The drug is a rationally selected complex metabolic substances and vitamins. Trifosadenin is derived adenosine stimulates metabolic processes. It has vasodilating effects, including coronary and cerebral arteries.
It improves metabolism and energy supply of tissues. It possesses antihypertensive and antiarrhythmic action. Under the influence of ATP occurs lowering blood pressure, relaxing smooth muscle, improved conduction of nerve impulses. Cocarboxylase – coenzyme formed in the body from entering from the outside of thiamine (vitamin B1).
Included in the enzyme carboxylase catalyzes the carboxylation and decarboxylation of α-keto acids. Indirectly promotes the synthesis of nucleic acids, proteins and lipids. Decreases in the organism concentration of lactic and pyruvic acids, promotes the absorption of glucose. Improves trophic nervous tissue.
Cyanocobalamin (vitamin B12) in the body is transformed into methylcobalamin and 5-dezoksiadenozilkobalamin. Methylcobalamin is involved in the conversion reaction gomotsisteinav methionine and S-adenosylmethionine – key metabolic reactions pyrimidine and purine bases (and hence DNA and RNA). When vitamin deficiency in this reaction it may replace metiltetragidrofolievaya acid, wherein the reaction folievopotrebnye disturbed metabolism.
5-dezoksiadenozilkobalamin serves as a cofactor for the isomerization L- methylmalonyl-CoA to succinyl-CoA – important reaction carbohydrate and lipid metabolism. Deficiency of vitamin B12 leads to disruption of proliferation of rapidly dividing cells of hematopoietic tissue and epithelium, as well as to disruption of neuronal myelin sheath formation. Nikotinamid- one form of vitamin PP, is involved in redox processes in the cell, improves carbohydrate and nitrogen metabolism, regulates tissue respiration.
After parenteral administration Trifosadenin penetrates the cell bodies, wherein splits into adenosine and inorganic phosphate with the release of energy. Subsequently decomposition products are included in the resynthesis of ATP. Kokarboksilaza Rapidly absorbed following intramuscular injection. Penetrates into most tissues of the body. Undergoes metabolic degradation. The metabolic products are derived primarily by the kidneys.
Blood cyanocobalamin binds to transcobalamin I and II, which transports it to the fabric. Deposited mainly in the liver. Communication with plasma proteins 0 to 90%. Quickly and completely absorbed after intramuscular or subcutaneous injection. The maximum concentration after administration vnutriyshechnogo achieved after 1 hour. From the output liver bile into the intestine and again absorbed into the blood. The half-life – 500 days. Displayed with normal renal function – 7-10% kidneys, about 50% – intestine. With reduced renal function – 0-7% kidneys, 70-100% – intestine. Crosses the placental barrier, breast moloko.4
Rapidly distributed into all tissues. It crosses the placental barrier and into breast milk. It is metabolized in the liver to form the nicotinamide-N-methylnicotinamide. Excreted by the kidneys. Plasma half-life is approximately 1.3 hours, a fixed volume of distribution – about 60 liters, total clearance – about 0.6 L / min.
E.I.P.I.Ko EG, Egypt
Each vial of the drug contains:
trifosadenina disodium trihydrate – 10.0 mg
cocarboxylase – 50.0 mg
cyanocobalamin – 0.5 mg
nicotinamide – 20.0 mg;
glycine – 105.875 mg,
methyl parahydroxybenzoate – 0.6 mg
propyl parahydroxybenzoate – 0.15 mg.
Each solvent ampoule contains:
Lidocaine hydrochloride – 10 mg,
Water for injection – up to 2 ml
Symptomatic treatment of diabetic polyneuropathy.
- Hypersensitivity to any component of the drug or the solvent;
- cardiovascular diseases: acute heart failure, acute myocardial infarction, uncontrolled hypertension, hypotension, severe bradyarrhythmias, AV-block II-III degree, chronic heart failure (?. III IVst of NYHA), cardiogenic shock and other types of shocks, QT prolongation syndrome, thromboembolism, hemorrhagic stroke;
- inflammatory lung disease, chronic obstructive pulmonary disease, bronchial asthma;
- pregnancy, breast-feeding;
- Children under 18 years of age;
- hypercoagulation (including acute thrombosis) erythremia, erythrocytosis;
- gastric ulcer or duodenal ulcer in the acute stage;
- hepatitis, cirrhosis of the liver.
Precautions should be used drug for angina pectoris.
The incidence of adverse reactions is given in accordance with the WHO classifications: very often (1/10); often (less than 1/10, but more 1/100); infrequently (less than 1/100 but more 1/1000); rare (less than 1/1000, but more than 1/10000); very rare (less than 1/10000) including individual cases; frequency is unknown.
Immune system: rare – allergic reactions (skin rash, shortness of breath, anaphylaxis, angioedema).
Co nervous system: very rarely – dizziness, headache, agitation, confusion.
Co side of the heart: it is very rare-tachycardia; in some cases, bradycardia, arrhythmia; the frequency is unknown – pain in the heart.
From the side of blood vessels: the frequency is unknown – redness of the skin of the face and upper body with a feeling of tingling and burning, “hot flashes.”
Co gastrointestinal tract: rarely – vomiting, diarrhea.
Co Skin and subcutaneous tissue disorders: very rarely – increased sweating, acne, pruritus, urticaria.
Co Musculoskeletal and connective tissue disorders: very rarely – seizures.
General disorders and at the injection site: very rare – it may be irritation, pain and a burning sensation at the site of injection, weakness.
If any of these adverse reactions were aggravated or any other adverse reaction not mentioned in the instructions, you should inform your doctor.
If severe adverse reactions, medication overturned.
How to accept, acceptance rate and dosage
The drug is administered by deep intramuscular (into the gluteal muscle). In cases of severe pain syndrome treatment is advisable to start with intramuscular administration of 1 ampoule (2 ml) per day to relieve acute symptoms.
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 3-9 injections depending on the severity of the disease. The duration of treatment and repeat courses determined by the doctor depending on the nature and severity of the disease.
Use in children The efficacy and safety of the drug Kokarnit have no children.
In the dark place at a temperature of 15 to 25ºC. Keep out of the reach of children.
Trifosadenin, kokarboksilazu, cyanocobalamin, nicotinamide
In patients treated with hypoglycaemic agents group biguanide (metformin), due to malabsorption of cyanocobalamin from the gastrointestinal tract reducing the concentration of cyanocobalamin in the blood can be observed. With other drug interactions hypoglycemic agents are not described.
Cyanocobalamin is not compatible with the ascorbic acid, salts of heavy metals, bromide thiamine, pyridoxine, riboflavin, folic acid. Can not be used simultaneously with cyanocobalamin medications that increase blood clotting. Furthermore, it should avoid the simultaneous use of cyanocobalamin with chloramphenicol.
Aminoglycosides, salicylates, protivoeptilepticheskie drugs, colchicine, potassium drugs reduce the absorption of cyanocobalamin.
When the joint application of preparations containing trifosadenin, dipyridamole dipyridamole enhanced action, in particular vasodilating action. Dipyridamole enhances trifosadenina effect.
It exhibits some antagonism when used in conjunction with the preparation of purine derivatives (caffeine, theophylline).
Should not be administered simultaneously with cardiac glycosides in large doses as enhanced risk of adverse reactions on the part of the cardiovascular system.
In an application with xantinol nicotinate reduced drug effect.
Nicotinamide potentiates the effect of sedatives, tranquilizers, and antihypertensives
When aggravation of symptoms or no effect after 9 days you need a course correction treatment.
In applying the drug KOKARNIT requires the proper selection of a hypoglycemic medicament doses and adequate control of diabetes mellitus.
Color of the prepared solution must be pink.
You can not use the drug if the color of the solution changed.
The solution should be used immediately after its preparation!
The effect on the ability to operate vehicles, machinery
At occurrence of side effects on the central nervous system (dizziness, confusion) to refrain from driving vehicles and other machinery