zelapar (selegiline HCl) Orally Disintegrating Tablets
Healthcare Professionals
For Healthcare Professionals

 
 
 
 
Pharmacokinetics

Zelapar® (selegiline HCl) delivers MORE active drug at a lower dose than conventional selegiline 5 mg BID oral tablets.

  • Innovative transmucosal drug delivery significantly bypasses the gut and first-pass metabolism
  • Higher plasma levels of active drug, lower levels of amphetamine metabolites

Pharmacokinetic (PK) profile of Zelapar versus conventional selegiline

Zelapar 2.5 mg QD* vs. conventional selegiline
10 mg/day (5 mg BID)

• Peak plasma levels of active drug are more than twice as high and less variable with Zelapar (2.5mg QD)

• Conventional selegiline Tmax = 1 hour
Zelapar Tmax = 15 mins – 4x faster

80–90% reduction in amphetamine metabolites with Zelapar vs. 10 mg conventional selegiline oral tablets

Important safety information

Zelapar is contraindicated in patients with a known hypersensitivity to any formulation of selegiline or any of the inactive ingredients of Zelapar. Zelapar is also contraindicated for use with meperidine and should not be administered with the analgesic agents tramadol, methadone, and propoxyphene. Zelapar should not be used with the antitussive agent dextromethorphan and should not be administered along with other selegiline products. Daily doses of Zelapar should not exceed 2.5 mg/day because of the risks associated with nonselective inhibition of MAO. In general, the combination of Zelapar and tricyclic antidepressants, as well as Zelapar and serotonin reuptake inhibitors, should be avoided. In clinical trials, the incidence of adverse orthostatic hypotension was higher in geriatric patients than in nongeriatric patients. Zelapar may potentiate the dopaminergic side effects of levodopa and may cause or worsen preexisting dyskinesia. Decreasing the dose of levodopa may improve this side effect. Zelapar should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.

The most commonly observed adverse events reported during clinical trials were dizziness, nausea, pain, headache, insomnia, rhinitis, dyskinesia, back pain, skin disorders, stomatitis, and dyspepsia. In addition, 5.2% of patients discontinued Zelapar therapy due to adverse events (versus 1% with placebo).

Please see accompanying complete prescribing information.

Zydis® is a registered trademark of R.P. Scherer Corporation.
Valeant Pharmaceuticals