Jumex^® (Tablets) Instructions for Use

Marketing Authorization Holder

Chinoin Pharmaceutical and Chemical Works Private, Co. Ltd. (Hungary)

ATC Code

N04BD01 (Selegiline)

Active Substance

Selegiline (Rec.INN registered by WHO)

Dosage Form

Jumex®

Tablets 5 mg: 50 pcs.

Dosage Form, Packaging, and Composition

Tablets are white or almost white, round, flat, with the engraving “JU” on one side and a bevel on both sides.

Excipients: magnesium stearate, talc, povidone K-25, corn starch, lactose.

10 pcs. – blisters (5) – cardboard packs.

Clinical-Pharmacological Group

Antiparkinsonian drug – selective MAO type B inhibitor

Pharmacotherapeutic Group

Antiparkinsonian agent – MAO inhibitor

Pharmacological Action

Selegiline is a selective inhibitor of MAO type B, which is involved in the metabolism of dopamine and other catecholamines. It also inhibits the reuptake of dopamine at the level of presynaptic dopamine receptors, thereby contributing to an increase in its concentration in the nuclei of the extrapyramidal system and other parts of the brain.

Selegiline potentiates and prolongs the effect of levodopa in the treatment of parkinsonism.

Selegiline is not intended for use in patients with extrapyramidal symptoms not accompanied by dopamine deficiency (essential tremor, Huntington’s chorea).

Pharmacokinetics

When taken orally, Selegiline is rapidly and intensively absorbed. After oral administration of 10 mg of selegiline, the C_max of the unchanged drug in plasma is 2.7±2.2 ng/ml, the time to reach C_max is 0.5-2 hours. Plasma protein binding is 94%. Selegiline is rapidly distributed and metabolized in the body. The main metabolites are L-methamphetamine, L-amphetamine and N-desmethylselegiline. The active substance and its metabolites penetrate the blood-brain barrier well. Selegiline metabolites are excreted mainly in the urine (approximately 73% of the administered dose is excreted in the urine within 72 hours), about 15% through the intestines.

Indications

• Parkinson’s disease and symptomatic parkinsonism.

Selegiline can be used as monotherapy in the early stages of Parkinson’s disease to delay the prescription of levodopa (with or without a peripheral decarboxylase inhibitor (PDI)), and can also be used in combination with levodopa (with or without a PDI).

ICD codes

Dosage Regimen

The drug is prescribed orally at a dose of 5-10 mg/day, both as monotherapy and in combination with levodopa or a levodopa/PDI combination. The tablets should be taken without chewing, with a small amount of liquid.

Jumex^® can be taken once in the morning. If the daily dose is 10 mg, it can be divided into two doses – in the morning and in the evening.

When used in combination with levodopa, the dose of levodopa can be reduced by an average of 30%.

Adverse Reactions

During monotherapy, Jumex^® is usually well tolerated.

Allergic reactions: skin rash, shortness of breath, bronchospasm, photosensitization.

Gastrointestinal system: nausea, dry mouth, decreased appetite, constipation or diarrhea, dysphagia.

Cardiovascular system: orthostatic (postural) hypotension, rarely – increased blood pressure, arrhythmia.

CNS: insomnia, dizziness, mood changes, increased fatigue, dyskinesias, rarely – psychoses.

Liver: increased activity of liver transaminases.

Urinary system: in some cases – urinary retention, rarely – painful urge to urinate, nocturia.

Other: headache, blurred vision, diplopia, sometimes – hair loss, increased sweating, hypoglycemia.

When combined with levodopa

Since Jumex^® potentiates the clinical effect of levodopa, the adverse reactions of levodopa (agitation, hyperkinesis, abnormal movements, anxious agitation, confusion, hallucinations, postural hypotension, cardiac arrhythmias) may worsen during combination therapy (levodopa should always be given in combination with a peripheral decarboxylase inhibitor). During combination therapy with selegiline and levodopa, a further reduction in the dose of levodopa (up to 30%) is possible.

Contraindications

• Hypersensitivity to selegiline;
• Combination with serotonin reuptake inhibitors, tricyclic antidepressants, sympathomimetics and pethidine (meperidine), including the period up to 5 weeks after their withdrawal;
• Extrapyramidal disorders not associated with dopamine deficiency (essential tremor, Huntington’s chorea);
• Pregnancy;
• Breastfeeding.

With caution: in patients with gastric and duodenal ulcers (including history), with labile blood pressure, tachycardia, severe angina, psychosis, dementia, tardive dyskinesia, coarse tremor, thyrotoxicosis, diffuse toxic goiter, pheochromocytoma, prostatic hyperplasia (with residual urine), angle-closure glaucoma, under 18 years of age (insufficient experience with clinical use).

When combined with levodopa

• Open-angle glaucoma (chronic course);
• Hepatic and/or renal failure;
• Melanoma (including history);
• CNS depression;
• Convulsive seizures;
• Bronchial asthma;
• Pulmonary emphysema;
• Myocardial infarction (including history, as well as in combination with atrial, nodal or ventricular arrhythmias).

It is recommended to exercise caution regarding general anesthesia during surgical interventions in patients receiving MAO inhibitors.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Use in Hepatic Impairment

Use in combination with levodopa is contraindicated in hepatic failure.

Use in Renal Impairment

Use in combination with levodopa is contraindicated in renal failure.

Pediatric Use

With caution: in patients under 18 years of age (insufficient experience with clinical use).

Special Precautions

Since Jumex^® potentiates the effect of levodopa, the side effects of levodopa may be enhanced, especially when using high doses of levodopa. In such cases, strict monitoring of the patient’s condition is necessary. The use of Jumex^® in the treatment with levodopa may cause involuntary movements and/or agitation in patients. These side effects disappear when the dose of levodopa is reduced. When Jumex^® and levodopa are used simultaneously, the dose of levodopa can be reduced by an average of 30%.

Jumex^® should not be used in doses exceeding the recommended ones (10 mg/day), because the drug loses selectivity for MAO type B, which increases the risk of developing hypertension.

Effect on the ability to drive vehicles and mechanisms

Studies to evaluate the effect of Jumex^® on the ability to drive a car and perform work associated with increased danger have not been conducted.

Nevertheless, one should refrain from engaging in potentially hazardous activities that require increased attention and speed of mental and motor reactions.

Overdose

Overdose does not have a specific clinical picture.

However, since selective inhibition of MAO type B by selegiline is achieved only when taking doses recommended for the treatment of Parkinson’s disease (i.e., 5-10 mg/day), the symptoms of overdose may be similar to the symptoms of an overdose of non-selective MAO inhibitors (disorders of the central nervous and cardiovascular systems).

There is no specific antidote; treatment is symptomatic.

Drug Interactions

Contraindicated combinations.

Sympathomimetics: when treating with Jumex^®, the use of sympathomimetics should be avoided due to the danger of increased blood pressure.

Pethidine: the incompatibility between non-selective MAO inhibitors and pethidine is well known. Although the mechanism of this interaction is still unknown, the concomitant use of the selective MAO inhibitor, Jumex^®, and pethidine or another opioid analgesic is contraindicated.

Serotonin reuptake inhibitors: Jumex^® should not be used concomitantly with fluoxetine, as agitation, hypertension, convulsions, ataxia, hallucinations, and manic psychosis may develop, and fluoxetine should not be used for 14 days after discontinuation of Jumex^®. Since fluoxetine has a very long half-life, at least 5 weeks should elapse after discontinuation of fluoxetine and before prescribing Jumex^®. Similar phenomena have been described in patients receiving Jumex^® and two other serotonin reuptake inhibitors (sertraline and paroxetine). Since the mechanism of these reactions is not fully understood, it is recommended to avoid the combination of Jumex^® with serotonin reuptake inhibitors.

Tricyclic antidepressants: in some cases, severe toxicity of the central nervous system (dizziness, tremor, seizures), sometimes accompanied by hypertension, hypotension, profuse sweating, has been described in patients using a combination of tricyclic antidepressants and Jumex^®. Since the mechanism of these reactions is not fully understood, it is recommended to avoid the concomitant administration of Jumex^® with tricyclic antidepressants.

Not recommended combinations.

MAO inhibitors: Concomitant use of Jumex^® and MAO inhibitors may cause a sharp drop in blood pressure.

Food interaction

Unlike traditional MAO inhibitors, which suppress both MAO type A and MAO type B enzymes, Jumex^® is a specific inhibitor of MAO type B.

When taking food containing tyramine during treatment with Jumex^® at recommended doses, no hypertensive effect has been described (i.e., it does not cause the so-called “cheese effect”).

Therefore, patients receiving Jumex^® may not adhere to a strict diet.

However, in the case of combined use of Jumex^® and traditional MAO inhibitors or MAO type A inhibitors, it is recommended to adhere to dietary restrictions (i.e., avoid foods high in tyramine, such as: mature cheese and yeast products).

Other interactions

It enhances the effects of levodopa, ethanol, drugs that depress the central nervous system, and increases the risk of side effects of amantadine.

Storage Conditions

At a temperature not exceeding 30°C (86°F). Keep out of reach of children! List B.

Shelf Life

Shelf life – 3 years. Do not use the drug after the expiration date printed on the package.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.