Rasagiline

What is Rasagiline?

• Rasagiline (Azilect), a monoamine oxidase (MAO)-B inhibitor (MAOI) used for the treatment of Parkinson’s disease.

Rasagiline skeletal

Rasagiline-3D-balls-A

What are the uses of this medicine?

• Rasagiline (Azilect) used as a monotherapy to treat symptoms in early Parkinson's disease or as an adjunct therapy in more advanced cases.

How does this medicine work?

• Rasagiline (ra sa' ji leen) is a specific inhibitor of monamine oxidase (MAO) type B which is a major enzyme in the pathway of dopamine and levodopa metabolism.
• As a result, rasagiline results in an increase in the bioavailability of levodopa enhancing and increasing the duration of its effects in Parkinson disease.

Who Should Not Use this medicine ?

This medicine cannot be used with:

• meperidine, tramadol, methadone, propoxyphene dextromethorphan, St. John’s wort, cyclobenzaprine, or another (selective or non-selective) MAO inhibitor.

What drug interactions can this medicine cause?

• Serious, sometimes fatal reactions have been precipitated with concomitant use of meperidine (e.g., Demerol and other tradenames) and MAO inhibitors including selective MAO-B inhibitors.
• Dextromethorphan is contraindicated for use with AZILECT.
• AZILECT is contraindicated for use with other MAO inhibitors.
• Severe hypertension has been reported in patients taking the recommended dose of AZILECT and ophthalmic drops containing sympathomimetic medications. Caution should be exercised when concomitantly using recommended doses of AZILECT with any sympathomimetic medications including nasal, oral, and ophthalmic decongestants and cold remedies.
• Concomitant use of AZILECT with one of many classes of antidepressants (e.g., SSRIs, SNRIs, triazolopyridine, tricyclic, or tetracyclic antidepressants) is not recommended.
• Patients taking concomitant ciprofloxacin or other CYP1A2 inhibitors should not exceed a dose of AZILECT 0.5 mg once daily.
• Patients should be advised to avoid foods (e.g., from fermented cheese, herring, over-the-counter cough/cold medications) containing a very large amount of tyramine while taking recommended doses of AZILECT.

Is this medicine FDA approved?

• Rasagiline was approved for use in the United States in 2007, the second MAO-B inhibitor approved for use in the therapy of Parkinson disease, and is currently approved for use monotherapy or as an adjunct to levodopa therapy.

How should this medicine be used?

Recommended dosage:

• Monotherapy: AZILECT 1 mg once daily.
• As adjunct without levodopa: AZILECT 1 mg once daily.
• As adjunct to levodopa: AZILECT 0.5 mg once daily. Increase dose to 1 mg daily as needed for sufficient clinical response.
• Patients taking ciprofloxacin or other CYP1A2 inhibitors: AZILECT 0.5 mg once daily.
• Patients with mild hepatic impairment: AZILECT 0.5 mg once daily. AZILECT should not be used in patients with moderate or severe hepatic impairment.

Administration:

• AZILECT must be administered orally once daily.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 0.5 mg tablets
• 1 mg tablets

This medicine is available in fallowing brand namesː

• AZILECT

What side effects can this medication cause?

The most common side effects of this medicine include:

• When AZILECT used as monotherapy: flu syndrome, arthralgia, depression, dyspepsia.
• When AZILECT used as adjunct without levodopa: peripheral edema, fall, arthralgia, cough, and insomnia.
• when AZILECT used as adjunct to levodopa: dyskinesia, accidental injury, weight loss, postural hypotension, vomiting, anorexia, arthralgia, abdominal pain, nausea, constipation, dry mouth, rash, abnormal dreams, fall, and tenosynovitis.

What special precautions should I follow?

• Exacerbation of hypertension may occur during treatment with AZILECT. Monitor patients for new onset hypertension or hypertension that is not adequately controlled after starting AZILECT.
• Serotonin syndrome has been reported with concomitant use of an antidepressant. Serotonin syndrome has also been reported with concomitant use of AZILECT with meperidine, tramadol, methadone, or propoxyphene. AZILECT is contraindicated for use with meperidine, tramadol, methadone, propoxyphene, and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors.
• It has been reported that falling asleep while engaged in activities of daily living always occurs in a setting of preexisting somnolence, although patients may not give such a history. Avoid driving and other potentially dangerous activities.
• Rasagiline plasma concentration may increase in patients with hepatic impairment. AZILECT should not be used in patients with moderate or severe hepatic impairment.
• AZILECT may cause hypotension, especially orthostatic.
• When used as an adjunct to levodopa, AZILECT may cause dyskinesia. Decreasing the dose of levodopa may mitigate this side effect.
• Hallucinations reported as an adverse event was in patients treated with AZILECT. Consider dose reduction or stopping the medication if a patient develops hallucinations or psychotic like behaviors while taking AZILECT.
• Intense urges to gamble, increased sexual urges, intense urges to spend money, binge eating, and/or other intense urges, and the inability to control these urges while taking one or more of the medications, including AZILECT. Consider dose reduction or stopping the medication if a patient develops such urges while taking AZILECT.
• A symptom complex resembling neuroleptic malignant syndrome (characterized by elevated temperature, muscular rigidity, altered consciousness, and autonomic instability), with no other obvious etiology, has been reported in association with rapid dose reduction, withdrawal of, or changes in drugs.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Signs and symptoms of MAOI overdose may include: drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucinations, trismus, opisthotonos, convulsions, and coma; rapid and irregular pulse, hypertension, hypotension and vascular collapse; precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis, and cool, clammy skin.

Management of overdosage:

• There is no specific antidote for AZILECT overdose.
• The following suggestions are offered based upon the assumption that AZILECT overdose may be modeled after nonselective MAO inhibitor poisoning.
• Treatment of overdose with nonselective MAO inhibitors is symptomatic and supportive.
• Respiration should be supported by appropriate measures, including management of the airway, use of supplemental oxygen, and mechanical ventilatory assistance, as required.
• Body temperature should be monitored closely.
• Intensive management of hyperpyrexia may be required.
• Maintenance of fluid and electrolyte balance is essential.
• For this reason, in cases of overdose with AZILECT, dietary tyramine restriction should be observed for several weeks to reduce the risk of hypertensive tyramine reaction.

Can this medicine be used in pregnancy?

• There are no adequate data on the developmental risks associated with the use of AZILECT in pregnant women.

Can this medicine be used in children?

• The safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active Ingredient:

• RASAGILINE MESYLATE

Inactive ingredients:

• MANNITOL
• STARCH, CORN
• SILICON DIOXIDE
• STEARIC ACID
• TALC

Who manufactures and distributes this medicine?

Distributed by: Teva Pharmaceuticals USA, Inc., Parsippany, NJ

What should I know about storage and disposal of this medication?

• Store at 25°C (77°F) with excursions permitted to 15°-30°C (59°-86°F).

• Dailymed label info on Rasagiline
• FDA Rasagiline

Rasagiline Resources
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