Azilect

rasagiline

(ra-za-ji-leen) ,

Azilect

(trade name)

Classification

Therapeutic: antiparkinson agents
Pharmacologic: monoamine oxidase type b inhibitors
Pregnancy Category: C

Indications

Parkinson's disease (monotherapy and adjunctive to levodopa).

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's disease, allowing increase in function.

Pharmacokinetics

Absorption: 36% absorbed following oral administration.
Distribution: Readily crosses the blood-brain barrier.
Metabolism and Excretion: Extensively metabolized by the liver (CYP1A2 enzyme) to an inactive metabolite; less than 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.

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Concurrent meperidine, tramadol, methadone, sympathomimetic amines, dextromethorphan, mirtazapine, cyclobenzaprine, cocaine, St. John's wort, another MAO inhibitor;Moderate to severe hepatic impairment;Elective surgery requiring general anesthesia; allow 14 days after discontinuation;Pheochromocytoma;Psychotic disorder.
Use Cautiously in: Mild hepatic impairment (↑ blood levels); Obstetric: Use only if maternal benefit outweighs fetal risk; Lactation: May inhibit lactation; Pediatric: Safety not established.

Adverse Reactions/Side Effects

Central nervous system

  • depression
  • dizziness
  • hallucinations
  • malaise
  • vertigo

Ear, Eye, Nose, Throat

  • conjunctivitis
  • rhinitis

Respiratory

  • asthma

Cardiovascular

  • ↑ BP
  • chest pain
  • postural hypotension (may ↑ levodopa-induced hypotension)
  • syncope

Gastrointestinal

  • anorexia
  • dizziness
  • dyspepsia
  • gastroenteritis
  • vomiting

Genitourinary

  • albuminuria
  • ↓ libido

Dermatologic

  • alopecia
  • ecchymosis
  • ↑ melanoma risk
  • rash

Endocrinologic

  • weight loss

Hematologic

  • leukopenia

Musculoskeletal

  • arthralgia
  • arthritis
  • neck pain

Neurologic

  • dyskinesia (may ↑ levodopa-induced dyskinesia)
  • paresthesia

Miscellaneous

  • allergic reactions
  • flu-like syndrome
  • ↑ fall risk
  • fever

Interactions

Drug-Drug interaction

Ciprofloxacin and other inhibitors of the CYP1A2 enzyme ↑ rasagiline levels; dose adjustment is recommended.Meperidine has resulted in life-threatening reactions when used with other MAO inhibitors; wait at least 14 days after discontinuation of rasagiline to initiate meperidine.Similar reactions may occur with tramadol, methadone ; concurrent use should be avoided.Concurrent use with dextromethorphan may result in psychosis/bizarre behavior and should be avoided.↑ risk of adverse reactions with mirtazapine and cyclobenzapine ; concurrent use should be avoided.Hypertensive crisis may occur with sympathomimetic amines including amphetamines, cold products, and some weight loss products containing vasoconstrictors such as pseudoephedrine, phenylephrine, or ephedrine ; avoid concurrent use.↑ risk of serotonin syndrome with tricyclic antidepressants, SSRI antidepressants, SNRI antidepressants, and other MAO inhibitors ; rasagiline should be discontinued ≥14 days prior to initiation of antidepressants (fluoxetine should be discontinued ≥5 wk prior to rasagiline therapy).Hypertensive crisis may also occur when rasagiline is used with other MAO inhibitors ; allow at least 14 days between usage.Risk of toxicity is ↑ with St. John's wort.Ingestion of foods containing high amounts of tyramine (>150 mg) (e.g., cheese) may result in life-threatening hypertensive crisis.

Route/Dosage

Oral (Adults) Monotherapy—1 mg daily; adjunct therapy—0.5 mg daily, may ↑ to 1 mg daily; concurrent ciprofloxacin or other CYP1A2 inhibitors—0.5 mg daily.

Hepatic Impairment

Oral (Adults) Mild hepatic impairment—0.5 mg daily.

Availability (generic available)

Tablets: 0.5 mg, 1 mg

Nursing implications

Nursing assessment

  • Assess signs and symptoms of Parkinson's disease (tremor, muscle weakness and rigidity, ataxic gait) prior to and 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).
  • Lab Test Considerations: May cause albuminuria, leukopenia, and abnormal liver function tests.
  • 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.

Potential Nursing Diagnoses

Impaired physical mobility (Indications)
Risk for injury (Indications,  Side Effects)

Implementation

  • Do not confuse Azilect (rasagiline) with Aricept (donepezil).
  • If used in combination with levodopa, a reduction in levodopa dose may be considered based on individual results.
  • Oral: 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 ) 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, rapacuronium, 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 or increased gambling, sexual, or other intense urges occur.
  • Advise patient to notify health care professional immediately if severe headache, neck stiffness, heart racing, or palpitations, occur.
  • Advise female patients to notify health care professionals if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Improvement in symptoms of Parkinson's disease, allowing increase in function.

Azilect

a trademark for rasagiline.
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