Trade Names:Azilect- Tablets 0.5 mg- Tablets 1 mg
Irreversible MAOI suspected to increase extracellular levels of dopamine. Although rasagiline inhibits MAO type B, studies are inadequate to determine whether the drug is selective for MAO type B.
Rapidly absorbed, reaching C max in approximately 1 h. Bioavailability is about 36%.
Vd at steady state is 87 L, indicating tissue binding exceeds plasma protein binding. Plasma protein binding ranges from 88% to 94%.
Almost complete metabolism in the liver by N-dealkylation and/or hydroxylation prior to excretion.
Steady state t ½ is 3 h. Primarily eliminated in the urine (62%) and secondarily in the feces (7%) over 7 days.
Data are inclusive; however, because unconjugated rasagiline is not excreted by the kidney, usual doses can be given to patients with mild renal function impairment.Hepatic Function Impairment
In patients with mild hepatic function impairment, AUC and C max are increased 2- and 1.4-fold, respectively. In patients with moderate hepatic function impairment, the AUC and C max are increased 7- and 2-fold, respectively.
Treatment of signs and symptoms of idiopathic Parkinson disease.
Patients receiving local and general anesthesia, cocaine, cyclobenzaprine, dextromethorphan, meperidine and other analgesics (eg, methadone, propoxyphene, tramadol), mirtazapine, other MAOIs, St. John's wort, sympathomimetic amines (eg, ephedrine, pseudoephedrine); patients with pheochromocytoma.
PO Monotherapy: 1 mg/day. Adjunctive therapy: 0.5 mg/day initially; increase dose to 1 mg/day if clinical response is not sufficient.Hepatic Function ImpairmentAdults
PO 0.5 mg/day (mild hepatic function impairment). Do not use rasagiline in patients with moderate or severe hepatic function impairment.CYP1A2 Inhibitors (eg, Ciprofloxacin)Adults
PO 0.5 mg/day.
Store at 59° to 86°F.
May be associated with hypertensive crisis requiring immediate treatment and possible hospitalization.Analgesics (eg, methadone, propoxyphene, tramadol), anesthesia (eg, local and general anesthesia), cocaine, cyclobenzaprine, mirtazapine, St. John's wort
Coadministration with rasagiline is contraindicated.Antidepressants (eg, SSRIs [eg, fluoxetine, fluvoxamine, paroxetine, sertraline], tricyclic antidepressants [eg, amitriptyline])
Serious, sometimes fatal, reactions with signs and symptoms including autonomic instability, coma, delirium, hyperthermia, myoclonus, and rigidity may occur.CYP1A2 inhibitors (eg, ciprofloxacin)
Rasagiline plasma concentrations may be elevated 2-fold, increasing the pharmacologic and adverse effects.Dextromethorphan
Contraindicated; episodes of psychosis and bizarre behavior have been reported; risk of hypotension, coma, and death may be increased.Levodopa
Dopaminergic adverse reactions and exacerbation of preexisting dyskinesia may be potentiated.Meperidine
Contraindicated; may increase risk of severe reactions, including apnea, coma, seizures, and death.Other MAOIs
Contraindicated; increased risk of nonselective MAO inhibition, leading to hypertensive crisis.Sympathomimetic amines (eg, dopamine, pseudoephedrine)
Risk of severe headache, hypertension, and hypertensive crisis may be increased.
None well documented.
Angina pectoris, bundle branch block, syncope (at least 1%).
Headache (14%); depression (5%); malaise, paresthesia, vertigo (2%); hallucinations (1%); abnormal gait, anxiety, asthenia, decreased libido, dizziness, hallucinations, hyperkinesia, hypertonia, neuropathy, tremor (at least 1%).
Alopecia, skin carcinoma, vesiculobullous rash (at least 1%).
Conjunctivitis, rhinitis (3%).
Dyspepsia (7%); gastroenteritis (3%); anorexia, diarrhea, GI hemorrhage, vomiting (at least 1%).
Albuminuria, hematuria, impotence, urinary incontinence (at least 1%).
Ecchymosis (2%); leukopenia (at least 1%).
Abnormal LFTs (at least 1%).
Arthralgia (7%); arthritis, neck pain (2%).
Asthma, increased cough (at least 1%).
Falling, flu syndrome (5%); fever (3%); allergic reaction, chest pain (at least 1%).
Periodic skin examinations for melanomas.
Category C .
Safety and efficacy not established.
Associated with ingestion of tyramine-rich foods, beverages, or dietary supplements or amines; may be fatal. Consists of marked systemic blood pressure elevation; requires immediate attention/hospitalization.
Risk of melanoma may be increased, although it is unclear if the increased risk is due to rasagiline or Parkinson disease.
Occurs most frequently in the first 2 months of treatment.
Based on overdosage with other MAOIs, signs and symptoms of overdosage may include agitation, coma, convulsions, cool and clammy skin, death, diaphoresis, dizziness, drowsiness, faintness, hallucinations, hyperactivity, hyperpyrexia, hypertension, hypotension, irritability, opisthotonos, precordial pain, rapid and irregular pulse, respiratory depression and failure, severe headache, trismus, vascular collapse.
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