Ardeparin
Identification
- Name
- Ardeparin
- Accession Number
- DB00407 (APRD00803)
- Type
- Small Molecule
- Groups
- Approved, Investigational, Withdrawn
- Description
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 Normiflo was withdrawn from the US market in March 2000.
- Synonyms
- Not Available
- International/Other Brands
- Normiflo (Wyeth-Ayerst (United States))
- Categories
- UNII
- VL0L558GCB
- CAS number
- 9005-49-6
- Weight
- Not Available
- Chemical Formula
- Not Available
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
Pharmacology
- Indication
For prevention of deep vein thrombosis, which may result in pulmonary embolism, following knee surgery.
- 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 potentiatorHuman AHeparin cofactor 2 agonistHuman - 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
- Toxicity
Symptoms of overdose may include excessive bleeding and bruising.
- Affected organisms
- Humans and other mammals
- Pathways
Pathway Category Ardeparin Action Pathway Drug action Enoxaparin Action Pathway Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction (1,2,6,7-3H)Testosterone The therapeutic efficacy of Ardeparin can be increased when used in combination with (1,2,6,7-3H)Testosterone. (R)-warfarin The risk or severity of bleeding can be increased when Ardeparin is combined with (R)-warfarin. (S)-Warfarin The risk or severity of bleeding can be increased when Ardeparin is combined with (S)-Warfarin. 1-Testosterone The therapeutic efficacy of Ardeparin can be increased when used in combination with 1-Testosterone. 18-methyl-19-nortestosterone The therapeutic efficacy of Ardeparin can be increased when used in combination with 18-methyl-19-nortestosterone. 4-hydroxycoumarin The risk or severity of bleeding can be increased when Ardeparin is combined with 4-hydroxycoumarin. 4-Hydroxytestosterone The therapeutic efficacy of Ardeparin can be increased when used in combination with 4-Hydroxytestosterone. 5beta-dihydrotestosterone The therapeutic efficacy of Ardeparin can be increased when used in combination with 5beta-dihydrotestosterone. Abciximab 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. - Food Interactions
- Not Available
References
- General References
- Not Available
- External Links
- KEGG Drug
- D02980
- PubChem Substance
- 46505194
- Therapeutic Targets Database
- DAP000428
- PharmGKB
- PA164754878
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ardeparin
- MSDS
- Download (65.5 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 1 Completed Basic Science Altered Heparin Response / Cardiopulmonary Bypass 1 2 Completed Prevention Venous Thromboembolism (VTE) 1 2 Terminated Prevention Thrombosis Prophylaxis (Risk of Thrombosis Due to Central Venous Line (CVL) 1 2 Withdrawn Treatment Diabetes, Diabetes Mellitus Type 1 1 3 Completed Prevention Malignancies / Venous Thromboembolism (VTE) 1 3 Completed Prevention Venous Thromboembolism (VTE) 5 3 Completed Treatment Deep Vein Thrombosis (DVT) 1 3 Recruiting Prevention Catheter-Related Infections / Chronic Renal Failure (CRF) 1 3 Terminated Prevention Venous Thromboembolism (VTE) 1 4 Recruiting Treatment Infertilities 1 Not Available Recruiting Not Available Intra Operative Bleeding, Blood Salvage 1
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
Taxonomy
- Classification
- Not classified
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Potentiator
- General Function
- Serine-type endopeptidase inhibitor activity
- Specific Function
- Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade. AT-III inhibits thrombin, matriptase-3/TMPRSS7, as well as factors IXa, Xa and XIa. Its inhibitory 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. [PubMed:12397367]
- 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. [PubMed:11287128]
- 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. [PubMed:7632944]
- Kind
- Protein
- Organism
- Human
- 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. [PubMed:17139284]
- 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. [PubMed:17016423]
- Mousa SA: The low molecular weight heparin, tinzaparin, in thrombosis and beyond. Cardiovasc Drug Rev. 2002 Fall;20(3):199-216. [PubMed:12397367]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Drug created on June 13, 2005 07:24 / Updated on November 02, 2018 04:43