Cockarnite (COCARNIT)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Dosage form: & nbsplyophilizate for the preparation of a solution for intramuscular injection
Composition:

Each ampoule contains:

active components: trifosadenine disodium trihydrate 10.0 mg, cocarboxylase 50.0 mg, cyanocobalamin 0.5 mg, nicotinamide 20.0 mg;

Excipients: glycine 105.875 mg, methyl parahydroxybenzoate 0.6 mg, propyl parahydroxybenzoate 0.15 mg.

Each ampoule of the solvent contains: lidocaine hydrochloride 10 mg, water for injection up to 2 ml.

Description:

Lyophilized mass Pink colour.

The reconstituted solution is a transparent, pink color.

Pharmacotherapeutic group:Metabolic means
ATX: & nbsp
  • B group vitamins in combination with other drugs
    • Pharmacodynamics:

    The drug is a rationally selected complex of metabolic substances and vitamins.

    Trifosadenin is an adenosine derivative, stimulates metabolic processes. Has a vasodilating effect, including on the coronary and cerebral arteries. Improves metabolism and energy supply of tissues. Has antihypertensive and antiarrhythmic action. Under the influence of ATP, blood pressure decreases, smooth muscle relaxation, and nerve impulses are improved.

    Cocarboxylase - coenzyme formed in the body from the incoming thiamine (vitaminAT1). It is part of the enzyme carboxylase, which catalyzes the carboxylation and decarboxylation of α-keto acids. Mediates the synthesis of nucleic acids, proteins and lipids indirectly. Reduces the concentration of lactic and pyruvic acids in the body, promotes the absorption of glucose. Improves the trophism of nervous tissue.

    Cyanocobalamin (vitamin B12) in the body is converted to methylcobalamin and 5-deoxyadenosylcobalamin. Methylcobalamin participates in the homocysteine ​​conversion reaction in methionine and S-adenosylmethionine - the key reactions of the metabolism of pyrimidine and purine bases (and, consequently, DNA and RNA). If the vitamin is deficient in this reaction, it can be replaced by methyltetrahydrofolic acid, with folic acid reactions of metabolism being disturbed.

    5-deoxyadenosyl cobalamin serves cofactor in isomerization L-methylmalonyl-CoA in succinyl-CoA - an important reactions metabolism of carbohydrates and lipids.

    Vitamin B deficiency12 leads to a violation of the proliferation of rapidly dividing cells of the hematopoietic tissue and epithelium, as well as to the violation of the formation of the myelin sheath of neurons.

    Nicotinamide - one of the forms of vitamin PP, participates in oxidation-reduction processes in the cell, improves carbohydrate and nitrogen metabolism, regulates tissue respiration.

    Pharmacokinetics:

    Trifosadenin

    After parenteral administration, it penetrates into the cells of the organs, where it is split into adenosine and inorganic phosphate with energy release. Subsequently, decay products are included in the resynthesis of ATP.

    Cocarboxylase

    Quickly absorbed after intramuscular injection. Penetrates into most body tissues. It is subject to metabolic decomposition. Metabolism products are excreted mainly by the kidneys.

    Cyanocobalamin

    In blood cyanocobalamin binds to the trans-balanamines I and II, which transport it into tissues. It is deposited mainly in the liver. The connection with plasma proteins is 90%. Quickly and completely absorbed after intramuscular and subcutaneous injection. The maximum concentration after intramuscular injection is achieved after 1 hour.

    From the liver is excreted bile in the intestine and again absorbed into the blood. Half-life is 500 days. It is excreted at normal kidney function - 7-10% by kidneys, about 50% - by the intestine.With reduced renal function - 0-7% kidney, 70-100% - intestine. Penetrates through the placental barrier, into breast milk.

    Nicotinamide

    Quickly distributed into all tissues. Penetrates through the placental barrier and into breast milk. Metabolized in the liver with the formation of nicotinamide-N-methylnicotinamide. It is excreted by the kidneys.

    The half-life of plasma is about 1.3 hours, the stationary volume of distribution is about 60 liters, and the total clearance is about 0.6 liters per minute.

    Indications:

    Symptomatic treatment of diabetic polyneuropathy.

    Contraindications:

    - Hypersensitivity to any component of the drug or a solvent;

    - cardiovascular diseases: acute heart failure, acute myocardial infarction, uncontrolled arterial hypertension, arterial hypotension, severe forms of bradyarrhythmia, AV-blockade II-III degree, chronic heart failure (III- IV art. by NYHA), cardiogenic shock and other types of shocks, prolongation syndrome QT, thromboembolism, hemorrhagic stroke;

    - inflammatory lung diseases, chronic obstructive pulmonary disease, bronchial asthma;

    - pregnancy, the period of breastfeeding;

    - children's age till 18 years;

    - hypercoagulation (including acute thrombosis), erythremia, erythrocytosis;

    - peptic ulcer of the stomach or duodenum in the stage of exacerbation;

    - gout;

    - hepatitis, cirrhosis.

    Carefully:With angina pectoris.
    Pregnancy and lactation:

    It is not recommended to use the drug KOKARNIT during pregnancy.

    It is recommended to stop breastfeeding for the duration of treatment with the drug.

    Dosing and Administration:

    The drug is injected deeply intramuscularly (in the gluteus muscle).

    In cases of severe pain, it is advisable to start treatment with intramuscular injection of 1 ampoule (2 ml) per day until acute symptoms are removed. Duration of application - 9 days.

    After improvement of symptoms or in cases of moderate symptoms of polyneuropathy: 1 ampoule 2-3 times a week for 2-3 weeks. The recommended course of treatment is 3-9 injections, depending on the severity of the disease.

    The duration of treatment and the holding of repeated courses is determined by the doctor depending on the nature and severity of the disease.

    Use in children

    Data on the efficacy and safety of the drug Kokarnita children are absent.

    Side effects:

    The incidence of adverse reactions is given in accordance with the WHO classification: very often (more than 1/10); often (less than 1/10, but more than 1/100); infrequently (less than 1/100, but more than 1/1000); rarely (less than 1/1000, but more than 1/10000); very rarely (less than 1/10000), including individual cases; frequency is unknown.

    From the immune system: rarely - allergic reactions (skin rash, shortness of breath, anaphylactic shock, Quincke's edema).

    From the nervous system: very rarely - dizziness, headache, agitation, confusion.

    From the heart: very rarely - tachycardia; in some cases, bradycardia, arrhythmia; frequency unknown - pain in the region of the heart

    From the side of the vessels: frequency unknown - redness of the face and upper half of the trunk with a sensation of tingling and burning, "hot flashes".

    From the gastrointestinal tract: very rarely - vomiting, diarrhea.

    From the skin and subcutaneous tissues: very rarely - increased sweating, acne, itching, urticaria.

    From the osteomuscular and connective tissue: very rarely - cramps.

    General disorders and disorders at the site of administration: very rarely - there may be irritation, pain and burning at the injection site, weakness.

    If any of these unwanted reactions worsen or any other unwanted reactions appear that are not listed in the instructions, you should notify the doctor.

    With the development of severe undesirable reactions, the drug is canceled.
    Overdose:

    The components of the drug KOKARNIT have a wide therapeutic range.

    Overdose Symptoms

    Trifosadenin: exceeding the maximum daily dose (about 600 mg for an adult) can lead to the development of the following symptoms: dizziness, lowering of arterial pressure, short-term loss of consciousness, arrhythmia, atrioventricular block of II and III degree, asystole, bronchospasm, ventricular disorders, sinus bradycardia and tachycardia .

    Cocarboxylase: the following symptoms are reported after administration of a dose that exceeds the recommended dose by more than 100 times: muscle spasm, muscle weakness, paralysis, arrhythmia.

    Cyanocobalamin: after parenteral administration of a high dose, eczematous skin disorders and a benign form of acne were observed. When used in high doses, it is possible to develop hypercoagulation, violation of purine metabolism.

    Nicotinamide: when using large doses, hyperpigmentation, jaundice, amblyopia, weakness, exacerbation of peptic ulcer of the stomach and duodenum were observed. With long-term use, development of steatohepatosis, increased concentration of uric acid in the blood, violation of glucose tolerance were noted.

    Treatment

    The drug is immediately discontinued, symptomatic therapy, including desensitizing therapy, is prescribed.

    Interaction:

    In patients using the hypoglycemic agents of the biguanide group (metformin), due to a violation of absorption of cyanocobalamin from the gastrointestinal tract, a decrease in the concentration of cyanocobalamin in the blood can be observed. With other hypoglycemic agents, drug interactions are not described.

    Cyanocobalamin is incompatible with ascorbic acid, heavy metal salts, thiamine, thiamine bromide, pyridoxine, riboflavin, folic acid.

    Can not be used simultaneously cyanocobalamin with drugs that increase blood coagulability.

    In addition, simultaneous use of cyanocobalamin with chloramphenicol should be avoided.

    Aminoglycosides, salicylates, antiepileptic drugs, colchicine, potassium preparations reduce the absorption of cyanocobalamin.

    When combined use of drugs containing trifosadenine, with dipyridamole, the action of dipyridamole is enhanced, in particular the vasodilating effect.

    Dipyridamole enhances the effect of trifosadenin.

    There is some antagonism in the joint use of the drug with purine derivatives (caffeine, theophylline).

    Do not administer simultaneously with cardiac glycosides in large doses, as the risk of developing adverse reactions from the cardiovascular system increases.

    With simultaneous application of xanthinal nicotinate, the effect of the drug is reduced.

    Nicotinamide potentiates the action of sedatives, tranquilizers, as well as antihypertensive drugs.

    Special instructions:

    With aggravation of the symptoms of the disease or lack of effect after 9 days, correction of the course of treatment is necessary.

    When using the drug KOKARNIT needed proper selection of a dose of hypoglycemic drug and adequate control of the course of diabetes.

    The color of the prepared solution should be pink.

    Do not use the drug if the color of the solution has changed.

    The solution should be applied immediately after its preparation!

    Effect on the ability to drive transp. cf. and fur:

    If there are side effects from the central nervous system (dizziness, confusion), it is recommended to refrain from controlling vehicles and other mechanisms.

    Form release / dosage:

    Lyophilizate for the preparation of solution for intramuscular injection / complete with a solvent.

    Packaging:

    By 187,125 mg of the drug in ampoules of dark glass with one or two fracture rings with a volume of 3 ml.

    For 2 ml of solvent (0.5% solution of lidocaine hydrochloride) in ampoules of dark glass with a breakdown ring of 2 ml.

    3 ampoules with the preparation complete with 3 ampoules of the solvent in the contour cell package.

    1, or 3, or 4, or 5 contour squares with instructions for use are put in a cardboard box.

    Storage conditions:

    In the dark place at a temperature of 15 to 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    Preparation: 3 years.

    Solvent: 4 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002839
    Date of registration:23.01.2015 / 14.03.2016
    Expiration Date:23.01.2020
    The owner of the registration certificate:World Medical Co., Ltd.World Medical Co., Ltd. Egypt
    Representation: & nbspTROKAS PHARMA LLCTROKAS PHARMA LLCRussia
    Information update date: & nbsp30.01.2018
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