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:
- dizziness
- abdominal pain
- dry mouth
- nausea
- stomach upset
- trouble sleeping (insomnia)
- headache
- weakness
- runny or stuffy nose
- back pain
- constipation
- redness/pain/swelling of the mouth/throat
- mouth sores or ulcers, and
- pain with swallowing
Tell your doctor if you have serious side effects of Zelapar including:
- fainting,
- loss of balance,
- mental/mood changes (e.g., agitation, confusion, depression, hallucinations),
- unusual strong urges (such as increased gambling, increased sexual urges),
- worsening muscle stiffness or twitching,
- changes in sexual ability or interest,
- increased shaking (tremor),
- swollen ankles or legs,
- difficulty urinating,
- unusual weight gain,
- easy bleeding or bruising,
- black or tarry stools, or
- vomit that looks like coffee grounds.
What is the dosage for Zelapar?
- Initiate treatment with 1.25 mg given once a day for at least 6 weeks. After 6 weeks, the dose may be increased to 2.5 mg given once a day if a desired benefit has not been achieved and the patient is tolerating
Zelapar. - There is no evidence that doses greater than 2.5 mg a day provide additional benefit, and they should ordinarily be avoided because of the potential increased risk of adverse events.
- Take Zelapar in the morning before breakfast and without liquid. Patients should avoid ingesting food or liquids for 5 minutes before and after taking
Zelapar. - Patients should not attempt to push Zelapar through the foil backing. Patients should PEEL BACK the backing of one or two blisters (as prescribed) with dry hands, and GENTLY remove the tablet(s). Patients should IMMEDIATELY place the
Zelapar tablet(s) on top of the tongue where it will disintegrate in seconds.
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).
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.