Rasagiline

Reviewed on 6/21/2022

What Is Rasagiline and How Does It Work?

Rasagiline is a prescription medication used for the treatment of Parkinson's disease. 

  • Rasagiline is available under the following different brand names: Azilect

What Are Side Effects Associated with Using Rasagiline?

Common side effects of Rasagiline include:

  • depressed mood,
  • sleep problems (insomnia),
  • strange dreams,
  • involuntary muscle movements,
  • loss of appetite,
  • weight loss,
  • indigestion,
  • stomach pain,
  • nausea,
  • vomiting,
  • constipation,
  • joint pain or stiffness,
  • rash,
  • cough,
  • flu symptoms,
  • dry mouth, and
  • swelling in the hands or feet

Serious side effects of Rasagiline include:

  • hives,
  • difficulty breathing,
  • swelling of the face, lips, tongue, or throat,
  • severe headache,
  • blurred vision,
  • pounding in the neck or ears,
  • extreme drowsiness,
  • unusual changes in mood or behavior,
  • hallucinations,
  • lightheadedness,
  • worsening symptoms of Parkinson’s disease,
  • agitation,
  • hallucinations,
  • fever,
  • sweating,
  • shivering,
  • fast heart rate,
  • muscle stiffness,
  • twitching,
  • loss of coordination,
  • nausea,
  • vomiting, and
  • diarrhea

Rare side effects of Rasagiline include:

  • none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

QUESTION

Parkinson's disease is only seen in people of advanced age. See Answer

What Are Dosages of Rasagiline?

 Adult dosage

Tablet

  • 0.5 mg
  • 1 mg
  • Parkinson Disease
  • Adult dosage
  • Monotherapy: 1 mg orally every day
  • Adjunct without levodopa: 1 mg orally every day
  • Adjunct to levodopa: 0.5 mg orally every day  initially, may increase to 1 mg/day if needed and tolerated; consider reducing levodopa dose

Dosage Considerations – Should be Given as Follows

  • See “Dosages”

What Other Drugs Interact with Rasagiline?

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first

  • Rasagiline has severe interactions with at least 40 other drugs.
  • Rasagiline has serious interactions with at least 70 other drugs.
  • Rasagiline has moderate interactions with at least 64 other drugs.
  • Rasagiline has minor interactions with the following drug:

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

What Are Warnings and Precautions for Rasagiline?

Contraindications

  • Coadministration with meperidine, tramadol, methadone, and MAOIs, including other selective MAO-B inhibitors increases the risk of serotonin syndrome; at least 14 days should elapse between discontinuation of rasagiline and initiation of treatment with these medications
  • Coadministration with St. John’s wort and with cyclobenzaprine
  • Coadministration with dextromethorphan because of the risk of an episode of psychosis or bizarre behavior

Effects of drug abuse

  • None

Short-Term Effects

  • See “What Are Side Effects Associated with Using Rasagiline?”

Long-Term Effects

  • See “What Are Side Effects Associated with Using Rasagiline?”

Cautions

  • Rasagiline is a selective inhibitor of MAO-B at the recommended doses of 0.5 or 1 mg daily; selectivity for inhibiting MAO-B diminishes in a dose-related manner as the dose is progressively increased above the recommended daily doses
  • May exacerbate hypertension; antihypertensive drugs may require a dosage adjustment
  • May cause hypotension, especially orthostatic
  • May cause or exacerbate dyskinesia; decreasing the levodopa dose may lessen or eliminate this side effect
  • Withdrawal-emergent hyperpyrexia and confusion are reported with rapid dose reduction of drugs that increase central dopaminergic tone; this is characterized by elevated temperature, muscular rigidity, altered consciousness, and autonomic instability
  • Patients with Parkinson's disease have a higher risk (2 to 6-fold higher) of developing melanoma than the general population; unclear if this is due to the disease or other factors (eg, drug therapy); monitor for melanomas frequently and regularly

Psychiatric effects

  • Hallucinations and psychotic-like behavior reported
  • The abnormal thinking and behavior can consist of one or more of a variety of manifestations including paranoid ideation, delusions, hallucinations, confusion, psychotic-like behavior, disorientation, aggressive behavior, agitation, and delirium
  • Patients should be informed of the possibility of developing hallucinations and instructed to report them to their healthcare provider promptly should they develop
  • Patients with a major psychotic disorder should ordinarily not be treated because of the risk of exacerbating the psychosis with an increase in central dopaminergic tone; in addition, many treatments for psychosis that decrease central dopaminergic tone may decrease therapy effectiveness
  • Consider dose reduction or stopping the medication if a patient develops hallucinations or psychotic-like behaviors while taking the drug

Falling asleep and somnolence

  • Daytime drowsiness and somnolence were reported during activities of daily living
  • Prescribers should monitor patients for drowsiness or sleepiness because some of the events occur well after initiation of treatment with dopaminergic medication
  • Prescribers should also be aware that patients may not acknowledge drowsiness or sleepiness until directly questioned about drowsiness or sleepiness during specific activities
  • Although many patients have reported somnolence while on therapy with rasagiline and other dopaminergic medications, some perceived that they had no warning signs, such as excessive drowsiness, and believed that they were alert immediately before activities that resulted in accidents
  • Before initiating treatment, patients should be advised of the potential to develop drowsiness and specifically asked about factors that may increase risk with therapy such as concomitant sedating medications, presence of sleep disorders, and concomitant medications that increase rasagiline plasma levels (eg, ciprofloxacin)
  • If a patient develops significant daytime sleepiness or episodes of falling asleep during activities that require active participation (eg, driving a motor vehicle, conversations, eating), therapy should ordinarily be discontinued
  • If a decision is made to continue patients on therapy, advise them to avoid driving and other potentially dangerous activities; there is insufficient information to establish that dose reduction will eliminate episodes of falling asleep while engaged in activities of daily living

Tyramine

  • Dietary tyramine restriction is not required during treatment with recommended doses; however, certain foods may contain very high amounts (i.e., above 150 mg) of tyramine that could potentially cause severe hypertension, including various clinical syndromes referred to as hypertensive urgency, crisis, or emergency, in patients receiving therapy, even at recommended doses, due to increased sensitivity to tyramine
  • Patients should be advised to avoid foods containing a very large amount of tyramine while taking recommended doses of rasagiline because of the potential for large increases in blood pressure including clinical syndromes referred to as hypertensive urgency, crisis, or emergency
  • Serotonin syndrome
  • Serotonin syndrome has been reported with the concomitant use of an antidepressant (eg, selective serotonin reuptake inhibitors-SSRIs, serotonin-norepinephrine reuptake inhibitors-SNRIs, tricyclic antidepressants, tetracyclic antidepressants, triazolopyridine antidepressants) and a nonselective MAOI (e.g., phenelzine, tranylcypromine) or selective MAO-B inhibitors, such as selegiline and rasagiline
  • Serotonin syndrome has been reported with concomitant use of rasagiline with meperidine, tramadol, methadone, or propoxyphene; rasagiline is contraindicated for use with meperidine, tramadol, methadone, propoxyphene, and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors
  • In the postmarketing period, potentially life-threatening serotonin syndrome was reported in patients treated with antidepressants concomitantly with drug
  • Concomitant use with one of many classes of antidepressants (e.g., SSRIs, SNRIs, triazolopyridine, tricyclic or tetracyclic antidepressants) was not recommended [
  • The symptoms of serotonin syndrome have included behavioral and cognitive/mental status changes (e.g., confusion, hypomania, hallucinations, agitation, delirium, headache, and coma), autonomic effects (e.g., syncope, shivering, sweating, high fever/hyperthermia, hypertension, tachycardia, nausea, diarrhea), and somatic effects (e.g., muscular rigidity, myoclonus, muscle twitching, hyperreflexia manifested by clonus, and tremor)
  • At least 14 days should elapse between discontinuation of rasagiline and initiation of treatment with an SSRI, SNRI, tricyclic, tetracyclic, or triazolopyridine antidepressant
  • Because of long half-lives of certain antidepressants (e.g., fluoxetine and its active metabolite), at least five weeks (perhaps longer, especially if fluoxetine has been prescribed chronically and/or at higher doses) should elapse between discontinuation of fluoxetine and initiation of rasagiline
  • Compulsive behavior
  • Impulse control/compulsive behaviors reported; case reports describe patients with intense urges to gamble, increased sexual urges, intense urges to spend money, or binge eat, and the inability to control these urges while taking one or more of the medications that increase central dopaminergic tone and that are generally used for the treatment of Parkinson’s disease
  • In some cases, although not all, these urges were reported to have stopped when the dose was reduced or the medication was discontinued; because patients may not recognize these behaviors as abnormal, it is important for prescribers to specifically ask patients or their caregivers about the development of new or increased gambling urges, sexual urges, uncontrolled spending, or other urges while receiving therapy
  • Consider dose reduction or stopping the medication if a patient develops such urges while taking medication

Pregnancy & Lactation

  • There are no adequate data on developmental risks associated with use in pregnant women; in animal studies, oral administration to rats during gestation and lactation resulted in decreased survival and reduced body weight in offspring at doses similar to those used clinically; when administered to pregnant animals in combination with levodopa/carbidopa, there were increased incidences of fetal skeletal variations in rats and increases in embryofetal death and cardiovascular abnormalities in rabbits

Lactation

  • There are no data on the presence of the drug in human milk or its effects on the breastfed infant; in rats, rasagiline was shown to inhibit prolactin secretion; the clinical relevance in humans is unknown, and there are no data on the effects of rasagiline on prolactin secretion in humans

The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and potential adverse effects on the breastfed infant from drugs or an underlying maternal condition

SLIDESHOW

Dementia, Alzheimer's Disease, and Aging Brains See Slideshow
References
https://reference.medscape.com/drug/azilect-rasagiline-343055#6

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