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Pronunciation(se LE ji leen)
U.S. Brand NamesEldepryl®
SynonymsDeprenyl; L-Deprenyl; Selegiline Hydrochloride
Generic AvailableYes
Canadian Brand NamesApo-Selegiline®; Eldepryl®; Gen-Selegiline; Novo-Selegiline; Nu-Selegiline
UseAdjunct in the management of parkinsonian patients in which levodopa/carbidopa therapy is deteriorating
Use - Unlabeled/InvestigationalEarly Parkinson's disease; attention-deficit/hyperactivity disorder (ADHD); negative symptoms of schizophrenia; extrapyramidal symptoms; depression; Alzheimer's disease (studies have shown some improvement in behavioral and cognitive performance)
Pregnancy Risk FactorC
LactationExcretion in breast milk unknown
ContraindicationsHypersensitivity to selegiline or any component of the formulation; concomitant use of meperidine
Warnings/PrecautionsIncreased risk of nonselective MAO inhibition occurs with doses >10 mg/day; it is a MAO inhibitor type "B", there should not be a problem with tyramine-containing products as long as the typical doses are employed, however, rare reactions have been reported. Use with tricyclic antidepressants and SSRIs has also been associated with rare reactions and should generally be avoided. Addition to levodopa therapy may result in exacerbation of levodopa adverse effects, requiring a reduction in levodopa dosage. The possibility of a suicide attempt is inherent in major depression and may persist until remission occurs. Use caution in high-risk patients during initiation of therapy. Prescriptions should be written for the smallest quantity consistent with good patient care.
Adverse ReactionsFrequency not defined. Cardiovascular: Orthostatic hypotension, hypertension, arrhythmia, palpitation, angina, tachycardia, peripheral edema, bradycardia, syncope
Central nervous system: Hallucinations, dizziness, confusion, anxiety, depression, drowsiness, behavior/mood changes, dreams/nightmares, fatigue, delusions
Dermatologic: Rash, photosensitivity
Gastrointestinal: Xerostomia, nausea, vomiting, constipation, weight loss, anorexia, diarrhea, heartburn
Genitourinary: Nocturia, prostatic hyperplasia, urinary retention, sexual dysfunction
Neuromuscular & skeletal: Tremor, chorea, loss of balance, restlessness, bradykinesia
Ocular: Blepharospasm, blurred vision
Miscellaneous: Diaphoresis (increased)
Overdosage/ToxicologySymptoms of overdose include tachycardia, palpitations, muscle twitching, and seizures. Both hypertension or hypotension can occur with intoxication. While treating hypertension, care is warranted to avoid sudden drops in blood pressure, since this may worsen MAO inhibitor toxicity. Cardiac arrhythmias are best treated with phenytoin or procainamide. Treatment is generally symptom-directed and supportive.
Drug InteractionsSubstrate of CYP1A2 (minor), 2A6 (minor), 2B6 (major), 2C8/9 (major), 2D6 (minor), 3A4 (minor); Inhibits CYP1A2 (weak), 2A6 (weak), 2C8/9 (weak), 2C19 (weak), 2D6 (weak), 2E1 (weak), 3A4 (weak) Note: Many drug interactions involving selegiline are theoretical, primarily based on interactions with nonspecific MAO inhibitors; at doses <10 mg/day, the risk of these interactions with selegiline may be very low
Amphetamines: MAO inhibitors in combination with amphetamines may result in severe hypertensive reaction or serotonin syndrome; these combinations are best avoided
Anorexiants: Concurrent use of selegiline (high dose) in combination with CNS stimulants or anorexiants may result in serotonin syndrome; these combinations are best avoided; includes dexfenfluramine, fenfluramine, or sibutramine
Barbiturates: MAO inhibitors may inhibit the metabolism of barbiturates and prolong their effect
CNS stimulants: MAO inhibitors in combination with stimulants (methylphenidate) may result in serotonin syndrome; these combinations are best avoided
CYP2B6 inducers: May decrease the levels/effects of selegiline. Example inducers include carbamazepine, nevirapine, phenobarbital, phenytoin, and rifampin.
CYP2B6 inhibitors: May increase the levels/effects of selegiline. Example inhibitors include desipramine, paroxetine, and sertraline.
CYP2C8/9 inducers: May decrease the levels/effects of selegiline. Example inducers include carbamazepine, phenobarbital, phenytoin, rifampin, rifapentine, and secobarbital.
CYP2C8/9 inhibitors: May increase the levels/effects of selegiline. Example inhibitors include delavirdine, fluconazole, gemfibrozil, ketoconazole, nicardipine, NSAIDs, pioglitazone, and sulfonamides.
Dextromethorphan: Concurrent use of selegiline (high dose) may result in serotonin syndrome; these combinations are best avoided
Disulfiram: MAO inhibitors may produce delirium in patients receiving disulfiram; monitor
Guanadrel and guanethidine: MAO inhibitors inhibit the antihypertensive response to guanadrel or guanethidine; use an alternative antihypertensive agent
Hypoglycemic agents: MAO inhibitors may produce hypoglycemia in patients with diabetes; monitor
Levodopa: MAO inhibitors in combination with levodopa may result in hypertensive reactions; monitor
Lithium: MAO inhibitors in combination with lithium have resulted in malignant hyperpyrexia; this combination is best avoided
Meperidine: Concurrent use of selegiline (high dose) may result in serotonin syndrome; these combinations are best avoided
Nefazodone: Concurrent use of selegiline (high dose) may result in serotonin syndrome; these combinations are best avoided
Norepinephrine: MAO inhibitors may increase the pressor response of norepinephrine (effect is generally small); monitor
Oral contraceptives: Increased selegiline levels have been noted with concurrent administration; monitor
Reserpine: MAO inhibitors in combination with reserpine may result in hypertensive reactions; monitor
SSRIs: Concurrent use of selegiline with an SSRI may result in mania or hypertension; it is generally best to avoid these combinations
Sympathomimetics (indirect-acting): MAO inhibitors in combination with sympathomimetics such as dopamine, metaraminol, phenylephrine, and decongestants (pseudoephedrine) may result in severe hypertensive reaction; these combinations are best avoided
Succinylcholine: MAO inhibitors may prolong the muscle relaxation produced by succinylcholine via decreased plasma pseudocholinesterase
Tramadol: May increase the risk of seizures and serotonin syndrome in patients receiving an MAO inhibitor
Trazodone: Concurrent use of selegiline (high dose) may result in serotonin syndrome; these combinations are best avoided
Tricyclic antidepressants: May cause serotonin syndrome when combined with an MAO inhibitor; avoid this combination
Tyramine: Selegiline (>10 mg/day) in combination with tyramine (cheese, ethanol) may increase the pressor response; avoid high tyramine-containing foods in patients receiving >10 mg/day of selegiline
Venlafaxine: Concurrent use of selegiline (high dose) may result in serotonin syndrome; these combinations are best avoided
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Ethanol/Nutrition/Herb InteractionsEthanol: Avoid ethanol. Avoid beverages containing tyramine (wine [Chianti and hearty red] and beer).
Food: Selegiline may cause sudden and severe high blood pressure when taken with food high in tyramine (cheeses, sour cream, yogurt, pickled herring, chicken liver, canned figs, raisins, bananas, avocados, soy sauce, broad bean pods, yeast extracts, meats prepared with tenderizers, and many foods aged to improve flavor). Small amounts of caffeine may produce irregular heartbeat or high blood pressure and can interact with this medication for up to 2 weeks after stopping its use.
Herb/Nutraceutical: Avoid valerian, St John's wort, SAMe, kava kava (may increase risk of serotonin syndrome and/or excessive sedation).
Mechanism of ActionPotent monoamine oxidase (MAO) type-B inhibitor; MAO type B plays a major role in the metabolism of dopamine; selegiline may also increase dopaminergic activity by interfering with dopamine reuptake at the synapse
Pharmacodynamics/KineticsOnset of action: Therapeutic: Within 1 hour
Duration: 24-72 hours
Half-life elimination: Steady state: 10 hours
Metabolism: Hepatic to amphetamine and methamphetamine
DosageOral: Children and Adolescents: ADHD (unlabeled use): 5-15 mg/day
Adults: Parkinson's disease: 5 mg twice daily with breakfast and lunch or 10 mg in the morning
Elderly: Parkinson's disease: Initial: 5 mg in the morning, may increase to a total of 10 mg/day
Monitoring ParametersBlood pressure, symptoms of parkinsonism
Patient EducationTake exactly as directed (may be prescribed in conjunction with levodopa/carbidopa); do not change dosage or discontinue without consulting prescriber. Therapeutic effects may take several weeks or months to achieve and you may need frequent monitoring during first weeks of therapy. Take with meals if GI upset occurs, before meals if dry mouth occurs, after eating if drooling or if nausea occurs. Take at the same time each day. Avoid tyramine-containing foods (low potential for reaction). Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake; void before taking medication. Do not use alcohol and prescription or OTC sedatives or CNS depressants without consulting prescriber. You may experience drowsiness, dizziness, confusion, or vision changes (use caution when driving, climbing stairs, or engaging in tasks requiring alertness until response to drug is known); orthostatic hypotension (use caution when changing position - rising to standing from sitting or lying); constipation (increased exercise, fluids, fruit, or fiber may help); runny nose or flu-like symptoms (consult prescriber for appropriate relief); or nausea, vomiting, loss of appetite, or stomach discomfort (small, frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help). Report unresolved constipation or vomiting; chest pain, palpitations, irregular heartbeat; CNS changes (hallucination, loss of memory, seizures, acute headache, nervousness, etc); painful or difficult urination; increased muscle spasticity, rigidity, or involuntary movements; skin rash; or significant worsening of condition. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.
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Nursing ImplicationsMAO type B inhibitor; there should not be a problem with tyramine-containing products as long as the typical doses are employed
Additional InformationWhen adding selegiline to levodopa/carbidopa, the dose of the latter can usually be decreased. Studies are investigating the use of selegiline in early Parkinson's disease to slow the progression of the disease.
Anesthesia and Critical Care Concerns/Other ConsiderationsWhen adding selegiline to levodopa/carbidopa, the dose of the latter can usually be decreased. Studies are investigating the use of selegiline in early Parkinson's disease to slow the progression of the disease. With doses >10 mg/day, selegiline loses MAO type "B" specificity.
Dental Health: Effects on Dental TreatmentKey adverse event(s) related to dental treatment: Xerostomia and changes in salivation (normal salivary flow resumes upon discontinuation). Anticholinergic side effects can cause a reduction of saliva production or secretion, contributing to discomfort and dental disease (ie, caries, oral candidiasis, and periodontal disease).
Dental Health: Vasoconstrictor/Local Anesthetic PrecautionsSelegiline in doses of 10 mg a day or less does not inhibit type-A MAO. Therefore, there are no precautions with the use of vasoconstrictors.
Mental Health: Child/Adolescent ConsiderationsTwenty-nine children 6-18 years of age (mean: 11.2 years) with ADHD refractory to conventional treatments received an average daily dose of 8.1 mg (5-15 mg/day) for an average of 6.7 months (Jankovic, 1993). Jankovic J, "Deprenyl in Attention Deficit Associated With Tourette's Syndrome,"Arch Neurol, 1993, 50(3):286-8.
Dosage FormsCapsule, as hydrochloride (Eldepryl®): 5 mg
Tablet, as hydrochloride: 5 mg
ReferencesBurke WJ, Roccaforte WH, Wengel SP, et al, "L-Deprenyl in the Treatment of Mild Dementia of the Alzheimer Type: Results of a 15-Month Trial,"J Am Geriatr Soc, 1993, 41(11):1219-25.
Collier DS, Berg MJ, and Fincham RW, "Parkinsonism Treatment: Part III - Update,"Ann Pharmacother, 1992, 26(2):227-33.
Jankovic J, "Deprenyl in Attention Deficit Associated With Tourette's Syndrome,"Arch Neurol, 1993, 50(3):286-8.
Koller WC, Silver DE, and Lieberman A, "An Algorithm for the Management of Parkinson's Disease,"Neurology, 1994, 44(12 Suppl 10):1-52.
Lawlor BA, Aisen PS, and Green C, "Selegiline in the Treatment of Behavioural Disturbances in Alzheimer's Disease,"Int J Geriatr Psychiatry, 1997, 12(3):319-22.
Sano M, Ernesto C, Thomas RG, et al, "A Controlled Trial of Selegiline, Alpha-Tocopherol, or Both as Treatment for Alzheimer's Disease,"N Engl J Med, 1997, 336(17):1216-22.
Schneider LS, Pollock VE, Zemansky MF, et al, "A Pilot Study of Low-Dose L-Deprenyl in Alzheimer's Disease,"J Geriatr Psychiatry Neurol, 1991, 4(3):143-8.
Stern MB, "Contemporary Approaches to the Pharmacotherapeutic Management of Parkinson's Disease: An Overview,"Neurology, 1997, 49(1 Suppl 1):2-9.
The Parkinson Study Group, "Effect of Deprenyl on the Progression of Disability in Early Parkinson's Disease,"N Engl J Med, 1989, 321(20):1364-71.
The Parkinson Study Group, "Effects of Tocopherol and Deprenyl on the Progression of Disability in Early Parkinson's Disease,"N Engl J Med, 1993, 328(3):176-83.
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International Brand NamesAmboneural® (AT); Amindan® (DE); Antiparkin® (DE, LU); Apo-Seleg® (CZ); Apo-Selegiline® (CA, NZ); Brintenal® (AR); Cloridrato de Selegilina® (BR); Cognitiv® (AT, RO, RU); Déprényl® (FR); Deprilan® (BR); Egibren® (IT); Eldepryl® (BE, CA, DK, FI, GB, IE, NL, NO, NZ, SE); Elepril® (BR); Endopryl® (CY); Gen-Selegiline (CA); Julab® (TH); Jumexal® (CH, CR, GT, HN, PA, SV); Jumex® (AR, AT, CR, CZ, GT, HK, HN, HR, HU, ID, IL, IT, PA, PL, PT, RO, SG, SI, SV, TH); Jumexil® (BR); Juprenil® (YU); Jutagilin® (DE); Kinabide® (AR); MAOtil® (DE); Moverdin® (TR); Movergan® (DE); Niar® (BR, CZ, HR, MX, PL, RU); Novo-Selegiline (CA); Nu-Selegiline (CA); Otrasel® (FR); Oxan® (CL); Parkinil® (PL); Plurimen® (ES); Primulex® (HU); Regepar® (AT); Sedicel® (CO); Sefmex® (TH); Segan® (PL); Seldepar® (TR); Selecim® (CH, RO); Selecom® (IT); Seledat® (IT); Selegam® (DE); Selegil® (CO); Selegilina Davur® (ES); Selegilin AL® (DE); Selegilin Alpharma® (DK); Selegilina Profas® (ES); Selegilin® (AT, CZ, NO); Selegilin Azu® (DE); Selegiline-Chinoin® (HU); Selegiline Hydrochloride® (GB); Selegiline® (IL); Selegiline Merck® (HU); Selegiline Teva® (RO); Selegilin Genericon® (AT); Selegilin Generics® (FI); Selegilin HCl-Austropharm® (AT); Selegilin Helvepharm® (CH); Selegilin Heumann® (DE); Selegilin-Mepha® (CH); Selegilin-neuraxpharm® (DE); Selegilin NM® (DK); Selegilin NM Pharma® (SE); Selegilin-ratiopharm® (DE); Selegilin Sandoz® (DE); Selegilin Sofotec® (DE); Selegilin Stada® (DE); Selegilin-TEVA® (DE); selegilin von ct® (DE); Selegos® (BG, RO, RU, SG); Selemerck® (DE); Selenor® (PL); Selepark® (DE); Selerin® (PL); Selgene® (AU, NZ); Selgimed® (DE); Selgin® (PL); Selgres® (PL); Seline® (TH); Seliratio® (PL); Silin Sofotec® (DE); Xilopar® (AT, DE, IT); Zelapar® (GB)
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