Rasagiline is an irreversible monoamine oxidase (MAO) inhibitor that is thought to exert its effect by specifically inhibiting MAO-B, thereby causing an increase in the extracellular levels of dopamine in the striatum.
First once-daily oral treatment for Parkinson's disease approved
Rasagiline is an irreversible monoamine oxidase (MAO) inhibitor that is thought to exert its effect by specifically inhibiting MAO-B, thereby causing an increase in the extracellular levels of dopamine in the striatum. Rasagiline was approved on May 16, 2005, for the treatment of the signs and symptoms of idiopathic Parkinson's disease (PD) as initial monotherapy and as adjunct therapy to levodopa.
Safety. Rasagiline is contraindicated for use with the analgesics meperidine, tramadol, methadone, and propoxyphene. Patients taking rasagiline should not take dextromethorphan or sympathomimetic amines such as pseudoephedrine and phenylephrine. Rasagiline should not be administered along with other MAO inhibitors due to the increased risk of non-selective MAO inhibition that may lead to hypertensive crisis. The coadministration of rasagiline with selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants, or tetracyclic antidepressants is not recommended. Patients taking rasagiline should not undergo elective surgery requiring general anesthesia, and the agent should be discontinued at least 14 days prior to elective surgery because of hypertension concerns. Due to the risk of a hypertensive crisis/"cheese reaction," a dietary tyramine restriction is necessary in patients currently taking rasagiline and for 2 weeks following discontinuation of the drug. The most common adverse events associated with rasagiline monotherapy include flu syndrome, arthralgia, depression, dyspepsia, and fall.
Dosing. The recommended dose of rasagiline as monotherapy is 1.0 mg administered once daily. The recommended initial dose of rasagiline as adjunct therapy to levodopa is 0.5 mg administered once daily. If a sufficient clinical response is not achieved with 0.5 mg, the dose may be increased to 1.0 mg administered once daily. When rasagiline is administered in combination with levodopa, a reduction of the levodopa dose may be considered based upon individual response. The rasagiline dose should be reduced to 0.5 mg daily in patients taking ciprofloxacin and other CYP1A2 inhibitors. Patients with mild hepatic impairment should take 0.5 mg of rasagiline daily. Patients with moderate-to-severe hepatic impairment should not take rasagiline.