Identification
- Summary
Heparin is an anticoagulant indicated for thromboprophylaxis and to treat thrombosis associated with a variety of conditions such as pulmonary embolism and atrial fibrillation.
- Brand Names
- Defencath, Heparin Leo
- Generic Name
- Heparin
- DrugBank Accession Number
- DB01109
- Background
Unfractionated heparin (UH) is a heterogenous preparation of anionic, sulfated glycosaminoglycan polymers with weights ranging from 3000 to 30,000 Da. It is a naturally occurring anticoagulant released from mast cells. It binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin (factor IIa) and factor Xa. UH is different from low molecular weight heparin (LMWH) in the following ways: the average molecular weight of LMWH is about 4.5 kDa whereas it is 15 kDa for UH; UH requires continuous infusions; activated partial prothrombin time (aPTT) monitoring is required when using UH; and UH has a higher risk of bleeding and higher risk of osteoporosis in long term use. Unfractionated heparin is more specific than LMWH for thrombin. Furthermore, the effects of UH can typically be reversed by using protamine sulfate.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Synonyms
- Eparina
- Heparina
- Heparine
- Heparinic acid
- Heparinum
- Unfractionated heparin
- External IDs
- CY 216
- CY 222
- CY216
- KB 101
- OP 386
- OP 622
Pharmacology
- Indication
Unfractionated heparin is indicated for prophylaxis and treatment of venous thrombosis and its extension, prevention of post-operative deep venous thrombosis and pulmonary embolism and prevention of clotting in arterial and cardiac surgery. In cardiology, it is used to prevent embolisms in patients with atrial fibrillation and as an adjunct antithrombin therapy in patients with unstable angina and/or non-Q wave myocardial infarctions (i.e. non-ST elevated acute coronary artery syndrome) who are on platelet glycoprotein (IIb/IIIa) receptor inhibitors. Additionally, it is used to prevent clotting during dialysis and surgical procedures, maintain the patency of intravenous injection devices and prevent in vitro coagulation of blood transfusions and in blood samples drawn for laboratory values.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination for symptomatic treatment of Blunt injuries Combination Product in combination with: Polysorbate 80 (DB11063), Salicylic acid (DB00936), Levomenthol (DB00825) ••• ••• ••• Prevention of Clotting •••••••••••• ••••••••• Prevention of Clotting •••••••••••• ••••••••• Treatment of Consumption coagulopathy •••••••••••• ••••••••• Used in combination for symptomatic treatment of Contusions Combination Product in combination with: Dexpanthenol (DB09357) •••••••••••• •••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
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Unfractionated heparin is a highly acidic mucopolysaccharide formed of equal parts of sulfated D-glucosamine and D-glucuronic acid with sulfaminic bridges. The molecular weight ranges from 3000 to 30,000 daltons. Heparin is obtained from liver, lung, mast cells, and other cells of vertebrates. Heparin is a well-known and commonly used anticoagulant which has antithrombotic properties. Heparin inhibits reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo. Small amounts of heparin in combination with antithrombin III, a heparin cofactor,) can inhibit thrombosis by inactivating Factor Xa and thrombin. Once active thrombosis has developed, larger amounts of heparin can inhibit further coagulation by inactivating thrombin and preventing the conversion of fibrinogen to fibrin. Heparin also prevents the formation of a stable fibrin clot by inhibiting the activation of the fibrin stabilizing factor. Heparin prolongs several coagulation tests. Of all the coagulation tests, activated partial prothrombin time (aPTT) is the most clinically important value.
- Mechanism of action
Under normal circumstances, antithrombin III (ATIII) inactivates thrombin (factor IIa) and factor Xa. This process occurs at a slow rate. Administered heparin binds reversibly to ATIII and leads to almost instantaneous inactivation of factors IIa and Xa The heparin-ATIII complex can also inactivate factors IX, XI, XII and plasmin. The mechanism of action of heparin is ATIII-dependent. It acts mainly by accelerating the rate of the neutralization of certain activated coagulation factors by antithrombin, but other mechanisms may also be involved. The antithrombotic effect of heparin is well correlated to the inhibition of factor Xa. Heparin is not a thrombolytic or fibrinolytic. It prevents progression of existing clots by inhibiting further clotting. The lysis of existing clots relies on endogenous thrombolytics.
Target Actions Organism AAntithrombin-III potentiatorHumans ACoagulation factor X inhibitorHumans UP-selectin inhibitorHumans UFibroblast growth factor receptor 4 Not Available Humans UFibroblast growth factor 4 Not Available Humans UFibroblast growth factor 19 Not Available Humans UFibroblast growth factor receptor 1 Not Available Humans UFibroblast growth factor 1 Not Available Humans UFibroblast growth factor receptor 2 Not Available Humans UFibroblast growth factor 2 Not Available Humans UPlatelet factor 4 Not Available Humans UHepatocyte growth factor Not Available Humans - Absorption
Heparin is not absorbed through the gastrointestinal tract and is therefore administered via a parenteral route. Peak plasma concentration and the onset of action are achieved immediately after intravenous administration.11
Plasma heparin concentrations may be increased and activated partial thromboplastin times (aPTTs) may be more prolonged in geriatric adults (older than 60 years of age) compared with younger adults.11
- Volume of distribution
The volume of distribution is 0.07 L/kg.11 Although heparin does not distribute into adipose tissues, clinicians should use actual body weight in obese patients to account for extra vasculature.6
- Protein binding
Heparin is highly bound to antithrombin, fibrinogens, globulins, serum proteases, and lipoproteins.11
- Metabolism
Heparin does not undergo enzymatic degradation.11
- Route of elimination
Heparin undergoes biphasic clearance, a) rapid saturable clearance (zero-order process due to binding to proteins, endothelial cells, and macrophages), and b) slower first-order elimination. Low doses of heparin are cleared mostly by a saturable, rapid, zero-order process. Slower first-order elimination usually occurs with very high doses of heparin and is dependent on renal function.11 High-molecular-weight moieties are cleared more rapidly than lower molecular-weight moieties.4
- Half-life
The plasma half-life is dose-dependent, and it ranges from 0.5 to 2 h.11 For the purpose of choosing a protamine dose, heparin can be assumed to have a half-life of about 30 minutes after intravenous injection.11 The plasma half-life of heparin increases from about 30 min after an IV bolus of 25 units/kg to 60 minutes with a 100 unit/kg dose or to about 150 minutes with a 400 unit/kg dose.4
- Clearance
The clearance in adults receiving a bolus dose of 75 units/kg and preterm newborns receiving a bolus dose of 100 units/kg were calculated to be 0.43 ml/kg/min and 1.49 ml/kg/min respectively.7
- Adverse Effects
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In mouse, the median lethal dose is greater than 5000 mg/kg. Another side effect is heparin-induced thrombocytopenia (HIT syndrome). Platelet counts usually do not fall until between days 5 and 12 of heparin therapy. HIT is caused by an immunological reaction that makes platelets form clots within the blood vessels, thereby using up coagulation factors. It can progress to thrombotic complications such as arterial thrombosis, gangrene, stroke, myocardial infarction and disseminated intravascular coagulation. Symptoms of overdose may show excessive prolongation of aPTT or by bleeding, which may be internal or external, major or minor. Therapeutic doses of heparin give for at least 4 months have been associated with osteoporosis and spontaneous vertebral fractures. Osteoporosis may be reversible once heparin is discontinued. Although a causal relationship has not been established, administration of injections preserved with benzyl alcohol has been associated with toxicity in neonates. Toxicity appears to have resulted from administration of large amounts (i.e., about 100–400 mg/kg daily) of benzyl alcohol in these neonates. Its use is principally associated with the use of bacteriostatic 0.9% sodium chloride intravascular flush or endotracheal tube lavage solutions.
- Pathways
Pathway Category Heparin Action Pathway Drug action Fc Epsilon Receptor I Signaling in Mast Cells Signaling - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of bleeding can be increased when Abciximab is combined with Heparin. Acebutolol The risk or severity of hyperkalemia can be increased when Heparin is combined with Acebutolol. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Heparin. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Heparin is combined with Acemetacin. Acenocoumarol The risk or severity of bleeding can be increased when Heparin is combined with Acenocoumarol. - Food Interactions
- Administer calcium supplement. This drug decreases calcium levels.
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Heparin calcium M4F288ZCTR 37270-89-6 Not applicable Heparin sodium ZZ45AB24CA Not Available Not applicable - International/Other Brands
- Calcilean / Calciparine / Hepalean / Heparin LEO / Liquaemin / Liquemin / Multiparin / Novoheparin
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Calcilean Inj 20000unit/0.8ml Liquid 20000 unit / .8 mL Subcutaneous Organon Teknika Canada Inc. 1987-12-31 1997-08-11 Canada 
Calciparine Inj 20000iu/amp Liquid 20000 unit / amp Subcutaneous Choay Lab 1974-12-31 1998-06-09 Canada Calciparine Inj 5000iu Liquid 5000 unit / syr Subcutaneous Choay Lab 1977-12-31 1998-06-09 Canada Hep-Lock Solution 100 [USP'U]/1mL Intravenous Baxter Laboratories 1972-03-22 2010-02-02 US 
Hep-Lock Solution 10 [USP'U]/1mL Intravenous Baxter Laboratories 1972-03-22 2010-02-02 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Heparin Lock Flush Injection, solution 10 [USP'U]/1mL Intravenous Hospira, Inc. 1943-04-27 2011-03-01 US Heparin Lock Flush Injection, solution 100 [USP'U]/1mL Intravenous Hospira, Inc. 1943-04-27 2011-07-01 US Heparin Sodium Injection, solution 1000 [USP'U]/1mL Intravenous; Subcutaneous Cardinal Health 107, LLC 2014-06-12 Not applicable US Heparin Sodium Injection, solution 2000 [USP'U]/2mL Intravenous; Subcutaneous BE Pharmaceuticals Inc. 2020-12-29 Not applicable US Heparin sodium Injection, solution 20000 [USP'U]/1mL Intravenous; Subcutaneous Mylan Institutional LLC 2018-06-14 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image BARICUS 50 IU/%1/%10 JEL , 50 G Heparin sodium (0.4 mg/g) + Allantoin (10 mg/g) + Onion (100 mg/g) Gel Topical SANTA FARMA İLAÇ SAN. A.Ş. 2017-06-06 Not applicable Turkey 
CONTRACTUBEX ® GEL Heparin sodium (5000 IU) + Allantoin (1 g) + Onion (10 g) Gel Topical LABORATORIOS BIOPAS S.A 2006-11-10 2012-07-24 Colombia 
Contractubex Gel Heparin sodium (5000 IU/100g) + Allantoin (1 g) + Onion (10 g/100g) Gel Cutaneous Merz Pharma Austria Gmb H 1968-08-13 Not applicable Austria 
CONTRACTUBEX JEL, 100 G Heparin sodium (40 mg/100g) + Allantoin (1 g/100g) + Onion (10 g/100g) Gel Topical ASSOS İLAÇ KİMYA GIDA ÜRÜNLERİ ÜRETİM VE TİC. A.Ş. 2003-05-12 Not applicable Turkey CONTRACTUBEX JEL, 120 G Heparin sodium (40 mg/100g) + Allantoin (1 g/100g) + Onion (10 g/100g) Gel Topical ASSOS İLAÇ KİMYA GIDA ÜRÜNLERİ ÜRETİM VE TİC. A.Ş. 2003-05-12 Not applicable Turkey - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Heparin Lock Flush Heparin sodium (10 [USP'U]/1mL) Injection, solution Intravenous Fresenius Kabi USA, LLC 2009-08-29 2017-11-06 US Heparin Lock Flush Heparin sodium (100 [USP'U]/1mL) Injection, solution Intravenous Fresenius Kabi USA, LLC 2009-08-12 2019-06-06 US Heparin Sodium Heparin sodium (50 [USP'U]/1mL) Injection, solution Intravenous Cantrell Drug Company 2012-08-09 Not applicable US Heparin Sodium Heparin sodium (50 [USP'U]/1mL) Injection, solution Intravenous Cantrell Drug Company 2012-12-21 Not applicable US Heparin Sodium Heparin sodium (100 [USP'U]/1mL) Injection, solution Intravenous Cantrell Drug Company 2015-05-15 Not applicable US
Categories
- ATC Codes
- B01AB51 — Heparin, combinations
- B01AB — Heparin group
- B01A — ANTITHROMBOTIC AGENTS
- B01 — ANTITHROMBOTIC AGENTS
- B — BLOOD AND BLOOD FORMING ORGANS
- C05BA — Heparins or heparinoids for topical use
- C05B — ANTIVARICOSE THERAPY
- C05 — VASOPROTECTIVES
- C — CARDIOVASCULAR SYSTEM
- S01XA — Other ophthalmologicals
- S01X — OTHER OPHTHALMOLOGICALS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- C05BA — Heparins or heparinoids for topical use
- C05B — ANTIVARICOSE THERAPY
- C05 — VASOPROTECTIVES
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- Agents causing hyperkalemia
- Anticoagulants
- Antivaricose Therapy
- Blood and Blood Forming Organs
- Carbohydrates
- Cardiovascular Agents
- Fibrin Modulating Agents
- Glycosaminoglycans
- Hematologic Agents
- Heparin and similars
- Heparin Group
- Heparins or Heparinoids for Topical Use
- Miscellaneous Therapeutic Agents
- Narrow Therapeutic Index Drugs
- Ophthalmologicals
- Polysaccharides
- Sensory Organs
- Thyroxine-binding globulin substrates
- Vasoprotectives
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- T2410KM04A
- CAS number
- 9005-49-6
References
- Synthesis Reference
Fernando Fussi, Gianfranco Fedeli, "Oligo-heteropolysaccharides having a heparin-like activity method for their preparation and pharmaceutical compositions based thereon." U.S. Patent US4757057, issued June, 1952.
US4757057- General References
- Linhardt RJ, Gunay NS: Production and chemical processing of low molecular weight heparins. Semin Thromb Hemost. 1999;25 Suppl 3:5-16. [Article]
- Ferro DR, Provasoli A, Ragazzi M, Casu B, Torri G, Bossennec V, Perly B, Sinay P, Petitou M, Choay J: Conformer populations of L-iduronic acid residues in glycosaminoglycan sequences. Carbohydr Res. 1990 Jan 15;195(2):157-67. [Article]
- Mulloy B, Forster MJ, Jones C, Davies DB: N.m.r. and molecular-modelling studies of the solution conformation of heparin. Biochem J. 1993 Aug 1;293 ( Pt 3):849-58. [Article]
- Hirsh J, Raschke R: Heparin and low-molecular-weight heparin: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest. 2004 Sep;126(3 Suppl):188S-203S. [Article]
- Petitou M, Herault JP, Bernat A, Driguez PA, Duchaussoy P, Lormeau JC, Herbert JM: Synthesis of thrombin-inhibiting heparin mimetics without side effects. Nature. 1999 Apr 1;398(6726):417-22. [Article]
- Spruill WJ, Wade WE, Huckaby WG, Leslie RB: Achievement of anticoagulation by using a weight-based heparin dosing protocol for obese and nonobese patients. Am J Health Syst Pharm. 2001 Nov 15;58(22):2143-6. [Article]
- McDonald MM, Jacobson LJ, Hay WW Jr, Hathaway WE: Heparin clearance in the newborn. Pediatr Res. 1981 Jul;15(7):1015-8. [Article]
- Authors unspecified: Benzyl alcohol: toxic agent in neonatal units. Pediatrics. 1983 Sep;72(3):356-8. [Article]
- Authors unspecified: Benzyl alcohol may be toxic to newborns. FDA Drug Bull. 1982 Aug;12(2):10-1. [Article]
- Authors unspecified: Neonatal deaths associated with use of benzyl alcohol--United States. MMWR Morb Mortal Wkly Rep. 1982 Jun 11;31(22):290-1. [Article]
- FDA Approved Drug Products: HEPARIN SODIUM IN 5% DEXTROSE INJECTION, for intravenous use [Link]
- BASG Product Information: Sensicutan (bisabolol/heparin sodium) topical ointment [Link]
- AIFA Package Leaflet: PROCTOSOLL (benzocaine, heparin, hydrocortisone) rectal cream [Link]
- FDA approved drug product: HEPARIN SODIUM IN SODIUM CHLORIDE injection for intravenous infusion [Link]
- FDA approved drug product: HEPARIN SODIUM INJECTION, for intravenous or subcutaneous use [Link]
- External Links
- KEGG Compound
- C00374
- PubChem Substance
- 46507594
- 5224
- ChEBI
- 28304
- ChEMBL
- CHEMBL1909300
- Therapeutic Targets Database
- DAP000189
- PharmGKB
- PA449855
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Heparin
- FDA label
- Download (198 KB)
- MSDS
- Download (72.1 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Prevention Microvascular Coronary Dysfunction (MCD) 1 4 Active Not Recruiting Treatment Coronavirus Disease 2019 (COVID‑19) 1 4 Completed Not Available Renal Insufficiency, Acute 1 4 Completed Diagnostic Insulin Resistance Syndrome X / Pancreatic Beta Cell Function 1 4 Completed Diagnostic Mesenteric vascular insufficiency 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Amerisource Health Services Corp.
- Amsino Medical Usa
- APP Pharmaceuticals
- B. Braun Melsungen AG
- Baxter International Inc.
- Becton Dickinson
- Bioiberica Sa
- Cardinal Health
- Eisai Inc.
- General Injectables and Vaccines Inc.
- Hospira Inc.
- Mason Distributors
- Medefil Inc.
- Medical Techniques LLC
- Neuman Distributors Inc.
- Pfizer Inc.
- Pharmacia Inc.
- Sagent Pharmaceuticals
- Sandhills Packaging Inc.
- Spectrum Pharmaceuticals
- Tyco Healthcare Group LP
- Vetter Pharma Fertigung GmbH and Co. KG
- Dosage Forms
Form Route Strength Gel Topical Capsule Solution Intravenous Liquid Subcutaneous 20000 unit / .8 mL Injection, solution Intravenous; Parenteral 20000 UI/4ML Injection, solution Parenteral; Subcutaneous 12500 IU/0.5ML Injection, solution Parenteral; Subcutaneous 5000 IU/0.2ML Injection, solution Subcutaneous 12500 IU/0.5ml Injection, solution Subcutaneous 12500 IU Injection, solution Subcutaneous 125000 IU/0.5ml Injection, solution Subcutaneous 20000 IU/0.8ml Injection, solution Subcutaneous 20000 IU Injection, solution Subcutaneous 5000 IU/0.2ml Liquid Subcutaneous 20000 unit / amp Liquid Subcutaneous 5000 unit / syr Tablet, delayed release Tablet, extended release Injection, solution Gel Cutaneous Injection, solution Subcutaneous Injection Intravenous; Subcutaneous 1000 iu/ml Injection Intravenous; Subcutaneous 35000 iu/35ml Solution Intraluminal Injection, solution Subcutaneous 25000 IU/mL Injection, solution Intravenous Injection, solution Intravenous; Subcutaneous 50000 U Injection, solution Parenteral 5000 IU/ML Injection Intravenous; Subcutaneous Injection, solution Intravenous 25000 IU/5ML Injection, solution Intravenous; Subcutaneous 5000 IU/1ML Solution Parenteral 250 IU/5ML Solution Parenteral 300 IU/3ML Solution Parenteral 500 IU/2ML Gel Topical 60000 IE Ointment 60000 IE Injection, solution Intravenous; Subcutaneous Injection, solution 11400 UI/0.6ML Gel Topical 50000 IE Injection Intravenous; Subcutaneous 25000 iu/5ml Pill 100 MG Pill 50 MG Solution Intravenous 10 [USP'U]/1mL Solution Intravenous 100 [USP'U]/1mL Gel Topical 30000 IE Ointment 30000 IE Gel Topical 150000 IE Gel Topical 200 IU Solution Intravenous; Subcutaneous 25000 unit / mL Solution Intravenous 10 unit / mL Solution Intravenous 100 unit / mL Injection, solution Intravenous 100 1/1mL Cream Topical 300 IU Cream Topical 600 IU Ointment 60000 IU Gel Topical 50000 IU Ointment 30000 IU Ointment 50000 IU Gel Topical 300 IU Solution / drops Ophthalmic Injection, solution Parenteral 100 I.E./ml Injection, solution Parenteral 1000 IE Injection, solution Parenteral 5000 IE Injection, solution Parenteral 5000 I.E./ml Injection Intravenous 1000 iu/ml Liquid Unknown 100 unit / mL Liquid Intravenous; Subcutaneous 10000 unit / mL Liquid Intravenous; Subcutaneous 1000 unit / mL Liquid Intravenous; Subcutaneous 25000 unit / mL Injection, solution Intravenous 10 [USP'U]/1mL Injection, solution Intravenous 100 [USP'U]/1mL Solution Intraperitoneal 10 unit / mL Solution Intravenous; Irrigation 10 unit / mL Solution Intravenous; Irrigation 100 unit / mL Injection, solution Parenteral 25000 IE Injection, solution Parenteral 25000 IE/5ML Injection, solution Parenteral 25000 IU/5mL Injection, solution Parenteral 5000 IU/0.2mL Injection, solution Parenteral 7500 IU/0.3mL Injection, solution Parenteral 250000 IU/10mL Injection, solution Parenteral 5000 IU Gel Topical 180000 IU Ointment 300 IU/g Ointment 600 IU/g Injection, solution Parenteral 25000 IU Injection Injection Intravenous; Subcutaneous 1000 Injection Intravenous; Subcutaneous 1000 [USP'U]/1mL Injection Intravenous; Subcutaneous 10000 Injection Intravenous; Subcutaneous 10000 [USP'U]/1mL Injection Intravenous; Subcutaneous 2000 [USP'U]/2mL Injection Intravenous; Subcutaneous 20000 [USP'U]/1mL Injection Intravenous; Subcutaneous 5000 [USP'U]/1mL Injection Intravenous; Subcutaneous 5000 [USP'U]/0.5mL Injection, solution Intravenous 0.5 [USP'U]/1mL Injection, solution Intravenous 1 [USP'U]/1mL Injection, solution Intravenous 2 [USP'U]/1mL Injection, solution Intravenous 200 [USP'U]/100mL Injection, solution Intravenous 30 [USP'U]/1mL Injection, solution Intravenous 4 [USP'U]/1mL Injection, solution Intravenous 40 [USP'U]/1mL Injection, solution Intravenous 5 [USP'U]/1mL Injection, solution Intravenous 50 [USP'U]/1mL Injection, solution Intravenous; Subcutaneous 1000 Injection, solution Intravenous; Subcutaneous 1000 [USP'U]/1mL Injection, solution Intravenous; Subcutaneous 10000 Injection, solution Intravenous; Subcutaneous 10000 [USP'U]/1mL Injection, solution Intravenous; Subcutaneous 2000 [USP'U]/2mL Injection, solution Intravenous; Subcutaneous 20000 [USP'U]/1mL Injection, solution Intravenous; Subcutaneous 5000 [USP'U]/0.5mL Injection, solution Intravenous; Subcutaneous 5000 [USP'U]/1mL Injection, solution Intravenous; Subcutaneous 5000 Injection, solution, concentrate Intravenous 10000 [USP'U]/5mL Injection, solution, concentrate Intravenous 12500 Injection, solution, concentrate Intravenous 20000 Injection, solution, concentrate Intravenous 25000 [USP'U]/10mL Solution Intravenous 40 unit / mL Solution Intravenous 50 unit / mL Liquid Intravenous Injection, solution Intravenous 1000 [iU]/500mL Injection, solution Intravenous 2000 [iU]/1000mL Solution Intravenous 2 unit / mL Solution Intravenous Injection Intravenous Injection, solution Intravenous 10000 [USP'U]/100mL Injection, solution Intravenous 4000 [USP'U]/100mL Injection, solution Intravenous 5000 [USP'U]/100mL Injection Intravenous 200 [USP'U]/100mL Solution Intravenous; Subcutaneous 5000 unit / mL Solution Subcutaneous 5000 unit / 0.5 mL Solution Intravenous; Subcutaneous 1000 unit / mL Solution Intravenous; Subcutaneous 10000 unit / mL Solution Intravenous 25000 iu/5ml Solution Intravenous 25000 IU Solution Parenteral 5000 U Solution Subcutaneous 1000 IU Solution Intravenous 5000 IU Solution Subcutaneous 5000 IU Solution Intravenous; Subcutaneous 5000 IU Solution Subcutaneous 5 IU Injection Intravenous 10 iu/ml Injection 5000 IU/5ml Injection Intravenous Cream Topical 30000 IU Cream Topical 60000 IU Gel Topical 0.3 g Solution Parenteral 1000.000 UI Injection, solution 25000 iu/5ml Gel Topical 1000 IE Gel Topical 100000 IU Gel Topical 2400 iu/g Gel Topical 100.000 UI Gel Topical 000 UI Injection 25000 iu Injection, solution Intravenous; Subcutaneous 25000 iu/5mL Injection, solution Intravenous 5000 IU/ml Injection, solution Intravenous; Parenteral 12500 UI/2.5ML Injection, solution Intravenous; Parenteral 5000 UI/1ML Injection, solution Parenteral; Subcutaneous 5000 UI/ML Injection, solution Subcutaneous 5000 IU/ml Paste Topical Injection, solution Intravenous; Parenteral 25000 IU/5ML Injection, solution Parenteral; Subcutaneous 5000 IU/ML Solution Intravenous; Subcutaneous 25000 iu/5ml Injection, solution Intramuscular Cream Rectal Solution Parenteral 5000 UI Injection, solution Parenteral 12500 IU/0.5ML Injection, solution Parenteral 12500 UI Injection, solution Parenteral 20000 UI Injection, solution Parenteral 5000 UI Injection, solution Parenteral 5000 UI/0.2ML Injection, solution 5000 iu/5ml Ointment Topical Injection, solution Parenteral; Subcutaneous 12500 UI/0.5ML Tablet Gel Topical 100000 IE Ointment 100000 IE Gel Topical 180000 IE Ointment 180000 IE Gel Topical 200 IU/G Gel Topical 20000 IU/100g Gel Topical 30000 IU/100g Cream Topical 600 IU/g Gel Topical 600 IU/g Pill Injection Intravenous; Subcutaneous 5000 IU/ML Tablet, film coated Gel Topical 60000 IU/100g Injection, solution Parenteral 5000 U.I./1ML Gel Topical 30000 IU Cream Topical Gel Topical Gel Topical 60000 IU Gel Topical 150.000 IE Spray Cutaneous 2400 IU/g Solution 5000 unit/1ml Injection, solution 5000 unit/1ml - Prices
Unit description Cost Unit Heparin sod 1000000 unit powder 1318.63USD each Heparin sod 100000 unit powder 256.73USD each Heparin Sodium (Porcine) 1000 unit/ml Solution 10ml Vial 188.99USD vial Heparin sod 25000 unit powder 58.8USD each Heparin Sodium (Porcine) 10000 unit/ml Solution 5ml Vial 29.99USD vial Heparin Sodium (Porcine) 10000 unit/ml vial 10.37USD vial Hep-lock flush 100 unit/ml kit 10.08USD kit Hep-lock flush 10 unit/ml kit 8.91USD kit Heparin Leo 25000 unit/ml 8.42USD ml Heparin sod 1000 unit/ml vial 7.92USD ml Heparin sod 5000 unit/ml syringe 3.08USD ml Heparin iv flush 100 unit/ml 2.71USD ml Hepalean 10000 unit/ml 2.32USD ml Heparin Leo 10000 unit/ml 2.03USD ml Heparin lock flush 10 unit/ml 1.21USD ml Heparin lock flush 100 unit/ml 1.13USD ml Hep-lock u-p 10 unit/ml vial 0.98USD ml Hepalean 1000 unit/ml 0.98USD ml Hep-lock u-p 100 unit/ml vial 0.96USD ml Heparin Leo 1000 unit/ml 0.43USD ml Heparin Leo 100 unit/ml Lock Flush 0.36USD ml Heparin Lock Flush 100 unit/ml Lock Flush 0.3USD ml Heparin Lock Flush 10 unit/ml Lock Flush 0.29USD ml Heparin iv flush 1 unit/ml syr 0.19USD ml Heparin iv flush 2 unit/ml syr 0.19USD ml Heparin lock 100 unit/ml vial 0.13USD ml Heparin lock 10 unit/ml vial 0.1USD ml Heparin-1/2ns 25000 unit/250 0.03USD ml Heparin-1/2ns 12500 unit/250 0.02USD ml Heparin-ns 2000 unit/1000 ml 0.01USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8541393 No 2004-11-02 2024-11-02 US US7696182 No 2005-05-16 2025-05-16 US US11738120 No 2022-04-15 2042-04-15 US US9339036 No 2004-11-02 2024-11-02 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Soluble Not Available logP -13.2 Not Available - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- General Function
- Serine-type endopeptidase inhibitor activity
- Specific Function
- Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade. AT-III inhibits thrombin, matriptase-3/TMPRSS7, as well as factors IXa, Xa and XIa. Its inhibitory a...
- Gene Name
- SERPINC1
- Uniprot ID
- P01008
- Uniprot Name
- Antithrombin-III
- Molecular Weight
- 52601.935 Da
References
- Mirow N, Zimmermann B, Maleszka A, Knobl H, Tenderich G, Koerfer R, Herberg FW: Plasma protein binding properties to immobilized heparin and heparin-albumin conjugate. Artif Organs. 2007 Jun;31(6):466-71. [Article]
- Sun W, Bandmann H, Schrader T: A fluorescent polymeric heparin sensor. Chemistry. 2007;13(27):7701-7. [Article]
- Pappalardo F, Franco A, Crescenzi G, De Simone F, Torracca L, Zangrillo A: Anticoagulation management in patients undergoing open heart surgery by activated clotting time and whole blood heparin concentration. Perfusion. 2006 Dec;21(5):285-90. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Chuang YJ, Swanson R, Raja SM, Olson ST: Heparin enhances the specificity of antithrombin for thrombin and factor Xa independent of the reactive center loop sequence. Evidence for an exosite determinant of factor Xa specificity in heparin-activated antithrombin. J Biol Chem. 2001 May 4;276(18):14961-71. Epub 2001 Feb 7. [Article]
- Petitou M, Herault JP, Bernat A, Driguez PA, Duchaussoy P, Lormeau JC, Herbert JM: Synthesis of thrombin-inhibiting heparin mimetics without side effects. Nature. 1999 Apr 1;398(6726):417-22. [Article]
- Schedin-Weiss S, Richard B, Olson ST: Kinetic evidence that allosteric activation of antithrombin by heparin is mediated by two sequential conformational changes. Arch Biochem Biophys. 2010 Dec 15;504(2):169-76. doi: 10.1016/j.abb.2010.08.021. Epub 2010 Sep 15. [Article]
- Gettins PG, Olson ST: Activation of antithrombin as a factor IXa and Xa inhibitor involves mitigation of repression rather than positive enhancement. FEBS Lett. 2009 Nov 3;583(21):3397-400. doi: 10.1016/j.febslet.2009.10.005. Epub 2009 Oct 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serine-type endopeptidase activity
- Specific Function
- Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.
- Gene Name
- F10
- Uniprot ID
- P00742
- Uniprot Name
- Coagulation factor X
- Molecular Weight
- 54731.255 Da
References
- Ignjatovic V, Summerhayes R, Gan A, Than J, Chan A, Cochrane A, Bennett M, Horton S, Shann F, Lane G, Ross-Smith M, Monagle P: Monitoring Unfractionated Heparin (UFH) therapy: which Anti-Factor Xa assay is appropriate? Thromb Res. 2007;120(3):347-51. Epub 2006 Nov 21. [Article]
- Patey SJ, Edwards EA, Yates EA, Turnbull JE: Heparin derivatives as inhibitors of BACE-1, the Alzheimer's beta-secretase, with reduced activity against factor Xa and other proteases. J Med Chem. 2006 Oct 5;49(20):6129-32. [Article]
- Rezaie AR: Heparin-binding exosite of factor Xa. Trends Cardiovasc Med. 2000 Nov;10(8):333-8. [Article]
- Rosenberg RD: Role of heparin and heparinlike molecules in thrombosis and atherosclerosis. Fed Proc. 1985 Feb;44(2):404-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sialic acid binding
- Specific Function
- Ca(2+)-dependent receptor for myeloid cells that binds to carbohydrates on neutrophils and monocytes. Mediates the interaction of activated endothelial cells or platelets with leukocytes. The ligan...
- Gene Name
- SELP
- Uniprot ID
- P16109
- Uniprot Name
- P-selectin
- Molecular Weight
- 90833.105 Da
References
- Simonis D, Fritzsche J, Alban S, Bendas G: Kinetic analysis of heparin and glucan sulfates binding to P-selectin and its impact on the general understanding of selectin inhibition. Biochemistry. 2007 May 22;46(20):6156-64. Epub 2007 Apr 26. [Article]
- Maugeri N, Di Fabio G, Barbanti M, de Gaetano G, Donati MB, Cerletti C: Parnaparin, a low-molecular-weight heparin, prevents P-selectin-dependent formation of platelet-leukocyte aggregates in human whole blood. Thromb Haemost. 2007 Jun;97(6):965-73. [Article]
- Simonis D, Christ K, Alban S, Bendas G: Affinity and kinetics of different heparins binding to P- and L-selectin. Semin Thromb Hemost. 2007 Jul;33(5):534-9. [Article]
- Asberg AE, Videm V: Inhibition of platelet receptors involved in neutrophil-platelet interaction in model cardiopulmonary bypass. Artif Organs. 2007 Aug;31(8):617-26. [Article]
- Gao Y, Li N, Fei R, Chen Z, Zheng S, Zeng X: P-Selectin-mediated acute inflammation can be blocked by chemically modified heparin, RO-heparin. Mol Cells. 2005 Jun 30;19(3):350-5. [Article]
- Koenig A, Norgard-Sumnicht K, Linhardt R, Varki A: Differential interactions of heparin and heparan sulfate glycosaminoglycans with the selectins. Implications for the use of unfractionated and low molecular weight heparins as therapeutic agents. J Clin Invest. 1998 Feb 15;101(4):877-89. [Article]
- Nelson RM, Cecconi O, Roberts WG, Aruffo A, Linhardt RJ, Bevilacqua MP: Heparin oligosaccharides bind L- and P-selectin and inhibit acute inflammation. Blood. 1993 Dec 1;82(11):3253-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays a role in the regulation of cell proliferation, differentiation and migration, and in regulation o...
- Gene Name
- FGFR4
- Uniprot ID
- P22455
- Uniprot Name
- Fibroblast growth factor receptor 4
- Molecular Weight
- 87953.535 Da
References
- Loo BM, Kreuger J, Jalkanen M, Lindahl U, Salmivirta M: Binding of heparin/heparan sulfate to fibroblast growth factor receptor 4. J Biol Chem. 2001 May 18;276(20):16868-76. Epub 2001 Feb 21. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Heparin binding
- Specific Function
- Plays an important role in the regulation of embryonic development, cell proliferation, and cell differentiation. Required for normal limb and cardiac valve development during embryogenesis.
- Gene Name
- FGF4
- Uniprot ID
- P08620
- Uniprot Name
- Fibroblast growth factor 4
- Molecular Weight
- 22047.355 Da
References
- Bellosta P, Iwahori A, Plotnikov AN, Eliseenkova AV, Basilico C, Mohammadi M: Identification of receptor and heparin binding sites in fibroblast growth factor 4 by structure-based mutagenesis. Mol Cell Biol. 2001 Sep;21(17):5946-57. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Fibroblast growth factor receptor binding
- Specific Function
- Involved in the suppression of bile acid biosynthesis through down-regulation of CYP7A1 expression, following positive regulation of the JNK and ERK1/2 cascades. Stimulates glucose uptake in adipoc...
- Gene Name
- FGF19
- Uniprot ID
- O95750
- Uniprot Name
- Fibroblast growth factor 19
- Molecular Weight
- 24002.345 Da
References
- Harmer NJ, Pellegrini L, Chirgadze D, Fernandez-Recio J, Blundell TL: The crystal structure of fibroblast growth factor (FGF) 19 reveals novel features of the FGF family and offers a structural basis for its unusual receptor affinity. Biochemistry. 2004 Jan 27;43(3):629-40. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation ...
- Gene Name
- FGFR1
- Uniprot ID
- P11362
- Uniprot Name
- Fibroblast growth factor receptor 1
- Molecular Weight
- 91866.935 Da
References
- Ibrahimi OA, Zhang F, Hrstka SC, Mohammadi M, Linhardt RJ: Kinetic model for FGF, FGFR, and proteoglycan signal transduction complex assembly. Biochemistry. 2004 Apr 27;43(16):4724-30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- S100 protein binding
- Specific Function
- Plays an important role in the regulation of cell survival, cell division, angiogenesis, cell differentiation and cell migration. Functions as potent mitogen in vitro.
- Gene Name
- FGF1
- Uniprot ID
- P05230
- Uniprot Name
- Fibroblast growth factor 1
- Molecular Weight
- 17459.58 Da
References
- Robinson CJ, Harmer NJ, Goodger SJ, Blundell TL, Gallagher JT: Cooperative dimerization of fibroblast growth factor 1 (FGF1) upon a single heparin saccharide may drive the formation of 2:2:1 FGF1.FGFR2c.heparin ternary complexes. J Biol Chem. 2005 Dec 23;280(51):42274-82. Epub 2005 Oct 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosi...
- Gene Name
- FGFR2
- Uniprot ID
- P21802
- Uniprot Name
- Fibroblast growth factor receptor 2
- Molecular Weight
- 92024.29 Da
References
- Robinson CJ, Harmer NJ, Goodger SJ, Blundell TL, Gallagher JT: Cooperative dimerization of fibroblast growth factor 1 (FGF1) upon a single heparin saccharide may drive the formation of 2:2:1 FGF1.FGFR2c.heparin ternary complexes. J Biol Chem. 2005 Dec 23;280(51):42274-82. Epub 2005 Oct 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Ligand-dependent nuclear receptor transcription coactivator activity
- Specific Function
- Plays an important role in the regulation of cell survival, cell division, angiogenesis, cell differentiation and cell migration. Functions as potent mitogen in vitro.
- Gene Name
- FGF2
- Uniprot ID
- P09038
- Uniprot Name
- Fibroblast growth factor 2
- Molecular Weight
- 30769.715 Da
References
- Rose K, Kriha D, Pallast S, Junker V, Klumpp S, Krieglstein J: Basic fibroblast growth factor: lysine 134 is essential for its neuroprotective activity. Neurochem Int. 2007 Jul;51(1):25-31. Epub 2007 Apr 19. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Heparin binding
- Specific Function
- Released during platelet aggregation. Neutralizes the anticoagulant effect of heparin because it binds more strongly to heparin than to the chondroitin-4-sulfate chains of the carrier molecule. Che...
- Gene Name
- PF4
- Uniprot ID
- P02776
- Uniprot Name
- Platelet factor 4
- Molecular Weight
- 10844.78 Da
References
- Greinacher A, Althaus K, Krauel K, Selleng S: Heparin-induced thrombocytopenia. Hamostaseologie. 2010 Jan;30(1):17-8, 20-8. [Article]
- Visentin GP, Ford SE, Scott JP, Aster RH: Antibodies from patients with heparin-induced thrombocytopenia/thrombosis are specific for platelet factor 4 complexed with heparin or bound to endothelial cells. J Clin Invest. 1994 Jan;93(1):81-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Serine-type endopeptidase activity
- Specific Function
- Potent mitogen for mature parenchymal hepatocyte cells, seems to be a hepatotrophic factor, and acts as a growth factor for a broad spectrum of tissues and cell types. Activating ligand for the rec...
- Gene Name
- HGF
- Uniprot ID
- P14210
- Uniprot Name
- Hepatocyte growth factor
- Molecular Weight
- 83133.115 Da
References
- Sakata H, Stahl SJ, Taylor WG, Rosenberg JM, Sakaguchi K, Wingfield PT, Rubin JS: Heparin binding and oligomerization of hepatocyte growth factor/scatter factor isoforms. Heparan sulfate glycosaminoglycan requirement for Met binding and signaling. J Biol Chem. 1997 Apr 4;272(14):9457-63. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Syndecan binding
- Specific Function
- Endoglycosidase that cleaves heparan sulfate proteoglycans (HSPGs) into heparan sulfate side chains and core proteoglycans. Participates in extracellular matrix (ECM) degradation and remodeling. Se...
- Gene Name
- HPSE
- Uniprot ID
- Q9Y251
- Uniprot Name
- Heparanase
- Molecular Weight
- 61148.17 Da
References
- Wang B, Jia J, Zhang X, Zcharia E, Vlodavsky I, Pejler G, Li JP: Heparanase affects secretory granule homeostasis of murine mast cells through degrading heparin. J Allergy Clin Immunol. 2011 Dec;128(6):1310-1317.e8. doi: 10.1016/j.jaci.2011.04.011. Epub 2011 May 14. [Article]
- Nadir Y, Brenner B: Heparanase procoagulant effects and inhibition by heparins. Thromb Res. 2010 Apr;125 Suppl 2:S72-6. doi: 10.1016/S0049-3848(10)70018-9. [Article]
- Levy-Adam F, Feld S, Suss-Toby E, Vlodavsky I, Ilan N: Heparanase facilitates cell adhesion and spreading by clustering of cell surface heparan sulfate proteoglycans. PLoS One. 2008 Jun 11;3(6):e2319. doi: 10.1371/journal.pone.0002319. [Article]
- Vlodavsky I, Ilan N, Naggi A, Casu B: Heparanase: structure, biological functions, and inhibition by heparin-derived mimetics of heparan sulfate. Curr Pharm Des. 2007;13(20):2057-73. [Article]
- Katz BZ, Muhl L, Zwang E, Ilan N, Herishanu Y, Deutsch V, Naparstek E, Vlodavsky I, Preissner KT: Heparanase modulates heparinoids anticoagulant activities via non-enzymatic mechanisms. Thromb Haemost. 2007 Dec;98(6):1193-9. [Article]
- Nasser NJ, Sarig G, Brenner B, Nevo E, Goldshmidt O, Zcharia E, Li JP, Vlodavsky I: Heparanase neutralizes the anticoagulation properties of heparin and low-molecular-weight heparin. J Thromb Haemost. 2006 Mar;4(3):560-5. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54