Heme Drugs EC Flashcards
Heparin (MOA, Use, Tox, Antidote)
Cofactor for antithrombin activation (decraese thrombin and Xa)
Immediate anticoagulation for PE, acute coronary syndrome, MI, DVT.
Used during pregnancy (big and does not cross placenta)
Can cause bleeding, thrombocytopenia, osteoporosis, drug-drug interactions
Antidote= Protamine sulfate (+ charged so it binds)
Follow PTT
Enoxaparin, Dalteparin (MOA, Advantages/Disadvantages)
Low-molecular-weight heparin (mainly decrease Xa)
Better bio availability
SubQ available
No monitoring
Not easily reversible
What is Heparin-Induced Thrombocytopenia (HIT)?
development of IgG antibodies against heparin bound to platelet factor 4
Antibody-heparin-PF4 complex activates platelets leading to THROMBOSIS AND THROMBOCYTOPENIA
Lepirudin, Bivalirudin (MOA, Use)
Derivative of leech anticoagulant (hirudin)
INHIBITS THROMBIN
alternative to heparin in patients with HIT
Warfarin (MOA, Kinetics, Use, Tox)
Interferes with gamma carboxylation of vit. K dependent clotting factors (II, VII, IX, X, proteins C&S)
Metabolized by P450s
Effect on EXTRINSIC PATHWAY AND PT (follow INR)
Chronic anticoagulation
NOT USED IN PREGNANT WOMEN
Bleeding, teratogenic, skin/tissue necrosis, drug-drug interactions
Alteplase (tPA), Reteplase (rPA), Tenecteplase (TNK-tPA) (MOA, Use, Tox)
Thrombolytics
Aid in conversion of plasminogen to plasmin (cleaves thrombin and fibrin clots)
Increases PT and PTT with no change in platelet count
Used in early MI, ischemic stroke, sever PE
Treat toxicity with AMINOCAPROIC ACID (inhibits fibrinolysis)
Aspirin (MOA, Bleeding, PT, PTT, Use, Tox)
Irreversibly inhibits COX1&2 by covalent acetylation
Platelets cannot synthesize new enzyme (lasts until new platelets are produced)
Increases bleeding time, Decreases TXA2 and prostaglandins
No effect on PT or PTT
Antipyretic, Analgesic, Anti-Inflammatory, Antiplatelet
Can cause gastric ulceration, tinnitus.
Acute renal failure, interstitial nephritis, upper GI bleed.
Reye’s syndrome in children with viral infection
Overuse causes respiratory alkalosis and metabolic acidosis
Clopidogrel, Ticlopidine, Prasugrel, Ticagrelor (MOA, Use, Tox)
ADP receptor inhibitors (inhibit platelet aggregation)
Inhibit fibrinogen binding to glycoprotein IIb/IIIa
Acute coronary syndrome, Coronary stenting, Decrease incidence of thrombotic stroke
Neutropenia (ticlopidine)
Cilostazol, Dipyridamole (MOA, Use, Tox)
PDE III inhibitor (increase cAMP in platelets, inhibiting aggregation)
Vasodilate
Intermittent claudication, coronary vasodilation, prevent stroke, angina prophylaxis
Nausea, headache, facial flushing, hypotension, abdominal pain
Abciximab, Eptifibatide, Tirofiban (MOA, Use, Tox)
GP IIb/IIIa inhibitors (preventing aggregation)
Abciximab MAB to Fab fragments
Acute coronary syndromes, percutaneous transluminal coronary angioplasty
Bleeding, thrombocytopenia