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Eldepryl is an antiparkinsonian drug that selectively and irreversibly blocks monoamine oxidase B in the brain (this enzyme takes part mainly in the dopamine destruction). Selegiline, the main component of Eldepryl, inhibits the metabolism of dopamine, increases its concentration in the central nervous system and prevents the deficiency of this substance in the extrapyramidal system. Selegiline does not affect the activity of serotonin and indirect adrenomimetics.
In the process of selegiline metabolism, derivatives are formed that inhibit the reuptake of dopamine in synapses.
Selegiline as part of complex therapy with levodopa prolongs and enhances its effect. It is possible to prescribe this drug during the use of levodopa only after reaching equilibrium concentrations. If the patient has fluctuations in the effectiveness of levodopa, the intake of selegiline is undesirable.
Indications for use
Eldepryl is used in the treatment of Parkinson’s disease, as well as in patients with symptomatic parkinsonism.
Eldepryl is recommended to be used as a monotherapy in the initial diagnosis. It is also possible to use these tablets in treatment regimens simultaneously with levodopa and other drugs.
Mode of application
Eldepryl is taken orally. Tablets are recommended to be taken as a whole with a small amount of liquid. Immediately after the first meal or after breakfast and lunch.
The starting dose of Eldepryl is 5–10 mg/day (in monotherapy or in combination with a peripheral decarboxylase inhibitor and levodopa).
The maximum maintenance dose of this antiparkinson drug is 10 mg/day. The use of higher doses of these tablets is not recommended.
A daily dose of 10 mg of selegiline can be divided into 2 portions.
After the start of combination therapy with levodopa, it is allowed to reduce the dose of the latter by 10-30% in the first 2-3 days of taking selegiline (the dose of levodopa can be reduced to a minimum that will allow you to control the symptoms of the disease).
The duration of Eldepryl is determined by a specialist.
While taking Eldepryl in patients, dry mouth, sleep disorders, and dizziness are possible. Less often, the development of a transient increase in the activity of aspartate and alanine transaminases was recorded (after the termination of Eldepryl intake, the activity of these enzymes returns to normal).
Rarely enough, during treatment with this medication, the appearance of cardiac arrhythmias (for example, supraventricular arrhythmia), atrioventricular blockade, and bradycardia was recorded.
Patients who received selegiline concurrently with levodopa also showed the appearance of motor disorders (e.g., dyskinesia), nausea, hypotension, xerostomia, vomiting, psychosis (including impaired orientation and hallucinations), sleep disturbances and headaches.
In rare cases, with combined treatment with levodopa and selegiline, the appearance of urination disorders, stool disorders, arrhythmias, appetite disorders, increased fatigue, tissue fluid retention, hypertension, and excessive arousal were noted. Also, in rare cases, the occurrence of skeletal muscle spasms, shortness of breath, angina attacks, leukopenia and an increase in the number of platelets were noted.
The occurrence of agitation and autokinesis was noted with the combined use of selegiline and maximum therapeutic doses of levodopa. These symptoms usually disappear on their own when the dose of levodopa is reduced.
Eldepryl is contraindicated in case of intolerance to the active and excipients of the tablets.
These tablets are not used in the treatment of patients suffering from peptic ulcer, extrapyramidal disorders that are not associated with a lack of dopamine (for example, Huntington’s chorea or essential tremor), as well as impaired function of the urinary system and liver.
Eldepryl is not used in pediatrics.
The complex administration of selegiline with levodopa is contraindicated in patients with thyrotoxicosis, arterial hypertension, angle-closure glaucoma, and pheochromocytoma.
The complex administration of levodopa and selegiline should not be prescribed to patients with tachyarrhythmia, benign prostatic hyperplasia, a pronounced form of angina pectoris, as well as progressive dementia and mental disorders.
Eldepryl is contraindicated during pregnancy.
- The combined use of Eldepryl tablets with drugs that inhibit the reuptake of serotonin (including paroxetine, fluoxetine, citalopram, fluvoxamine, sertraline), narcotic analgesics, monoamine oxidase inhibitors and other drugs that are serotonin agonists.
- Drugs that block the reuptake of serotonin can be taken only 14 days after taking the last Eldepryl tablet.
- Eldepryl can only be started within 7 days from the withdrawal of serotonin reuptake inhibitors (if the patient received fluoxetine, only within 5 weeks).
- Sumatriptan can be used only a day after taking the last selegiline tablet.
- Simultaneous administration of Eldepryl and preparations of the sympathomimetic group is not recommended.
- Eldepryl, when combined, potentiates and prolongs the effect of levodopa.
- An increase in the frequency of side effects with the combined use of selegiline with anticholinergics or amantadine is possible.
- It is forbidden to take alcohol on the background of treatment with selegiline tablets.
Eldepryl is characterized by low toxicity. There is the rapid destruction of selegiline in the body and a high rate of elimination of derivatives, which ensures low toxicity.
With an overdose of selegiline, a decrease in the selectivity and blockade of monoamine oxidase A is observed, which results in the lability of blood pressure. Significant inhibition of monoamine oxidase B results in vomiting.
There is no evidence of a specific antidote.
Monitoring of the patient’s condition is necessary with an overdose of selegiline. By the doctor’s decision, therapy may be conducted in accordance with the symptoms.