Ardeparin

Identification

Generic Name
Ardeparin
DrugBank Accession Number
DB00407
Background

Ardeparin, marketed under the US trade name Normiflo, is a low molecular weight heparin (LMWH) anticoagulant used for the prevention of postoperative venous thrombosis. Ardeparin is derived via peroxide degradation of heparin extracted from porcine intestinal mucosa. Its molecular weight ranges from 2000 to 15,000 with an average molecular weight of 5500 to 6500. Normiflo was withdrawn from the US market in March 2000.

Type
Small Molecule
Groups
Approved, Investigational, Withdrawn
Synonyms
Not Available

Pharmacology

Indication

For prevention of deep vein thrombosis, which may result in pulmonary embolism, following knee surgery.

Pharmacology
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Ardeparin, an anticoagulant, is a fractionated heparin. It acts at multiple sites in the normal coagulation system to inhibit reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo.

Mechanism of action

Ardeparin binds to antithrombin III, accelerating its activity in inactivating factor Xa and thrombin, thereby inhibiting thrombosis. Ardeparin also binds to heparin cofactor II, inhibiting thrombin. Ardeparin does not effect prothrombin time (PT) assays and may prolong activated partial thromboplastin time (APTT). Ardeparin has double the anti-factor Xa activity versus anti-factor IIa activity, compared to unfractionated heparin which has approximately equal anti-factor Xa activity and anti-factor IIa activity.

TargetActionsOrganism
AAntithrombin-III
potentiator
Humans
AHeparin cofactor 2
agonist
Humans
Absorption

Well absorbed following subcutaneous administration, with a mean bioavailability of 92% (based on anti-factor Xa activity).

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Liver and the reticulo-endothelial system are the sites of biotransformation.

Route of elimination

Not Available

Half-life

Elimination half-life for anti-factor Xa activity averages 3.3 hours following a single intravenous dose, while elimination half-life for anti-factor IIa activity averages 1.2 hours following a single intravenous dose.

Clearance

Not Available

Adverse Effects
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Toxicity

Symptoms of overdose may include excessive bleeding and bruising.

Pathways
PathwayCategory
Enoxaparin Action PathwayDrug action
Ardeparin Action PathwayDrug action
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 Ardeparin.
AcebutololThe risk or severity of hyperkalemia can be increased when Ardeparin is combined with Acebutolol.
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Ardeparin.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Ardeparin.
AcenocoumarolThe risk or severity of bleeding can be increased when Ardeparin is combined with Acenocoumarol.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Ardeparin.
Albutrepenonacog alfaThe therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Ardeparin.
AlclofenacThe risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Ardeparin.
AldesleukinThe risk or severity of bleeding can be increased when Ardeparin is combined with Aldesleukin.
AlemtuzumabThe risk or severity of bleeding can be increased when Ardeparin is combined with Alemtuzumab.
Interactions
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Food Interactions
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include ginseng, ginkgo, ginger, and garlic.

Products

Products
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International/Other Brands
Normiflo (Wyeth-Ayerst (United States))

Categories

Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
VL0L558GCB
CAS number
9005-49-6
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
Not Available
KEGG Drug
D02980
PubChem Substance
46505194
RxNav
87866
Therapeutic Targets Database
DAP000428
PharmGKB
PA164754878
Drugs.com
Drugs.com Drug Page
Wikipedia
Ardeparin_sodium
MSDS
Download (65.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
  • Wyeth ayerst laboratories
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

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

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets
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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. Mousa SA: The low molecular weight heparin, tinzaparin, in thrombosis and beyond. Cardiovasc Drug Rev. 2002 Fall;20(3):199-216. [Article]
  2. Lin P, Sinha U, Betz A: Antithrombin binding of low molecular weight heparins and inhibition of factor Xa. Biochim Biophys Acta. 2001 Apr 3;1526(1):105-13. [Article]
  3. Shaughnessy SG, Young E, Deschamps P, Hirsh J: The effects of low molecular weight and standard heparin on calcium loss from fetal rat calvaria. Blood. 1995 Aug 15;86(4):1368-73. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Serine-type endopeptidase inhibitor activity
Specific Function
Thrombin inhibitor activated by the glycosaminoglycans, heparin or dermatan sulfate. In the presence of the latter, HC-II becomes the predominant thrombin inhibitor in place of antithrombin III (AT...
Gene Name
SERPIND1
Uniprot ID
P05546
Uniprot Name
Heparin cofactor 2
Molecular Weight
57070.16 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Mousa SA: The low molecular weight heparin, tinzaparin, in thrombosis and beyond. Cardiovasc Drug Rev. 2002 Fall;20(3):199-216. [Article]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Drug created on June 13, 2005 13:24 / Updated on March 04, 2021 11:12