Classifications: monoamine oxidase inhibitor; antiparkinson agent; Therapeutic:antiparkinson agent
Pregnancy Category: C
0.5 mg, 1 mg tablets
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.
Rasagiline helps to overcome dopaminergic motor dysfunction in Parkinson's disease.
Treatment of Parkinson's disease, either as monotherapy or as an adjunct to levodopa.
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.
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
Adult: PO 1 mg/d as monotherapy; 0.51 mg/d if adjunctive therapy
Mild Impairment: 0.5 mg/d
- May be given without regard to food.
- Store at 1530° C (5986° 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,
fever, flu syndrome
, hallucinations, headache,
hyperkinesias, hypertonia, malaise
, neck pain, paresthesia
, somnolence, syncope, tremor, vertigo. CV:
Angina pectoris, bundle branch block, cerebrovascular accident,
chest pain, postural hypotension. GI:
Abdominal pain, anorexia, constipation
, dry mouth, dyspepsia, dysphagia, gastroenteritis, GI hemorrhage, nausea,
vomiting. Hematologic: Anemia
, hemorrhage. Metabolic:
Abnormal liver function tests, albuminuria, weight loss. Musculoskeletal: Arthralgia
, bursitis, leg cramps, myasthenia, tenosynovitis. Respiratory: Asthma
, epistaxis, increased cough, rhinitis. Skin:
, skin carcinoma, skin ulcer, sweating, urticaria, vesiculobullous rash. Special Senses: Conjunctivitis
Decreased libido, hematuria, impotence, urinary incontinence.
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,
resulting in coma, severe hypertension or hypotension, severe respiratory depression
, convulsions, and death. Herbal:
Rasagiline increases the plasma
levels of St. John's wort.
Rapidly absorbed with 36% bioavailability. Peak:
1 h. Distribution:
8894% protein bound. Metabolism:
Extensive hepatic metabolism
(62%) with minor fecal elimination. Half-Life:
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.