Ipidacrin-zdorovya

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT IPIDACRINE-ZDOROVYE (IPIDACRINE-ZDOROVYE)

Composition:

Active substance: ipidacrine;

1 ml (1 ampoule) of the preparation contains ipidacrine hydrochloride 5 mg or 15 mg;

Excipients: concentrated hydrochloric acid, water for injections.

Pharmaceutical form. Solution for injection.

Main physico-chemical properties: clear, colorless solution.

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

Pharmacological properties.

Pharmacodynamics.

Ipidacrine is a reversible cholinesterase inhibitor.

Ipidacrine exerts a direct stimulating effect on impulse conduction along nerve fibers, interneuronal and neuromuscular synapses of the peripheral and central nervous systems (PNS and CNS).

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

• blockade of potassium channels in the membranes of neurons and muscle cells;
• reversible inhibition of cholinesterase in synapses.

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

Ipidacrine demonstrates the following important pharmacological effects:

• restores and stimulates impulse conduction in the nervous system and neuromuscular transmission;
• enhances contractility of smooth-muscle organs under the influence of all antagonists of acetylcholine, adrenergic, serotonergic, histaminergic, and oxytocin receptors, except potassium chloride;
• improves memory and inhibits the progressive development of dementia;
• restores impulse conduction in the PNS impaired due to various factors such as trauma, inflammation, local anesthetics, certain antibiotics, potassium chloride, toxins, etc.;
• moderately stimulates the CNS combined with manifestations of certain sedative effects;
• exhibits analgesic effect;
• exhibits antiarrhythmic effect.

The drug does not exert teratogenic, embryotoxic, mutagenic or carcinogenic, as well as allergenic or immunotoxic effects, and does not affect the endocrine system.

Pharmacokinetics.

Ipidacrine is rapidly absorbed after subcutaneous or intramuscular administration. Maximum blood concentration is reached within 25–30 minutes; 40–50% of the active substance binds to plasma proteins. Ipidacrine rapidly penetrates into tissues; the elimination half-life in the phase is 40 minutes. It is metabolized in the liver. The drug is excreted by the kidneys and also extrarenally (through the gastrointestinal tract). The elimination half-life after parenteral administration is 2–3 hours. Excretion occurs mainly via tubular secretion, with only 1/3 of the dose eliminated by glomerular filtration. After parenteral administration, 34.8% of the drug dose is excreted unchanged in urine.

Clinical characteristics.

Indications.

PNS disorders: mono- and polyneuropathy, polyradiculopathy, myasthenia and myasthenic syndrome of various etiologies.

CNS disorders: bulbar paralysis and paresis; recovery period of organic CNS lesions accompanied by motor disturbances.

Contraindications.

Hypersensitivity to ipidacrine.

Epilepsy.

Extrapyramidal disorders with hyperkinesia.

Angina pectoris.

Marked bradycardia.

Bronchial asthma.

Vestibular disorders.

Mechanical intestinal or urinary tract obstruction.

Active stage of gastric or duodenal ulcer.

Pregnancy.

Breastfeeding period.

Interaction with other medicinal products and other forms of interaction.

Ipidacrine enhances the sedative effect when used in combination with CNS depressants. The action and adverse effects are enhanced when ipidacrine is used concomitantly with other cholinesterase inhibitors and M-cholinomimetic agents. In patients with myasthenia, the risk of developing a "cholinergic" crisis increases if ipidacrine is used simultaneously with cholinergic agents. The risk of bradycardia increases if β-adrenoblockers were administered prior to the initiation of ipidacrine therapy.

Ipidacrine may be used in combination with nootropic agents.

Alcohol enhances the adverse effects of the drug.

Special precautions for use.

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

Use during pregnancy or breastfeeding.

Ipidacrin increases uterine tone and may induce premature labor; therefore, the use of this medicinal product during pregnancy is contraindicated.

The use of the drug is contraindicated during breastfeeding.

Ability to influence reaction speed when driving or operating machinery.

During treatment, patients should refrain from driving vehicles and from engaging in potentially hazardous activities requiring high concentration and fast psychomotor reactions.

Administration and Dosage.

The injection solution should be administered intramuscularly or subcutaneously. The dosage and duration of treatment should be determined individually, depending on the severity of the disease.

Peripheral Nervous System (PNS) Disorders.
Mononeuropathy and polyneuropathy of various etiologies: administer 5–15 mg subcutaneously or intramuscularly 1–2 times daily for 10–15 days (up to 30 days in severe cases); thereafter, treatment should continue with ipidacrine tablets.

Myasthenia and myasthenic syndrome: administer 5–30 mg subcutaneously or intramuscularly 1–3 times daily, followed by transition to tablet form. The total treatment course is 1–2 months. If necessary, treatment may be repeated several times with 1–2 month intervals between courses.

Central Nervous System (CNS) Disorders.
Bulbar palsies and paresis: administer 5–15 mg subcutaneously or intramuscularly 1–2 times daily for 10–15 days; transition to tablet form is recommended when possible.

Recovery Period in Organic CNS Lesions.
Administer 10–15 mg intramuscularly 1–2 times daily for up to 15 days, followed by 1–2 times daily if possible.

Children.

There are no systematic data on the use of the parenteral form of the drug in children (under 18 years of age); therefore, the drug should not be used in pediatric patients.

Overdose.

Symptoms. In severe overdose, a "cholinergic crisis" may develop, characterized by bronchospasm, lacrimation, increased sweating, miosis, nystagmus, enhanced gastrointestinal peristalsis, spontaneous defecation and urination, vomiting, jaundice, bradycardia, impaired cardiac conduction, arrhythmia, hypotension, restlessness, anxiety, excitement, fear, ataxia, seizures, coma, speech disturbances, drowsiness, and general weakness.

Treatment. Symptomatic therapy should be administered; use M-cholinoblockers such as atropine, cyclodol, metacyne, etc.

Side effects.

Ipidacrine, like other medicinal products, may cause adverse reactions, although they do not occur in all patients.

Frequency of adverse reactions according to the MedDRA classification (Medical Dictionary for Regulatory Activities): very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥ 1/1000 to < 1/100); rare (≥ 1/10,000 to < 1/1000); very rare (< 1/10,000); frequency not known (cannot be estimated from the available data).

Cardiac disorders: common – palpitations, bradycardia.

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

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

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

Hepatic disorders: frequency not known – jaundice.

Skin and subcutaneous tissue disorders: common – increased sweating; uncommon – allergic reactions, including rash, pruritus, urticaria, angioneurotic edema.

Reproductive system disorders: increased uterine tone.

Musculoskeletal and connective tissue disorders: uncommon – muscle cramps (with high-dose administration).

Immune system disorders: frequency not known – hypersensitivity reactions (including allergic dermatitis, anaphylactic shock, asthma, toxic epidermal necrolysis, erythema, urticaria, wheezing, laryngeal edema, injection site rash).

General disorders and administration site conditions: uncommon – weakness (with high-dose administration).

Anticholinergic agents such as atropine may reduce salivation and bradycardia.

If undesirable adverse reactions occur, the dose should be reduced or the administration of the medicinal product temporarily interrupted (for 1–2 days).

Reporting of adverse reactions. Reporting adverse reactions after medicinal product registration is important. It enables ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals, pharmacists, patients, and their legal representatives are encouraged to report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 2 years.

Storage conditions.

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

Keep out of reach and sight of children.

Incompatibilities.

The medicinal product should not be mixed with other solutions except those specified in the section "Administration and dosage".

Packaging. 1 ml in a vial, pack of 10 (5x2), pack of 10 (10x1) in blister pack in a carton.

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.