RASAGILINE

RASAGILINE
(ras-a-gi'leen)
Azilect
Classifications: monoamine oxidase inhibitor; antiparkinson agent;
Therapeutic:antiparkinson agent

Prototype: Levodopa
Pregnancy Category: C

Availability

0.5 mg, 1 mg tablets

Action

Rasagiline is a potent monoamine oxidase B inhibitor (MAOI-B) that prevents the enzyme monoamine oxidase B from breaking down dopamine in the brain. Rasagiline also interferes with dopamine reuptake at synapses in the brain.

Therapeutic Effect

Rasagiline helps to overcome dopaminergic motor dysfunction in Parkinson's disease.

Uses

Treatment of Parkinson's disease, either as monotherapy or as an adjunct to levodopa.

Contraindications

Moderate to severe hepatic impairment; alcoholism; biliary cirrhosis; cardiac arrhythmias, cardiac disease, CHF, angina, acute MI; migraine headaches, increased intracranial pressure, cerebrovascular disease, intracranial bleeding, recent head trauma, stroke; hypertension, concurrent use of antihypertensive drugs; concurrent use of MAOI therapy; pregnancy (category C); elective surgery; children.

Cautious Use

Mild hepatic dysfunction; concurrent anticholingeric drugs or CNS depressant drugs; diabetes mellitus; asthma, bronchitis, hyperthyroidism; postural or orthostatic hypotension; moderate to severe renal impairment, anuria; epilepsy or preexisting seizure disorders; lactation.

Route & Dosage

Parkinson's Disease
Adult: PO 1 mg/d as monotherapy; 0.5–1 mg/d if adjunctive therapy

Hepatic Impairment
Mild Impairment: 0.5 mg/d

Administration

Oral
  • May be given without regard to food.
  • Store at 15–30° C (59–86° F).

Adverse Effects (≥1%)

Body as a Whole: Accidental injury, allergic reaction, alopecia, gingivitis, hernia, infection, neck pain, pruritus. CNS: Abnormal dreams, abnormal gait, amnesia, anxiety, asthenia, ataxia, confusion, depression, dizziness, dyskinesia, dystonia, fall, fever, flu syndrome, hallucinations, headache, hyperkinesias, hypertonia, malaise, neuropathy, neck pain, paresthesia, somnolence, syncope, tremor, vertigo. CV: Angina pectoris, bundle branch block, cerebrovascular accident, chest pain, postural hypotension. GI: Abdominal pain, anorexia, constipation, diarrhea, dry mouth, dyspepsia, dysphagia, gastroenteritis, GI hemorrhage, nausea, vomiting. Hematologic: Anemia, hemorrhage. Metabolic: Abnormal liver function tests, albuminuria, weight loss. Musculoskeletal: Arthralgia, arthritis, bursitis, leg cramps, myasthenia, tenosynovitis. Respiratory: Asthma, dyspnea, epistaxis, increased cough, rhinitis. Skin: Ecchymosis, eczema, skin carcinoma, skin ulcer, sweating, urticaria, vesiculobullous rash. Special Senses: Conjunctivitis. Urogenital: Decreased libido, hematuria, impotence, urinary incontinence.

Interactions

Drug: Inhibitors of CYP1A2 (e.g., atazanavir, ciprofloxacin, mexiletine, tacrine) may increase rasagiline plasma levels. Rasagiline increases the plasma levels of anesthetics; thus it must be discontinued 14 d prior to elective surgery. Rasagiline can cause severe CNS toxicity, including hyperpyrexia and death, with antidepressants, selective serotonin reuptake inhibitors (ssri), serotonin-norepinephrine reuptake inhibitors (snri), nonselective mao inhibitors, or selective mao-b inhibitors. Rasagiline can increase the plasma levels of cyclobenzaprine and sympathomimetic amines. Rasagiline and dextromethorphan can cause brief episodes of psychosis and bizarre behavior. Rasagiline can potentiate the dopaminergic effects of levodopa. Rasagiline can increase the plasma levels of meperidine, methadone, propoxyphene, and tramadol, resulting in coma, severe hypertension or hypotension, severe respiratory depression, convulsions, and death. Herbal: Rasagiline increases the plasma levels of St. John's wort.

Pharmacokinetics

Absorption: Rapidly absorbed with 36% bioavailability. Peak: 1 h. Distribution: 88–94% protein bound. Metabolism: Extensive hepatic metabolism. Elimination: Primarily renal (62%) with minor fecal elimination. Half-Life: 3 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for and report S&S of dopaminergic side effects (e.g., dyskinesia, hallucinations, etc.) with concurrent levodopa.
  • Monitor for and report suspicious skin changes suggestive of melanoma or other skin cancers.
  • Lab tests: Baseline and periodic LTFs; periodic renal function tests, CBC with Hct & Hgb.
  • Note all contraindicated drugs and drug groups and exercise caution not to administer a contraindicated substance.
  • Note all drug interactions and monitor for the indicated effects.

Patient & Family Education

  • Do not take any prescription or nonprescription drug without consulting physician.
  • Periodic skin examinations should be scheduled with a dermatologist. If you notice changes in a skin mole or new skin lesion, contact the dermatologist.
  • Avoid foods and beverages containing tyramine (e.g., aged cheeses and meats, tap beer, red wine, soybean products).
  • Make position changes slowly, especially when standing from a lying or sitting position.
  • Do not drive or engage in potentially hazardous activities until response to drug is known.
  • Report immediately any of the following to a health care provider: palpitations, severe headache, blurred vision, difficulty thinking, seizures, chest pain, unexplained nausea or vomiting, or any sudden weakness or paralysis.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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