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Argatroban
drug data and news
Argatroban 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 | Argatroban | ||
| Brand Names/Synonyms | Argatroban | ||
| Indication | For prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Argatroban is a synthetic direct thrombin inhibitor derived from L-arginine indicated as an anticoagulant for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia. Argatroban is a direct thrombin inhibitor that reversibly binds to the thrombin active site. Argatroban does not require the co-factor antithrombin III for antithrombotic activity. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation. Argatroban is highly selective for thrombin with an inhibitory constant (Ki) of 0.04 µM. At therapeutic concentrations, Argatroban has little or no effect on related serine proteases (trypsin, factor Xa, plasmin, and kallikrein). Argatroban is capable of inhibiting the action of both free and clot-associated thrombin. | ||
| Mechanism Of Action | Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation. | ||
| Argatroban News (When available) |
(PRN) Encysive Pharmaceuticals Announces Retirement of Frank C. ... Mar 3, 2006 Encysive Pharmaceuticals Reports Fourth Quarter and Year End 2005 ... Mar 1, 2006 Vegan? Sorry, We Have Porcine Heparin on the Menu! Feb 21, 2006 (PRN) Encysive Pharmaceuticals Announces Presentation/Webcast at ... Feb 2, 2006 Encysive Pharmaceuticals Appoints George W. Cole as Chief ... Nov 14, 2005 Encysive Pharmaceuticals Appoints Paul Manierre as Vice President ... Oct 6, 2005 Encysive Pharmaceuticals Presents Thelin(TM) Data at European ... Sep 6, 2005 Mitsubishi Pharma Launches Selective Antithrombin Agent Argatroban ... Jul 21, 2005 Encysive Pharmaceuticals Reports Second Quarter 2005 Financial ... Aug 4, 2005 Encysive Pharmaceuticals Announces Presentation/Webcast at the ... Jul 25, 2005 Medicure's Antithrombotic Program to be Highlighted at the ... Jul 18, 2005 ARGATROBAN IN POST-CARDIOVASCULAR SURGERY PATIENT WITH HEPARIN ... Jun 22, 2005 SEC Declares Encysive Resale Registration Statement on Form S-3 ... Jun 15, 2005 ARGATROBAN IN POST-CARDIOVASCULAR SURGERY PATIENT WITH HEPARIN ... Jun 22, 2005 SEC Declares Encysive Resale Registration Statement on Form S-3 ... Jun 15, 2005 Encysive Pharmaceuticals Reports First Quarter 2005 Financial ... Apr 28, 2005 New Thelin Data to be Presented at American Thoracic Society's ... Apr 20, 2005 Encysive Pharmaceuticals Reports First Quarter 2005 Financial ... 28 Apr 2005 Encysive Pharmaceuticals Restructures Agreement with Revotar ... Apr 26, 2005 Medicure reports trial successes for novel antithrombotic Mar 1, 2005 Leading Experts In Anticoagulation Recommend That the Medical ... Feb 16, 2005 The Management of Patients With Heparin-Induced Thrombocytopenia ... Feb 21, 2005 Encysive Announces Pricing of $115 Million of Convertible Senior ... Mar 10, 2005 Medicure Reports Positive Preclinical Results For Novel ... Feb 28, 2005 Encysive Pharmaceuticals Reports Fourth Quarter and Year End 2004 ... Feb 17, 2005 Option Activity Watch: Toys "R" Us, Encysive Pharmaceuticals, and ... Feb 14, 2005 Encysive Pharmaceuticals Announces Presentation/Webcast at the BIO ... Feb 17, 2005 Encysive Stock Moves Up 12 Percent On Thelin Data Feb 14, 2005 | ||
| Dosage Forms | SOLUTION | ||
| Drug_Category | Anticoagulants; Anticoagulants; ATC:B01AE03 | ||
| Absorption | Not Available | ||
| Interactions |
Interactions for Argatroban: Heparin: Since heparin is contraindicated in patients with heparin-induced thrombocytopenia, the co-administration of Argatroban and heparin is unlikely for this indication. However, if Argatroban is to be initiated after cessation of heparin therapy, allow sufficient time for heparin's effect on the aPTT to decrease prior to initiation of Argatroban therapy. Aspirin/Acetaminophen: Pharmacokinetic or pharmacodynamic drug-drug interactions have not been demonstrated between Argatroban and concomitantly administered aspirin (162.5 mg orally given 26 and 2 hours prior to initiation of Argatroban 1 µg/kg/min. over 4 hours) or acetaminophen (1000 mg orally given 12, 6 and 0 hours prior to, and 6 and 12 hours subsequent to, initiation of Argatroban 1.5 µg/kg/min. over 18 hours). Oral anticoagulant agents: Pharmacokinetic drug-drug interactions between Argatroban and warfarin (7.5 mg single oral dose) have not been demonstrated. However, the concomitant use of Argatroban and warfarin (5-7.5 mg initial oral dose followed by 2.5-6 mg/day orally for 6-10 days) results in prolongation of the prothrombin time (PT) and International Normalized Ratio (INR). Thrombolytic agents: The safety and effectiveness of Argatroban with thrombolytic agents have not been established. Co-administration: Concomitant use of Argatroban with antiplatelet agents, thrombolytics, and other anticoagulants may increase the risk of bleeding. Drug-drug interactions have not been observed between Argatroban and digoxin or erythromycin. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 1-[5-guanidino-2-[(3-methyl-1,2,3,4-tetrahydroquinolin-8-yl)sulfonylamino]pentanoyl]-4-methyl-piperidine-2-carboxylicacid | ||
| Chemical Formula | C23H36N6O5S | ||
| Molecular Weight | 508.635 g/mol | ||
| Smiles String | CC1CCN(C(C1)C(=O)O)C(=O)C(CCCN=C(N)N)NS(=O)(=O)C2=CC=CC3=C2NCC(C3)C | ||
| Melting Point | Not Available | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | 0.749 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Not Available | ||
| Half Life | 39 and 51 minutes | ||
| Protein Binding [%] | 54% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference | http://www.rxlist.com/cgi/generic2/argatroban.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00105 | ||
| CAS Registry Number | 74863-84-6 | ||
| KEGG Compound ID | C04931 | ||
| PubChem ID | SID:730451 | ||
| PharmGKB ID | PA448477 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2243835 |
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