Eldepryl: Advanced Adjunctive Therapy 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 to enhance the therapeutic management of Parkinson’s disease. As an adjunctive treatment to levodopa/carbidopa therapy, it represents a sophisticated pharmacological approach to modulating dopamine metabolism in the central nervous system. This medication demonstrates particular efficacy in managing motor fluctuations and “wearing-off” phenomena associated with long-term levodopa treatment. Clinical evidence supports its role in potentially delaying the need for levodopa dose escalation while maintaining neurological function.
Features
- Contains selegiline hydrochloride as active pharmaceutical ingredient
- Selective MAO-B inhibition with minimal effect on MAO-A at therapeutic doses
- Available in 5 mg oral tablet formulation
- Demonstrated blood-brain barrier permeability
- Standardized manufacturing under cGMP conditions
- Multiple pharmacokinetic studies establishing bioavailability profile
Benefits
- Extends duration of levodopa effectiveness by reducing dopamine metabolism
- May allow reduction of levodopa dosage while maintaining therapeutic effect
- Demonstrates potential neuroprotective properties in preclinical models
- Reduces frequency and severity of “off” periods in Parkinson’s patients
- May improve motor coordination and daily functioning
- Compatible with most standard Parkinson’s treatment regimens
Common use
Eldepryl is primarily indicated as adjunctive therapy in the management of Parkinson’s disease patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. It is particularly valuable for patients experiencing end-of-dose akinesia or the “wearing-off” phenomenon. The medication may be used throughout various stages of Parkinson’s disease, though clinical assessment should determine appropriate timing of initiation. Off-label uses may include certain cases of treatment-resistant depression, though this application requires careful specialist supervision due to pharmacological considerations.
Dosage and direction
The recommended initial dosage of Eldepryl is 5 mg orally twice daily, taken with breakfast and lunch. Dosage should not exceed 10 mg per day due to increased risk of non-selective MAO inhibition at higher doses. Administration with meals may help minimize potential gastrointestinal discomfort. Patients should maintain consistent timing of doses to ensure stable pharmacological effects. Dose adjustments should be made gradually under medical supervision, typically at 2-3 day intervals. Elderly patients or those with hepatic impairment may require dosage modification based on individual tolerance and metabolic capacity.
Precautions
Patients should be carefully monitored for the emergence of serotonin syndrome, particularly when used concomitantly with other serotonergic agents. Blood pressure monitoring is recommended, especially during initial treatment phases. Caution is advised in patients with cardiovascular disease, hepatic impairment, or peptic ulcer history. Regular assessment of psychiatric status is recommended due to potential mood alterations. Patients should be advised about the potential for orthostatic hypotension and educated about appropriate positional changes. Dental professionals should be informed of Eldepryl use due to potential interactions with vasoconstrictors.
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 severe reactions. Combination with other MAO inhibitors is prohibited. Use with sympathomimetic amines, including amphetamines and cold products containing pseudoephedrine or phenylephrine, is contraindicated. Patients with pheochromocytoma should not receive Eldepryl. Concomitant use with dextromethorphan is contraindicated due to risk of psychotic episodes.
Possible side effects
Common adverse reactions (≥5%) include nausea, dizziness, insomnia, and abdominal pain. Orthostatic hypotension may occur, particularly during dose titration. Less frequently reported effects include confusion, hallucinations, arrhythmias, and skin eruptions. Approximately 15% of patients may experience increased levodopa-associated side effects such as dyskinesias. Rare but serious effects include hypertensive crisis (particularly with tyramine-containing foods at higher doses), serotonin syndrome, and priapism. Most side effects are dose-dependent and may diminish with continued therapy or dosage adjustment.
Drug interaction
Eldepryl demonstrates significant interactions with numerous medication classes. Serotonergic agents (SSRIs, SNRIs, tricyclic antidepressants, tramadol) may precipitate serotonin syndrome. Concomitant use with sympathomimetics may cause hypertensive crisis. Opioid analgesics, particularly meperidine, are contraindicated. CYP450 interactions are possible, though selegiline is primarily metabolized via multiple pathways. Alcohol may enhance CNS depression effects. Antihypertensive agents may have potentiated effects. Careful medication review is essential before initiation and during therapy.
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. Patients should not double doses to make up for missed medication. Consistent timing is important for maintaining stable dopamine levels, but occasional missed doses are unlikely to cause significant clinical deterioration. Patients should maintain a medication diary if missed doses occur frequently.
Overdose
Symptoms of overdose may include severe hypertension, agitation, hallucinations, hyperpyrexia, and convulsions. In massive overdose, symptoms may progress to coma and cardiovascular collapse. Management requires immediate medical attention with supportive care and symptomatic treatment. Gastric lavage may be considered if presentation is early. Blood pressure management with appropriate antihypertensives may be necessary. There is no specific antidote; treatment should focus on supportive measures and management of specific symptoms. Dialysis is unlikely to be effective due to high protein binding.
Storage
Store at controlled room temperature between 20°C to 25°C (68°F to 77°F). Protect from light and moisture. Keep in original container with tight closure. Do not store in bathroom medicine cabinet due to humidity fluctuations. Keep out of reach of children and pets. Do not use if tablets show signs of discoloration or deterioration. 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 should be made by qualified healthcare professionals based on individual patient assessment. The prescribing physician should be consulted for specific dosage recommendations and treatment duration. Patients should not alter their medication regimen without professional guidance. While every effort has been made to ensure accuracy, pharmaceutical information may change as new clinical data emerges.
Reviews
Clinical studies demonstrate that approximately 60-70% of patients experience measurable improvement in motor fluctuations when Eldepryl is added to levodopa therapy. Long-term extension studies suggest sustained benefit for up to several years in responsive patients. Neurologists frequently report satisfactory management of wearing-off phenomena, though individual response varies. Some studies indicate potential slowing of disease progression, though this remains an area of ongoing research. Patient-reported outcomes often note improved quality of life and reduced “off” time duration. The medication generally maintains favorable tolerability profiles in appropriate patient populations.