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Identification
NameHeparin
Accession NumberDB01109  (APRD00056)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionUnfractionated 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
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Calcilean Inj 20000unit/0.8mlLiquid20000 unitSubcutaneousOrganon Teknika Canada Inc.1987-12-311997-08-11Canada
Calciparine Inj 20000iu/ampLiquid20000 unitSubcutaneousChoay Lab1974-12-311998-06-09Canada
Calciparine Inj 5000iuLiquid5000 unitSubcutaneousChoay 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, Inc2010-08-01Not applicableUs
Heparin Lock FlushInjection, solution100 [USP'U]/mLIntravenousAPP Pharmaceuticals, LLC2009-08-12Not applicableUs
Heparin Lock FlushInjection, solution10 [USP'U]/mLIntravenousAPP Pharmaceuticals, LLC2009-08-29Not applicableUs
Heparin Lock FlushSolution10 [USP'U]/mLIntravenousGeneral Injectables & Vaccines, Inc2010-08-01Not applicableUs
Heparin Lock Flush Solution Inj 10unit/mlSolution10 unitIntraperitonealHospira Healthcare Corporation1986-12-312012-08-03Canada
Heparin Lock Flush Solution Injection USPSolution100 unitIntravenous; IrrigationHospira Healthcare Corporation1989-12-31Not applicableCanada
Heparin Lock Flush Solution Injection USPSolution10 unitIntravenous; IrrigationHospira Healthcare Corporation1989-12-31Not applicableCanada
Heparin SodiumInjection10000 [USP'U]/mLIntravenous; SubcutaneousWest Ward Pharmaceutical Corp.1972-03-22Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/.5mLIntravenous; SubcutaneousCardinal Health2010-06-18Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/.5mLIntravenous; SubcutaneousFresenius Kabi USA, LLC2010-12-03Not applicableUs
Heparin SodiumInjection, solution, concentrate10000 [USP'U]/5mLIntravenousGeneral Injectables & Vaccines, Inc2010-03-01Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousFresenius Kabi USA, LLC2010-06-18Not applicableUs
Heparin SodiumInjection10000 [USP'U]/mLIntravenous; SubcutaneousPfizer Laboratories Div Pfizer Inc2011-07-21Not applicableUs
Heparin SodiumInjection, solution, concentrate25000 [USP'U]/10mLIntravenousHospira, Inc.2010-10-222016-10-13Us
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2010-06-18Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2009-08-12Not applicableUs
Heparin SodiumInjection1000 [USP'U]/mLIntravenous; SubcutaneousWest Ward Pharmaceutical Corp.1972-03-22Not applicableUs
Heparin SodiumInjection5000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2011-07-21Not applicableUs
Heparin SodiumInjection1000 [USP'U]/mLIntravenous; SubcutaneousPfizer Laboratories Div Pfizer Inc2011-07-21Not applicableUs
Heparin SodiumInjection, solution4000 [USP'U]/100mLIntravenousHospira, Inc.1989-01-25Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/100mLIntravenousHospira, Inc.1984-01-31Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousGeneral Injectables & Vaccines, Inc2010-08-01Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/mLIntravenous; SubcutaneousFresenius Kabi USA, LLC2011-04-25Not applicableUs
Heparin SodiumInjection1000 [USP'U]/mLIntravenous; SubcutaneousPfizer Laboratories Div Pfizer Inc2013-03-11Not applicableUs
Heparin SodiumInjection1000 [USP'U]/mLIntravenous; SubcutaneousWest Ward Pharmaceutical Corp.1972-03-22Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2010-06-18Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousFresenius Kabi USA, LLC2010-06-18Not applicableUs
Heparin SodiumInjection, solution200 [USP'U]/100mLIntravenousHospira, Inc.1984-01-31Not applicableUs
Heparin SodiumInjection5000 [USP'U]/mLIntravenous; SubcutaneousWest Ward Pharmaceutical Corp.1972-03-22Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2010-06-18Not applicableUs
Heparin SodiumInjection1000 [USP'U]/mLIntravenous; SubcutaneousPfizer Laboratories Div Pfizer Inc2011-07-21Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/100mLIntravenousHospira, Inc.1989-01-25Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/100mLIntravenousHospira, Inc.1984-01-31Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousGeneral Injectables & Vaccines, Inc2010-08-01Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousFresenius Kabi USA, LLC2009-08-12Not applicableUs
Heparin SodiumInjection5000 [USP'U]/mLIntravenous; SubcutaneousWest Ward Pharmaceutical Corp.1972-03-22Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2010-06-18Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousFresenius Kabi USA, LLC2009-08-12Not applicableUs
Heparin SodiumInjection, solution, concentrate10000 [USP'U]/5mLIntravenousHospira, Inc.2010-10-222016-10-13Us
Heparin SodiumInjection, solution10000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2010-06-18Not applicableUs
Heparin SodiumInjection5000 [USP'U]/mLIntravenous; SubcutaneousPfizer Laboratories Div Pfizer Inc2011-07-21Not applicableUs
Heparin SodiumInjection, solution20000 [USP'U]/mLIntravenous; SubcutaneousFresenius Kabi USA, LLC2010-06-18Not applicableUs
Heparin SodiumInjection, solution100000 [USP'U]/mLIntravenous; SubcutaneousGeneral Injectables & Vaccines, Inc2010-03-01Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/mLIntravenous; SubcutaneousFresenius Kabi USA, LLC2010-06-18Not applicableUs
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.1985-03-27Not applicableUs
Heparin Sodium and DextroseInjection, solution10000 [USP'U]/100mLIntravenousHospira, Inc.1985-03-27Not applicableUs
Heparin Sodium and Sodium ChlorideInjection, solution200 [USP'U]/100mLIntravenousBaxter Healthcare Corporation1982-04-28Not applicableUs
Heparin Sodium and Sodium ChlorideInjection, solution200 [USP'U]/100mLIntravenousBaxter Healthcare Corporation1982-04-28Not applicableUs
Heparin Sodium In DextroseInjection, solution4000 [USP'U]/100mLIntravenousBaxter Healthcare Corporation2010-12-31Not applicableUs
Heparin Sodium In DextroseInjection, solution5000 [USP'U]/100mLIntravenousBaxter Healthcare Corporation2010-12-31Not applicableUs
Heparin Sodium In DextroseInjection, solution10000 [USP'U]/100mLIntravenousBaxter Healthcare Corporation2010-12-31Not applicableUs
Heparin Sodium In Sodium ChlorideInjection200 [USP'U]/100mLIntravenousB. Braun Medical Inc.1992-07-20Not applicableUs
Heparin Sodium Injection USPSolution5000 unitIntravenous; SubcutaneousPfizer Canada IncNot applicableNot applicableCanada
Heparin Sodium Injection USPSolution1000 unitIntravenous; SubcutaneousPfizer Canada Inc2013-03-01Not applicableCanada
Heparin Sodium Injection USPSolution10000 unitIntravenous; SubcutaneousPfizer Canada Inc2013-03-01Not applicableCanada
Heparin Sodium Injection USPSolution5000 unitIntravenous; SubcutaneousPfizer Canada Inc2013-03-012015-06-01Canada
Heparin Sodium Injection USPSolution5000 unitSubcutaneousSterinova Inc2016-11-17Not applicableCanada
Heparin Sodium Injection USPSolution1000 unitIntravenous; SubcutaneousPfizer Canada IncNot applicableNot 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, USPSolution1000 unitIntravenous; SubcutaneousFresenius Kabi Canada Ltd2005-05-26Not applicableCanada
Heparin Sodium Injection, USPSolution10000 unitIntravenous; SubcutaneousFresenius Kabi Canada Ltd2013-05-20Not applicableCanada
Heparin Sodium Injection, USPSolution10000 unitIntravenous; SubcutaneousFresenius Kabi Canada Ltd2005-05-27Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousGeneral Injectables & Vaccines, Inc2011-09-13Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/mLIntravenous; SubcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousHospira, Inc.2009-08-31Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2005-01-31Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousBd Rx, Inc.2016-06-10Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousHospira, Inc.2005-01-31Not applicableUs
Heparin SodiumInjection5000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2010-07-06Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not applicableUs
Heparin SodiumInjection20000 [USP'U]/mLIntravenous; SubcutaneousSagent Pharmaceuticals2010-07-06Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousGeneral Injectables & Vaccines, Inc2011-09-13Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/mLIntravenous; SubcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/mLIntravenous; SubcutaneousHospira, Inc.2009-08-31Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2009-08-31Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousSagent Pharmaceuticals2010-07-06Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousSafecor Health, LLC2014-09-30Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2009-12-07Not applicableUs
Heparin SodiumInjection, solution20000 [USP'U]/mLIntravenous; SubcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousHospira, Inc.2009-08-31Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2009-08-31Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousSagent Pharmaceuticals2010-07-06Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/mLIntravenous; SubcutaneousSafecor Health, LLC2014-09-30Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/mLIntravenous; SubcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not applicableUs
Heparin SodiumInjection1000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2010-07-06Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/mLIntravenous; SubcutaneousHospira, Inc.1987-05-04Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not applicableUs
Heparin SodiumInjection1000 [USP'U]/mLIntravenous; SubcutaneousSagent Pharmaceticals2010-07-06Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/mLIntravenous; SubcutaneousCardinal Health2009-08-31Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/mLIntravenous; SubcutaneousSagent Pharmaceuticals2010-07-06Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Heparin SodiumInjection, solution4 [USP'U]/mLIntravenousCantrell Drug Company2012-05-09Not applicableUs
Heparin SodiumInjection, solution30 [USP'U]/mLIntravenousCantrell Drug Company2013-11-22Not applicableUs
Heparin SodiumInjection, solution100 [USP'U]/mLIntravenousCantrell Drug Company2015-05-15Not applicableUs
Heparin SodiumInjection, solution1 [USP'U]/mLIntravenousCantrell Drug Company2011-02-22Not applicableUs
Heparin SodiumInjection, solution2 [USP'U]/mLIntravenousCantrell Drug Company2012-08-29Not applicableUs
Heparin SodiumInjection, solution5 [USP'U]/mLIntravenousCantrell Drug Company2011-02-18Not applicableUs
Heparin SodiumInjection, solution4 [USP'U]/mLIntravenousCantrell Drug Company2012-11-13Not applicableUs
Heparin SodiumInjection, solution10 [USP'U]/mLIntravenousCantrell Drug Company2011-11-07Not applicableUs
Heparin SodiumInjection, solution100 [USP'U]/mLIntravenousCantrell Drug Company2012-08-29Not applicableUs
Heparin SodiumInjection, solution5 [USP'U]/mLIntravenousCantrell Drug Company2012-05-09Not applicableUs
Heparin SodiumInjection, solution40 [USP'U]/mLIntravenousCantrell Drug Company2014-04-08Not applicableUs
Heparin SodiumInjection, solution50 [USP'U]/mLIntravenousCantrell Drug Company2012-08-09Not applicableUs
Heparin SodiumInjection, solution.5 [USP'U]/mLIntravenousCantrell Drug Company2012-03-22Not applicableUs
Heparin SodiumInjection, solution10 [USP'U]/mLIntravenousCantrell Drug Company2011-06-30Not applicableUs
Heparin SodiumInjection, solution50 [USP'U]/mLIntravenousCantrell Drug Company2012-12-21Not applicableUs
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
Heparin Sodium In DextroseB. Braun Medical Inc.
Salts
Name/CASStructureProperties
Heparin calcium
ThumbNot applicableDBSALT001434
Heparin sodium
ThumbNot applicableDBSALT000417
Categories
UNII4QW4AN84NQ
CAS number9005-49-6
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
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.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Antithrombin-IIIProteinyes
potentiator
HumanP01008 details
Coagulation factor XProteinyes
inhibitor
HumanP00742 details
P-selectinProteinunknown
inhibitor
HumanP16109 details
Related Articles
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
Interactions
Drug Interactions
DrugInteractionDrug group
AbciximabAbciximab may increase the anticoagulant activities of Heparin.Approved
AceclofenacAceclofenac may increase the anticoagulant activities of Heparin.Approved
AcenocoumarolHeparin may increase the anticoagulant activities of Acenocoumarol.Approved
AcetovanilloneAcetovanillone may increase the anticoagulant activities of Heparin.Investigational
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Heparin.Approved, Vet Approved
AdapaleneAdapalene may increase the anticoagulant activities of Heparin.Approved
AliskirenHeparin may increase the hyperkalemic activities of Aliskiren.Approved, Investigational
AllylestrenolThe therapeutic efficacy of Heparin can be decreased when used in combination with Allylestrenol.Approved
AlprostadilAlprostadil may increase the anticoagulant activities of Heparin.Approved, Investigational
AlteplaseAlteplase may increase the anticoagulant activities of Heparin.Approved
AltrenogestThe therapeutic efficacy of Heparin can be decreased when used in combination with Altrenogest.Vet Approved
ALX-0081ALX-0081 may increase the anticoagulant activities of Heparin.Investigational
AmilorideHeparin may increase the hyperkalemic activities of Amiloride.Approved
Aminosalicylic AcidAminosalicylic Acid may increase the anticoagulant activities of Heparin.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Heparin.Approved
AncrodHeparin may increase the anticoagulant activities of Ancrod.Investigational
AnisodamineAnisodamine may increase the anticoagulant activities of Heparin.Investigational
AnistreplaseAnistreplase may increase the anticoagulant activities of Heparin.Approved
AntipyrineAntipyrine may increase the anticoagulant activities of Heparin.Approved
Antithrombin III humanHeparin may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanApixaban may increase the anticoagulant activities of Heparin.Approved
ApremilastApremilast may increase the anticoagulant activities of Heparin.Approved, Investigational
AprotininThe therapeutic efficacy of Heparin can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinArdeparin may increase the anticoagulant activities of Heparin.Approved, Withdrawn
ArgatrobanArgatroban may increase the anticoagulant activities of Heparin.Approved, Investigational
AstaxanthinAstaxanthin may increase the anticoagulant activities of Heparin.Investigational
AzapropazoneAzapropazone may increase the anticoagulant activities of Heparin.Withdrawn
AzelastineAzelastine may increase the anticoagulant activities of Heparin.Approved
Azilsartan medoxomilHeparin may increase the hyperkalemic activities of Azilsartan medoxomil.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Heparin.Approved, Investigational
BatroxobinBatroxobin may increase the anticoagulant activities of Heparin.Experimental
BazedoxifeneBazedoxifene may decrease the anticoagulant activities of Heparin.Approved, Investigational
BecaplerminBecaplermin may increase the anticoagulant activities of Heparin.Approved, Investigational
BemiparinBemiparin may increase the anticoagulant activities of Heparin.Approved
BenazeprilHeparin may increase the hyperkalemic activities of Benazepril.Approved, Investigational
BenoxaprofenBenoxaprofen may increase the anticoagulant activities of Heparin.Withdrawn
BeraprostBeraprost may increase the anticoagulant activities of Heparin.Investigational
Betulinic AcidBetulinic Acid may increase the anticoagulant activities of Heparin.Investigational
BivalirudinBivalirudin may increase the anticoagulant activities of Heparin.Approved, Investigational
BromfenacBromfenac may increase the anticoagulant activities of Heparin.Approved
BucillamineBucillamine may increase the anticoagulant activities of Heparin.Investigational
ButylphthalideButylphthalide may increase the anticoagulant activities of Heparin.Investigational
CanagliflozinHeparin may increase the hyperkalemic activities of Canagliflozin.Approved
CandesartanHeparin may increase the hyperkalemic activities of Candesartan.Approved
CandoxatrilHeparin may increase the hyperkalemic activities of Candoxatril.Experimental
CangrelorCangrelor may increase the anticoagulant activities of Heparin.Approved
CaptoprilHeparin may increase the hyperkalemic activities of Captopril.Approved
CarprofenCarprofen may increase the anticoagulant activities of Heparin.Approved, Vet Approved, Withdrawn
CastanospermineCastanospermine may increase the anticoagulant activities of Heparin.Experimental
CelecoxibCelecoxib may increase the anticoagulant activities of Heparin.Approved, Investigational
CertoparinHeparin may increase the anticoagulant activities of Certoparin.Approved
ChloroquineChloroquine may increase the anticoagulant activities of Heparin.Approved, Vet Approved
ChlorotrianiseneChlorotrianisene may decrease the anticoagulant activities of Heparin.Withdrawn
CilazaprilHeparin may increase the hyperkalemic activities of Cilazapril.Approved
CilostazolCilostazol may increase the anticoagulant activities of Heparin.Approved
Citric AcidHeparin may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClonixinClonixin may increase the anticoagulant activities of Heparin.Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Heparin.Approved, Nutraceutical
CollagenaseThe risk or severity of adverse effects can be increased when Heparin is combined with Collagenase.Approved
Conjugated Equine EstrogensConjugated Equine Estrogens may decrease the anticoagulant activities of Heparin.Approved
Corticorelin ovine triflutateThe risk or severity of adverse effects can be increased when Heparin is combined with Corticorelin ovine triflutate.Approved
CurcuminCurcumin may increase the anticoagulant activities of Heparin.Investigational
D-LimoneneD-Limonene may increase the anticoagulant activities of Heparin.Investigational
Dabigatran etexilateDabigatran etexilate may increase the anticoagulant activities of Heparin.Approved
DalteparinHeparin may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidHeparin may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DasatinibDasatinib may increase the anticoagulant activities of Heparin.Approved, Investigational
DeferasiroxThe risk or severity of adverse effects can be increased when Heparin is combined with Deferasirox.Approved, Investigational
DefibrotideDefibrotide may increase the anticoagulant activities of Heparin.Approved, Investigational
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Heparin is combined with Deoxycholic Acid.Approved
dersalazinedersalazine may increase the anticoagulant activities of Heparin.Investigational
DesirudinHeparin may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseDesmoteplase may increase the anticoagulant activities of Heparin.Investigational
DesogestrelThe therapeutic efficacy of Heparin can be decreased when used in combination with Desogestrel.Approved
DextranHeparin may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Heparin may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Heparin may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Heparin may increase the anticoagulant activities of Dextran 75.Approved
DiclofenacDiclofenac may increase the anticoagulant activities of Heparin.Approved, Vet Approved
DicoumarolDicoumarol may increase the anticoagulant activities of Heparin.Approved
DienestrolDienestrol may decrease the anticoagulant activities of Heparin.Approved
DienogestThe therapeutic efficacy of Heparin can be decreased when used in combination with Dienogest.Approved
DiethylstilbestrolDiethylstilbestrol may decrease the anticoagulant activities of Heparin.Approved
DiflunisalDiflunisal may increase the anticoagulant activities of Heparin.Approved
DipyridamoleDipyridamole may increase the anticoagulant activities of Heparin.Approved
DitazoleDitazole may increase the anticoagulant activities of Heparin.Approved, Withdrawn
DrospirenoneThe therapeutic efficacy of Heparin can be decreased when used in combination with Drospirenone.Approved
Drotrecogin alfaDrotrecogin alfa may increase the anticoagulant activities of Heparin.Approved, Investigational, Withdrawn
DroxicamDroxicam may increase the anticoagulant activities of Heparin.Approved
DuvelisibDuvelisib may increase the anticoagulant activities of Heparin.Investigational
DydrogesteroneThe therapeutic efficacy of Heparin can be decreased when used in combination with Dydrogesterone.Approved, Withdrawn
E6201E6201 may increase the anticoagulant activities of Heparin.Investigational
EbselenEbselen may increase the anticoagulant activities of Heparin.Investigational
Edetic AcidEdetic Acid may increase the anticoagulant activities of Heparin.Approved, Vet Approved
EdoxabanEdoxaban may increase the anticoagulant activities of Heparin.Approved
EnalaprilHeparin may increase the hyperkalemic activities of Enalapril.Approved, Vet Approved
EnalaprilatHeparin may increase the hyperkalemic activities of Enalaprilat.Approved
EnoxaparinHeparin may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the anticoagulant activities of Heparin.Approved, Investigational
EpirizoleEpirizole may increase the anticoagulant activities of Heparin.Approved
EplerenoneHeparin may increase the hyperkalemic activities of Eplerenone.Approved
eplivanserineeplivanserine may increase the anticoagulant activities of Heparin.Investigational
EpoprostenolEpoprostenol may increase the anticoagulant activities of Heparin.Approved
EprosartanHeparin may increase the hyperkalemic activities of Eprosartan.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Heparin.Approved, Investigational
EstradiolEstradiol may decrease the anticoagulant activities of Heparin.Approved, Investigational, Vet Approved
EstriolEstriol may decrease the anticoagulant activities of Heparin.Approved, Vet Approved
EstroneEstrone may decrease the anticoagulant activities of Heparin.Approved
EtanerceptEtanercept may increase the anticoagulant activities of Heparin.Approved, Investigational
Ethinyl EstradiolEthinyl Estradiol may decrease the anticoagulant activities of Heparin.Approved
Ethyl biscoumacetateHeparin may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ethynodiol diacetateThe therapeutic efficacy of Heparin can be decreased when used in combination with Ethynodiol diacetate.Approved
EtodolacEtodolac may increase the anticoagulant activities of Heparin.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may increase the anticoagulant activities of Heparin.Approved
EtonogestrelThe therapeutic efficacy of Heparin can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoricoxibEtoricoxib may increase the anticoagulant activities of Heparin.Approved, Investigational
Evening primrose oilEvening primrose oil may increase the anticoagulant activities of Heparin.Approved
exisulindexisulind may increase the anticoagulant activities of Heparin.Investigational
FenbufenFenbufen may increase the anticoagulant activities of Heparin.Approved
FenoprofenFenoprofen may increase the anticoagulant activities of Heparin.Approved
FibrinolysinFibrinolysin may increase the anticoagulant activities of Heparin.Approved
FloctafenineFloctafenine may increase the anticoagulant activities of Heparin.Approved, Withdrawn
FluindioneHeparin may increase the anticoagulant activities of Fluindione.Investigational
FlunixinFlunixin may increase the anticoagulant activities of Heparin.Vet Approved
FlurbiprofenFlurbiprofen may increase the anticoagulant activities of Heparin.Approved, Investigational
FondaparinuxHeparin may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumFondaparinux sodium may increase the anticoagulant activities of Heparin.Approved, Investigational
ForasartanHeparin may increase the hyperkalemic activities of Forasartan.Experimental
FosinoprilHeparin may increase the hyperkalemic activities of Fosinopril.Approved
GabexateHeparin may increase the anticoagulant activities of Gabexate.Investigational
GenisteinGenistein may decrease the anticoagulant activities of Heparin.Investigational
GestodeneThe therapeutic efficacy of Heparin can be decreased when used in combination with Gestodene.Approved
GestrinoneThe therapeutic efficacy of Heparin can be decreased when used in combination with Gestrinone.Approved
HeminHemin may increase the anticoagulant activities of Heparin.Approved
HexestrolHexestrol may decrease the anticoagulant activities of Heparin.Withdrawn
HigenamineHigenamine may increase the anticoagulant activities of Heparin.Investigational
HirulogHeparin may increase the anticoagulant activities of Hirulog.Experimental
HMPL-004HMPL-004 may increase the anticoagulant activities of Heparin.Investigational
Hydroxyprogesterone caproateThe therapeutic efficacy of Heparin can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Heparin is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Heparin.Approved
IbudilastIbudilast may increase the anticoagulant activities of Heparin.Approved, Investigational
IbuprofenIbuprofen may increase the anticoagulant activities of Heparin.Approved
IbuproxamIbuproxam may increase the anticoagulant activities of Heparin.Withdrawn
IcatibantIcatibant may increase the anticoagulant activities of Heparin.Approved
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Heparin.Approved, Nutraceutical
idraparinuxHeparin may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Heparin.Approved, Withdrawn
IloprostIloprost may increase the anticoagulant activities of Heparin.Approved, Investigational
ImidaprilHeparin may increase the hyperkalemic activities of Imidapril.Investigational
IndobufenIndobufen may increase the anticoagulant activities of Heparin.Investigational
IndomethacinIndomethacin may increase the anticoagulant activities of Heparin.Approved, Investigational
IndoprofenIndoprofen may increase the anticoagulant activities of Heparin.Withdrawn
IrbesartanHeparin may increase the hyperkalemic activities of Irbesartan.Approved, Investigational
IsoxicamIsoxicam may increase the anticoagulant activities of Heparin.Withdrawn
Kct 0809Kct 0809 may increase the anticoagulant activities of Heparin.Investigational
KebuzoneKebuzone may increase the anticoagulant activities of Heparin.Experimental
KetanserinKetanserin may increase the anticoagulant activities of Heparin.Investigational
KetoprofenKetoprofen may increase the anticoagulant activities of Heparin.Approved, Vet Approved
KetorolacKetorolac may increase the anticoagulant activities of Heparin.Approved
LeflunomideLeflunomide may increase the anticoagulant activities of Heparin.Approved, Investigational
LepirudinLepirudin may increase the anticoagulant activities of Heparin.Approved
LevonorgestrelThe therapeutic efficacy of Heparin can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Heparin.Approved
LisinoprilHeparin may increase the hyperkalemic activities of Lisinopril.Approved, Investigational
LisofyllineLisofylline may increase the anticoagulant activities of Heparin.Investigational
LornoxicamLornoxicam may increase the anticoagulant activities of Heparin.Approved
LosartanHeparin may increase the hyperkalemic activities of Losartan.Approved
LoxoprofenLoxoprofen may increase the anticoagulant activities of Heparin.Approved
LumiracoxibLumiracoxib may increase the anticoagulant activities of Heparin.Approved, Investigational
LynestrenolThe therapeutic efficacy of Heparin can be decreased when used in combination with Lynestrenol.Investigational
Magnesium salicylateMagnesium salicylate may increase the anticoagulant activities of Heparin.Approved
MasoprocolMasoprocol may increase the anticoagulant activities of Heparin.Approved
Meclofenamic acidMeclofenamic acid may increase the anticoagulant activities of Heparin.Approved, Vet Approved
MedrogestoneThe therapeutic efficacy of Heparin can be decreased when used in combination with Medrogestone.Approved
Medroxyprogesterone acetateThe therapeutic efficacy of Heparin can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Mefenamic acidMefenamic acid may increase the anticoagulant activities of Heparin.Approved
Megestrol acetateThe therapeutic efficacy of Heparin can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MeloxicamMeloxicam may increase the anticoagulant activities of Heparin.Approved, Vet Approved
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Heparin.Approved
MestranolMestranol may decrease the anticoagulant activities of Heparin.Approved
MetamizoleMetamizole may increase the anticoagulant activities of Heparin.Withdrawn
MethallenestrilMethallenestril may decrease the anticoagulant activities of Heparin.Experimental
MilrinoneMilrinone may increase the anticoagulant activities of Heparin.Approved
MizoribineMizoribine may increase the anticoagulant activities of Heparin.Investigational
MoexiprilHeparin may increase the hyperkalemic activities of Moexipril.Approved
Mycophenolate mofetilMycophenolate mofetil may increase the anticoagulant activities of Heparin.Approved, Investigational
Mycophenolic acidMycophenolic acid may increase the anticoagulant activities of Heparin.Approved
NabumetoneNabumetone may increase the anticoagulant activities of Heparin.Approved
NadroparinHeparin may increase the anticoagulant activities of Nadroparin.Approved
NafamostatNafamostat may increase the anticoagulant activities of Heparin.Investigational
NaftifineNaftifine may increase the anticoagulant activities of Heparin.Approved
NaftopidilNaftopidil may increase the anticoagulant activities of Heparin.Investigational
NaproxenNaproxen may increase the anticoagulant activities of Heparin.Approved, Vet Approved
NCX 4016NCX 4016 may increase the anticoagulant activities of Heparin.Investigational
NepafenacNepafenac may increase the anticoagulant activities of Heparin.Approved
Niflumic AcidNiflumic Acid may increase the anticoagulant activities of Heparin.Approved
NimesulideNimesulide may increase the anticoagulant activities of Heparin.Approved, Withdrawn
NintedanibThe risk or severity of adverse effects can be increased when Heparin is combined with Nintedanib.Approved
NitroaspirinNitroaspirin may increase the anticoagulant activities of Heparin.Investigational
NitroglycerinNitroglycerin may decrease the anticoagulant activities of Heparin.Approved, Investigational
NomegestrolThe therapeutic efficacy of Heparin can be decreased when used in combination with Nomegestrol.Approved
NorethisteroneThe therapeutic efficacy of Heparin can be decreased when used in combination with Norethisterone.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Heparin is combined with Obinutuzumab.Approved
OlmesartanHeparin may increase the hyperkalemic activities of Olmesartan.Approved, Investigational
OlopatadineOlopatadine may increase the anticoagulant activities of Heparin.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Heparin.Approved
Omacetaxine mepesuccinateThe risk or severity of adverse effects can be increased when Heparin is combined with Omacetaxine mepesuccinate.Approved
OmapatrilatHeparin may increase the hyperkalemic activities of Omapatrilat.Investigational
Omega-3 fatty acidsOmega-3 fatty acids may increase the anticoagulant activities of Heparin.Approved
OrgoteinOrgotein may increase the anticoagulant activities of Heparin.Vet Approved
OritavancinThe therapeutic efficacy of Heparin can be decreased when used in combination with Oritavancin.Approved, Investigational
OtamixabanHeparin may increase the anticoagulant activities of Otamixaban.Investigational
OxaprozinOxaprozin may increase the anticoagulant activities of Heparin.Approved
OxyphenbutazoneOxyphenbutazone may increase the anticoagulant activities of Heparin.Withdrawn
PaliferminThe serum concentration of Palifermin can be increased when it is combined with Heparin.Approved
ParecoxibParecoxib may increase the anticoagulant activities of Heparin.Approved
ParnaparinParnaparin may increase the anticoagulant activities of Heparin.Approved
Pentosan PolysulfatePentosan Polysulfate may increase the anticoagulant activities of Heparin.Approved
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Heparin.Approved, Investigational
PerindoprilHeparin may increase the hyperkalemic activities of Perindopril.Approved
PhenindionePhenindione may increase the anticoagulant activities of Heparin.Approved
PhenprocoumonPhenprocoumon may increase the anticoagulant activities of Heparin.Approved
PhenylbutazonePhenylbutazone may increase the anticoagulant activities of Heparin.Approved, Vet Approved
PimecrolimusPimecrolimus may increase the anticoagulant activities of Heparin.Approved, Investigational
PirfenidonePirfenidone may increase the anticoagulant activities of Heparin.Investigational
PiroxicamPiroxicam may increase the anticoagulant activities of Heparin.Approved, Investigational
PlasminPlasmin may increase the anticoagulant activities of Heparin.Investigational
Polyestradiol phosphatePolyestradiol phosphate may decrease the anticoagulant activities of Heparin.Approved
PrasugrelPrasugrel may increase the anticoagulant activities of Heparin.Approved
ProgesteroneThe therapeutic efficacy of Heparin can be decreased when used in combination with Progesterone.Approved, Vet Approved
PromestrienePromestriene may decrease the anticoagulant activities of Heparin.Investigational
PropacetamolPropacetamol may increase the anticoagulant activities of Heparin.Approved
Protein CHeparin may increase the anticoagulant activities of Protein C.Approved
Protein S humanHeparin may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeHeparin may increase the anticoagulant activities of Protocatechualdehyde.Approved
PTC299PTC299 may increase the anticoagulant activities of Heparin.Investigational
QuinaprilHeparin may increase the hyperkalemic activities of Quinapril.Approved, Investigational
QuinestrolQuinestrol may decrease the anticoagulant activities of Heparin.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Heparin.Investigational
RamiprilHeparin may increase the hyperkalemic activities of Ramipril.Approved
RescinnamineHeparin may increase the hyperkalemic activities of Rescinnamine.Approved
ResveratrolResveratrol may increase the anticoagulant activities of Heparin.Experimental, Investigational
ReteplaseReteplase may increase the anticoagulant activities of Heparin.Approved
ReviparinHeparin may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Heparin.Approved
RivaroxabanHeparin may increase the anticoagulant activities of Rivaroxaban.Approved
RofecoxibRofecoxib may increase the anticoagulant activities of Heparin.Investigational, Withdrawn
RosiglitazoneRosiglitazone may increase the anticoagulant activities of Heparin.Approved, Investigational
S EquolS Equol may decrease the anticoagulant activities of Heparin.Investigational
SacubitrilHeparin may increase the hyperkalemic activities of Sacubitril.Approved
SalicylamideSalicylamide may increase the anticoagulant activities of Heparin.Approved
Salicylic acidSalicylic acid may increase the anticoagulant activities of Heparin.Approved, Vet Approved
SalsalateSalsalate may increase the anticoagulant activities of Heparin.Approved
SaprisartanHeparin may increase the hyperkalemic activities of Saprisartan.Experimental
SaralasinHeparin may increase the hyperkalemic activities of Saralasin.Investigational
SCH-530348SCH-530348 may increase the anticoagulant activities of Heparin.Investigational
SecoisolariciresinolSecoisolariciresinol may decrease the anticoagulant activities of Heparin.Investigational
SelexipagSelexipag may increase the anticoagulant activities of Heparin.Approved
SeratrodastSeratrodast may increase the anticoagulant activities of Heparin.Approved, Investigational
SevofluraneSevoflurane may increase the anticoagulant activities of Heparin.Approved, Vet Approved
SpiraprilHeparin may increase the hyperkalemic activities of Spirapril.Approved
SpironolactoneHeparin may increase the hyperkalemic activities of Spironolactone.Approved
SRT501SRT501 may increase the anticoagulant activities of Heparin.Investigational
StreptokinaseStreptokinase may increase the anticoagulant activities of Heparin.Approved
SugammadexSugammadex may increase the anticoagulant activities of Heparin.Approved
SulfasalazineThe risk or severity of adverse effects can be increased when Sulfasalazine is combined with Heparin.Approved
SulindacSulindac may increase the anticoagulant activities of Heparin.Approved
SulodexideHeparin may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SuprofenSuprofen may increase the anticoagulant activities of Heparin.Approved, Withdrawn
Synthetic Conjugated Estrogens, ASynthetic Conjugated Estrogens, A may decrease the anticoagulant activities of Heparin.Approved
Synthetic Conjugated Estrogens, BSynthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Heparin.Approved
TasosartanHeparin may increase the hyperkalemic activities of Tasosartan.Approved
TelavancinThe therapeutic efficacy of Heparin can be decreased when used in combination with Telavancin.Approved
TelmisartanHeparin may increase the hyperkalemic activities of Telmisartan.Approved, Investigational
TemocaprilHeparin may increase the hyperkalemic activities of Temocapril.Experimental, Investigational
TenecteplaseTenecteplase may increase the anticoagulant activities of Heparin.Approved
TenoxicamTenoxicam may increase the anticoagulant activities of Heparin.Approved
TepoxalinTepoxalin may increase the anticoagulant activities of Heparin.Vet Approved
TeriflunomideTeriflunomide may increase the anticoagulant activities of Heparin.Approved
TesmilifeneTesmilifene may increase the anticoagulant activities of Heparin.Investigational
Tiaprofenic acidTiaprofenic acid may increase the anticoagulant activities of Heparin.Approved
TiboloneTibolone may increase the anticoagulant activities of Heparin.Approved
TicagrelorTicagrelor may increase the anticoagulant activities of Heparin.Approved
TiclopidineTiclopidine may increase the anticoagulant activities of Heparin.Approved
TinoridineTinoridine may increase the anticoagulant activities of Heparin.Investigational
TinzaparinTinzaparin may increase the anticoagulant activities of Heparin.Approved
TipranavirTipranavir may increase the anticoagulant activities of Heparin.Approved, Investigational
TirofibanTirofiban may increase the anticoagulant activities of Heparin.Approved
Tolfenamic AcidTolfenamic Acid may increase the anticoagulant activities of Heparin.Approved
TolmetinTolmetin may increase the anticoagulant activities of Heparin.Approved
TositumomabThe risk or severity of adverse effects can be increased when Heparin is combined with Tositumomab.Approved
TrandolaprilHeparin may increase the hyperkalemic activities of Trandolapril.Approved
TranilastTranilast may increase the anticoagulant activities of Heparin.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Heparin.Approved
TreprostinilTreprostinil may increase the anticoagulant activities of Heparin.Approved, Investigational
TriamtereneHeparin may increase the hyperkalemic activities of Triamterene.Approved
TriflusalTriflusal may increase the anticoagulant activities of Heparin.Approved
Trisalicylate-cholineTrisalicylate-choline may increase the anticoagulant activities of Heparin.Approved
UrokinaseUrokinase may increase the anticoagulant activities of Heparin.Approved, Investigational, Withdrawn
ValdecoxibValdecoxib may increase the anticoagulant activities of Heparin.Investigational, Withdrawn
ValsartanHeparin may increase the hyperkalemic activities of Valsartan.Approved, Investigational
Vitamin EVitamin E may increase the anticoagulant activities of Heparin.Approved, Nutraceutical, Vet Approved
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Heparin.Approved
WarfarinWarfarin may increase the anticoagulant activities of Heparin.Approved
XimelagatranHeparin may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Ym150Heparin may increase the anticoagulant activities of Ym150.Investigational
ZaltoprofenZaltoprofen may increase the anticoagulant activities of Heparin.Approved
ZeranolZeranol may decrease the anticoagulant activities of Heparin.Vet Approved
ZileutonZileuton may increase the anticoagulant activities of Heparin.Approved, Investigational, Withdrawn
ZomepiracZomepirac may increase the anticoagulant activities of Heparin.Withdrawn
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
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 CodesS01XA14C05BA03C05BA53B01AB01B01AB51
AHFS Codes
  • 20:12.04.16
  • 92:00.00
PDB Entries
FDA labelDownload (198 KB)
MSDSDownload (72.1 KB)
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
LiquidSubcutaneous20000 unit
LiquidSubcutaneous5000 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
SolutionIntravenous; Irrigation10 unit
SolutionIntravenous; Irrigation100 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
InjectionIntravenous
Injection, solutionIntravenous10000 [USP'U]/100mL
Injection, solutionIntravenous4000 [USP'U]/100mL
Injection, solutionIntravenous5000 [USP'U]/100mL
InjectionIntravenous200 [USP'U]/100mL
SolutionIntravenous; Subcutaneous5000 unit
SolutionSubcutaneous5000 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
Taxonomy
ClassificationNot classified

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 August 17, 2016 12:23