selegiline hydrochloride
selegiline hydrochloride
Pharmacologic class: MAO inhibitor (type B)
Therapeutic class: Antidyskinetic Pregnancy risk category C
FDA Box Warning
• Drug may increase risk of suicidal thinking and behavior in children and adolescents with major depressive disorder (MDD) and other psychiatric disorders. Anyone considering using it for MDD in a child or adolescent must balance risk with clinical need, as depression itself increases suicide risk. With patient of any age, observe closely for clinical worsening, suicidality, and unusual behavior changes when therapy begins. Advise family and caregivers to observe patient closely and communicate with prescriber as needed.
• Drug isn't approved for use in pediatric patients.
Action
Unknown. Thought to increase dopaminergic activity by inhibiting MAO type B in nerve cells, increasing dopamine availability to brain cells.
Availability
Capsules: 5 mg
Tablets: 5 mg
Tablets (orally disintegrating): 1.25 mg
Transdermal system: 6 mg/24 hours, 9 mg/24 hours, 12 mg/24 hours
Indications and dosages
➣ Adjunctive treatment of Parkinson's disease in patients who don't respond to carbidopa-levodopa alone
Adults: 10 mg P.O. daily in divided doses. After 2 to 3 days, attempt to reduce carbidopa-levodopa dosage (typically by 10% to 30%). Or initially, 1.25 mg (orally disintegrating tablets) P.O. daily for at least 6 weeks. May increase after 6 weeks to 2.5 mg P.O. daily based on effect and tolerability.
➣ Major depressive disorder
Adults: Initially, apply 6 mg/24 hours patch; increase in dose increments of 2 mg/24 hours up to a maximum dose of 12 mg/24 hours at intervals of no less than two weeks, if needed.
Off-label uses
• Initial therapy for Parkinson's disease
• Alzheimer's disease
• Narcolepsy
• Adjunct in schizophrenia
Contraindications
• Hypersensitivity to drug or its components
• Concurrent meperidine therapy
Precautions
Use cautiously in:
• patients receiving tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SRRIs), or dextromethorphan, carbamazepine, and analgesics such as tramadol, methadone, and propoxyphene
• patients with pheochromocytoma
• elderly patients
• pregnant or breastfeeding patients
• children.
Administration
• Give orally disintegrating tablets in the morning before breakfast; don't give food or liquid 5 minutes before and after administration.
• Give capsules or regular tablets with breakfast and lunch, but restrict foods high in tyramine (such as aged cheese, red wine, yogurt, and smoked high-protein foods).
See Don't give within 14 days of TCAs or SSRIs (5 weeks for fluoxetine because of its long half-life).
• Apply patch to dry, intact skin on the upper torso (below the neck and above the waist), upper thigh, or the outer surface of the upper arm once every 24 hours.
Adverse reactions
CNS: agitation, anxiety, bradykinesia, chorea, confusion, delusions, depression, dizziness, hallucinations, headache, dyskinesias, increased akinetic involuntary movements, insomnia, lethargy, light-headedness, loss of balance, syncope, vivid dreams
CV: orthostatic hypotension, hypertension, new or increased angina, palpitations, arrhythmias
GI: nausea, diarrhea, abdominal pain, dry mouth, buccal mucosa irritation (with orally disintegrating tablets)
GU: urinary retention
Musculoskeletal: leg pain, low back pain
Other: generalized aches, weight loss
Interactions
Drug-drug. Adrenergics: increased pressor response
Buspirone: elevated blood pressure
Dextromethorphan: brief episodes of psychosis or bizarre behavior
Levodopa: increased adverse reactions to levodopa
Meperidine and analgesics such as tramadol, methadone, and propoxyphene: stupor, muscle rigidity, severe agitation, fever, death
Other MAO inhibitors: hypertensive crisis
SSRIs, TCAs: severe mental status changes, CNS toxicity (with possible hyperpyrexia and death)
Drug-food. Tyramine-rich foods (such as aged cheese, red wine, yogurt, smoked high-protein foods): hypertensive crisis
Drug-herbs. Cacao: vasopressor effects
Ginseng: headache, tremor, mania
St. John's wort: life-threatening adverse reactions
Patient monitoring
• Monitor vital signs and cardiovascular status.
• Assess neurologic status and motor function. Institute safety measures as needed to prevent injury.
• Monitor weight and fluid intake and output.
• Monitor CBC and liver and kidney function tests.
Patient teaching
• Tell patient to take capsules or regular tablets with or without food, but he should avoid foods and beverages high in tyramine. Provide a list of these foods and beverages.
• Instruct patient (and caregiver as appropriate) to take orally disintegrating tablets in the morning before breakfast and not to push these tablets through the foil backing. Tell patient to peel back the backing of one or two blisters (as prescribed) with dry hands, gently remove the tablet, then immediately place the tablet on top of the tongue where it will disintegrate in seconds. Remind patient to avoid ingesting food or liquids for 5 minutes before and after taking orally disintegrating tablets.
• Inform patient to avoid tyramine-rich foods and beverages beginning on the first day of application of 9mg/24hours-or 12mg/24hours-patch and continue to avoid these foods and beverages for two weeks after a dose reduction to the 6mg/24hours-patch or following the discontinuation of the 9mg/24hours-or 12mg/24hours-patch.
• Instruct patient (and caregiver as appropriate) to monitor neurologic status and motor function and to institute safety precautions as needed to prevent injury.
• Instruct patient to move slowly when sitting up or standing, to avoid dizziness from sudden blood pressure decrease.
• Tell patient (or caregiver) that drug may cause serious interactions with many drugs. Instruct him to tell all prescribers he's taking it.
• Tell patient not to use St. John's wort without consulting with prescriber.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, foods, and herbs mentioned above.