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
