Ipidacrine-SZ (Tablets) Instructions for Use

Marketing Authorization Holder

Severnaya Zvezda NAO (Russia)

Contact Information

SEVERNAYA ZVEZDA NAO (Russia)

ATC Code

N07AA (Anticholinesterase agents)

Active Substance

Ipidacrine (Rec.INN registered by WHO)

Dosage Form

Ipidacrine-SZ

Tablets 20 mg: 30 or 50 pcs.

Dosage Form, Packaging, and Composition

Tablets white or almost white, round, flat-cylindrical with a bevel.

Excipients: potato starch, lactose monohydrate (milk sugar) – 65 mg, polyvinyl alcohol, calcium stearate.

10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (5) – cardboard packs.
50 pcs. – polymer jars (1) – cardboard packs.
50 pcs. – polymer bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Cholinesterase inhibitor

Pharmacotherapeutic Group

Cholinesterase inhibitor

Pharmacological Action

Ipidacrine has a direct stimulating effect on the conduction of impulses along nerve fibers, interneuronal and neuromuscular synapses of the peripheral and central nervous systems.

The pharmacological action of ipidacrine is based on a combination of two mechanisms of action:

• Blockade of potassium channels in the membrane of neurons and muscle cells;

• Reversible inhibition of cholinesterase in synapses.

Ipidacrine enhances the effect on smooth muscles not only of acetylcholine, but also of adrenaline, serotonin, histamine, and oxytocin.

The drug Ipidacrine-SZ has the following pharmacological effects:

• Improves and stimulates impulse conduction in the nervous system and neuromuscular transmission;

• Enhances the contractility of smooth muscle organs under the influence of agonists of acetylcholine, adrenaline, serotonin, histamine, and oxytocin receptors, with the exception of potassium chloride;

• Improves memory, inhibits the progressive course of dementia.

In preclinical studies, Ipidacrine did not have teratogenic, embryotoxic, mutagenic, carcinogenic, or immunotoxic effects and did not affect the endocrine system.

Pharmacokinetics

Absorption

After oral administration, the drug is rapidly absorbed from the gastrointestinal tract. C_max in blood plasma is reached after 1 hour.

Distribution

Binding to blood plasma proteins is 40-50%. Ipidacrine quickly enters the tissues; the distribution half-life is 40 min.

Metabolism and excretion

It is metabolized in the liver. Excretion is carried out through the kidneys, as well as extrarenally (through the gastrointestinal tract). Excretion of ipidacrine by the kidneys occurs mainly through tubular secretion, and only 1/3 of the dose is excreted by glomerular filtration.

Indications

Diseases of the peripheral nervous system:

• Mono- and polyneuropathy;

• Polyradiculopathy;

• Myasthenia gravis and myasthenic syndrome of various etiologies.

Diseases of the central nervous system:

• Bulbar palsies and paresis;

• Recovery period of organic lesions of the central nervous system, accompanied by motor and/or cognitive impairments.

Treatment and prevention of intestinal atony.

ICD codes

Dosage Regimen

Orally. Doses and duration of treatment are determined individually depending on the severity of the disease.

Diseases of the peripheral nervous system: mono- and polyneuropathy, polyradiculopathy, myasthenia gravis and myasthenic syndrome of various etiologies

The recommended dose is 10-20 mg (0.5-1 tablet) 1-3 times/day.

The course of treatment is from 1 to 2 months. If necessary, the course of treatment can be repeated several times with a break of 1-2 months between courses.

To prevent myasthenic crises, in cases of severe neuromuscular conduction disorders, 1-2 ml (15-30 mg) of a 1.5% ipidacrine injection solution is administered parenterally for a short period, then treatment is continued with Ipidacrine-SZ tablets, the dose can be increased to 20-40 mg (1-2 tablets) 5 times/day.

Diseases of the central nervous system: bulbar palsies and paresis; recovery period of organic lesions of the central nervous system (traumatic, vascular and other genesis), accompanied by motor and/or cognitive impairments

The recommended dose is 10-20 mg (0.5-1 tablet) 2-3 times/day.

The course of treatment is from 2 to 6 months. If necessary, the course of treatment is repeated.

Treatment and prevention of intestinal atony

The recommended dose is 20 mg (1 tablet) 2-3 times/day for 1-2 weeks.

If a dose is not taken on time, it should not be taken additionally.

The maximum daily dose is 200 mg.

Use in children and adolescents

The safety and efficacy of the drug Ipidacrine-SZ in children aged 0 to 18 years have not been established. The drug Ipidacrine-SZ is contraindicated for use in children under 18 years of age (see section “Contraindications”).

Adverse Reactions

The drug is well tolerated. Adverse reactions associated with excitation of m-cholinergic receptors are possible.

Classification of adverse reactions by frequency of occurrence: very common (≥1/10); common (≥1/100 but <1/10); uncommon (≥1/1000 but <1/100); rare (≥1/10000 but <1/1000); very rare (<1/10000), frequency unknown (cannot be estimated from available data).

Salivation and bradycardia can be reduced with cholinoblockers (e.g., atropine).

In case of adverse reactions, the dose is reduced or the drug is temporarily discontinued (for 1-2 days).

Reporting of suspected adverse reactions

It is important to report suspected adverse reactions after drug registration to ensure continuous monitoring of the benefit-risk ratio of the drug. Healthcare professionals are recommended to report any suspected adverse drug reactions through the national adverse reaction reporting system of the member states of the Eurasian Economic Union.

Contraindications

• Hypersensitivity to ipidacrine or to any of the excipients included in the drug;
• Epilepsy (because the drug may exacerbate the disease);
• Extrapyramidal diseases with hyperkinesis;
• Angina pectoris;
• Severe bradycardia;
• Bronchial asthma;
• Mechanical obstruction of the intestine or urinary tract;
• Vestibular disorders;
• Peptic ulcer of the stomach or duodenum in the acute phase;
• Pregnancy (the drug increases uterine tone);
• Breastfeeding period;
• Children and adolescents under 18 years of age (insufficient data on efficacy and safety).

With caution

• Peptic ulcer of the stomach and duodenum;
• Thyrotoxicosis;
• Cardiovascular diseases;
• Patients with a history of obstructive respiratory diseases or with acute respiratory diseases. .

Use in Pregnancy and Lactation

Pregnancy

Ipidacrine increases uterine tone and may cause premature birth, therefore the drug Ipidacrine-SZ is contraindicated during pregnancy (see section “Contraindications”).

Breastfeeding

The drug Ipidacrine-SZ is contraindicated during breastfeeding (see section “Contraindications”).

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Special Precautions

The drug Ipidacrine-SZ contains lactose monohydrate (milk sugar). Patients with rare hereditary galactose intolerance, lactase deficiency, or glucose-galactose malabsorption should not take this drug.

Effect on ability to drive vehicles and operate machinery

During treatment, one should refrain from driving a car, as well as engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

In severe overdose, a “cholinergic crisis” may develop.

Symptoms: decreased appetite, bronchospasm, lacrimation, increased sweating, constriction of the pupils, nystagmus, spontaneous defecation and urination, vomiting, bradycardia, heart block, arrhythmias, decreased blood pressure, restlessness, anxiety, agitation, feeling of fear, ataxia, slurred speech, convulsions, coma, drowsiness and general weakness. Symptoms may be mild.

Treatment: symptomatic therapy with the use of m-cholinoblockers: atropine, trihexyphenidyl, metacin, etc.

Drug Interactions

Drugs that depress the central nervous system

The drug Ipidacrine-SZ enhances the sedative effect in combination with drugs that depress the central nervous system.

Other cholinesterase inhibitors and m-cholinomimetics

The action and adverse reactions are enhanced when used concomitantly with other cholinesterase inhibitors and m-cholinomimetic agents. In patients with myasthenia gravis, the risk of developing a cholinergic crisis increases if Ipidacrine-SZ is used simultaneously with other cholinergic agents.

Beta-blockers

The risk of bradycardia increases if beta-blockers were used before starting treatment with ipidacrine.

Nootropic drugs

Ipidacrine-SZ can be used in combination with nootropic drugs. Cerebrolysin improves the mental activity of the drug Ipidacrine-SZ.

Local anesthetics, aminoglycosides, potassium chloride

Ipidacrine weakens the inhibitory effect on neuromuscular transmission and conduction of excitation along peripheral nerves of local anesthetics, aminoglycosides, and potassium chloride.

Alcohol

Alcohol enhances the adverse reactions of the drug. Alcohol should be avoided during treatment with the drug.

Storage Conditions

The drug should be stored out of the reach of children at a temperature below 25°C (77°F).

Shelf Life

Shelf life – 3 years. Do not use 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.