Selegiline Hydrochloride (3 brand names, 3 dosage forms, 1 route)
Available dosage forms: TABLET, CAPSULE, TABLET, ORALLY DISINTEGRATING.
Routes of administration: ORAL.
Brand Names
- ELDEPRYL
- SELEGILINE HYDROCHLORIDE
- ZELAPAR
Indications and Usage
ZELAPAR is indicated as an adjunct in the management of patients with Parkinson’s disease being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. There is no evidence from controlled studies that ZELAPAR has any beneficial effect in the absence of concurrent levodopa therapy [see Clinical Studies (14 )].
Contraindications
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 medications [see Warnings and Precautions (5.2)]. • Concomitant use of other drugs in the monoamine oxidase inhibitor (MAOI) class or other drugs that are potent inhibitors of monoamine oxidase, including linezolid), because of an increased risk for hypertensive crisis [see Warnings and Precautions (5.1)]. At least 14 days should elapse between discontinuation of ZELAPAR and initiation of treatment with any MAO inhibitor. •Concomitant use of St. John’s wort or cyclobenzaprine (a tricyclic muscle relaxant). •Concomitant use of dextromethorphan, because of reported episodes of psychosis or bizarre behavior.
Adverse Reactions
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-Like Behavior [see Warnings and Precautions (5.6)] •Impulse Control/Compulsive Behaviors [see Warnings and Precautions (5.7)] •Withdrawal Emergent Hyperpyrexia and Confusion [see Warnings and Precautions (5.8)] •Irritation of the Buccal Mucosa [see Warnings and Precautions (5.9)] •Risk for Patients with Phenylketonuria [see Warnings and Precautions (5.10)]
Mechanism of Action
Selegiline is an irreversible inhibitor of monoamine oxidase (MAO), which regulates the metabolic degradation of catecholamines and serotonin in the central nervous system and peripheral tissues. At recommended doses, selegiline is selective for MAO type B (MAO-B), the major form in the brain. Inhibition of MAO-B activity, by blocking the catabolism of dopamine, may result in increased dopamine levels; however, there is evidence that selegiline may act through other mechanisms to increase dopaminergic activity.