rasagiline


Also found in: Wikipedia.

rasagiline

Pharmacologic class: MAO inhibitor (type B)

Therapeutic class: Antiparkinsonian agent, antidyskinetic

Pregnancy risk category C

Action

Unknown. Thought to increase dopaminergic activity by irreversibly inhibiting MAO type B in nerve cells, increasing dopamine availability to brain cells

Availability

Tablets: 0.5 mg, 1 mg

Indications and dosages

Initial monotherapy for idiopathic Parkinson's disease

Adults: 1 mg P.O. daily

Adjunctive treatment of idiopathic Parkinson's disease in patients receiving levodopa

Adults: 0.5 mg P.O. once daily. If patient doesn't achieve sufficient clinical response, dosage may be increased to 1 mg P.O. once daily.

Dosage adjustment

• Mild hepatic impairment
• Concurrent use of ciprofloxacin and other CYP1A2 inhibitors

Contraindications

• Within 14 days of other MAO inhibitors or meperidine
• Concurrent use with cyclobenzaprine, dextromethorphan, methadone, propoxyphene, tramadol, and St. John's wort

Precautions

Use cautiously in:
• mild hepatic impairment (use not recommended in moderate or severe hepatic impairment), melanoma
• concurrent use of levodopa, antidepressants, or CYP1A2 inhibitors (such as ciprofloxacin)
• pregnant or breastfeeding patients
• children (safety and efficacy not established).

Administration

• Give with or without food.

Don't give tyramine-rich foods, beverages, dietary supplements, or over-the-counter (OTC) cough or cold medications during therapy because of possible hypertensive crisis.

Don't give within 14 days of other MAO inhibitors, meperidine, cyclobenzaprine, dextromethorphan, methadone, propoxyphene, tramadol, or St. John's wort.

Adverse reactions

CNS: headache, vertigo, dizziness, agitation, anxiety, somnolence, amnesia, confusion, dystonia, hypertonia, abnormal gait, ataxia, dyskinesia, hyperkinesia, paresthesia, neuropathy, tremor, depression, malaise, abnormal dreams, asthenia, myasthenia, hallucinations, stroke

CV: orthostatic hypotension, syncope, angina, bundle-branch block

EENT: conjunctivitis, epistaxis, rhinitis

GI: abdominal pain, dyspepsia, indigestion, nausea, vomiting, diarrhea, constipation, dysphagia, gastroenteritis, dry mouth, gingivitis, anorexia, GI hemorrhage

GU: hematuria, urinary incontinence, erectile dysfunction, decreased libido

Hematologic: leukopenia, anemia, hemorrhage

Musculoskeletal: arthralgia, arthritis, neck pain, tenosynovitis, bursitis, leg cramps

Respiratory: asthma, dyspnea, increased cough

Skin: alopecia, skin cancer, rash, sweating, pruritus, skin ulcer, ecchymosis, photosensitivity reaction

Other: falls, accidental injury, flulike syndrome, chest pain, fever, infection, hernia, weight loss, allergic reaction

Interactions

Drug-drug.Antidepressants (selective serotonin reuptake inhibitors, tricyclic and tetracyclic antidepressants): severe CNS toxicity, high fever, possible death

Carbidopa-levodopa, levodopa: increased incidence of dyskinesia, hallucinations, and orthostatic hypotension

CYP1A2 inhibitors (including ciprofloxacin): increased rasagiline blood level and possible increased adverse reactions

Dextromethorphan: bizarre behavior

Meperidine, methadone, propoxyphene, tramadol: increased risk of serious and possibly fatal reactions

Other MAO inhibitors, vitamin supplements containing tyramine: increased risk of hypertensive crisis

Sympathomimetics (including amphetamines, cold remedies, nasal decongestants, and weight-loss preparations containing vasoconstrictors): severe hypertensive reactions

Drug-diagnostic tests.Albumin: increased value

Drug-food.Tyramine-containing foods (aged, dried, fermented meats; pickled fish; improperly stored meats and fish; broad bean pods; aged cheeses; unpasteurized beers; red wines; concentrated yeast extracts; sauerkraut; soybean products): increased risk of hypertensive crisis

Drug-herbs.St. John's wort: bizarre behavior

Drug-behaviors.Alcohol use: hypertensive crisis

Patient monitoring

Stay alert for hypertensive crisis in patients using concurrent drugs that may cause this serious interaction.
• Be alert for dopaminergic adverse effects and exacerbation of preexisting dyskinesias when rasagiline is used as adjunct to levodopa. Levodopa dosage may need to be reduced.
• Monitor for orthostatic hypotension during first 2 months of therapy, especially when drug is used as adjunct to levodopa.
• Inspect patient frequently for signs of melanoma.
• In patient with hepatic insufficiency, obtain periodic liver function tests.

Patient teaching

• Tell patient he may take drug with or without food.

Stress importance of avoiding alcohol and certain foods, beverages, prescription drugs, and OTC preparations during therapy and for 14 days afterward. Ask pharmacist to give patient complete list of foods, beverages, and medications to avoid.
• Instruct patient to avoid using herbs during therapy unless prescriber approves.

Instruct patient or caregiver to immediately report occipital headache, confusion, palpitations, stiff neck, unexplained nausea or vomiting, sweating, dilated pupils, and visual disturbances (indications of hypertensive crisis).

Instruct patient to immediately report skin changes.
• Tell patient drug may cause blood pressure to drop if he stands or sits up suddenly. Advise him to rise slowly and carefully.
• Instruct patient to report hallucinations promptly.
• Caution patient to avoid hazardous activities until he knows how drug affects concentration and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.

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.

rasagiline

an antiparkinson agent.
indications This drug is used alone or with levodopa to treat idiopathic Parkinson's disease.
contraindications Lactation, pheochromocytoma, and known hypersensitivity to this drug or monoamine oxidase inhibitors prohibit its use.
adverse effects Adverse effects of this drug include drowsiness, hallucinations, depression, headache, malaise, paresthesia, vertigo, syncope, angina, orthostatic hypotension, diarrhea, dry mouth, dyspepsia, impotence, decreased libido, conjunctivitis, fever, flu syndrome, neck pain, allergic reaction, alopecia, arthralgia, arthritis, dyskinesia, and rhinitis. A life-threatening side effect is hypertensive crisis (after ingestion of tyramine products).
Mentioned in ?
References in periodicals archive ?
Contract notice: Supply of rasagiline 1 mg tablets.
Monoamine oxidase-B inhibitors: Selegiline, Rasagiline.
Two studies reviewed modafinil (Provigil) as a pharmacological intervention, and one study utilized rasagiline (Azilect) as an intervention.
A Turkish woman,42, after being diagnosed with onset of Parkinson was on the drug rasagiline, which is known to increase dopamine level in the brain.
MOA-B inhibitors: Selegiline and rasagiline can be used on their own in early PD to prolong the activity of naturally occurring dopamine in the CNS.
Monoamine oxidase B (MAO-B) inhibitors, such as seliginine and rasagiline, may be used to slow down the breakdown of dopamine at the synapse.
Rasagiline, an MAO inhibitor, improves parkinsonian symptoms, and its potential role in slowing the progression of the degenerative process is being investigated.
Rasagiline appears to slow the progression of Parkinson's disease, not just ameliorate its symptoms in the short term, according to a report in the New England Journal of Medicine.
London, Sept 24 (ANI): Scientists from Mount Sinai School of Medicine have found that drug rasagiline not only helps treat the symptoms of Parkinson's Disease, but also slows the rate of disease progression.
Rasagiline may also be utilized in combination with lev-odopa in patients with moderate or advanced PD, starting at 0.
25mg 1X Dizziness, nausea, pain, Orally daily headache, insomnia, disintegrating rhinitis, dyskinesias, tablet back pain, stomatitis, (Zelapar [R]) dyspepsia Rasagiline 0.