rasagiline

Absorption: 36% absorbed following oral administration.

Distribution: Extensively distributed to tissues; readily crosses the blood-brain barrier.

Metabolism/Excretion: Extensively metabolized by the liver primarily by the CYP1A2 isoenzyme to an inactive metabolite; <1% excreted in urine.

Half-Life: 1.3 hr; does not correlate with duration of MAO-B inhibition.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	rapid	1 hr	40 days*

*Recovery of MAO-B function.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Concurrent use of meperidine, tramadol, methadone, or another MAO inhibitor;
Moderate to severe hepatic impairment;
Elective surgery requiring general anesthesia;
Pheochromocytoma;
Psychotic disorder.

Use Cautiously in:

Mild hepatic impairment;
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: orthostatic hypotension (may ↑ levodopa-induced hypotension), ↑BP, chest pain, syncope

Derm: ↑melanoma risk, alopecia, ecchymosis, rash

EENT: conjunctivitis, rhinitis

GI: ↓weight, anorexia, dizziness, dyspepsia, gastroenteritis, vomiting

GU: ↓libido, albuminuria

Hemat: leukopenia

MS: arthralgia, arthritis, neck pain

Neuro: depression, dizziness, drowsiness, dyskinesia (may ↑ levodopa-induced dyskinesia), hallucinations, impulse control disorders (gambling, sexual), malaise, paresthesia, sleep driving, vertigo

Resp: asthma

Misc: fever, flu-like syndrome

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of meperidine, tramadol, methadone, or other MAO inhibitors may ↑ risk of serotonin syndrome; concurrent use contraindicated.
CYP1A2 inhibitors, including ciprofloxacin, may ↑ levels and risk of toxicity; dose adjustment is recommended.
Dextromethorphan may ↑ risk of psychosis/bizarre behavior; avoid concurrent use.
↑risk of adverse reactions with mirtazapine and cyclobenzapine; avoid concurrent use.
Hypertensive crisis may occur with sympathomimetic amines, including amphetamines, pseudoephedrine, phenylephrine, or ephedrine; avoid concurrent use.
↑risk of serotonin syndrome with tricyclic antidepressants, SSRIs, and SNRIs; rasagiline should be discontinued ≥14 days prior to initiation of antidepressants (fluoxetine should be discontinued ≥5 wk prior to rasagiline therapy).

Drug-Natural Products:

St. John's wort may ↑ risk of serotonin syndrome; avoid concurrent use.

Drug-Food:

Ingestion of foods containing high amounts of tyramine (>150 mg) (e.g., cheese) may result in life-threatening hypertensive crisis.

Route/Dosage ⬆ ⬇

PO (Adults ): Monotherapy or as adjunct therapy in patients not taking levodopa: 1 mg once daily; Concurrent levodopa therapy: 0.5 mg once daily, may ↑ to 1 mg once daily; Concurrent use of ciprofloxacin or other CYP1A2 inhibitors: 0.5 mg once daily.

Hepatic Impairment

PO (Adults ): Mild hepatic impairment: 0.5 mg once daily.

Availability ⬆ ⬇

(Generic available)

Tablets: 0.5 mg; 1 mg

Assessment ⬆ ⬇

Assess signs and symptoms of Parkinson's disease (tremor, muscle weakness and rigidity, ataxic gait) prior to and periodically during therapy.
Monitor BP periodically during therapy.
Assess skin for melanomas periodically during therapy.
Assess for serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile BP, hyperthermia], neuromuscular aberrations [hyperreflexia, incoordination], and/or GI symptoms [nausea, vomiting, diarrhea]), especially in patients taking other serotonergic drugs (SSRIs, SNRIs, triptans).
Monitor for drowsiness or sleepiness. May cause patients to fall asleep while engaged in activities of daily living, including the operation of motor vehicles.

Lab Test Considerations:

May cause albuminuria, leukopenia, and abnormal liver function tests.

Toxicity and Overdose:

Concurrent ingestion of tyramine-rich foods and many medications may result in a life-threatening hypertensive crisis. Signs and symptoms of hypertensive crisis include chest pain, tachycardia or bradycardia, severe headache, neck stiffness or soreness, nausea and vomiting, sweating, photosensitivity, and enlarged pupils.

Implementation ⬆ ⬇

Do not confuse Azilect with Aricept. Do not confuse rasagiline with repaglinide.
If used in combination with levodopa, a reduction in levodopa dose may be considered based on individual results.
PO: Administer once daily.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take rasagiline as directed. Missed doses should be omitted and next dose taken at usual time the following day. Do not double doses. Do not discontinue abruptly; may cause elevated temperature, muscular rigidity, altered consciousness, and autonomic instability.
Caution patient to avoid alcohol, CNS depressants, and foods or beverages containing tyramine (see Food Sources for Specific Nutrients) during and for at least 2 wk after therapy has been discontinued; they may precipitate a hypertensive crisis. Contact health care professional immediately if symptoms of hypertensive crisis or serotonin syndrome develop.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications. Caution patient to avoid use of St. John's wort and analgesics meperidine, tramadol, or methadone during therapy.
Caution patient to avoid elective surgery requiring general anesthesia, cocaine, or local anesthesia containing sympathomimetic vasoconstrictors within 14 days of discontinuing rasagiline. If surgery is necessary sooner, benzodiazepines, rocuronium, fentanyl, morphine, and codeine may be used cautiously.
May cause dizziness or drowsiness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
Caution patient to change positions slowly to minimize orthostatic hypotension. Geriatric patients are at increased risk for this side effect.
Advise patient to monitor for melanomas frequently and on a regular basis.
Caution patient to notify health care professional if new skin lesions, agitation, aggression, delirium, hallucinations, sleep driving, or new or increased gambling, sexual, or other intense urges occur.
Inform patient that rasagiline may cause falling asleep while engaged in activities of daily living, including the operation of motor vehicles, conversations, and eating. Notify health care professional if periods of daytime sleepiness occur.
Advise patient to notify health care professional immediately if severe headache, neck stiffness, heart racing, or palpitations occur.
Rep: Advise female patients to notify health care professionals if pregnancy is planned or suspected, or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇