rasagiline (Azilect)

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.

What brand names are available for rasagiline?

Azilect

Is rasagiline available as a generic drug?

No

Do I need a prescription for rasagiline?

Yes

The most common adverse effects of rasagiline are:

• flu like symptoms,
• headache,
• nausea,
• joint pain,
• upset stomach,
• depression,
• falls,
• constipation,
• postural hypotension (a drop in blood pressure when moving from a lying or sitting position to a sitting or standing position, respectively),
• dry mouth,
• rash,
• hallucinations,
• vomiting, and
• difficulty moving.

Rasagiline also may cause low or high blood pressure. A hypertensive crisis may occur if foods high in tyramine are consumed while taking rasagiline. Tyramine in food usually is broken down in the intestine by MAO-A in the intestinal wall as the tyramine is absorbed into the body. There are no adequate studies in humans to determine whether rasagiline also inhibits MAO-A; however, if MAO-A is inhibited, tyramine ingested in food may enter the body in larger amounts and result in a hypertensive crisis. Foods high in tyramine include those that are aged, fermented, pickled, or smoked. Examples include aged cheeses, air-dried meats, sauerkraut, soy sauce, tap/draft beers and red wines. As a precaution, foods high in tyramine should be avoided when taking rasagiline.

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.

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.

Rasagiline should not be used with sympathomimetic amine drugs such as amphetamines and products containing vasoconstrictors (blood vessel narrowing drugs, for example, pseudoephedrine, ephedrine, phenylpropanolamine, phenylephrine). Severe hypertensive reactions have occurred when such drugs were combined with other MAO inhibitors. Patients taking rasagiline should not be given cocaine or local anesthetics containing sympathomimetic vasoconstrictor drugs. They also should not undergo elective surgery requiring general anesthesia. Rasagiline should be discontinued at least 14 days before surgery. Rasagiline should not be used with other MAO inhibitors because of the risk of a hypertensive crisis. Rasagiline should be discontinued at least 14 days before starting other MAO inhibitors.

There are no adequate studies of rasagiline in pregnant women. Rasagiline should only be used in pregnant women if the benefit is felt to justify the unknown risk.

It is not known whether rasagiline is secreted in human milk.

What preparations of rasagiline are available?

Tablets: 0.5 and 1 mg.

How should I keep rasagiline stored?

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