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Sevacitol ®- injection

MEDICAL INSTRUCTIONS FOR USE

SEVACITOL®

Trade name of the drug: Sevacitol®

Active substance (INN): Ethylmethylhydroxypyridine succinate

Pharmaceutical form: solution for injection

Contents per 1 ml:

Active substance: Ethylmethylhydroxypyridine succinate-50 mg

Excipients: sodium metabisulfite, water for injection.

Description: clear colorless or slightly yellowish liquid.

Pharmacotherapeutic group: Antioxidant agent.

ATX code: N07XX

Pharmacological properties

Pharmacodynamics

It has antihypoxic, membranoprotective, nootropic, anticonvulsant, anxiolytic effect, increases resistance to stress. The drug increases the body’s resistance to the effects of major damaging factors, to oxygen-dependent pathological states (shock, hypoxia and ischemia, cerebral circulation disorders, intoxication with alcohol and antipsychotic drugs (neuroleptics).

The drug improves cerebral metabolism and blood supply to the brain, improves microcirculation and blood rheological properties, reduces platelet aggregation. Stabilizes membrane structures of blood cells (erythrocytes and platelets) in hemolysis. It has a hypolipidemic effect, reduces the level of total cholesterol and LDL. It reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

The mechanism of action of the drug is due to its antihypoxant, antioxidant and membrane-protective effects. It inhibits lipid peroxidation processes, increases superoxide dismutase activity, increases lipid-protein ratio, reduces membrane viscosity and increases its fluidity. Modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which increases their ability to bind to ligands, helps maintain the structural and functional organization of biomembranes, transport neurotransmitters and improve synaptic transmission. The drug increases dopamine content in the brain. Causes enhancement of compensatory activity of aerobic glycolysis and reduction of the degree of inhibition of oxidative processes in the Krebs cycle under hypoxia, with an increase in ATP, creatine phosphate and activation of energy-synthesizing functions of mitochondria, stabilization of cell membranes. The drug normalizes metabolic processes in ischemic myocardium, reduces the zone of necrosis, restores and improves myocardial electrical activity and contractility, as well as increases coronary blood flow in the ischemic area, reduces the effects of reperfusion syndrome in acute coronary failure.

Pharmacokinetics

Absorption

Time to reach maximum concentration (Tmax) – 0.45-0.5 h. Cmax when 400-500 mg dose is administered is 3.5-4.0 mcg/ml.

Distribution

When administered intravenously, it is determined in plasma for 4 hours after injection. The drug rapidly passes from the bloodstream to organs and tissues and is rapidly eliminated from the body. Time retention time (MRT) is 0.7-1.3 hours.

Excretion

The drug is eliminated mainly with urine, mainly in glucuron conjugated form and in small amounts unchanged.

Indications for use

  • Acute disorders of cerebral circulation;
  • craniocerebral trauma, consequences of craniocerebral injuries;
  • discirculatory encephalopathy;
  • vegetative dystonia syndrome;
  • Mild cognitive disorders of atherosclerotic genesis;
  • Anxiety disorders in neurotic and neurosis-like conditions;
  • Acute myocardial infarction (from the first day) as part of the treatment;
  • Primary open-angle glaucoma of different stages, as part of complex therapy;
  • acute intoxication with antipsychotic drugs;
  • acute pyo-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis) as part of the treatment.

Methods of administration and dosage

The drug is administered v/m or intravenously (by stream or dropwise). When administering by infusion the drug should be diluted in 0.9% sodium chloride solution. The drug shall be administered by jetting slowly for 5-7 minutes, by drip infusion at a rate of 40-60 drops/min. The maximum daily dose should not exceed 1200 mg.

In acute cerebral circulation disorders the drug is administered in the first 10-14 days by IV drops 200-500 mg 2-4 times daily, then by IV drops 200-250 mg 2-3 times daily for 2 weeks. In case of craniocerebral trauma and craniocerebral injuries sequelae the drug is used for 10-15 days by IV drip 200-500 mg 2-4 times per day.

In decompensated dyscirculatory encephalopathy the drug should be administered by IV streaming or dropwise in a dose of 200-500 mg 1-2 times per day for 14 days, then by IM 100-250 mg per day during next 2 weeks.

For course prophylaxis of discirculatory encephalopathy the drug is administered in a monthly dose of 200-250 mg 2 times per day for 10-14 days.

In mild cognitive impairment in elderly patients and in cases of anxiety disorders the drug is administered in a daily dose of 100-300 mg/m for 14-30 days.

In acute myocardial infarction, as part of complex therapy, the drug is administered v/v or intravenously for 14 days against the background of traditional therapy of myocardial infarction, including nitrates, beta-adrenoblockers, ACE inhibitors, thrombolytics, anticoagulants and antiplatelet agents, as well as symptomatic drugs according to indications.

In the first 5 days, to achieve maximum effect, the drug should be administered v/v, in the next 9 days the drug may be administered v/m.

The preparation is administered intravenously by drop infusion, slowly (in order to avoid side effects) using 0.9% sodium chloride solution or 5% dextrose (glucose) solution in the amount of 100-150 ml in 30-90 minutes. If necessary, slow trickle administration of the drug for at least 5 min is possible.

The drug is administered (intravenously or intramuscularly) 3 times/day every 8 hours. The daily therapeutic dose is 6-9 mg/kg of body weight/day, single dose – 2-3 mg/kg of body weight. The maximum daily dose should not exceed 800 mg, a single dose – 250 mg.

In open angle glaucoma of various stages the drug is administered as part of complex therapy intravenously in 100-300 mg/day 1-3 times/day for 14 days.

In acute intoxication with antipsychotic drugs the drug is administered in an IV dose of 200-500 mg/day for 7-14 days.

In acute pyo-inflammatory processes of abdominal cavity (acute necrotizing pancreatitis, peritonitis) the drug is prescribed in the first day, both in preoperative and in postoperative period. Administered doses depend on the form and severity of the disease, process prevalence, variants of the clinical course. Withdrawal of the drug should be carried out gradually.

In acute edematous (interstitial) pancreatitis drug is prescribed 200-500 mg 3 times per day by IV drops (in 0.9% sodium chloride solution) and intravenously.

Mild degree of necrotic pancreatitis severity – 100-200 mg 3 times per day by IV drops (in 0.9% sodium chloride solution) and intravenously.

Moderate severity of necrotic pancreatitis – 200 mg 3 times/day by IV drip (in 0.9% sodium chloride solution).

A severe course of necrotic pancreatitis – in pulse dosage of 800 mg during the first day, twice daily, further – 200-500 mg 2 times per day with gradual decrease of daily dose.

Extremely severe necrotic pancreatitis – initial dose is 800 mg per day until symptoms of pancreatogenic shock are relieved; after stabilization, the daily dose is reduced gradually by 300-500 mg twice a day by IV drip (in 0.9% sodium chloride solution).

Side effects

Nausea and dry mouth, drowsiness and allergic reactions are possible.

Contraindications

  • Acute liver dysfunction;
  • acute renal dysfunction;
  • Individual hypersensitivity to the drug.

Strictly controlled clinical studies on the safety of the drug in children and during pregnancy and lactation have not been conducted.

Drug interactions

Increases the effect of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian drugs (levodopa). Reduces the toxic effects of ethyl alcohol.

Special indications

In individual cases, especially in predisposed patients with bronchial asthma with hypersensitivity to sulfites, severe hypersensitivity reactions may develop.

Overdose:

In case of overdose, drowsiness may develop.

Form of production

Solution for injection 50 mg/ml 2 ml, 5 ml, #5 #10(2×5,1×10) (ampoules).

Storage conditions

Store in a dry, dark place at temperatures under 25°C. Keep out of the reach of children!

Shelf life

2 years. Do not use after the expiration date.

Conditions for dispensing from pharmacies

Released by a doctor’s prescription.

Nevaron ® Neo – injection

INSTRUCTIONS FOR MEDICAL USE

NEVARON® NEO

Trade name of the drug: Nevaron® Neo

Active ingredients (INN): thiamine hydrochloride + pyridoxine hydrochloride + cyanocobalamin + lidocaine hydrochloride

Dosage form: solution for injection

Contents:

2 ml of the drug contains:

Active ingredients: thiamine hydrochloride 100.0 mg, pyridoxine hydrochloride 100.0 mg, cyanocobalamin 1.0 mg, lidocaine hydrochloride 20.0 mg;

Excipients: benzyl alcohol, sodium polyphosphate, potassium ferricyanide, sodium hydroxide, water for injection up to 2 ml.

Description: clear red solution.

Pharmacotherapeutic group: vitamin.

ATX code: A11E

Pharmacological properties

B-group neurotropic vitamins have a beneficial effect on inflammatory and degenerative diseases of the nerves and the motor system. Contribute to increased blood flow and improve nervous system function.

Thiamine plays a key role in metabolism of carbohydrates, as well as in the Krebs cycle, with subsequent participation in the synthesis of TPP (thiamine pyrophosphate) and ATP (adenosine triphosphate).

Pyridoxine is involved in protein metabolism and, in part, in carbohydrate and fat metabolism. The physiological function of both vitamins is to potentiate each other’s action, manifesting itself in a positive effect on the nervous, neuromuscular and cardiovascular systems. In vitamin B6 deficiency, widespread deficiency states are quickly ameliorated after administration of these vitamins.

Cyanocobalamin is involved in the synthesis of myelin sheath, stimulates hematopoiesis, reduces pain associated with lesions of the peripheral nervous system, stimulates nucleic metabolism through activation of folic acid.

Lidocaine is a local anesthetic agent, causing all types of local anesthesia: terminal, infiltration, conduction.

Pharmacokinetics

After intramuscular administration, thiamine is rapidly absorbed from the injection site and enters the blood (484 ng/ml after 15 min on the first day of administration of a dose of 50 mg) and is irregularly distributed in the body, containing 15% in leukocytes, 75% in erythrocytes and 10% in plasma. Because of the lack of significant stores of the vitamin in the body, it must be administered daily. Thiamine penetrates the blood-brain and placental barriers and is found in mother’s milk. Thiamine is excreted in the urine in the alpha phase after 0.15 hours, in the beta phase after 1 hour, and in the terminal phase within 2 days. The main metabolites are thiamine carboxylic acid, pyramine and some unknown metabolites. Of all vitamins, thiamine is retained in the body in the smallest amounts. The adult body contains about 30 mg of thiamine as 80% thiamine pyrophosphate, 10% thiamine triphosphate, and the remainder as thiamine monophosphate.

After intramuscular injection, pyridoxine is rapidly absorbed into the bloodstream and distributed in the body, acting as a coenzyme after phosphorylation of the CH2ON group at the 5th position. About 80% of the vitamin is bound to plasma proteins. Pyridoxine is distributed throughout the body and crosses the placenta and is found in the mother’s milk, deposited in the liver and oxidized to 4-pyridoxic acid, which is excreted in the urine, 2-5 hours maximum after absorption. The human body contains 40-150 mg of vitamin B6 and its daily elimination rate is about 1.7-3.6 mg with a replenishment rate of 2.2-2.4%.

Indications for use

As a pathogenetic and symptomatic agent in the treatment of diseases and syndromes of the nervous system of various origins: neuralgia, neuritis, facial nerve paresis, retrobulbar neuritis, ganglionitis (including shingles), plexopathy, neuropathy, polyneuropathy (diabetic, alcoholic, etc.), night-time muscle cramps. ), nocturnal muscle cramps, especially in older age groups, neurological manifestations of spinal osteochondrosis: radiculopathy, lumboishalgia, muscle-tonic syndromes.

Dosage and administration

Injections are performed deeply intramuscularly, once a day.

In cases of pronounced pain syndrome to quickly reach high levels of the drug in the blood, it is advisable to start treatment with 2.0 ml daily for 5-10 days. Further, after pain syndrome has subsided and in mild forms of the disease, the therapy is transferred either to oral dosage form or to more rare injections (2-3 times a week for 2-3 weeks) with possible continuation of therapy with oral dosage form. Weekly monitoring of therapy by a physician is recommended. Transition to therapy by oral dosage form is recommended to be carried out as soon as possible.

Side effects

Frequency of manifestation of adverse reactions is given in accordance with the WHO classification:

Very oftenMore than 1 in 10 of those treated
OftenLess than 1 in 10, but more than 1 in 100 treated
In some casesLess than 1 in 100, but more than 1 in 1000 treated
RarelyLess than 1 in 1,000, but more than 1 in 10,000 treated
Very rarelyless than 1 in 10,000, including individual cases

*In some cases, symptoms occur with unknown frequency;

Immune system disorders:

Rarely: allergic reactions (skin rash, difficulty in breathing, anaphylactic shock, Quincke’s edema);

Nervous system disorders:

In some cases: dizziness, confusion;

Cardiovascular system disorders:

Very rarely: tachycardia;

In some cases: bradycardia, arrhythmia;

Gastrointestinal tract:

In some cases: vomiting;

Skin and subcutaneous tissue:

Very rare: increased sweating, acne, itching, urticaria;

Musculoskeletal and connective tissue disorders:

In some cases: seizures;

General disorders and disorders at the injection site:

In some cases: irritation at the site of administration may occur; Systemic reactions are possible with rapid administration or in case of overdose.

If any of the side effects mentioned in the instructions are aggravated, or if you notice any other side effects not specified in the instructions, inform your doctor.

Contraindications

Pregnancy and breastfeeding (See “Administration during pregnancy and breastfeeding”). Childhood age under 16 years old. Decompensated heart failure. Increased individual sensitivity to the components of the drug.

Drug interactions

Thiamine is completely disintegrated in solutions containing sulfites. As a consequence, the products of thiamine decomposition inactivate the activity of other vitamins. Thiamine is incompatible with oxidizing reducing compounds, including: iodides, carbonates, acetates, tannic acid, ammonium iron citrate, phenobarbital, riboflavin, benzylpenicillin, dextrose, desulfites, etc. Copper accelerates thiamine breakdown; in addition, thiamine loses its effectiveness when pH values (more than 3) increase. Therapeutic doses of pyridoxine weaken the effect of levodopa (the antiparkinsonian effect of levodopa is reduced) when taken simultaneously. Interaction with cycloserine, penicillamine, isoniazine is also observed. When parenteral administration of lidocaine in case of additional use of norepinephrine, an increased side effect on the heart is possible. Interaction with sulfonamides is also observed. Cyanocobalamin is incompatible with salts of heavy metals. Riboflavin also has a destructive effect, especially when simultaneously exposed to light; nicotinamide accelerates photolysis, while antioxidants have an inhibitory effect.

There is no information about caution regarding the use of the drug by drivers of vehicles and persons working with potentially dangerous mechanisms.

Special Indications

In case of accidental intravenous administration, the patient should be monitored by a doctor or hospitalized depending on the severity of symptoms.

Administration during pregnancy and breastfeeding

The drug is contraindicated during pregnancy and breastfeeding (see section “Contraindications”).

Influence on the reaction rate while driving motor transport or operating other mechanisms

There is no information concerning caution as to the use of the drug by drivers of vehicles and persons working with potentially dangerous mechanisms.

Overdose

Treatment of overdose consists in withdrawal of the drug and symptomatic therapy.

Form of production

Solution for injection of 2 ml in a contour cell pack.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of reach of children.

Shelf life

2 years.

Do not use after the expiration date.

Conditions for dispensing from pharmacies

Released by a doctor’s prescription.

Costapherol – oral drops

MEDICAL INSTRUCTIONS FOR USE

COSTAPHEROL

Trade name of the drug: Costaferool

Active substance (INN): Cholecalciferol

Dosage form: Oral drops.

Contents:

1 ml of the solution contains:

Active substance: Cholecalciferol – 15 000 ME

Excipients: macrogol glycerylcyanoleate, sucrose, sodium hydrophosphate dodecahydrate, citric acid monohydrate, anise flavoring, benzyl alcohol, purified water.

Description: colorless, transparent or slightly opalescent liquid with aniseed odor.

Pharmacotherapeutic group: Vitamins.

ATX code:A11CC05

Pharmacological properties

Pharmacodynamics

Aqueous solution of vitamin D3 is better absorbed than the oil-based solution (which is important when used in premature babies). After oral administration, colecalciferol is absorbed in the small intestine. It is metabolized in the liver and kidneys. Half-life of colocalciferol from blood is several days and may be prolonged in case of renal insufficiency. The drug penetrates through the placental barrier and into the mother’s milk. It is excreted with urine and feces.

Pharmacokinetics

Vitamin D3 is an active anti-rachitis factor. The most important function of vitamin D is to regulate calcium and phosphate metabolism, which promotes mineralization and skeletal growth. Vitamin D3 is a natural form of vitamin D, which is formed in the human skin by the action of sunlight. It plays an essential role in the absorption of calcium and phosphate from the intestine, in the transport of mineral salts and in the calcification of bones, and regulates the excretion of calcium and phosphate by the kidneys. The concentration of calcium ions acts on a number of important biochemical processes responsible for maintaining muscle tone in the skeletal muscles, in conducting nerve excitement, and in the process of blood clotting. Vitamin D is also involved in the immune system by affecting the production of lymphokines.

Indications for use

  • Prevention and treatment of vitamin D deficiency
  • Prevention and treatment of rickets
  • Prevention and treatment of rickets-like diseases (inherited tubulopathies)
  • Hypocalcemic tetany
  • Osteomalacia and metabolic disorders of the bones (such as hypoparathyreosis and pseudohypoparathyreosis)
  • Complex treatment of osteoporosis, including postmenopausal

Dosage and administration

The drug is taken orally with a small amount of liquid. One drop contains about 500 ME of vitamin D3.

The drug is used in the following dosages:

Prophylactic doses:

  • Premature infants from 3-4 weeks of life, up to 2-3 years of age with proper care and sufficient exposure to fresh air: 500-1000 ME (1-2 drops) per day;
  • Premature infants, from 7-10 days of age, twins, infants in poor living conditions: 1000-1500 ME (2-3 drops) per day. In summertime, the dose may be limited to 500 ME (1 drop) per day.
  • Pregnant women: a daily dose of 500 ME (1 drop)/day of vitamin D3, for the duration of pregnancy, or 1000 ME (2 drops) /day, starting at 28 weeks of pregnancy.
  • In postmenopausal period 500-1000 IU (1-2 drops) per day are prescribed.

Therapeutic doses:

  • For rickets: 2000-5000 ME (4-10 drops) daily, depending on the severity of rickets (I, II or III) and the course variant, for 4-6 weeks, under careful monitoring of the clinical condition and the examination of biochemical parameters (calcium, phosphorus, alkaline phosphatase) of blood and urine. It should be started with 2000 ME for 3-5 days. Then, if tolerated well, the dose is increased to an individual therapeutic dose (usually 3000 ME). The dose of 5000 ME is prescribed only in case of marked bone changes.

If necessary, after a one-week break, the treatment can be repeated.

Treatment is continued until a clear therapeutic effect is achieved, followed by a prophylactic dose of 500 to 1500 ME/day.

  • In the treatment of rickets-like diseases: 20,000-30,000 ME per day (40-60 drops) depending on the age, body weight and severity of the disease, under the control of biochemical blood and urine tests. The course of treatment is 4-6 weeks. The treatment is carried out under the supervision of a doctor.
  • In the complex treatment of postmenopausal osteoporosis: 500-1000 ME (1-2 drops) per day.

The dosage is usually prescribed taking into account the amount of vitamin D coming from food.

Side effects

Not observed when used in the recommended doses.

In case of rare individual hypersensitivity to vitamin D3 or as a result of using too high doses for a long period, hypervitaminosis D3 may occur:

  • loss of appetite, nausea, vomiting
  • Headaches, muscle and joint pains.
  • constipation, dry mouth, and polyuria
  • mental disorders, including depression, weight loss, increased calcium levels in blood and excretion of calcium in urine
  • Renal stone formation and calcification of soft tissues.

Contraindications

  • hypervitaminosis D
  • High calcium levels in blood and urine
  • calcium kidney stones
  • sarcoidosis
  • Hypersensitivity to drug components, especially benzyl alcohol
  • In case of hepatic or renal impairment

Drug interactions

Antiepileptic agents, rifampicin, cholestyramine reduce the reabsorption of vitamin D3. Simultaneous use with thiazide diuretics increases the risk of hypercalcemia.

Simultaneous use with cardiac glycosides may increase their toxic effect (increased risk of cardiac arrhythmias).

Cautions

Avoid overdose.

Individual provision of a certain need should take into account all possible sources of this vitamin. Too high doses of vitamin D3 administered for long periods or shock doses can cause chronic hypervitaminosis D3. Determination of the child’s daily vitamin D requirement and method of administration should be determined by the physician individually and adjusted each time during periodic examinations, especially in the first months of life.

Use with caution in immobilized patients.

Do not use calcium preparations in high doses simultaneously with vitamin D3. Treatment is carried out under periodic monitoring of calcium levels in blood and urine. Caution is necessary when prescribing the drug to elderly people because calcium deposition in the body increases in this category of people.

Pregnancy and lactation

It is not recommended to use high doses of vitamin D3 during pregnancy because of possible teratogenic action in case of overdose.

Caution should be exercised when prescribing vitamin D3 for breastfeeding women, since the drug taken in high doses by the mother may cause overdose symptoms in the child.

Effect on the ability to drive vehicles and maintain mechanical equipment

No effect

Overdose

Symptoms of overdose: decreased appetite, nausea, vomiting, constipation, restlessness, thirst, polyuria, diarrhea, intestinal colic. Frequent symptoms are headache, muscle and joint pain, mental disorders, including depression, stupor, ataxia and progressive weight loss. Renal dysfunction develops with albinuria, erythrocyturia and polyuria, increased potassium loss, hypostenuria, nycturia and increased blood pressure. In severe cases there may be corneal clouding, less often edema of the optic nerve papilla, iris inflammation up to cataract development. Kidney stones may form, calcification of soft tissues, including blood vessels, heart, lungs and skin may occur. Rarely cholestatic jaundice develops.

Treatment: Discontinue use of the drug. Consult a doctor. Take plenty of fluids. If necessary, hospitalization may be required.

Form of production

Oral drops 15 000 IU/ml in 10 ml, 20 ml, 30 ml in dropper bottles, vials.

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25°C. Keep out of the reach of children!

Shelf life

2 years. Do not use after the expiration date.

Conditions of dispensing from pharmacies

Released without a prescription.

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