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Winter Exam #2 - Anticoagulants, Antiplatelet Drugs
n/a
17
Pharmacology
Graduate
01/08/2010

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Term
aspirin
Definition
irreversibly inhibits COX --> inhibits thromboxane (TXA2) synthesis, but preserves PGI2 production --> suppresses platelet aggregation & aggravation; Uses: prevents MIs, ischemic attacks, stroke; ADRs: abdominal discomfort, epigastric pain, heartburn, nausea, GI bleeding, impairment of surgical hemostasis, do not use in pregancy (impaired hemostasis in mothery & fetus)
Term
dipyridamole [Persantine]
Definition
inhibits phosphodiesterase --> increases cAMP --> blocks TXA2 production --> blocks platelet adhesion to vascualr subendothelium; also found in combo with aspirin [Aggrenox}; Toxicities: hypotension, minimal side effects
Term
clopidogrel (Plavix)
Definition
selectively inhibits binding of ADP to platelet receptors by irreversibly modifying ADP, preventing ADP-mediated activation of GPIIb/IIIa complex; Uses: reduces atherosclerotic events (MI, stroke, vascular death); Toxicities: bleeding
Term
tirofiban [Aggrastat]
Definition
reversible antagonist of fibrinogen binding to GPIIb/IIIa receptor
Term
Anticoagulants - heparin, protamine sulfate, warfarin, lepirudin,
Definition
drugs that interfere with fibrin formation & are used to prevent thrombus development & extension; Uses: venous thromboembolisms; Precautions: maintain equilibrium between antithrombotic effect & actual bleeding; bleedings is hazard & main complication of therapy; C/Is: cerebral hemorrhage, open ulcerative wounds, traumatic surgery, avoid in pregnancy (teratogenicity & intrauterine hemorrhage)
Term
heparin (Calciparine), enoxaparin sodium (Lovenox)
Definition
anticoagulant that binds to antithrombin III, inactivating factor Xa, inhibiting thrombin formation; Uses: venous thromboembolic dx, arterial thromboembolic dx; Toxicities: bleeding, thrombocytopenia, local capillary rupture, hypersensitivity (porcine or bovine); Adminster SC ONLY, NO IM
Term
protamine sulfate
Definition
cationic low MW proteins that binds to negatively charged heparin to form salt; Uses: tx of severe heparin overdose (IV); Toxicities: hypotension, hypersensitivyt (fish); Administer IV
Term
lepirudin [Refludan]
Definition
recombinant polypeptide that blocks thrombin; Use: anticoagulation in Heparin-Induced Thrombocytopenia (HIT) pts; Toxicities: hypersensitivity, bleeding; Administer IV only
Term
warfarin (Coumadin)
Definition
oral drug that inhibits synthesis of Factors II, VII, IX, X, proteins C & S; Uses: venous thromboemoblic dx, arterial thromboembolic dx; Toxicities: hemorrhage, HTN, skin necrotic lesions, fetal abnormalities (Use heparin instead), drug interactions; ORAL use
Term
streptokinase (Kabikinase)
Definition
non-enzymatic protein that combines with plasminogen coverting it to plasmin; T1/2 = 23 min; Uses: thrombolytic, coronary artery thrombosis, MI; Toxicities: bleeding, hypersensitivity (antibodies), fever; Administer IV infusion
Term
urokinase (Abbokinase)
Definition
u-PA enzyme that cleaves plasminogen to plasmin; T1/2 = 16 min; Uses: thrombolytic, coronary artery thrombosis, MI; Toxicities: bleeding, fever; Administer IV infusion
Term
alteplase (Activase)
Definition
human t-PA that cleaves plasminogen to plasmin in presence of fibrin; T1/2 = 3.6-4.6 min; Uses: thrombolytic, coronary artery thrombosis, MI; Toxicities: bleeding, arrhythmias; Administer IV infusion
Term
aminocaproic acid (Amicar)
Definition
monoamino carboxylic acid that inhibits binding & activation of plasminogen & plasmin to fibrinogen; Uses: overactive fibrinolysis; Toxicities: very mild if any; Administer ORAL or IV
Term
desmopressin acetate (DDAVP)
Definition
synthetic polypeptide analog of vasopressin that causes dose-dependent increase of Factor VIII & von Willebrand factor (vWf); Uses: hemophilia A, von Willebrand dx, decrease blood loss & transfusions; Toxicities: rare --> nausea, thrombosis; aka ADH
Term
factor VIII (Hemofil)
Definition
human blood coagulation factor necessary for coagulation cascade, needed to convert prothrombin to thrombin; Uses: hemophilia A; Toxicities: few & dose related; Other: risk of hepatitis & HIV
Term
factor IX (Konyne)
Definition
human coagulation factor necessary for coagulation cascade (prothrombin to thrombin); Uses: hemophilia B; Toxicities: few & dose related; Risk for HIV & hepatitis
Term
phytonadione (Aquamephyton)
Definition
fat soluble napthoquinone identical to vitamin K1, required for synthesis of blood coagulation factors II, VII, IX, & X; Uses: hypoprothombinemia caused by coumarins, newborn hemorrhagic dx; Toxicities: nontoxic, though anaphylaxis is observed
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