A-Z Drug Facts > Selegiline Hydrochloride (L-Deprenyl)

Selegiline Hydrochloride

( L-Deprenyl ) Pronouncation: (se-LEJ-i-leen HYE-droe-KLOR-ide)
Class: Antiparkinson agent

Trade Names:
Eldepryl
- Capsules 5 mg

Trade Names:
Selegiline
- Tablets 5 mg

Trade Names:
Zelapar
- Tablets, orally disintegrating 1.25 mg

Apo-Selegiline (Canada)
Gen-Selegiline (Canada)
Novo-Selegiline (Canada)
Nu-Selegiline (Canada)

Pharmacology

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Selective type B MAOI thought to increase dopaminergic activity. MAO enzyme breaks down catecholamines and serotonin. Selegiline may also interfere with dopamine reuptake at synapse.

Pharmacokinetics

Absorption

C _max of metabolites following a single oral dose of 10 mg are from 4 to almost 20 times greater than the C _max of selegiline (1 ng/mL). Bioavailability is increased 3- to 4-fold when taken with food.

Compared with the swallowed tablet, absorption is more rapid with the orally disintegrating tablet. After single dose of 1.25 and 2.5 mg orally disintegrating tablet, the mean C _max is 3.34 and 4.47 ng/mL, respectively, compared with 1.12 ng/mL with the swallowed tablet.

Distribution

Protein binding is up to 85%.

Metabolism

Selegiline undergoes extensive metabolism. Major metabolites are N-desmethylselegiline, L-amphetamine, and L-methamphetamine. Only N-desmethylselegiline has MAO-B inhibiting activity. Metabolism is via CYP2B6 and CYP3A4 isozymes, and, to a minor extent, CYP2A6.

Elimination

Excretion is primarily in the urine. Following a single oral dose, the mean t _½ is 2 h. The t _½ increases to 10 h under steady-state conditions.

Special Populations

Elderly

Systemic exposure is about twice as great in elderly patients compared with a younger population given a single 10 mg oral dose.

Hepatic function impairment

No information is available in hepatic function impairment.

Renal function impairment

No information is available in renal function impairment.

Indications and Usage

Adjunct to levodopa/carbidopa in Parkinson disease.

Contraindications

Use with meperidine or other analgesics (eg, tramadol, methadone, propoxyphene), other or MAOIs, or dextromethorphan; hypersensitivity to any component of the product.

Dosage and Administration

Tablet, capsule
Adults

PO 10 mg/day as divided dose of 5 mg each taken at breakfast and lunch. Do not exceed 10 mg/day. After 2 to 3 days of treatment, try reducing levodopa/carbidopa dose by 10% to 30%. Further reductions may be possible during continued selegiline therapy.

Orally disintegrating tablet
Adults

PO Start with 1.25 mg once a day for at least 6 wk. After 6 wk, the dose may be increased to 2.5 mg once a day if desired benefit has not been achieved and the medication is tolerated.

General Advice

• Take the orally disintegrating tablet in the morning before breakfast without liquid.
• Administer the orally disintegrating tablet by peeling back the backing of 1 or 2 blisters (do not push tablet through foil backing), and, using dry hands, remove tablet(s) and place on top of tongue where it will disintegrate within seconds.
• Patient should avoid ingesting food or liquids for 5 min before or after taking the orally disintegrating tablet.
• Each oraly disintegrating tablet contains phenylalanine 1.25 mg. Patients taking the 2.5 mg dose will receive phenylalanine 2.5 mg.

Storage/Stability

Store tablets at 59° to 86°F. Store capsules at 68° to 77°F. Dispense contents in a tight, light-resistant container. Store orally disintegrating tablet at 59° to 86°F. Use within 3 mo of opening pouch and immediately upon opening individual blister.

Drug Interactions

Bupropion

Coadministration of bupropion and selegiline is contraindicated. Allow at least 14 days to elapse between discontinuing selegiline and starting bupropion.

CYP3A4 inducers (eg, carbamazepine, phenytoin, rifampin)

May reduce selegiline concentrations; use with caution.

Dextromethorphan

Brief episodes of psychosis or bizarre behavior may occur.

Levodopa

The dopaminergic adverse reactions of levodopa may be potentiated and preexisting dyskinesia may be exacerbated.

MAOIs

Increased risk of nonselective MAO inhibition, leading to hypertensive crisis. Allow at least 14 days between discontinuation of selegiline and administration of other MAOIs, including other selegiline products. Hyperpyrexia and death have been reported with coadministration of other MAOIs (eg, phenelzine).

Meperidine

Serious, life-threatening reactions (eg, agitation, diaphoresis, fever, seizures), which may progress to coma, apnea, and death, may occur.

SSRIs (eg, fluoxetine)

Severe, life-threatening, toxicity, including serotonin syndrome (eg, altered consciousness, CNS irritability, increased muscle tone), may occur.

Sympathomimetics

Hypertensive crisis has been reported.

Tricyclic antidepressants (eg, amitriptyline)

Sever toxicity, including hyperpyrexia and death, may occur.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension (3%).

CNS

Dizziness (11%); headache, insomnia (7%); dyskinesia (6%); hallucinations (4%); ataxia, confusion, somnolence, tremor (3%); depression, headache, vivid dreams (2%).

Dermatologic

Skin disorders (6%); rash (4%).

EENT

Rhinitis (7%); pharyngitis (4%).

GI

Nausea (11%); dyspepsia, stomatitis (5%); abdominal pain, constipation (4%); dry mouth, vomiting (3%); diarrhea, dysphagia, flatulence, tooth disorder (2%).

Hematologic-Lymphatic

Ecchymosis (2%).

Metabolic-Nutritional

Hypokalemia (2%).

Musculoskeletal

Back pain (5%); leg cramps, myalgia (3%).

Respiratory

Dyspnea (3%).

Miscellaneous

Pain (8%); chest pain (2%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Capsules/Tablets

Safety and efficacy not established.

Zelapar

Safety and efficacy not established in children younger than 16 yr of age.

Elderly

In patients at least 65 yr of age compared with younger patients, the relative risk for treatment-related adverse reactions was at least 2-fold higher for abnormal dreams, anxiety, cheilitis, diarrhea, dizziness, dyspepsia, ECG abnormality, flu syndrome, hyperkalemia, hypertension, infection, nausea, orthostatic hypotension, pharyngitis, somnolence.

Renal Function

Serum BUN and creatinine may be increased. Use with caution in patients with history of, or known or suspected, renal function impairment.

Hepatic Function

Use with caution in patients with a history of, or known or suspected, hepatic function impairment.

Buccal mucosa irritation

In patients who were normal prior to therapy, the frequency of mild oropharyngeal abnormality (eg, swallowing pain, mouth pain, ulceration) was higher at the end of selegiline therapy compared with placebo.

Hallucinations

When used as an adjunct to levodopa, hallucinations have been reported.

Hyperpyrexia and confusion

Rapid dose reduction, withdrawal, or changes in antiparkinsonian therapy have been associated with a symptom complex resembling neuroleptic malignant syndrome.

Hypertensive crisis risk

Selegiline can be given with active amine-containing medications and tyramine-containing foods as long as recommended dose is not exceeded. However, report any possible symptoms suggestive of hypertensive crisis.

Orthostatic hypotension

There may be an increased risk for orthostatic hypotension in the period after increasing the daily dose of selegiline.

Max

Do not exceed recommended daily dose of 10 mg/day (2.5 mg/day for orally disintegrating tablets) because of risks associated with nonselective inhibition of MAO (potentially serious food or drug interactions may occur at higher doses).

Melanoma

Risk of melanoma is higher in Parkinson disease compared with the general population; however, it has not been determined if this is caused by the disease or the treatment.

Overdosage

Symptoms

Hypotension, psychomotor agitation.

Patient Information

• Encourage patient to change position slowly to prevent orthostatic hypotension.
• Instruct patient to avoid driving or other potentially hazardous activities until effect of medication is determined.
• Explain that dosage of levodopa/carbidopa may be reduced after initiation of adjunctive therapy.
• Identify tyramine-containing foods; explain rationale for exclusion from diet.
• Instruct patient to report twitching and/or eye spasms.
• Inform patient that hallucinations may occur.
• Advise patient not to remove blister from the outer pouch until just prior to taking the orally disintegrating tablet. The blister pack should be peeled open with dry hands and the tablet placed on the tongue, where it will disintegrate.
• Instruct patient to avoid drinking liquids or eating food 5 min before or after taking the orally disintegrating tablet.
• Caution patient to use drug exactly as prescribed. Explain that if drug is suddenly discontinued, parkinsonian crisis may occur.
• Advise patient not to exceed 10 mg/day dose (tablets or capsules); 2.5 mg/day for the orally disintegrating tablet.
• Inform patient and family of symptoms of hypertensive crisis. Instruct them to report severe headache or other unusual symptoms to health care provider immediately.

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