Rasagiline

Mechanism-of-action classes: Monoamine Oxidase-B Inhibitors; Monoamine Oxidase Inhibitors.

• Rasagiline tablets are indicated for the treatment of Parkinson's disease (PD).ICD-10: G20

• Rasagiline is contraindicated for use with meperidine, tramadol, methadone, propoxyphene and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors, because of risk of serotonin syndrome [See Warnings and Precautions (5.2)] . At least 14 days should elapse between discontinuation of rasagiline and initiation of treatment with these medications.contraindicated

Monotherapy: Rasagiline Tablets 1 mg once daily (2.1) As adjunct without levodopa: Rasagiline Tablets 1 mg once daily (2.1) As adjunct to levodopa: Rasagiline Tablets 0.5 mg once daily. Increase dose to 1 mg daily as needed for sufficient clinical response (2.1) Patients taking ciprofloxacin or other CYP1A2 inhibitors: Rasagiline Tablets 0.5 mg once daily (2.2, 5.4) Patients with mild hepatic impairment: Rasagiline Tablets 0.5 mg once daily. Rasagiline Tablets should not be used in patients with moderate or severe hepatic impairment (2.3, 5.5) 2.1 General Dosing Recommendations When rasagiline tablets are prescribed as monotherapy or as adjunct therapy in patients not taking levodopa, patients may start rasagiline tablets at the recommended dose of 1 mg administered orally once daily. In patients taking levodopa, with or without other PD drugs (e.g., dopamine agonist, amantadine, anticholinergics), the recommended initial dose of rasagiline tablet is 0.5 mg once daily. If the patient tolerates the daily 0.5 mg dose, but a sufficient clinical response is not achieved, the dose may be increased to 1 mg once daily. When rasagiline tablets are used in combination with levodopa, a reduction of the levodopa dose may be considered, based upon individual response. The recommended doses of rasagiline tablets should not be exceeded because of risk of hypertension [see Warnings and Precautions (5.1)].

May cause hypertension (including severe hypertensive syndromes) at recommended doses (5.1) May cause serotonin syndrome when used with antidepressants (5.2) May cause falling asleep during activities of daily living, daytime drowsiness, and somnolence (5.3) May cause hypotension, especially orthostatic (5.6) May cause or exacerbate dyskinesia. Decreasing the levodopa dose may lessen or eliminate this side effect (5.7) May cause hallucinations and psychotic-like behavior (5.8) May cause impulse control/compulsive behaviors (5.9) May cause withdrawal-emergent hyperpyrexia and confusion (5.10) 5.1 Hypertension Exacerbation of hypertension may occur during treatment with rasagiline tablets. Medication adjustment may be necessary if elevation of blood pressure is sustained. Monitor patients for new onset hypertension or hypertension that is not adequately controlled after starting rasagiline tablets. In Study 3, rasagiline (1 mg/day) given in conjunction with levodopa, produced an increased incidence of significant blood pressure elevation (systolic > 180 or diastolic > 100 mm Hg) of 4% compared to 3% for placebo [see Adverse Reactions (6.1)] . When used as an adjunct to levodopa (Studies 3 and 4), the risk for developing post-treatment high blood pressure (e.g., systolic > 180 or diastolic >100 mm Hg) combined with a significant increase from baseline (e.g., systolic > 30 or diastolic > 20 mm Hg) was higher for rasagiline (2%) compared to placebo (1%). Dietary tyramine restriction is not required during treatment with recommended doses of rasagiline.

The following adverse reactions are described in more detail in the Warnings and Precautions section of the label: Hypertension [ see Warnings and Precautions (5.1) ] Serotonin Syndrome [ see Warnings and Precautions (5.2) ] Falling Asleep During Activities of Daily Living and Somnolence [ see Warnings and Precautions (5.3) ] Hypotension / Orthostatic Hypotension [ see Warnings and Precautions (5.6) ] Dyskinesia [ see Warnings and Precautions (5.7) ] Hallucinations / Psychotic-Like Behavior [ see Warnings and Precautions (5.8) ] Impulse Control /Compulsive Behaviors [ see Warnings and Precautions (5.9) ] Withdrawal-Emergent Hyperpyrexia and Confusion [ see Warnings and Precautions (5.10) ] Most common adverse reactions (incidence 3% or greater than placebo): Rasagiline monotherapy: flu syndrome, arthralgia, depression, dyspepsia ( 6.1 ) Rasagiline used as adjunct without levodopa: peripheral edema, fall, arthralgia, cough, and insomnia ( 6.1 ) Rasagiline 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 ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Torrent Pharma Inc. at 1-800-912-9561 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

Pregnancy: Based on animal data, may cause fetal harm. (8.1) 8.1 Pregnancy Risk Summary There are no adequate data on the developmental risks associated with the use of rasagiline in pregnant women. In animal studies, oral administration of rasagiline to rats during gestation and lactation resulted in decreased survival and reduced body weight in the 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 [ see Data] . In the US general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. The background risks of major birth defects and miscarriage for the indicated population is unknown. Data Animal Data In a combined mating/fertility and embryofetal development study in pregnant rats, no effect on embryofetal development was observed at oral doses up to 3 mg/kg/day (approximately 30 times the plasma exposure (AUC) in humans at the maximum recommended human dose [MRHD, 1 mg/day]). In pregnant rabbits administered rasagiline throughout the period of organogenesis at oral doses of up to 36 mg/kg/day, no developmental toxicity was observed.

In a dose escalation study in patients on chronic levodopa therapy treated with 10 mg of rasagiline there were three reports of cardiovascular side effects (including hypertension and postural hypotension) which resolved following treatment discontinuation. Although no cases of overdose have been observed with rasagiline during the clinical development program, the following description of presenting symptoms and clinical course is based upon overdose descriptions of nonselective MAO inhibitors. The signs and symptoms of nonselective MAOI overdose may not appear immediately. Delays of up to 12 hours after ingestion of drug and the appearance of signs may occur. The peak intensity of the syndrome may not be reached until for a day following the overdose. Death has been reported following overdose; therefore, immediate hospitalization, with continuous patient observation and monitoring for at least two days following the ingestion of such drugs in overdose, is strongly recommended. The severity of the clinical signs and symptoms of MAOI overdose varies and may be related to the amount of drug consumed. The central nervous and cardiovascular systems are prominently involved.

• May 16, 2006NDANDA021641Teva
• Mar 15, 2016ANDAANDA201970Orbion Pharms
• Oct 30, 2017ANDAANDA201889Alkem Labs Ltd
• Jul 27, 2018ANDAANDA201892Chartwell Rx
• Mar 29, 2019ANDAANDA207004Micro Labs
• Oct 4, 2019ANDAANDA206153Regcon Holdings
• Nov 18, 2021ANDAANDA201942Carnegie
• Apr 9, 2024ANDAANDA218163Rising

1. 1Fall1,0469.6%
2. 2Hallucination9288.5%
3. 3Dyskinesia7466.9%
4. 4Drug Ineffective7416.8%
5. 5Tremor6395.9%
6. 6Dizziness6365.9%
7. 7Death6135.6%
8. 8Confusional State5364.9%
9. 9Parkinson^s Disease5224.8%
10. 10Somnolence4984.6%
11. 11Gait Disturbance4934.5%
12. 12Nausea4784.4%
13. 13Fatigue4614.2%
14. 14Constipation3953.6%
15. 15Insomnia3693.4%

The 10 most recently updated of 65 ClinicalTrials.gov registrations naming Rasagiline as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Relative Bioavailability Study of HNC364 Injectable Suspension
  Active not recruiting · Phase 1 · Interventional · 30 enrolled · Guangzhou Henovcom Bioscience Co. Ltd.
  NCT06798519updated 2026-06-02
• Effect of Rasagiline on Balance in Parkinson's Disease as Measured by Computerized Posturography
  Withdrawn · Phase 4 · Interventional · 0 enrolled · New York Medical College
  NCT07077187updated 2025-07-24
• Efficacy and Safety of Rasagiline in Prodromal Parkinson's Disease
  Withdrawn · Phase 2 · Phase 3 · Interventional · 0 enrolled · Second Affiliated Hospital, School of Medicine, Zhejiang University
  NCT05611372updated 2025-01-07
• A Study to Evaluate the Safety, Tolerability, PK and PD of HNC364 Injectable Suspension
  Completed · Phase 1 · Interventional · 34 enrolled · Guangzhou Henovcom Bioscience Co. Ltd.
  NCT05523570updated 2024-09-27
• An Observational Study on Safinamide, Rasagiline and Other Standard of Care in PD
  Completed · Observational · 1,235 enrolled · Zambon SpA
  NCT03994328updated 2024-04-11
• Overnight Switch From Rasagiline To Safinamide
  Completed · Phase 4 · Interventional · 20 enrolled · IRCCS San Raffaele Roma
  NCT03843944updated 2024-04-10
• Rasagiline Tablets Special Drug Use-Results Survey "Survey on Long-term Safety"
  Completed · Observational · 1,021 enrolled · Takeda
  NCT03727139updated 2024-03-08
• Image Parkinson's Disease Progression Study
  Completed · Phase 2 · Interventional · 96 enrolled · University of Florida
  NCT02789020updated 2023-09-06
• Study to Evaluate the Pressor Effect of Oral Tyramine During Ozanimod Treatment in Healthy Adult Participants
  Completed · Phase 1 · Interventional · 128 enrolled · Celgene
  NCT04978298updated 2023-08-31
• MAO-B Occupancy in Depressed Patients
  Completed · Interventional · 50 enrolled · Centre for Addiction and Mental Health
  NCT04841798updated 2023-07-27

Frequently asked questions

How does Rasagiline work?

Mechanism-of-action classes: Monoamine Oxidase-B Inhibitors; Monoamine Oxidase Inhibitors.

What is Rasagiline used for?

According to FDA labeling, Rasagiline carries indications including: Rasagiline tablets are indicated for the treatment of Parkinson's disease (PD).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Rasagiline?

Rasagiline is classified as Monoamine oxidase B inhibitors, Monoamine Oxidase Inhibitor, Monoamine Oxidase-B Inhibitors, Monoamine Oxidase Inhibitors, Increased Dopamine Activity, Increased Serotonin Activity.

What are the brand names for Rasagiline?

Rasagiline is marketed under brand names including Azilect.

What are the contraindications for Rasagiline?

Rasagiline labeling lists contraindications including: Rasagiline is contraindicated for use with meperidine, tramadol, methadone, propoxyphene and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors, because of risk of serotonin syndrome [See Warnings and Precautions (5.2)] . At least 14 days should elapse between discontinuation of rasagiline and initiation of treatment with these medications.. Always consult the full prescribing information and a clinician.