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. Clinical evidence demonstrates its efficacy in reducing motor fluctuations and extending therapeutic windows for patients experiencing symptom re-emergence. This second-generation MAO-B inhibitor offers neurologists a targeted mechanism of action with a well-established safety profile when administered within recommended parameters.
Features
- Contains selegiline hydrochloride 5 mg oral tablet formulation
- Selective and irreversible monoamine oxidase-B inhibition
- Blood-brain barrier permeable with preferential CNS activity
- Minimal dietary tyramine restrictions at recommended Parkinson’s doses (10 mg/day or less)
- Hepatic metabolism via cytochrome P450 system with active metabolites
- Compatible with standard levodopa/carbidopa regimens
Benefits
- Extends duration of levodopa efficacy by reducing dopamine catabolism
- Permits reduction of levodopa dosage while maintaining therapeutic effect
- Decreases “off” time periods and improves motor fluctuation management
- Demonstrates neuroprotective potential in preclinical models
- Delays disease progression milestones in early Parkinson’s patients
- Provides complementary mechanism to existing dopaminergic therapies
Common use
Eldepryl is primarily indicated as adjunctive therapy in the management of Parkinson’s disease patients being treated with levodopa/carbidopa who exhibit deteriorating response patterns. It is particularly valuable for patients experiencing end-of-dose akinesia or “wearing-off” phenomena. The medication may be initiated when motor fluctuations become clinically significant despite optimized levodopa dosing. Some practitioners also utilize Eldepryl in early Parkinson’s disease as monotherapy to delay the need for levodopa initiation, though this represents an off-label application. The drug’s mechanism makes it suitable for long-term management of neurodegenerative symptoms.
Dosage and direction
The recommended initial dosage for Parkinson’s patients is 5 mg administered orally twice daily, typically with breakfast and lunch. Administration later in the day may contribute to insomnia due to metabolite amphetamine effects. The maximum recommended daily dose is 10 mg. When used as adjunct therapy to levodopa/carbidopa, a approximately 10-30% reduction in levodopa dosage may be possible after several days of Eldepryl therapy. Dose adjustments should be made gradually under neurological supervision. Tablets should be swallowed whole with water and not crushed or chewed. Elderly patients may require dosage adjustments based on renal or hepatic function.
Precautions
Patients should be monitored for development of dyskinesias, hallucinations, or confusion, particularly when initiating therapy. Orthostatic hypotension may occur, requiring blood pressure monitoring. Caution is advised in patients with hepatic impairment or peptic ulcer disease. Abrupt withdrawal should be avoided due to potential rebound Parkinsonian symptoms. Dental procedures may require special consideration due to potential interactions with vasoconstrictors. Patients should be educated about recognizing serotonin syndrome symptoms when used with other serotonergic agents. Regular assessment of mental status and motor function is recommended throughout therapy.
Contraindications
Eldepryl is contraindicated in patients with known hypersensitivity to selegiline or any component of the formulation. Concurrent use with meperidine is absolutely contraindicated due to risk of severe reactions including hyperpyrexia and coma. It should not be administered with other MAO inhibitors or within 14 days of discontinuing such therapy. Contraindicated in patients with pheochromocytoma due to catecholamine interactions. Not recommended for use with dextromethorphan, tramadol, or other serotonin reuptake inhibitors due to serotonin syndrome risk. Patients with severe hepatic impairment should not receive this medication.
Possible side effects
Common adverse reactions (≥5%) include nausea, dizziness, insomnia, and orthostatic hypotension. Dyskinesias may occur or worsen in approximately 15% of patients. Less frequently reported effects include dry mouth, vivid dreams, hallucinations (particularly in elderly patients), and peripheral edema. Cardiovascular effects may include arrhythmias or palpitations. Gastrointestinal disturbances such as abdominal pain or constipation affect approximately 5-10% of users. Psychiatric effects including anxiety, confusion, or agitation may occur, particularly at higher doses. Skin reactions including rash have been reported in clinical trials.
Drug interaction
Significant interactions occur with other MAO inhibitors, SSRIs, SNRIs, tricyclic antidepressants, and sympathomimetic amines. Meperidine interaction may produce serotonin syndrome or hyperpyrexic crisis. Concomitant use with tyramine-rich foods is generally not restricted at Parkinson’s doses (≤10 mg/day), though caution is advised with very high tyramine content. May potentiate effects of CNS depressants including alcohol. Interactions with antihypertensive medications may produce orthostatic hypotension. Metabolism may be affected by CYP2B6 and CYP3A4 inhibitors or inducers. Caution with other dopaminergic agents may increase dopaminergic side effects.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is接近 time for the next scheduled dose. In that case, skip the missed dose and resume the regular dosing schedule. Do not double doses to make up for a missed dose. If multiple doses are missed, contact the prescribing physician for guidance on resumption of therapy. Consistent daily administration is important for maintaining stable dopamine levels. Patients should establish routine administration times to minimize forgetting doses.
Overdose
Symptoms of overdose may include severe hypertension, agitation, hallucinations, hyperpyrexia, and tachycardia. Serotonin syndrome manifestations including confusion, hyperreflexia, and incoordination may occur. In severe cases, seizures, coma, or cardiovascular collapse may develop. Management involves immediate discontinuation of the drug, symptomatic treatment, and supportive care. Hypertension may require alpha-adrenergic blocking agents. Benzodiazepines may be used for agitation or seizures. Dialysis is not effective due to high protein binding. Patients should seek immediate medical attention if overdose is suspected.
Storage
Store at controlled room temperature between 20°C to 25°C (68°F to 77°F). Excursions permitted between 15°C to 30°C (59°F to 86°F). Keep container tightly closed and protect from moisture and light. Keep out of reach of children and pets. Do not use after expiration date printed on packaging. Do not transfer tablets to other containers as moisture protection may be compromised. Properly dispose of unused medication through medication take-back programs.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Individual patient responses may vary. Treatment decisions should be made by qualified healthcare professionals based on comprehensive patient assessment. Full prescribing information should be consulted before administration. Not all potential interactions or side effects are listed here. Patients should report any adverse effects to their healthcare provider promptly.
Reviews
Clinical studies demonstrate that approximately 60-70% of patients experience meaningful reduction in “off” time when Eldepryl is added to levodopa therapy. Neurology specialists frequently report improved motor control and extended therapeutic windows in responsive patients. Some practitioners note particular benefit in patients with early wearing-off phenomena. Patient satisfaction surveys indicate improved quality of life measures related to reduced motor fluctuations. The medication generally receives positive evaluation in neurological practice for its targeted mechanism and generally manageable side effect profile when properly dosed.