• Basic Info
• Top Questions
• Clinical Info
• Interactions

Uses

Parkinsonian Syndrome

Symptomatic treatment of idiopathic parkinsonian syndrome.

Used as initial monotherapy in patients with early disease or as adjunctive therapy to levodopa in patients with more advanced disease who exhibit a deteriorating response to levodopa/carbidopa.

Dosage and Administration

General

Concomitant Levodopa/Carbidopa Therapy
• Consider reduction of levodopa dosage if adverse dopaminergic effects (e.g., dyskinesia, hallucinations) occur. In clinical studies, approximately 9–17% of patients receiving 0.5 or 1 mg rasagiline daily required reduction of levodopa dosage (average reduction: about 9–13%).

Administration

Oral Administration

Administer orally once daily without regard to meals.

Dosage

Available as rasagiline mesylate; dosage expressed in terms of rasagiline.

Adults

Parkinsonian Syndrome

Monotherapy

Oral

1 mg once daily.

Adjunctive Therapy with Levodopa

Oral

Initially, 0.5 mg once daily.

If adequate response is not achieved, may increase dosage to 1 mg once daily.

Special Populations

Dosage in Hepatic Impairment

0.5 mg once daily in patients with mild (Child-Pugh score of 5–6) hepatic impairment.

Use not recommended in patients with moderate or severe (Child-Pugh score ≥7) hepatic impairment. (See Special Populations under Pharmacokinetics.)

Dosage in Renal Impairment

No dosage adjustment required in patients with mild renal impairment.

Geriatric Patients

No dosage adjustment required.

Cautions

Contraindications

• Concomitant use with cyclobenzaprine, dextromethorphan, meperidine, mirtazapine, methadone, propoxyphene, tramadol, St. John’s wort (Hypericum perforatum), sympathomimetic amines (e.g., amphetamines, ephedrine, phenylephrine, phenylpropanolamine [no longer commercially available in the US], pseudoephedrine), or other MAO inhibitors. (See Interactions.)
• Elective surgery that requires general anesthetics, cocaine, or local anesthetics containing sympathomimetic vasoconstrictors. Discontinue rasagiline ≥14 days prior to elective surgery; if surgery is needed sooner, may use benzodiazepines, mivacurium, rapacuronium, fentanyl, morphine, or codeine with caution.
• Pheochromocytoma.

Warnings/Precautions

Warnings

Risks Associated with MAO Inhibition

Selectivity for MAO-B (and not MAO-A) in humans not sufficiently elucidated to permit rasagiline treatment without restriction of dietary tyramine or sympathomimetic amines. Even for relatively selective MAO-B inhibitors, selectivity for MAO-B usually diminishes and ultimately is lost at high dosages, and the drug will inhibit both MAO-B and MAO-A.

Possibly severe hypertensive reaction or hypertensive crisis (i.e., cheese reaction) following ingestion of foods, beverages, or dietary supplements containing large amounts of tyramine. (See Interactions and see also Advice to Patients.)

Severe hypertensive reaction or hypertensive crisis reported following concomitant use of selective (i.e., selegiline) or nonselective (e.g., phenelzine, tranylcypromine) MAO inhibitors with sympathomimetic amines (e.g., ephedrine). (See Interactions and see also Advice to Patients.)

Severe, sometimes fatal reactions resembling serotonin syndrome reported following concomitant use of selective or nonselective MAO inhibitors with highly serotonergic drugs (e.g., selective serotonin- and norepinephrine-reuptake inhibitors [SNRIs], SSRIs, tricyclic antidepressants). (See Interactions.)

Concomitant Use with Ciprofloxacin or Other CYP1A2 Inhibitors

Concomitant use with ciprofloxacin or other CYP1A2 inhibitors shown, or expected, to increase plasma rasagiline concentrations by up to twofold. Adjustment of rasagiline dosage recommended. (See Drugs Affecting Hepatic Microsomal Enzymes under Interactions.)

Major Toxicities

Orthostatic Hypotension

Orthostatic hypotension reported in patients receiving rasagiline as monotherapy or as adjunctive therapy with levodopa. Occurs most frequently during the first 2 months of therapy and less frequently over time.

Hallucinations

Hallucinations reported in patients receiving rasagiline as monotherapy or as adjunctive therapy with levodopa. (See Advice to Patients.)

General Precautions

Melanoma

Risk of melanoma developingin patients receiving rasagiline appears to be greater than that in the general population but comparable to that in patients with Parkinson’s disease.

Monitor for melanomas frequently. Perform dermatologic examinations periodically; frequency of examinations determined by patient’s dermatologist.

Specific Populations

Pregnancy

Category C.

Lactation

Inhibits prolactin secretion in rats; may inhibit milk secretion in women. Not known whether rasagiline is distributed into milk; caution if used in nursing women.

Pediatric Use

Safety and efficacy not established in pediatric patients <18 years of age.

Geriatric Use

No overall differences in safety relative to younger adults.

Hepatic Impairment

Dosage adjustment recommended in patients with mild (Child-Pugh score of 5–6) hepatic impairment.

Use not recommended in patients with moderate or severe (Child-Pugh score ≥7) hepatic impairment. (See Special Populations under Pharmacokinetics.)

Common Adverse Effects

Monotherapy: Flu syndrome, arthralgia, depression, dyspepsia, fall.

Adjunctive therapy with levodopa: Dyskinesia, accidental injury, weight loss, orthostatic hypotension, vomiting, anorexia, arthralgia, abdominal pain, nausea, constipation, dry mouth, rash, ecchymosis, somnolence, paresthesia.