Rasagiline

Rasagiline, sold under the brand name Azilect, is an oral medication that acts as a selective, irreversible inhibitor of monoamine oxidase B (MAO-B). By inhibiting MAO-B, rasagiline reduces the breakdown of dopamine in the brain, increasing dopaminergic activity and helping to improve motor symptoms in Parkinson's disease.

Indications for rasagiline include two main uses in adults with Parkinson's disease: as monotherapy in early disease and as an adjunct to levodopa in patients with advancing disease who experience wearing-off or insufficient response to levodopa.

Dosing typically starts at 0.5 mg once daily for monotherapy, and 1 mg once daily when used as an add-on to levodopa. It can be taken with or without food. Rasagiline’s effects are long-lasting because it irreversibly inhibits MAO-B; the enzyme activity resumes only after new MAO-B is synthesized.

Pharmacokinetically, rasagiline is well absorbed orally and is metabolized in the liver, with elimination primarily via urine and feces.

Common adverse effects include headache, joint pain or stiffness, nausea, indigestion, dizziness, and fatigue. Rare but serious risks include hypertensive reactions, especially with high-tyramine foods or other adrenergic agents, and serotonin syndrome when used with serotonergic medications.

Drug interactions center on avoiding concomitant use with other MAO inhibitors and caution with antidepressants (SSRIs, SNRIs, TCAs), meperidine, and other serotonergic or sympathomimetic drugs. When switching therapies, a washout period is often recommended.

Rasagiline was approved for Parkinson's disease in various jurisdictions and is marketed as Azilect.