Rasagiline is a potent, irreversible, and selective monoamine oxidase-B (MAO-B) inhibitor used primarily as monotherapy or adjunctive therapy in the treatment of Parkinson's disease (PD). It enhances dopaminergic neurotransmission in the striatum by reducing the metabolic breakdown of dopamine, thereby improving motor symptoms. Unlike older non-selective MAO inhibitors, rasagiline has a favorable safety profile with minimal risk of the 'cheese effect' (tyramine-induced hypertensive crisis) at the recommended dose of 1 mg/day.
Adult: Monotherapy: 1 mg orally once daily. Adjunctive therapy with levodopa: 0.5 mg orally once daily. May be increased to 1 mg once daily based on clinical response and tolerability.
Note: Can be taken with or without food, at any time of day. Consistency in timing is recommended. Tablet should be swallowed whole with water. Do not crush or chew.
Rasagiline irreversibly and selectively inhibits the enzyme monoamine oxidase type B (MAO-B) in the brain. MAO-B is responsible for the catabolism of dopamine in the striatum. By inhibiting this enzyme, rasagiline increases the availability of synaptic dopamine, thereby improving the dopaminergic neurotransmission that is deficient in Parkinson's disease.
Pregnancy: Category C. Animal studies have shown adverse effects. There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Driving: May cause dizziness, orthostatic hypotension, and somnolence. Patients should be cautioned about operating machinery or driving until they are reasonably certain that rasagiline does not affect them adversely.
| Other MAO Inhibitors (e.g., Selegiline, Phenelzine, Isocarboxazid, Linezolid) | Risk of severe hypertensive crisis, hyperpyrexia, serotonin syndrome. | Contraindicated |
| Sympathomimetics (e.g., Ephedrine, Pseudoephedrine, Amphetamines) | Exaggerated pressor response, risk of hypertensive crisis. | Major |
| Serotonergic Drugs (SSRIs, SNRIs, TCAs, Tramadol, Meperidine, Dextromethorphan, Triptans) | Increased risk of serotonin syndrome (confusion, hyperthermia, rigidity, myoclonus). | Contraindicated/Major |
| Tyramine-rich foods (Aged cheeses, cured meats, fermented products) | Potential for hypertensive crisis ('cheese effect'), though risk at 1 mg/day is considered low. | Moderate |
| Ciprofloxacin, Fluoroquinolones | Inhibit CYP1A2, may increase rasagiline plasma levels. | Moderate |
| Omeprazole | Weak CYP1A2 inducer, may slightly decrease rasagiline levels. | Minor |