Rasagiline
- I. Introduction
- II. Uses of Rasagiline
- III. How Rasagiline Works
- IV. Composition of Rasagiline
- V. Dosage and Administration
- VI. Side Effects of Rasagiline
- VII. Interaction with Other Drugs and Substances
- VIII. Warnings and Contraindications
- IX. Careful Administration and Important Precautions
- X. Special Populations
- XI. Overdose Management
- XII. Storage and Handling Precautions
I. Introduction
Brief Overview of Rasagiline
Rasagiline is a drug known for its ability to inhibit monoamine oxidase B (MAO B). This remarkable medication is primarily used to help manage the symptoms of Parkinsons' Disease.
FDA-approved Indications
The FDA has approved rasagiline for the treatment of Parkinsons' Disease, either as a therapy or in combination with other medications such, as levodopa.
Importance of Rasagiline in Medical Treatment
The introduction of rasagiline has brought about a change in the way Parkinsons' Disease is managed. It has improved motor control. Helped reduce fluctuations in the condition of patients.
Scope of the Article
This detailed article explores the facets of rasagiline, including its applications, potential side effects, recommended dosages, and contraindications.
II. Uses of Rasagiline
FDA-Approved Uses
Parkinson's Disease Management
Rasagiline is a monoamine oxidase type B (MAO-B) inhibitor that can be used as monotherapy or adjuvant therapy to levodopa in Parkinson’s disease (PD) 1. According to a retrospective case-control study, long-term use of MAO-B inhibitors resulted in a significant reduction in levodopa requirements and a lower frequency of dyskinesias in patients with PD. Selegiline and rasagiline had equal efficacy in controlling motor symptoms in PD patients on optimized therapy 1.
1: Cereda, E., Cilia, R., Canesi, M., Tesei, S., Mariani, C. B., Zecchinelli, A. L., & Pezzoli, G. (2017). Efficacy of rasagiline and selegiline in Parkinson’s disease: a head-to-head 3-year retrospective case–control study. Journal of Neurology, 264(6), 1254-1263. Link
Monoamine Oxidase Inhibitor
Rasagiline is a monoamine oxidase type B (MAO-B) inhibitor 1 that can be used as monotherapy or adjuvant therapy to levodopa in Parkinson’s disease (PD) 2. According to a retrospective case-control study, long-term use of MAO-B inhibitors resulted in a significant reduction in levodopa requirements and a lower frequency of dyskinesias in patients with PD. Selegiline and rasagiline had equal efficacy in controlling motor symptoms in PD patients on optimized therapy 2.
MAO-B is an enzyme that breaks down several chemicals in the brain, including dopamine. An MAO-B inhibitor makes more dopamine available to the brain, which can modestly improve many PD movement symptoms 1. Rasagiline’s MAO-B inhibitory activity causes an increase in extracellular levels of dopamine in the striatum. The elevated dopamine level and subsequent increased dopaminergic activity are likely to mediate rasagiline’s beneficial effects seen in models of dopaminergic motor dysfunction 3.
2: Cereda, E., Cilia, R., Canesi, M., Tesei, S., Mariani, C. B., Zecchinelli, A. L., & Pezzoli, G. (2017). Efficacy of rasagiline and selegiline in Parkinson’s disease: a head-to-head 3-year retrospective case–control study. Journal of Neurology, 264(6), 1254-1263. Link 1: Parkinson’s Foundation. (n.d.). MAO-B Inhibitors.
Off-Label Uses
Depression Management
According to some doctors, rasagiline can be used as an additional treatment option for patients struggling with resistant depression, although it is not officially approved by the FDA for this purpose1.
1: For more information, please refer to this article on JAMA Network.
Other Neurological Disorders
Research is being conducted to investigate the effectiveness of rasagiline in treating neurological conditions such as restless legs syndrome and multiple system atrophy 12.
1: Thin film hydration versus modified spraying technique to fabricate intranasal spanlastic nanovesicles for rasagiline mesylate brain delivery: Characterization, statistical optimization, and in vivo pharmacokinetic evaluation. Springer. Link 2: In a randomized trial, rasagiline did not alter clinical disease progression in multiple system atrophy. Rasagiline is one of several monoamine oxidase inhibitors that have been proposed as possible disease-modifying therapies for Parkinson disease (PD). NEJM Journal Watch. Link
III. How Rasagiline Works
Mechanism of Action
MOA in Parkinson’s Disease
The primary way that Rasagiline works is by blocking the MAO B enzyme. This causes dopamine levels in the space between nerve cells to increase, which helps with communication, between them.
MOA in Off-Label Uses
The specific processes involved in off-label uses are still unclear, although certain studies indicate a mode of action, through the enhancement of serotonin levels.
Metabolism and Excretion
The liver primarily breaks down Rasagiline. Then eliminated from the body through the kidneys.
IV. Composition of Rasagiline
Active Ingredient
Rasagiline mesylate serves as the component in rasagiline.
Inactive Ingredients
Typically, these ingredients may consist of substances, like mannitol and colloidal silicon dioxide.
Available Formulations
Rasagiline is commonly found in strengths as oral tablets.
V. Dosage and Administration
Standard Dosages
Dosage for Parkinson's Disease
The typical recommended dosage usually falls between 0.5 and 1 milligram, per day.
Dosage for Off-Label Uses
For uses that are not officially approved the recommended dosage may vary depending on the doctors judgment. Is usually lower.
Methods of Administration
Oral Tablet
Rasagiline is mostly given in the form of tablets.
Combined Therapy
In instances rasagiline is employed as part of combination therapy alongside other medications, for the treatment of Parkinsons disease.
Missed Dose Protocols
If you happen to miss a dose it's an idea to take the medication as soon as you can unless its almost time, for your next scheduled dose.
VI. Side Effects of Rasagiline
Common Side Effects
Gastrointestinal Issues
Many patients frequently experience feelings of queasiness and discomfort in the abdomen.
Neuropsychiatric Symptoms
There have been reported instances of sleeplessness and feelings of unease.
Serious Side Effects
Serotonin Syndrome
This is a situation that requires urgent medical attention.
Hypertension
There have been observations of higher blood pressure levels, especially in overdose cases.
Managing Side Effects
Adjusting the dosage and providing treatment for symptoms are management practices.
VII. Interaction with Other Drugs and Substances
Drug-Drug Interactions
Antidepressants
Taking agents can increase the likelihood of developing serotonin syndrome.
Hypertensive Agents
Taking rasagiline together with antihypertensive medications may lead to an increase in blood pressure levels.
Food and Alcohol Interactions
Although there aren't interactions, with food, it's essential to avoid consuming alcohol as it can worsen the potential side effects.
VIII. Warnings and Contraindications
Absolute Contraindications
Allergic Reactions
Patients who have a known allergy or sensitivity to the drug rasagiline should not take it.
Certain Medical Conditions
Patients who have previously experienced medical conditions such, as liver disorders should exercise caution.
Relative Contraindications
Liver Disorders
Patients with liver damage need to be monitored.
Other Neurological Conditions
Individuals with neurological disorders must seek guidance from a healthcare professional.
IX. Careful Administration and Important Precautions
Monitoring Parameters
Blood Pressure
Regularly checking blood pressure is not a good idea but essential as rasagiline has the potential to cause high blood pressure. Using a blood pressure monitor is recommended, especially when starting the medication and adjusting the dosage.
Neurological Status
Regular neurological assessments are necessary to evaluate the effectiveness of the medication and identify any adverse effects, on the nervous system.
Safety Protocols
Periodic Tests
It is essential to conduct thorough laboratory evaluations, which should include tests to assess liver function and complete blood counts.
Consultation with Healthcare Providers
To avoid any consequences or potential issues with drug interactions, it is highly recommended to have regular discussions, with healthcare professionals.
X. Special Populations
Administration to Elderly Patients
Dosage Adjustments
When it comes to adults, it may be necessary to carefully adjust medication doses because their bodies may process and distribute drugs differently due to changes, in their physiology.
Monitoring
Given the increased likelihood of outcomes in this particular group, it is crucial to maintain close monitoring and surveillance.
Administration to Pregnant Women and Nursing Mothers
Risk Category
Rasagiline falls into a pregnancy risk category that is not clearly determined, so it should be used with caution during pregnancy and breastfeeding.
Recommendations
Healthcare providers are responsible for carefully considering the advantages and risks before prescribing rasagiline in these situations.
Administration to Children
Safety and Efficacy
Considering the amount of definitive information available regarding the use of rasagiline, in children, the safety and effectiveness of this medication still remain uncertain.
Dosage Guidelines
If the medication is given, it is essential to adjust and customize the dosages based on the specific requirements of each patient. Typically it is advisable to start with doses, within the recommended range.
XI. Overdose Management
Symptoms of Overdose
Typical signs of an overdose can include high blood pressure, serotonin-related symptoms, and severe disturbances in mental health.
Immediate Steps for Management
It is crucial to stop taking the medication to provide symptom relief and seek urgent medical advice in drug overdose cases.
Long-Term Consequences
The consequences of an overdose can have lasting effects impacting both the neurological and cardiovascular systems, with potential long-term complications.
XII. Storage and Handling Precautions
Optimal Storage Conditions
The medication must be kept in a container at average room temperature and away from sunlight and moisture to ensure its effectiveness, as a medicine.
Disposal Protocols
It is recommended to dispose of any medication that's unused or expired by following the medication disposal guidelines provided by the FDA. The preferable method of disposal is through participation in a take-back program.
Guidelines to Prevent Contamination and Degradation
Always make sure to close the container after administering the medication. Avoid transferring tablets to containers that are not the original ones.