Eldepryl (selegiline hydrochloride) is a selective monoamine oxidase-B inhibitor indicated as an adjunct treatment in the management of Parkinson’s disease. It is used alongside levodopa/carbidopa therapy to help reduce motor fluctuations and extend the therapeutic window of levodopa. By inhibiting the breakdown of dopamine in the brain, Eldepryl supports more stable dopamine levels, contributing to improved symptom control. This medication represents a key option in the long-term management strategy for patients experiencing “wearing-off” phenomena.

Features

• Active ingredient: Selegiline hydrochloride
• Available in 5 mg oral tablet and orally disintegrating tablet formulations
• Selective and irreversible inhibition of monoamine oxidase-B (MAO-B)
• Metabolized to active metabolites: L-amphetamine and L-methamphetamine
• Designed for convenient once or twice daily dosing, depending on indication and formulation

Benefits

• Extends the duration of levodopa effect, reducing “off” time in Parkinson’s disease
• May allow for reduction in the total daily dose of levodopa
• Contributes to smoother motor function throughout the day
• Supports long-term management of Parkinsonian symptoms
• Oral disintegrating formulation offers administration flexibility for patients with swallowing difficulties

Common use

Eldepryl is primarily used as an adjunctive treatment to levodopa/carbidopa in the management of Parkinson’s disease patients who exhibit deterioration in the quality of their response to levodopa therapy. It is particularly beneficial for individuals experiencing end-of-dose “wearing off” phenomena. The medication may be used in both newly diagnosed patients and those with more advanced disease. Some clinicians may consider its use in early Parkinson’s disease as monotherapy, though this is not the primary indication.

Dosage and direction

For adjunct treatment with levodopa/carbidopa in Parkinson’s disease: The recommended starting dose is 5 mg taken orally at breakfast and lunch. After two or three days, the morning dose may be increased to 10 mg if necessary. The maximum recommended daily dose is 10 mg. For the orally disintegrating formulation: 1.25 mg once daily before breakfast without liquid. The tablet should be placed on the tongue and allowed to disintegrate. Dosage adjustments should be made gradually under medical supervision based on therapeutic response and tolerability. Patients should be advised to avoid taking Eldepryl in the evening or late afternoon due to potential insomnia.

Precautions

Patients should be monitored for the development of hypertension, especially during dose titration. Orthostatic hypotension may occur, particularly when beginning therapy. Caution should be exercised in patients with hepatic impairment, as selegiline is extensively metabolized in the liver. Regular monitoring for mood changes, including depression or suicidal ideation, is recommended. Patients should be advised about the potential for dizziness and cautioned against driving or operating machinery until they know how Eldepryl affects them. Dental health should be monitored in patients using the orally disintegrating formulation due to its acidic nature.

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 the risk of serotonin syndrome and other serious reactions. The combination with other MAO inhibitors is contraindicated. Use with sympathomimetic amines, including amphetamines, cold products containing decongestants, and weight control products should be avoided. Eldepryl is contraindicated in patients with pheochromocytoma due to the risk of hypertensive crisis.

Possible side effects

Common adverse reactions (≥5%) include nausea, dizziness, lightheadedness, abdominal pain, dry mouth, vivid dreams, and sleep disturbances. Less frequently reported effects include orthostatic hypotension, arrhythmias, angina, confusion, hallucinations, and skin rash. The orally disintegrating formulation may cause mouth irritation or ulceration. Some patients may experience increased dyskinesias due to enhanced dopaminergic activity. Mood changes, including anxiety and agitation, have been reported. Most side effects are dose-dependent and may diminish with dosage adjustment.

Drug interaction

Eldepryl exhibits significant interactions with numerous medications. Concomitant use with SSRIs, SNRIs, tricyclic antidepressants, and other serotonergic drugs may precipitate serotonin syndrome. The combination with sympathomimetics can cause hypertensive crisis. Concurrent use with dextromethorphan may lead to psychosis or bizarre behavior. Coadministration with certain opioids, particularly meperidine, is contraindicated. Eldepryl may potentiate the effects of CNS depressants including alcohol, benzodiazepines, and opioids. Caution is advised with tyramine-containing foods, though dietary restrictions are less stringent with the selective MAO-B inhibition at recommended doses.

Missed dose

If a dose is missed, it should be taken as soon as remembered unless it is close to 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 one. For the orally disintegrating formulation, if a dose is missed, it should be taken as soon as remembered unless it is after 12:00 noon, in which case it should be skipped. Consistency in dosing timing is important for maintaining stable drug levels and therapeutic effect.

Overdose

Symptoms of overdose may include severe hypertension, agitation, hallucinations, hyperpyrexia, and tachycardia. In severe cases, seizures, coma, or cardiovascular collapse may occur. Management is supportive and symptomatic. Gastric lavage may be considered if presentation is early. Activated charcoal may be administered. Hypertension should be managed with appropriate antihypertensive agents, preferably short-acting ones such as phentolamine. Close monitoring of vital signs and cardiac function is essential. There is no specific antidote for selegiline overdose.

Storage

Store at controlled room temperature between 20°C to 25°C (68°F to 77°F). Keep in the original container with the lid tightly closed to protect from moisture and light. The orally disintegrating tablets should be kept 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. Do not transfer tablets to other containers, as this may affect stability. Protect from excessive heat and humidity.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Individual patient needs may vary. Treatment decisions should be made in consultation with a qualified healthcare professional familiar with the patient’s specific medical history and current condition. The prescribing physician should be consulted for complete prescribing information, including boxed warnings. Dosage must be individualized based on therapeutic response and tolerance.

Reviews

Clinical studies have demonstrated Eldepryl’s efficacy in reducing “off” time by approximately 1-2 hours per day when used as adjunct therapy to levodopa. Many patients report improved consistency in motor function throughout the day. Neurologists often note that the medication is particularly valuable for patients experiencing predictable end-of-dose deterioration. Some patients report improved overall quality of life and reduced dependency on caregivers. The orally disintegrating formulation has been praised for its convenience, especially in patients with swallowing difficulties. Long-term follow-up studies suggest sustained benefits with appropriate dose management.