Ipigrix solution 15mg / ml, No. 10

• diseases of the peripheral nervous system (neuritis, polyneuritis, polyneuropathy, polyradiculopathy, myasthenia gravis and myasthenic syndrome of various etiologies);

• diseases of the central nervous system (bulbar paralysis and paresis);

• the period of convalescence after organic lesions of the central nervous system, accompanied by movement disorders.

The drug is used intramuscularly or subcutaneously.

Doses and duration of treatment are determined individually, depending on the severity of the disease.

Diseases of the peripheral nervous system

With mono- and polyneuropathy of various origins: s / c and i / m 5-15 mg 1-2 times / day; a course of 10-15 days (in severe cases - up to 30 days); then they switch to taking ipidacrine tablets.

With myasthenia gravis and myasthenic syndrome: s / c and i / m 5-30 mg 1-3 times / day; then they switch to taking ipidacrine tablets. The general 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.

Diseases of the central nervous system

With bulbar paralysis and paresis: s / c and i / m 5-15 mg 1-2 times / day, course 10-15 days; then they switch to taking ipidacrine tablets.

During the rehabilitation period with organic lesions of the central nervous system: i / m 10-15 mg 1-2 times / day, course up to 15 days; then they switch to taking ipidacrine tablets.

The solution for intramuscular and subcutaneous administration is transparent, colorless.

1 ml

ipidacrine hydrochloride

Excipients: 1M hydrochloric acid solution - up to pH 2.8-4.0, d / i water - up to 1 ml.

• epilepsy;

• extrapyramidal disorders with hyperkinesis;

• angina pectoris;

• severe bradycardia;

• bronchial asthma;

• vestibular disorders;

• exacerbation of stomach or duodenal ulcers;

• mechanical obstruction of the intestine or urinary tract;

• pregnancy;

• breastfeeding period;

• children and adolescents up to 18 years of age (there are no systematized data on the safety of use);

• hypersensitivity to ipidacrine and / or any of the excipients of the drug.

The drug should be prescribed with caution in case of gastric ulcer and duodenal ulcer, thyrotoxicosis, diseases of the cardiovascular system, as well as patients with a history of obstructive respiratory diseases or acute respiratory diseases

pharmachologic effect

Ipidacrine is a reversible cholinesterase inhibitor. Directly stimulates the conduction of impulses in the central nervous system and neuromuscular synapses, blocking the potassium channels of the membranes. It enhances the effect on smooth muscles not only of the acetylcholine mediator, but also of 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 smooth muscles of internal organs;

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

• improving memory.

The therapeutic effect is manifested 15-20 minutes after parenteral administration. The duration of action of the drug is 3-5 hours.

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

Pharmacokinetics

Absorption and distribution

After oral administration, ipidacrine is rapidly absorbed from the gastrointestinal tract. Cmax in plasma after s / c or i / m administration is achieved within 25-30 minutes. About 40-55% of the active substance binds to plasma proteins.

The drug penetrates the BBB. Ipidacrine quickly enters the tissues; in an equilibrium state, only 2% of the drug is found in the plasma.

Metabolism and excretion

The drug is metabolized in the liver. The excretion of ipidacrine is carried out by the kidneys and through the intestines, excretion in the urine prevails. T1 / 2 of ipidacrine is 40 minutes. After parenteral administration, 34.8% of the administered dose of ipidacrine is excreted unchanged in the urine. This indicates a rapid metabolism of the drug in the body.

Side effect

Generally, ipidacrine is well tolerated. Side effects are mainly associated with the stimulation of m-cholinergic receptors.

The following side effects of ipidacrine are classified by groups of systems and organs, indicating the frequency of occurrence: often (from? 1/100 to <1/10), infrequently (from? 1/1000 to <1/100), rarely (from? 1 / 10,000 to <1/1000).

From the digestive system: often - hypersalivation, nausea; infrequently - vomiting; rarely - diarrhea, epigastric pain; frequency unknown - dyspepsia.

From the nervous system: infrequently - dizziness, headaches, drowsiness, muscle spasm, weakness.

From the side of the cardiovascular system: often - palpitations, bradycardia.

From the side of the organ of vision: the frequency is unknown - miosis.

From the respiratory system: infrequently - an increase in bronchial secretion, bronchospasm.

From the musculoskeletal system: the frequency is unknown - tremors, convulsions.

On the part of the skin and subcutaneous tissue: often - sweating; infrequently - allergic reactions (itching, rash), usually when using large doses of the drug.

Others: frequency unknown - hypothermia, chest pain, jaundice, increased uterine tone.

If the listed side effects appear, as well as if a side effect not mentioned in the instructions appears, the patient should consult a doctor.

Application during pregnancy and lactation

Ipidacrine increases the tone of the uterus and can cause premature labor, so the drug is contraindicated during pregnancy.

The use of ipidacrine during breastfeeding is contraindicated.

Application for impaired renal function

The use of the drug is contraindicated in case of mechanical obstruction of the urinary tract.

Application in children

The use of the drug in children and adolescents under 18 years of age is contraindicated (there are no systematic data on the safety of use).

special instructions

During treatment, alcohol should be excluded, which enhances the side effects of ipidacrine.

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

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

Due to the possible risk of bradycardia with the use of ipidacrine, cardiac activity should be monitored.

Use in pediatrics

There is no systematic data on the use in children.

Influence on the ability to drive vehicles and mechanisms

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

Overdose

Symptoms: in severe overdose, a cholinergic crisis may develop (decreased appetite, bronchospasm, lacrimation, increased sweating, pupillary constriction, nystagmus, increased gastrointestinal motility, spontaneous defecation and urination, vomiting, jaundice, bradycardia, arterial hypotension, anxiety, conductivity , 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).

Drug interactions

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

The sedative effect of drugs that depress the central nervous system, incl. ethanol, as well as the effect of other cholinesterase inhibitors and m-cholinomimetics under the influence of ipidacrine is enhanced.

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

Beta-blockers increase the severity of bradycardia caused by ipidacrine.

Cerebrolysin potentiates the action of ipidacrine.

Ethanol enhances the unwanted side effects of ipidacrine.

Ipidacrine can be used in combination with nootropic drugs.