Rasagiline

Trade names

• AZILECT

Actions

• Irreversible inhibitor of monoamine oxidase-B.

Route of Administration

Oral

Bioavailability

36%

Plasma protein binding

88-94%

Half-life

3 hours

Metabolism

Hepatic

Elimination

Renal 62%, biliary 7%

Important side-effects

Exacerbation of hypertension.

Certain foods that contain very high amounts (>150 mg) of tyramine may cause severe hypertension in patients treated with MAO-B inhibitors.

Serotonin syndrome when concomitantly administrated with serotonergic medication (SSRI, SNRI, tricyclic and tetracyclic antidepressants, etc).

Excessive somnolence.

Dyskinesias.

Orthostatic hypotension.

Hallucinations and psychosis.

Impaired impulse control and compulsive behaviors.

Increased risk (2 to 6-fold compaired to the general population) of developing melanoma.

Recommended dose

1 mg once daily

Renal impairment

No dose reduction is necessary.

Hepatic impairment

Caution is advised when treating patients with mild hepatic dysfunction.

Patients with moderate and severe hepatic function impairment should not be treated with rasagiline.