se-LE-ji-leen

• Management of Parkinson’s disease (with levodopa or levodopa/carbidopa) in patients who fail to respond to levodopa/carbidopa alone.

• Following conversion by MAO to its active form, selegiline inactivates MAO by irreversibly binding to it at type B (brain) sites.
• Inactivation of MAO leads to increased amounts of dopamine available in the CNS.

• Increased response to levodopa/dopamine therapy in Parkinson’s disease.

Absorption: Appears to be well absorbed following oral administration.

Distribution: Widely distributed.

Metabolism/Excretion: Metabolism involves some conversion to amphetamine and methamphetamine. 45% excreted in urine as metabolites.

Half-life: Unknown; orally disintegrating tablets 1.3 hr.

Contraindicated in:

• Hypersensitivity
• Major psychotic disorder
• Concurrent use of opioids, other MAO inhibitors, St. John's wort, cyclobenzaprine, or dextromethorphan
• Lactation: Lactation.

Use Cautiously in:

• Doses >10 mg/day (tablets/capsules) or >2.5 mg/day (orally disintegrating tablets) (↑ risk of hypertensive reactions with tyramine-containing foods and some medications)
• History of peptic ulcer disease
• Phenylketonuria (orally disintegrating tablets only)
• OB: Safety not established in pregnancy
• Pedi: Safety and effectiveness not established in children
• Geri: ↑risk of orthostatic hypotension in older adults.

CV: orthostatic hypotension.

GI: nausea, abdominal pain, dry mouth.

Neuro: SEROTONIN SYNDROME, aggression, agitation, confusion, delirium, delusions, disorientation, dizziness, fainting, hallucinations, insomnia, paranoia, psychosis, sedation, urges (gambling, sexual), vivid dreams.

Drug-Drug:

• Use with opioid analgesic (e.g. meperidine) or cyclobenzaprine may ↑ risk of serotonin syndrome; concurrent use contraindicated. Selegiline should be discontinued for 2 wk before initiating any of these medications.
• Use with other MAO inhibitors, including linezolid, may ↑ risk of hypertensive crises; concurrent use contraindicated. Selegiline should be discontinued for 2 wk before initiating any other medication with MAO inhibitor properties.
• Use with products containing dextromethorphan may lead to episodes of psychosis or bizarre behavior; concurrent use contraindicated.
• Drugs that affect serotonergic neurotransmitter systems, including tricyclic antidepressants, SSRIs, SNRIs, fentanyl, buspirone, amphetamines, and triptans may ↑ risk of serotonin syndrome; avoid concurrent use with any antidepressant. Selegiline should be discontinued for 14 days before initiating any antidepressant. Fluoxetine should be discontinued for 5 wk before initiating selegiline.
• May initially ↑ risk of side effects (primarily dyskinesia) of levodopa/carbidopa (dose of levodopa/carbidopa may need to be ↓ by 10–30%).
• Antipsychotics and metoclopramide may ↓ effectiveness.

Drug-Natural Products:

• Use with St. John's wort may ↑ risk of serotonin syndrome; concurrent use contraindicated.

Drug-Food:

• Doses >10 mg/day (tablets/capsules) or >2.5 mg/day (orally disintegrating tablets) may produce hypertensive reactions with tyramine-containing foods (see Appendix M).

• PO (Adults): Capsules or tablets — 5 mg twice daily with breakfast and lunch (some patients may require further dividing of doses — 2.5 mg 4 times daily). Orally disintegrating tablets — 1.25 mg once daily for 6 wk. After 6 wk, may ↑ to 2.5 mg once daily if effect not achieved and patient is tolerating medication.

• Do not confuse selegiline with Salagen (pilocarpine). Do not confuse Zelapar (selegiline) with Zyprexa (olanzapine).
  • An attempt to reduce the dose of levodopa/carbidopa by 10–30% may be made after 2–3 days of selegiline therapy.
• PO: Administer 5-mg tablet with breakfast and lunch.
  • Administer orally disintegrating tablets in the morning, before breakfast and without liquid. Remove tablet gently from blister pack with clean, dry hands immediately before administering. Do not attempt to push tablet through backing. Tablet will disintegrate within sec when placed on tongue. Avoid food or liquid within 5 min of administering orally disintegrating tablets.

Eldepryl, Zelapar

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: monoamine oxidase type b inhibitors

(Generic available)

• Capsules: 5 mg;
• Tablets: 5 mg;
• Orally disintegrating tablets (contain phenylalanine) (grapefruit-flavor): 1.25 mg;

(onset of beneficial effects in Parkinson’s disease)

• Assess patient for signs and symptoms of Parkinson’s disease (tremor, muscle weakness and rigidity, ataxic gait) prior to and during therapy.
• Assess BP periodically during therapy.

• Instruct patient to take medication as directed. Take missed doses as soon as possible, but not if late afternoon or evening or almost time for next dose. Do not double doses. Caution patient that taking more than the prescribed dose may increase side effects and place patient at risk for hypertensive crisis if foods containing tyramine are consumed (see Appendix M).
• Advise patients taking selegiline 20 mg/day to avoid large amounts of tyramine-containing foods (see Appendix M), alcoholic beverages, large quantities of caffeine-containing beverages, or OTC or herbal cough or cold medications.
• Caution patient and caregiver that selegiline may cause drowsiness and dizziness. Monitor and assist with ambulation and caution patient to avoid driving and other activities requiring alertness until response to medication is known.
• Inform patient and family of the signs and symptoms of MAO inhibitor–induced hypertensive crisis (severe headache, chest pain, nausea, vomiting, photosensitivity, enlarged pupils). Advise patient to notify health care professional immediately if severe headache or any other unusual symptoms occur.
• Caution patient to change positions slowly to minimize orthostatic hypotension.
• Advise patient to notify health care professional of signs and symptoms of serotonin syndrome (mental status changes [agitation, hallucinations, delirium, and coma], autonomic instability [tachycardia, labile BP, dizziness, diaphoresis, flushing, hyperthermia], neuromuscular changes [tremor, rigidity, myoclonus, hyperreflexia, incoordination], seizures, and/or gastrointestinal symptoms [nausea, vomiting, diarrhea]).
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Advise patient to notify health care professional if agitation, aggression, delirium, hallucinations, new or increased gambling, sexual, or other intense urges occur.
• Advise patient that increasing fluids, sugarless gum or candy, ice, or saliva substitutes may help minimize dry mouth. Consult health care professional if dry mouth continues for >2 wk.
• Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected. Advise patient to avoid breastfeeding during and for 7 days after final dose.

• Improved response to levodopa/carbidopa in patients with Parkinson’s disease.

NDC Code^*

• 0187- Valeant Pharmaceuticals North America LLC
  • 0187-0453- ZELAPAR
    • 0187-0453-02- 6 POUCH in 1 CARTON (0187-0453-02) > 10 TABLET, ORALLY DISINTEGRATING in 1 POUCH

• 16571- Rising Pharmaceuticals, Inc.
  • 16571-659- Selegiline Hydrochloride
    • 16571-659-06- 60 CAPSULE in 1 BOTTLE (16571-659-06)

• 16571- Rising Pharmaceuticals, Inc.
  • 16571-659- Selegiline Hydrochloride
    • 16571-659-50- 500 CAPSULE in 1 BOTTLE (16571-659-50)

• 49502- Mylan Specialty L.P.
  • 49502-900- EMSAM
    • 49502-900-05- 5 POUCH in 1 CARTON (49502-900-05) > 1 PATCH in 1 POUCH (49502-900-11) > 24 h in 1 PATCH

• 49502- Mylan Specialty L.P.
  • 49502-900- EMSAM
    • 49502-900-30- 30 POUCH in 1 CARTON (49502-900-30) > 1 PATCH in 1 POUCH (49502-900-01) > 24 h in 1 PATCH

• 49502- Mylan Specialty L.P.
  • 49502-901- EMSAM
    • 49502-901-30- 30 POUCH in 1 CARTON (49502-901-30) > 1 PATCH in 1 POUCH (49502-901-01) > 24 h in 1 PATCH

• 49502- Mylan Specialty L.P.
  • 49502-902- EMSAM
    • 49502-902-30- 30 POUCH in 1 CARTON (49502-902-30) > 1 PATCH in 1 POUCH (49502-902-01) > 24 h in 1 PATCH

• 50090- A-S Medication Solutions
  • 50090-2918- Selegiline Hydrochloride
    • 50090-2918-0- 4 TABLET in 1 BOTTLE (50090-2918-0)

• 60429- Golden State Medical Supply, Inc.
  • 60429-019- SELEGILINE HYDROCHLORIDE
    • 60429-019-60- 60 CAPSULE in 1 BOTTLE (60429-019-60)

• 60429- Golden State Medical Supply, Inc.
  • 60429-176- Selegiline Hydrochloride
    • 60429-176-60- 60 TABLET in 1 BOTTLE (60429-176-60)

• 60505- Apotex Corp.
  • 60505-0055- SELEGILINE HYDROCHLORIDE
    • 60505-0055-1- 60 CAPSULE in 1 BOTTLE (60505-0055-1)

• 60505- Apotex Corp.
  • 60505-0055- SELEGILINE HYDROCHLORIDE
    • 60505-0055-2- 1000 CAPSULE in 1 BOTTLE (60505-0055-2)

• 60505- Apotex Corp.
  • 60505-0055- SELEGILINE HYDROCHLORIDE
    • 60505-0055-3- 500 CAPSULE in 1 BOTTLE (60505-0055-3)

• 60505- Apotex Corp.
  • 60505-3438- Selegiline Hydrochloride
    • 60505-3438-3- 60 TABLET in 1 BOTTLE (60505-3438-3)

• 60505- Apotex Corp.
  • 60505-3438- Selegiline Hydrochloride
    • 60505-3438-8- 500 TABLET in 1 BOTTLE (60505-3438-8)

• 67253- Par Pharmaceutical
  • 67253-700- SELEGILINE HYDROCHLORIDE
    • 67253-700-06- 60 CAPSULE in 1 BOTTLE (67253-700-06)