Heparin

Identification

Summary

Heparin is an anticoagulant indicated for thromboprophylaxis and to treat thrombosis associated with a variety of conditions such as pulmonary embolism and atrial fibrillation.

Brand Names
Heparin Leo
Generic Name
Heparin
DrugBank Accession Number
DB01109
Background

Unfractionated heparin (UH) is a heterogenous preparation of anionic, sulfated glycosaminoglycan polymers with weights ranging from 3000 to 30,000 Da. It is a naturally occurring anticoagulant released from mast cells. It binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin (factor IIa) and factor Xa. UH is different from low molecular weight heparin (LMWH) in the following ways: the average molecular weight of LMWH is about 4.5 kDa whereas it is 15 kDa for UH; UH requires continuous infusions; activated partial prothrombin time (aPTT) monitoring is required when using UH; and UH has a higher risk of bleeding and higher risk of osteoporosis in long term use. Unfractionated heparin is more specific than LMWH for thrombin. Furthermore, the effects of UH can typically be reversed by using protamine sulfate.

Type
Small Molecule
Groups
Approved, Investigational
Synonyms
  • Eparina
  • Heparina
  • Heparine
  • Heparinic acid
  • Heparinum
  • Unfractionated heparin
External IDs
  • CY 216
  • CY 222
  • CY216
  • KB 101
  • OP 386
  • OP 622

Pharmacology

Indication

Unfractionated heparin is indicated for prophylaxis and treatment of venous thrombosis and its extension, prevention of post-operative deep venous thrombosis and pulmonary embolism and prevention of clotting in arterial and cardiac surgery. In cardiology, it is used to prevent embolisms in patients with atrial fibrillation and as an adjunct antithrombin therapy in patients with unstable angina and/or non-Q wave myocardial infarctions (i.e. non-ST elevated acute coronary artery syndrome) who are on platelet glycoprotein (IIb/IIIa) receptor inhibitors. Additionally, it is used to prevent clotting during dialysis and surgical procedures, maintain the patency of intravenous injection devices and prevent in vitro coagulation of blood transfusions and in blood samples drawn for laboratory values.

Pharmacology
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Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Unfractionated heparin is a highly acidic mucopolysaccharide formed of equal parts of sulfated D-glucosamine and D-glucuronic acid with sulfaminic bridges. The molecular weight ranges from 3000 to 30,000 daltons. Heparin is obtained from liver, lung, mast cells, and other cells of vertebrates. Heparin is a well-known and commonly used anticoagulant which has antithrombotic properties. Heparin inhibits reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo. Small amounts of heparin in combination with antithrombin III, a heparin cofactor,) can inhibit thrombosis by inactivating Factor Xa and thrombin. Once active thrombosis has developed, larger amounts of heparin can inhibit further coagulation by inactivating thrombin and preventing the conversion of fibrinogen to fibrin. Heparin also prevents the formation of a stable fibrin clot by inhibiting the activation of the fibrin stabilizing factor. Heparin prolongs several coagulation tests. Of all the coagulation tests, activated partial prothrombin time (aPTT) is the most clinically important value.

Mechanism of action

Under normal circumstances, antithrombin III (ATIII) inactivates thrombin (factor IIa) and factor Xa. This process occurs at a slow rate. Administered heparin binds reversibly to ATIII and leads to almost instantaneous inactivation of factors IIa and Xa The heparin-ATIII complex can also inactivate factors IX, XI, XII and plasmin. The mechanism of action of heparin is ATIII-dependent. It acts mainly by accelerating the rate of the neutralization of certain activated coagulation factors by antithrombin, but other mechanisms may also be involved. The antithrombotic effect of heparin is well correlated to the inhibition of factor Xa. Heparin is not a thrombolytic or fibrinolytic. It prevents progression of existing clots by inhibiting further clotting. The lysis of existing clots relies on endogenous thrombolytics.

TargetActionsOrganism
AAntithrombin-III
potentiator
Humans
ACoagulation factor X
inhibitor
Humans
UP-selectin
inhibitor
Humans
UFibroblast growth factor receptor 4Not AvailableHumans
UFibroblast growth factor 4Not AvailableHumans
UFibroblast growth factor 19Not AvailableHumans
UFibroblast growth factor receptor 1Not AvailableHumans
UFibroblast growth factor 1Not AvailableHumans
UFibroblast growth factor receptor 2Not AvailableHumans
UFibroblast growth factor 2Not AvailableHumans
UPlatelet factor 4Not AvailableHumans
UHepatocyte growth factorNot AvailableHumans
Absorption

Heparin 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 binding

Very 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 elimination

The 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-life

1.5 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

Adverse Effects
Adverseeffects
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Toxicity

In mouse, the median lethal dose is greater than 5000 mg/kg. Another side effect is heparin-induced thrombocytopenia (HIT syndrome). Platelet counts usually do not fall until between days 5 and 12 of heparin therapy. HIT is caused by an immunological reaction that makes platelets form clots within the blood vessels, thereby using up coagulation factors. It can progress to thrombotic complications such as arterial thrombosis, gangrene, stroke, myocardial infarction and disseminated intravascular coagulation. Symptoms of overdose may show excessive prolongation of aPTT or by bleeding, which may be internal or external, major or minor. Therapeutic doses of heparin give for at least 4 months have been associated with osteoporosis and spontaneous vertebral fractures. Osteoporosis may be reversible once heparin is discontinued. Although a causal relationship has not been established, administration of injections preserved with benzyl alcohol has been associated with toxicity in neonates. Toxicity appears to have resulted from administration of large amounts (i.e., about 100–400 mg/kg daily) of benzyl alcohol in these neonates. Its use is principally associated with the use of bacteriostatic 0.9% sodium chloride intravascular flush or endotracheal tube lavage solutions.

Pathways
PathwayCategory
Heparin Action PathwayDrug action
Fc Epsilon Receptor I Signaling in Mast CellsSignaling
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Heparin.
AcebutololThe risk or severity of hyperkalemia can be increased when Heparin is combined with Acebutolol.
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Heparin.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Heparin is combined with Acemetacin.
AcenocoumarolThe risk or severity of bleeding can be increased when Heparin is combined with Acenocoumarol.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Heparin.
Albutrepenonacog alfaThe therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Heparin.
AlclofenacThe risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Heparin.
AldesleukinThe risk or severity of bleeding can be increased when Heparin is combined with Aldesleukin.
AlemtuzumabThe risk or severity of bleeding can be increased when Heparin is combined with Alemtuzumab.
Interactions
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Food Interactions
  • Administer calcium supplement. This drug decreases calcium levels.
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Products

Products2
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dosage, form, labeller, route of administration, and marketing period.
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Product Ingredients
IngredientUNIICASInChI Key
Heparin calciumM4F288ZCTR37270-89-6Not applicable
Heparin sodiumZZ45AB24CANot AvailableNot applicable
International/Other Brands
Calcilean / Calciparine / Hepalean / Heparin LEO / Liquaemin / Liquemin / Multiparin / Novoheparin
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Calcilean Inj 20000unit/0.8mlLiquid20000 unit / .8 mLSubcutaneousOrganon Teknika Canada Inc.1987-12-311997-08-11Canada flag
Calciparine Inj 20000iu/ampLiquid20000 unit / ampSubcutaneousChoay Lab1974-12-311998-06-09Canada flag
Calciparine Inj 5000iuLiquid5000 unit / syrSubcutaneousChoay Lab1977-12-311998-06-09Canada flag
Hep-LockSolution10 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-02-02US flag
Hep-LockSolution10 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-02-02US flag
Hep-LockSolution100 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-06-28US flag
Hep-LockSolution100 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-06-28US flag
Hep-LockSolution10 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-02-02US flag
Hep-LockSolution100 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-02-02US flag
Hep-LockSolution10 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-02-02US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Heparin Lock FlushInjection, solution10 [USP'U]/1mLIntravenousHospira, Inc.1943-04-272011-03-01US flag
Heparin Lock FlushInjection, solution100 [USP'U]/1mLIntravenousHospira, Inc.1943-04-272011-07-01US flag
Heparin SodiumInjection, solution1000 [USP'U]/1mLIntravenous; SubcutaneousCardinal Health2010-07-062017-09-11US flag
Heparin SodiumInjection, solution10000 [USP'U]/1mLIntravenous; SubcutaneousCardinal Health2009-12-07Not applicableUS flag
Heparin SodiumInjection1000 [USP'U]/1mLIntravenous; SubcutaneousMeitheal Pharmaceuticals Inc.2019-06-15Not applicableUS flag
Heparin SodiumInjection, solution200 [USP'U]/100mLIntravenousFresenius Kabi Norge As2020-07-24Not applicableUS flag
Heparin SodiumInjection1000 [USP'U]/1mLIntravenous; SubcutaneousMylan Institutional LLC2019-03-192021-07-31US flag
Heparin SodiumInjection, solution5000 [USP'U]/1mLIntravenous; SubcutaneousHospira, Inc.2009-08-31Not applicableUS flag
Heparin SodiumInjection, solution1000 [USP'U]/1mLIntravenous; SubcutaneousSagent Pharmaceticals2014-07-012020-02-29US flag
Heparin SodiumInjection, solution5000 [USP'U]/1mLIntravenous; SubcutaneousAurobindo Pharma Limited2014-06-12Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
BARICUS JEL , 50 GHeparin sodium (0.4 mg/g) + Allantoin (10 mg/g) + Onion (100 mg/g)GelTopicalSANTA FARMA İLAÇ SAN. A.Ş.2020-08-14Not applicableTurkey flag
CONTRACTUBEX ® GELHeparin sodium (5000 IU) + Allantoin (1 g) + Onion (10 g)GelTopicalLABORATORIOS BIOPAS S.A2006-11-102012-07-24Colombia flag
CONTRACTUBEX JEL, 100 GHeparin sodium (40 mg/100g) + Allantoin (1 g/100g) + Onion (10 g/100g)GelTopicalASSOS İLAÇ KİMYA GIDA ÜRÜNLERİ ÜRETİM VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
CONTRACTUBEX JEL, 120 GHeparin sodium (40 mg/100g) + Allantoin (1 g/100g) + Onion (10 g/100g)GelTopicalASSOS İLAÇ KİMYA GIDA ÜRÜNLERİ ÜRETİM VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
CONTRACTUBEX JEL, 150 GHeparin sodium (40 mg/100g) + Allantoin (1 g/100g) + Onion (10 g/100g)GelTopicalASSOS İLAÇ KİMYA GIDA ÜRÜNLERİ ÜRETİM VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
CONTRACTUBEX JEL, 50 GHeparin sodium (40 mg/100g) + Allantoin (1 g/100g) + Onion (10 g/100g)GelTopicalASSOS İLAÇ KİMYA GIDA ÜRÜNLERİ ÜRETİM VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
Heparin Sod and 0.9% Sod Chloride InjHeparin (2 unit / mL) + Sodium chloride (9 mg / mL)SolutionIntravenousBaxter Laboratories1990-12-31Not applicableCanada flag
Heparin Sodium & 5% Dextrose Injection LiqHeparin sodium (10000 unit / 100 mL) + Dextrose, unspecified form (5 g / 100 mL)SolutionIntravenousBaxter Laboratories1992-12-312011-02-01Canada flag
Heparin Sodium & Dextrose 5% In Viaflex LiqHeparin sodium (5000 unit / 100 mL) + Dextrose, unspecified form (5 g / 100 mL)SolutionIntravenousBaxter Laboratories1991-12-312011-02-01Canada flag
Heparin Sodium 20000units In 5% Dextrose InjHeparin sodium (4000 unit / 100 mL) + Dextrose, unspecified form (5 g / 100 mL)SolutionIntravenousB. Braun Medical Inc.1996-09-10Not applicableCanada flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Heparin Lock FlushHeparin sodium (100 [USP'U]/1mL)Injection, solutionIntravenousFresenius Kabi USA, LLC2009-08-122019-06-06US flag
Heparin Lock FlushHeparin sodium (10 [USP'U]/1mL)Injection, solutionIntravenousFresenius Kabi USA, LLC2009-08-292017-11-06US flag
Heparin SodiumHeparin sodium (40 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2014-04-08Not applicableUS flag
Heparin SodiumHeparin sodium (4 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-11-13Not applicableUS flag
Heparin SodiumHeparin sodium (0.5 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-03-22Not applicableUS flag
Heparin SodiumHeparin sodium (30 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2013-11-22Not applicableUS flag
Heparin SodiumHeparin sodium (10 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-10-26Not applicableUS flag
Heparin SodiumHeparin sodium (5 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2011-02-18Not applicableUS flag
Heparin SodiumHeparin sodium (4 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-05-09Not applicableUS flag
Heparin SodiumHeparin sodium (100 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-08-29Not applicableUS flag

Categories

ATC Codes
B01AB51 — Heparin, combinationsC05BA03 — HeparinS01XA14 — HeparinC05BA53 — Heparin, combinationsB01AB01 — Heparin
Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
T2410KM04A
CAS number
9005-49-6

References

Synthesis Reference

Fernando Fussi, Gianfranco Fedeli, "Oligo-heteropolysaccharides having a heparin-like activity method for their preparation and pharmaceutical compositions based thereon." U.S. Patent US4757057, issued June, 1952.

US4757057
General References
  1. Linhardt RJ, Gunay NS: Production and chemical processing of low molecular weight heparins. Semin Thromb Hemost. 1999;25 Suppl 3:5-16. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  7. McDonald MM, Jacobson LJ, Hay WW Jr, Hathaway WE: Heparin clearance in the newborn. Pediatr Res. 1981 Jul;15(7):1015-8. [Article]
  8. Authors unspecified: Benzyl alcohol: toxic agent in neonatal units. Pediatrics. 1983 Sep;72(3):356-8. [Article]
  9. Authors unspecified: Benzyl alcohol may be toxic to newborns. FDA Drug Bull. 1982 Aug;12(2):10-1. [Article]
  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. [Article]
KEGG Compound
C00374
PubChem Substance
46507594
RxNav
5224
ChEBI
28304
ChEMBL
CHEMBL1909300
Therapeutic Targets Database
DAP000189
PharmGKB
PA449855
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Heparin
FDA label
Download (198 KB)
MSDS
Download (72.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingPreventionComplications; Catheter / End Stage Renal Disease (ESRD) / Hemodialysis Access Failure (Disorder) / Hemodialysis Catheter Infection / Vascular Access Complications1
4CompletedNot AvailableRenal Insufficiency, Acute1
4CompletedDiagnosticInsulin Resistance Syndrome X / Pancreatic Beta Cell Function1
4CompletedDiagnosticMesenteric vascular insufficiency1
4CompletedDiagnosticPulmonary Embolism1
4CompletedPreventionAnaesthesia therapy / Pediatrics / Vasospasm1
4CompletedPreventionAnticoagulation / Cardiopulmonarybypass / Surgery, Cardiac1
4CompletedPreventionCatheter Related Infections1
4CompletedPreventionChronic Kidney Disease (CKD)1
4CompletedPreventionCirculation, Extracorporeal / Surgery, Cardiac1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Amerisource Health Services Corp.
  • Amsino Medical Usa
  • APP Pharmaceuticals
  • B. Braun Melsungen AG
  • Baxter International Inc.
  • Becton Dickinson
  • Bioiberica Sa
  • Cardinal Health
  • Eisai Inc.
  • General Injectables and Vaccines Inc.
  • Hospira Inc.
  • Mason Distributors
  • Medefil Inc.
  • Medical Techniques LLC
  • Neuman Distributors Inc.
  • Pfizer Inc.
  • Pharmacia Inc.
  • Sagent Pharmaceuticals
  • Sandhills Packaging Inc.
  • Spectrum Pharmaceuticals
  • Tyco Healthcare Group LP
  • Vetter Pharma Fertigung GmbH and Co. KG
Dosage Forms
FormRouteStrength
GelTopical
Capsule
SolutionIntravenous
LiquidSubcutaneous20000 unit / .8 mL
Injection, solutionIntravenous; Parenteral20000 UI/4ML
Injection, solutionParenteral; Subcutaneous12500 IU/0.5ML
Injection, solutionParenteral; Subcutaneous5000 IU/0.2ML
Injection, solutionSubcutaneous12500 IU/0.5ml
Injection, solutionSubcutaneous12500 IU
Injection, solutionSubcutaneous125000 IU/0.5ml
Injection, solutionSubcutaneous20000 IU
Injection, solutionSubcutaneous20000 IU/0.8ml
Injection, solutionSubcutaneous5000 IU/0.2ml
LiquidSubcutaneous20000 unit / amp
LiquidSubcutaneous5000 unit / syr
Tablet, delayed release
Tablet, extended release
Injection, solution
GelCutaneous
Injection, solutionSubcutaneous
Injection, solutionSubcutaneous25000 IU/ml
Injection, solutionIntravenous
Injection, solutionIntravenous; Subcutaneous50000 U
Injection, solutionParenteral5000 IU/ML
Injection, solutionIntravenous25000 IU/5ML
Injection, solutionIntravenous; Subcutaneous5000 IU/1ML
SolutionParenteral250 IU/5ML
SolutionParenteral300 IU/3ML
SolutionParenteral500 IU/2ML
GelTopical60000 IE
Ointment60000 IE
GelTopical50000 IE
Pill
SolutionIntravenous10 [USP'U]/1mL
SolutionIntravenous100 [USP'U]/1mL
GelTopical30000 IE
Ointment30000 IE
GelTopical150000 IE
SolutionIntravenous; Subcutaneous25000 unit / mL
SolutionIntravenous10 unit / mL
SolutionIntravenous100 unit / mL
Injection, solutionIntravenous100 1/1mL
CreamTopical300 IU
CreamTopical600 IU
Ointment60000 IU
GelTopical50000 IU
Ointment30000 IU
Ointment50000 IU
GelTopical300 IU
Solution / dropsOphthalmic
Injection, solutionParenteral
InjectionParenteral
LiquidUnknown100 unit / mL
LiquidIntravenous; Subcutaneous10000 unit / mL
LiquidIntravenous; Subcutaneous1000 unit / mL
LiquidIntravenous; Subcutaneous25000 unit / mL
Injection, solutionIntravenous10 [USP'U]/1mL
Injection, solutionIntravenous100 [USP'U]/1mL
SolutionIntraperitoneal10 unit / mL
SolutionIntravenous; Irrigation10 unit / mL
SolutionIntravenous; Irrigation100 unit / mL
Injection, solutionParenteral25000 IE
Injection, solutionParenteral25000 IE/5ML
Injection, solutionParenteral25000 IU/5mL
Injection, solutionParenteral5000 IU/0.2mL
Injection, solutionParenteral7500 IU/0.3mL
Injection, solutionParenteral250000 IU/10mL
Injection, solutionParenteral5000 IU
GelTopical180000 IU
Ointment300 IU/g
Ointment600 IU/g
Injection, solutionParenteral25000 IU
SolutionIntravenous
InjectionIntravenous; Subcutaneous1000
InjectionIntravenous; Subcutaneous1000 [USP'U]/1mL
InjectionIntravenous; Subcutaneous10000
InjectionIntravenous; Subcutaneous10000 [USP'U]/1mL
InjectionIntravenous; Subcutaneous2000 [USP'U]/2mL
InjectionIntravenous; Subcutaneous20000 [USP'U]/1mL
InjectionIntravenous; Subcutaneous5000 [USP'U]/0.5mL
InjectionIntravenous; Subcutaneous5000 [USP'U]/1mL
Injection, solutionIntravenous0.5 [USP'U]/1mL
Injection, solutionIntravenous1 [USP'U]/1mL
Injection, solutionIntravenous2 [USP'U]/1mL
Injection, solutionIntravenous200 [USP'U]/100mL
Injection, solutionIntravenous30 [USP'U]/1mL
Injection, solutionIntravenous4 [USP'U]/1mL
Injection, solutionIntravenous40 [USP'U]/1mL
Injection, solutionIntravenous5 [USP'U]/1mL
Injection, solutionIntravenous50 [USP'U]/1mL
Injection, solutionIntravenous; Subcutaneous1000 [USP'U]/1mL
Injection, solutionIntravenous; Subcutaneous1000
Injection, solutionIntravenous; Subcutaneous10000 [USP'U]/1mL
Injection, solutionIntravenous; Subcutaneous10000
Injection, solutionIntravenous; Subcutaneous2000 [USP'U]/2mL
Injection, solutionIntravenous; Subcutaneous20000 [USP'U]/1mL
Injection, solutionIntravenous; Subcutaneous5000 [USP'U]/0.5mL
Injection, solutionIntravenous; Subcutaneous5000 [USP'U]/1mL
Injection, solutionIntravenous; Subcutaneous5000
Injection, solution, concentrateIntravenous10000 [USP'U]/5mL
Injection, solution, concentrateIntravenous12500
Injection, solution, concentrateIntravenous20000
Injection, solution, concentrateIntravenous25000 [USP'U]/10mL
SolutionIntravenous40 unit / mL
SolutionIntravenous50 unit / mL
LiquidIntravenous
Injection, solutionIntravenous1000 [iU]/500mL
Injection, solutionIntravenous2000 [iU]/1000mL
SolutionIntravenous2 unit / mL
InjectionIntravenous
Injection, solutionIntravenous10000 [USP'U]/100mL
Injection, solutionIntravenous4000 [USP'U]/100mL
Injection, solutionIntravenous5000 [USP'U]/100mL
InjectionIntravenous200 [USP'U]/100mL
Injection, solutionIntravesical200 [USP'U]/100mL
SolutionIntravenous; Subcutaneous5000 unit / mL
SolutionSubcutaneous5000 unit / 0.5 mL
SolutionIntravenous; Subcutaneous1000 unit / mL
SolutionIntravenous; Subcutaneous10000 unit / mL
SolutionIntravenous25000 IU
SolutionParenteral5000 U
SolutionSubcutaneous1000 IU
SolutionIntravenous5000 IU
SolutionSubcutaneous5000 IU
SolutionIntravenous; Subcutaneous5000 IU
SolutionSubcutaneous5 IU
Injection
InjectionIntravenous
CreamTopical30000 IU
CreamTopical60000 IU
GelTopical0.3 g
GelTopical
GelTopical100000 IU
Injection, solutionIntravenous; Subcutaneous
Injection, solutionIntravenous5000 IU/ml
Injection, solutionIntravenous; Parenteral12500 UI/2.5ML
Injection, solutionIntravenous; Parenteral5000 UI/1ML
Injection, solutionParenteral; Subcutaneous5000 UI/ML
Injection, solutionSubcutaneous5000 IU/ml
PasteTopical
Injection, solutionIntravenous; Parenteral25000 IU/5ML
Injection, solutionParenteral; Subcutaneous5000 IU/ML
SolutionIntravenous; Subcutaneous
Injection, solutionIntramuscular
CreamRectal
Injection, solutionParenteral12500 IU/0.5ML
Injection, solutionParenteral12500 UI
Injection, solutionParenteral20000 UI
Injection, solutionParenteral5000 UI/0.2ML
Injection, solutionParenteral5000 UI
OintmentTopical
Injection, solutionParenteral; Subcutaneous12500 UI/0.5ML
Tablet
GelTopical100000 IE
Ointment100000 IE
GelTopical180000 IE
Ointment180000 IE
GelTopical200 IU/G
CreamTopical600 IU/g
GelTopical600 IU/g
InjectionIntravenous; Subcutaneous
Tablet, film coated
Injection, solutionParenteral5000 U.I./1ML
GelTopical30000 IU
CreamTopical
GelTopical60000 IU
GelTopical150.000 IE
SprayCutaneous
Solution5000 unit/1ml
Injection, solution5000 unit/1ml
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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Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySolubleNot Available
logP-13.2Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Potentiator
General Function
Serine-type endopeptidase inhibitor activity
Specific Function
Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade. AT-III inhibits thrombin, matriptase-3/TMPRSS7, as well as factors IXa, Xa and XIa. Its inhibitory a...
Gene Name
SERPINC1
Uniprot ID
P01008
Uniprot Name
Antithrombin-III
Molecular Weight
52601.935 Da
References
  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. [Article]
  2. Sun W, Bandmann H, Schrader T: A fluorescent polymeric heparin sensor. Chemistry. 2007;13(27):7701-7. [Article]
  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. [Article]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Serine-type endopeptidase activity
Specific Function
Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.
Gene Name
F10
Uniprot ID
P00742
Uniprot Name
Coagulation factor X
Molecular Weight
54731.255 Da
References
  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. [Article]
  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. [Article]
  3. Rezaie AR: Heparin-binding exosite of factor Xa. Trends Cardiovasc Med. 2000 Nov;10(8):333-8. [Article]
  4. Rosenberg RD: Role of heparin and heparinlike molecules in thrombosis and atherosclerosis. Fed Proc. 1985 Feb;44(2):404-9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sialic acid binding
Specific Function
Ca(2+)-dependent receptor for myeloid cells that binds to carbohydrates on neutrophils and monocytes. Mediates the interaction of activated endothelial cells or platelets with leukocytes. The ligan...
Gene Name
SELP
Uniprot ID
P16109
Uniprot Name
P-selectin
Molecular Weight
90833.105 Da
References
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays a role in the regulation of cell proliferation, differentiation and migration, and in regulation o...
Gene Name
FGFR4
Uniprot ID
P22455
Uniprot Name
Fibroblast growth factor receptor 4
Molecular Weight
87953.535 Da
References
  1. Loo BM, Kreuger J, Jalkanen M, Lindahl U, Salmivirta M: Binding of heparin/heparan sulfate to fibroblast growth factor receptor 4. J Biol Chem. 2001 May 18;276(20):16868-76. Epub 2001 Feb 21. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Heparin binding
Specific Function
Plays an important role in the regulation of embryonic development, cell proliferation, and cell differentiation. Required for normal limb and cardiac valve development during embryogenesis.
Gene Name
FGF4
Uniprot ID
P08620
Uniprot Name
Fibroblast growth factor 4
Molecular Weight
22047.355 Da
References
  1. Bellosta P, Iwahori A, Plotnikov AN, Eliseenkova AV, Basilico C, Mohammadi M: Identification of receptor and heparin binding sites in fibroblast growth factor 4 by structure-based mutagenesis. Mol Cell Biol. 2001 Sep;21(17):5946-57. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Fibroblast growth factor receptor binding
Specific Function
Involved in the suppression of bile acid biosynthesis through down-regulation of CYP7A1 expression, following positive regulation of the JNK and ERK1/2 cascades. Stimulates glucose uptake in adipoc...
Gene Name
FGF19
Uniprot ID
O95750
Uniprot Name
Fibroblast growth factor 19
Molecular Weight
24002.345 Da
References
  1. Harmer NJ, Pellegrini L, Chirgadze D, Fernandez-Recio J, Blundell TL: The crystal structure of fibroblast growth factor (FGF) 19 reveals novel features of the FGF family and offers a structural basis for its unusual receptor affinity. Biochemistry. 2004 Jan 27;43(3):629-40. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation ...
Gene Name
FGFR1
Uniprot ID
P11362
Uniprot Name
Fibroblast growth factor receptor 1
Molecular Weight
91866.935 Da
References
  1. Ibrahimi OA, Zhang F, Hrstka SC, Mohammadi M, Linhardt RJ: Kinetic model for FGF, FGFR, and proteoglycan signal transduction complex assembly. Biochemistry. 2004 Apr 27;43(16):4724-30. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
S100 protein binding
Specific Function
Plays an important role in the regulation of cell survival, cell division, angiogenesis, cell differentiation and cell migration. Functions as potent mitogen in vitro.
Gene Name
FGF1
Uniprot ID
P05230
Uniprot Name
Fibroblast growth factor 1
Molecular Weight
17459.58 Da
References
  1. Robinson CJ, Harmer NJ, Goodger SJ, Blundell TL, Gallagher JT: Cooperative dimerization of fibroblast growth factor 1 (FGF1) upon a single heparin saccharide may drive the formation of 2:2:1 FGF1.FGFR2c.heparin ternary complexes. J Biol Chem. 2005 Dec 23;280(51):42274-82. Epub 2005 Oct 11. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosi...
Gene Name
FGFR2
Uniprot ID
P21802
Uniprot Name
Fibroblast growth factor receptor 2
Molecular Weight
92024.29 Da
References
  1. Robinson CJ, Harmer NJ, Goodger SJ, Blundell TL, Gallagher JT: Cooperative dimerization of fibroblast growth factor 1 (FGF1) upon a single heparin saccharide may drive the formation of 2:2:1 FGF1.FGFR2c.heparin ternary complexes. J Biol Chem. 2005 Dec 23;280(51):42274-82. Epub 2005 Oct 11. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ligand-dependent nuclear receptor transcription coactivator activity
Specific Function
Plays an important role in the regulation of cell survival, cell division, angiogenesis, cell differentiation and cell migration. Functions as potent mitogen in vitro.
Gene Name
FGF2
Uniprot ID
P09038
Uniprot Name
Fibroblast growth factor 2
Molecular Weight
30769.715 Da
References
  1. Rose K, Kriha D, Pallast S, Junker V, Klumpp S, Krieglstein J: Basic fibroblast growth factor: lysine 134 is essential for its neuroprotective activity. Neurochem Int. 2007 Jul;51(1):25-31. Epub 2007 Apr 19. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Heparin binding
Specific Function
Released during platelet aggregation. Neutralizes the anticoagulant effect of heparin because it binds more strongly to heparin than to the chondroitin-4-sulfate chains of the carrier molecule. Che...
Gene Name
PF4
Uniprot ID
P02776
Uniprot Name
Platelet factor 4
Molecular Weight
10844.78 Da
References
  1. Greinacher A, Althaus K, Krauel K, Selleng S: Heparin-induced thrombocytopenia. Hamostaseologie. 2010 Jan;30(1):17-8, 20-8. [Article]
  2. Visentin GP, Ford SE, Scott JP, Aster RH: Antibodies from patients with heparin-induced thrombocytopenia/thrombosis are specific for platelet factor 4 complexed with heparin or bound to endothelial cells. J Clin Invest. 1994 Jan;93(1):81-8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Serine-type endopeptidase activity
Specific Function
Potent mitogen for mature parenchymal hepatocyte cells, seems to be a hepatotrophic factor, and acts as a growth factor for a broad spectrum of tissues and cell types. Activating ligand for the rec...
Gene Name
HGF
Uniprot ID
P14210
Uniprot Name
Hepatocyte growth factor
Molecular Weight
83133.115 Da
References
  1. Sakata H, Stahl SJ, Taylor WG, Rosenberg JM, Sakaguchi K, Wingfield PT, Rubin JS: Heparin binding and oligomerization of hepatocyte growth factor/scatter factor isoforms. Heparan sulfate glycosaminoglycan requirement for Met binding and signaling. J Biol Chem. 1997 Apr 4;272(14):9457-63. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Syndecan binding
Specific Function
Endoglycosidase that cleaves heparan sulfate proteoglycans (HSPGs) into heparan sulfate side chains and core proteoglycans. Participates in extracellular matrix (ECM) degradation and remodeling. Se...
Gene Name
HPSE
Uniprot ID
Q9Y251
Uniprot Name
Heparanase
Molecular Weight
61148.17 Da
References
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Serine-type endopeptidase inhibitor activity
Specific Function
Major thyroid hormone transport protein in serum.
Gene Name
SERPINA7
Uniprot ID
P05543
Uniprot Name
Thyroxine-binding globulin
Molecular Weight
46324.12 Da
References
  1. CYTOMEL (liothyronine) FDA label [File]

Drug created on June 13, 2005 13:24 / Updated on September 28, 2021 07:54