Zelapar (selegiline) is an oral adjunctive therapy used along with carbidopa and levodopa to treat symptoms of Parkinson’s disease, particularly in patients who experience a deteriorating response to levodopa/carbidopa treatment. Those declining responses include “end-dose” type fluctuations (when the drug wears off), “on-off” symptoms (sudden events when medication works or does not work), or dyskinesias (spontaneous, involuntary movements).
Zelapar is an oral tablet containing a chemical called selegiline hydrochloride that prevents the breakdown of dopamine in the brain and helps levodopa work for a longer period of time.
How Zelapar works
The mechanisms of how Zelapar provides benefits in the treatment of Parkinson’s disease are not fully understood. One main mechanism that is speculated is the selegiline-mediated inhibition of monoamine oxidase type B (MAO-B), an enzyme that catalyzes the breakdown of dopamine in the brain, which would increase the net amount of dopamine available.
In addition, there is evidence that selegiline may act through other mechanisms to increase dopaminergic activity, including interfering with dopamine re-uptake at the junction between nerve cells.
Dosage and administration
The tablet is available for oral administration (dissolved in the mouth) at a strength of 1.25 mg.
Zelapar treatment should be initiated with 1.25 mg given once a day for at least six weeks. If the patient is able to tolerate the drug. But if the desired benefit has not been achieved after six weeks, the dose may be increased to 2.5 mg once a day.
Zelapar should be taken in the morning before breakfast; the tablet should be placed on the tongue and allowed to dissolve. Patients should avoid eating, drinking or mouth-rinsing for five minutes before and after taking it to allow the medicine to be absorbed. Zelapar disintegrates within seconds after being placed on the tongue.
The drug should not be discontinued abruptly as this may cause severe side effects. A missed dose should be skipped to avoid overdose.
While taking Zelapar, alcohol should be avoided. Foods rich in tyramine, a chemical that induces the release of dopamine from nerve cells, should be avoided while taking Zelapar, as should over-the-counter medicines that contain tyramine. Examples of tyramine-rich foods include air-dried, aged or fermented meats, beef, poultry, fish or liver, unpasteurized beer, aged cheeses, soybeans, soy sauce, sauerkraut, and yeast extracts. Consuming tyramine while using Zelapar can raise blood pressure to dangerous levels, causing life-threatening side effects.
Serious drug interactions may occur when certain medications are used at the same time as Zelapar. The drug is contraindicated in patients with a known hypersensitivity to any formulation of selegiline, or to any of Zelapar’s inactive ingredients.
It should not be used if the patient has taken fluoxetine (Prozac) within the past five weeks. The drug also should not be used along with other selegiline products such as Eldepryl because it may lead to a severe increase in blood pressure. Zelapar should not be administered with analgesic agents such as tramadol, methadone, and propoxyphene.
Zelapar also is contraindicated for use with meperidine, cyclobenzaprine (Flexeril), antidepressants (citalopram, duloxetine etc.), MAO inhibitors (linezolid, rasagiline etc.), and cough medicines containing dextromethorphan.
The contraindications that apply to levodopa also must be taken into account.
Warnings and precautions
Zelapar should not be used at daily doses exceeding those recommended (2.5 mg/day) because of the risks associated with non-selective inhibition of MAO, which may lead to high blood pressure. Zelapar also may cause irritation of the buccal mucosa.
The drug may increase the dopaminergic side effects of levodopa and may cause or exacerbate pre-existing involuntary movements.
Zelapar should be taken with caution by patients with certain conditions such as liver or kidney disease, high blood pressure, and phenylketonuria.
Patients should be cautioned about the possibility of developing hallucinations.
Although the safety of Zelapar during pregnancy or breastfeeding is not known, the doctor should be informed and caution should be taken for its use in these circumstances.
The commonly observed side effects of Zelapar include dizziness, nausea, abdominal pain, constipation, sleep problems, involuntary movements, back pain, and mouth sores or ulcers.
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