Rasagiline

Rasagiline is a monoamine oxidase (MAO) type B inhibitor. It works by inhibiting the accumulation of certain natural substances in the brain. Rasagiline is used to treat Parkinson's disease symptoms, either alone or in combination with other medications. Parkinson's disease is a condition in which certain regions of the brain gradually weaken over time. Parkinson's symptoms include involuntary shaking of specific body parts, sluggish movement, and stiff and inflexible muscles. Parkinson's patients experience decreases in dopamine levels as the nerve cells that produce dopamine die. It increases the amount of dopamine, a chemical messenger that controls brain movements. Thus, it contributes to the treatment of Parkinson's disease. The FDA approved rasagiline in 2006.

BRAND NAME:

Azilect – It contains the active ingredients of rasagiline. It is available in tablets used to treat Parkinson’s disease.

MECHANISM OF ACTION:

Rasagiline is a monoamine oxidase type B inhibitor that raises dopamine levels in the striatum. Rasagiline's beneficial effects in a model of dopaminergic motor dysfunction are likely mediated by elevated dopamine levels and subsequent increased dopaminergic activity.

PHARMACOKINETICS:

Absorption: Rasagiline is rapidly absorbed by oral administration. The absolute bioavailability of rasagiline is 36%.

Distribution: The total mean volume of distribution of rasagilin is 87 L.

Metabolism: Rasagiline undergoes almost biotransformation in the liver prior to excretion. The rasagiline metabolism depends on the Cytochrome P450 system, with CYP1A2 being the major isoenzyme involved in rasagiline metabolism.

Excretion: Rasagiline is excreted primarily in urine and through feces.

PHARMACODYNAMICS:

Rasagiline is a propargylamine that acts as an irreversible inhibitor of monoamine oxidase. MAO, a flavin-containing enzyme, regulates the metabolic degradation of catecholamines and serotonin in the central and peripheral nervous systems.

DOSAGE AND ADMINISTRATION:

Rasagiline comes as a tablet to take by orally. It is usually taken once a day with or without food.

It is available in the form of tablets with the strengths of 0.5mg and 1mg.

DRUG INTERACTIONS:

Drug interactions of rasagiline may includes

Pain killers – amitriptyline and tramadol
Anti-depressant drugs – sertraline, bupropion and mirtazapine

CONTRAINDICATIONS:

Rasagiline tablets are not recommended for use with meperidine, tramadol, methadone, propoxyphene, or MOA inhibitors, including other selective MAO-B inhibitors, due to the risk of serotonin syndrome. At least 14 days should pass between the discontinuation of rasgiline tablets and the start of treatment with these medications. Rasagiline tablets are not recommended for use with dextromethorphan due to the risk of psychosis.

SIDE EFFECTS:

Side effects of rasagiline may include

Joint pain
Vomiting
Mild headache
Nausea
Diarrhea
Constipation
Stomach pain
Fever
Weight loss
Flu-like symptoms
Dry mouth
Loss of appetite
Sweating
Swollen gums
Lack of energy
Rash
Abnormal dreams
Depression
Blurred vision
Chest pain
Seizures
Confusion
Unconsciousness
Faintness
Blurred vision
Severe headache
Numbness of arms
Extreme restlessness
Difficult speech

OVERDOSE:

Symptoms of overdose may include

Drowsiness
Faintness
Hyperactivity
Severe headache
Irritability
Confusion
Seizures
Diarrhea
Sweating
Irritability
Agitation
Difficulty in opening the mouth
Fast or irregular heartbeats
Cool skin
Shivering

TOXICITY:

Excessive overdose of rasagiline may cause severe CNS toxicity with hyperpyrexia has been reported with the combined treatment of an antidepressant and rasagiline. Avoid combination within 14 days of MAOI use. Rasagiline increases the toxicity of benzhydrocodone/ acetaminophen by serotonin levels. Avoid or use alternative drugs.

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