Zelapar - reduces “off time” in Parkinson’s

Company:

Valeant

Pharmacologic class:

Antiparkinson agent (MAO-B inhibitor)

Active ingredient:

Selegiline 1.25 mg; orally-disintegrating tabs; contains phenylalanine.

Indication:

Adjunct in Parkinson’s disease in patients with deteriorating response to levodopa/carbidopa.

Pharmacology:

Zelapar is an orally disintegrating tablet form of selegiline that disintegrates within seconds after placement on the tongue and which is then rapidly absorbed. Selegiline is absorbed faster from Zelapar (1.25 mg or 2.5 mg dose) than from the swallowed 5-mg selegiline tablet. On a dose-normalized basis, the relative bioavailability of selegiline from Zelapar is greater than from the swallowed formulation.

Selegiline is a monoamine oxidase inhibitor (MAOI) which is relatively selective for MAOI type B over type A. However, selectivity diminishes with increasing dose, and some patients may experience untoward effects associated with MAOI type A inhibition even at recommended doses. When it is given at the recommended dose (up to 2.5 mg/day), patients using this orally disintegrating product will not need to follow strict dietary limitations that restrict the intake of tyramine. However, several cases of hypertensive crises have occurred in patients who took the recommended dose of selegiline as a swallowed product.

Clinical trials:

Zelapar has been shown to be effective in treating Parkinson’s disease only as an adjunct to levodopa/carbidopa in patients with significant “off” periods (average seven hours per day). In a three-month study involving 140 patients with deteriorating Parkinson’s disease, those patients treated with Zelapar had an average of 2.2 hours per day less of self-reported “off” time compared with 0.6 hours with those given placebo.

Adults:

Take (without liquids) in the am before breakfast; do not eat/drink within five minutes (before or after). Place tablet on tongue, do not swallow. ≥16 years: 1.25 mg once daily for at least six weeks; if needed, may increase to max 2.5 mg once daily if tolerated. Do not exceed max dose. Not bioequivalent to other forms of selegiline.

Children:

<16 years: not recommended.

Contraindications:

During or within two weeks of meperidine, MAOIs (e.g., other forms of selegiline). Concomitant tramadol, methadone, propoxyphene, dextromethorphan. Avoid sympathomimetic amines, tricyclics, SSRIs, SNRIs; allow at least 14 days after discontinuing selegiline before starting an SSRI (e.g., fluoxetine), tricyclic, or SNRI; allow five weeks after discontinuing fluoxetine before starting selegiline.

Precautions:

Renal or hepatic impairment. Monitor for melanoma. Elderly (higher risk of orthostatic hypotension). Pregnancy (Cat. C). Nursing mothers: not recommended.

Interactions:

See Contraindications. Caution with CYP3A4 inducers (e.g., phenobarbital, phenytoin, carbamazepine, nafcillin, rifampin). Consider reducing concomitant levodopa/carbidopa dose if dyskinesia occurs.

Adverse reactions:

Postural hypotension (usually transient), dizziness, GI upset, pain, headache, insomnia, rhinitis, stomatitis, hypertension, ECG abnormality, hallucinations.

How supplied:

Tabs—60.

For more information, call 877.361.2719 or visit www.Zelapar.com.

Loading links....
You must be a registered member of Clinical Advisor to post a comment.

Sign Up for Free e-newsletters