestinal Disorders

• Abdominal pain
• Constipation
• Nausea and vomiting
• Dry mouth

Endocrine and Metabolic Disorders

• Decreased weight
• Decreased appetite

Musculoskeletal Disorders

• Arthralgia
• Neck pain

Skin and Subcutaneous Tissue Disorders

• Rash
• Skin melanoma

Immune, Blood and Lymphatic System Disorders 

• Fever 

• Monoamine oxidase inhibitors
• Pethidine
• St. John's Wort
• Fluoxetine
• Fluvoxamine
• Dextromethorphan
• Sympathomimetics
• Antidepressants
• CYP1A2 inhibitors
• Smoking
• Entacapone

None routine 

Rasagiline was shown to be a potent, irreversible monoamine oxidase B selective inhibitor, which may cause an increase in extracellular levels of dopamine in the striatum. The elevated dopamine level and subsequent increased dopaminergic activity are likely to mediate rasagiline's beneficial effects seen in models of dopaminergic motor dysfunction.

Tablet 1mg

• Azilect (Teva) originator