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Identification
NameHeparin
Accession NumberDB01109  (APRD00056)
TypeSmall Molecule
GroupsApproved, Investigational
Description

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.

Structure
Thumb
Synonyms
Calciparine
Eparina
Hep-lock
Heparinate
Heparinic acid
Liquaemin
Panheprin
Unfractionated heparin
External Identifiers
  • CY216
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Calcilean Inj 20000unit/0.8mlliquid20000 unitsubcutaneousOrganon Teknika Canada Inc.1987-12-311997-08-11Canada
Calciparine Inj 20000iu/ampliquid20000 unitChoay Lab1974-12-311998-06-09Canada
Calciparine Inj 5000iuliquid5000 unitChoay Lab1977-12-311998-06-09Canada
Hepalean 10,000 USPsolution10000 unitintravenous; subcutaneousSchering Plough Canada Inc1987-12-312011-11-30Canada
Hepalean 1000 USPsolution1000 unitintravenous; subcutaneousSchering Plough Canada Inc1987-12-312011-11-30Canada
Hepalean 25,000 USPsolution25000 unitintravenous; subcutaneousSchering Plough Canada Inc1987-12-312011-11-30Canada
Hepalean-lok 10 USPsolution10 unitintravenousSchering Plough Canada Inc1997-04-072010-02-09Canada
Hepalean-lok 100 USPsolution100 unitintravenousSchering Plough Canada Inc1988-12-312011-11-30Canada
Heparin Leo 100unit/mlliquid100 unitirrigationLeo Pharma Inc1984-12-31Not applicableCanada
Heparin Leo Inj 10000unit/mlliquid10000 unitintravenous; subcutaneousLeo Pharma Inc1984-12-312015-07-02Canada
Heparin Leo Inj 1000unit/mlliquid1000 unitintravenous; subcutaneousLeo Pharma Inc1987-12-31Not applicableCanada
Heparin Leo Inj 25000unit/mlliquid25000 unitintravenous; subcutaneousLeo Pharma Inc1987-12-312013-03-31Canada
Heparin Lock Flushsolution100 [USP'U]/mLintravenousGeneral Injectables & Vaccines, Inc2010-08-012016-04-05Us
Heparin Lock Flushsolution10 [USP'U]/mLintravenousGeneral Injectables & Vaccines, Inc2010-08-012016-04-05Us
Heparin Lock Flushinjection, solution10 [USP'U]/mLintravenousAPP Pharmaceuticals, LLC2009-08-292016-04-05Us
Heparin Lock Flushinjection, solution100 [USP'U]/mLintravenousAPP Pharmaceuticals, LLC2009-08-122016-04-05Us
Heparin Lock Flush Solution Inj 10unit/mlsolution10 unitintraperitonealHospira Healthcare Corporation1986-12-312012-08-03Canada
Heparin Lock Flush Solution Injection USPsolution100 unitirrigation; intravenousHospira Healthcare Corporation1989-12-31Not applicableCanada
Heparin Lock Flush Solution Injection USPsolution10 unitirrigation; intravenousHospira Healthcare Corporation1989-12-31Not applicableCanada
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousPfizer Laboratories Div Pfizer Inc2011-07-212016-04-23Us
Heparin Sodiuminjection, solution2 [USP'U]/mLintravenousCantrell Drug Company2012-08-292016-04-05Us
Heparin Sodiuminjection, solution30 [USP'U]/mLintravenousCantrell Drug Company2013-11-222016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/100mLintravenousHospira, Inc.1989-01-252016-04-23Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousCardinal Health2010-06-182016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousGeneral Injectables & Vaccines, Inc2010-08-012016-04-05Us
Heparin Sodiuminjection, solution100 [USP'U]/mLintravenousCantrell Drug Company2012-08-292016-04-05Us
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-06-182016-04-05Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousCardinal Health2010-06-182016-04-05Us
Heparin Sodiuminjection, solution4000 [USP'U]/100mLintravenousHospira, Inc.1989-01-252016-04-23Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousCardinal Health2010-06-182016-04-05Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2009-08-122016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/100mLintravenousHospira, Inc.1984-01-312016-04-23Us
Heparin Sodiuminjection, solution4 [USP'U]/mLintravenousCantrell Drug Company2012-05-092016-04-05Us
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-03-222016-04-23Us
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2011-04-252016-04-05Us
Heparin Sodiuminjection, solution10000 [USP'U]/100mLintravenousHospira, Inc.1984-01-312016-04-23Us
Heparin Sodiuminjection, solution50 [USP'U]/mLintravenousCantrell Drug Company2012-08-092016-04-05Us
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-03-222016-04-23Us
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousCardinal Health2010-06-182016-04-05Us
Heparin Sodiuminjection, solution200 [USP'U]/100mLintravenousHospira, Inc.1984-01-312016-04-23Us
Heparin Sodiuminjection, solution10 [USP'U]/mLintravenousCantrell Drug Company2011-11-072016-04-05Us
Heparin Sodiuminjection10000 [USP'U]/mLintravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-03-222016-04-23Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousCardinal Health2010-06-182016-04-05Us
Heparin Sodiuminjection, solution50 [USP'U]/mLintravenousCantrell Drug Company2012-12-212016-04-05Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-06-182016-04-05Us
Heparin Sodiuminjection, solution, concentrate25000 [USP'U]/10mLintravenousHospira, Inc.2010-10-222016-04-23Us
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousPfizer Laboratories Div Pfizer Inc2013-03-112016-04-23Us
Heparin Sodiuminjection, solution1 [USP'U]/mLintravenousCantrell Drug Company2011-02-222016-04-05Us
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-03-222016-04-23Us
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousCardinal Health2011-07-212016-04-05Us
Heparin Sodiuminjection, solution40 [USP'U]/mLintravenousCantrell Drug Company2014-04-082016-04-05Us
Heparin Sodiuminjection, solution20000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-06-182016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2009-08-122016-04-05Us
Heparin Sodiuminjection, solution, concentrate10000 [USP'U]/5mLintravenousHospira, Inc.2010-10-222016-04-23Us
Heparin Sodiuminjection10000 [USP'U]/mLintravenous; subcutaneousPfizer Laboratories Div Pfizer Inc2011-07-212016-04-23Us
Heparin Sodiuminjection, solution10 [USP'U]/mLintravenousCantrell Drug Company2011-06-302016-04-05Us
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-03-222016-04-23Us
Heparin Sodiuminjection, solution, concentrate10000 [USP'U]/5mLintravenousGeneral Injectables & Vaccines, Inc2010-03-012016-04-05Us
Heparin Sodiuminjection, solution4 [USP'U]/mLintravenousCantrell Drug Company2012-11-132016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-06-182016-04-05Us
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousPfizer Laboratories Div Pfizer Inc2011-07-212016-04-23Us
Heparin Sodiuminjection, solution5 [USP'U]/mLintravenousCantrell Drug Company2012-05-092016-04-05Us
Heparin Sodiuminjection, solution100000 [USP'U]/mLintravenous; subcutaneousGeneral Injectables & Vaccines, Inc2010-03-012016-04-05Us
Heparin Sodiuminjection, solution100 [USP'U]/mLintravenousCantrell Drug Company2015-05-152016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousCardinal Health2009-08-122016-04-05Us
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousPfizer Laboratories Div Pfizer Inc2011-07-212016-04-23Us
Heparin Sodiuminjection, solution5 [USP'U]/mLintravenousCantrell Drug Company2011-02-182016-04-05Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousGeneral Injectables & Vaccines, Inc2010-08-012016-04-05Us
Heparin Sodiuminjection, solution.5 [USP'U]/mLintravenousCantrell Drug Company2012-03-222016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/.5mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-12-032016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/.5mLintravenous; subcutaneousCardinal Health2010-06-182016-04-05Us
Heparin Sodium 20000unit/500ml In Dext 5% Injsolution40 unitintravenousHospira Healthcare Corporation1991-12-31Not applicableCanada
Heparin Sodium 25000unit/500ml In 5% Dextr Injsolution50 unitintravenousHospira Healthcare Corporation1991-12-31Not applicableCanada
Heparin Sodium 5000unit/500ml In Sodium Chloride 0.9%solution10 unitintravenousHospira Healthcare Corporation1998-06-05Not applicableCanada
Heparin Sodium and Dextroseinjection, solution5000 [USP'U]/100mLintravenousHospira, Inc.1985-03-272016-04-23Us
Heparin Sodium and Dextroseinjection, solution10000 [USP'U]/100mLintravenousHospira, Inc.1985-03-272016-04-23Us
Heparin Sodium and Sodium Chlorideinjection, solution200 [USP'U]/100mLintravenousBaxter Healthcare Corporation1982-04-282016-04-23Us
Heparin Sodium and Sodium Chlorideinjection, solution200 [USP'U]/100mLintravenousBaxter Healthcare Corporation1982-04-282016-04-23Us
Heparin Sodium In Dextroseinjection, solution4000 [USP'U]/100mLintravenousBaxter Healthcare Corporation2010-12-312016-04-23Us
Heparin Sodium In Dextroseinjection, solution10000 [USP'U]/100mLintravenousBaxter Healthcare Corporation2010-12-312016-04-23Us
Heparin Sodium In Dextroseinjection, solution5000 [USP'U]/100mLintravenousBaxter Healthcare Corporation2010-12-312016-04-23Us
Heparin Sodium In Sodium Chlorideinjection200 [USP'U]/100mLintravenousB. Braun Medical Inc.1992-07-202016-04-23Us
Heparin Sodium Injection USPsolution5000 unitintravenous; subcutaneousPfizer Canada IncNot applicableNot applicableCanada
Heparin Sodium Injection USPsolution1000 unitintravenous; subcutaneousPfizer Canada IncNot applicableNot applicableCanada
Heparin Sodium Injection USPsolution5000 unitintravenous; subcutaneousPfizer Canada Inc2013-03-012015-06-01Canada
Heparin Sodium Injection USPsolution10000 unitintravenous; subcutaneousPfizer Canada Inc2013-03-01Not applicableCanada
Heparin Sodium Injection USPsolution1000 unitintravenous; subcutaneousPfizer Canada Inc2013-03-01Not applicableCanada
Heparin Sodium Injection USP (single Use Vial-preservative Free)solution10000 unitintravenous; subcutaneousSandoz Canada Incorporated2008-05-19Not applicableCanada
Heparin Sodium Injection USP (multidose Vial-with Preservative)solution1000 unitintravenous; subcutaneousSandoz Canada Incorporated2008-05-19Not applicableCanada
Heparin Sodium Injection USP (multidose Vial-with Preservative)solution10000 unitintravenous; subcutaneousSandoz Canada Incorporated2008-05-19Not applicableCanada
Heparin Sodium Injection, USPsolution10000 unitintravenous; subcutaneousFresenius Kabi Canada Ltd2005-05-27Not applicableCanada
Heparin Sodium Injection, USPsolution10000 unitintravenous; subcutaneousFresenius Kabi Canada Ltd2013-05-20Not applicableCanada
Heparin Sodium Injection, USPsolution1000 unitintravenous; subcutaneousFresenius Kabi Canada Ltd2005-05-26Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousCardinal Health2009-08-312016-04-05Us
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousCardinal Health2010-07-062016-04-05Us
Heparin Sodiuminjection10000 [USP'U]/mLintravenous; subcutaneousSagent Pharmaceticals2010-07-062016-04-05Us
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.1987-05-042016-04-23Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-122016-04-05Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-122016-04-05Us
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousCardinal Health2010-07-062016-04-05Us
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousSagent Pharmaceticals2010-07-062016-04-05Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-122016-04-05Us
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousCardinal Health2009-12-072016-04-05Us
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousSagent Pharmaceticals2010-07-062016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-122016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousGeneral Injectables & Vaccines, Inc2011-09-132016-04-05Us
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousSagent Pharmaceticals2010-07-062016-04-05Us
Heparin Sodiuminjection, solution20000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-122016-04-05Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-122016-04-05Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousGeneral Injectables & Vaccines, Inc2011-09-132016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.2009-08-312016-04-23Us
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-122016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousCardinal Health2005-01-312016-04-05Us
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousSafecor Health, LLC2014-09-302016-04-05Us
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.2009-08-312016-04-23Us
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-122016-04-05Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousCardinal Health2009-08-312016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousSafecor Health, LLC2014-09-302016-04-05Us
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.2009-08-312016-04-23Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-122016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousCardinal Health2009-08-312016-04-05Us
Heparin Sodiuminjection20000 [USP'U]/mLintravenous; subcutaneousSagent Pharmaceuticals2010-07-062016-04-05Us
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.2005-01-312016-04-23Us
Over the Counter ProductsNot Available
International Brands
NameCompany
CalcileanNot Available
CalciparineNot Available
HepaleanNot Available
Heparin LEONot Available
LiquaeminNot Available
LiqueminNot Available
MultiparinNot Available
NovoheparinNot Available
Brand mixtures
NameLabellerIngredients
Heparin Sod and 0.9% Sod Chloride InjBaxter Corporation
Heparin Sodium & 5% Dextrose Injection LiqBaxter Corporation
Heparin Sodium & Dextrose 5% In Viaflex LiqBaxter Corporation
Heparin Sodium 1000units In 0.9% Sodium Chloride Injection USPB. Braun Medical Inc
Heparin Sodium 20000units In 5% Dextrose InjB. Braun Medical Inc
Heparin Sodium 25000units In 5% Dextrose InjB. Braun Medical Inc
Heparin Sodium and Dextrose 5% Inj USPBaxter Corporation
Heparin Sodium In .9% Sodium Chloride InjectionHospira Healthcare Corporation
Heparin Sodium In 5% Dextrose Injection, 25000unit/500mlB. Braun Medical Inc
Salts
Name/CASStructureProperties
Heparin calcium
ThumbNot applicableDBSALT001434
Heparin sodium
ThumbNot applicableDBSALT000417
Categories
UNII1K5KDI46KZ
CAS number9005-49-6
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Taxonomy
ClassificationNot classified
Pharmacology
IndicationUnfractionated 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.
PharmacodynamicsUnfractionated 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 actionUnder 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.
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AbsorptionHeparin must be given parenterally as it is not absorbed through the gastrointestinal mucosa. It is usually given by iv infusion or deep sc injection. The onset of action is immediate after iv injection but can be delayed 20 to 60 minutes following sc injection. 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.
Volume of distribution

40-70 mL/min (approximately the same as blood volume)
Although heparin does not distribute into adipose tissues, clinicians should use actual body weight in obese patients to account for extra vasculature.

Protein bindingVery high, mostly to low-density lipoproteins. It is also extensively bound by globulins and fibrinogens.
Metabolism

Liver and the reticulo-endothelial system are the sites of biotransformation. The metabolic fate of heparin is not well understood.

Route of eliminationThe drug appears to be removed mainly by the reticuloendothelial system. A small fraction of unchanged heparin also appears to be excreted in urine. Heparin cannot be eliminated by hemodialysis.
Half life1.5 hours. The plasma half-life of heparin increases from about 60 minutes with a 100 unit/kg dose to about 150 minutes with a 400 unit/kg dose.
Clearance

Adult Clearance = 0.43 ml/kg/min
25-28 weeks gestation = 1.49 ml/kg/min

ToxicityIn 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.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Heparin Action PathwayDrug actionSMP00274
Fc Epsilon Receptor I Signaling in Mast CellsSignalingSMP00358
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Liquidsubcutaneous20000 unit
Liquid20000 unit
Liquid5000 unit
Solutionintravenous; subcutaneous25000 unit
Solutionintravenous100 unit
Liquidirrigation100 unit
Liquidintravenous; subcutaneous10000 unit
Liquidintravenous; subcutaneous1000 unit
Liquidintravenous; subcutaneous25000 unit
Solutionintravenous10 [USP'U]/mL
Solutionintravenous100 [USP'U]/mL
Solutionintraperitoneal10 unit
Solutionirrigation; intravenous10 unit
Solutionirrigation; intravenous100 unit
Solutionintravenous
Injectionintravenous; subcutaneous1000 [USP'U]/mL
Injectionintravenous; subcutaneous10000 [USP'U]/mL
Injectionintravenous; subcutaneous20000 [USP'U]/mL
Injectionintravenous; subcutaneous5000 [USP'U]/mL
Injection, solutionintravenous.5 [USP'U]/mL
Injection, solutionintravenous1 [USP'U]/mL
Injection, solutionintravenous10 [USP'U]/mL
Injection, solutionintravenous100 [USP'U]/mL
Injection, solutionintravenous2 [USP'U]/mL
Injection, solutionintravenous30 [USP'U]/mL
Injection, solutionintravenous4 [USP'U]/mL
Injection, solutionintravenous40 [USP'U]/mL
Injection, solutionintravenous5 [USP'U]/mL
Injection, solutionintravenous50 [USP'U]/mL
Injection, solutionintravenous; subcutaneous1000 [USP'U]/mL
Injection, solutionintravenous; subcutaneous10000 [USP'U]/mL
Injection, solutionintravenous; subcutaneous100000 [USP'U]/mL
Injection, solutionintravenous; subcutaneous20000 [USP'U]/mL
Injection, solutionintravenous; subcutaneous5000 [USP'U]/.5mL
Injection, solutionintravenous; subcutaneous5000 [USP'U]/mL
Injection, solution, concentrateintravenous10000 [USP'U]/5mL
Injection, solution, concentrateintravenous25000 [USP'U]/10mL
Solutionintravenous40 unit
Solutionintravenous50 unit
Solutionintravenous10 unit
Liquidintravenous
Injection, solutionintravenous200 [USP'U]/100mL
Injection, solutionintravenous10000 [USP'U]/100mL
Injection, solutionintravenous4000 [USP'U]/100mL
Injection, solutionintravenous5000 [USP'U]/100mL
Injectionintravenous200 [USP'U]/100mL
Solutionintravenous; subcutaneous5000 unit
Solutionintravenous; subcutaneous10000 unit
Solutionintravenous; subcutaneous1000 unit
Prices
Unit descriptionCostUnit
Heparin sod 1000000 unit powder1318.63USD each
Heparin sod 100000 unit powder256.73USD each
Heparin Sodium (Porcine) 1000 unit/ml Solution 10ml Vial188.99USD vial
Heparin sod 25000 unit powder58.8USD each
Heparin Sodium (Porcine) 10000 unit/ml Solution 5ml Vial29.99USD vial
Heparin Sodium (Porcine) 10000 unit/ml vial10.37USD vial
Hep-lock flush 100 unit/ml kit10.08USD kit
Hep-lock flush 10 unit/ml kit8.91USD kit
Heparin Leo 25000 unit/ml8.42USD ml
Heparin sod 1000 unit/ml vial7.92USD ml
Heparin sod 5000 unit/ml syringe3.08USD ml
Heparin iv flush 100 unit/ml2.71USD ml
Hepalean 10000 unit/ml2.32USD ml
Heparin Leo 10000 unit/ml2.03USD ml
Heparin lock flush 10 unit/ml1.21USD ml
Heparin lock flush 100 unit/ml1.13USD ml
Hep-lock u-p 10 unit/ml vial0.98USD ml
Hepalean 1000 unit/ml0.98USD ml
Hep-lock u-p 100 unit/ml vial0.96USD ml
Heparin Leo 1000 unit/ml0.43USD ml
Heparin Leo 100 unit/ml Lock Flush0.36USD ml
Heparin Lock Flush 100 unit/ml Lock Flush0.3USD ml
Heparin Lock Flush 10 unit/ml Lock Flush0.29USD ml
Heparin iv flush 1 unit/ml syr0.19USD ml
Heparin iv flush 2 unit/ml syr0.19USD ml
Heparin lock 100 unit/ml vial0.13USD ml
Heparin lock 10 unit/ml vial0.1USD ml
Heparin-1/2ns 25000 unit/2500.03USD ml
Heparin-1/2ns 12500 unit/2500.02USD ml
Heparin-ns 2000 unit/1000 ml0.01USD ml
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PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySolubleNot Available
logP-13.2Not Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
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
  1. Linhardt RJ, Gunay NS: Production and chemical processing of low molecular weight heparins. Semin Thromb Hemost. 1999;25 Suppl 3:5-16. [PubMed:10549711 ]
  2. 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. [PubMed:2331699 ]
  3. 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. [PubMed:8352752 ]
  4. 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. [PubMed:15383472 ]
  5. 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. [PubMed:10201371 ]
  6. 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. [PubMed:11760916 ]
  7. McDonald MM, Jacobson LJ, Hay WW Jr, Hathaway WE: Heparin clearance in the newborn. Pediatr Res. 1981 Jul;15(7):1015-8. [PubMed:7254945 ]
  8. Authors unspecified: Benzyl alcohol: toxic agent in neonatal units. Pediatrics. 1983 Sep;72(3):356-8. [PubMed:6889041 ]
  9. Authors unspecified: Benzyl alcohol may be toxic to newborns. FDA Drug Bull. 1982 Aug;12(2):10-1. [PubMed:7188569 ]
  10. Authors unspecified: Neonatal deaths associated with use of benzyl alcohol--United States. MMWR Morb Mortal Wkly Rep. 1982 Jun 11;31(22):290-1. [PubMed:6810084 ]
External Links
ATC CodesB01AB01B01AB51C05BA03C05BA53S01XA14
AHFS Codes
  • 20:12.04.16
  • 92:00.00
PDB Entries
FDA labelDownload (198 KB)
MSDSDownload (72.1 KB)
Interactions
Drug Interactions
Drug
AbciximabAbciximab may increase the anticoagulant activities of Heparin.
AcenocoumarolAcenocoumarol may increase the anticoagulant activities of Heparin.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Heparin.
AliskirenHeparin may increase the hyperkalemic activities of Aliskiren.
AlteplaseAlteplase may increase the anticoagulant activities of Heparin.
AmilorideHeparin may increase the hyperkalemic activities of Amiloride.
Aminosalicylic AcidAminosalicylic Acid may increase the anticoagulant activities of Heparin.
AnagrelideAnagrelide may increase the anticoagulant activities of Heparin.
AnistreplaseAnistreplase may increase the anticoagulant activities of Heparin.
ApixabanApixaban may increase the anticoagulant activities of Heparin.
ArgatrobanHeparin may increase the anticoagulant activities of Argatroban.
Azilsartan medoxomilHeparin may increase the hyperkalemic activities of Azilsartan medoxomil.
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Heparin.
BenazeprilHeparin may increase the hyperkalemic activities of Benazepril.
Bismuth SubsalicylateBismuth Subsalicylate may increase the anticoagulant activities of Heparin.
BivalirudinHeparin may increase the anticoagulant activities of Bivalirudin.
CaffeineCaffeine may increase the anticoagulant activities of Heparin.
CanagliflozinHeparin may increase the hyperkalemic activities of Canagliflozin.
CandesartanHeparin may increase the hyperkalemic activities of Candesartan.
CangrelorCangrelor may increase the anticoagulant activities of Heparin.
CaptoprilHeparin may increase the hyperkalemic activities of Captopril.
CelecoxibCelecoxib may increase the anticoagulant activities of Heparin.
ChlorotrianiseneChlorotrianisene may decrease the anticoagulant activities of Heparin.
CilazaprilHeparin may increase the hyperkalemic activities of Cilazapril.
CilostazolCilostazol may increase the anticoagulant activities of Heparin.
CitalopramCitalopram may increase the anticoagulant activities of Heparin.
Citric AcidCitric Acid may increase the anticoagulant activities of Heparin.
ClopidogrelClopidogrel may increase the anticoagulant activities of Heparin.
CollagenaseThe risk or severity of adverse effects can be increased when Heparin is combined with Collagenase.
Collagenase clostridium histolyticumThe risk or severity of adverse effects can be increased when Heparin is combined with Collagenase clostridium histolyticum.
Corticorelin ovine triflutateThe risk or severity of adverse effects can be increased when Heparin is combined with Corticorelin.
Cyproterone acetateThe therapeutic efficacy of Heparin can be decreased when used in combination with Cyproterone acetate.
Dabigatran etexilateDabigatran etexilate may increase the anticoagulant activities of Heparin.
DalteparinDalteparin may increase the anticoagulant activities of Heparin.
DanaparoidHeparin may increase the anticoagulant activities of Danaparoid.
DasatinibDasatinib may increase the anticoagulant activities of Heparin.
DeferasiroxThe risk or severity of adverse effects can be increased when Heparin is combined with Deferasirox.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Heparin is combined with Deoxycholic Acid.
DesirudinHeparin may increase the anticoagulant activities of Desirudin.
DesogestrelThe therapeutic efficacy of Heparin can be decreased when used in combination with Desogestrel.
DesvenlafaxineDesvenlafaxine may increase the anticoagulant activities of Heparin.
DiclofenacDiclofenac may increase the anticoagulant activities of Heparin.
DicoumarolDicoumarol may increase the anticoagulant activities of Heparin.
DienogestThe therapeutic efficacy of Heparin can be decreased when used in combination with Dienogest.
DiflunisalDiflunisal may increase the anticoagulant activities of Heparin.
DihydrocodeineDihydrocodeine may increase the anticoagulant activities of Heparin.
DipyridamoleDipyridamole may increase the anticoagulant activities of Heparin.
DrospirenoneDrospirenone may decrease the anticoagulant activities of Heparin.
DuloxetineDuloxetine may increase the anticoagulant activities of Heparin.
DydrogesteroneThe therapeutic efficacy of Heparin can be decreased when used in combination with Dydrogesterone.
Edetic AcidEdetic Acid may increase the anticoagulant activities of Heparin.
EdoxabanEdoxaban may increase the anticoagulant activities of Heparin.
EnalaprilHeparin may increase the hyperkalemic activities of Enalapril.
EnalaprilatHeparin may increase the hyperkalemic activities of Enalaprilat.
EnoxaparinEnoxaparin may increase the anticoagulant activities of Heparin.
EplerenoneHeparin may increase the hyperkalemic activities of Eplerenone.
EpoprostenolThe risk or severity of adverse effects can be increased when Epoprostenol is combined with Heparin.
EprosartanHeparin may increase the hyperkalemic activities of Eprosartan.
EptifibatideEptifibatide may increase the anticoagulant activities of Heparin.
EscitalopramEscitalopram may increase the anticoagulant activities of Heparin.
EstradiolEstradiol may decrease the anticoagulant activities of Heparin.
EstropipateEstropipate may decrease the anticoagulant activities of Heparin.
Ethinyl EstradiolEthinyl Estradiol may decrease the anticoagulant activities of Heparin.
Ethyl biscoumacetateEthyl biscoumacetate may increase the anticoagulant activities of Heparin.
Ethynodiol diacetateEthynodiol may decrease the anticoagulant activities of Heparin.
EtodolacEtodolac may increase the anticoagulant activities of Heparin.
EtonogestrelThe therapeutic efficacy of Heparin can be decreased when used in combination with Etonogestrel.
FenoprofenFenoprofen may increase the anticoagulant activities of Heparin.
FloctafenineFloctafenine may increase the anticoagulant activities of Heparin.
FluoxetineFluoxetine may increase the anticoagulant activities of Heparin.
FlurbiprofenFlurbiprofen may increase the anticoagulant activities of Heparin.
FluvoxamineFluvoxamine may increase the anticoagulant activities of Heparin.
Fondaparinux sodiumHeparin may increase the anticoagulant activities of Fondaparinux sodium.
FosinoprilHeparin may increase the hyperkalemic activities of Fosinopril.
GestodeneThe therapeutic efficacy of Heparin can be decreased when used in combination with Gestodene.
HomoharringtonineThe risk or severity of adverse effects can be increased when Heparin is combined with Homoharringtonine.
Hydroxyprogesterone caproateThe therapeutic efficacy of Heparin can be decreased when used in combination with Hydroxyprogesterone caproate.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Heparin is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Heparin.
IbuprofenIbuprofen may increase the anticoagulant activities of Heparin.
IcosapentIcosapent may increase the anticoagulant activities of Heparin.
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Heparin.
IloprostThe risk or severity of adverse effects can be increased when Iloprost is combined with Heparin.
IndomethacinIndomethacin may increase the anticoagulant activities of Heparin.
InfliximabInfliximab may increase the anticoagulant activities of Heparin.
IrbesartanHeparin may increase the hyperkalemic activities of Irbesartan.
KetoprofenKetoprofen may increase the anticoagulant activities of Heparin.
KetorolacKetorolac may increase the anticoagulant activities of Heparin.
LevomilnacipranLevomilnacipran may increase the anticoagulant activities of Heparin.
LevonorgestrelThe therapeutic efficacy of Heparin can be decreased when used in combination with Levonorgestrel.
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Heparin.
LisinoprilHeparin may increase the hyperkalemic activities of Lisinopril.
LosartanHeparin may increase the hyperkalemic activities of Losartan.
Magnesium salicylateMagnesium salicylate may increase the anticoagulant activities of Heparin.
Medroxyprogesterone AcetateThe therapeutic efficacy of Heparin can be decreased when used in combination with Medroxyprogesterone Acetate.
Mefenamic acidMefenamic acid may increase the anticoagulant activities of Heparin.
Megestrol acetateThe therapeutic efficacy of Heparin can be decreased when used in combination with Megestrol acetate.
MeloxicamMeloxicam may increase the anticoagulant activities of Heparin.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Heparin.
MestranolMestranol may decrease the anticoagulant activities of Heparin.
MilnacipranMilnacipran may increase the anticoagulant activities of Heparin.
MoexiprilHeparin may increase the hyperkalemic activities of Moexipril.
NabumetoneNabumetone may increase the anticoagulant activities of Heparin.
NadroparinHeparin may increase the anticoagulant activities of Nadroparin.
NaproxenNaproxen may increase the anticoagulant activities of Heparin.
NintedanibThe risk or severity of adverse effects can be increased when Heparin is combined with Nintedanib.
NitroglycerinNitroglycerin may decrease the anticoagulant activities of Heparin.
NorethisteroneThe therapeutic efficacy of Heparin can be decreased when used in combination with Norethindrone.
NorgestimateNorgestimate may decrease the anticoagulant activities of Heparin.
ObinutuzumabThe risk or severity of adverse effects can be increased when Heparin is combined with Obinutuzumab.
OlmesartanHeparin may increase the hyperkalemic activities of Olmesartan.
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Heparin.
Omega-3 fatty acidsOmega-3 fatty acids may increase the anticoagulant activities of Heparin.
Omega-3-acid ethyl estersOmega-3-acid ethyl esters may increase the anticoagulant activities of Heparin.
OritavancinThe therapeutic efficacy of Heparin can be decreased when used in combination with Oritavancin.
OxaprozinOxaprozin may increase the anticoagulant activities of Heparin.
PaliferminThe serum concentration of Palifermin can be increased when it is combined with Heparin.
ParoxetineParoxetine may increase the anticoagulant activities of Heparin.
Pentosan PolysulfatePentosan Polysulfate may increase the anticoagulant activities of Heparin.
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Heparin.
PerindoprilHeparin may increase the hyperkalemic activities of Perindopril.
PhenindionePhenindione may increase the anticoagulant activities of Heparin.
PhenprocoumonPhenprocoumon may increase the anticoagulant activities of Heparin.
PiroxicamPiroxicam may increase the anticoagulant activities of Heparin.
Potassium ChlorideHeparin may increase the hyperkalemic activities of Potassium Chloride.
Potassium CitrateHeparin may increase the hyperkalemic activities of Potassium Citrate.
Potassium IodideHeparin may increase the hyperkalemic activities of Potassium Iodide.
PrasugrelPrasugrel may increase the anticoagulant activities of Heparin.
ProgesteroneThe therapeutic efficacy of Heparin can be decreased when used in combination with Progesterone.
QuinaprilHeparin may increase the hyperkalemic activities of Quinapril.
RamiprilHeparin may increase the hyperkalemic activities of Ramipril.
ReteplaseReteplase may increase the anticoagulant activities of Heparin.
RidogrelRidogrel may increase the anticoagulant activities of Heparin.
RivaroxabanHeparin may increase the anticoagulant activities of Rivaroxaban.
SalsalateSalsalate may increase the anticoagulant activities of Heparin.
SertralineSertraline may increase the anticoagulant activities of Heparin.
SpironolactoneHeparin may increase the hyperkalemic activities of Spironolactone.
StreptokinaseStreptokinase may increase the anticoagulant activities of Heparin.
SugammadexSugammadex may increase the anticoagulant activities of Heparin.
SulindacSulindac may increase the anticoagulant activities of Heparin.
SulodexideSulodexide may increase the anticoagulant activities of Heparin.
TelavancinThe therapeutic efficacy of Heparin can be decreased when used in combination with Telavancin.
TelmisartanHeparin may increase the hyperkalemic activities of Telmisartan.
TenecteplaseTenecteplase may increase the anticoagulant activities of Heparin.
Tiaprofenic acidTiaprofenic acid may increase the anticoagulant activities of Heparin.
TiboloneTibolone may increase the anticoagulant activities of Heparin.
TicagrelorTicagrelor may increase the anticoagulant activities of Heparin.
TiclopidineTiclopidine may increase the anticoagulant activities of Heparin.
TinzaparinHeparin may increase the anticoagulant activities of Tinzaparin.
TipranavirTipranavir may increase the anticoagulant activities of Heparin.
TirofibanTirofiban may increase the anticoagulant activities of Heparin.
TolmetinTolmetin may increase the anticoagulant activities of Heparin.
TositumomabThe risk or severity of adverse effects can be increased when Heparin is combined with Tositumomab.
TrandolaprilHeparin may increase the hyperkalemic activities of Trandolapril.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Heparin.
TriamtereneHeparin may increase the hyperkalemic activities of Triamterene.
UrokinaseUrokinase may increase the anticoagulant activities of Heparin.
ValsartanHeparin may increase the hyperkalemic activities of Valsartan.
VenlafaxineVenlafaxine may increase the anticoagulant activities of Heparin.
VilazodoneVilazodone may increase the anticoagulant activities of Heparin.
Vitamin EVitamin E may increase the anticoagulant activities of Heparin.
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Heparin.
VortioxetineVortioxetine may increase the anticoagulant activities of Heparin.
WarfarinHeparin may increase the anticoagulant activities of Warfarin.
Food Interactions
  • Adequate calcium intake is recommended, needs increased with long term use, supplement recommended.
  • Many herbs with anticoagulant properties (e.g. ginger, garlic, ginseng, green tea, evening primrose) may increase the risk of bleeding in patients on anticoagulant therapy such as heparin

Targets

Kind
Protein
Organism
Human
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 activity is greatly enhanced in the presence of heparin.
Gene Name:
SERPINC1
Uniprot ID:
P01008
Molecular Weight:
52601.935 Da
References
  1. 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. [PubMed:17537059 ]
  2. Sun W, Bandmann H, Schrader T: A fluorescent polymeric heparin sensor. Chemistry. 2007;13(27):7701-7. [PubMed:17600786 ]
  3. 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. [PubMed:17201083 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  5. 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. [PubMed:11278930 ]
  6. 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. [PubMed:10201371 ]
  7. 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. [PubMed:20816747 ]
  8. 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. [PubMed:19818773 ]
Kind
Protein
Organism
Human
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
Molecular Weight:
54731.255 Da
References
  1. 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. [PubMed:17118432 ]
  2. 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. [PubMed:17004727 ]
  3. Rezaie AR: Heparin-binding exosite of factor Xa. Trends Cardiovasc Med. 2000 Nov;10(8):333-8. [PubMed:11369259 ]
  4. Rosenberg RD: Role of heparin and heparinlike molecules in thrombosis and atherosclerosis. Fed Proc. 1985 Feb;44(2):404-9. [PubMed:3155697 ]
Kind
Protein
Organism
Human
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 ligand recognized is sialyl-Lewis X. Mediates rapid rolling of leukocyte rolling over vascular surfaces during the initial steps in inflammation through interaction with PSGL1.
Gene Name:
SELP
Uniprot ID:
P16109
Molecular Weight:
90833.105 Da
References
  1. 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. [PubMed:17458940 ]
  2. 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. [PubMed:17549299 ]
  3. 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. [PubMed:17629851 ]
  4. 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. [PubMed:17651117 ]
  5. 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. [PubMed:15995351 ]
  6. 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. [PubMed:9466983 ]
  7. 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. [PubMed:7694675 ]

Enzymes

Kind
Protein
Organism
Human
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. Selectively cleaves the linkage between a glucuronic acid unit and an N-sulfo glucosamine unit carrying either a 3-O-sulfo or a 6-O-sulfo group. Can also cleave the linkage between a glucuronic acid uni...
Gene Name:
HPSE
Uniprot ID:
Q9Y251
Molecular Weight:
61148.17 Da
References
  1. 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. [PubMed:21575986 ]
  2. 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. [PubMed:20434010 ]
  3. 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. [PubMed:18545691 ]
  4. 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. [PubMed:17627539 ]
  5. 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. [PubMed:18064313 ]
  6. 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. [PubMed:16460439 ]
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Drug created on June 13, 2005 07:24 / Updated on November 30, 2015 12:10