Axamon, tablets 20 mg 50 pcs

Pharmacodynamics.

A reversible cholinesterase inhibitor. Due to blockade of potassium channels of cell membranes and inhibition of cholinesterase activity it stimulates neuromuscular transmission and conduction of impulses in the nervous system.

It has M- and H-cholinomimetic action. It increases the effect of acetylcholine, serotonin, histamine and oxytocin on smooth muscles which results in increased smooth muscle contractility of organs including GI and bronchi, decreases heart rate, increases salivary glands secretion, myometrium contractile activity and skeletal muscle tone.

It has a stimulating effect on the CNS in combination with some manifestations of sedation; it helps to improve learning and memory.

Pharmacokinetics.

It is rapidly absorbed from the gastrointestinal tract. The maximum plasma concentration is reached after one hour.

40-55% of the active substance is bound to plasma proteins.

The elimination half-life is about 40 minutes. It is metabolized in the liver.

Extraction is through the kidneys (mainly by tubular secretion and only 1/3 of the drug is excreted by glomerular filtration) and also extrarenal (through the gastrointestinal tract).

Indications

Alzheimer’s disease, Attention and memory disorders, Stroke sequelae, Polyneuropathy

• Diseases of the peripheral nervous system (neuritis, polyneuritis and polyneuropathy, polyradiculopathies, myasthenia and myasthenic syndrome of various etiologies);
• Developmental period of organic lesions of the central nervous system accompanied by motor disorders, including bulbar palsy.Restorative period of organic affections of the central nervous system accompanied with motor disorders, including bulbar paralysis and paresis;
• Comprehensive therapy of demyelinating diseases
• Senile dementia, Alzheimer’s disease, encephalopathies of different genesis.

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Active ingredient

Ipidacrine

Composition

1 tablet contains:

the active ingredient:

ipidacrine hydrochloride monohydrate (Axamon) 20 mg (in terms of ipidacrine hydrochloride);

auxiliary substances:

Ludipress (lactose monohydrate 93%, povidone 3.5%, crosspovidone 3.5%) 65 mg,

sodium carboxymethyl starch 14 mg,

calcium stearate 1 mg.

How to take, the dosage

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

Diseases of peripheral nervous system, myasthenia gravis, myasthenic syndrome: 10-20 mg 1-3 times a day. The course of treatment is from one to two months. If necessary, the course of treatment may be repeated several times with a break between courses of 1-2 months.

Alzheimer’s disease, encephalopathies, convalescent period of organic diseases of central nervous system accompanied by motor disorders, including bulbar paralysis and paresis: daily dose is chosen individually, usually 10-20 mg 2-3 times a day.

In demyelinating lesions of the nervous system, the dose can be increased to 20-40 mg 5-6 times a day. The maximum daily dose is 200 mg.

If one dose is missed, the next dose is taken as usual.

Interaction

Axamon® increases the sedative effect in combination with drugs that depress the central nervous system.

The action and side effects are increased when combined with other cholinesterase inhibitors and m-cholinomimetic agents.

In patients with myasthenia gravis, the risk of cholinergic crisis increases if Axamon® is used concomitantly with other cholinergic agents.

The risk of bradycardia increases if β-adrenoblockers were used prior to treatment with Axamon®.

Limits the inhibitory effect of local anesthetics, aminoglycosides, potassium chloride on neuromuscular transmission and peripheral nerve excitation.

Axamon® may be used in combination with nootropic drugs.

Alcohol increases the side effects of the drug.

Special Instructions

At the time of treatment, one should refrain from driving a vehicle, other vehicles and mechanisms, as well as from potentially hazardous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

Hypersensitivity to any of the components of the drug, epilepsy, extrapyramidal disorders with hyperkinesias, angina pectoris, marked bradycardia, bronchial asthma, mechanical intestinal or urinary tract obstruction, Vestibular disorders, acute gastric or duodenal ulcer, galactose intolerance, lactase deficiency or glucose-galactose malabsorption, pregnancy and lactation, children under 18 years of age.

With caution in: gastric and duodenal ulcer in remission, thyrotoxicosis, intracardiac conduction disorders; obstructive pulmonary disease in history or acute respiratory diseases.

Side effects

Activated by excitation of m-cholinoreceptors: salivation, increased sweating, nausea, diarrhea, jaundice, bradycardia, epigastric pain, increased discharge of bronchial secretion, bronchospasm, seizures, increased uterine tone.

Salivation and bradycardia can be reduced

m-cholinoblockers: atropine, trihexyphenidyl (cyclodol), metocinium iodide (metacin), etc.

Rarely, after using higher doses, dizziness, ataxia, headache, vomiting, general weakness, drowsiness, skin reactions (itching, rash) were observed. In these cases, the dose is reduced or the drug intake is interrupted for a short time (1-2 days).

Overdose

Symptoms: decreased appetite, bronchospasm, lacrimation, increased sweating, constricted pupils, nystagmus, increased gastrointestinal peristalsis, spontaneous defecation and urination, vomiting, jaundice, bradycardia, intracardiac conduction disturbances, arrhythmias, lower blood pressure, anxiety, restlessness, agitation, fear, ataxia, seizures, coma, speech disorders, sleepiness and general weakness.

Treatment:the use of m-cholinoblockers (atropine, cyclodol, methacin, etc.), symptomatic therapy.

Pregnancy use

The use of the drug increases uterine tone and may lead to premature labor, therefore, ipidacrine is contraindicated during pregnancy.

There are no data on the use of the drug during breastfeeding.

Similarities

Neuromidine, Ipigrix