Eldepryl: Advanced MAO-B Inhibition for Parkinson's Disease Management
Eldepryl
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Synonyms
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Eldepryl (selegiline hydrochloride) represents a cornerstone in the adjunctive treatment of Parkinson’s disease, specifically engineered to enhance dopaminergic activity through selective monoamine oxidase type B (MAO-B) inhibition. This medication works by irreversibly blocking the MAO-B enzyme, which is responsible for breaking down dopamine in the brain, thereby prolonging the therapeutic effect of levodopa and reducing motor fluctuations. Clinical evidence supports its role in decreasing “off” time and improving motor control when used in combination with levodopa/carbidopa. For appropriate patients under specialist supervision, Eldepryl offers a mechanism to optimize long-term neurological management.
Features
- Active ingredient: Selegiline hydrochloride
- Available in 5 mg oral tablet and 1.25 mg orally disintegrating tablet formulations
- Selective, irreversible monoamine oxidase type B (MAO-B) inhibitor
- Compatible with levodopa/carbidopa regimens
- Manufactured under strict pharmaceutical quality controls
Benefits
- Extends the duration of levodopa effect, reducing “wearing-off” phenomena
- May allow for reduction in levodopa dosage, potentially minimizing dyskinesias
- Contributes to improved motor scores and daily living activities in Parkinson’s disease
- Selective MAO-B inhibition minimizes dietary tyramine restrictions at low doses
- Supports long-term dopaminergic therapy strategy
Common use
Eldepryl is indicated as an adjunctive treatment to levodopa/carbidopa in the management of Parkinson’s disease. It is used in patients experiencing motor fluctuations, particularly those with end-of-dose “wearing off” effects. It is not recommended as monotherapy in early Parkinson’s disease except in specific clinical circumstances. Off-label uses may include support in certain cases of treatment-resistant depression, though this application requires careful specialist evaluation due to pharmacological considerations.
Dosage and direction
The recommended initial dosage of Eldepryl tablets is 5 mg taken orally twice daily, with breakfast and lunch. The orally disintegrating formulation is typically initiated at 1.25 mg once daily for at least six weeks, after which the dose may be increased to a maximum of 2.5 mg daily. Administration should occur before noon to minimize potential insomnia. Dosage adjustments should be made gradually under neurological supervision, often with concurrent reduction in levodopa dosage by approximately 10-30% to optimize therapeutic effect while minimizing adverse reactions.
Precautions
Patients should be monitored for the emergence or worsening of dyskinesias, orthostatic hypotension, and mental status changes including confusion, hallucinations, or impulsive behaviors. Caution is advised in patients with hepatic impairment, severe cardiovascular disease, or history of peptic ulcer disease. Elderly patients may require more gradual titration. Abrupt discontinuation should be avoided. At doses exceeding 10 mg daily, non-selective MAO inhibition occurs, requiring strict dietary tyramine restriction to prevent hypertensive crisis.
Contraindications
Eldepryl is contraindicated in patients with known hypersensitivity to selegiline or any component of the formulation. Concomitant use with meperidine is absolutely contraindicated due to risk of serotonin syndrome and severe adverse reactions. Combination with other MAO inhibitors, serotonin reuptake inhibitors (SSRIs, SNRIs), tricyclic antidepressants, sympathomimetics, or dextromethorphan is prohibited. Use is contraindicated in patients with pheochromocytoma due to catecholamine interaction risks.
Possible side effects
Common adverse reactions (≥5%) include nausea, dizziness, insomnia, abdominal pain, dry mouth, and orthostatic hypotension. Less frequently reported effects include confusion, hallucinations, vivid dreams, arrhythmias, mouth ulcers (with orally disintegrating tablets), and skin rash. Dyskinesias may occur or worsen due to enhanced dopaminergic activity. At higher doses (>10 mg/day), hypertensive crisis may occur with tyramine-containing foods. Most side effects are dose-dependent and may diminish with dosage adjustment.
Drug interactions
Significant interactions occur with serotonergic agents (SSRIs, SNRIs, tricyclics, tramadol, triptans) risking serotonin syndrome. Concomitant use with sympathomimetics (decongestants, stimulants) may cause hypertensive crisis. Opioids, particularly meperidine, are contraindicated. Coadministration with carbamazepine, oxcarbazepine, or other MAO inhibitors is not recommended. Tyramine-containing foods and beverages require caution at doses exceeding 10 mg daily. Alcohol may enhance CNS depression effects.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is接近 the time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Doubling doses is not recommended due to increased risk of adverse effects. Patients should maintain consistent dosing times to optimize therapeutic levels and minimize motor fluctuations.
Overdose
Symptoms of overdose may include severe hypertension, agitation, hallucinations, hyperpyrexia, and seizures. Serotonin syndrome manifestations include mental status changes, autonomic instability, and neuromuscular abnormalities. Management involves immediate discontinuation of Eldepryl, symptomatic and supportive care, with careful monitoring of vital signs. Benzodiazepines may be used for agitation or seizures. Hypertension may require management with alpha-adrenergic blockers. Dialysis is not effective due to high protein binding.
Storage
Store at controlled room temperature (20-25°C or 68-77°F) in the original container, protected from light and moisture. Keep orally disintegrating tablets in the blister package until immediately before use. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging. Proper disposal of unused medication should follow local regulations for pharmaceutical waste.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient circumstances. Dosage and administration should follow prescribing information and professional guidelines. Patients should consult their neurologist before making any changes to their medication regimen.
Reviews
Clinical studies demonstrate that approximately 60-70% of patients experience measurable reduction in “off” time when Eldepryl is added to levodopa therapy. Long-term extension studies suggest sustained benefit for up to 5 years in responsive patients. Patient-reported outcomes indicate improved quality of life measures related to motor function and daily activities. Specialist consensus supports its role as a valuable adjunct therapy in appropriately selected Parkinson’s disease patients experiencing motor complications.