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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
SynonymLanguageCode
CalciparineNot AvailableNot Available
EparinaItalianDCIT
Hep-lockNot AvailableNot Available
HeparinateNot AvailableNot Available
Heparinic acidNot AvailableNot Available
LiquaeminNot AvailableNot Available
PanheprinNot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousPfizer Laboratories Div Pfizer Inc2011-07-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousPfizer Laboratories Div Pfizer Inc2011-07-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousPfizer Laboratories Div Pfizer Inc2011-07-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection10000 [USP'U]/mLintravenous; subcutaneousPfizer Laboratories Div Pfizer Inc2011-07-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousPfizer Laboratories Div Pfizer Inc2013-03-11Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution, concentrate10000 [USP'U]/5mLintravenousHospira, Inc.2010-10-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution, concentrate25000 [USP'U]/10mLintravenousHospira, Inc.2010-10-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution200 [USP'U]/100mLintravenousHospira, Inc.1984-01-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution10000 [USP'U]/100mLintravenousHospira, Inc.1984-01-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/100mLintravenousHospira, Inc.1984-01-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution4000 [USP'U]/100mLintravenousHospira, Inc.1989-01-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/100mLintravenousHospira, Inc.1989-01-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-03-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-03-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection10000 [USP'U]/mLintravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-03-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-03-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousWest Ward Pharmaceutical Corp.1972-03-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Lock Flushsolution10 [USP'U]/mLintravenousGeneral Injectables & Vaccines, Inc2010-08-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Lock Flushsolution100 [USP'U]/mLintravenousGeneral Injectables & Vaccines, Inc2010-08-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousGeneral Injectables & Vaccines, Inc2010-08-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousGeneral Injectables & Vaccines, Inc2010-08-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution100000 [USP'U]/mLintravenous; subcutaneousGeneral Injectables & Vaccines, Inc2010-03-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution, concentrate10000 [USP'U]/5mLintravenousGeneral Injectables & Vaccines, Inc2010-03-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousCardinal Health2011-07-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP&apos'U]/mLintravenous; subcutaneousCardinal Health2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution10000 [USP&apos'U]/mLintravenous; subcutaneousCardinal Health2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP&apos'U]/mLintravenous; subcutaneousCardinal Health2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP&apos'U]/mLintravenous; subcutaneousCardinal Health2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousCardinal Health2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP&apos'U]/.5mLintravenous; subcutaneousCardinal Health2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP&apos'U]/mLintravenous; subcutaneousCardinal Health2009-08-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2009-08-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2011-04-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2009-08-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/.5mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-12-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Lock Flushinjection, solution100 [USP'U]/mLintravenousAPP Pharmaceuticals, LLC2009-08-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Lock Flushinjection, solution10 [USP'U]/mLintravenousAPP Pharmaceuticals, LLC2009-08-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution20000 [USP'U]/mLintravenous; subcutaneousFresenius Kabi USA, LLC2010-06-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.2005-02-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.1987-05-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.2005-01-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.2009-08-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.2009-08-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousHospira, Inc.2009-08-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousSagent Pharmaceticals2010-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection1000 [USP&apos'U]/mLintravenous; subcutaneousSagent Pharmaceticals2014-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousSagent Pharmaceticals2010-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousSagent Pharmaceticals2010-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection5000 [USP&apos'U]/mLintravenous; subcutaneousSagent Pharmaceticals2014-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection10000 [USP'U]/mLintravenous; subcutaneousSagent Pharmaceticals2010-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection10000 [USP&apos'U]/mLintravenous; subcutaneousSagent Pharmaceticals2014-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection20000 [USP'U]/mLintravenous; subcutaneousSagent Pharmaceuticals2010-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP&apos'U]/mLintravenous; subcutaneousSafecor Health, LLC2014-09-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution10000 [USP&apos'U]/mLintravenous; subcutaneousSafecor Health, LLC2014-09-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousGeneral Injectables & Vaccines, Inc2011-09-13Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousGeneral Injectables & Vaccines, Inc2011-09-13Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousCardinal Health2009-12-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection1000 [USP'U]/mLintravenous; subcutaneousCardinal Health2010-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection5000 [USP'U]/mLintravenous; subcutaneousCardinal Health2010-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousCardinal Health2009-08-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousCardinal Health2009-08-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousCardinal Health2009-08-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousCardinal Health2005-01-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution1000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution5000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution10000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heparin Sodiuminjection, solution20000 [USP'U]/mLintravenous; subcutaneousMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2014-06-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
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 mixturesNot Available
Salts
Name/CASStructureProperties
Heparin sodium
ThumbNot applicableDBSALT000417
Categories
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.
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 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 2C19 substrateNot AvailableNot Available
CYP450 3A4 substrateNot 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
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injectionintravenous; subcutaneous1000 [USP&apos'U]/mL
Injectionintravenous; subcutaneous1000 [USP'U]/mL
Injectionintravenous; subcutaneous10000 [USP&apos'U]/mL
Injectionintravenous; subcutaneous10000 [USP'U]/mL
Injectionintravenous; subcutaneous20000 [USP'U]/mL
Injectionintravenous; subcutaneous5000 [USP&apos'U]/mL
Injectionintravenous; subcutaneous5000 [USP'U]/mL
Injection, solutionintravenous10 [USP'U]/mL
Injection, solutionintravenous100 [USP'U]/mL
Injection, solutionintravenous10000 [USP'U]/100mL
Injection, solutionintravenous200 [USP'U]/100mL
Injection, solutionintravenous4000 [USP'U]/100mL
Injection, solutionintravenous5000 [USP'U]/100mL
Injection, solutionintravenous; subcutaneous1000 [USP&apos'U]/mL
Injection, solutionintravenous; subcutaneous1000 [USP'U]/mL
Injection, solutionintravenous; subcutaneous10000 [USP&apos'U]/mL
Injection, solutionintravenous; subcutaneous10000 [USP'U]/mL
Injection, solutionintravenous; subcutaneous100000 [USP'U]/mL
Injection, solutionintravenous; subcutaneous20000 [USP'U]/mL
Injection, solutionintravenous; subcutaneous5000 [USP&apos'U]/.5mL
Injection, solutionintravenous; subcutaneous5000 [USP&apos'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
Solutionintravenous10 [USP'U]/mL
Solutionintravenous100 [USP'U]/mL
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
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySolubleNot Available
logP-13.2Not Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
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 Reference
  1. Linhardt RJ, Gunay NS: Production and chemical processing of low molecular weight heparins. Semin Thromb Hemost. 1999;25 Suppl 3:5-16. Pubmed
  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
  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
  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
  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
  6. American Academy of Pediatrics Committee on Fetus and Newborn and Committee on Drugs. Benzyl alcohol: toxic agent in neonatal units. Pediatrics. 1983; 72:356-8. [PubMed] [IDIS 175725]
  7. Anon. Benzyl alcohol may be toxic to newborns. FDA Drug Bull. 1982; 12:10-1. [PubMed]
  8. Anon. Neonatal deaths associated with use of benzyl alcohol—United States. MMWR Morb Mortal Wkly Rep. 1982; 31:290-1. [PubMed] [IDIS 150868]
  9. Abbott Laboratories. Heparin lock flush solution, USP 100 USP units/mL prescribing information. North Chicago, IL; 1998 Jul.
  10. 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
  11. McDonald MM, Jacobson LJ, Hay WW Jr, Hathaway WE: Heparin clearance in the newborn. Pediatr Res. 1981 Jul;15(7):1015-8. Pubmed
External Links
ATC CodesB01AB01C05BA03S01XA14
AHFS Codes
  • 20:12.04.16
  • 92:00.00
PDB Entries
FDA labelDownload (198 KB)
MSDSDownload (72.1 KB)
Interactions
Drug Interactions
Drug
AbciximabAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
AcenocoumarolMay enhance the anticoagulant effect of other Anticoagulants.
Acetylsalicylic acidAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
AliskirenHeparin may enhance the hyperkalemic effect of Aliskiren.
AlteplaseThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
AmilorideMay enhance the hyperkalemic effect of Potassium-Sparing Diuretics.
Aminosalicylic AcidSalicylates may enhance the anticoagulant effect of Anticoagulants.
AnagrelideAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
AnistreplaseMay enhance the anticoagulant effect of Anticoagulants.
ApixabanMay enhance the anticoagulant effect of Anticoagulants.
ArgatrobanMay enhance the anticoagulant effect of other Anticoagulants.
Azilsartan medoxomilMay enhance the hyperkalemic effect of Angiotensin II Receptor Blockers.
Balsalazide5-ASA Derivatives may enhance the adverse/toxic effect of Heparin. Specifically, the risk for bleeding/bruising may be increased.
BenazeprilMay enhance the hyperkalemic effect of ACE Inhibitors.
Bismuth SubsalicylateSalicylates may enhance the anticoagulant effect of Anticoagulants.
BivalirudinMay enhance the anticoagulant effect of other Anticoagulants.
CanagliflozinHeparin may enhance the hyperkalemic effect of Canagliflozin.
CandesartanMay enhance the hyperkalemic effect of Angiotensin II Receptor Blockers.
CaptoprilMay enhance the hyperkalemic effect of ACE Inhibitors.
CelecoxibNonsteroidal Anti-Inflammatory Agents may enhance the anticoagulant effect of Anticoagulants.
CilazaprilMay enhance the hyperkalemic effect of ACE Inhibitors.
CilostazolAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
CitalopramAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
Citric AcidMay enhance the anticoagulant effect of other Anticoagulants.
ClopidogrelAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
Cyproterone acetateProgestins may diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects.
Dabigatran etexilateMay enhance the anticoagulant effect of Anticoagulants.
DalteparinMay enhance the anticoagulant effect of other Anticoagulants.
DanaparoidMay enhance the anticoagulant effect of other Anticoagulants.
DasatinibMay enhance the anticoagulant effect of Anticoagulants.
DeferasiroxAnticoagulants may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
Deoxycholic AcidAnticoagulants may enhance the adverse/toxic effect of Deoxycholic Acid. Specifically, the risk for bleeding or bruising in the treatment area may be increased.
DesogestrelEstrogen Derivatives may diminish the anticoagulant effect of Anticoagulants. More specifically, the potential prothrombotic effects of some estrogens and progestin-estrogen combinations may counteract anticoagulant effects.
DesvenlafaxineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
DicoumarolMay enhance the anticoagulant effect of other Anticoagulants.
DiflunisalAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
DipyridamoleAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
DrospirenoneEstrogen Derivatives may diminish the anticoagulant effect of Anticoagulants. More specifically, the potential prothrombotic effects of some estrogens and progestin-estrogen combinations may counteract anticoagulant effects.
DuloxetineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
DydrogesteroneMay diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects.
Edetic AcidMay enhance the anticoagulant effect of other Anticoagulants.
EnalaprilMay enhance the hyperkalemic effect of ACE Inhibitors.
EnoxaparinMay enhance the anticoagulant effect of other Anticoagulants.
EplerenoneMay enhance the hyperkalemic effect of Eplerenone.
EpoprostenolProstacyclin Analogues may enhance the adverse/toxic effect of Anticoagulants. Specifically, the antiplatelet effects of these agents may lead to an increased risk of bleeding with the combination.
EprosartanMay enhance the hyperkalemic effect of Angiotensin II Receptor Blockers.
EptifibatideAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
EscitalopramAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
EstropipateEstrogen Derivatives may diminish the anticoagulant effect of Anticoagulants. More specifically, the potential prothrombotic effects of some estrogens and progestin-estrogen combinations may counteract anticoagulant effects.
Ethinyl EstradiolEstrogen Derivatives may diminish the anticoagulant effect of Anticoagulants. More specifically, the potential prothrombotic effects of some estrogens and progestin-estrogen combinations may counteract anticoagulant effects.
Ethyl biscoumacetateMay enhance the anticoagulant effect of other Anticoagulants.
EthynodiolEstrogen Derivatives may diminish the anticoagulant effect of Anticoagulants. More specifically, the potential prothrombotic effects of some estrogens and progestin-estrogen combinations may counteract anticoagulant effects.
EtodolacAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
EtonogestrelProgestins may diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects.
FenoprofenAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
FloctafenineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
FluoxetineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
FluvoxamineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
Fondaparinux sodiumMay enhance the anticoagulant effect of other Anticoagulants.
FosinoprilMay enhance the hyperkalemic effect of ACE Inhibitors.
GestodeneMay diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects.
HomoharringtonineMay enhance the adverse/toxic effect of Omacetaxine. Specifically, the risk for bleeding-related events may be increased.
IbritumomabMay enhance the adverse/toxic effect of Ibritumomab. Both agents may contribute to an increased risk of bleeding.
IbuprofenAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
IcosapentOmega-3 Fatty Acids may enhance the anticoagulant effect of Anticoagulants.
Icosapent ethylOmega-3 Fatty Acids may enhance the anticoagulant effect of Anticoagulants.
IloprostProstacyclin Analogues may enhance the adverse/toxic effect of Anticoagulants. Specifically, the antiplatelet effects of these agents may lead to an increased risk of bleeding with the combination.
IndomethacinAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
IrbesartanMay enhance the hyperkalemic effect of Angiotensin II Receptor Blockers.
KetoprofenAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
KetorolacAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
LevomilnacipranAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
LevonorgestrelProgestins may diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects.
LisinoprilMay enhance the hyperkalemic effect of ACE Inhibitors.
LosartanMay enhance the hyperkalemic effect of Angiotensin II Receptor Blockers.
Magnesium salicylateSalicylates may enhance the anticoagulant effect of Anticoagulants.
Medroxyprogesterone AcetateProgestins may diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects.
Mefenamic acidAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
Megestrol acetateProgestins may diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects.
MeloxicamAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
Mesalazine5-ASA Derivatives may enhance the adverse/toxic effect of Heparin. Specifically, the risk for bleeding/bruising may be increased.
MestranolEstrogen Derivatives may diminish the anticoagulant effect of Anticoagulants. More specifically, the potential prothrombotic effects of some estrogens and progestin-estrogen combinations may counteract anticoagulant effects.
MilnacipranAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
MoexiprilMay enhance the hyperkalemic effect of ACE Inhibitors.
NabumetoneAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
NadroparinMay enhance the anticoagulant effect of other Anticoagulants.
NaproxenAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
NitroglycerinNitroglycerin may diminish the anticoagulant effect of Heparin. Nitroglycerin may decrease the serum concentration of Heparin.
NorelgestrominEstrogen Derivatives may diminish the anticoagulant effect of Anticoagulants. More specifically, the potential prothrombotic effects of some estrogens and progestin-estrogen combinations may counteract anticoagulant effects.
NorethindroneProgestins may diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects.
NorgestimateEstrogen Derivatives may diminish the anticoagulant effect of Anticoagulants. More specifically, the potential prothrombotic effects of some estrogens and progestin-estrogen combinations may counteract anticoagulant effects.
ObinutuzumabAnticoagulants may enhance the adverse/toxic effect of Obinutuzumab. Specifically, the risk of serious bleeding-related events may be increased.
OlmesartanMay enhance the hyperkalemic effect of Angiotensin II Receptor Blockers.
Olsalazine5-ASA Derivatives may enhance the adverse/toxic effect of Heparin. Specifically, the risk for bleeding/bruising may be increased.
OritavancinMay diminish the therapeutic effect of Heparin. Specifically, oritavancin may artificially increase the results of laboratory tests commonly used to monitor IV heparin effectiveness, which could lead to incorrect decisions to decrease heparin doses.
OxaprozinAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
ParoxetineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
Pentosan PolysulfatePentosan Polysulfate Sodium may enhance the anticoagulant effect of Anticoagulants.
PentoxifyllinePentoxifylline may enhance the anticoagulant effect of Heparin.
PerindoprilMay enhance the hyperkalemic effect of ACE Inhibitors.
PhenindioneMay enhance the anticoagulant effect of other Anticoagulants.
PhenprocoumonMay enhance the anticoagulant effect of other Anticoagulants.
PiperazineEstrogen Derivatives may diminish the anticoagulant effect of Anticoagulants. More specifically, the potential prothrombotic effects of some estrogens and progestin-estrogen combinations may counteract anticoagulant effects.
PiroxicamAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
Potassium ChlorideMay enhance the hyperkalemic effect of Potassium Salts.
Potassium IodideMay enhance the hyperkalemic effect of Potassium Salts.
PrasugrelAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
ProgesteroneProgestins may diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects.
QuinaprilMay enhance the hyperkalemic effect of ACE Inhibitors.
RamiprilMay enhance the hyperkalemic effect of ACE Inhibitors.
ReteplaseThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
RidogrelMay enhance the anticoagulant effect of Anticoagulants.
RivaroxabanAnticoagulants may enhance the anticoagulant effect of Rivaroxaban.
Salicylate-sodiumMay enhance the anticoagulant effect of Anticoagulants.
SalsalateSalicylates may enhance the anticoagulant effect of Anticoagulants.
SertralineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
SpironolactoneMay enhance the hyperkalemic effect of Potassium-Sparing Diuretics.
StreptokinaseMay enhance the anticoagulant effect of Heparin.
SugammadexMay enhance the anticoagulant effect of Anticoagulants.
Sulfasalazine5-ASA Derivatives may enhance the adverse/toxic effect of Heparin. Specifically, the risk for bleeding/bruising may be increased.
SulindacAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
SulodexideMay enhance the anticoagulant effect of other Anticoagulants.
TelavancinMay diminish the therapeutic effect of Heparin. Specifically, telavancin may artificially increase the results of laboratory tests commonly used to monitor IV heparin effectiveness, which could lead to incorrect decisions to decrease heparin doses.
TelmisartanMay enhance the hyperkalemic effect of Angiotensin II Receptor Blockers.
TenecteplaseThrombolytic Agents may enhance the anticoagulant effect of Anticoagulants.
Tiaprofenic acidAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
TicagrelorAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
TiclopidineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
TinzaparinMay enhance the anticoagulant effect of other Anticoagulants.
TipranavirTipranavir may enhance the anticoagulant effect of Anticoagulants.
TirofibanAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
TolmetinAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
TositumomabMay enhance the adverse/toxic effect of Tositumomab and Iodine I 131 Tositumomab. Specifically, the risk of bleeding-related adverse effects may be increased.
TrandolaprilMay enhance the hyperkalemic effect of ACE Inhibitors.
TreprostinilProstacyclin Analogues may enhance the adverse/toxic effect of Anticoagulants. Specifically, the antiplatelet effects of these agents may lead to an increased risk of bleeding with the combination.
TriamtereneMay enhance the hyperkalemic effect of Potassium-Sparing Diuretics.
UrokinaseMay enhance the anticoagulant effect of Anticoagulants.
ValsartanMay enhance the hyperkalemic effect of Angiotensin II Receptor Blockers.
VenlafaxineAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
VilazodoneAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
Vitamin EVitamin E may enhance the anticoagulant effect of Anticoagulants. Vitamin E may also increase the overall risk for bleeding.
VorapaxarMay enhance the adverse/toxic effect of Anticoagulants. More specifically, this combination is expected to increase the risk of bleeding.
WarfarinMay enhance the anticoagulant effect of other Anticoagulants.
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

1. Antithrombin-III

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Antithrombin-III P01008 Details

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
    Pubmed
  2. 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
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  4. 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
  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
  6. 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. Epub 2010 Sep 15. Pubmed
  7. 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. Epub 2009 Oct 9. Pubmed

2. Coagulation factor X

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Coagulation factor X P00742 Details

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
  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
  3. Rezaie AR: Heparin-binding exosite of factor Xa. Trends Cardiovasc Med. 2000 Nov;10(8):333-8. Pubmed
  4. Rosenberg RD: Role of heparin and heparinlike molecules in thrombosis and atherosclerosis. Fed Proc. 1985 Feb;44(2):404-9. Pubmed

3. P-selectin

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
P-selectin P16109 Details

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
  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
  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
  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
  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
  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
  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

Enzymes

1. Heparanase

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Heparanase Q9Y251 Details

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 May 14. Pubmed
  2. Nadir Y, Brenner B: Heparanase procoagulant effects and inhibition by heparins. Thromb Res. 2010 Apr;125 Suppl 2:S72-6. Pubmed
  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. Pubmed
  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
  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
  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

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Drug created on June 13, 2005 07:24 / Updated on September 13, 2013 11:03