Pharmacy Editor: Jay W. Marks
GENERIC NAME: rasagiline
BRAND NAME: Azilect
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.
PRESCRIPTION: Yes
GENERIC AVAILABLE: No
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 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.
Tyramine rich food, beverages and supplements should be avoided while taking
rasagiline.
DRUG INTERACTIONS: Rasagiline is eliminated by enzymes in the liver.
Ciprofloxacin inhibits the enzymes in the liver that eliminate rasagiline,
thereby increasing blood levels and possibly side effects 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 be avoided include selective serotonin
uptake inhibitors (e.g., fluoxetine, sertraline), tricyclic antidepressants
(e.g., amitriptyline), serotonin-norepinephrine uptake inhibitors (e.g.,
venlafaxine) and other MAO inhibitors (e.g., 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 discontinued at least 5 weeks before initiating rasagiline.
Rasagiline should not be used with meperidine, propoxyphene, tramadol,
methadone, mirtazapine, cyclobenzaprine, dextromethorphan and St. John's Wort.
Serious reactions, including the serotonin syndrome, 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, e.g., 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.
PREGNANCY: 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.
NURSING MOTHERS: It is not known whether rasagiline is secreted in human
milk.
SIDE EFFECTS: Adverse events reported in clinical studies include headache,
nausea, joint pain, upset stomach, depression, falls, constipation, postural
hypotension (a drop in blood pressure when going from a lying or sitting
position to a sitting or standing position, respectively), dry mouth, rash,
hallucinations, vomiting and difficulty moving.
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.
Last Editorial Review: 7/19/2006
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
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