Names and pronunciation
(se-le′ji-leen) Eldepryl, Emsam, Zelapar
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Drug reference
(se-le′ji-leen) Eldepryl, Emsam, Zelapar
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Func. class.: Antiparkinson agent, antidepressant
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Chem. class.: MAOI, type B
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Do not confuse: selegiline/Salagen Zelapar/ZyPREXA
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ACTION: Increased dopaminergic activity by inhibition of MAO type B activ- ity; not fully understood
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USES: Adjunct management of Parkin- son’s disease for patients being treated with levodopa/carbidopa who had poor response to therapy; depression (transdermal)
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CONTRAINDICATIONS: Children/adolescents (suicide/hyperten- sive crisis), hypersensitivity, breastfeed- ing, MAOIs
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Black Box Warning: Suicidal ideation Precautions: Pregnancy, abrupt dis- continuation, alcoholism, ambient temperature increase, behavioral changes, bipolar disorders, driving or operating machinery, geriatrics, heat- ing pad, hepatic disease, hypertension, hypotension, melanoma, phenylketon- uria, psychosis, renal disease, sunlight exposure Black Box Warning: Do not use in chil- dren <12 yr • When using 9 mg/24 hr or 12 mg/24 hr, specific manufacturer’s recommenda- tion for tyramine intake must be followed to prevent hypertensive crisis Black Box Warning: Depression: affect, mood, behavioral changes, depression; perform suicide assessment on all pa- tients; suicidal ideation may occur • Opioids: if patient has received, do not administer selegiline; fatal reactions have occurred • Orthostatic hypotension: may occur during first few months of treatment, usually in patients >60 yr Black Box Warning: Suicidal ideation: to report change in symptoms, worsening de- pression, or suicidal thoughts, behaviors; treatment may need to be changed • Not to exceed recommended dose of 10 mg (PO) because this might precipitate hypertensive crisis; to report severe headache, other unusual symptoms • Pregnancy: to report if pregnancy is planned or suspected; not to breastfeed
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SIDE EFFECTS CNS: Increased tremors, tardive dyskine- sia, dystonic symptoms, hallucinations, dizziness, mood changes, nightmares, delusions, serotonin syndrome, headache, migraine, confusion, anxiety, suicide in child/adolescent, suicidal ideation in adults CV: Orthostatic hypotension, angina pec- toris, hypertensive crisis (children) EENT: Tinnitus GI: Nausea, weight loss, vomiting, flatulence GU: Slow urination, nocturia, prostatic hypertrophy, urinary hesitation, reten- tion, frequency, sexual dysfunction INTEG: Increased sweating, melanoma, acne, pruritus; site reactions (transdermal) RESP: Asthma, SOB
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INTERACTIONS • Fatal interaction: opioids (especially meperidine); do not administer together • Serotonin syndrome (confusion, sei- zures, fever, hypertension, agitation; death): FLUoxetine, PARoxetine, sertraline, fluvoxaMINE (discontinue 5 wk before sele- giline treatment); do not use together Increase: side effects of levodopa/ carbidopa Increase: unusual behavior, psychosis— dextromethorphan Increase: hypotension—antihypertensives Drug/Lab Test Decrease: VMA False positive: urine ketones, urine S glucose False negative: urine glucose (glucose oxidase) False increase: uric acid, urine protein
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TREATMENT OF OVERDOSE: IV fluids for hypertension, IV dilute pres- sure agent for B/P titration See Appendix B
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DOSAGE AND ROUTES • Adult: PO 5 mg bid given with le- vodopa/carbidopa in divided doses, after 2-3 days, begin to reduce dose of le- ORAL vodopa/carbidopa 10%-30%; DISINTEGRATING 1.25 mg (1 tab) × 6 wk or more initially, then 2.5 mg (2 tabs) dissolved on tongue daily before break- fast; max 2.5 mg/day; TRANSDERMAL (depression) 6 mg/24 hr initially, in- crease by 3 mg/24 hr at ≥2 wk, up to 12 mg/24 hr if needed Major depression Adult: TD 6 mg/24 hr daily, may increase by 3 mg/24 hr q2wK
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Available forms: Tabs 5 mg; caps 5 mg; oral disintegrating tabs 1.25 mg; transder- mal 6 mg/24 hr (20 mg/20 cm2), 9 mg/24 hr (30 mg/30 cm2), 12 mg/24 hr (40 mg/40 cm2)
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Administer: PO route • Do not use in children due to risk for hypertensive crisis • Product until NPO before surgery • Adjust dosage to response • With meals; limit protein taken with product • Dosing bid in AM and afternoon; avoid PM or bedtime dosing • At doses of <10 mg/day because of risks associated with nonselective inhibi- tion of MAO • Oral disintegrating tab: peel back foil; remove tab; do not push through foil; place tab on tongue; allow to dissolve; swallow with saliva; no fluids 5 min be- fore or after use; avoid using >2.5 mg/ day, hypertensive crisis is more common Transdermal route (depression) • Apply to dry intact skin on upper torso, upper thigh, or outer surface of upper arm q24hr
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Assess: • Parkinson’s symptoms: decreased ri- gidity, unsteady gait, weakness, tremors • Cardiac status: tachycardia/bradycar- dia; B/P, respiration throughout treat- ment
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Evaluate: • Therapeutic response: decrease in akathisia, improved mood
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To change positions slowly to prevent orthostatic hypotension • Hypertensive crisis: to notify pre- scriber immediately of nausea, vomiting, sweating, agitation, change in mental sta- tus, headache, chest pain • Serotonin syndrome: to report twitch- ing, sweating, shivering, diarrhea to pre- scriber immediately • To use product exactly as prescribed; that if discontinued abruptly, parkinso- nian crisis may occur • To use during the day to prevent insomnia • To avoid heating pads, hot tubs when using transdermal products • To avoid hazardous activities until re- sponse is known • To avoid foods high in tyramine: cheese, pickled products, wine, beer, large amounts of caffeine as per manufacturer
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PHARMACOKINETICS PO peak 1⁄2-2 hr, orally disintegrating tab 10-15 min, TD 2 wk; rapidly metabolized (active metabolites: N-desmethyldeprenyl, amphetamine, methamphetamine); metab- olites excreted in urine; half-life 10 hr, orally disintegrating tab 1.3 hr, transdermal 18-25 hr; protein binding up to 85%
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• Adult: PO 5 mg bid given with le- vodopa/carbidopa in divided doses, after 2-3 days, begin to reduce dose of le- ORAL vodopa/carbidopa 10%-30%; DISINTEGRATING 1.25 mg (1 tab) × 6 wk or more initially, then 2.5 mg (2 tabs) dissolved on tongue daily before break- fast; max 2.5 mg/day; TRANSDERMAL (depression) 6 mg/24 hr initially, in- crease by 3 mg/24 hr at ≥2 wk, up to 12 mg/24 hr if needed Major depression Adult: TD 6 mg/24 hr daily, may increase by 3 mg/24 hr q2wK
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