rasagiline(redirected from Rasagiline mesylate)
Pharmacologic class: MAO inhibitor (type B)
Therapeutic class: Antiparkinsonian agent, antidyskinetic
Pregnancy risk category C
Unknown. Thought to increase dopaminergic activity by irreversibly inhibiting MAO type B in nerve cells, increasing dopamine availability to brain cells
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.
• Mild hepatic impairment
• Concurrent use of ciprofloxacin and other CYP1A2 inhibitors
• Within 14 days of other MAO inhibitors or meperidine
• Concurrent use with cyclobenzaprine, dextromethorphan, methadone, propoxyphene, tramadol, and St. John's wort
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).
• 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.
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
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
☞ 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.
• 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.
ClassificationTherapeutic: antiparkinson agents
Pharmacologic: monoamine oxidase type b inhibitors
|PO||rapid||1 hr||40 days*|
Adverse Reactions/Side Effects
Central nervous system
Ear, Eye, Nose, Throat
- ↑ BP
- chest pain
- postural hypotension (may ↑ levodopa-induced hypotension)
- ↓ libido
- ↑ melanoma risk
- weight loss
- neck pain
- dyskinesia (may ↑ levodopa-induced dyskinesia)
- allergic reactions
- flu-like syndrome
- ↑ fall risk
Drug-Drug interactionCiprofloxacin 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.
Hepatic ImpairmentOral (Adults) Mild hepatic impairment—0.5 mg daily.
Availability (generic available)
- 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 DiagnosesImpaired physical mobility (Indications)
Risk for injury (Indications, Side Effects)
- 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.
- 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.
- Improvement in symptoms of Parkinson's disease, allowing increase in function.