Rasagiline

Trade Names:
Azilect
- Tablets 0.5 mg
- Tablets 1 mg

Pharmacology

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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.

Pharmacokinetics

Absorption

Rapidly absorbed, reaching C _max in approximately 1 h. Bioavailability is about 36%.

Distribution

Vd at steady state is 87 L, indicating tissue binding exceeds plasma protein binding. Plasma protein binding ranges from 88% to 94%.

Metabolism

Almost complete metabolism in the liver by N-dealkylation and/or hydroxylation prior to excretion.

Elimination

Steady state t _½ is 3 h. Primarily eliminated in the urine (62%) and secondarily in the feces (7%) over 7 days.

Special Populations

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.

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.

Indications and Usage

Treatment of signs and symptoms of idiopathic Parkinson disease.

Contraindications

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.

Dosage and Administration

PO Monotherapy: 1 mg/day. Adjunctive therapy: 0.5 mg/day initially; increase dose to 1 mg/day if clinical response is not sufficient.

PO 0.5 mg/day (mild hepatic function impairment). Do not use rasagiline in patients with moderate or severe hepatic function impairment.

PO 0.5 mg/day.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

May be associated with hypertensive crisis requiring immediate treatment and possible hospitalization.

Coadministration with rasagiline is contraindicated.

Serious, sometimes fatal, reactions with signs and symptoms including autonomic instability, coma, delirium, hyperthermia, myoclonus, and rigidity may occur.

Rasagiline plasma concentrations may be elevated 2-fold, increasing the pharmacologic and adverse effects.

Contraindicated; episodes of psychosis and bizarre behavior have been reported; risk of hypotension, coma, and death may be increased.

Dopaminergic adverse reactions and exacerbation of preexisting dyskinesia may be potentiated.

Contraindicated; may increase risk of severe reactions, including apnea, coma, seizures, and death.

Contraindicated; increased risk of nonselective MAO inhibition, leading to hypertensive crisis.

Risk of severe headache, hypertension, and hypertensive crisis may be increased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Angina pectoris, bundle branch block, syncope (at least 1%).

CNS

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%).

Dermatologic

Alopecia, skin carcinoma, vesiculobullous rash (at least 1%).

EENT

Conjunctivitis, rhinitis (3%).

GI

Dyspepsia (7%); gastroenteritis (3%); anorexia, diarrhea, GI hemorrhage, vomiting (at least 1%).

Genitourinary

Albuminuria, hematuria, impotence, urinary incontinence (at least 1%).

Hematologic-Lymphatic

Ecchymosis (2%); leukopenia (at least 1%).

Hepatic

Abnormal LFTs (at least 1%).

Musculoskeletal

Arthralgia (7%); arthritis, neck pain (2%).

Respiratory

Asthma, increased cough (at least 1%).

Miscellaneous

Falling, flu syndrome (5%); fever (3%); allergic reaction, chest pain (at least 1%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hypertensive crisis

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.

Melanoma

Risk of melanoma may be increased, although it is unclear if the increased risk is due to rasagiline or Parkinson disease.

Postural hypotension

Occurs most frequently in the first 2 months of treatment.

Overdosage

Symptoms

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.

Patient Information

• Advise patients about the tyramine content of foods and beverages and to avoid these items.
• Instruct patients about the signs and symptoms of marked BP elevation that could represent a hypertensive emergency.
• Instruct patient to immediately contact health care provider if severe headache or other atypical or unusual symptoms that could be caused by hypertensive crisis occurs.
• Advise patients to take the medication as prescribed.
• Advise patients that if a dose is missed to take the next dose at the usual time on the following day.

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