Rasagiline (Azilect) is an irreversible monoamine oxidase type B (MAO-B) inhibitor used in the treatment of Parkinson's disease. It was developed by Teva Pharmaceutical Industries Ltd. of Israel and received approval from the U.S. Food and Drug Administration (FDA) for marketing in 2006.

What is Rasagiline (Azilect)?

Rasagiline (Azilect) is an irreversible monoamine oxidase type B (MAO-B) inhibitor for the treatment of Parkinson's disease. It exerts its effect by irreversibly inhibiting the MAO-B enzyme, which reduces the degradation of dopamine and increases the extracellular level of dopamine in the striatum, thereby improving motor function.

Dosage Forms, Strengths and Properties of Rasagiline (Azilect)

Drug Components and Dosage Forms

Active Ingredient: Each tablet contains rasagiline mesylate, equivalent to 0.5 mg or 1 mg of rasagiline base.

Excipients: Mannitol, starch, pregelatinized starch, colloidal silicon dioxide, stearic acid, and talc.

Appearance and Strengths

0.5 mg Tablets: White to off-white, round, flat-faced tablets with beveled edges. One side is engraved with "GIL 0.5" and the other side is blank.

1 mg Tablets: White to off-white, round, flat-faced tablets with beveled edges. One side is engraved with "GIL 1" and the other side is blank.

Packaging: Each bottle contains 30 tablets (NDC 68546-229-56 and NDC 68546-142-56).

Storage Conditions

Store at room temperature below 25°C (77°F). Short-term storage between 15°C and 30°C (59°F and 86°F) is permitted.

Dosage and Administration of Rasagiline (Azilect)

Recommended Dosage

Monotherapy: 1 mg orally once daily.

Combination Therapy with Levodopa: The initial dose is 0.5 mg orally once daily. If the therapeutic effect is insufficient, the dose may be increased to 1 mg once daily.

Dosage Adjustments for Special Populations

Hepatic Impairment: For patients with mild hepatic impairment (Child-Pugh score 5-6), reduce the dose to 0.5 mg per day; it is contraindicated in patients with moderate to severe hepatic impairment.

Concomitant Use with CYP1A2 Inhibitors: When used concomitantly with strong CYP1A2 inhibitors (e.g., ciprofloxacin), the dose should be reduced to 0.5 mg per day.

Administration Precautions

Dietary Restrictions: Avoid foods high in tyramine (e.g., aged cheese, pickled herring) and amine-containing drugs (e.g., pseudoephedrine) to prevent hypertensive crisis.

Missed Dose: Skip the missed dose and take the next dose at the regularly scheduled time the next day.

Serious Risks

Hypertensive Crisis: Associated with tyramine intake and requires emergency treatment.

Serotonin Syndrome: Concomitant use with selective serotonin reuptake inhibitors (SSRIs) or serotonin-norepinephrine reuptake inhibitors (SNRIs) (a class of antidepressants) should be avoided.

Contraindications

Concomitant use with meperidine, dextromethorphan, or St. John's wort is prohibited.

Contraindicated in patients with pheochromocytoma.