Ipidacrin-healthy

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT IPIDACRINE-ZDOROVYE

Composition:

Active substance: ipidacrine;

1 tablet contains 20 mg of ipidacrine hydrochloride;

Excipients: lactose monohydrate; potato starch; calcium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties: tablets from white to almost white, round-shaped, with a flat surface and bevelled edge.

Pharmacotherapeutic group. Other agents acting on the nervous system. Parasympathomimetics. Anticholinesterase agents. ATC code: N07AA.

Pharmacological Properties

Pharmacodynamics

The drug has a biologically favorable combination of two molecular effects – blockade of membrane potassium permeability and cholinesterase inhibition. In this combination, blockade of membrane potassium permeability plays the decisive role.

Blockade of membrane potassium permeability primarily leads to prolongation of the repolarization phase of the action potential in the excited membrane and enhances the activity of the presynaptic axon. This results in increased calcium ion influx into the presynaptic terminal, which in turn increases neurotransmitter release into the presynaptic cleft in all synapses. Elevated neurotransmitter concentration in the synaptic cleft promotes stronger stimulation of the postsynaptic cell due to enhanced mediator-receptor interaction. In cholinergic synapses, cholinesterase inhibition further increases neurotransmitter accumulation in the synaptic cleft and enhances functional activity of the postsynaptic cell (muscle contraction, impulse conduction).

The drug potentiates the effects of acetylcholine, adrenaline, serotonin, histamine, and oxytocin on smooth muscles.

The drug exhibits the following important pharmacological effects:

• Stimulation and restoration of neuromuscular transmission;
• Restoration of impulse conduction in the peripheral nervous system following its blockade by various agents (trauma, inflammation, local anesthetics, certain antibiotics, potassium chloride, toxins, etc.);
• Enhanced contractility of smooth-muscle organs;
• Moderate, specific stimulation of the central nervous system (CNS) with some manifestations of sedative effect;
• Improved memory and learning ability;
• Analgesic effect.

The drug does not exhibit teratogenic, embryotoxic, mutagenic or carcinogenic effects, nor does it have allergizing or immunotoxic effects, and does not affect the endocrine system.

Pharmacokinetics

After oral administration, the drug is rapidly absorbed from the gastrointestinal tract. Maximum plasma concentration of the active substance is reached within 1 hour after administration. The drug rapidly distributes from blood into tissues; at the steady-state phase, only 2% of the drug remains in blood serum. The elimination half-life during the distribution phase is 40 minutes. 40–50% of the active substance is bound to plasma proteins. The drug is predominantly absorbed from the duodenum, to a lesser extent from the small and ileal intestine, and only 3% of the dose is absorbed from the stomach. Drug elimination from the body occurs through a combination of renal and extrarenal mechanisms (biotransformation, biliary secretion), with urinary excretion being predominant. Only 3.7% of the drug is excreted unchanged in urine, indicating rapid metabolism of the drug in the body.

Clinical characteristics.

Indications.

Diseases of the peripheral nervous system (neuropathies, neuritis, polyneuritis and polyneuropathies, myelopolyradiculoneuritis), myasthenia and myasthenic syndrome of various etiologies.

Bulbar palsies and paresis.

Memory disorders of various etiologies (Alzheimer's disease and other forms of senile dementia); in delayed mental development in children.

Recovery period following organic lesions of the central nervous system associated with motor disturbances.

In complex therapy of multiple sclerosis and other forms of demyelinating diseases of the nervous system.

Intestinal atony.

Contraindications.

Hypersensitivity to ipidacrine and other components of the drug.

Epilepsy.

Extrapyramidal disorders with hyperkinesia.

Angina pectoris.

Severe bradycardia.

Bronchial asthma.

Vestibular disorders.

Mechanical obstruction of the intestine or urinary tract.

Acute phase of gastric or duodenal ulcer.

Interaction with other medicinal products and other types of interactions.

The drug enhances the sedative effect when used in combination with medicinal products that suppress the central nervous system. The action and adverse effects are enhanced when used concomitantly with other cholinesterase inhibitors and m-cholinomimetic agents.

In patients with myasthenia, the risk of developing a "cholinergic" crisis increases if the drug is used simultaneously with cholinergic agents. The risk of bradycardia increases if β-adrenergic blockers are used prior to treatment with this drug.

The drug may be used in combination with nootropic agents.

Alcohol enhances the adverse effects of the drug.

Cerebrolysin enhances the psychotropic effect of the drug.

Special precautions for use.

Use with caution in patients with a history of gastric or duodenal peptic ulcer, respiratory tract diseases including acute respiratory infections, cardiovascular disorders not related to coronary pain, and in patients with thyrotoxicosis.

The drug contains lactose; therefore, if the patient has known intolerance to certain sugars, medical advice should be sought before taking this medication.

Use during pregnancy or breastfeeding.

The drug increases uterine tone and may cause premature labor; therefore, its use during pregnancy is contraindicated.

The use of the drug is contraindicated during breastfeeding.

Ability to influence reaction rate when driving or operating machinery.

The drug may produce sedative effects; therefore, caution should be exercised when driving or operating machinery.

Administration and Dosage.

Tablets are intended for oral use.

For neuritis – 1 tablet 2–3 times daily. Treatment duration: 10–15 days for acute neuritis, up to 20–30 days for chronic neuritis. If necessary, repeat the course 2–3 times with 2–4 week intervals until maximum effect is achieved.

For myelopolyradiculoneuritis and paresis – 1 tablet 2–3 times daily for 30–40 days. Treatment courses may be repeated multiple times with 1–2 month breaks. Repeat courses until therapeutic effect is achieved.

For myasthenia and myasthenic syndromes – 1–2 tablets 2–3 times daily. In severe cases, the dose may be increased up to 200 mg daily (2 tablets 5 times daily every 2–3 hours). Treatment is administered in courses, alternating with conventional anticholinesterase agents.

For multiple sclerosis and other forms of demyelinating disorders of the nervous system, bulbar paralysis – 1 tablet 3–5 times daily for 60 days, 2–3 times per year.

For Alzheimer's disease and other forms of senile cognitive impairment – begin with a dose of 1–2 tablets daily, divided into 2 doses, gradually increasing the dose by 2 tablets weekly up to 6–10 tablets daily (2 tablets 3–5 times daily). Treatment duration: from 4 months up to 1 year. Course therapy is possible – 4–5 months of treatment followed by a 1–2 month break.

For organic CNS disorders associated with motor disturbances – 1 tablet 2–3 times daily. Average treatment duration: 30 days. The course may be repeated if necessary.

For intestinal atony – 1 to 3 tablets daily, divided into 3 doses. Treatment duration: 1–3 weeks.

Children aged 12 years and older with delayed mental development and peripheral nervous system disorders – administer 1 tablet (20 mg) 2–3 times daily. Treatment duration: 1–2 months, depending on the clinical presentation.

Children.

The drug may be used in children aged 12 years and older.

Overdose.

In cases of severe intoxication, cholinergic crisis may develop.

Symptoms: bronchospasm, lacrimation, increased sweating, miosis, nystagmus, increased gastrointestinal peristalsis, spontaneous defecation and urination, vomiting, jaundice, bradycardia, cardiac conduction disturbances, arrhythmias, decreased arterial pressure, restlessness, anxiety, excitement, fear sensation, ataxia, seizures, coma, speech disturbances, drowsiness, general weakness.

Treatment: symptomatic therapy. Use of M-cholinoblocking agents (atropine, cyclodol, metacyne).

Adverse reactions.

Classification of adverse reaction frequencies: very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥ 1/1000 to < 1/100); rare (≥ 1/10000 to < 1/1000); very rare (< 1/10000), including isolated cases; unknown (cannot be estimated from available data).

The drug is generally well tolerated. Possible adverse effects related to stimulation of M-cholinoreceptors may occur.

Cardiac disorders: common – palpitations, bradycardia, chest pain.

Nervous system disorders: uncommon (with high-dose administration) – dizziness, headache, drowsiness, general weakness, muscle cramps.

Respiratory, thoracic and mediastinal disorders: uncommon – increased bronchial secretion, bronchospasm.

Gastrointestinal disorders: common – salivation, nausea; uncommon (with high-dose administration) – vomiting; rare – diarrhea, epigastric pain.

Hepatobiliary disorders: jaundice (frequency unknown).

Skin and subcutaneous tissue disorders: common – increased sweating; uncommon (after high-dose administration) – allergic reactions, including urticaria, angioneurotic edema, pruritus, rash.

Reproductive system disorders: increased uterine tone.

Salivation and bradycardia may be reduced by cholinoblockers (e.g., atropine, etc.). If adverse effects occur, the dose should be reduced or a short break in treatment (1–2 days) should be taken.

Reporting of adverse reactions. Reporting of suspected adverse reactions after drug registration is important. It enables ongoing monitoring of the benefit-risk balance of the drug. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of drug efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 2 years.

Storage conditions. Store in original packaging at a temperature not exceeding 25 °C.

Keep out of reach and sight of children.

Packaging. Tablets, 10×5 in blisters, in a cardboard box.

Prescription status. Prescription only.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROV'YA".

Manufacturer's address and place of business. 22, Shevchenka Street, Kharkiv, Kharkiv Oblast, 61013, Ukraine.