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Active ingredients
Ipidacrine
Release form
Pills
Composition
1 g of gel contains 25 mg of ketoprofen excipients: ethanol 96%, carbomer, diethanol amine, lavender oil, methyl parahydroxy benzoate (E-218), orange oil, propyl parahydroxy benzoate (E-216), purified water.
Pharmacological effect
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 neuronal membrane and muscle cells, reversible inhibition of cholinesterase at 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 (for example, trauma, inflammation, the action of local anesthetics, antibiotics, toxins and potassium chloride); restoration and stimulation of neuromuscular conduction; specific moderate CNS stimulation in combination with individual manifestations of a sedative effect; increased contractility and tone of the smooth muscles of the internal organs; 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, in the equilibrium state in the plasma is only 2% of the drug. 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
Ipigrix is indicated for: CNS diseases: bulbar paralysis andparesis, the recovery period of organic lesions of the CNS, accompanied by motor and / or cognitive impairment. Peripheral nervous system diseases: mono- and polyneuropathy, polyradiculopathy, myasthenia gravis, and myasthenic syndrome of various etiologies. Treatment of intestinal atony.
Contraindications
Do not apply for: Epilepsy. Hypersensitivity to ipidacrine and / or to any of the excipients of the drug. Angina pectoris Extrapyramidal disorders with hyperkinesis. 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.
Precautionary measures
With care: lactase deficiency; lactose intolerance; lactose / isomaltose malabsorption syndrome, as the preparation contains lactose.
Use during pregnancy and lactation
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.
Dosage and administration
For oral administration. Doses and duration of treatment are determined individually depending on the severity of the disease. For diseases of the peripheral nervous system, use 20 mg (1 tablet) 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 pills) 5 times a day. For diseases of the central nervous system, use 20 mg 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 use 20 mg 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.
Side effects
Ipidacrine is usually well tolerated. Side effects are observed in less than 10% of patients and, mainly, associated with stimulation of m-cholinergic receptors. Further, the listed side effects are classified according to the groups of systems and organs, indicating the frequency of occurrence: often (≥1 / 100 to infrequently (≥1 / 1000 to rarely (≥1 / 10 000 to Disruption of the gastrointestinal tract Often: hypersalivation, nausea Infrequently: vomiting Rarely: diarrhea, epigastric pains Unknown: dyspepsia Nervous system disorders Infrequently: dizziness, headaches, drowsiness, muscle spasm, weakness Cardiac function disorders Frequently: palpitations, bradycardia. rhenium Unknown: miosis Disorders of the respiratory system, chest and mediastinum Infrequent: increased bronchial secretion, bronchospasm Disorders of the musculoskeletal system and connective tissue : sweating Infrequently: allergic reactions (itching, rash), usually when using large doses of the drug.
Overdose
Symptoms: in severe overdose may develop a cholinergic crisis (loss of appetite, bronchospasm, lacrimation, sweating, constriction of the pupils, nystagmus, increased gastrointestinal peristalsis,spontaneous defecation and urination, vomiting, jaundice, bradycardia, impaired intracardiac conduction, arrhythmias, hypotension, anxiety, anxiety, agitation, anxiety, ataxia, convulsions, coma, speech disorder, drowsiness, general weakness). Treatment: carry out symptomatic therapy, apply m-cholinolytic substances (including atropine, cyclodol, metacin, etc.).
Interaction with other drugs
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 cholinesterase inhibitors and m, cholinomimetic substances under the influence of ipidacrine are 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. Alcohol increases the unwanted side effects of ipidacrine.
special instructions
Precautions for use There are no systematic data on the use in 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. Ipigrix pills contain lactose, therefore, in patients with rare congenital intolerance to galactose, Lapp's lactase deficiency or glucose – galactose malabsorption, this drug cannot be used. Impact on the ability to drive and work with mechanisms Ipidacrine can have a sedative effect, so patients exposed to this effect, when using ipidacrine, should be careful when driving and working with mechanisms.