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Fondaparinux
drug data and news
Fondaparinux drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Fondaparinux | ||
| Brand Names/Synonyms | Arixtra; Fondaparinux sodium | ||
| Indication | For the treatment of prophylaxis of deep vein thrombosis. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Fondaparinux is a synthetic and specific inhibitor of activated Factor X (Xa) indicated for the prophylaxis of deep vein thrombosis, which may lead to pulmonary embolism. Fondaparinux is also indicated for the treatment of acute deep vein thrombosis when administered in conjunction with warfarin, and the treatment of acute pulmonary embolism when administered in conjunction with warfarin. Fondaparinux does not inactivate thrombin (activated Factor II) and has no known effect on platelet function. At the recommended dose, Fondaparinux does not affect fibrinolytic activity or bleeding time. | ||
| Mechanism Of Action | The antithrombotic activity of Fondaparinux is the result of antithrombin III (ATIII)-mediated selective inhibition of Factor Xa. By selectively binding to ATIII, Fondaparinux potentiates (about 300 times) the innate neutralization of Factor Xa by ATIII. Neutralization of Factor Xa interrupts the blood coagulation cascade and thus inhibits thrombin formation and thrombus development. | ||
| Fondaparinux News (When available) |
Pivotal Study Published in British Medical Journal Reports ... Feb 13, 2006 Arixtra Effective and Well Tolerated in Acutely Ill Medical ... Feb 14, 2006 Arixtra Administered the Morning After Orthopedic Surgery ... Feb 3, 2006 ARIXTRA(R) Administered the Morning After Orthopedic Surgery ... Feb 3, 2006 Arixtra® Was Effective And Well Tolerated In Acutely Ill Medical ... Feb 14, 2006 GSK's Arixtra Shows Promise in Acutely Ill Patients Feb 14, 2006 Pivotal Study Published in British Medical Journal Reports ... Feb 13, 2006 Arixtra® administered the morning after orthopedic surgery ... Feb 3, 2006 ARIXTRA(R) Administered the Morning After Orthopedic Surgery ... Feb 3, 2006 New Oral Anticoagulants Show Promise Feb 14, 2006 ARIXTRA drug for venous thromboembolism Feb 4, 2006 Arixtra halves blood clot risk, study shows Feb 14, 2006 Arixtra Administered the Morning After Orthopedic Surgery ... Feb 3, 2006 ARIXTRA(R) Administered the Morning After Orthopedic Surgery ... Feb 3, 2006 Arixtra® administered the morning after orthopedic surgery ... Feb 3, 2006 ARIXTRA(R) Administered the Morning After Orthopedic Surgery ... Feb 3, 2006 ARIXTRA drug for venous thromboembolism Feb 4, 2006 New anti-thrombotic therapy effective, safer for patients Sep 10, 2005 Safer, More Effective Anti-Thrombotics Sep 6, 2005 Glaxo drug safer than Sanofi's Lovenox -study Sep 5, 2005 Health Highlights: Sept. 5, 2005 Sep 5, 2005 European Society of Cardiology 2005: Round up Sep 7, 2005 The robot resuscitator Sep 7, 2005 ESC: Lovenox Reduces Bleeding in Elective Angioplasty Sep 7, 2005 ECS: Arixtra Halves Major Bleeding Events in Acute Coronary ... Sep 5, 2005 FDA Safety Labeling Changes: Arixtra and Alora Aug 10, 2005 Prevention of Venous Thromboembolic Disease After Total Hip and ... Sep 1, 2005 Journal of the American Podiatric Medical Association Jul 21, 2005 International Approvals: Tarceva, Arixtra, 1D09C3 Jul 18, 2005 EU Commission approves new use of Arixtra® for prevention of ... Jul 23, 2005 European Commission Approves New Use of Arixtra for Prevention of ... Jul 12, 2005 FDA Approves New Indication for ARIXTRA(R) (fondaparinux sodium) ... May 27, 2005 FDA Approves New Indication for ARIXTRA(R) (Fondaparinux Sodium) ... May 27, 2005 FDA Approves Fondaparinux sodium for Prevention of Venous ... May 27, 2005 Arixtra for prevention of venous thromboembolism in abdominal ... Jun 3, 2005 FDA Approvals: Zemplar Capsules, Arixtra, Glumetza Jun 9, 2005 GlaxoSmithKline's Arixtra gets nod from European Medicines Agency May 27, 2005 Reviparin in Acute Myocardial Infarction—Reply May 31, 2005 EU AUTHORITIES APPROVE GSK'S ACQUISITION OF TWO SANOFI THROMBOSIS ... May 26, 2005 International Approvals: Pegasys, Arixtra, SOT-107 Mar 7, 2005 The Management of Patients With Heparin-Induced Thrombocytopenia ... Feb 21, 2005 | ||
| Dosage Forms | Solution | ||
| Drug_Category | Anticoagulants; Antithrombotics; ATC:B01AX05 | ||
| Absorption | 100% | ||
| Interactions | Interactions for Fondaparinux: In clinical studies performed with Fondaparinux, the concomitant use of oral anticoagulants (warfarin), platelet inhibitors (acetylsalicylic acid), NSAIDs (piroxicam), and digoxin did not significantly affect the pharmacokinetics/pharmacodynamics of fondaparinux sodium. In addition, Fondaparinux neither influenced the pharmacodynamics of warfarin, acetylsalicylic acid, piroxicam, and digoxin, nor the pharmacokinetics of digoxin at steady state. Agents that may enhance the risk of hemorrhage should be discontinued prior to initiation of Fondaparinux therapy. If co-administration is essential, close monitoring may be appropriate. In an in vitro study in human liver microsomes, inhibition of CYP2A6 hydroxylation of coumarin by fondaparinux (200 m m M i.e., 350 mg/L) was 17-28%. Inhibition of the other isozymes evaluated (CYPs 2A1, 2C9, 2C19, 2D6, 3A4, and 3E1) was 0-16%. Since fondaparinux does not markedly inhibit CYP450s (CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4) in vitro, fondaparinux sodium is not expected to significantly interact with other drugs in vivo by inhibition of metabolism mediated by these isozymes. Since fondaparinux sodium does not bind significantly to plasma proteins other than ATIII, no drug interactions by protein-binding displacement are expected. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | decasodium 6-[6-[2-carboxylato-4-hydroxy-6-[4-hydroxy-6-methoxy-5-sulfonatoamino-2-(sulfonatooxymethyl)oxan-3-yl]oxy-5-sulfonatooxy-oxan-3-yl]oxy-5-sulfonatoamino-4-sulfonatooxy-2-(sulfonatooxymethyl)oxan-3-yl]oxy-3-[4,5-dihydroxy-3-sulfonatoamino-6-(sulfonatooxymethyl)oxan-2-yl]oxy-4,5-dihydroxy-oxane-2-carboxylate | ||
| Chemical Formula | C31H43N3Na10O49S8 | ||
| Molecular Weight | 1726.77 g/mol | ||
| Smiles String | COC1C(C(C(C(O1)COS(=O)(=O)[O-])OC2C(C(C(C(O2)C(=O)[O-])OC3C(C(C(C(O3)COS(=O)(=O)[O-])OC4C(C(C(C(O4)C(=O)[O-])OC5C(C(C(C(O5)COS(=O)(=O)[O-])O)O)NS(=O)(=O)[O-])O)O)OS(=O)(=O)[O-])NS(=O)(=O)[O-])O)OS(=O)(=O)[O-])O)NS(=O)(=O)[O-].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+] | ||
| Melting Point | Not Available | ||
| Water Solubility | Not Available | ||
| State | Liquid | ||
| LogP/Hphobicity | Not Available | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Not Available | ||
| Half Life | 17-21 hours | ||
| Protein Binding [%] | 94% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Fondaparinux.html http://www.rxlist.com/cgi/generic3/arixtra.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00500 | ||
| CAS Registry Number | 114870-03-0 | ||
| KEGG Compound ID | C13316 | ||
| PubChem ID | SID:586060 | ||
| PharmGKB ID | PA10083 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2245531 |
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