rasagiline

Actions and Spectrum: 

• rasagiline is a medication used for the treatment of Parkinson’s disease. Its mechanism of action involves the inhibition of the enzyme monoamine oxidase B (MAO-B), which is responsible for the breakdown of dopamine in the brain. By inhibiting MAO-B, rasagiline increases the concentration of dopamine in the brain, which can help to improve the symptoms of Parkinson’s disease. 
• In addition to its effects on MAO-B, rasagiline has also been shown to have neuroprotective properties. The drug may help protect brain neurons from damage and improve the survival of dopaminergic neurons. 
• The spectrum of activity of rasagiline is primarily limited to treating Parkinson’s disease. It is not practical for other conditions, as its mechanism of action is specific to Parkinson’s disease and the breakdown of dopamine in the brain. rasagiline is generally used with other medications for Parkinson’s disease, such as levodopa or carbidopa, to improve the control of symptoms and slow the progression of the disease. 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency defined 

>10% 

Headache (14%) 

EPS (dyskinesia/dystonia) (18%) 

Nausea (10-12%)  

1-10% 

Constipation (4-9%) 

Arthralgia (7%) 

Xerostomia (2-6%) 

Fall (5%) 

Hallucination (4-5%) 

Postural hypotension (6-9%) 

Weight loss (2-9%) 

Dyspepsia (7%) 

Depression (5%) 

Flu-like syndrome (5%) 

Conjunctivitis (3%) 

Gastroenteritis (3%) 

Arthritis (2%) 

Malaise (2%) 

Parasthesia (2%) 

Fever (3%) 

Rhinitis (3%) 

Bruising (2%) 

Neck pain (2%) 

Vertigo (2%) 

 

<1% 

MI 

CVA 

Gastrointestinal hemorrhage 

Bundle branch block  

Post-marketing reports 

Melanoma 

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: rasagiline is contraindicated in patients with known hypersensitivity to the drug or its components. 

• Use with other MAO inhibitors: rasagiline should not be used with other MAO inhibitors or within 14 days of discontinuing treatment with another MAO inhibitor. Concurrent use of rasagiline and other MAO inhibitors can lead to a potentially life-threatening hypertensive crisis. 

• Pheochromocytoma: rasagiline is contraindicated in patients with pheochromocytoma, a rare adrenal gland tumor that can cause high blood pressure and other symptoms. 

• Severe hepatic impairment: rasagiline is contraindicated in patients with severe hepatic impairment as the liver extensively metabolizes the drug. 

• Concomitant use of opioids: The use of rasagiline with opioids can increase the risk of serotonin syndrome, a potentially life-threatening condition characterized by symptoms such as agitation, confusion, rapid heartbeat, high blood pressure, and muscle rigidity. 

• Concomitant use with certain antidepressants: Using rasagiline with certain antidepressants, such as selective serotonin reuptake inhibitors (SSRIs), can also increase the risk of serotonin syndrome. 

Caution: 

• Hypotension: rasagiline can cause orthostatic hypotension, a sudden drop in blood pressure when standing up from a lying or sitting position. Patients should be advised to rise slowly from a seated or lying to avoid falls or injury. 

• Tyramine-containing foods: Patients taking rasagiline should avoid consuming large amounts of tyramine-containing foods, such as aged cheese, cured meats, and fermented foods, as these can interact with MAO inhibitors and cause a hypertensive crisis. 

• Serotonin syndrome: Patients taking rasagiline should be monitored for symptoms of serotonin syndrome, which can occur when the drug is combined with other serotonergic drugs, such as antidepressants and opioids. 

• Hepatic impairment: Patients with mild to moderate hepatic impairment should be monitored closely for adverse effects when taking rasagiline. The liver extensively metabolizes the drug, and its safety and Efficacy have not been established in patients with severe hepatic impairment. 

• Cardiovascular disease: rasagiline should be used cautiously in patients with a history of cardiovascular disease, as it can increase the risk of cardiovascular events, such as myocardial infarction, angina, and stroke. 

• Surgery: Patients taking rasagiline should inform their healthcare provider if they are scheduled for surgery, as the drug can interact with anesthesia and other medications used during surgery. 

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology: 

• rasagiline is a medication used in the treatment of Parkinson’s disease. It belongs to a class of drugs known as monoamine oxidase inhibitors (MAOIs). The drug is rapidly and extensively absorbed after oral administration, with peak plasma concentrations reached within 0.5-2 hours. 
• rasagiline is metabolized primarily by the liver, with the primary metabolite being aminoindan, which is also a selective MAO-B inhibitor. The half-life of rasagiline is approximately 1-3 hours, and it is primarily eliminated through urine. 
• As a selective MAO-B inhibitor, rasagiline has been shown to increase dopamine levels in the brain, which can help improve the symptoms of Parkinson’s disease. In addition to its effects on MAO-B, rasagiline has also been shown to have neuroprotective properties. Studies have suggested that the drug may help protect brain neurons from damage and improve the survival of dopaminergic neurons. 

Pharmacodynamics: 

• The pharmacodynamics of rasagiline involve its action as a selective and irreversible inhibitor of the monoamine oxidase B (MAO-B) enzyme. MAO-B is an enzyme responsible for the breakdown of dopamine in the brain, and its inhibition leads to an increase in dopamine levels in the brain. 
• rasagiline is a selective MAO-B inhibitor, which binds specifically to the enzyme and does not affect other enzymes in the MAO family. The drug irreversibly binds to the enzyme’s active site and inhibits its activity. This results in an increase in dopamine levels in the brain, which can help to improve the symptoms of Parkinson’s disease. 
• In addition to its effects on MAO-B, rasagiline has been shown to have neuroprotective properties. The drug may help protect brain neurons from damage and improve the survival of dopaminergic neurons. The exact mechanism by which rasagiline exerts its neuroprotective effects is not fully understood, but it may involve regulating oxidative stress, inflammation, and apoptosis in the brain. 

Pharmacokinetics: 

Absorption 

The peak plasma time of rasagiline is 1 hour, indicating that the drug is rapidly absorbed after oral administration. The onset of action is also within 1 hour, suggesting that the drug has a relatively fast onset.The bioavailability of rasagiline is 36%, which means that only a fraction of the drug is absorbed into the systemic circulation after oral administration.  

Distribution 

rasagiline is highly protein-bound, with 88-94% of the drug bound to plasma proteins. The volume of distribution (Vd) of rasagiline is 87 L, indicating that the drug is widely distributed throughout the body.  

Metabolism 

rasagiline is primarily metabolized by the liver, with the CYP1A2 enzyme playing a vital role in the drug’s metabolism. The main metabolites of rasagiline are 1-aminoindan, 3-hydroxy-N-propargyl-1-aminoindan, and 3-hydroxy-1-aminoindan.  

Elimination and Excretion 

The half-life of rasagiline is 1.3-3 hours, indicating that the drug is rapidly eliminated from the body. The drug is primarily excreted in the urine, with 62% of the drug excreted in this way. A small amount of the drug (7%) is also excreted in the feces. 

Administration: 

rasagiline is administered orally, usually once daily, with or without food. The recommended dose for treating Parkinson’s disease is 0.5 mg/day, but your doctor may adjust the dose based on your individual needs and response to the drug 

Patient information leaflet 

Generic Name: rasagiline 

Why do we use rasagiline? 

rasagiline is a medication that is primarily used for the treatment of Parkinson’s disease. It is indicated as an adjunct therapy to levodopa/carbidopa in patients with advanced Parkinson’s disease, as well as for the treatment of early-stage Parkinson’s disease as monotherapy. 

rasagiline is a selective monoamine oxidase-B (MAO-B) inhibitor, which works by inhibiting the enzyme that breaks down dopamine in the brain. By inhibiting the breakdown of dopamine, rasagiline can help increase dopamine levels in the brain, a crucial neurotransmitter involved in regulating movement. 

The use of rasagiline has been shown to improve symptoms of Parkinson’s disease, such as tremors, rigidity, and bradykinesia (slowness of movement). In addition, it has also been shown to have neuroprotective effects, which may slow the progression of Parkinson’s disease.