|SELEGILINE HYDROCHLORIDE (L-DEPRENYL)
Carbex, Eldepryl, Emsam, Zelapar
Classifications: anticholinergic; antiparkinson agent; Therapeutic: antiparkinson agent; antidepressant (maoi)
Prototype: Levodopa (L-dopa)
Pregnancy Category: C
5 mg tablets, capsules; 1.25 mg orally disintegrating tab; 6 mg, 9 mg, 12 mg transdermal patch
Increase in dopaminergic activity is thought to be primarily due to selective inhibition of MAO type B activity. Ability
of selegiline to control parkinsonism is thought to be due to increased dopaminergic activity. It interferes with dopamine
reuptake at the synapse of neurons as well as its inhibition of MAO type B dopaminergic activity in the brain. Interference
with dopamine reuptake at the MAO type A dopaminergic receptors in the brain is thought to be the mechanism for antidepression.
Effectiveness is measured in decreased tremors, reduced akinesia, improved speech and motor abilities as well as improved
walking. At slightly higher doses it is an effective antidepressant.
Adjunctive therapy of Parkinson's disease for patients being treated with levodopa and carbidopa who exhibit deterioration
in the quality of their response to therapy, major depressive disorder.
Attention deficit/hyperactivity disorder, extrapyramidal symptoms.
Hypersensitivity to selegiline; uncontrolled hypertension; concomitant use with meperidine and other opioids; suidical ideation;
pregnancy (category C); lactation.
Hypertension; history of suicide, bipolar disorder; psychosis. Safety and efficacy in adolescents and children are not established.
Route & Dosage
Adult: PO 5 mg b.i.d. with breakfast and lunch (doses >10 mg/d are associated with increased risk of toxicity due to MAO inhibition) PO (Zelapar) 1.25 mg q.d. x 6 weeks (max: 2.5 mg q.d.)
Geriatric: PO Start with 5 mg qa.m.
Adult: Transdermal 6 mg/d, may increase by 3 mg/d q2wk up to 12 mg/d
- Do not give daily doses exceeding 10 mg/d.
- Note: Concurrent levodopa and carbidopa doses are usually reduced 1030% after 23 d of selegiline therapy.
- Do not use concurrently with opioids (especially meperidine).
- Store at 15°30° C (59°86° F).
- Do not cut or trim patch.
- Before application wash the area with soap and warm water. Dry thoroughly.
- Apply to upper torso, upper thigh, or outer surface of upper arm. Do not apply to hairy, oily, irritated, broken, or calloused
- Rotate sites.
- Wash hands after application.
Adverse Effects (≥1%)CNS:
Sleep disturbances, psychosis, agitation, confusion, dyskinesia, dizziness, hallucinations, dystonia, akathisia. CV:
vomiting, abdominal pain, constipation
InteractionsDrug: tricyclic antidepressants
may cause hyperpyrexia, seizures; fluoxetine, sertraline, paroxetine
may cause hyperthermia, diaphoresis, tremors, seizures, delirium; sympathomimetic agents
(e.g., amphetamine, phenylephrine, phenylpropanolamine
may cause hypertensive crisis; cns depressants
have additive CNS
depressive effects; opiate analgesics
) may cause hypertensive crisis and circulatory collapse; buspirone,
hypertension; general anesthetics
prolonged hypotensive and CNS
depressant effects; hypertension, headache, hyperexcitability reported with dopamine, methyldopa, levodopa, tryptophan; metrizamide
may increase risk of seizures; hypotensive agents
have additive hypotensive effects. Food:
Aged meats or aged cheeses, protein extracts, sour cream, alcohol
, anchovies, liver, sausages, overripe figs, bananas, avocados,
chocolate, soy sauce, bean curd, natural yogurt, fava beanstyramine
-containing foodsmay precipitate hypertensive crisis (less frequent with usual doses of selegiline
than with other maoi
s). Herbal: Ginseng, ephedra, ma huang, St. John's wort
may cause hypertensive crisis.
Rapid; 73% reaches systemic circulation. Onset:
1 h. Duration:
13 d. Distribution:
Crosses placenta; not known if distributed into breast milk. Metabolism:
In liver to N
-desmethyldeprenyl-amphetamine and methamphetamine. Elimination:
In urine. Half-Life:
15 min (metabolites 220 h).
Assessment & Drug Effects
- Monitor vital signs, particularly during period of dosage adjustment. Report alterations in BP or pulse. Indications for
discontinuation of the drug include orthostatic hypotension, hypertension, and arrhythmias.
- Monitor for changes in behavior that may indicate increase suicidality, especially in adolescents or children being treated
- Monitor all patients closely for behavior changes (e.g., hallucinations, confusion, depression, delusions).
Patient & Family Education
- Do not exceed the prescribed drug dose.
- Report symptoms of MAO inhibitor-induced hypertension (e.g., severe headache, palpitations, neck stiffness, nausea, vomiting) immediately to physician.
- Do not drive or engage in potentially hazardous activities until response to drug is known.
- Make positional changes slowly and in stages. Orthostatic hypotension is possible as well as dizziness, light-headedness,
- If the transdermal patch falls off, apply a new patch to a new area, and resume previous schedule.
- Only one should be worn at a given time. Remove the old transdermal patch.