Instructions Ipidacrin-Health solution for injection 15 mg/ml ampoules 1 ml No. 10
Composition
active ingredient: ipidacrine;
1 ml (1 ampoule) of the drug contains ipidacrine hydrochloride 5 mg or 15 mg;
Excipients: concentrated hydrochloric acid, water for injection.
Dosage form
Solution for injection.
Main physicochemical properties: transparent colorless solution.
Pharmacotherapeutic group
Other agents acting on the nervous system. Parasympathomimetics. Anticholinesterase agents. ATX code N07A A.
Pharmacological properties
Pharmacodynamics.
Ipidacrine is a reversible cholinesterase inhibitor.
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 (PNS and CNS).
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 of not only acetylcholine, but also adrenaline, serotonin, histamine, and oxytocin.
Ipidacrine exhibits the following important pharmacological effects:
- restores and stimulates impulse conduction in the nervous system and neuromuscular transmission;
- enhances the contractility of smooth muscle organs under the influence of all antagonists of acetylcholine, adrenaline, serotonin, histamine and oxytocin receptors, with the exception of potassium chloride;
- improves memory, slows down the progressive development of dementia;
- restores impulse conduction in the PNS, disrupted due to the influence of various factors, such as trauma, inflammation, the action of local anesthetics, some antibiotics, potassium chloride, toxins, etc.;
- moderately stimulates the CNS in combination with manifestations of individual sedative effects;
- exhibits an analgesic effect;
- exhibits antiarrhythmic effect.
The drug does not have teratogenic, embryotoxic, mutagenic and carcinogenic, as well as allergenic and immunotoxic effects, and does not affect the endocrine system.
Pharmacokinetics.
Ipidacrine is rapidly absorbed after subcutaneous or intramuscular administration. The maximum concentration in the blood is reached after 25-30 minutes, 40-50% of the active substance binds to blood plasma proteins. Ipidacrine quickly enters the tissues; the half-life in the phase is 40 minutes. It is metabolized in the liver. The drug is excreted by the kidneys, as well as extrarenal (through the gastrointestinal tract). The half-life with parenteral administration of the drug is 2-3 hours. Excretion occurs mainly due to tubular secretion, and only 1/3 of the dose is excreted by glomerular filtration. With parenteral administration, 34.8% of the dose of the drug is excreted in the urine unchanged.
Indication
PNS diseases: mono- and polyneuropathy, polyradiculopathy, myasthenia and myasthenic syndrome of various etiologies.
CNS diseases: bulbar palsies and paresis; recovery period of organic CNS lesions accompanied by motor disorders.
Contraindication
Hypersensitivity to ipidacrine.
Epilepsy.
Extrapyramidal disorders with hyperkinesis.
Angina pectoris.
Marked bradycardia.
Bronchial asthma.
Vestibular disorders.
Mechanical obstruction of the intestines and urinary tract.
Gastric or duodenal ulcer in the acute stage.
Pregnancy.
Breastfeeding period.
Interaction with other medicinal products and other types of interactions
Ipidacrine enhances the sedative effect in combination with drugs that depress the central nervous system. The effect and side effects are enhanced when used together with other cholinesterase inhibitors and m-cholinomimetics. In patients with myasthenia gravis, the risk of developing a "cholinergic" crisis increases if ipidacrine is used simultaneously with cholinergic drugs. The risk of developing bradycardia increases if β-blockers were used before starting treatment with ipidacrine.
Ipidacrine can be used in combination with nootropic drugs.
Alcohol increases the side effects of the drug.
Application features
Use with caution in patients with a history of peptic ulcer of the stomach and duodenum, respiratory diseases, including acute respiratory diseases, cardiovascular diseases not associated with coronary pain, and thyrotoxicosis.
Use during pregnancy or breastfeeding
Ipidacrine increases uterine tone and can cause premature birth, so the use of the drug is contraindicated during pregnancy.
The use of the drug is contraindicated during breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
During the treatment period, it is necessary to refrain from driving a car, as well as from potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
Method of administration and doses
The solution for injection is administered intramuscularly or subcutaneously. The dose and duration of treatment should be determined individually depending on the severity of the disease.
PNS diseases. Mono- and polyneuropathy of various genesis: subcutaneously or intramuscularly administer 5–15 mg 1–2 times a day, the course of treatment is 10–15 days (in severe cases – up to 30 days); then treatment should be continued with the tablet form of ipidacrine.
Myasthenia and myasthenic syndrome: subcutaneously or intramuscularly inject 5–30 mg 1-3 times a day, followed by switching to tablet form. The total course of treatment is 1–2 months. If necessary, the treatment can be repeated several times with a break between courses of 1–2 months.
CNS diseases. Bulbar palsies and paresis: subcutaneously and intramuscularly 5–15 mg 1–2 times a day, course of treatment – 10–15 days, if possible, switch to tablet form.
Recovery period in organic CNS lesions. Intramuscularly 10–15 mg 1–2 times a day, course of treatment – up to 15 days, then if possible – 1–2 times a day.
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 children.
Overdose
Symptoms: In severe overdose, a "cholinergic crisis" may develop, which is characterized by: bronchospasm, lacrimation, increased sweating, constriction of the pupils, nystagmus, increased gastrointestinal peristalsis, spontaneous defecation and urination, vomiting, jaundice, bradycardia, intracardiac conduction disorders, arrhythmia, decreased blood pressure, anxiety, agitation, fear, ataxia, convulsions, coma, speech disorders, drowsiness, general weakness.
Treatment: Symptomatic therapy should be used, m-cholinoblockers should be used: atropine, cyclodol, metacin, etc.
Adverse reactions
Like all medicines, Ipidacrine can cause side effects, although not everybody gets them.
Frequency of adverse reactions according to MedDRA classification (Medical Dictionary of Regulatory Activities): very common (≥ 1/10); common (≥ 1/100 to
Cardiac: often - palpitations, bradycardia.
From the nervous system: infrequently - dizziness, headache, drowsiness (when taking high doses).
Respiratory, thoracic and mediastinal disorders: infrequently - increased bronchial secretion, bronchospasm.
From the gastrointestinal tract: often - increased salivation, nausea; infrequently - when using high doses - vomiting; rarely - diarrhea, epigastric pain.
Hepatic: frequency unknown – jaundice.
Skin and subcutaneous tissue disorders: often - increased sweating; infrequently - allergic reactions, including rash, itching, urticaria, angioedema.
From the reproductive system: increased uterine tone.
Musculoskeletal and connective tissue disorders: infrequently - muscle cramps (when using high doses).
Immune system disorders: frequency unknown - 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 (when using high doses).
Anticholinergic agents such as atropine may reduce salivation and bradycardia.
In case of development of undesirable side reactions, the dose should be reduced or the use of the drug should be interrupted for a short time (for 1–2 days).
Reporting of adverse reactions. Reporting of adverse reactions after registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of a medicinal product via the Automated Pharmacovigilance Information System at the link: https://aisf.dec.gov.ua.
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Incompatibility
The medicinal product should not be mixed with other solutions, except those specified in the "Method of administration and dosage" section.
Packaging
1 ml in ampoule No. 10 (5x2), No. 10 (10x1) in a blister in a box.
Vacation category
According to the recipe.
Producer
Limited Liability Company "Pharmaceutical Company "Zdorovya".
Location of the manufacturer and address of its place of business
Ukraine, 61013, Kharkiv region, Kharkiv city, Shevchenko street, building 22.
