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 Normiflo was withdrawn from the US market in March 2000.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- Approved, Investigational, Withdrawn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.
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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.
Target Actions Organism AAntithrombin-III potentiatorHumans AHeparin cofactor 2 agonistHumans - 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
Pathway Category Enoxaparin Action Pathway Drug action Ardeparin Action Pathway Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of bleeding can be increased when Abciximab is combined with Ardeparin. Acebutolol The risk or severity of hyperkalemia can be increased when Ardeparin is combined with Acebutolol. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Ardeparin. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Ardeparin is combined with Acemetacin. Acenocoumarol The risk or severity of bleeding can be increased when Ardeparin is combined with Acenocoumarol. - Food Interactions
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include ginseng, ginkgo, ginger, and garlic.
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
- External Links
- KEGG Drug
- D02980
- PubChem Substance
- 46505194
- 87866
- Therapeutic Targets Database
- DAP000428
- PharmGKB
- PA164754878
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ardeparin
- MSDS
- Download (65.5 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
Pharmacoeconomics
- Manufacturers
- Wyeth ayerst laboratories
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Soluble Not Available - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- 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
- Mousa SA: The low molecular weight heparin, tinzaparin, in thrombosis and beyond. Cardiovasc Drug Rev. 2002 Fall;20(3):199-216. [Article]
- 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]
- 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
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- 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]
- Mousa SA: The low molecular weight heparin, tinzaparin, in thrombosis and beyond. Cardiovasc Drug Rev. 2002 Fall;20(3):199-216. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Drug created at June 13, 2005 13:24 / Updated at November 03, 2023 23:41