Ipidacrin - instructions for use, dose, side effects, contraindications

The drug is a cholinesterase inhibitor inhibits the enzymatic hydrolysis of acetylcholine, prolonging its effects. It blocks potassium channels of membranes and promotes their depolarization.

When administered anticholinesterases stimulating action of acetylcholine on M-cholinergic receptors leads to constriction of the pupil, spasm of accommodation, bradycardia, decrease cardiac output, increase the tone of bronchial smooth muscle tone and motility of the gastrointestinal tract, bladder, increased secretion of exocrine glands, to improve tone and contractility of myometrial . Anticholinesterase drugs have virtually no effect on vascular tone. This is due to the fact that in the vessels are mostly non-innervated (extra-synaptic) M₃-cholinoreceptors. Arterial blood pressure is reduced to a much lesser extent than with the introduction of m-cholinomimetics (mainly by reducing the cardiac output).

With the introduction of anticholinesterase drugs from the n-cholinomimetic effects of acetylcholine, its stimulating effect on neuromuscular transmission is most clearly manifested, as a result of which the tone of skeletal muscles increases.

Has a stimulating effect on the central nervous system in combination with individual manifestations of sedation; improves learning and memory.

Pharmacokinetics:

When subcutaneous and intramuscular the introduction is rapidly absorbed. T_max in the blood - 25-30 minutes after administration. The connection with plasma proteins is 40-50%. The drug quickly enters the tissues. Metabolised in the liver. The drug is excreted through the kidneys (mainly by tubular secretion and only 1/3 by glomerular filtration) and extrarenally (through GIT).

Half-life drug for parenteral administration is 2-3 hours. After parenteral administration, 34.8% of the dose is excreted unchanged in the urine.

Indications:

- diseases of the peripheral nervous system: mono- and polyneuropathy, polyradiculopathy, myasthenia gravis and myasthenic syndrome of various etiologies;

- diseases CNS: bulbar paralysis and paresis;

- Alzheimer's disease, senile dementia of the Alzheimer's type;

- recovery period of organic lesions CNS, accompanied by motor impairment;

- demyelinating diseases (as part of complex therapy);

- Functional disorders of the central nervous system (memory loss, ability to concentrate, motivation, initiative, disorientation, emotional lability, etc.) with encephalopathy (traumatic, vascular and other genesis), cerebral blood flow, cerebral trauma, cerebral dysfunction with learning difficulties in children ;

- intestinal atony;

- intoxication with anticholinergics;

- weakness of labor.

ICD-10

V.F00-F09.F00 * Dementia in Alzheimer's disease (G30 .- +)

V.F00-F09.F07 Personality and behavioral disorders due to illness, damage or dysfunction of the brain

VI.G10-G13.G12.2 Disease of the motor neuron

VI.G30-G32.G30 Alzheimer's disease

VI.G50-G59.G58 Other mononeuropathies

VI.G60-G64.G60 Hereditary and idiopathic neuropathy

VI.G60-G64.G61 Inflammatory polyneuropathy

VI.G60-G64.G62 Other polyneuropathies

VI.G60-G64.G62.1 Alcoholic polyneuropathy

VI.G60-G64.G63.2 * Diabetic polyneuropathy (E10-E14 + with common fourth sign .4)

VI.G60-G64.G63.6 * Polyneuropathy with other musculoskeletal lesions (M00-M25 +, M40-M96 +)

VI.G70-G73.G70 Myasthenia gravis and other disorders of the neuromuscular synapse

VI.G70-G73.G70.2 Congenital or acquired myasthenia gravis

VI.G80-G83.G83.9 Paralytic syndrome, unspecified

VI.G90-G99.G96.9 Disorder of central nervous system, unspecified

XIII.M50-M54.M54.1 Radiculopathy

XIII.M70-M79.M79.2 Neuralgia and neuritis, unspecified

XV.O60-O75.O62 Violations of labor [of the clan]

Contraindications:

- epilepsy;

- angina pectoris;

- bronchial asthma;

- pregnancy and lactation;

- extrapyramidal disorders with hyperkinesis;

- severe bradycardia;

- mechanical obstruction of the intestine or urinary tract;

- peptic ulcer of the stomach or duodenum in the stage of exacerbation;

- propensity to vestibular disorders;

- hypersensitivity;

- children under 18 years of age (no systematic data on use in children).

Carefully:

- stomach ulcer;

- diseases of the cardiovascular system;

- thyrotoxicosis;

- obstructive diseases of the respiratory system in the anamnesis or acute diseases of the respiratory tract.

Pregnancy and lactation:

Category FDA - B. The drug is contraindicated in pregnancy (use of the drug increases the tone of the uterus and can cause premature birth) and breastfeeding.

Dosing and Administration:

Inside, intramuscularly, subcutaneously. A single dose of the drug - 10-40 mg. The maximum daily dose is 200 mg per day.

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

Diseases of the peripheral nervous system

Mono- and polyneuropathies of various genesis, polyradiculopathy: subcutaneously or intramuscularly 5-15 mg 1-2 times a day, course 10-15 days (in severe cases - up to 30 days); further treatment continues with the tablet form of the drug.

Myasthenia gravis and myasthenic syndrome: subcutaneously or intramuscularly 15-30 mg 1-3 times a day with a further transition to the tablet form. The general course of treatment is 1-2 months. If necessary, treatment can be repeated several times with a break between courses in 1-2 months.

Diseases CNS

Bulbar paralysis and paresis: subcutaneously or intramuscularly 5-15 mg 1-2 times a day, the course is 10-15 days; further, if possible, switch to a tablet form.

Restorative period of organic lesions CNS, accompanied by motor impairment: intramuscularly 10-15 mg 1-2 times a day, course up to 15 days; further, if possible, switch to a tablet form.

Treatment and prevention of intestinal atony

The initial dose is 10-15 mg 1-2 times a day for 1-2 weeks.

Side effects:

Disorders of the psyche: infrequently - drowsiness.

From the nervous system: infrequently - dizziness, ataxia, headache, convulsions; an unknown frequency is a tremor.

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

From the heart: often - palpitations, bradycardia; unknown frequency - pain behind the sternum.

From the respiratory system, chest and mediastinum: infrequently - increased secretion of bronchial secretions, bronchospasm.

From the side GIT: often - drooling, nausea, anorexia; infrequently - vomiting; rarely - diarrhea, epigastric pain, increased peristalsis,

From the liver and bile ducts: unknown frequency - jaundice.

From the skin and subcutaneous tissues: infrequently - itching, rash.

General disorders and disorders at the site of administration: often - increased sweating; infrequently, general weakness; unknown frequency - hypothermia.

Other: allergic reactions.

Salivation and bradycardia can be reduced by m-holinoblokatorami (including atropine, cyclodol, methacin).

In case of an itch or rash, stop taking the medication. In other cases, reduce the dose or briefly (for 1-2 days) interrupt the reception of the drug.

If any of the side effects listed in the manual are aggravated or the patient has noticed any other side effects not listed in the instructions, you should inform your doctor.

Overdose:

Symptoms: decreased appetite, bronchospasm, lacrimation, increased sweating, narrowing of the pupils, nystagmus, increased peristalsis GIT, spontaneous defecation and urination, vomiting, jaundice, bradycardia, violation of intracardiac conduction, arrhythmias, lowering blood pressure, anxiety, anxiety, arousal, fear, ataxia, convulsions, coma, speech disorders, drowsiness and general weakness.

Treatment: use of m-holinoblokatorov (including atropine, cyclodol, metacin), symptomatic therapy.

Interaction:

Atropine, metocinium iodide - reduce the symptoms of an overdose.

Relieves the depressing effect on neuromuscular transmission and conduction of excitation along the peripheral nerves of local anesthetics, aminoglycosides, potassium chloride.

The drug enhances the action of the oppressive central nervous system.

Effects and side effects are enhanced when combined with other cholinesterase inhibitors and m-cholinomimetic agents.

In patients with myasthenia gravis, the risk of developing a cholinergic crisis increases if the drug is used concomitantly with other cholinergic agents.

The risk of developing a bradycardia increases, if before the start of treatment with the drug, β-blockers were used.

Alcohol increases the side effects of the drug.

Special instructions:

For the duration of treatment should be excluded from drinking alcohol.

Impact on the ability to manage motor transport and other technical devices

During treatment should refrain from driving, other vehicles and mechanisms, as well as from the employment of potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Instructions

Ipidacrin (Ipidacrinum)