Ipigrix, tablets 20 mg 50 pcs

Pharmacotherapeutic group:

Anticholinesterase agents.

The ATC code: N07AA.

Pharmacological properties

Pharmacodynamics

Ipidacrine is a reversible cholinesterase inhibitor. It directly stimulates impulse conduction along nerve fibers, inter-neuronal and neuromuscular synapses of the peripheral and central nervous system (CNS). The pharmacological action of ipidacrine is based on a combination of two mechanisms of action:

• potassium channel blockade of neuronal and muscle cell membranes,
• reversible inhibition of cholinesterase in synapses.

Ipidacrine enhances the effect on smooth muscles not only of acetylcholine, but also of adrenaline, serotonin, histamine and oxytocin. It has the following pharmacological effects:

• restoration of impulse conduction in the peripheral nervous system after blockade caused by certain factors (e.g., trauma, inflammation, effects of local anesthetics, antibiotics, toxins and potassium chloride);
• recovery and stimulation of neuromuscular conduction;
• specific moderate stimulation of the CNS in combination with certain manifestations of sedation;
• enhancing the contractility and tone of the smooth muscles of the internal organs;
• improving 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 is reached after one hour. About 40-55% of the active substance is bound to plasma proteins.

Distribution

The drug penetrates the blood-brain barrier. Imidacrine enters the tissues quickly, only 2% of the drug is in the plasma in equilibrium state. The half-life is 40 minutes.

Metabolism and excretion

The drug is metabolized in the liver. Excretion of ipidacrine is renal (through the kidneys) and extrarenal (through the gastrointestinal tract), excretion with the urine predominates (mainly by tubular secretion, only ? of the dose is excreted by glomerular filtration). The half-life of ipidacrine is 40 minutes.

Indications

Ipigrix is indicated in:

CNS diseases: bulbar paralysis and paresis, recovery period of organic CNS lesions accompanied by motor and/or cognitive impairment.

Peripheral nervous system diseases: mono- and polyneuropathy, polyradiculopathy, myasthenia gravis and myasthenic syndrome of different etiologies.

The treatment of bowel atony.

Active ingredient

Composition

Pills.

One tablet contains:

the active ingredient:

ipidacrine hydrochloride monohydrate – 21.6 mg (in terms of ipidacrine hydrochloride – 20.0 mg);

auxiliary substances:

Lactose monohydrate – 65.0 mg;

Potato starch – 12.6 mg;

Dried potato starch – 1.4 mg;

calcium stearate – 1.0 mg.

How to take, the dosage

For oral administration. Doses and duration of treatment are determined individually depending on the severity of the disease.

In diseases of the peripheral nervous system it is used 20 mg (1 tablet) 1? 3 times a day. The duration of the course of treatment is 1? 2 months. If necessary the course of treatment may be repeated several times with a break between courses of 1-2 months.

To prevent myasthenic crises, in severe disorders of neuromuscular conduction, 1-2 ml (15-30 mg) of solution for intramuscular and subcutaneous administration, containing 15 mg of ipidacrine in 1 ml, are given briefly parenterally, then treatment is continued with ipidacrine tablets in a dose of 20-40 mg (1-2 tablets) 5 times a day.

In diseases of the central nervous system, 20 mg 2-3 times a day is used. The course of treatment is from 2 to 6 months. If necessary the course of treatment is repeated.

In the treatment of bowel atony 20 mg 2 to 3 times a day for 1-2 weeks.

Elderly patients and patients with liver and/or kidney dysfunction do not require dose adjustment.

The maximum daily dose is 200 mg.

If you miss another dose of the drug, take it immediately. Do not use a double dose to replace the dose you missed. Continue taking it as recommended by your doctor.

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 are 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.

Special Instructions

Precautions 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.

The tablets of IPIGRIX® contain lactose, therefore patients with rare congenital galactose intolerance, Lapp lactase deficiency, or glucose malabsorption should not use this medicine.

Influence on driving and operating machinery

Ipidacrine may have a sedative effect, so patients with this effect should exercise caution when using ipidacrine when driving and operating machinery.

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 occur in less than 10% of patients and are mainly related to stimulation of m-cholinoreceptors.

The side effects listed below are classified according to system and organ groups by frequency of occurrence: frequently (≥1/100 to infrequently (≥1/1000 to rarely (≥1/10,000 to

Gastrointestinal disorders

Often: hypersalivation, nausea.

Infrequent: vomiting.

Rarely: diarrhea, epigastric pain.

Unknown: dyspepsia.

Nervous system disorders

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

Disorders of 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.

Overdose

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

Treatment: symptomatic therapy is carried out, m-cholinolytic agents (including atropine, cyclodol, methacin, etc.) are used.

Similarities