INSTRUCTION

(information for professionals)

for medical use of the drug

TSEREKARD

 

Registration number: LSR-003013/09-160409

Trade name TSEREKARD

INN or grouping name ethylmethylhydroxypyridine succinate Dosage Form: Solution for intravenous and intramuscular injection

Composition

Active ingredient:

Ethylmethylhydroxypyridine succinate .................. 0.050 g;

Excipients:

Water for injection ............................................. to 1 ml.

Description: Colorless, clear liquid

Pharmacotherapeutic group: Anti-oxidant agent

Code ATX N07XX

Pharmacological properties

Pharmacodynamics

Preparation of 3 - hydroxypyridine group. Is an inhibitor of free radical processes - membrane protectors, providing also antihypoxia , stress protective, nootropic, antiepileptic and anxiolytic effects. The mechanism of action is due to antioxidant and membrane-protective properties. Inhibits lipid peroxidation, increases the activity superoksidoksidazy, increases the ratio of lipid- protein, improves the structure and function of cell membranes. Modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase) receptor complexes ( benzodiazepine, GABA, acetylcholine), which contributes to their ligand binding, preservation of structural and functional organization of biological membranes, transport of neurotransmitters and improve synaptic transmission. Increases the concentration of dopamine in the brain.

Compensatory activation enhances aerobic glycolysis and reduces the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions with an increase in ATP and creatine phosphate activates energosinteziruyuschuyu mitochondrial function.

Increases the body's resistance to a variety of damaging factors in pathological conditions. Metabolism and improves blood flow to the brain, microcirculation and blood rheology, reduce platelet aggregation. Stabilizes the membranes of red blood cells (erythrocytes and platelets), reducing the likelihood of developing hemolysis. Has hypolipidemic effect, reduces total cholesterol and low density lipoprotein.

Improve the functional status of ischemic myocardium in myocardial infarction, the contractile function of the heart and reduces the appearance of systolic and diastolic left ventricular dysfunction. In terms of the critical reduction in coronary blood flow helps to preserve the structural and functional organization of membranes of cardiomyocytes, stimulates the activity of membrane enzymes - phosphodiesterase, adenylate cyclase, acetylcholinesterase. Support developing in acute ischemia and activation of aerobic glycolysis in hypoxia promotes recovery of mitochondrial redox processes, increases the synthesis of ATP and creatine phosphate. Ensures the integrity of the morphological structures and physiological functions of the ischemic myocardium.

Improves the clinical course of myocardial infarction, increases the effectiveness of the therapy , accelerates the recovery of functional activity of the left ventricular myocardium, reduces the incidence of arrhythmias and intracardiac conduction disorders. Normalises metabolic processes in the ischemic myocardium reduces the zone of necrosis, restores and / or improves the electrical activity and cardiac contractility, and coronary blood flow increases in the ischemic area, improves nitropreparatov antianginal activity, improves the rheological properties of blood and reduces the consequences of reperfusion syndrome of acute coronary insufficiency.

 

Pharmacokinetics

Time to reach maximum concentration when administered intramuscularly - 0,3-0,58 hour. This maximum value of concentration when administered intramuscularly at a dose of 400-500 mg is from 2.5 to 4 ug / ml. Rapidly distributed in tissues and organs. Mean residence time of the drug in the body when administered intramuscularly - 0.7-1.3 hours.

Metabolized in the liver by glyukuronirovaniya. 5 metabolites found:

  • 3 - hydroxypyridine phosphate (produced by the liver and involvement of alkaline phosphatase is decomposed into phosphoric acid and 3 - hydroxypyridin);
  • 2-y is the pharmacologically active metabolite found in urine and 1-2 days after injection;
  • Third - shows in large quantities in the urine;
  • 4th and 5th are conjugates with glucuronic acid.

Rapidly excreted in the urine mainly as metabolites (50 % in 12 hours) and in small quantities - unchanged ( 0.3 % in 12 h ) . Most intensively excreted within the first 4 hours after ingestion. Indicators of urinary excretion of unchanged drug and metabolites have significant individual variability .

 

Indications for use

The drug is used as part of combination therapy with:

  • Anxiety neurotic and conditions;
  • Dystonia;
  • Encephalopathy;
  • Acute cerebrovascular accident (ischemic stroke);
  • Mild cognitive disorders atherosclerotic;
  • Alcohol withdrawal syndrome with prevalence of neurosis and vegetovascular disorders;
  • Acute intoxication antipsychotic drugs;
  • Acute myocardial infarction from the first day.

 

Contraindications

  • Individual hypersensitivity to the drug;
  • Acute hepatic and / or renal failure;
  • Age 18 (efficacy and safety have not been established);
  • Pregnancy;
  • Breastfeeding.

Precautions

Allergic diseases.

 

Dosing and Administration

The drug is administered intravenously or intramuscularly ( within 5-7 minutes) or infusion ( at 60 drops per minute).

When the infusion method of administering a drug in a pre-diluted with 200 ml of 0.9 % sodium chloride solution. Initial dose is 50-100 mg 1-3 times a day with gradual increase to a therapeutic effect. The maximum daily dose - 800 mg.

When acute cerebral circulatory administered intravenously 200-300 mg 1 time a day for the first 2-4 days, followed by intramuscular injection of 100 mg 3 times a day.

When vascular encephalopathy ( decompensation phase ) is administered intravenously or infusion of 100 mg 2-3 times a day for 14 days, followed by intramuscular injection of 100 mg for 14 days. For prevention of vascular encephalopathy course prescribed by intramuscular injection of 100 mg 2 times a day for 10-14 days.

Vegetative-vascular dystonia , neurotic and neurosis-like states: the drug is administered intramuscularly to 50-400 mg per day, course of treatment - 14 days.

When alcohol withdrawal syndrome is administered intramuscularly at 100-200 mg 2-3 times a day intravenously or 100-200 mg 1-2 times a day for 5-7 days.

Acute intoxication with antipsychotic drugs administered intravenously at 50-300 mg per day for 7-14 days.

Mild cognitive disorders: intramuscular injection of 100-300 mg per day for 14-30 days. Acute myocardial infarction: the first 5 days of the drug is administered intravenous infusion for 30-90 minutes ( 100-150 ml of 0.9% sodium chloride or 5 % dextrose) or intravenously for at least 5 min. In the next nine days the drug is administered intramuscularly 3 times a day (every 8 hours). The daily dose - 9.6 mg / kg / day, a single dose - 3.2 mg / kg. The maximum daily dose should not exceed 800 mg, single dose - 250 mg .

 

Side effect

May develop (especially when administered intravenously) dry mouth, "metallic" taste in your mouth, feeling "pours heat" throughout the body odor, sore throat and chest discomfort, feeling short of breath (which, as a rule, due to the extremely high rate of introduction and a short-term nature), allergic reactions.

With prolonged use may experience nausea, flatulence; sleep disturbances (drowsiness or violation of sleep).

 

Verdose

Overdose symptoms : sleep disorders (insomnia , in some cases - drowsiness) , when administered intravenously - slight and short-term ( up to 1.5-2 h ) increase in blood pressure.

In case of overdosage, treatment is usually not required, since the symptoms disappear on their own within a day . In severe cases of insomnia sleeping pills recommended the appointment of a group of benzodiazepines ( 10 mg nitrazepam , oxazepam , diazepam 10 mg or 5 mg).

In marked increase in blood pressure should be the appointment of antihypertensive drugs for the control of blood pressure and / or complementary therapy nitropreparatov.

 

Interaction with other drugs

The drug enhances the effect of the benzodiazepine group of anxiolytics, antiepileptics (carbamazepine), antiparkinsonian (levodopa) drugs, nitrates. Reduces the toxic effects of ethanol.

Cautions

During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and speed of psychomotor reactions.

 

Form of

Solution for intravenous or intramuscular injection of 50 mg / ml in ampoules import 1st hydrolytic class colorless or lighting glass ring with the point of fracture, or 2 ml or 5 ml.

5 vials contour blister of PVC film and aluminum foil. May be packed in preparation contour cell pack without foil. 1 or 2 stripes package along with instructions for medical use in the stack of cardboard.

 

Shelf life

3 years. Do not use beyond the expiration date.

 

Storage conditions

List B. In a dry, dark place at a temperature not exceeding 25 ° C. Keep out of reach of children.

 

Terms of supply of pharmacies

Prescription.

 

manufacturer

Ltd. "Altair"

142100, Moscow region., Podolsk, st. Komsomolskaya 1, fax (495) 963-04-66 142279, Moscow region, Serpukhov District, Obolensk, Building 31, tel / fax (4967) 31 - 20-74

 

Organization receiving complaints from consumers

Ltd. "Altair"

142100, Moscow region., Podolsk, st. Komsomolskaya 1, tel. / Fax (495) 963-04-66 142279, Moscow region, Serpukhov District, Obolensk, Building 31, tel / fax (4967) 31-20-74

 

Marketing in Russia

LLC «ESKO PHARMA»

115093, Moscow, ul. Pavlovian, 6

Tel.: +7 (495) 980 95 15

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