Heparin

Гепарин Drug photo

The description is actual on 04.08.2016

  • Latin name: Heparin
  • ATH code: C05BA03
  • Active ingredient: Heparin sodium (Heparin sodium)
  • Producer: Synthesis of joint stock company, Murom instrument-making plant, Tatkhimfarmpreparata, Mikrogen NPO Federal State Unitary Enterprise, Armavir biofactory, Slavic drugstore of FC of Ltd company, Moscow endocrine plant (Russia), Belmedpreparata of RUP (Republic of Belarus)

Structure

Solution for injections contains heparin sodium in concentration of 5 thousand. Piece/ml. As auxiliary components sodium chloride, benzyl alcohol, water are a part of drug for and.

1 gram of gel contains 1 thousand. Heparin sodium piece, and also auxiliary components: 96% ethanol, carbomer, a dimethyl sulfoxide, propylene glycol, diethanol amide, methyl - and propylparaben (additives E 218, E 216), oil of a lavender and the purified water.

Release form

  • Gel for external use of 1 thousand. Piece/g (the ATH code — C05BA03). Tubas of 30 g.
  • Solution for and 5 thousand. Piece/ml on 1 and 2 ml in ampoules No. 10, on 2 and 5 ml in ampoules No. 5, on 5 ml in bottles No. 1 and No. 5.

Pharmacological action

Pharmacological group: anticoagulants.

Group of the drug Heparin which is let out in the form of gel: means for treatment of diseases of CCC.

Group of the drug Heparin which is let out in an injection form: the means influencing blood and a hemopoiesis.

Contained in the drug Heparin sodium has antitrombotichesky effect, slows down aggregation and adhesion of leukocytes, thrombocytes and erythrocytes; reduces a spasm of a wall and degree of permeability of vessels; promotes improvement of collateral circulation.

Pharmacodynamics and pharmacokinetics

What is Heparin?

Heparin (MNN: Heparin) is an acid mucopolysaccharide with Mr about 16 kd. The anticoagulant of direct action promoting delay of formation of fibrin.

Gross - a heparin formula — C12H19NO20S3.

Pharmacodynamics

The mechanism of effect of heparin is based first of all on its linkng with AT III (the plasma cofactor). Being physiological anticoagulant, it potentsiirut ability of AT III to suppress the activated coagulation factors (in particular, IHa, Ha, of HIA, HIIA).

In case of use in high concentration heparin also suppresses activity of thrombin.

Suppresses the activated factor of X which participates in internal and in external system of a blood coagulation.

Action is shown when using considerably of smaller doses of heparin, than it is required for inhibition of activity of a coagulative factor of II (thrombin) which promotes formation of fibrin from plasma protein of fibrinogen.

It is justification of a possibility of use of small doses of heparin (subcutaneously) in the preventive purposes, and big — for treatment.

Heparin is not fibrinolitiky (i.e. it is capable to dissolve blood clots), however can reduce the sizes of blood clot and stop its increase. Thus, blood clot is partially dissolved under the influence of fibrinolitic enzymes of a natural origin.

Suppresses activity of enzyme of hyaluronidase, promotes reduction of activity of surfactant in lungs.

Reduces risk of development by IT, acute thromboses of arteries of a myocardium and sudden death. In small doses it is effective for prevention of VTE, in high — at venous thrombosis and embolisms of pulmonary vessels.

Deficit of AT III in the place of thrombosis or plasma can reduce expressiveness of antitrombotichesky effect of drug

At external use means renders local antiexudative, antitrombotichesky and moderate antiinflammatory action.

Promotes activation of fibrinolitic properties of blood, inhibits activity of hyaluronidase, blocks formation of thrombin. Being gradually released from gel and passing through skin, heparin promotes reduction of an inflammation and has antitrombotichesky effect.

At the same time at the patient microcirculation improves and the exchange is activated fabric and, as a result of it, processes of a rassasyvaniye of blood clots and hematomas accelerate, and also puffiness of fabrics decreases.

Pharmacokinetics

At external use absorption is insignificant.

After introduction under TCmax skin — 4-5 hours. To 95% of substance there is in the state connected with plasma proteins, Vp — 0.06 l/kg (substance does not leave a vascular bed because of strong linkng with plasma proteins).

Through a placental barrier and does not get into breast milk.

It is metabolized in a liver. Substance is characterized by a fast biological inactivation and short duration of action that is explained by participation in its biotransformation of an anti-heparin factor and linkng of heparin with system of macrophages.

T1/2 — 30-60 minutes. It is allocated with kidneys. In not changed look to 50% of substance it can be removed only in case of use of high doses. By means of a hemodialysis it is not removed.

Indications to use

Indications to gel use

Gel Heparin is applied to treatment and prevention of thrombophlebitis of superficial veins, phlebitis (post-injection and post-infusional), a lymphangitis, a superficial periphlebitis, elephantiasis, the localized infiltrates, bruises, hypostases and injuries (including muscles, joints, sinews), superficial mastitis, hypodermic hematomas.

Indications to solution use

Pricks of Heparin are appointed at a deep vein thrombosis, arteries of a myocardium, renal veins, TELA, thrombophlebitis, a ciliary arrhythmia (including if disturbance of a cordial rhythm is followed by embolization), unstable stenocardia, the IDCS, acute by IT, mitral heart disease (prevention of formation of blood clots), a bacterial endocarditis, a gemolitikouremichesky syndrome, lupoid nephrite, a glomerulonephritis, for prevention and treatment of a microthrombogenesis and disturbances of microcirculation.

In the preventive purposes drug is used during surgical interventions at which extracorporal methods of blood circulation are used, when carrying out a cytapheresis, peritoneal dialysis, hemodialysis, artificial diuresis, hemosorption, when washing venous catheters.

At administration of Heparin in/in a blood coagulation it is slowed down almost at once, at introduction to a muscle — in 15-30 minutes, at introduction under skin — in 20-60 minutes, at an inhalation route of administration the effect is most expressed in a day.

Contraindications

Heparin the containing ointments (Heparin, Geparin-Akrigel 1000, etc.) are contraindicated at hypersensitivity to the components which are contained in them, and also at the diseases which are followed by ulcer and necrotic processes and injuries which are followed by disturbances of integrity of an integument.

With care gel (ointment) Heparin should be used at thrombocytopenia and the increased tendency to bleeding.

Contraindications to use of an injection form of drug:

  • hypersensitivity;
  • followed by the raised illness bleeding (a vasculitis, hemophilia and so forth);
  • bleeding;
  • stratification of an aorta, intracranial aneurism;
  • anti-phospholipidic syndrome;
  • craniocereberal injury;
  • hemorrhagic stroke;
  • uncontrollable AG;
  • the cirrhosis which is followed by pathological change of veins of a gullet;
  • the menacing abortion;
  • menstrual period;
  • pregnancy;
  • childbirth (including recent);
  • lactation period;
  • erosive cankers of a stomach and intestinal path;
  • the surgical interventions postponed in the recent past on a prostate gland, a brain, eyes, bilious ways and a liver, and also a state after a lumbar puncture.

With care patients should appoint Heparin injections with a polyvalent allergy (including bronchial asthma), a diabetes mellitus, arterial hypertension, active tuberculosis, endo-and a pericardis, HPN, a liver failure; to patients to whom carrying out stomatologic manipulations or radiation therapy is necessary; to persons 60 years are more senior (especially to women); to the women using VMK.

Side effects

At external use of Heparin sodium can cause a dermahemia and reactions of hypersensitivity.

At administration of solution are possible:

  • Hypersensitivity reactions (medicinal fever, an integument hyperemia, rhinitis, feeling of heat in soles, urticaria, a skin itch, a collapse, a bronchospasm, an acute anaphylaxis).
  • Headaches, dizziness, diarrhea, loss of appetite, nausea, vomiting;
  • Thrombocytopenia (approximately at 6% of patients), sometimes (seldom) — with a lethal outcome. The Heparin-induced Thrombocytopenia (HIT) is followed: arterial thrombosis, necrosis of skin and gangrene, stroke, myocardial infarction. In case of heavy GIT (when the quantity of thrombocytes decreases twice from initial number or lower than 100 thousand / mkl) administration of heparin should be stopped immediately.
  • Local reactions (a hematoma, a hyperemia, pain, an ulceration, irritation in an injection site, bleeding).
  • Bleedings. Are considered typical — from uric ways and a gastrointestinal tract, in areas which are exposed to pressure, in a drug injection site, from operational wounds. Hemorrhages in various internals are also possible: in retroperitoneal space, a yellow body, adrenal glands etc.

Against prolonged use of Heparin the coming alopecia, osteoporosis, a hypoaldosteronism develop, soft tissues kaltsifitsirutsya, there are spontaneous fractures of bones, activity of transaminases of a liver increases.

Application instruction of Heparin (Way and dosage)

Heparin pricks, application instruction, features of introduction

Heparin in ampoules is appointed in a look:

  • regular injections in a vein;
  • continuous infusion;
  • subcutaneously (pricks in a stomach).

In the preventive purposes heparin sodium is entered subcutaneously on 5 thousand ME/days, maintaining for 8-12 hours between injections (for the warning of thromboses to the patient of 2 rubles/days enter 1 ml of solution under stomach skin).

In the medical purposes pour in solution intravenously (an introduction method — drop infusion). A dose — 15 Me/kg/ch (that is to the adult with average body weight appoint 1 thousand. ME/h).

For achievement of fast anticoagulating effect to the patient in/in struyno enter 1 ml of solution just before infusion. If introduction to a vein for any reason is impossible, then medicine enter under skin 4 rubles/days on 2 ml.

The highest daily dose — 60-80 thousand ME. It is allowed to apply Heparin in the specified dose more than 10 days only in exceptional cases.

To children solution is entered into a vein kapelno. The dose is selected depending on age: aged from 1 till 3 months a daily dose — 800 ME/kg, from 4 months to one year — 700 ME/kg, to children are more senior than 6 years appoint (under control of AChTV) 500 Me/kg/sut.

Technology of administration of Heparin, preparation for manipulation and administration of solution

Hypodermic injections are given, as a rule, in an anterolateral wall of a stomach (if it is impossible, it is allowed to enter medicine into the upper area of a hip/shoulder).

For an injection use a fine needle.

The first injection is given in 1-2 hours prior to operation; in the postoperative period the drug continues to be administered within 7-10 days (if in it there is a need — longer).

Treatment begin with jet introduction to a vein 5 thousand ME of heparin then solution continues to be entered with use into infusions (for cultivation of medicine take NaCl solution of 0,9%).

Maintenance doses are calculated depending on a route of administration.

Algorithm of administration of Heparin following:

  • In 15-20 minutes prior to administration of drug to the place of a prick in a stomach put cold (it will allow to reduce probability of formation of bruises).
  • Procedure is carried out with observance of rules of an asepsis.
  • The needle is entered into the fold basis (a fold before the end of introduction of medicine hold between big and index fingers) at an angle 90 °.
  • To move a needle tip after introduction or to take away back the piston is impossible. Otherwise damage of fabrics and formation of hematomas is possible.
  • It is necessary to enter solution slowly (for decrease in pain and in order to avoid damage of fabrics).
  • The needle is removed easily, under the same corner under which it was entered.
  • It is not necessary to wipe skin, the place of an injection slightly and slightly press a sterile dry tampon (the tampon is held during 30-60 sec.).
  • It is recommended to alternate anatomic sites for injections. Sites in which within a week give injections have to be at distance of 2,5 cm from each other.

Ointment Heparin, application instruction

Gel is applied as outside means. It is necessary to apply it on an affected area to from 1 to 3 rubles/days. A single dose — a column from 3 to 10 cm long.

At fibrinferment of hemorrhoidal veins drug is used rektalno.

The laying impregnated with gel from cotton fabric imposes on the inflamed nodes and fixes a bandage. The tampons impregnated with gel enter into an anus. Treatment lasts usually 3-4 days.

At a shin ulcer ointment is carefully applied on the inflamed skin around an ulcer.

Frequency rate of uses — 2-3 rubles/day. Treatment is continued before disappearance of the inflammatory phenomena. Usually the course lasts from 3 to 7 days. The issue of need of carrying out longer course is resolved by the doctor.

Others heparin the containing ointments are applied similarly (so, for example, the instruction on Geparin-Akrigel practically does not differ 1000 from the instruction on gel Heparin or gel Lioton 1000).

For treatment of hemorrhoids (outside and internal), cracks of an anus, thrombophlebitis of veins of an anus, and also for removal of an itch and elimination of eczema in the field of an anus as an alternative of Unguentum Heparini can candles from hemorrhoids are used (for example, Gepatrombin).

Additional information

Heparin is issued only in the form of solution, ointment or gel (gel unlike ointment contains bigger amount of actively active ingredient and it is better absorbed in skin).

Tablets with heparin are not issued as heparin is practically not soaked up from a digestive tract.

Overdose

Overdose symptoms at parenteral use are bleedings of varying severity.

Treatment: at the small bleedings provoked by drug overdose it is enough to stop its use. If bleeding extensive, for neutralization of excess of heparin use protamin sulfate (1 mg on 100 ME heparins).

It is necessary to consider that heparin is removed quickly. Thus, if protamin sulfate is appointed in 30 minutes after the previous dose of heparin, it needs to be entered in a half dose; the highest dose of protamin of sulfate — 50 mg.

By means of a hemodialysis it is not removed.

Overdose cases at external use of means are not described. Because of low system absorption of drug overdose is considered improbable. At prolonged use on extensive surfaces hemorrhagic complications are possible.

Treatment: drug withdrawal, if necessary use of one-percentage solution of protamin of sulfate (antagonist of heparin).

Interaction

The drugs blocking the canalicular secretion, indirect anticoagulants reducing formation of vitamin K intestinal microflora antibiotics, NPVS, Dipiridamolum, ASK and reducing aggregation of thrombocytes other means strengthen effect of heparin.

Weakening of action is promoted: cardiac glycosides, alkaloids of an ergot, fenotiazina, antihistaminic HP, nicotine, ethacrynic and nicotinic acids, nitroglycerine (in/in introduction), AKTG, tetracyclines, alkaline amino acids and polypeptides, thyroxine, protamin.

It is impossible to mix solution in one syringe with other medicines.

At topical administration anticoagulative effect of drug amplifies when using gel in a combination with antiagregant, NPVS, anticoagulants. Tetracycline, thyroxines, nicotine and antihistamines reduce effect of heparin.

Terms of sale

Gel is means of non-prescription dispensing, the recipe is necessary for acquisition of solution.

The recipe of Heparin on Latin (sample):

Rp: Heparini 5 ml
D. t. d. N. 5
S. In/in on 25 000 PIECES, previously to part contents of a bottle in isotonic NaCl solution.

Storage conditions

Ampoules with solution have to be stored In dry, protected from light, the place, unavailable to children.

Gel has to be stored in the place, unavailable to children, at a temperature below 25C. A period of validity after opening — 28 days.

Period of validity

Two years.

Special instructions

Because of risk of formation of hematomas in the place of an injection solution should not be entered into a muscle.

Solution can get a yellowish shade that does not influence its activity or portability.

At purpose of drug in the medical purposes, the dosage should be selected taking into account AChTV value.

It is not necessary to carry out by drug a biopsy of bodies to the treatment period and to enter other drugs in oil.

For cultivation of solution only 0.9% NaCl solution can be used.

Gel should not be applied on mucous membranes and on open wounds. Besides, it is not used in the presence of purulent processes. Use of ointment is not recommended at TGV.

Unfractionated Heparin

Unfractionated call Heparin with an average molecular weight of 12-16 thousand dalton which is allocated from a bull lung or a mucous membrane of an intestinal path of pigs. Use it in production of HP which have local and systemic effect (heparin the containing ointments and solutions for parenteral administration).

Drug due to interaction with AT III (indirectly) suppresses the main enzyme of coagulant system of blood, and also other factors of coagulation, and it in turn leads to antitrombotichesky and anti-coagulative effects.

Endogenous heparin in a human body can be found in muscles, mucous intestines, lungs. On structure it is mix of fractions of glikozaminoglikan which consist of the sulfatidny remains of a D-glycosamine and D-glucuronic acid with a molecular weight from 2 to 50 thousand dalton.

The fractioned Heparin

The fractioned (low-molecular) heparins receive by an enzymatic or chemical depolymerization of unfractionated. Such Heparin consists of polysaccharides with an average molecular weight — 4-7 thousand dalton.

NMG are characterized as weak anticoagulative and highly effective antitrombotichesky means of direct action. Effect of such drugs is directed to compensation of processes of hypercoagulation.

NMG begins to work at once after introduction, at the same time its antitrombotichesky action is expressed and prolonged (the drug is administered by only 1 rubles/days).

Classification of low-molecular Heparins:

  • the drugs used for prevention of thromboses/thromboembolisms (Klivarin, Troparin, etc.);
  • the drugs used for treatment of unstable stenocardia and to THEM without pathological tooth of Q, thromboses and thromboembolisms, acute TGV, TELA (Fragmin, Kleksan, Fraksiparin);
  • the drugs used for treatment of a heavy vein thrombosis (Fraksiparin Forta);
  • the drugs used for prevention of a thrombogenesis of coagulation when carrying out haemo filtering and a hemodialysis (Fraksiparin, Fragmin, Kleksan).

Analogs

Coincidence on the ATH code of the 4th level:

Analogs of gel: Geparin-Akrigel 1000, Lioton 1000, Lavenum, Trombless.

Generics of an injection form: Heparin of J, Geparin-Fereyn, Geparin-Sandoz.

Drugs with the close mechanism of action: tablets — Piyavit, Angioflyuks, Wessel Due F; solution — Angioflyuks, Gemapaksan, Antithrombin III human, Wessel Due F, Flyuksum, Anfibra, Fraksiparin, Eniksum.

Zdravzona

  • Geparin-Fereyn solution for injections 5000ME/ml of 5 ml No. 5 bottles
  • Heparin solution for injections 5000ME/ml of 5 ml No. 50 flakonysintez joint stock company
  • Unguentum Heparini 25gnizhfarm joint stock company
  • No. 1 heparin 5000ed/1ml-5ml fl.
  • Heparin solution for injections 5000ME/ml of 5 ml No. 5 flakonymoskovsky endocrine plant of federal state unitary enterprise

Drugstore of IFC

  • Heparin ointment 25 of, Nizhpharm (N. Novgorod) Russia
  • Heparin solution for in 5 thousand ME/ml 5 of ml No. 5, Belmedpreparata (Minsk) Belarus
  • Geparin-Akrigel 1000 ME 30 0, HFK (г.Москва) Russia Quinacrine
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Apteka24

  • Heparin solution for injections of 5000 PIECES/ml 5 ml a bottle No. 5 Biolik (Ukraine, Kharkiv)
  • Heparin solution for injections of 5000 PIECES/ml a bottle of 5 ml No. 5farma Layf (Ukraine, Lviv)
  • Geparin-D gel of 600 PIECES 30gdarnitsa (Ukraine, Kiev)
  • Geparin-Novofarm solution for injections 5000 MO bottle of 5 ml No. 5novofarm-Biosintez (Ukraine, Novograd-Volynsky)
  • Geparinbelmedpreparata (Belarus)

Paniapteka

  • Unguentum Heparini 25gzhitomirskaya FF
  • Unguentum Heparini 25gzhitomirskaya FF

BIOSPHERE

  • Heparin 25 g ointment in a tuba
  • Heparin 25 g ointment in a tuba
  • ME/ml 5 heparin 5000 of ml No. 1 solution for infection.
  • Heparin 25 g ointment in a tuba
  • ME/ml 5 heparin 5000 of ml No. 5 solution for infection.
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Section: Cardiovascular
PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use Heparin surely consult with the attending physician.