rasagiline mesilate: clinical use

Prescribing considerations

• Review all prescription, non-prescription and herbal products for MAO-related and serotonergic interactions.
• When used with levodopa, assess for worsening dyskinesia and postural hypotension.
• Warn about excessive daytime sleepiness, sudden sleep onset and driving restrictions.
• Discuss possible hallucinations, confusion and impulse-control disorders with patients and carers.
• Advise assessment of new or changing suspicious skin lesions.
• Use cautiously in mild hepatic impairment and avoid use in moderate hepatic impairment.

Contraindications and cautions

• Hypersensitivity to rasagiline or an excipient
• Concurrent use of another MAO inhibitor, including St John’s wort
• Concurrent use of pethidine
• Severe hepatic impairment

Monitoring

• Clinical response and Parkinson’s motor fluctuations
• Dyskinesia and postural blood-pressure symptoms, particularly with levodopa
• Somnolence or sudden sleep onset
• Hallucinations, confusion and impulse-control behaviours
• New or changing skin lesions
• Hepatic status and changes in smoking or interacting medicines

Clinical pharmacology

Rasagiline is a potent, irreversible, selective MAO-B inhibitor that increases extracellular striatal dopamine. It is extensively metabolised hepatically, principally through CYP1A2; its major active metabolite, 1-aminoindan, does not inhibit MAO-B.

Formulation and product differences

• The selected product is a white to off-white, round oral tablet containing rasagiline as the mesilate salt.
• Only one selected formulation is represented, so no product-to-product formulation comparison can be made.

Tablet

Route: Oral

Strengths: 1 mg