Selegiline

Selegiline is a monoamine oxidase type B (MAO-B) inhibitor prescribed for the management of the symptoms of Parkinson's disease in patients already taking levodopa-carbidopa (also a drug prescribed for the treatment of Parkinson's disease).

Selegiline is available under the following different brand names: Eldepryl and Zelapar.

Dosage Forms and Strengths

Tablet/capsule

• 1.25 mg
• 5 mg

Dosage Considerations – Should be Given as Follows:

Parkinson's Disease

Adult and geriatric

Conventional

• 5 mg orally at breakfast and 5 mg at lunch (10 mg/day)
• Geriatric: less than 5 mg/day when combined with levodopa
• After 2-3 days of selegeline therapy, can begin to taper levadopa dose by 10-30% as tolerated; continue to taper based upon patient response
• Not to exceed 10 mg/day

Orally-disintegrating (with levodopa/carbidopa)

• Initial 1.25 mg orally once/day, may increase after 6 weeks if inadequate response, no more than 2.5 mg/day
• Do not take food or liquid for 5 minutes after dose

Pediatric: Safety and efficacy not established

Renal Impairment

Use caution; safety and efficacy not established

Hepatic Impairment

• Use caution; safety and efficacy not established

Common side effects or health problems may include:

• Abnormal, involuntary movements
• Nausea
• Abdominal pain
• Dry mouth
• Fainting

Other side effects of selegiline include:

• Irregular heartbeats
• Confusion
• Extrapyramidal symptoms (muscle spasms, restlessness, muscle rigidity, slowness of movement, tremor, and jerky movements)
• Generalized pain
• Hallucinations
• Headache
• High blood pressure (hypertension)
• Sleep problems (insomnia)
• Mood changes
• Dizziness on standing
• Urinary retention
• Vomiting
• Heartburn
• Diarrhea
• Gas
• Constipation
• Dizziness
• Weakness
• Runny or stuffy nose
• Back pain
• Mouth sores or ulcers
• Pain with swallowing

This is not a complete list of side effects and other serious side effects or health problems may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of this medicine or any drug before seeking medical advice from your doctor, healthcare provider or pharmacist first. To do so may result in serious consequences or side effects.

• Selegiline has severe interactions with at least 58 different drugs.
• Selegiline has serious interactions with at least 33 different drugs.
• Selegiline has moderate interactions with at least 73 different drugs.
• Mild interactions of selegiline include:
  • ruxolitinib
  • protein A column

Selegiline has mild interactions with at least 65 different drugs.
This document does not contain all possible interactions from the use of this medication. Therefore, before using this drug, tell your doctor or pharmacist of all the drugs you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

• In short-term studies, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults (under 24 years of age) taking antidepressants for major depressive disorders and other psychiatric illnesses.
• This increase was not seen in patients aged over 24 years; a slight decrease in suicidal thinking was seen in adults over 65 years.
• In children and young adults, risks must be weighed against the benefits of taking antidepressants.
• Patients should be monitored closely for changes in behavior, clinical worsening, and suicidal tendencies; this should be done during initial 1-2 months of therapy and dosage adjustments.
• The patient's family should communicate any abrupt changes in behavior to the healthcare provider.
• Worsening behavior and suicidal tendencies that are not part of the presenting symptoms may require discontinuation of therapy.
• This drug is not approved for use in pediatric patients.
• This medication contains selegiline. Do not take Eldepryl or Zelapar if you are allergic to selegiline or any ingredients contained in this drug.
• Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity to drug or other ACE inhibitors
• Concomitant meperidine, possibly other opioids, many other drugs (check interactions)

Effects of Drug Abuse

• No information provided

Short-Term Effects

• See "What Are Side Effects Associated with Using Selegiline?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Selegiline?"

Cautions

• Loses selectivity for MAO-B receptors at higher doses.
• Patients with Parkinson disease treated with drugs that increase dopaminergic tone have reported falling asleep while engaged in activities of daily living, including the operation of motor vehicles.
• Diminished impulse control; Reports of intense urges to gamble, increased sexual urges, intense urges to spend money, binge eating, and/or other intense urges.

Pregnancy and Lactation

• Use selegiline with caution during pregnancy if benefits outweigh risks. Animal studies show risk and human studies are not available or neither animal nor human studies were done.
• It is unknown if selegiline passes into breast milk or how it would affect a nursing infant; use caution if breastfeeding.