Azilect for Parkinson’s disease treatment

Azilect (rasagiline) is a selective monoamine oxidase-B (MAO-B) inhibitor used to treat Parkinson’s disease. It can be prescribed alone or together with other Parkinson’s medications to help manage symptoms by affecting brain chemistry.

Azilect is approved for the treatment of Parkinson’s disease in adults.

• As monotherapy or adjunct therapy without levodopa, Azilect is given at 1 mg orally once daily.
• When used with levodopa, the starting dose is 0.5 mg once daily; if tolerated but not fully effective, the dose may be increased to 1 mg once daily.
• Patients taking CYP1A2 inhibitors like ciprofloxacin should not exceed 0.5 mg daily.
• Patients with mild hepatic impairment should also be limited to 0.5 mg daily, and Azilect is contraindicated in moderate to severe hepatic impairment.

Rasagiline mesylate

Azilect works by selectively inhibiting monoamine oxidase-B, an enzyme that breaks down dopamine in the brain. By blocking this enzyme, Azilect increases dopamine levels, helping to improve motor function in Parkinson’s disease. At recommended doses, it selectively inhibits MAO-B, but selectivity decreases at higher doses.

The recommended dosage depends on the treatment context:

• Monotherapy or adjunct without levodopa: 1 mg once daily orally.
• With levodopa: Start 0.5 mg once daily; may increase to 1 mg once daily if tolerated and needed.
• With CYP1A2 inhibitors (e.g., ciprofloxacin): Maximum 0.5 mg once daily.
• Mild hepatic impairment: Maximum 0.5 mg once daily.
• Moderate or severe hepatic impairment: Azilect should not be used.

Do not exceed recommended doses to avoid increased risk of hypertension.

Azilect must not be used with:

• Meperidine, tramadol, methadone, propoxyphene (opioids with serotonin syndrome risk)
• Other monoamine oxidase inhibitors, including selective MAO-B inhibitors
• St. John's wort
• Cyclobenzaprine
• Dextromethorphan

At least 14 days should separate discontinuation of Azilect and initiation of these drugs.

Important safety information

• Hypertension: Azilect may cause or exacerbate high blood pressure, including severe hypertensive episodes. Monitor blood pressure routinely and adjust medications if sustained hypertension occurs. Avoid foods very high in tyramine (>150 mg) due to risk of hypertensive crisis.
• Serotonin syndrome: Risk when combined with antidepressants (SSRIs, SNRIs, tricyclics, tetracyclics, triazolopyridine), meperidine, tramadol, methadone, propoxyphene, or other MAO inhibitors. Azilect is contraindicated with these agents. Allow at least 14 days between stopping Azilect and starting these drugs, or longer (5 weeks) for fluoxetine.
• Somnolence and falling asleep: Patients may experience sudden sleep episodes during activities of daily living, sometimes without warning. Monitor closely, especially if using other sedatives or medications increasing rasagiline levels. Discontinue Azilect if this occurs, and advise patients to avoid driving or hazardous tasks.
• Orthostatic hypotension: Azilect can cause drops in blood pressure upon standing, leading to dizziness or fainting. Frequency is dose related and monitored during treatment.
• Dyskinesia: Azilect may worsen or cause involuntary movements, particularly when used with levodopa. Reducing levodopa dose may reduce this effect.
• Psychiatric effects: Hallucinations, psychotic-like behavior, and impulse control disorders (such as pathological gambling, increased sexual urges, or compulsive spending) have been reported. Monitor patients and consider dose adjustment or discontinuation if these occur.
• Withdrawal-emergent hyperpyrexia and confusion: Resembling neuroleptic malignant syndrome may occur with abrupt dose reduction or withdrawal.

Common and serious side effects

• Common: Somnolence (6% with Azilect vs 4% placebo), orthostatic hypotension, dyskinesia (18% on Azilect adjunct vs 10% placebo), hallucinations (up to 5% with Azilect adjunct to levodopa).
• Serious: Severe hypertension, serotonin syndrome, psychotic behavior, impulse control disorders, neuroleptic malignant syndrome-like symptoms.

Key drug interactions

• Contraindicated with meperidine, tramadol, methadone, propoxyphene, other MAO inhibitors, St. John's wort, cyclobenzaprine, and dextromethorphan due to serious risks including serotonin syndrome and psychosis.
• Concomitant use with CYP1A2 inhibitors such as ciprofloxacin can double rasagiline plasma levels; dose adjustment to 0.5 mg daily is required.
• Use with antidepressants (SSRIs, SNRIs, tricyclics, tetracyclics, triazolopyridine) is not recommended due to serotonin syndrome risk; appropriate washout periods must be observed.