Rasagiline

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Rasagiline

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Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Rasagiline

Property Description
Active ingredient Rasagiline Mesylate
Form Oral Tablet
Pharmacological class Selective Monoamine Oxidase B (MAO-B) Inhibitor
Common use Management of Parkinson's Disease
Origin Synthetic compound

Rasagiline is a prescription medicine intended for use as an antiparkinsonian agent, classified as a synthetic compound derived from propargylamine. It is supplied as a single-ingredient product in the form of an oral tablet. This compound is distinguished by its unique chemical structure as a Propargylamine derivative.

The Composition and Identity of Rasagiline

The active constituent in this medicine is Rasagiline Mesylate, which is the stable salt form of the Rasagiline molecule combined with solid excipients necessary for the final oral preparation. This choice of the Mesylate salt ensures a precise and reproducible chemical entity for consistent action. The development of Rasagiline as a single, synthetic entity was aimed at maximizing the selective action of the MAO-B Inhibitor class.

What Pharmacological Class Does Rasagiline Belong To?

Rasagiline belongs to the Monoamine Oxidase Inhibitor (MAOI) class of medications, specifically designated as a selective, irreversible Monoamine Oxidase B (MAO-B) Inhibitor. This means its primary action is highly targeted: it permanently blocks the MAO-B enzyme, which is the major form responsible for breaking down the neurotransmitter Dopamine in the brain. This selective inhibitor action is intended to provide neurological support while minimizing interactions associated with non-selective MAO inhibitors.

Rasagiline's General Therapeutic Purpose

The overall purpose of Rasagiline is to assist in managing the functional symptoms associated with the neurodegenerative disorder known as Parkinson's disease. The compound is typically used to help maintain daily motor function in patients. By utilizing its core mechanism, Rasagiline slows the metabolic breakdown of the neurotransmitter Dopamine within the brain. This Dopamine preservation approach serves to increase and sustain the available levels of Dopamine, thereby helping to compensate for the reduction in dopamine-producing neurons that characterizes the condition.

What side effects are possible with Rasagiline?

Possible Side Effects and Safety Information

The official safety profile for Rasagiline, a selective Monoamine Oxidase B (MAO-B) inhibitor, is established through regulatory classifications that document adverse reactions and safety restrictions.

Frequency-Classified Adverse Reactions

Adverse reactions are grouped by frequency and System-Organ Class (SOC) based on clinical data. Common reactions (occurring in ge 1/100 to < 1/10 users) typically involve the Nervous System (e.g., headache, dizziness), Gastrointestinal system (e.g., nausea, dyspepsia), and general disorders (e.g., flu-like syndrome). Uncommon reactions (occurring in ge 1/1,000 to < 1/100 users) include cerebrovascular accident, myocardial infarction, and hallucinations.

Serious Adverse Reactions and Restrictions

Regulatory documents highlight the risk of Hypertensive Crisis due to interactions with certain tyramine-containing foods or drinks, and the potential for Serotonin Syndrome when used alongside serotonergic medications. Post-marketing surveillance suggests a possible association with an increased risk of melanoma, necessitating monitoring for skin changes. Official labeling includes constraints regarding excessive somnolence and mandates blood pressure monitoring during treatment initiation.

Population-Specific Safety Constraints

Rasagiline is contraindicated (should not be used) in individuals with severe hepatic (liver) impairment. Safety and effectiveness have not been established in the pediatric population. When initiated in patients already taking levodopa, an increase in dyskinesia may occur, a pattern that sometimes requires adjustment of the levodopa dose.

Overdose and Emergency Response

Overdose and when to seek help

The official overdose profile for Rasagiline indicates that manifestations may have a delayed onset, potentially appearing up to 12 to 24 hours after the ingestion of a dose higher than recommended. Symptoms are similar to those of non-selective MAOI overdose, involving severe effects on the central nervous and cardiovascular systems.

Classification Field Official Regulatory Statement
Severity Classification Overdose can be fatal and may result in coma or life-threatening events.
Severe Outcomes Documented risks include Serotonin Syndrome, hypertensive crisis, seizures, and profound hyperthermia.
Antidote Information No specific antidote is known for overdose with Rasagiline.

When to seek immediate medical help:

Regulatory documents mandate that patients seek emergency medical attention or call a poison control center immediately if an overdose is suspected. Urgent medical services (such as 911) must be called if the affected individual has collapsed, experienced a seizure, is having trouble breathing, or cannot be awakened. Due to the absence of a known antidote, treatment is symptomatic and supportive, requiring close observation for signs of CNS and cardiovascular toxicity.

Therapeutic Uses of Rasagiline

What Rasagiline Treats: Main Uses and Benefits

Rasagiline is used alone or in combination with other medications to treat the symptoms of Parkinson's disease. This is a core function of the medicine. Rasagiline is applied across domains where additional symptomatic support is needed, including situations involving motor symptoms, symptom fluctuations, and early-stage manifestations of the disease.


Managing Motor Symptoms in Parkinson's Disease

This is a core therapeutic domain. Rasagiline helps address the major symptoms of increased neurological or muscular activity associated with Parkinson's, such as tremor, rigidity, and slow movement. It is applied across domains where additional symptomatic support is needed and assists with maintaining functional stability.


Supportive Management and Symptom Fluctuations

Rasagiline is commonly used in situations involving recurrent or episodic manifestations. It offers symptomatic relief that helps patients cope more steadily with the developing condition, and is applied in settings where short-term symptom stabilization is important. When applied in clinical settings that involve acute or unstable symptom patterns, it assists with maintaining functional stability.


Quick Fact: Support for Stiffness and Tremor

Regulatory References

  1. NIH MedlinePlus overview

Eligibility and Restrictions for Use

Regulatory documents establish clear eligibility criteria for the use of Rasagiline in adults, with several populations being excluded or restricted from treatment.

Contraindicated Populations

Rasagiline is formally contraindicated and must not be used by patients who have a known hypersensitivity to the active substance or any excipients. It is also prohibited for patients with severe hepatic impairment. A mandatory exclusion applies to individuals currently taking or having recently discontinued (within 14 days) certain medications, including:

  • Other Monoamine Oxidase (MAO) inhibitors (selective or non-selective, including medicinal or natural products like St. John's Wort).
  • The opioid analgesics meperidine, tramadol, methadone, or propoxyphene.
  • The cough suppressant dextromethorphan.

Restricted and Non-Recommended Use

Use is not recommended or should be avoided in patients with moderate hepatic impairment. In cases of mild hepatic impairment, caution is advised. The medicine's safety and efficacy have not been established in the pediatric population (children and adolescents), so its use in this age group is not recommended. During pregnancy, Rasagiline should generally be avoided as a precautionary measure due to a lack of complete human data. Breast-feeding mothers should use the drug with caution, as experimental data indicates Rasagiline may inhibit milk secretion.

What should I know about interactions with other medicines?

Rasagiline, an irreversible monoamine oxidase B (MAO-B) inhibitor, has a number of clinically significant drug interactions, primarily due to its MAO inhibitory activity.

Contraindicated Combinations

Co-administration is contraindicated with other MAO inhibitors (including herbal products like St. John's Wort) and certain strong opioid analgesics, such as meperidine and tramadol. This is due to the potential for severe adverse reactions, including the risk of hypertensive crisis or serotonin syndrome.

Restricted and Cautionary Use

  • Antidepressants: Use with selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), and tricyclic/tetracyclic antidepressants should be approached with caution, as this combination increases the risk of serotonin syndrome.
  • Sympathomimetics: Combining rasagiline with sympathomimetic medicinal products, including those found in over-the-counter cold and cough preparations (e.g., ephedrine, pseudoephedrine, dextromethorphan), is not recommended due to the risk of significant blood pressure increase.
  • CYP1A2 Inhibitors: The primary enzyme responsible for rasagiline metabolism is Cytochrome P450 1A2 (CYP1A2). Co-administration with potent CYP1A2 inhibitors, such as ciprofloxacin, increases rasagiline plasma levels. In this circumstance, the rasagiline dose should not exceed 0.5 mg once daily.

Timing-Based Rules

Patients must wait at least 14 days after discontinuing rasagiline before initiating treatment with any MAO inhibitor or the contraindicated opioids (e.g., meperidine).

Mechanism of Action

Selective Enzyme Inhibition

Rasagiline acts as a selective and irreversible inhibitor of the enzyme Monoamine Oxidase B (MAO-B). This molecular binding covalently blocks the enzyme's active site, preventing it from performing the metabolic breakdown of specific monoamines, thereby initiating the pharmacodynamic cascade.

Modulation of Dopaminergic Signaling

By preventing the enzymatic degradation of dopamine, the drug increases the concentration of available dopamine in the synaptic clefts. This resulting increase in neurotransmitter availability alters signal propagation within the central dopaminergic pathways.

Alteration of Motor Regulation Signaling

The higher concentrations of dopamine lead to increased stimulation of dopamine receptors. This results in an alteration of nerve signal transmission associated with motor regulation, a change in signaling dynamics that contributes to the drug's resulting physiological profile.

Dosage and Administration Information

Rasagiline is administered orally as a tablet, once a day, and may be taken with or without food. The official dosing schedule for adults is strictly determined by whether the medicine is used alone or in combination with other treatments.

Official Dosing Schedule

Usage Context Recommended Daily Dose
Monotherapy (used alone) 1 mg once daily
Adjunct to Levodopa Initial dose: 0.5 mg once daily. May be increased to 1 mg once daily for sufficient clinical response.

Dose Adjustments and Administration Rules

The maximum recommended daily dose is 1 mg. Specific adjustments to this dose are mandated under certain conditions to ensure correct use:

  • Hepatic Impairment: Patients with mild hepatic impairment should not exceed a dose of 0.5 mg once daily. The medicine should not be used in patients with moderate or severe hepatic impairment.
  • Concomitant Use with CYP1A2 Inhibitors: If taken with strong CYP1A2 inhibitors, such as ciprofloxacin, the dose of rasagiline must not exceed 0.5 mg once daily.
  • Missed Dose: If a dose is missed, patients are instructed not to double up to make up for the forgotten dose. Instead, the next dose should be taken at the usual time on the following day.

Use in children and adolescents under 18 years of age is not recommended, as safety and efficacy have not been established in this population.

Recent Clinical Evidence

Rasagiline: Recent Clinical Evidence

Rasagiline is a selective, irreversible monoamine oxidase B (MAO-B) inhibitor investigated for the symptomatic management of idiopathic Parkinson's disease (PD). Its primary mechanism is believed to be the inhibition of the MAO-B enzyme, which subsequently increases dopamine levels in the brain's striatum.

Clinical research has evaluated rasagiline in two primary treatment settings:


Early-Stage Monotherapy

Multiple randomized, placebo-controlled trials, such as the TEMPO study, assessed rasagiline as initial treatment for patients with early, untreated PD. These studies showed that rasagiline monotherapy was associated with an improved score on the Unified Parkinson’s Disease Rating Scale (UPDRS) compared to placebo over 26 weeks. Furthermore, long-term open-label extensions of these trials, like the ADAGIO study, explored whether starting treatment early was associated with slower functional decline compared to a delayed start.


Advanced-Stage Adjunctive Therapy

Studies like the PRESTO and LARGO trials examined rasagiline's use as an adjunct to levodopa therapy in patients experiencing motor fluctuations (or "wearing-off" time). In these cohorts, rasagiline was associated with a reduction in daily "off" time and an increase in functional "on" time compared to placebo. A recent meta-analysis affirmed that rasagiline demonstrates comparable symptomatic effects in improving motor symptoms in both early- and advanced-stage disease.


Safety and Tolerability

Across multiple large trials, rasagiline has been observed to be generally well-tolerated. The most common adverse events reported in these studies included headache, joint pain, and flu-like symptoms. Safety data has consistently shown a low incidence of hypertensive crises at the approved dosage, and unlike some older MAO-B inhibitors, rasagiline does not metabolize into amphetamine-like compounds.

Frequently Asked Questions (FAQ)

Common questions about Rasagiline (FAQ)


Q: What is the main difference between Rasagiline and Selegiline?

Both are MAO-B inhibitors, but official medical summaries note a key difference in how the body processes them. Rasagiline is distinguished from selegiline because its primary metabolite (amioindan) is not associated with having amphetamine-like properties.


Q: What is Rasagiline used for besides Parkinson's?

According to the official product information, Rasagiline is indicated solely for the treatment of idiopathic Parkinson's disease. It is indicated for use alone (monotherapy) or alongside levodopa (adjunct therapy).


Q: How quickly does Rasagiline start to work or show an effect?

Clinical studies have examined the onset of symptomatic relief. Evidence indicates that measurable beneficial effects on Parkinson's disease symptoms can be observed within approximately one week of starting the once-daily treatment.


Q: What kinds of foods should people be careful about when taking Rasagiline?

While dietary tyramine restriction is generally not required at the usual recommended doses, official guidance emphasizes caution. Official product information suggests avoiding foods that contain very high amounts of tyramine, as this combination could potentially lead to a severe spike in blood pressure known as a hypertensive crisis.


Q: Why is aged cheese sometimes mentioned with Rasagiline?

Aged cheese is mentioned because it is a food that can naturally contain high amounts of tyramine. In combination with MAO inhibitors like Rasagiline, high levels of tyramine in the diet carry a risk of significantly increasing blood pressure.


Q: Is it safe to drink alcohol while using Rasagiline?

Official warnings describe that Rasagiline may add to the effects of alcohol and other medicines that cause drowsiness, which could increase the risk of side effects like sleepiness and dizziness. Some alcoholic beverages also contain tyramine.


Q: Does Rasagiline cause fatigue or insomnia?

Yes, sleep-related changes are noted in the safety profile. Insomnia (difficulty sleeping) is reported as a common side effect in clinical trials. Unusual tiredness or weakness has also been reported.


Q: Is weight gain or weight loss a common effect of Rasagiline?

In clinical trials, weight loss and loss of appetite have been reported as adverse events, particularly when Rasagiline is used in combination with levodopa. Weight gain is not frequently reported as an adverse event in the regulatory summaries.


Q: Does Rasagiline affect sleep quality?

Yes, regulatory information indicates possible impacts on sleep. Side effects reported include the common occurrence of insomnia (difficulty sleeping) and warnings regarding excessive daytime sleepiness (somnolence), both of which can affect overall sleep quality.


Q: Is there a chance of experiencing hallucinations while on Rasagiline?

Yes, hallucinations (seeing, hearing, or feeling things that are not there) are listed as a possible adverse reaction. Clinical data describes this event as uncommon.


Q: Why is it important to tell my doctor about all other medicines I take before starting Rasagiline?

It is critical because Rasagiline has potentially severe interactions with many other medicines, including certain antidepressants, pain relievers, and cold medicines. Official guidance warns that co-administration risks conditions like serotonin syndrome or hypertensive crisis. Full disclosure is necessary to help minimize the risk of serious reactions.


Q: Does Rasagiline have any known interactions with herbal supplements?

Yes, the official product information explicitly states that the use of Rasagiline is contraindicated with certain herbal products. This specifically includes St. John's wort because its MAO inhibitory activity may cause a dangerous interaction.


Q: How does Rasagiline differ from dopamine agonists?

The difference is in the core mechanism. Rasagiline works as an MAO-B inhibitor to preserve and increase the brain's natural dopamine levels, whereas dopamine agonists are a different class of medicine that directly stimulate dopamine receptors.


Q: Is it common for people to switch from one MAO-B inhibitor to Rasagiline?

Official information outlines the necessary safety measures for switching between MAO inhibitors. This includes a washout period, which is a required safety measure involving waiting at least 14 days after stopping a different MAO inhibitor before initiating Rasagiline.


Q: What are the signs that Rasagiline is working?

In clinical trials, the medication's effects were measured by objective clinical metrics, such as an improvement in the overall score on a standard Parkinson's disease assessment scale and a reduction in the daily time spent in the 'off' state.


Q: Does Rasagiline help with non-motor symptoms of Parkinson's?

While the primary indication is for motor symptoms, some documents supporting the drug's use indicate that a positive therapeutic response may include symptomatic control of non-motor and behavioral symptoms.


Q: Are there any specific monitoring tests required while taking Rasagiline?

Patients are advised to be monitored for new or changing skin growths (due to a reported melanoma risk). Official documents note that blood pressure monitoring is also necessary, especially when treatment begins, because of the risk of hypertension.


Q: Why is Rasagiline not for people with certain heart conditions?

The primary cardiovascular concerns relate to the drug’s potential to cause a hypertensive crisis (a severe spike in blood pressure) or hypotension (low blood pressure). This is why the medicine is generally used with caution in patients with blood pressure instability.


Q: How long can a person safely stay on Rasagiline?

The medication has been studied in long-term open-label trials lasting 12 months or more. Regulatory information does not specify a maximum duration for continuous treatment.


Q: Does Rasagiline cause changes to vision or eye health?

Yes, changes to vision have been reported. Abnormal vision and conjunctivitis (pink eye) are listed as common side effects in the official adverse reactions data.


Q: Does Rasagiline affect blood sugar levels?

Information on drug interactions suggests that Rasagiline may affect the activity of certain medications used to manage blood sugar. This indicates a potential indirect effect on glucose regulation.


Q: What should I do if I suspect a severe side effect from Rasagiline?

In cases of suspected severe side effects, such as symptoms of serotonin syndrome or a hypertensive crisis (including a severe headache, confusion, or chest pain), official guidance emphasizes the need for immediate medical attention.

How should Rasagiline be stored and disposed of?

How to Store and Dispose of Rasagiline Mesylate Tablets

Rasagiline mesylate tablets must be stored at Controlled Room Temperature, which is 20 C to 25 C (68 F to 77 F), with permitted excursions up to 30 C.

Storage Conditions

  • Temperature: Store at Controlled Room Temperature; do not store above 25 C.
  • Protection: Keep the medication in its original package and dispense in a tight, light-resistant container that is kept tightly closed to protect it from light and moisture.
  • Child Safety: Keep this and all medication out of the reach and sight of children.

Disposal

Disposal of unused or expired Rasagiline must be done in accordance with local requirements.

The medication should not be disposed of via wastewater or household waste.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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