Ipidacrine

Pharmacological properties

ipigrix has a direct stimulating effect on the conduction of an impulse along nerve fibers, interneuronal and neuromuscular synapses of the peripheral nervous system and central nervous system. The pharmacological action of ipigrix is ​​based on a combination of two mechanisms of action:

• blockade of potassium channels of the membrane of neurons and muscle cells;
• reversible inhibition of cholinesterase in synapses.

Ipigrix enhances the effect on smooth muscles not only of acetylcholine, but also of adrenaline, serotonin, histamine and oxytocin.

Ipigrix improves and stimulates the conduction of an impulse in the nervous system and neuromuscular transmission.

Ipigrix enhances contractility of smooth muscle organs under the influence of all antagonists of acetylcholine, adrenaline, serotonin, histamine and oxytocin receptors, with the exception of potassium chloride.

Ipigrix improves memory, inhibits the progradient development of dementia.

The drug restores the impulse in the peripheral nervous system, disrupted due to various factors, such as trauma, inflammation, the action of local anesthetics, some antibiotics, potassium chloride, toxins, etc.

Moderately stimulates the central nervous system with individual manifestations of a sedative effect; It has an analgesic and antiarrhythmic effect.

The drug does not have teratogenic, embryotoxic, mutagenic and carcinogenic, as well as allergenic and immunotoxic effects, and also does not affect the endocrine system.

Pharmacokinetics Ipidacrine is rapidly absorbed after sc or intramuscular administration. C_max in the blood is reached after 25-30 minutes; quickly enters the tissue; T_½ is 40 minutes Approximately 40–55% of the active substance binds to plasma proteins. Metabolized in the liver. Isolation of the drug is carried out by the kidneys, as well as extrarenal (via the digestive tract).

T_½ with parenteral administration of the drug is 2-3 hours. Excretion occurs mainly due to tubular secretion, and only ¹/₃ doses are excreted by glomerular filtration. With parenteral administration, 34.8% of ipidacrine 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 of the central nervous system: bulbar paralysis and paresis; recovery period of organic lesions of the central nervous system, accompanied by motor disorders.

Application

Doses and duration of treatment are determined individually depending on the severity of the disease. solutions of ipidacrine containing 5 and 15 mg / ml, are administered in / m or s / c.

Diseases of the peripheral nervous system. Mono-and polyneuropathies of various origins: SC or IM administered 5-15 mg 1-2 times a day, the course of treatment - 10-15 days (in severe cases - up to 30 days); further treatment is continued with the tablet form of the drug.

Myasthenia gravis and myasthenic syndrome: subcutaneous or intramuscularly administered 5-30 mg 1-3 times a day, followed by the transition to the tablet form. The general course of treatment is 1-2 months. If necessary, therapy can be repeated several times with a break between courses of 1-2 months.

CNS diseases. Bulbar paralysis and paresis: s / c and / m are administered 5-15 mg 1-2 times a day, the course of treatment - 10-15 days, if possible, switch to the tablet form.

The recovery period with organic lesions of the central nervous system. V / m - 10-15 mg 1-2 times a day, the course of treatment - up to 15 days, then, if possible - 1-2 times a day.

Contraindications

Hypersensitivity to ipidacrine or other components of the drug; epilepsy; extrapyramidal disorders with hyperkinesis; angina pectoris, severe bradycardia; ba; vestibular disorders; an ulcer of the stomach or duodenum in the acute stage; mechanical obstruction of the intestines and urinary tract.

Side effects

Ipidacrine is well tolerated, side effects rarely occur (in 6.5% of cases), are mild and, as a rule, are not manifested in all patients.

Disorders of cardiac activity: increased heart rate, decreased heart rate.

From the nervous system: when used in high doses - dizziness, headache, drowsiness, general weakness, cramps.

From the respiratory system: increased secretion of bronchial secretions, bronchospasm.

From the digestive system: increased salivation, nausea; when used in high doses - vomiting, diarrhea, jaundice, pain behind the sternum.

From the skin and subcutaneous tissues: excessive sweating, when used in high doses - skin allergic reactions (itching, rash).

From the reproductive system: increased uterine tone.

In case of development of undesirable side effects, reduce the dose or interrupt the use of the drug for a short time (1-2 days). Salivation and a decrease in heart rate can be reduced with M-anticholinergics (atropine, etc.).

special instructions

The course of asthma, epilepsy, thyrotoxicosis, gastric ulcer and duodenal ulcer may worsen. caution should also be exercised in diseases of the cardiovascular system.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. During the treatment period, it is necessary to refrain from driving vehicles, as well as from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Use during pregnancy or lactation. The drug increases the tone of the uterus and can cause premature birth, therefore, during pregnancy, the use of the drug is contraindicated.

The use of the drug during lactation is contraindicated.

Children. Due to the lack of data on the safety of the drug in children, it is not prescribed to patients of this age category.

Interactions

Ipigrix enhances sedation in combination with drugs that suppress the central nervous system. the effect and side effects are enhanced when combined with other cholinesterase inhibitors and m-cholinomimetic agents. in patients with myasthenia, the risk of developing a “cholinergic” crisis is increased if ipigrix is ​​used simultaneously with cholinergic agents. the risk of developing bradycardia increases if β-adrenergic receptor blockers were used before treatment with the drug.

Ipigrix can be used in combination with nootropic drugs.

Alcohol enhances the side effects of the drug.

Overdose

Symptoms: bronchospasm, increased sweating, narrowing of the pupils, nystagmus, increased peristalsis of the gastrointestinal tract, spontaneous defecation and urination, vomiting, jaundice, bradycardia, cardiac conduction disturbances, arrhythmia, arterial hypotension, anxiety, anxiety, anxiety, anxiety, anxiety, fear , speech impairment, drowsiness, general weakness.

Treatment: apply symptomatic therapy, M-anticholinergics: atropine, cyclodol, metacin, etc.

Storage conditions

At a temperature not exceeding 25 ° c. do not freeze!