rasagiline

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).

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rasagiline

Azilect

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

• Pheochromocytoma
• Within 14 days of other MAO inhibitors or meperidine
• Concurrent use with cyclobenzaprine; dextromethorphan; methadone; mirtazapine; propoxyphene; tramadol; or sympathomimetic amines, including amphetamines, cold products, and anorexiants that contain vasoconstrictors (such as pseudoephedrine, phenylephrine, phenylpropanolamine, ephedrine); 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, cyclobenzaprine, dextromethorphan, meperidine, methadone, mirtazapine, propoxyphene, tramadol, sympathomimetic amines (including amphetamines, cold products, and anorexiants that contain vasoconstrictors, such as pseudoephedrine, phenylephrine, phenylpropanolamine, ephedrine), or St. John's wort.

Route	Onset	Peak	Duration
P.O.	Unknown	1 hr	Unknown

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.
• Advise patient to discontinue drug at least 10 days before elective surgery, as instructed.
☞ 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.