Heparin

Heparin – anticoagulant of direct action.

Form of release and structure

Dosage forms of drug:

• Solution for intravenous (in/in) and hypodermic (п / to) introductions: light yellow or colourless transparent liquid (a bottle (bottle) of 1 ml on 5 or 10 pieces in planimetric strip or plastic (pallets) packaging, in a cardboard pack 1 or 2 packagings; on 5 or 10 pieces in a pack cardboard unpacked. An ampoule of 1 ml with an ampoule knife on 5 or 10 pieces in planimetric strip or plastic (pallets) packaging, in a cardboard pack 1 or 2 packagings; on 5 or 10 pieces in a pack cardboard unpacked. An ampoule of 2 ml with an ampoule knife, on 5 pieces in a blister strip packaging, in a pack cardboard 1 or 2 packagings. An ampoule of 5 ml with an ampoule knife, on 5 or 10 pieces in planimetric strip or plastic (pallets) packaging, in a pack cardboard 1 or 2 packagings. An ampoule of 5 ml with an ampoule knife, 5 or 10 pieces in a pack cardboard. An ampoule of 5 ml, 5 or 10 pieces in a pack cardboard. Bottle (bottle) of 5 ml, on 5 or 10 pieces in planimetric strip or plastic packaging (pallets), in a pack cardboard 1 or 2 packagings. A bottle (bottle) of 5 ml, 1, 5 or 10 pieces in a pack cardboard. An ampoule of polymeric 5 ml, on 5 pieces in a pack cardboard. A bottle (bottle) of 5 ml, on 5 pieces in a container polystyrene);
• Ointment for external use (on 10 or 25 g in tubas aluminum, in a cardboard pack 1 tuba);
• Gel for external use (on 15, 20, 30, 50 or 100 g in tubas aluminum, in a cardboard pack 1 tuba).

Active ingredient – heparin sodium:

• 1 ml of solution – 5000 ME;
• 1 g of ointment – 100 ME;
• 1 g of gel – 1000 ME.

Auxiliary components:

• Solution: sodium chloride – 3,4 mg, benzyl alcohol – 9 mg, water for injections to 1 ml;
• Ointment: benzocaine – 40 mg, бензилникотинат – 0,8 mg.

Indications to use

• Therapy and prevention: thrombophlebitises, a thrombembolia of a pulmonary artery (including in case of diseases of peripheral veins), a deep vein thrombosis, thrombosis of coronary arteries, unstable stenocardia, an acute myocardial infarction, a ciliary arrhythmia (including followed by an embolism), a syndrome of the disseminated intravascular coagulation (DIC), disturbance of microcirculation and a microthrombogenesis, fibrinferments of renal veins, a gemolitikouremichesky syndrome, a bacterial endocarditis, a glomerulonephritis, lupoid nephrite;
• Prevention: a blood coagulation during operations in which extracorporal methods of blood circulation, mitral heart disease, a hemodialysis, peritoneal dialysis, hemosorption, an artificial diuresis, a cytapheresis are used;
• Washing of venous catheters;
• Preparation of samples of not turning blood for the laboratory purposes and hemotransfusion.

Contraindications

Contraindications to use of Heparin in the form of solution:

• The heparin-induced thrombocytopenia in the anamnesis or now, with thrombosis or without it;
• Pregnancy and period of breastfeeding;
• Bleeding if the potential risk exceeds estimated advantage of use.

With care appoint solution at the morbid conditions interfaced to the increased risk of bleedings:

• Craniocereberal injury, hemorrhagic stroke;
• Malignant new growths;
• Cardiovascular system: aneurism of vessels of a brain, acute and subacute infectious endocarditis, heavy uncontrollable arterial hypertension, stratifying of an aorta;
• Bodies of lymphatic system and hemopoiesis: hemorrhagic diathesis, leukosis, hemophilia, thrombocytopenia;
• Ulcer colitis, erosive cankers of bodies of the digestive tract (DT), gullet varicosity, long use of gastric and enteric drainages, hemorrhoids;
• Inborn deficit of synthesis of antithrombin III and replacement therapy by antithrombin III drugs (for reduction of risk of bleedings it is necessary to use small doses of drug).

Other physiological states and pathologies at which it is necessary to apply solution Heparin with care: chronic renal failure; a serious illness of a liver with disturbance of proteinaceous and synthetic function; vasculites; proliferative diabetic retinopathy; recent surgical interventions on back or a brain, eyes; early puerperal period; recently carried out epidural anesthesia or a lumbar puncture; the menacing abortion; periods period.

Under fixed observation of the doctor it is recommended to use solution at treatment of children under 3 years and patients 60 years, especially are more senior than women.

Contraindications to use of ointment and gel:

• The diseases which are followed by disturbance of processes of a blood coagulation, bleeding, an aneurysm of vessels of a brain, the assumption of intracraneal hemorrhage, a hemorrhagic stroke, the stratifying aortic aneurysm, malignant arterial hypertension, a subacute bacterial endocarditis, an anti-phospholipidic syndrome;
• GIT erosive cankers, malignant new growths in a liver, severe defeats of a parenchyma of a liver, cirrhosis with a gullet varicosity, depressed cases;
• The recovery period after surgical intervention on a liver and bilious ways, a brain, eyes, a prostate gland, a puncture of a spinal cord;
• Recent childbirth, periods, the menacing abortion.

Ointment and gel cannot be applied at ulcer and necrotic processes, on mucous membranes or open wounds.

Putting ointment or gel at pregnancy and during breastfeeding (lactation) is possible under careful medical observation, only according to strict indications.

Use of all dosage forms of Heparin is contraindicated to patients with hypersensitivity to drug components.

Route of administration and dosage

Solution is entered intravenously kapelno or bolyusno and subcutaneously into the area of a stomach. It is impossible to administer the drug intramusculary! Dosing is appointed by the doctor on the basis of clinical indications and taking into account age of the patient. Usually treatment is begun with intravenous administration 5000 ME, then passed to subcutaneous injections or drop intravenous administration.

The supporting dosing depending on a solution route of administration:

• Continuous intravenous infusion – 24000-48000 ME in days with a speed of 1000-2000 ME an hour;
• Regular intravenous injections – 5000-10000 ME with an interval of 4-6 hours;
• Subcutaneous injections – 15000-20000 ME 2 time or on 8000-10000 ME – 3 times a day.

For infusional introduction drug is dissolved by 0,9% with chloride sodium solution. Correction of each subsequent dose is made on the basis of regular researches of the activated partial tromboplastinovy time (APTT) and/or a blood clotting time. At hypodermic introduction 10000-15000 ME in days regular control of AChTV is not obligatory.

The period of treatment depends on a way of introduction and indications. Intravenously drug is used within 7-10 days, then treatment should be continued by peroral anticoagulants. It is recommended to appoint peroral anticoagulants from the first or from 5 to 7 days of treatment, cancellation of solution is appointed to 4-5 day of the combined treatment.

Use of Heparin at special clinical situations is made according to the special scheme.

Ointment and gel apply depending on clinical testimonies and age of the patient.

Side effects

• From coagulant system of blood: thrombocytopenia in a passing and severe form, in rare instances with a lethal outcome, can cause development of a necrosis of skin, arterial thrombosis, gangrene, stroke, myocardial infarction; hemorrhagic complications in the form of bleeding of a GIT or urinary tract, retroperitoneal hemorrhages in ovaries, adrenal glands with risk of development of acute adrenal insufficiency;
• From bodies of a GIT: nausea, vomiting, diarrhea, a loss of appetite, increase in level of transaminases in blood;
• From a musculoskeletal system: in case of prolonged use – calcification of soft tissues, osteoporosis and spontaneous fractures;
• Allergic reactions: urticaria, skin itch, dermahemia, bronchospasm, rhinitis, medicinal fever, anaphylactoid reactions, acute anaphylaxis;
• Local reactions: pain, a hematoma, bleeding, a hyperemia or ulcerations in an injection site;
• Others: oppression of synthesis of Aldosteronum, passing alopecia.

Special instructions

Prolonged treatment by high doses is recommended to be carried out in stationary conditions.

Use of solution has to take place taking into account blood coagulation indicators, in case of sharp decrease in quantity of thrombocytes it is necessary to cancel drug use immediately.

In case of purpose of drug in high doses or in the absence of reaction to Heparin it is necessary to control antithrombin III level.

Administration of other medicines in oil against the background of drug solution use is not recommended.

At patients with arterial hypertension treatment should be accompanied with regular control of arterial pressure.

With care patients should use drug at radiation therapy, dental manipulations, active tuberculosis, in the presence of an intrauterine contraceptive.

At treatment of women 60 years use of heparin sodium are more senior can increase bleeding therefore this category of patients should reduce a solution dose.

Adequate dosing, regular control of a blood coagulation and careful assessment of contraindications reduce risk of bleeding.

Medicinal interaction

Solution of Heparin is compatible only from 0,9% chloride sodium solution.

Heparin sodium strengthens effect of the drugs containing benzodiazepine derivatives, Phenytoinum, propranolol, quinidine.

Activity of drug tricyclic antidepressants, protamin reduce sulfates, polypeptides.

Anticoagulating effect of drug strengthens simultaneous use of thrombolytic means (an alteplaza, an urokinase, Streptokinasa), antiagregant (acetylsalicylic acid, Dipiridamolum, klopidogret, тиклопидин, prasugret), anticoagulants of indirect action (warfarin, аценокумарол, Fenindionum), non-steroidal anti-inflammatory drugs (NPVS).

The risk of bleedings increases simultaneous use of Heparin with a dextran, glucocorticosteroids, cytostatics, hydroxychloroquine, tsefamandoly, valproyevy and Acidum etacrynicum, propylthiouracil.

Anticoagulating effect of drug reduces a concomitant use of corticotropin, ascorbic acid, nitroglycerine, alkaloids of an ergot, quinine, nicotine, tetracycline, cardiac glycosides, antihistamines or thyroxine.

Drug can reduce action of glucocorticosteroids, adrenocorticotropic hormone, insulin.

Terms and storage conditions

To store in the unavailable to children, dry, protected from light place at a temperature: solution and gel – is not above 25 °C; ointment – to 20 °C.

Period of validity: solution, ointment – 3 years; gel – 2 years.