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MedChem II - stack 4
Anticoagulants and related drugs
| Drug name | Description |
|---|---|
| Heparin | Glycosaminoglycan, serves as template for clotting factor proteases and antithrombin III, decreasing blood clotting, drug of choice in pregnancy |
| Protamine sulfate | Treats bleeding due to heparin overdose |
| Dalteparin Sodium (Fragmin) Enoxaparin Sodium (Lovenox) | Low molecular weight derivatives of heparin, induce conformational changes in antithrombin III, absorbed more uniformly, have longer half-lives |
| Lepirudin (Refludon) | Recombinant derivative of hirudin-a protein (from medical leeches), inhibits thrombin, used as anticoagulant, may lead to antibody formation |
| Danaparoid (Oganon) | Heparan glycosaminoglycan, inhibits factor Xa, used to treat deep venous thrombosis and heparin-induced thrombocytopenia |
| Vitamin K | Lipid soluble vitamin, acts as a cofactor in prothrombin activation, promotes clotting |
| Warfarin Sodium (Coumadin) | Inhibits regeneration of active vitamin K form by inhibiting VKORC1, has multiple drug interactions, binds to plasma proteins, main oral anticoagulant used |
| Dipyridamole (Persantine) | Vasodilator, also capable of increasing c-AMP levels by inhibiting phosphodiesterase, which leads to inhibition of platelet aggregation |
| Ticlopidine HCl (Ticlid) | Inhibits platelet aggregation and the release of platelet granule substances, used to prevent thrombosis in both cerebral vascular and coronary artery disease |
| Clopidogrel bisulfate (Plavix) | Thienopyridine, similar to ticlopidine, somewhat faster and results in an irreversible modification of platelet glycoprotein IIb/IIIa |
| Tirofiban HCl (Aggrastat) | Reversible antagonist of fibrinogen binding to platelet IIb/IIIa receptor, not a thienopyridine, used in conjunction with aspirin and heparin |
| Prasugrel (Effient) | Prodrug that yields an active metabolite which binds irreversibly to P2Y adenosine diphosphate receptor, thus inhibiting aggregatory ability of the platelet |
| Eptifibatide (Integrilin) | First peptide agent to be used as reversible antagonist of platelet receptor IIb/IIIa, may also involve von Willebrand factor and other adhesive ligands, used in unstable angina and non-Q wave MIs |
| Abciximab (Reopro) | FAB fragment of human-murine monoclonal immunoglobulin, binds selectively to platelet IIb/IIIa receptor, used together with aspirin and heparin to prevent abrupt ischemic closure |
| Alteplase (Activase) | Recombinant tissue plasminogen activator, initiates breaking of clots that are already formed |
| Reteplase (Retavase) | Nonglycosylated version of native tPA, has been shown to restore complete blood flow to a higher percentage of patients than alteplase |
| Urokinase (Abbokinase) | Serine protease, activates plasminogen, but is not fibrin-specific |
| Streptokinase (Kabikinase) | Peptide with no intrinsic enzymatic activity, which results in formation of plasmin |
| Aminocaproid Acid (Amicar) | Inhibitor of excessive fibrinolysis, used in hemophiliacs and during prostatic surgery |
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