Heme Drugs EC

Question 1

Heparin (MOA, Use, Tox, Antidote)

Answer 1

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

Question 2

Enoxaparin, Dalteparin (MOA, Advantages/Disadvantages)

Answer 2

Low-molecular-weight heparin (mainly decrease Xa)

Better bio availability
SubQ available
No monitoring
Not easily reversible

Question 3

What is Heparin-Induced Thrombocytopenia (HIT)?

Answer 3

development of IgG antibodies against heparin bound to platelet factor 4

Antibody-heparin-PF4 complex activates platelets leading to THROMBOSIS AND THROMBOCYTOPENIA

Question 4

Lepirudin, Bivalirudin (MOA, Use)

Answer 4

Derivative of leech anticoagulant (hirudin)
INHIBITS THROMBIN

alternative to heparin in patients with HIT

Question 5

Warfarin (MOA, Kinetics, Use, Tox)

Answer 5

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

Question 6

Alteplase (tPA), Reteplase (rPA), Tenecteplase (TNK-tPA) (MOA, Use, Tox)

Answer 6

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)

Question 7

Aspirin (MOA, Bleeding, PT, PTT, Use, Tox)

Answer 7

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

Question 8

Clopidogrel, Ticlopidine, Prasugrel, Ticagrelor (MOA, Use, Tox)

Answer 8

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)

Question 9

Cilostazol, Dipyridamole (MOA, Use, Tox)

Answer 9

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

Question 10

Abciximab, Eptifibatide, Tirofiban (MOA, Use, Tox)

Answer 10

GP IIb/IIIa inhibitors (preventing aggregation)
Abciximab MAB to Fab fragments

Acute coronary syndromes, percutaneous transluminal coronary angioplasty

Bleeding, thrombocytopenia