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Uses

Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.

Parkinsonian Syndrome

Symptomatic treatment of parkinsonian syndrome; designated an ophan drug by FDA for this condition.

Used as adjunctive therapy in parkinsonian patients who exhibit a deteriorating response to levidopa/carbidopa. Appears to be most beneficial when used during the early stages of the “wearing off” effect. Epecially useful in improving “end-of-dose” motor fluctuations.

Has been used effectively as monotherapy in patients with newly diagnosed parkinsonian syndrome†. Because selegiline is well tolerated and possibly neuroprotective (i.e., reduces the rate of progression of parkinsonian syndrome), some clinicians initiate therapy with selegiline in such patients, reserving levodopa or another agent (i.e., dopamine agonist) until manifestations become severe enough to warrant more aggressive therapy.

Alzheimer’s Disease

Has been used with equivocal results for the palliative treatment of mild to moderate dementia of the Alzheimer’s type† (Alzheimer’s disease, presenile or senile dementia).

Dosage and Administration

General

Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.

Concomitant Levodopa/Carbidopa Therapy
• In patients receiving concomitant levodopa/carbidopa, an attempt to reduce levodopa/carbidopa dosage may be made after 2–3 days of selegiline therapy.
• Reduction in levodopa dosage of at least 10–30% may be needed if dyskinesias develop during selegiline therapy.
• Further reduction in levodopa/carbidopa dosage may be possible during continued selegiline therapy.

Administration

Oral Administration

Administer orally, usually in 2 equally divided doses daily (generally at breakfast and lunch to avoid interference with sleep).

Dosage

Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.

Available as selegiline hydrochloride; dosage expressed in terms of the salt.

Adults

Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.

Parkinsonian Syndrome

Oral

Usual dosage: 5 mg twice daily.

Some clinicians suggest an initial dosage of 2.5 mg daily in patients receiving concomitant levodopa/carbidopa; may increase dosage gradually up to 5 mg twice daily.

Prescribing Limits

Adults

Parkinsonian Syndrome

Oral

Maximum 10 mg daily. (See Risks Associated with MAO Inhibition under Cautions.)

Special Populations

No special population dosage recommendations.

Cautions

Contraindications

• Known hypersensitivity to selegiline or any ingredient in the formulation.
• Concomitant administration of meperidine and possibly other opiates. (See Specific Drugs and Foods under Interactions.)

Warnings/Precautions

Warnings

Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.

Risks Associated with MAO Inhibition

Selectivity for MAO-B is relative. At dosage of 10 mg daily, selegiline hydrochloride inhibits cerebral MAO-B while having little effect on MAO-A in the GI tract and liver. At high dosages (e.g., >30 mg daily), the selectivity usually diminishes and the drug will inhibit MAO-B and MAO-A.

Hypertensive crises following ingestion of foods containing large amounts of tyramine (i.e., cheese reaction) have occurred in patients receiving nonselective MAO inhibitors. Hypertensive reactions reported rarely in patients receiving selegiline hydrochloride 10 mg daily (the maximum recommended dosage); at dosages >10 mg daily, the likelihood of hypertensive reactions increases. Use selegiline with caution regardless of the dosage. (See Interactions and also Advice to Patients.)

Concomitant use of highly serotonergic drugs (e.g., SSRIs, tricyclic antidepressants) and MAO inhibitors, including selegiline, is potentially hazardous and may result in serotonin syndrome. Generally avoid concomitant use. (See Interactions.)

Because of the complexitiy of the MAO enzyme system, observe patients closely for atypical responses.

General Precautions

Exacerbation of Levodopa-associated Adverse Effects

Selegiline may exacerbate levodopa-associated adverse effects (e.g., dyskinesias), presumably by increasing dopaminergic activity; effects generally can be mitigated by reducing the levodopa dosage by 10–30%.

Specific Populations

Pregnancy

Category C.

Lactation

Not known whether selegiline is distributed into milk. Give consideration to discontinuing the use of all but absolutely essential drug therapy in nursing women.

Pediatric Use

Safety and efficacy not established.

Geriatric Use

Safety and efficacy in geriatric patients have not been studied specifically to date; however, parkinsonian syndrome, for which safety and efficacy have been established, occurs principally in patients >50 years of age.

Common Adverse Effects

Nausea; dizziness, lightheadedness, or fainting; abdominal pain; hallucinations; dry mouth; vivid dreams; dyskinesias; headache.

Many of the adverse effects in patients receiving selegiline plus levodopa result from increased dopaminergic activity and can be mitigated by reducing levodopa dosage; these effects include exacerbation of dyskinesias, confusion, and hallucinations.