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selegiline (Eldepryl, Zelapar): Dosing and Uses

 

Classes: Antiparkinson Agents, MAO Type B Inhibitors

Medically reviewed by Min Clinic Staff | Updated: January 2026

Dosing and uses of Eldepryl, Zelapar (selegiline)

 

Adult dosage forms and strengths

tablet/capsule

  • 1.25mg
  • 5mg

 

Parkinson Disease

ConventionaL

  • 5 mg PO at breakfast & 5 mg at lunch (10 mg/day)
  • 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 PO qDay, 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

 

Renal Impairment

Use caution; safety and efficacy not established

 

Hepatic Impairment

Use caution; safety and efficacy not established

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Geriatric dosage forms and strengths

 

Parkinson Disease

ConventionaL

- 5 mg PO at breakfast & 5 mg at lunch (10 mg/day)

- <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 PO qDay, 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

 

Eldepryl, Zelapar (selegiline) adverse (side) effects

>10%

Dyskinesia

Nausea (20%)

 

1-10%

Abdominal pain

Dry mouth

 

Frequency not defined (selected)

Arrhythmias

Confusion

EPs

Generalized pain

Hallucinations

Headache

HTn

Insomnia

Mood changes

Orthostatic hypotension

Syncope

Urinary retention

Vomiting

 

Warnings

Black box warnings

In short-term studies, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults (<24 yr of age) taking antidepressants for major depressive disorders and other psychiatric illnesses

This increase was not seen in patients aged >24 years; a slight decrease in suicidal thinking was seen in adults >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

 

Contraindications

Hypersensitivity

Concomitant meperidine, possibly other opioids, many other drugs (check interactions)

 

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

Pregnancy category: C

Lactation: unknown; use caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Eldepryl, Zelapar (selegiline)

Mechanism of action

Selective MAO-B inhibitor; may increase dopaminergic activity by interfering with dopamine reuptake at the synapse.

 

Pharmacokinetics

Peak plasma time: (conventional) 0.5-0.9 hr; (ODT) 15-40 min

Concentration: (conventional, 5 mg) 0.9-2.7 ng/mL; (ODT, 1.25 /2.5 mg) 3.34/4.47 ng/mL

Half-life elimination: 10 hr (PO); 18-25hr (TD)

Onset of action: Within 1 hr

Duration: 24-72hr (PO)

Bioavailability: 10%

Protein Bound: 90%

Vd: 300 L

Metabolism: cytochrome P-450 enzymes

Metabolites: L-amphetamine, L-desmethylselegiline, L-methamphetamine

Excretion: Urine