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 palsy and paresis.

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

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

Pharmacological effect

Pharmacotherapeutic group:

Anticholinesterase drugs.

ATX CODE: N07AA

Pharmacological properties

Pharmacodynamics

Ipidacrine is a reversible cholinesterase inhibitor. Directly stimulates the conduction of impulses in the central nervous system (CNS) and neuromuscular synapses, blocking membrane potassium channels. It enhances the effect on smooth muscles of not only the 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 certain factors (for example, trauma, inflammation, the action of local anesthetics, antibiotics, toxins and potassium chloride);

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

– specific moderate stimulation of the central nervous system in combination with individual manifestations of sedation;

– memory improvement.

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

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

Pharmacokinetics

Absorption

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

Distribution

The drug penetrates the blood-brain barrier. Ipidacrine quickly enters the tissues; at equilibrium, only 2% of the drug is found in the plasma.

Metabolism and excretion

The drug is metabolized in the liver. Ipidacrine is excreted renal and extrarenally (through the gastrointestinal tract), with urinary excretion predominating. The 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.

Special instructions

Impact on the ability to drive vehicles and operate machinery

Ipidacrine may have a sedative effect, therefore patients exposed to this effect when using the drug should be careful when driving vehicles and operating machinery.

Precautions for use

There are no systematic data on use in children.

During treatment, alcohol should be avoided, which increases the side effects of ipidacrine.

Ipidacrine can aggravate the course of epilepsy, as well as increase the negative effects of alcohol on the body.

In patients with depression, ipidacrine may increase symptoms of depression.

Due to the possible risk of bradycardia when using ipidacrine, cardiac activity should be monitored.

Active ingredient

Ipidacrine

Composition

solution for intramuscular and subcutaneous administration.

1 ml of solution contains:

active substance:

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

excipients:

1 M hydrochloric acid solution to pH 2.8-4.0,

water for injections up to 1 ml.

Contraindications

Do not use when:

Epilepsy.

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

Angina pectoris.

Extrapyramidal disorders with hyperkinesis.

Severe bradycardia.

Bronchial asthma.

Vestibular disorders.

Exacerbation of stomach or duodenal ulcers.

Mechanical obstruction of the intestine or urinary tract.

Pregnancy and breastfeeding period.

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

With caution in: gastric and duodenal ulcers, thyrotoxicosis, diseases of the cardiovascular system, as well as in patients with a history of obstructive diseases of the respiratory system or acute respiratory diseases.

With caution:

lactase deficiency;
lactose intolerance;
lactose/isomaltose malabsorption syndrome, since the drug contains lactose.

Side Effects

Ipidacrine is usually well tolerated. Side effects are mainly associated with stimulation of m-cholinergic receptors.

The following side effects of ipidacrine are classified into groups of systems and organs, indicating the frequency of occurrence: often (≥1/100 to infrequently (≥1/1000 to rarely (≥1/10,000 to

Gastrointestinal disorders

Common: hypersalivation, nausea.

Uncommon: vomiting.

Rarely: diarrhea, epigastric pain.

Unknown: dyspepsia.

Nervous system disorders

Uncommon: dizziness, headaches, drowsiness, muscle spasms, weakness.

Cardiac dysfunction

Common: palpitations, bradycardia.

Visual disorders

Unknown: miosis.

Respiratory, chest and mediastinal disorders

Uncommon: increased bronchial secretion, bronchospasm.

Musculoskeletal and connective tissue disorders

Unknown: tremor, convulsions, increased uterine tone.

Skin and subcutaneous tissue disorders

Common: sweating.

Uncommon: allergic reactions (itching, rashes), usually when using large doses of the drug.

General disorders and reactions at the injection site

Unknown: hypothermia, chest pain, jaundice.

If the listed side effects occur, as well as if a side effect not mentioned in the instructions occurs, you should consult a doctor.

Interaction

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

The sedative effect of drugs that depress the central nervous system, including ethanol, as well as the effect of other cholinesterase inhibitors and m-cholinomimetic substances are enhanced by ipidacrine.

With the simultaneous use of other cholinergic drugs, ipidacrine increases the risk of developing a cholinergic crisis in patients with myasthenia gravis.

Beta-adrenolytic substances increase the severity of bradycardia caused by ipidacrine.

Cerebrolysin potentiates the action of ipidacrine.

Alcohol increases the unwanted side effects of ipidacrine.

Ipidacrine can be used in combination with nootropic drugs.

Overdose

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

Treatment: symptomatic therapy is carried out, m-anticholinergic substances are used (including atropine, cyclodol, metacin).

Storage conditions

Store at a temperature not exceeding 25 oC. Do not freeze!
Keep out of the reach of children!

Shelf life

2 years.
Do not use after the expiration date stated on the package.

Manufacturer

HBM Pharma s.r.o., Slovakia