Heparin sodium

Chemical name

Mukopolisaharid ester poliserna acid

Characteristics

Obtained from the lungs of cattle. Amorphous powder white with a yellowish sheen, odourless. Rat in the water and physiological solution, pH 1% aqueous 6-7.5. Activity determine biological method of increasing the ability of the blood clotting and expressed in units of action.

Of drugs

The drugs-antikoagulyatine. Associated antitrombinom III, causes conformational changes in the molecule, and accelerates the synergy antitrombina III serinproteazami of coagulation; As a result of blocked trombin, enzyme activity of activated factor IX, X, XI, XII, and plazmina kallickreina. The highest bioavailability with the on / in the introduction; The p / to the introduction of low bioavailability, C_max is 2-4 hours; T_1/2 is 1-2 hours; Plasma is mainly associated with the protein; Intensively endotelialnami red cells and cells мононуклеарно-макроф��гальной system concentrated in the liver and spleen; and an inhalation method of absorption alveolarnami macrofagami, endoteliem capillaries, large blood and lymph vessels : these cells are the main point of the deposit unchanged from which it is released, maintaining a certain level of plasma; desulfatace be influenced N-desulfamidaza geparinaza and platelets, incluchateisa in metabolism unchanged at later stages; desulfatirovannae molecule as a result of kidney endoglikozidaza become molecular fragments; excretion takes place through the kidneys in the form of metabolites, and it is only when the high doses can be excreted unchanged to. Trombin Associates; This reaction is elektrostaticescuu nature, and to a large extent depends on the length of the molecule heparin; Only a handful of molecules heparin affinity is with ATIII, which is based on his antikoagulyazionnuu activity. Braking 821-828 antitrombinom-slow process; Formation of the complex Geparin-atiii greatly accelerated by directly linking unchanged гамма-аминолизиловым�� parts of the molecule ATIII and from the interplay between trombinom (through serine), and set Geparin-atiii (via arginine); after braking reaction 821-828 heparin released from the compound Geparin-atiii and can be used again organism, and the remaining complexes are removed endotelialna system; reduces the viscosity of the blood, reduces blood pressure, stimulirovannuyu bradikininom, gistaminom and other endogenous factors and hinders the development staza. on the surface of cells found endotelia special receptors for endogenous analogues unchanged; heparin sorbirovtsa capable on the surface membranes endotelia and loose elements of the blood, increase in the negative charge, which prevents adhesion and aggregation of platelets, red, white; heparin molecule with low affinity with ATIII, Braking is hyperplasia of smooth muscles, including by braking adhesion nine oppression releasing factor growth of these cells suppress activation lipoprotheidlipaza than hinder the development of atherosclerosis; heparin binding some parts of the complement system to reduce its active cooperation from lymphocytes and education immunoglobulins binds histamine, serotonin are made protiwallergiceski effect; interacts with surfaktantom, reducing its activity in the lungs; have influence on the endocrine system-suppressing excessive aldosterone synthesis in the Koryo napochechnikov binds adrenaline, modulating response to the ovarian hormones incentives increased activity paratgormona; as a result of the interaction with enzymes can increase activity tirosingidroksilazy brain pepsinoguena, Dnk-polimeraza and lower activity miozinova Atfaza, piruwatkinaza, Rnk-polimeraza, pepsina. In patients with ischemic heart disease (in combination with aspirin) reduced the risk of acute trombozov coronary arteries, myocardial infarction and sudden death. Reduces Frequency repeat heart attacks and mortality of patients after myocardial infarction. In high doses is effective in the lung emboliah receptacles and venoznom trombose, small for the prevention of venous tromboamboliy, incl. after surgery; in the on / in a down

Indications

The unstable stenocardia, acute myocardial infarction; Embolic complications of myocardial infarct, operations on the heart and blood vessels, tromboembolia lung and brain receptacles tromboflebita (prevention and treatment); Dvs-sindrom, prevention микротромбообразован ия and the violation of circulation; X renal veins; �емолитико-уремически й syndrome; mertzatelnaya Already, mitrale heart disease (prevention tromboobrazovania); endocardit bacterial; glomerulonefrit; volchanochny jade; arthritis; bronchial asthma; ekstrakorporalnah the methods (IVF blood circulation in heart surgery, gemosorbece, Hepatology, peritonealny dialysis, zitaferez) diureza big; wash venous catheters.

Contraindications

Diates bloody, leukaemia, anaemia, high blood pressure, polyps, neoplasia, and the defeat of ulcerated stomach, heavy human liver and kidney transplants, brain and spine.

Side-Effects

Dizziness, headaches, nausea, anorexia, vomiting, diarrhoea, alopecia; Early (2-4 days treatment), and late (pp) trombozitopenia; Hemorrhagic complications, bleeding in the digestive tract or urinary tract retroperitoneale bleeding of the ovaries, adrenal glands (with the development of acute napochechnikova deficiency), osteoporosis, calcification of soft tissues, oppression aldosterone synthesis, raising transaminaz in blood, allergic reactions (fever, skin, bronchial asthma, anaphylactoidnaya reaction), local irritation, bruise, soreness in the introduction.

Patient interaction

The growing acetylsalicylic acid dekstranom, fenilbutazonom, ibuprofenom, indometazinom, varfarinom, dikumarinom (the risk of bleeding), weakened heart-glycosides, tetratziklinami, antihistamines drugs, nicotine acid etakrinova acid.

Precautions

Continuous monitoring the blood clotting; Lifting should be done gradually.

Dosing and Administration

P / for (deep in the subcutaneous fat jirovu, changing places injection), in / in the (slow), in / m inhalation and the 20,000-50,000 U / day, depending on the evidence; In / in usually do load dose 5,000 U, and then to 20-40 thousand U / day through infuzing pump (used permanent or preravista the scheme for 5-10 thousand U every 4-6 h); For the prevention of postoperative trombozov in / enter in small doses - 17,000 U / day for three to five days; For the prevention tromboamboliy s / to 5,000 U for 2-8 hours before the operation, and then every 8 h the same dose being within 7 days; To improve circulation impose s / by-an average of 2.5-5 thousand U 3-4 times per day for 5-7 days, with a gradual decrease in dose.

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