Buy Heparin online. PayPal
Pharmacological group: Direct acting anticoagulants.
Active ingredient: sodium heparin.
Other brand names: Exhirud, Calciparine.
Dosage form: solution for injection.
Release form: solution for injection 5000IU/ml 5ml.
Heparin is known as a direct-acting anticoagulant, that is, as a blood-thinning agent. It is used for the prevention and treatment of thromboembolic diseases, during operations on the heart and blood vessels, to maintain the liquid state of blood in cardiopulmonary bypass and hemodialysis machines, as well as to prevent blood clotting in laboratory tests. For prophylactic purposes, heparin preparations are used in surgical interventions, with circulatory failure.
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Buy Heparin
Heparin belongs to the group of medium molecular weight heparins, slows down the formation of fibrin, is a physiological anticoagulant that potentiates the ability of antithrombin III to inhibit activated coagulation factors IXa, Xa, X1a, Xpa, and in high concentrations, thrombin activity. Of particular importance is the ability to inhibit thrombin and activated factor X.
Heparin is not able to dissolve the thrombus (it is not a fibrinolytic), but it can reduce the size of the thrombus, stopping its growth, and in this case, part of the thrombus is dissolved under the action of the fibrinolytic enzyme - plasmin. It inhibits the activity of hyaluronidase, 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, 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.
The drug has a blood-thinning effect, consult a specialist before use!
Heparin is used for:
- Prevention and treatment of venous thrombosis (including thrombosis of the superficial and deep veins of the lower extremities and renal vein thrombosis) and pulmonary embolism;
- prevention and treatment of thromboembolic complications associated with atrial fibrillation;
- prevention and treatment of peripheral arterial embolism (including those associated with mitral heart disease);
- treatment of acute and chronic consumption coagulopathy (including stage I DIC);
- acute coronary syndrome without persistent ST segment elevation on the ECG (unstable angina pectoris, myocardial infarction without ST segment elevation on the ECG);
- myocardial infarction with ST segment elevation: with thrombolytic therapy, with primary percutaneous coronary revascularization (balloon angioplasty with or without stenting) and with a high risk of arterial or venous thrombosis and thromboembolism;
- prevention and therapy of microthrombosis and microcirculation disorders, including with hemolytic-uremic syndrome;
- glomerulonephritis (including lupus nephritis) and with forced diuresis; prevention of blood coagulation during blood transfusion, in extracorporeal circulation systems (extracorporeal circulation during heart surgery, hemosorption, cytopheresis) and hemodialysis;
- treatment of peripheral venous catheters.
On the part of the circulatory system:
- it can provoke thrombocytopenia,
- gastrointestinal bleeding,
- bleeding at the injection site, in areas subjected to pressure, from surgical wounds, as well as hemorrhages in other organs.
From the digestive system:
- nausea,
- loss of appetite,
- vomiting,
- diarrhea,
- increased activity of hepatic transaminases.
Allergic reactions are also possible:
- skin flushing,
- pruritus,
- fever,
- urticaria,
- rhinitis,
- bronchospasm,
- collapse,
- anaphylactic shock.
With prolonged use, side effects are also detected from the musculoskeletal system:
- osteoporosis,
- spontaneous fractures.
Others:
- transient alopecia,
- hypoaldosteronism.
Bleeding
The main complications of heparin therapy are hemorrhagic. Severe bleeding was observed in 1-33% of patients (one study had 3 deaths out of 647 patients, (Levine and Hirsh, 1986)). In recent studies in patients with PE, severe bleeding was observed in less than 3% of patients treated with intravenous heparin (Levine et al., 1998). Comparable data were obtained in the treatment of PE with low molecular weight heparins. In general, the risk of bleeding increases with increasing daily dose and aPTT, but the correlation between these indicators is weak, and bleeding can occur even at therapeutic aPTT values. They are usually caused by comorbidities such as recent surgery, trauma, peptic ulcer disease, or thrombocytopathies. The anticoagulant effect of heparin stops a few hours after the drug is discontinued. For mild bleeding, there is usually no need to prescribe the antidote heparin. With life-threatening bleeding, the action of heparin can be quickly stopped by a slow infusion of protamine sulfate. The minimum dose of protamine sulfate should be administered to ensure the neutralization of heparin (1 mg for every 100 units of heparin remaining in the body, it is administered intravenously slowly (up to 50 mg per 10 minutes)).
Heparin thrombocytopenia
This diagnosis is made with a decrease in the number of platelets below 150,000 µl ~ 'or 50% of the original level. It occurs in approximately 3% of patients after 5–10 days of treatment with conventional heparin (Warkentin, 1999). Low molecular weight heparins rarely cause thrombocytopenia. A third of patients with this complication develop severe thrombosis (sometimes life-threatening or requiring limb amputation), which may precede thrombocytopenia. The most common are venous thrombosis and pulmonary embolism, but peripheral arterial thrombosis, myocardial infarction, and stroke are also possible. Heparin thrombocytopenia may be accompanied by bilateral adrenal necrosis, skin lesions at injection sites, and various systemic reactions. The appearance of thrombocytopenia or other complications mentioned above after 5 days of heparin therapy or later (regardless of the dose or route of administration) requires immediate discontinuation of the drug. In patients treated with heparin in the previous 3-4 months, heparin thrombocytopenia may develop more rapidly due to the remaining antibodies. The diagnosis can be confirmed by detection of antibodies to the complex of heparin with platelet factor 4, as well as by the study of heparin-dependent platelet activation. Since thrombosis may occur after discontinuation of the drug (Wallis et al., 1999; Warkentin, 1999), other anticoagulants are prescribed for heparin thrombocytopenia - lepirudin or danaparoid (see below). Low molecular weight heparins should not be used in such cases, as they often cross-react with antibodies to conventional heparin. Warfarin in patients with parin thrombocytopenia can cause wet gangrene (Warkentin et al., 1997) or multiple skin necrosis (Warkentin et al., 1999), it can be prescribed only after elimination of thrombocytopenia and treatment with other anticoagulants.
Other complications
In patients receiving heparin intravenously or subcutaneously, the activity of aminotransferases is often slightly increased with normal levels of bilirubin and normal alkaline phosphatase activity. Long-term treatment with therapeutic doses of heparin (more than 20,000 units / day for, for example, 3-6 months) can rarely cause osteoporosis with vertebral compression fractures. Heparin, even in small doses, inhibits the synthesis of aldosterone in the adrenal glands and occasionally causes hyperkalemia.
Contraindications
Various diseases accompanied by a slowdown in blood clotting; hemorrhagic diathesis; hemorrhagic stroke; bleeding of any localization (except for hemorrhages in embolic infarction of the lungs and kidneys); severe disorders of the kidneys and liver.
Heparin should not be used in pathological conditions associated with an increased risk of bleeding, such as:
- diseases of the cardiovascular system: acute and subacute infective endocarditis, severe uncontrolled arterial hypertension, aortic dissection, cerebral aneurysm;
- erosive and ulcerative lesions of the gastrointestinal tract (GIT) (including stress-induced), varicose veins of the esophagus in liver cirrhosis and other diseases, prolonged use of gastric and small intestine drains, ulcerative colitis, hemorrhoids;
- diseases of the hematopoietic organs and the lymphatic system: leukemia, hemophilia, thrombocytopenia, hemorrhagic diathesis;
- diseases of the central nervous system: hemorrhagic stroke, traumatic brain injury; malignant neoplasms; congenital deficiency of antithrombin III and replacement therapy with antithrombin III drugs (to reduce the risk of bleeding, it is necessary to use lower doses of heparin).
Heparin is administered subcutaneously, intravenously (bolus or drip). Heparin is prescribed as a continuous intravenous infusion or as regular intravenous injections, as well as subcutaneously (in the abdomen). Heparin sodium should not be administered intramuscularly due to the risk of developing intramuscular hematomas. Subcutaneous injections are preferably performed in the area of the anterolateral wall of the abdomen (in exceptional cases, they are injected into the upper region of the shoulder or thigh), while using a thin needle that should be inserted deeply, perpendicularly, into the fold of skin held between the thumb and forefinger until the end of the injection solution. It is necessary to alternate injection sites each time (to avoid the formation of a hematoma).
The dosage regimen is individual, depending on the dosage form used, the indications, the clinical situation and the age of the patient.
In acute myocardial infarction, it is recommended to administer intravenous heparin at a dose of 15,000-20,000 units already in an ambulance and continue in a hospital for at least 5-6 days, subcutaneous administration at a dose of 40,000 units per day (every 4-6-8 hours hours for 5000-10000 IU).
In case of peripheral thrombosis, first 5000 IU of heparin is administered intravenously, then 30000-40000 IU / day 3-6 times a day subcutaneously or through an infusion pump at the rate of 18 U / (kg h) under the control of APTT.
For the prevention of thromboembolism, heparin is administered at a dose of 5000 IU subcutaneously 1-2 times a day in the pre- and postoperative period.
With massive thrombosis of the pulmonary artery, the drug is administered drip at a dose of 40,000-60,000 IU for 4-6 hours, then they switch to intramuscular administration at 40,000 IU per day.
With direct blood transfusion, heparin is injected into the donor's vein at 7500-10000 IU.
Because of the potential for precipitation of the active ingredients, heparin sodium should not be mixed with other medicinal products.
Sodium heparin solution is incompatible with the following drug solutions: alteplase, amikacin, amiodarone, sodium ampicillin, sodium benzylpenicillin, ciprofloxacin, cytarabine dacarbazine, danorubicin, diazepam, dobutamine, doxorubicin hydrochloride, droperidol, erythromycin, gentamycin sulfate, haloperidol lactate, hyaluronidase, hydrocortisone sodium succinate, dextrose (glucose), idarubicin, kanamycin sulfate, sodium methicillin, netilmicin sulfate, opioids, oxytetracycline B hydrochloride promazine hydrochloride, promethazine hydrochloride, streptomycin sulfate, sulfafurasol diethanolamine, tetracycline hydrochloride, tobramycin sulfate, cephalothin sodium, cephaloridine, vancomycin hydrochloride, vinblastine sulfate, labetalol hydrochloride, nicardipine hydrochloride.
The anticoagulant effect of sodium heparin is enhanced when used simultaneously with other drugs that affect hemostasis, including antiplatelet drugs (acetylsalicylic acid, clopidogrel, prasugrel, ticlopidine, dipyridamole), indirect anticoagulants (warfarin, phenylin. Syncumar ), thrombolytic drugs (alteplase, streptokinase, urokinase), non-steroidal anti-inflammatory drugs (phenylbutazone, ibuprofen, indomethacin, diclofenac, etc.), glucocorticosteroids and dextran, resulting in an increased risk of bleeding. In addition, the anticoagulant effect of sodium heparin may be enhanced when used together with hydroxychloroquine, sulfinpyrazone. probenecid, ethacrynic acid, cytostatics, cefamandol, cefotetan, valproic acid, propylthiouracil.
The anticoagulant effect of sodium heparin decreases with simultaneous use with ACTH, antihistamines, ascorbic acid, ergot alkaloids, nicotine, nitroglycerin, cardiac glycosides, thyroxine, tetracycline and quinine. Heparin sodium can reduce the pharmacological action of ACTH, glucocorticosteroids and insulin.
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Laboratory monitoring of the efficacy and safety of sodium heparin therapy.
The dose of heparin sodium must be adjusted based on laboratory parameters of blood clotting. When using heparin sodium, it is necessary to control the activated partial thromboplastin time (APTT) or blood clotting time (CWT). The administered dose of heparin sodium is considered adequate if the APTT is 1.5-2.5 times the control values or if the patient's ROS is 2.5-3.0 times the control values. With continuous intravenous infusion of sodium heparin, it is recommended to determine the initial APTT, then determine the APTT every 4 hours, followed by an increase or decrease in the rate of sodium heparin infusion until the target level of APTT is reached (1.5-2.5 times higher than normal), then determine the APTT every 6 hours. When bolus intravenous sodium heparin is administered, it is recommended to determine the initial APTT, then determine the APTT before each bolus administration, followed by an increase or decrease in the administered dose of sodium heparin. With subcutaneous administration of sodium heparin, it is recommended to control the APTT 4-6 hours after injection, followed by an increase or decrease in the administered dose of sodium heparin. With subcutaneous administration of low doses of heparin sodium (5000ME 2-3 times a day) for the prevention of thrombosis, it is not necessary to regularly monitor the APTT, because. it increases slightly.
Before elective surgical interventions, in order to reduce blood loss during surgery and in the postoperative period, it is usually recommended to stop oral anticoagulants (warfarin) and antiplatelet drugs (acetylsalicylic acid, clopidogrel, ticlopidine) 7 days before surgery.
