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Home > Drug Category > Parkinson's Disease, Dopamine Agonists > Zelapar and Equivalent

Zelapar (Selegiline) Information

Zelapar (selegiline) is a drug belonging to the class of Monoamine Oxidase B (MAO-B) inhibitors. It is indicated as adjunctive therapy for the treatment of Parkinson's disease (PD) in patients who are currently receiving levodopa/carbidopa and are experiencing motor fluctuations, or "wearing off." Unlike the standard oral tablet form of selegiline (Eldepryl), Zelapar is an Orally Disintegrating Tablet (ODT) that dissolves rapidly on the tongue. The mechanism of action centers on selectively and irreversibly inhibiting the enzyme MAO-B, which breaks down dopamine in the central nervous system. By blocking this enzyme, Zelapar increases and prolongs the availability of dopamine to stimulate receptors, thereby extending the effects of levodopa and providing smoother control of motor symptoms. The ODT formulation is designed for absorption through the buccal (cheek) mucosa, which may bypass first-pass liver metabolism and reduce the production of potentially toxic amphetamine metabolites.

Treatment is typically initiated at 1.25 mg once daily for at least 6 weeks, taken in the morning before breakfast. The dose may be increased to a maximum of 2.5 mg once a day if a desired benefit has not been achieved and the patient is tolerating the medication. The ODT must be taken without liquid. Patients should be instructed to peel back the foil from the blister pack (do not push it through) and gently place the tablet on the tongue, where it will dissolve in seconds. To ensure proper absorption, patients must avoid eating or drinking anything for 5 minutes before and after taking the dose.

Zelapar Side Effects

Zelapar's most frequent side effects are related to the increased availability of dopamine, particularly when used in combination with levodopa/carbidopa. These include excessive involuntary movements (dyskinesia), which may necessitate a reduction in the levodopa dose, as well as dizziness, headache, insomnia, and confusion. Gastrointestinal issues such as dry mouth, nausea, and stomach pain are also common. Due to the ODT formulation, some patients may also experience localized side effects such as mouth/buccal irritation (e.g., soreness, inflammation, or ulcers on the tongue or in the mouth/throat). More serious side effects can occur, often related to drug interactions or elevated monoamine levels. If any of the following symptoms are experienced, the patient should stop taking the medication and seek immediate medical attention:

• Hallucinations/Psychotic-Like Behaviour.

• Hypertensive Crisis: Dangerously high blood pressure characterized by a severe headache, blurred vision, pounding in the neck or ears, chest pain, or severe anxiety. This risk increases substantially at doses above the recommended 2.5 mg daily.

• Neuroleptic Malignant Syndrome (NMS): A rare but potentially fatal reaction characterized by high fever, severe muscle rigidity, altered mental status, and autonomic dysfunction.

• New or Worsening Impulse Control/Compulsive Behaviours (e.g., intense urges for gambling, shopping, or sexual activity).

• Serotonin Syndrome: A potentially life-threatening condition marked by agitation, confusion, hallucinations, rapid heart rate, muscle tremors, severe sweating, and loss of coordination.

• Severe Worsening of Dyskinesia: Debilitating, uncontrolled involuntary movements.

Precautions

A thorough review of all concurrent medications is crucial before starting Zelapar. It is absolutely contraindicated for use in combination with: opioid drugs (including meperidine, tramadol, and methadone), other MAO inhibitors, antidepressants (SSRIs, SNRIs, and most TCAs), and other serotonin-enhancing agents such as dextromethorphan (in cough/cold medicines), St. John's Wort, and cyclobenzaprine. Patients must be carefully monitored, particularly when initiating therapy or increasing the dose, for signs of NMS or severe hypotension. The ODT formulation contains phenylalanine (a component of aspartame) and is thus contraindicated in patients with Phenylketonuria (PKU). Caution is also advised for patients with pre-existing psychoses, severe heart disease, or peptic ulcer disease. While Zelapar ODT at the recommended dose of 2.5 mg daily is generally safe regarding food interactions, the selectivity for MAO-B may be lost at higher doses. Therefore, the safe use of doses above 2.5 mg daily without a strict tyramine-restricted diet has not been established. Finally, patients should be warned that Zelapar, like other dopaminergic drugs, may cause sudden sleep onset during activities of daily living, and caution should be exercised when driving or operating dangerous machinery.

Do I need a prescription to order Zelapar?

Yes, a prescription is required from your physician to order Zelapar.