Heparin sodium injection, indications for the prevention and treatment of
thrombotic or embolistic diseases (such as myocardial infarction,
thrombophlebitis, pulmonary embolism, etc.); Diffuse intravascular coagulation
(DIC) due to various causes; It is also used in hemodialysis, extracorporeal
circulation, catheterization, microvascular surgery and other operations and
anticoagulation treatment of some blood samples or instruments.
1. Deep subcutaneous injection: 5000 ~ 10000 units for the first time, 8000 ~ 10000 units every 8 hours or 15000 ~ 20000 units every 12 hours thereafter; The total amount is about 30,000 ~ 40,000 units every 24 hours, and generally satisfactory results can be achieved.
2. Intravenous injection: after the first 5,000 ~ 10,000 units, or 100 units /kg every 4 hours according to body weight, dilute with sodium chloride injection and apply.
3. Intravenous infusion: 20,000 ~ 40,000 units per day were added to 1000ml sodium chloride injection for continuous infusion. An initial dose of 5000 units may be given intravenously before infusion.
4. Preventive treatment: High-risk thrombotic patients are mostly used after abdominal surgery to prevent deep venous thrombosis. 5000 units of heparin should be injected subcutaneously 2 hours before surgery, but the anesthetic method should avoid epidural anesthesia, and then 5000 units should be given every 8 to 12 hours for a total of 7 days.
The toxicity is relatively low, and the main adverse reaction is that too much medication can cause spontaneous bleeding, so the coagulation time should be measured before each injection. If serious bleeding occurs after injection, emergency treatment can be performed by intravenous injection of protamine sulfate (1mg protamine sulfate can neutralize 100U heparin).
Occasionally cause anaphylaxis and thrombocytopenia usually occur in the first 5-9 days, so the platelet count should be monitored regularly within 1 month after the beginning of treatment. Occasional hair loss and diarrhea. It can also cause osteoporosis and spontaneous fractures. Liver function is bad long-term use can cause antithrombin - Ⅲ depletion and thrombophilia.
To heparin allergy, the person that has spontaneous haemorrhage tendency, blood clotting is slow (be like hemophilia, purpura, thrombocytopenia), cankus disease, wound, postpartum haemorrhage and serious liver function is not complete person is forbidden.
Matters needing attention
Clotting time should be measured regularly during medication.
Pregnant and lactating women
The use of drugs in late pregnancy and postpartum may increase the risk of maternal bleeding and should be used with caution.
1. Intravenous injection: inject 50 units 1kg at a time according to body weight, and give 50 to 100 units every 4 hours thereafter;
2. Intravenous infusion: inject 50 units /kg according to body weight, then give 20,000 units /m2 per day according to body surface area for 24 hours, and add sodium chloride injection into the infusion slowly.
Elderly people over 60 years old, especially elderly women, are more sensitive to the drug and are prone to bleeding during medication. Therefore, dosage should be reduced and follow-up should be strengthened.
When used in combination with the following drugs, the risk of bleeding may be increased:
1. Coumarin and its derivatives, which can lead to severe factor IX deficiency and bleeding;
2. Aspirin and non-steroidal anti-inflammatory and analgesic drugs, including mefenac and salicylic acid, can inhibit platelet function and induce gastrointestinal ulcer bleeding;
3. Dipyridamole and dextran may inhibit platelet function;
4. Adrenocorticosteroids, adrenocorticotropin and other adrenocorticotropin can easily induce gastrointestinal ulcer bleeding;
5. Other beneficial uric acid, tissue plasminogen activator (T-PA), urokinase, streptokinase, etc.
2. Heparin with sodium bicarbonate, sodium lactate and other drugs to correct acidosis can promote the anticoagulation effect of heparin.
3. The mixed injection of heparin and hyaluronidase can not only relieve myodynia, but also promote heparin absorption. However, heparin can inhibit the activity of hyaluronidase, so the two should be used together temporarily, and should not be kept for a long time after drug mixing.
4. Heparin can act with insulin receptors, thus changing the binding and action of insulin. Hypoglycemia caused by Liver-village has been reported.
5. The following drugs and this has the compatibility taboo: kanamycin, amikacin, soft erythromycin, erythromycin, gentamycin sulfate, lactose acid hydrogenation of sodium succinate, polymyxin B, adriamycin, tobramycin, vancomycin, meng cephalosporin cefepime, oxygen more pp, cefalotin sodium, chloroquine, chlorpromazine, promethazine, narcotic analgesics.
6. Methimazole and prothiouracil have synergistic effect with the product.
Excessive use of this product may cause spontaneous bleeding tendency. When heparin is in excess, 1% protamine sulfate solution can be slowly drip, so as to neutralize heparin effect. Protamine neutralizes 100U of heparin per 1mg of protamine.
Pharmacology and toxicology
Due to its physical and chemical properties with strong negative charge, this product can interfere with many links of the blood coagulation process, and has anticoagulant effect in vivo and in vitro. Its mechanism is complex, mainly through and antithrombin Ⅲ (AT - Ⅲ), and enhance the latter to activate II, IX, X and XI, and assist the inhibitory effect of clotting factors. The results involve preventing platelet agglutination and destruction, and impeding the formation of thrombin-activating enzyme. Preventing prothrombin from becoming prothrombin; It inhibits thrombin, thereby preventing fibrinogen from becoming fibrin.
This product is not absorbed by oral administration and is well absorbed by subcutaneous, intramuscular or intravenous injection. But 80% of heparin binds to plasma albumin, is partially hemadsorbed, and partially diffuses into the extravascular space. Because of its high molecular weight, it cannot pass through the pleura. Peritoneal and placental tissue. This product is mainly in the reticuloendothelial system metabolism, renal excretion. A small amount is discharged in its original form. Its excretion after intravenous injection depends on the dose administered. When given 100, 400, or 800U/kg in one dose. T1/2 was 1 hour, 2.5 hours and 5 hours, respectively. Chronic liver and kidney dysfunction and excessive obesity, metabolic excretion delay, there is the possibility of accumulation; The onset time of this product is related to the way of administration. The anticoagulant effect is maximized immediately after intravenous injection, but the individual difference is great. The overall duration of subcutaneous injection is significantly prolonged due to the great individual difference in absorption. Plasma heparin concentration is not affected by dialysis.
To learn more about heparin sodium, consult the heparin sodium manufacturer Kowloon Pharmaceutical For details.