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Indications

REMS


Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

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

Derm: alopecia, ecchymosis, MELANOMA, rash

EENT: conjunctivitis, rhinitis

GI: anorexia, dizziness, dyspepsia, gastroenteritis, vomiting

GU: libido, albuminuria

Hemat: leukopenia

Metab: weight loss

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:

Drug-Natural Products:

Drug-Food:

Availability

(Generic available)

Route/Dosage

Hepatic Impairment

US Brand Names

Azilect

Action

  • Irreversibly inactivates monoamine oxidase (MAO) by binding to it at type B (brain sites); inactivation of MAO leads to increased amounts of dopamine available in the CNS.
  • Differs from selegiline by its nonamphetamine characteristics.
Therapeutic effects:
  • Improvement in symptoms of Parkinson disease, allowing increase in function.

Classifications

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: monoamine oxidase type b inhibitors

Pharmacokinetics

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

ROUTEONSETPEAKDURATION
POrapid1 hr40 days*

* Recovery of MAO-B function.

Patient/Family Teaching

  • Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
  • Instruct patient to omit missed doses and take next dose as scheduled the following day. Do not double doses or discontinue abruptly; may cause 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 2 wk after therapy has been discontinued; they may precipitate a hypertensive crisis. Instruct patient to contact health care provider immediately if symptoms of hypertensive crisis (chest pain, tachycardia, bradycardia, severe headache, stiff/sore, nausea, vomiting, sweating, photosensitivity, enlarged pupils) or serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability, hyperreflexia, incoordination, nausea, vomiting, diarrhea) occur.
  • Instruct patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care provider 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.
  • Caution patient to change positions slowly to minimize orthostatic hypotension. Older adults are at risk.
  • Caution patient to notify health care provider if new agitation; aggression; delirium; hallucinations; or new or 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 provider if periods of daytime sleepiness occur.
  • Advise patient to notify health care provider immediately if severe headache, neck stiffness, heart racing, or palpitations occur.
  • Rep: Advise women of reproductive potential to notify health care providers if pregnancy is planned or suspected or if breastfeeding.

Pronunciation

ra-SA-ji-leen

Code

NDC Code