IPIGRIX PILLS 20MG

Release form

Tablets 50 pcs

Pharmacology

Pharmacotherapeutic group: Anticholinesterase agents.

Pharmacological properties

Pharmacodynamics

Ipidacrine is a reversible inhibitor of cholinesterase. It directly stimulates the conduction of impulses along the nerve fibers, interneuronal 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:

• blockade of the potassium channels of the membrane of neurons and muscle cells,
• reversible cholinesterase inhibition 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 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 the internal organs;
• specific moderate CNS stimulation in combination with individual manifestations of a sedative effect;
• memory improvement.

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

Sufficient data from clinical studies of the safety of ipidacrine in children are not available.

Pharmacokinetics

Absorption

After oral administration, ipidacrine is rapidly absorbed from the gastrointestinal tract. The maximum concentration in a blood plasma is reached in one hour. About 40-55% of the active substance is bound to plasma proteins.

Distribution

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

Metabolism and excretion

The drug is metabolized in the liver. Ipidacrine is excreted renally (via the kidneys) and extrarenally (through the gastrointestinal tract), excretion in the urine prevails (mainly by canalicular secretion, only дозы the dose is eliminated by glomerular filtration). The half-life of ipidacrine is 40 minutes.

Indications

• Peripheral nervous system diseases: mono- and polyneuropathy, polyradiculopathy, myasthenia gravis, and myasthenic syndrome of various etiologies.
• Diseases of the central nervous system: bulbar paralysis iparesis, recovery period of organic lesions of the central nervous system, accompanied by motor and / or cognitive impairment.
• Treatment of intestinal atony.

Contraindications

• Hypersensitivity to ipidacrine and / or to any of the excipients of the drug.
• Epilepsy.
• Extrapyramidal disorders with hyperkinesis.
• Angina pectoris
• Severe bradycardia.
• Bronchial asthma.
• Vestibular disorders.
• Exacerbation of gastric or duodenal ulcers.
• Mechanical obstruction of the intestine or urinary tract.
• Pregnancy and breastfeeding period.
• Children under the age of 18 years (there is no systematic data on the safety of use).

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

To be used with caution in lactase deficiency, lactose intolerance, lactose / isomaltose malabsorption syndrome, as the preparation contains lactose.

Pregnanacy and breastfeeding

Ipidacrine enhances the tone of the uterus and can cause premature labor, therefore it is contraindicated during pregnancy. The use of ipidacrine during breastfeeding is contraindicated.

Special notes

Influence on ability to drive vehicles and work with mechanisms

Ipidacrine may have a sedative effect, so patients affected by this effectWhen applying ipidacrine, caution should be exercised when driving and working with machinery.

Precautions when applying

There are no systematic data on the use of children.

At the time of treatment should be excluded alcohol, which increases the side effects of ipidacrine.

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

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

In connection with the possible risk of bradycardia when using ipidacrine, cardiac activity should be monitored.

Tablets Ipigrix ®contain lactose, therefore, in patients with rare congenital intolerance to galactose, Lapp's lactase deficiency or glucose-malabsorption of galactose, this drug cannot be used.

Active ingredient

One pill contains:

active ingredient: ipidacrine hydrochloride monohydrate - 21.6 mg (in terms of ipidacrine hydrochloride - 20.0 mg);

excipients: lactose monohydrate - 65.0 mg; potato starch - 12.6 mg; potato starch, dried - 1.4 mg; Calcium stearate - 1.0 mg.

Description

Round flat-cylindrical pills of white or almost white color with a facet.

Dosage and administration

Tablets are used inside. Doses and duration of treatment are determined individually depending on the severity of the disease.

In diseases of the peripheral nervous system, 20 mg (1 tablet) is administered 1–3 times a day.Duration of treatment is 1–2 months. If necessary, the course of treatment can be repeated several times with a break between courses of 1-2 months.

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

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

In the treatment of intestinal atony, 20 mg is administered 2–3 times a day for 1–2 weeks.

Elderly patients and patients with impaired liver and / or kidney activity do not require dose selection.

The maximum daily dose is 200 mg.

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

Adverse effects

Ipidacrine is usually well tolerated. Side effects are observed in less than 10% of patients and, mainly, are associated with stimulation of m-cholinergic receptors.

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

Disorders of the gastrointestinal tract

Often: hypersalivation, nausea.

Infrequently: vomiting.

Rarely: diarrhea, epigastric pain.

Unknown: dyspepsia.

Nervous system disorders

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

Impaired cardiac function

Often: palpitations, bradycardia.

Violations of the organs of sight

Unknown: miosis.

Disorders of the respiratory system, chest and mediastinum

Infrequently: increase in bronchial secretion, bronchospasm.

Disorders of the musculoskeletal system and connective tissue

Unknown: tremor, convulsions, increasing the tone of the uterus.

Violations of the skin and subcutaneous tissues

Often: sweating.

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

Drug interaction

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

The sedative effect of drugs that inhibit the central nervous system, including ethanol, as well as the effect of other inhibitors of cholinesterase and m? Cholinomimetic substances under the influence of ipidacrine is enhanced.

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

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

Cerebrolysin potentiates the effect of ipidacrine.

Symptoms in severe overdosage may develop cholinergic crisis (decreased appetite, bronchospasm, lacrimation, sweating, pupillary constriction, nystagmus, hyperperistalsis gastrointestinal tract, spontaneous defecation and urination, vomiting, jaundice, bradycardia, impaired intracardiac conduction, arrhythmia, hypotension, anxiety, anxiety, agitation, fear, ataxia, convulsions, coma, speech disorder, drowsiness, general weakness).

Treatment: carry out symptomatic therapy, apply m-cholinolytic substances (including atropine, cyclodol, metacin, etc.).

Store at a temperature not higher than 25 aboutWITH.