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Zelapar for Parkinson’s Disease: Drug Side Effects & Warnings

Date

Generic drug: generic

Brand name: Zelapar

What is Zelapar, and how does it work?

Zelapar (selegiline hydrochloride) is an enzyme blocker (MAO inhibitor) that works by slowing the breakdown of certain natural substances in the brain (neurotransmitters such as dopamine, norepinephrine, and serotonin) used together with other medicines to treat symptoms of Parkinson’s disease.

What are the side effects of Zelapar?

Common side effects of Zelapar include:

Tell your doctor if you have serious side effects of Zelapar including:

What is the dosage for Zelapar?

Patients With Hepatic Impairment

  • In patients with mild to moderate hepatic disease (Child-Pugh score 5 to
    9), the daily dose of Zelapar should be reduced (from 2.5 to 1.25 mg daily),
    depending on the clinical response. Zelapar is not recommended in patients
    with severe hepatic impairment (Child-Pugh score greater than 9).

Patients With Renal Impairment

  • No dose adjustment of Zelapar is required in patients with mild to
    moderate renal impairment (creatinine clearance [CLcr] 30 to 89 mL/min). The
    maintenance dose of Zelapar (1.25 mg or 2.5 mg) is determined by the
    individual clinical response.
  • Zelapar is not recommended in patients with severe renal impairment and
    patients with end-stage renal disease [ESRD] (creatinine clearance [CLcr]
    <30 mL/min).




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What drugs interact with Zelapar?

Opioid Drugs

  • Because serious, sometimes fatal reactions have been precipitated with
    concomitant use of opioid drugs (e.g., meperidine and its derivatives,
    methadone, or tramadol) and MAOIs, including selective MAO-B inhibitors,
    concomitant use of these drugs with Zelapar is contraindicated. At least 14 days should elapse between discontinuation of
    Zelapar and initiation of treatment with these drugs.

Dextromethorphan

  • The combination of MAO inhibitors and dextromethorphan has been reported
    to cause brief episodes of psychosis or bizarre behavior. Therefore, in view
    of Zelapar’s MAO inhibitory activity, dextromethorphan should not be used
    concomitantly with Zelapar.

MAO Inhibitors

  • Zelapar is contraindicated for concomitant use with other drugs in the
    MAOI class or other drugs that are potent inhibitors of monoamine oxidase
    (including linezolid, an oxazolidinone antibacterial, which also has
    reversible nonselective MAO inhibition activity) because of the increased
    risk for hypertensive crisis. At least 14 days should elapse between discontinuation of
    Zelapar and initiation of treatment with other MAOIs.

Sympathomimetic Medications

  • Uncontrolled hypertension, including hypertensive crisis, has been reported when taking the recommended dose of swallowed selegiline and a sympathomimetic medication (ephedrine).

Tyramine/Selegiline Interaction

  • The enzyme, monoamine oxidase (MAO) (primarily type A), in the gastrointestinal tract and liver provides protection from ingested amines (e.g., tyramine) that, if absorbed, have the capacity to cause uncontrolled hypertension (tyramine reaction). If MAO is inhibited in the gastrointestinal tract and liver, ingestion of exogenous amines contained in some foods such as fermented cheese, herring, or over-the-counter cough/cold medicines may be absorbed systemically causing release of norepinephrine and a rise in systemic blood pressure with the potential for uncontrolled hypertension. Selective MAO-B inhibitors lose their selectivity for MAO-B when taken in doses higher than recommended. Non-selective MAOA inhibitors or MAO-B inhibitors in higher than recommended doses may result in MAO-A inhibition in the gastrointestinal tract and liver.
  • Results of a tyramine challenge study indicate that Zelapar is
    relatively selective for MAO-B at the recommended dose. In most cases, there
    is no need for dietary tyramine restriction in patients prescribed Zelapar at the recommended dose. Because the selectivity for inhibiting MAO-B diminishes as the dose of
    Zelapar is increased above the recommended daily dose, patients should not take more than 2.5 mg of
    Zelapar daily.
  • Reports of hypertensive reactions have occurred in patients who ingested tyramine-containing consumables (i.e., food or drink) while receiving swallowed selegiline at the recommended dose (a dose believed to be relatively selective for MAOB). Hypertensive crisis has also been reported with
    Zelapar use that was not above the recommended dosing.
  • Uncontrolled hypertension has been reported when taking the recommended dose of swallowed selegiline and a sympathomimetic medication (ephedrine).

Tricyclic Antidepressants And Selective Serotonin Reuptake Inhibitors

  • Severe toxicity has also been reported in patients receiving the
    combination of tricyclic antidepressants and swallowed selegiline, or
    selective serotonin reuptake inhibitors and swallowed selegiline.

Drugs That Induce CYP450

  • Adequate studies have not been done investigating the effect of CYP3A4 inducers on selegiline. Drugs that induce CYP3A4 (e.g., phenytoin, carbamazepine, nafcillin, phenobarbital, and rifampin) should be used with caution.

Dopaminergic Antagonists

  • It is possible that dopamine antagonists, such as antipsychotics or metoclopramide, could diminish the effectiveness of
    Zelapar.

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Is Zelapar safe to use while pregnant or breastfeeding?

  • There are no adequate data on the developmental risk associated with the use of
    Zelapar in pregnant women.
  • In animal studies, administration of selegiline during pregnancy was associated with developmental toxicity (decreased embryofetal and postnatal offspring growth and survival) at doses greater than those used clinically.
  • There are no data on the presence of selegiline or its metabolites in human milk, the effects on the breastfed infant, or the effects on milk production.
  •  Because of the potential for serious adverse reactions in breastfed infants from
    Zelapar, including the potential for hypertensive reactions, advise a woman that breastfeeding is not recommended during treatment with
    Zelapar and for 7 days after the final dose.





QUESTION


Parkinson’s disease is only seen in people of advanced age.
See Answer

Medically Reviewed on 6/29/2021

References


All sections courtesy of the U.S. Food and Drug Administration

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