Instructions for Mediathorn tablets 20mg No. 50
Composition
active ingredient: ipidacrine;
1 tablet contains ipidacrine hydrochloride monohydrate, calculated as anhydrous substance 20 mg;
Excipients: lactose monohydrate; potato starch; calcium stearate.
Dosage form
Pills.
Main physicochemical properties: tablets of white or almost white color, round shape with a flat surface, with a bevel.
Pharmacotherapeutic group
other agents acting on the nervous system. Parasympathomimetics. Anticholinesterase agents. ATX code N07A A.
Pharmacological properties
Pharmacodynamics
Mediathorn® is a drug that has a biologically beneficial combination of two molecular effects – blockade of membrane potassium permeability and inhibition of cholinesterase. In this case, blockade of membrane potassium permeability plays a crucial role.
Blockade of potassium permeability of the membrane leads primarily to a prolongation of the repolarization phase of the action potential of the excited membrane and an increase in the activity of the presynaptic axon. This causes an increase in the entry of calcium ions into the presynaptic terminal, which in turn leads to an increase in the release of the mediator into the presynaptic cleft in all synapses. An increase in the concentration of the mediator in the synaptic cleft contributes to a stronger stimulation of the postsynaptic cell due to the mediator-receptor interaction. In cholinergic synapses, inhibition of cholinesterase causes an even greater accumulation of the neurotransmitter in the synaptic cleft and an increase in the functional activity of the postsynaptic cell (contraction, conduction of excitation).
Ipidacrine enhances the effects of acetylcholine, adrenaline, serotonin, histamine, and oxytocin on smooth muscles.
Ipidacrine exhibits the following pharmacological effects:
- stimulation and restoration of neuromuscular transmission;
- restoration of impulse conduction in the peripheral nervous system after its blockade by various agents (trauma, inflammation, action of local anesthetics, some antibiotics, potassium chloride, toxins);
- increased contractility of smooth muscle organs;
- specifically moderate stimulation of the central nervous system (CNS) with individual manifestations of a sedative effect;
- improving memory and learning ability;
- analgesic effect.
The drug does not have teratogenic, embryotoxic, mutagenic and carcinogenic, as well as allergenic and immunotoxic effects, and does not affect the endocrine system.
Pharmacokinetics
After oral administration, the drug is rapidly absorbed from the digestive tract. The maximum concentration of the active substance is reached in the blood plasma 1 hour after administration. From the blood, ipidacrine quickly enters the tissues, in the stabilization stage only 2% of the drug is detected in the blood serum, the half-life in the distribution phase is 40 minutes.
40–50% of the active substance binds to blood plasma proteins. Ipidacrine is absorbed mainly from the duodenum, slightly less from the small and ileum, only 3% of the dose is absorbed in the stomach. Elimination of ipidacrine from the body is carried out by a combination of renal and extrarenal mechanisms (biotransformation, secretion with bile), with urinary secretion prevailing. Only 3.7% of ipidacrine is excreted in the urine in unchanged form, which indicates a rapid metabolism of the drug in the body.
Indication
‒ Diseases of the peripheral nervous system (neuropathy, neuritis, polyneuritis and polyneuropathy, myelopolyradiculoneuritis);
- myasthenia and myasthenic syndrome of various etiologies;
- bulbar palsies and paresis;
- memory impairment of various etiologies (Alzheimer's disease and other forms of senile mental impairment); mental retardation in children;
- the recovery period of organic lesions of the CNS, accompanied by motor disorders;
- in the complex therapy of multiple sclerosis and other forms of demyelinating diseases of the nervous system;
- intestinal atony.
Contraindication
- Hypersensitivity to ipidacrine and other components of the drug;
- epilepsy;
- extrapyramidal disorders with hyperkinesis;
- angina pectoris;
- pronounced bradycardia;
- bronchial asthma;
- vestibular disorders;
- mechanical obstruction of the intestines and urinary tract;
- gastric or duodenal ulcer in the acute stage;
- pregnancy;
- the breastfeeding period.
Interaction with other medicinal products and other types of interactions
Mediathorn® enhances the sedative effect in combination with drugs that depress the CNS. The effect and side effects are enhanced when used together with other cholinesterase inhibitors and m-cholinomimetics.
In patients with myasthenia gravis, the risk of developing a "cholinergic" crisis increases if Mediathorn® is used simultaneously with cholinergic agents. The risk of developing bradycardia increases if β-blockers are used before starting treatment with Mediathorn®.
Mediathorn® can be used in combination with nootropic drugs.
Alcohol increases the side effects of the drug.
Cerebrolysin improves the mental effect of the drug Mediathorn®.
Application features
The drug should be used with caution in patients with a history of peptic ulcer of the stomach and duodenum, respiratory diseases, including acute respiratory diseases, cardiovascular diseases not associated with coronary pain, and thyrotoxicosis.
The drug contains lactose, therefore patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use it.
Use during pregnancy or breastfeeding
Mediathorn® increases uterine tone and may cause premature birth, so the use of the drug is contraindicated during pregnancy.
The use of the drug is contraindicated during breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
Mediathorn® may have a sedative effect, so caution should be exercised when using the drug while driving.
Method of administration and doses
Mediathorn® tablets are used internally.
For neuritis – 1 tablet 2–3 times a day. The course of treatment is from 10–15 days for acute neuritis to 20–30 days for chronic neuritis. If necessary, the course of treatment should be repeated 2–3 times with an interval of 2–4 weeks until the maximum effect is achieved.
For myelopolyradiculoneuritis and paresis – 1 tablet 2–3 times a day for 30–40 days. Repeat the treatment courses several times with an interval of 1–2 months, until the therapeutic effect is achieved.
For myasthenia and myasthenic syndromes – 1–2 tablets 2–3 times a day. For severe forms, the dose can be increased to 200 mg per day (2 tablets 5 times a day after 2–3 hours). Treatment is a course, alternating with classic anticholinesterase drugs.
For multiple sclerosis and other forms of demyelinating diseases of the nervous system, bulbar paralysis - 1 tablet 3–5 times a day for 60 days 2–3 times a year.
In Alzheimer's disease and other forms of senile mental impairment, start with a dose of 1–2 tablets per day, divided into 2 doses, with a gradual increase in the dose by 2 tablets per week to 6–10 tablets per day (2 tablets 3–5 times a day). Duration of treatment is from 4 months to 1 year. Course therapy is possible - 4–5 months with a break of 1–2 months.
In organic lesions of the CNS, accompanied by motor disorders - 1 tablet 2-3 times a day. The average course of treatment is 30 days. If necessary, the course of treatment can be repeated.
For intestinal atony – 1–3 tablets per day, dividing the dose into 3 doses. The course of treatment is 1–3 weeks.
Children aged 12 years and older with mental retardation and peripheral nervous system diseases should be prescribed Mediathorn® 1 tablet (20 mg) 2–3 times a day. The course of treatment is 1–2 months (depending on the clinical picture).
Children
The drug can be used in children over 12 years of age.
Overdose
In severe intoxication, a cholinergic crisis may develop.
Symptoms: bronchospasm, lacrimation, increased sweating, constriction of the pupils, nystagmus, increased peristalsis of the digestive tract, spontaneous defecation and urination, vomiting, jaundice, bradycardia, cardiac conduction disorders, arrhythmia, decreased blood pressure, anxiety, agitation, feelings of fear, ataxia, convulsions, coma, speech disorders, drowsiness, general weakness.
Treatment: symptomatic therapy. Use of m-cholinoblockers (atropine, cyclodol, metacin).
Adverse reactions
Classification of the frequency of adverse reactions: very common (≥ 1/10); common (from 1/100 to 1/10); uncommon (from 1/1000 to 1/100); rare (from 1/10000 to 1/1000); very rare (< 1/10000), including isolated cases; frequency unknown (cannot be estimated from the available data).
Mediathorn® is well tolerated. Possible side effects are associated with the stimulation of m-cholinergic receptors.
On the part of the heart: often - palpitations, bradycardia, chest pain.
From the nervous system: infrequently (when using high doses) - dizziness, headache, drowsiness, general weakness, muscle cramps.
From the respiratory system, chest organs and mediastinum: infrequently - increased secretion of bronchial secretions, bronchospasm.
From the gastrointestinal tract: often - salivation, nausea; infrequently (when using high doses) - vomiting; rarely - diarrhea, pain in the epigastric region.
Hepatobiliary disorders: frequency unknown – jaundice.
Skin and subcutaneous tissue disorders: often - increased sweating; infrequently (after taking high doses) allergic reactions are possible, including itching, rash.
Immune system disorders: frequency unknown - hypersensitivity reactions (including allergic dermatitis, anaphylactic shock, asthma, toxic epidermal necrolysis, erythema, urticaria, wheezing, laryngeal edema).
From the reproductive system: increased uterine tone.
Salivation and bradycardia can be reduced by anticholinergics (e.g. atropine). If undesirable effects occur, the dose should be reduced or the drug should be discontinued for a short period (1–2 days).
Expiration date
2 years.
Storage conditions
In the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 tablets in a blister, 5 blisters in a pack.
Vacation category
According to the recipe.
Producer
PJSC "Kyivmedpreparat".
Location of the manufacturer and address of its place of business
Ukraine, 01032, Kyiv, Saksaganskoho St., 139.
