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MedChem II - stack 4

Anticoagulants and related drugs

Drug nameDescription
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
Created by: 100000197460889