Eldepryl: Advanced MAO-B Inhibitor for Parkinson's Disease Management
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Synonyms
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Eldepryl (selegiline hydrochloride) is a selective monoamine oxidase-B inhibitor specifically formulated for the treatment of Parkinson’s disease. As an adjunct therapy to levodopa/carbidopa, it enhances dopaminergic activity in the central nervous system by reducing the breakdown of dopamine, thereby extending therapeutic effects and improving motor control. Its targeted mechanism offers neurologists a valuable tool for optimizing long-term Parkinson’s management strategies while maintaining a favorable safety profile when administered at recommended doses.
Features
- Contains selegiline hydrochloride as active pharmaceutical ingredient
- Selective monoamine oxidase-B (MAO-B) inhibition
- Available in 5 mg oral tablet formulation
- Demonstrated blood-brain barrier penetration
- Tyramine-sparing effect at recommended Parkinson’s doses (≤10 mg/day)
- Synergistic action with levodopa therapies
Benefits
- Extends duration of levodopa effectiveness by reducing dopamine metabolism
- Allows reduction of levodopa dosage in some patients, potentially minimizing long-term side effects
- Improves motor symptoms including tremor, rigidity, and bradykinesia
- May provide neuroprotective effects through reduction of oxidative stress
- Delays disease progression in early Parkinson’s cases when initiated promptly
- Enhances overall quality of life through improved symptom control
Common use
Eldepryl is primarily indicated as adjunctive treatment in the management of Parkinson’s disease patients being treated with levodopa/carbidopa who exhibit deterioration in quality of symptom control. It is particularly valuable for patients experiencing end-of-dose “wearing off” phenomena, where the duration of levodopa effectiveness diminishes between doses. The medication may also be used as monotherapy in early Parkinson’s disease to delay the need for levodopa initiation, though this application requires careful patient selection and monitoring.
Dosage and direction
The recommended dosage for Parkinson’s disease patients is 5 mg taken orally twice daily, with breakfast and lunch. Administration with food may minimize potential gastrointestinal discomfort. The maximum daily dose should not exceed 10 mg. When used as adjunct therapy to levodopa, the dose of levodopa may need to be reduced gradually, typically by 10-30%, after several days of Eldepryl therapy to avoid excessive dopaminergic effects. For monotherapy in early Parkinson’s disease, the initial dose is 5 mg once daily, which may be increased to 5 mg twice daily if tolerated. Elderly patients or those with hepatic impairment may require dosage adjustment based on clinical response and tolerance.
Precautions
Patients should be carefully monitored for the emergence of excessive dopaminergic effects, including dyskinesias, hallucinations, or confusion. Blood pressure should be monitored regularly, particularly during initial therapy and dosage adjustments. Caution is advised in patients with history of peptic ulcer disease, as selegiline may increase gastric acid secretion. Hepatic function should be assessed periodically during long-term therapy. Patients should be educated about the potential for orthostatic hypotension and advised to rise slowly from sitting or lying positions. Those with cardiac arrhythmias or history of myocardial infarction require careful cardiovascular monitoring.
Contraindications
Eldepryl is contraindicated in patients with known hypersensitivity to selegiline hydrochloride or any component of the formulation. Concurrent use with meperidine is absolutely contraindicated due to risk of serotonin syndrome and severe adverse reactions. The medication should not be administered with other monoamine oxidase inhibitors (MAOIs), including linezolid and intravenous methylene blue. Contraindication extends to concomitant use with sympathomimetic amines, including amphetamines, cold products containing pseudoephedrine or phenylephrine, and weight control products. Patients with pheochromocytoma should not receive Eldepryl due to risk of hypertensive crisis.
Possible side effects
Common adverse reactions (≥5%) include nausea, dizziness, insomnia, and abdominal pain. Dopaminergic side effects may occur, such as dyskinesias, hallucinations, confusion, and vivid dreams. Orthostatic hypotension has been reported in approximately 4-9% of patients. Less frequently, patients may experience dry mouth, vivid dreams, arrhythmias, or skin rash. At higher doses (>10 mg/day), the risk of hypertensive crisis increases significantly due to loss of MAO-B selectivity. Serotonin syndrome may occur when combined with serotonergic drugs, characterized by agitation, confusion, tachycardia, and hyperthermia.
Drug interaction
Significant interactions occur with other MAO inhibitors, SSRIs, SNRIs, tricyclic antidepressants, and tramadol, potentially leading to serotonin syndrome. Concomitant use with sympathomimetic agents may precipitate hypertensive crisis. Eldepryl may potentiate the effects of CNS depressants including alcohol, benzodiazepines, and opioids. The metabolism of selegiline may be affected by CYP2B6 and CYP3A4 inhibitors or inducers. Careful monitoring is required when administering with antihypertensive agents due to potential additive hypotensive effects. Interaction with tyramine-containing foods is minimal at recommended Parkinson’s doses (≤10 mg/day) but becomes significant at higher doses.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed administration. Consistent timing of doses is important for maintaining stable drug levels and optimal therapeutic effect. If multiple doses are missed, consultation with a healthcare provider is recommended before resuming therapy, as dosage adjustment may be necessary.
Overdose
Symptoms of overdose may include severe hypertension, agitation, hallucinations, hyperpyrexia, and seizures. In massive overdose, the MAO-B selectivity is lost, and symptoms resemble those of non-selective MAOI overdose, including hypertensive crisis with potential for intracranial bleeding. Management requires immediate medical attention with intensive supportive care. Blood pressure should be controlled using rapidly titratable antihypertensive agents such as phentolamine. Symptomatic treatment for agitation or seizures may include benzodiazepines. Activated charcoal may be administered if presentation is early after ingestion. Patients require cardiac monitoring for at least 24 hours due to potential delayed toxicity.
Storage
Store at controlled room temperature between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). Keep in the original container with the lid tightly closed to protect from moisture and light. Do not store in bathroom areas where humidity fluctuations may occur. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the packaging. Properly dispose of any unused medication through medication take-back programs or according to local regulations.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made by qualified healthcare professionals based on individual patient circumstances. The prescribing physician should be consulted for specific dosage recommendations and treatment duration. Patients should not alter their medication regimen without medical supervision. While every effort has been made to ensure accuracy, medical knowledge evolves, and healthcare providers should consult current prescribing information and clinical guidelines.
Reviews
Clinical studies demonstrate that approximately 60-70% of Parkinson’s patients experience improved motor function and reduced “off” time when Eldepryl is added to levodopa therapy. Long-term extension studies show sustained benefit for up to 5 years in responsive patients. Neurologists report particular value in managing wearing-off phenomena and delaying disease progression in early-stage patients. Patient-reported outcomes indicate improvements in activities of daily living and quality of life measures. The medication is generally well-tolerated, with discontinuation rates due to adverse effects ranging from 5-8% in clinical trials. Specialist consensus supports its role as a valuable adjunct therapy in appropriately selected Parkinson’s disease patients.