No

Antidepressant, Monoamine Oxidase Inhibitor; Anti-Parkinson's Agent (Monoamine Oxidase Inhibitor)

Adjunct in the management of parkinsonian patients in which levodopa/carbidopa therapy is deteriorating

C

Hypersensitivity to selegiline; concomitant use of meperidine

Increased risk of nonselective MAO inhibition occurs with doses >10 mg/day; it is a monoamine oxidase 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.

Cardiovascular: Orthostatic hypotension, hypertension, arrhythmias, palpitations, 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 hypertrophy, urinary retention, sexual dysfunction

Neuromuscular & skeletal: Tremor, chorea, loss of balance, restlessness, bradykinesia

Ocular: Blepharospasm, blurred vision

Miscellaneous: Diaphoresis (increased)

Symptoms of overdose include tachycardia, palpitations, muscle twitching, seizures

Competent supportive care is the most important treatment; both hypertension or hypotension can occur with intoxication. Hypotension may respond to I.V. fluids or vasopressors, and hypertension usually responds to an alpha-adrenergic blocker. While treating the hypertension, care is warranted to avoid sudden drops in blood pressure, since this may worsen the MAO inhibitor toxicity. Muscle irritability and seizures often respond to diazepam, while hyperthermia is best treated antipyretics and cooling blankets. Cardiac arrhythmias are best treated with phenytoin or procainamide.

CYP2D6 enzyme substrate

Concurrent use of selegiline with an SSRI may result in mania or hypertension; it is generally best to avoid these combinations

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

Potent monoamine oxidase (MAO) type-B inhibitor; MAO-B plays a major role in the metabolism of dopamine; selegiline may also increase dopaminergic activity by interfering with dopamine reuptake at the synapse

Onset of therapeutic effects: Within 1 hour

Duration: 24-72 hours

Half-life: 9 minutes

Metabolism: In the liver to amphetamine and methamphetamine

Oral:

Elderly: Initial: 5 mg in the morning, may increase to a total of 10 mg/day

This medication 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; wine (Chianti and hearty red) and beer); 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

Blood pressure, symptoms of parkinsonism

Selegiline 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.

>10% of patients experience dry mouth; 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)

Take 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, or dietary fruit and fiber may help); runny nose or flu-like symptoms (consult prescriber for appropriate relief); 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 be pregnant. Consult prescriber if breast-feeding.

Monoamine oxidase inhibitor type "B"; there should not be a problem with tyramine-containing products as long as the typical doses are employed

Capsule, as hydrochloride (Eldepryl®): 5 mg

Tablet: 5 mg

Burke 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.

Koller WC, Silver DE, and Lieberman A, "An Algorithm for the Management of Parkinson's Disease," Neurology, 1994, 44(12 Suppl 10):S1-52.

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):S2-9.

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.