rasagiline, Azilect

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GENERIC NAME: rasagiline


DRUG CLASS AND MECHANISM: Rasagiline is an oral drug that is used for treating Parkinson's disease. It belongs to a class of drugs called monoamine oxidase inhibitors (MAO) that also includes selegiline and tranylcypromine. Monoamine oxidase is an enzyme that breaks down serotonin, norepinephrine, dopamine, tyramine and similar chemicals that serve as neurotransmitters, chemicals that nerves use to communicate with one another. There are two types of monoamine oxidase enzymes, MAO-A and MAO-B. Monoamine oxidase inhibitors inhibit one or both enzymes resulting in increased levels of the chemicals normally broken down by MAO-A or MAO-B. Rasagiline inhibits MAO-B, but it is not clear whether rasagiline also inhibits MAO-A. Rasagiline's exact mechanism of action is not known; however, by inhibiting MAO-B rasagiline reduces the breakdown of dopamine resulting in increased levels of dopamine in the brain. Increased dopamine levels alleviate the symptoms of Parkinson's disease. Rasagiline was approved by the FDA in May 2006.



PREPARATIONS: Tablets: 0.5 and 1 mg.

STORAGE: Tablets should be stored at 15-30 C (59-86 F).

PRESCRIBED FOR: Rasagiline is used alone or in combination with levodopa to treat signs and symptoms of Parkinson's disease.

DOSING: The recommended dose of rasagiline is 1 mg once daily when used alone (monotherapy). When combined with levodopa the recommended starting dose is 0.5 mg once daily. The dose may be increased to 1 mg once daily if the response is not adequate. Patients with mild liver disease should not use more than 0.5 mg daily. It should not be used by patients with moderate or severe liver disease. Tyramine rich food, beverages and supplements should be avoided while taking rasagiline.

DRUG INTERACTIONS: Rasagiline is eliminated by enzymes in the liver. Ciprofloxacin (Cipro, Cipro XR, Proquin XR) inhibits the enzymes in the liver that eliminate rasagiline, thereby increasing blood levels and possibly side effects of rasagiline. Patients taking ciprofloxacin should not exceed 0.5 mg daily of rasagiline.

Rasagiline should not be administered with antidepressants that increase serotonin levels. Combining rasagiline with such antidepressants may lead to excessive levels of serotonin and a fatal condition called the serotonin syndrome. Examples of antidepressants to avoid include selective serotonin uptake inhibitors (for example, fluoxetine [Prozac, Sarafem], sertraline [Zoloft]), tricyclic antidepressants (for example, amitriptyline [Elavil, Endep]), serotonin-norepinephrine uptake inhibitors (for example, venlafaxine [Effexor]) and other MAO inhibitors (for example, selegiline, tranylcypromine). Rasagiline should be discontinued at least 14 days before initiating treatment with antidepressants that increase serotonin levels.

Due to its long half-life, fluoxetine should be discontinuedhadone, mirtazapine [Remeron Soltab], cyclobenzaprine [Flexeril, Amrix] dextromethorphan and St. John's Wort. Serious reactions, including the serotonin syndro at least 5 weeks before initiating rasagiline.

 Rasagiline should not be used with meperidine, propoxyphene [Darvon, Darvon-N, Dolene], tramadol [Ultram, Ultram ER], metme, have occurred when other MAO inhibitors were combined with some of these drugs, and there is concern that rasagiline may cause similar serious reactions.

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