ZELAPAR

Absorption ZELAPAR disintegrates within seconds after placement on the tongue and is rapidly absorbed. Detectable levels of selegiline from ZELAPAR have been measured at 5 minutes after administration, the earliest time point examined. Selegiline is more rapidly absorbed from the 1.25 or 2.5 mg dose of ZELAPAR (T max range: 10-15 minutes) than from the swallowed 5 mg selegiline tablet (T max range: 40-90 minutes). Mean (SD) maximum plasma concentrations of 3.34 (1.68) and 4.47 (2.56) ng/mL are r...

The effectiveness of ZELAPAR as an adjunct to levodopa/carbidopa in the treatment of Parkinson’s disease was established in a multicenter, randomized, placebo-controlled trial (n=140; 94 received ZELAPAR, 46 received placebo) of three months’ duration. Patients randomized to ZELAPAR received a daily dose of 1.25 mg for the first 6 weeks, and a daily dose of 2.5 mg for the last 6 weeks. All patients were treated with concomitant levodopa products and could additionally have been on concomitant dopamine agonists, anticholinergics, amantadine, or any combination of these during the trial. COMT (c...

The following adverse reactions are discussed in more detail in the Warnings and Precautions section of labeling:

• Risk for Hypertension [see Warnings and Precautions (5.1) ]
• Risk of Serotonin Syndrome [see Warnings and Precautions (5.2) ]
• Falling Asleep During Activities of Daily Living and Somnolence [see Warnings and Precautions (5.3) ]
• Hypotension/Orthostatic Hypotension [see Warnings and Precautions (5.4) ]
• Dyskinesia [see Warnings and Precautions (5.5) ]
• Hallucinations/Psychotic...

ZELAPAR is contraindicated in patients with:

• Concomitant use of opioid drugs (e.g., meperidine, tramadol, or methadone). Serotonin syndrome, a potentially serious condition, which can result in death, has been reported with concomitant use of meperidine (e.g., Demerol and other trade names). At least 14 days should elapse between discontinuation of ZELAPAR and initiation of treatment with these ...

• May cause hypertension above 2.5 mg/day (5.1)
• May cause serotonin syndrome when used with antidepressants (5.2)
• May cause falling asleep during activities of daily living (5.3)
• May cause hypotension/orthostatic hypotension (5.4)
• May cause or exacerbate dyskinesia (5.5)
• May cause hallucinations and psychotic-like behavior (5.6)
• May cause problems with impulse control and compulsive behaviors (5.7)
• Abrupt discontinuation may cause hyperpyrexia and confusion (5.8)
• May cause irrita...

7 DRUG INTERACTIONS 7.1 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 [see Contraindications (4) and Warnings and Precautions (5.2)] . At least 14 days sho...