ra-ZA-ji-leen

• Parkinson's disease.

• 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.

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

Absorption: 36% absorbed following oral administration.

Distribution: Readily crosses the blood-brain barrier.

Metabolism/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.

Contraindicated in:

• Hypersensitivity
• Concurrent meperidine, tramadol, methadone, sympathomimetic amines, dextromethorphan, mirtazapine, cyclobenzaprine, cocaine, St. John's wort, or 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)
• OB: Safety not established
• Lactation: Use during breast feeding only if benefit to patient outweighs potential risk to infant
• Pedi: Safety and effectiveness not established.

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

Derm: alopecia, ecchymosis, ↑melanoma risk, rash.

EENT: conjunctivitis, rhinitis.

Endo: weight loss.

GI: anorexia, dizziness, dyspepsia, gastroenteritis, vomiting.

GU: albuminuria, ↓ libido.

Hemat: leukopenia.

MS: arthralgia, arthritis, neck pain.

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

Resp: asthma.

Misc: fever, flu-like syndrome, ↑ fall risk.

Drug-Drug:

• Concurrent use of meperidine, tramadol, methadone, or other MAO inhibitors may ↑ risk of serotonin syndrome; concurrent use contraindicated.
• Ciprofloxacin and other inhibitors of the CYP1A2 enzyme↑ rasagiline levels; dose adjustment is recommended.
• 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, 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:

• Risk of toxicity is ↑ with St. John's wort.

Drug-Food:

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

• 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 ciprofloxacin or other CYP1A2 inhibitors — 0.5 mg once daily.

• 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.
• PO: Administer once daily.

Azilect

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: monoamine oxidase type b inhibitors

(Generic available)

• Tablets: 0.5 mg; 1 mg;

*Recovery of MAO-B function.

• 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).

• 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.

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

• 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 Appendix M) 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 skin lesions, agitation, aggression, delirium, hallucinations, sleep driving or 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.

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

NDC Code^*

• 0093- Teva Pharmaceuticals USA, Inc.
  • 0093-3060- Rasagiline
    • 0093-3060-56- 30 TABLET in 1 BOTTLE (0093-3060-56)

• 0093- Teva Pharmaceuticals USA, Inc.
  • 0093-3061- Rasagiline
    • 0093-3061-56- 30 TABLET in 1 BOTTLE (0093-3061-56)

• 0378- Mylan Pharmaceuticals Inc.
  • 0378-1270- Rasagiline Mesylate
    • 0378-1270-93- 30 TABLET in 1 BOTTLE, PLASTIC (0378-1270-93)

• 0378- Mylan Pharmaceuticals Inc.
  • 0378-1271- Rasagiline Mesylate
    • 0378-1271-93- 30 TABLET in 1 BOTTLE, PLASTIC (0378-1271-93)

• 16714- NorthStar RxLLC
  • 16714-770- Rasagiline
    • 16714-770-01- 30 TABLET in 1 BOTTLE (16714-770-01)

• 16714- NorthStar RxLLC
  • 16714-771- Rasagiline
    • 16714-771-01- 30 TABLET in 1 BOTTLE (16714-771-01)

• 42571- Micro Labs Limited
  • 42571-220- RASAGILINE
    • 42571-220-05- 500 TABLET in 1 BOTTLE (42571-220-05)

• 42571- Micro Labs Limited
  • 42571-220- RASAGILINE
    • 42571-220-10- 1000 TABLET in 1 BOTTLE (42571-220-10)

• 42571- Micro Labs Limited
  • 42571-220- RASAGILINE
    • 42571-220-30- 30 TABLET in 1 BOTTLE (42571-220-30)

• 42571- Micro Labs Limited
  • 42571-221- RASAGILINE
    • 42571-221-05- 500 TABLET in 1 BOTTLE (42571-221-05)

• 42571- Micro Labs Limited
  • 42571-221- RASAGILINE
    • 42571-221-10- 1000 TABLET in 1 BOTTLE (42571-221-10)

• 42571- Micro Labs Limited
  • 42571-221- RASAGILINE
    • 42571-221-30- 30 TABLET in 1 BOTTLE (42571-221-30)

• 43353- Aphena Pharma Solutions - Tennessee, LLC
  • 43353-015- Azilect
    • 43353-015-18- 3000 TABLET in 1 BOTTLE (43353-015-18)

• 47781- Alvogen, Inc.
  • 47781-138- Rasagiline Mesylate
    • 47781-138-30- 30 TABLET in 1 BOTTLE, PLASTIC (47781-138-30)

• 47781- Alvogen, Inc.
  • 47781-139- Rasagiline Mesylate
    • 47781-139-30- 30 TABLET in 1 BOTTLE, PLASTIC (47781-139-30)

• 47781- Alvogen, Inc.
  • 47781-683- Rasagiline
    • 47781-683-30- 30 TABLET in 1 BOTTLE, PLASTIC (47781-683-30)

• 47781- Alvogen, Inc.
  • 47781-690- Rasagiline
    • 47781-690-30- 30 TABLET in 1 BOTTLE, PLASTIC (47781-690-30)

• 67877- Ascend Laboratories, LLC
  • 67877-259- Rasagiline
    • 67877-259-30- 30 TABLET in 1 BOTTLE (67877-259-30)

• 67877- Ascend Laboratories, LLC
  • 67877-260- Rasagiline
    • 67877-260-30- 30 TABLET in 1 BOTTLE (67877-260-30)

• 68546- Teva Neuroscience, Inc.
  • 68546-142- Azilect
    • 68546-142-56- 30 TABLET in 1 BOTTLE (68546-142-56)

• 68546- Teva Neuroscience, Inc.
  • 68546-229- Azilect
    • 68546-229-56- 30 TABLET in 1 BOTTLE (68546-229-56)