Description of the drug HEPARIN
Direct anticoagulant, belongs to the group of medium molecular heparins. In blood plasma, it activates antithrombin III, accelerating its anticoagulant effect. It disrupts the transition of prothrombin to thrombin, inhibits the activity of thrombin and activated factor X, and to some extent reduces platelet aggregation.
For unfractionated standard heparin, the ratio of antiplatelet activity (antifactor Xa) and anticoagulant activity (APTT) is 1:
- 1.
Increases renal blood flow; increases cerebral vascular resistance, reduces the activity of cerebral hyaluronidase, activates lipoprotein lipase and has a hypolipidemic effect. Reduces the activity of surfactant in the lungs, suppresses excessive synthesis of aldosterone in the adrenal cortex, binds adrenaline, modulates the ovarian response to hormonal stimuli, and increases the activity of parathyroid hormone. As a result of interaction with enzymes, it can increase the activity of brain tyrosine hydroxylase, pepsinogen, DNA polymerase and reduce the activity of myosin ATPase, pyruvate kinase, RNA polymerase, pepsin.
There is evidence that heparin has immunosuppressive activity.
In patients with coronary artery disease (in combination with ASA), it reduces the risk of acute coronary artery thrombosis, myocardial infarction and sudden death. Reduces the frequency of recurrent infarctions and mortality in patients who have had myocardial infarction. In high doses it is effective for pulmonary embolism and venous thrombosis, in small doses it is effective for the prevention of venous thromboembolism, incl. after surgical operations.
With intravenous administration, blood coagulation slows down almost immediately, with intramuscular injection - after 15-30 minutes, with subcutaneous administration - after 20-60 minutes, after inhalation the maximum effect is within 24 hours; the duration of the anticoagulant effect is respectively 4-5, 6, 8 hours and 1-2 weeks, the therapeutic effect - prevention of thrombus formation - lasts much longer. Deficiency of antithrombin III in plasma or at the site of thrombosis may reduce the antithrombotic effect of heparin.
When applied externally, it has a local antithrombotic, antiexudative, and moderate anti-inflammatory effect. Blocks the formation of thrombin, inhibits the activity of hyaluronidase, and activates the fibrinolytic properties of the blood. Heparin penetrating through the skin reduces the inflammatory process and has an antithrombotic effect, improves microcirculation and activates tissue metabolism, thereby accelerating the processes of resorption of hematomas and blood clots and reducing tissue swelling.
Compound
The injection solution contains sodium heparin at a concentration of 5 thousand units/ml.
The auxiliary components of the drug include sodium chloride, benzyl alcohol, and water. 1 gram of gel contains 1 thousand units of sodium heparin , as well as auxiliary components: 96% ethanol, carbomer , dimethyl sulfoxide, propylene glycol, dietanolamine, methyl and propylparaben (additives E 218, E 216), lavender oil and purified water.
Reviews
Heparin is an effective and well-studied antithrombotic agent , the mechanism of action of which is to suppress the activity of thrombin , which catalyzes the biotransformation of fibrinogen into fibrin and a number of other reactions in the hemostatic system.
Most often, the external use of gel and ointment forms of the drug is discussed on the Internet. Reviews of heparin-containing ointments and gels (in particular, reviews of Heparin Acrigel 1000 ) are overwhelmingly positive: such drugs really help with bruises, thrombophlebitis and hemorrhoids , and also remove localized infiltrates well.
Contraindications
Heparin containing ointments (Heparin, Heparin-Acrigel 1000, etc.) are contraindicated in cases of hypersensitivity to the components they contain, as well as in diseases accompanied by ulcerative-necrotic processes, and injuries that are accompanied by violations of the integrity of the skin.
Heparin gel (ointment) should be used with caution in case of thrombocytopenia and increased tendency to bleeding.
Contraindications to the use of the injection form of the drug:
- hypersensitivity;
- diseases accompanied by increased bleeding ( vasculitis, hemophilia , etc.);
- bleeding;
- aortic dissection , intracranial aneurysm;
- antiphospholipid syndrome;
- traumatic brain injury;
- hemorrhagic stroke;
- uncontrolled hypertension;
- liver cirrhosis , accompanied by pathological changes in the veins of the esophagus;
- threatened miscarriage;
- menstrual period;
- pregnancy;
- childbirth (including recent);
- lactation period;
- erosive and ulcerative lesions of the stomach and intestinal tract;
- recent surgical interventions on the prostate gland, brain, eyes, bile ducts and liver, as well as the condition after lumbar puncture .
Heparin injections should be prescribed with caution to patients with polyvalent allergies (including bronchial asthma ), diabetes mellitus , arterial hypertension , active tuberculosis , endo- and pericarditis , chronic renal failure, liver failure ; patients undergoing dental procedures or radiation therapy; persons over 60 years of age (especially women); women using an IUD.
Overdose
Symptoms of overdose with parenteral use are bleeding of varying severity.
Treatment: for minor bleeding caused by an overdose of the drug, it is enough to stop using it. If bleeding is extensive, protamine sulfate (1 mg per 100 IU of heparin) is used to neutralize excess heparin.
Please note that heparin is eliminated quickly. Thus, if protamine sulfate is administered 30 minutes after the previous dose of heparin, it should be administered at half the dose; The highest dose of protamine sulfate is 50 mg.
It is not excreted by hemodialysis.
Cases of overdose with external use of the drug have not been described. Due to the low systemic absorption of the drug, an overdose is considered unlikely. With prolonged use on large surfaces, hemorrhagic complications .
Treatment: discontinuation of the drug, if necessary, use of a one percent solution of protamine sulfate (heparin antagonist).
Analogs
Level 4 ATC code matches:
Girudoproct
Heparoid Zentiva
Heparin ointment
Gepatrombin G
Lyoton
Trombless
Venolife
Hepatrombin
Gel analogues: Heparin-Acrigel 1000 , Lyoton 1000 , Lavenum , Trombless .
Generic injection forms: Heparin J , Heparin-Ferein , Heparin-Sandoz .
Drugs with a similar mechanism of action: tablets - Piyavit , Angioflux , Wessel Due F ; solution - Angioflux , Hemapaxan , Antithrombin III human , Wessel Due F , Fluxum , Anfibra , Fraxiparine , Enixum .
Instructions for use of Heparin (Method and dosage)
Heparin injections, instructions for use, administration features
Heparin in ampoules is prescribed in the form of:
- regular injections into a vein;
- continuous infusion;
- subcutaneously (injections in the stomach).
For preventive purposes, sodium heparin is administered subcutaneously at a dose of 5 thousand IU/day, leaving 8-12 hours between injections (to prevent thrombosis, the patient is injected with 1 ml of solution under the skin of the abdomen 2 times/day).
For medicinal purposes, the solution is infused intravenously (the method of administration is drip infusion). Dose - 15 IU/kg/h (that is, an adult with average body weight is prescribed 1 thousand IU/h).
To achieve a rapid anticoagulant effect, 1 ml of solution is injected intravenously into the patient immediately before infusion. If administration into a vein is impossible for some reason, then the medicine is injected under the skin 4 times a day. 2 ml.
The highest daily dose is 60-80 thousand IU. The use of Heparin at the indicated dose for more than 10 days is permitted only in exceptional cases.
For children, the solution is injected into a vein by drip. The dose is selected depending on age: at the age of 1 to 3 months the daily dose is 800 IU/kg, from 4 months to a year - 700 IU/kg, children over 6 years of age are prescribed (under APTT monitoring) 500 IU/kg/ days
Technique for administering Heparin, preparation for manipulation and administration of solution
Subcutaneous injections are usually given into the anterolateral wall of the abdomen (if this is not possible, the medicine can be injected into the upper thigh/shoulder area).
A thin needle is used for injection.
The first injection is given 1-2 hours before the start of the operation; in the postoperative period, the drug continues to be administered for 7-10 days (if necessary, longer).
Treatment begins with a jet injection of 5 thousand IU of heparin into a vein, after which the solution is continued to be administered using an intravenous infusion (a 0.9% NaCl solution is used to dilute the drug).
Maintenance doses are calculated depending on the route of administration.
The algorithm for administering Heparin is as follows:
- 15-20 minutes before administering the drug, apply cold to the injection site in the abdominal area (this will reduce the likelihood of bruising).
- The procedure is performed in compliance with the rules of asepsis.
- The needle is inserted into the base of the fold (the fold is held between the thumb and forefinger until the end of drug administration) at an angle of 90°.
- Do not move the tip of the needle after insertion or retract the piston. Otherwise, tissue damage and hematoma formation may occur.
- The solution should be injected slowly (to reduce pain and avoid tissue damage).
- The needle is removed easily, at the same angle at which it was inserted.
- There is no need to wipe the skin; the injection site is lightly pressed with a sterile dry swab (the swab is held for 30-60 seconds).
- It is recommended to alternate anatomical sites for injection. The areas in which injections are given during the week should be 2.5 cm apart from each other.
Heparin ointment, instructions for use
The gel is used as an external agent. It should be applied to the affected area from 1 to 3 times a day. A single dose is a column 3 to 10 cm long.
For thrombosis of hemorrhoidal veins, the drug is used rectally.
Gel-impregnated cotton pads are applied to the inflamed nodes and secured with a bandage. Gel-soaked tampons are inserted into the anus. Treatment usually lasts 3-4 days.
For leg ulcers, the ointment is carefully applied to the inflamed skin around the ulcer.
Frequency of applications - 2-3 rubles/day. Treatment is continued until the inflammation disappears. Usually the course lasts from 3 to 7 days. The doctor decides whether a longer course is necessary.
Other heparin-containing ointments are used in a similar way (for example, the instructions for Heparin-Acrigel 1000 are practically no different from the instructions for Heparin gel or Lyoton 1000 ).
For the treatment of hemorrhoids (external and internal), anal fissures , thrombophlebitis of the anal veins , as well as to relieve itching and eliminate eczema suppositories for hemorrhoids (for example, Hepatrombin G can be used as an alternative to Heparin ointment .
Additional Information
Heparin is available only in the form of a solution, ointment or gel (gel, unlike ointment, contains a larger amount of the active substance and is better absorbed into the skin).
Heparin tablets are not available because heparin is practically not absorbed from the digestive tract.
Use during pregnancy and lactation
Heparin solution is not contraindicated for pregnant women. However, despite the fact that the active substance of the drug does not penetrate into milk, its use in nursing mothers in some cases led to the rapid (within 2-4 weeks) development of osteoporosis and spinal damage.
The feasibility of use should be decided individually, taking into account the risk to the fetus/benefit to the mother ratio.
There are no data on the use of the gel during pregnancy and lactation.
