Epigrix, 15 mg/ml 1 ml 10 pcs

Pharmacotherapeutic group:

Anticholinesterase agents.

The ATX CODE: N07AA

Pharmacological properties

Pharmacodynamics

Ipidacrine is a reversible cholinesterase inhibitor. It directly stimulates impulse conduction in the central nervous system (CNS) and neuromuscular synapses by blocking membrane potassium channels. It enhances the effect on smooth muscle not only mediator acetylcholine but also adrenaline, serotonin, histamine and oxytocin.

The main pharmacological effects of ipidacrine:

– restoration and stimulation of neuromuscular conduction;

– restoration of impulse conduction in the peripheral nervous system after blockade caused by some factors (such as trauma, inflammation, effects of local anesthetics, antibiotics, toxins and potassium chloride);

– enhancement of contractility and tone of the smooth muscles of internal organs;

– specific moderate stimulation of the CNS in combination with certain manifestations of sedation;

– improvement of memory.

In preclinical studies ipidacrine had no teratogenic, embryotoxic, mutagenic, carcinogenic and immunotoxic effects, and did not affect the endocrine system.

There are no sufficient data from clinical studies of the safety of ipidacrine in children.

Pharmacokinetics

Absorption

After oral administration, ipidacrine is rapidly absorbed from the gastrointestinal tract. Maximum plasma concentration after subcutaneous or intramuscular administration is reached within 25-30 minutes. About 40-55% of the active substance is bound to plasma proteins. Therapeutic effect appears 15-20 minutes after parenteral administration. The duration of action of the drug is 3-5 hours.

Distribution

The drug penetrates through the blood-brain barrier. Imidacrine enters the tissues rapidly; only 2% of the drug is found in plasma in equilibrium.

Metabolism and excretion

The drug is metabolized in the liver. Excretion of ipidacrine is renal and extrarenal (through the gastrointestinal tract), urinary excretion predominates. The elimination half-life of ipidacrine is 40 minutes. After parenteral administration, 34.8% of the administered dose of ipidacrine is excreted unchanged in the urine. This indicates rapid metabolism of the drug in the body.

Indications

– Diseases of the central nervous system: bulbar paralysis and paresis.

– Diseases of the peripheral nervous system (neuritis, polyneuritis, polyneuropathy, polyradiculopathy, myasthenia gravis and myasthenic syndrome of various etiologies).

– The period of recuperation after organic lesions of the central nervous system, accompanied by movement disorders.

Active ingredient

Composition

solution for intramuscular and subcutaneous administration.

1 ml of the solution contains:

the active ingredient:

ipidacrine hydrochloride monohydrate – 5.4 mg or 16.2 mg (in terms of ipidacrine hydrochloride – 5.0 mg or 15.0 mg);

auxiliary substances:

1 M hydrochloric acid solution to pH 2.8-4.0,

water for injection to 1 ml.

How to take, the dosage

Intramuscularly or subcutaneously.

The doses and duration of treatment are determined individually depending on the severity of the disease.

Diseases of peripheral nervous system

Mono- and polyneuropathies of various genesis: subcutaneously and intramuscularly 5-15 mg 1-2 times daily, 10-15 days course (in severe cases – up to 30 days); then the use of ipidacrine tablets is changed.

Miasthenia and myasthenic syndrome: subcutaneously and intramuscularly 5-30 mg 1?3 times a day; then switch to taking ipidacrine in tablets. The total course of treatment is 1? 2 months. If necessary, treatment can be repeated several times with a break between courses of 1-2 months.

Diseases of the central nervous system

Bulbar paralysis and paresis: subcutaneously and intramuscularly 5-15 mg 1-2 times a day, course 10-15 days; then switch to taking ipidacrine in tablets.

Rehabilitation for organic lesions of the CNS: intramuscularly 10-15 mg 1? 2 times a day, the course of up to 15 days; then the use of ipidacrine in tablets is changed.

Interaction

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

The sedative effect of CNS-depressant drugs, including ethanol, as well as the effect of other cholinesterase inhibitors and m-cholinomimetic substances is increased under the influence of ipidacrine.

In concomitant use of other cholinergic drugs, ipidacrine increases the risk of cholinergic crisis in myasthenic patients.

The beta-adrenolytic agents increase the severity of bradycardia caused by ipidacrine.

Cerebrolysin potentiates the effect of ipidacrine.

Alcohol increases the unwanted side effects of ipidacrine.

Ipidacrine can be used in combination with nootropic drugs.

Special Instructions

Influence on driving and operating machinery

Ipidacrine may have a sedative effect, so patients who are exposed to this effect when using the drug should exercise caution when driving and operating machinery./p>

Precautionary measures for use

There are no systematic data on use in children.

Alcohol, which increases the side effects of ipidacrine, should be avoided during treatment.

Ipidacrine may worsen the course of epilepsy, and also increase the negative effects of alcohol on the body.

In depressed patients, ipidacrine may worsen the symptoms of depression.

Because of the possible risk of bradycardia when using ipidacrine, heart activity should be monitored.

Contraindications

Do not use in:

Epilepsy.

Hypersensitivity to ipidacrine and/or any of the excipients of the drug.

Angina pectoris.

Extrapyramidal disorders with hyperkinesias.

Severe bradycardia.

Bronchial asthma.

Vestibular disorders.

Aggravation of gastric or duodenal ulcer.

Mechanical obstruction of the intestine or urinary tract.

Pregnancy and the period of breastfeeding.

Children under 18 years of age (no systematic safety data on use).

With caution in: gastric and duodenal ulcer, thyrotoxicosis, cardiovascular disease, and patients with a history of obstructive respiratory disease or acute respiratory conditions.

With caution:

Side effects

Ipidacrine is usually well tolerated. Side effects are mainly related to stimulation of m-cholinoreceptors.

The following side effects of ipidacrine are classified by system and organ group with the frequency of occurrence: Frequent (≥1/100 to infrequent (≥1/1000 to rare (≥1/10,000 to

Gastrointestinal disorders

Frequent: hypersalivation, nausea.

Infrequent: vomiting.

Rarely: diarrhea, epigastric pain.

Unknown: dyspepsia.

Nervous system disorders

Infrequent: dizziness, headaches, drowsiness, muscle spasm, weakness.

Disorders with cardiac function

Often: palpitations, bradycardia.

Visual disorders

Unknown: miosis.

Respiratory system, chest and mediastinum disorders

Infrequent: increased bronchial secretion, bronchospasm.

Skeletal and muscular system and connective tissue disorders

Unknown: tremors, cramps, increased uterine tone.

Skin and subcutaneous tissue disorders

Often: sweating.

Infrequent: allergic reactions (itching, rashes), usually with high doses of the drug.

General disorders and reactions at the site of administration

Unknown: hypothermia, chest pain, jaundice.

If any of the listed side effects occur, or if a side effect not mentioned in the instructions occurs, a physician should be consulted.

Overdose

Symptoms: In severe overdose, cholinergic crisis may develop (decreased appetite, bronchospasm, lacrimation, increased sweating, constriction of pupils, nystagmus, increased peristalsis of the gastrointestinal tract, spontaneous defecation and urination, vomiting, jaundice, bradycardia, intracardiac conduction disorders, arrhythmias, arterial hypotension, restlessness, anxiety, agitation, fear, ataxia, seizures, coma, speech disorders, drowsiness, general weakness).

Treatment: symptomatic therapy, use m-cholinolytic agents (including atropine, cyclodol, methacin).

Similarities