Chapter 20: Blood Drugs Flashcards
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor aspirin?
MOA: decrease the formation of a clot; inhibits thromboxane A2 synthesis from arachidonic acid in platelets by irreversible acetylation of serine; this prevents archidonic acid from binding and inhibits COX1 which occurs in the portal circulation
indications: prophylactic treatment of transient cerebral ischemia, reduce incidents of MI, decrease mortality in pre/post MI patients
pharmokinetics: repeated infusion with aspirin has a cumulative effect on the function of platelets; used in combo with heparin or clopidogrel
adverse effects: higher doses inhibit prostacyclin formation, hemmorhagic strokes, GI bleeds
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor Triclopidine?
MOA: irreversibly inhibit binding of ADP to platelet receptors which inactivates GP IIb/IIIa receptors which are required for the platelets to bind to fibrinogen and to each other
indications: prevention of transient ischemia ttack and strokes; used with aspirin after coronary stent implantation
pharmokinetics:
adverse effects: neutropenia/agranulocytosis, TTP, aplastic anemia
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor Clopidogrel?
MOA: irreversibly inhibit binding of ADP to platelet receptors which inactivates GP IIb/IIIa receptors which are required for the platelets to bind to fibrinogen and to each other
indications: prevention of atheroscleotic events; prophylaxis in acute coronary syndrome (ex unstable angina); prophylaxis in percutaneous coronary intervention; preferred in ischemic heart diseases
pharmokinetics: oral ingestion and undergo hepatic metabolism; eliminated fecally and through urine
adverse effects: black box warning for patients that are poor metabolizers
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor Prasugrel?
MOA: irreversibly inhibit binding of ADP to platelet receptors which inactivates GP IIb/IIIa receptors which are required for the platelets to bind to fibrinogen and to each other; newest ADP receptor antagonist
indications: decrease thrombotic cardiovascular events in patients with acute coronary syndrome; more effective than Clopidogrel in reducing cardiovascular death, nonfatal heart attack and nonfatal stroke
pharmokinetics: oral ingestion and undergo hepatic metabolism; eliminated fecally and through urine
adverse effects: black box warning for bleeding, strokes, abrupt discontinuation in patients undergoing percutaneous coronary interventions
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor Prasugrel?
MOA: irreversibly inhibit binding of ADP to platelet receptors which inactivates GP IIb/IIIa receptors which are required for the platelets to bind to fibrinogen and to each other; newest ADP receptor antagonist
indications: decrease thrombotic cardiovascular events in patients with acute coronary syndrome; more effective than Clopidogrel in reducing cardiovascular death, nonfatal heart attack and nonfatal stroke
pharmokinetics: oral ingestion and undergo hepatic metabolism; eliminated fecally and through urine
adverse effects: black box warning for bleeding, strokes, abrupt discontinuation in patients undergoing percutaneous coronary interventions
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor Abciximab?
MOA: block GP IIb/IIIa receptor that which inhibits platelet aggregation by preventing binding of fibrinogen and vWF so that aggregation doesn’t occur
indications: percutaneous coronary intervention to prevent cardiac ischemic complications; unresponsive unstable angina; prophylaxis in MI
pharmokinetics: given IV along with heparin or aspirin
adverse effects: potential for bleeding
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor Eptifibatide and Tirofiban?
MOA: block GP IIb/IIIa receptor
indications: can decrease the incidence of thombotic complciations associated with acute coronary syndrome
pharmokinetics: rapidly cleared in plasma; Eptifibatide is excreted by the kidney; Tirofiban unchanged by kidney and feces
adverse effects: bleeding
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor Eptifibatide and Tirofiban?
MOA: block GP IIb/IIIa receptor
indications: can decrease the incidence of thombotic complciations associated with acute coronary syndrome
pharmokinetics: rapidly cleared in plasma; Eptifibatide is excreted by the kidney; Tirofiban unchanged by kidney and feces
adverse effects: bleeding
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor Dipyridamole?
MOA: coronary vasodilator; decreases platelet adhesion to thrombogenic surfaces
indications: prophylactic treatment of angina pectoris; given in combo with aspirin or warfarin; inhibits embolization from prosthetic heart valves
pharmokinetics: inhibits cyclic nucleotide phosphodiesterase which increases intracellular levels of cAMP which results in decreased thromboxane A2 synthesis
adverse effects: inappropriate use in elderly as a sole agent due to GI and orthostatic problems
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor Cilostazol?
MOA: vasodilator
indications: reduce symptoms of intermittent cla
pharmokinetics:
adverse effects:
What is the MOA, indications, pharmokinetics and adverse effects of the platelet aggregation inhibitor Cilostazol?
MOA: vasodilator
indications: reduce symptoms of intermittent claudication, treatment of Buerger disease, vascular sclerosis complicating diabetes, chronic cerebral ischemia
pharmokinetics: inhibits phosphodiesterase type III which increases cAMP levels in platelets preventing platelet aggregation and promotes vasodilation of blood vessels
adverse effects: decreases levels of plasma triglyceridesl increases HDL; headaches and GI problems ; contraindicated in patients with CHF
What is the MOA, indications, pharmokinetics, and adverse effects of the thrombin inhibitors (anticoagulants)?
MOA: binds to antithrombin III and inactivates coagulation factors thrombin (factor IIa) and Factor Xa
- LMWHs complex with antithrombin III and inactivate Factor Xa but do not bind to thrombin
- LMWHs are less likely to activate resting platelets
indications: prevent/treat acute DVT; treatment of PE and acute MI;
- prevent fibrin formation; coagulant of choice in pregnant women with prosthetic heart valves or venous thrombosis since these agents don’t cross the placenta
pharmokinetics: heparin inject IV acts within minutes; LMWH subcutaneous injection acts within hours
- heparin must be given parenterally since it doesn’t readily cross membranes and it is administered as a bolus to achieve immediate anticoagulation
adverse effects: bleeding complications(managed with protamine sulfate), HS, thombosis, thombocytopenia, abnormal liver function tests
What is the MOA, indications, pharmokinetics, and adverse effects of the thrombin inhibitor dabigatran etexilate?
MOA: direct thrombin inhibitor
indications: prevention of stroke and systemic embolus in patients with atrial fibrillation
pharmokinetics: oral anticoagulant
adverse effects: bleeding
What is the MOA, indications, pharmokinetics, and adverse effects of the anticoagulant Lepirudin?
MOA: highly specific thombin antagonist with little effect on platelet aggregation
indications: treatment of HIT and other thomboembolic disorders and prevent further thombotic complications
pharmokinetics: administered IV; eliminated in urine
adverse effects: bleeding and about half of patients develop antibodies to this drug
What is the MOA, indications, pharmokinetics, and adverse effects of the anticoagulant of Argatroban?
MOA: directly inhibits thombin
indications: prophetically for the treatment of thrombosis in patients with HIT, approved for percutaneous coronary interventions in patients at risk for having HIT
pharmokinetics: parenteral anticoagulant; metabolized by liver
adverse effects: bleeding
What is the MOA, indications, pharmokinetics, and adverse effects of the anticoagulant Fondaparinux?
MOA: selectively inhibits antithrombin III which neutralizes the actions of Factor Xa
indications: prophylaxis of DVT; used in combo with warfarin for treatment of acute pulmonary embolism and acute DVT
pharmokinetics: subcutanous; eliminated in the urine
adverse effects: bleeding episodes but thombocytopenia is not a problem and this agent may be used in patients with HIT
What is the MOA, indications, pharmokinetics, and adverse effects of the anticoagulant Fondaparinux?
MOA: selectively inhibits antithrombin III which neutralizes the actions of Factor Xa
indications: prophylaxis of DVT; used in combo with warfarin for treatment of acute pulmonary embolism and acute DVT
pharmokinetics: subcutaneous; eliminated in the urine
adverse effects: bleeding episodes but thombocytopenia is not a problem and this agent may be used in patients with HIT
What is the MOA, indications, pharmokinetics, and adverse effects of Vitamin K antagonists? ex: Warfarin
MOA: warfarin treatment causes production of clotting factors with low activity due to lack of sufficient gamma-carboxyglutamyl side chains
indications: used to prevent acute DVT or PE after initial heparin treatment; prophylactically used in patients with acute MI, prosthetic heart valves and chronic atrial fibrillation
pharmokinetics: oral administration; 100% bioavailability; 99% plasma protein bound so it does not diffuse into CSF, urine, or breast milk; readily crosses placental barrier
adverse effects: bleeding disorders, drug interactions (sulfonamides), contraindicated in pregnancy since it is teratogenic and can cause abortion
What is the MOA, indications, pharmokinetics, and adverse effects of thombolytic drugs in general?
MOA: all act to cleave plasminogen to plasmin which cleaves fibrin causing lysis of thrombi; clots are more resistant to lysis the more they age so initiate therapy earlier
indications: not really used anymore in DVT and PE because there is too high of a risk of serious bleeding; but they are still used in catheter and shunt function to prevent occlusion; also used to resolve clots in strokes
pharmokinetics: intracoronary delivery however they are usually administered IV since this route is more rapid, inexpensive and doesn’t have the risk of catheterization
adverse effects: hemmorhage; contraindicated in patients with healing wounds, pregnancy, history of cerebrovascular events, head trauma, intracranial bleeding, and metastatic cancer
What is the MOA, indications, pharmokinetics, and adverse effects of thombolytic drugs in general?
MOA: all act to cleave plasminogen to plasmin which cleaves fibrin causing lysis of thrombi; clots are more resistant to lysis the more they age so initiate therapy earlier
indications: not really used anymore in DVT and PE because there is too high of a risk of serious bleeding; but they are still used in catheter and shunt function to prevent occlusion; also used to resolve clots in strokes
pharmokinetics: intracoronary delivery however they are usually administered IV since this route is more rapid, inexpensive and doesn’t have the risk of catheterization
adverse effects: hemmorhage; contraindicated in patients with healing wounds, pregnancy, history of cerebrovascular events, head trauma, intracranial bleeding, and metastatic cancer
What is the MOA, indications, pharmokinetics, and adverse effects of the thombolytic drug Alteplase?
- 9MOA: low affinity for free plasminogen but rapidly activates plasminogen that is bound to fibrin in a thrombus; at low doses it has the advantage of lysing only fibrin
indications: treatment of MI, massive PE, acute ischemic stroke; superior to streptokinase in dissolving older clots
pharmokinetics: administered in a total dose of 0.9mg/kg
adverse effects: bleeding complications, GI, cerebral hemorrhage
What is the MOA, indications, pharmokinetics, and adverse effects of the thombolytic drug Streptokinase?
MOA:
indications:
pharmokinetics:
adverse effects:
What is the MOA, indications, pharmokinetics, and adverse effects of the thombolytic drug Urokinase?
MOA:
indications:
pharmokinetics:
adverse effects:
What is the MOA, indications, pharmokinetics, and adverse effects of the thombolytic drug Streptokinase?
MOA: unspecific and systemic hydrolysis of fibrin plugs
indications: acute PE, DVT, acute MI, arterial thombosis, occluded shunts
pharmokinetics: administered within 4 hours of acute MI for 1hr
adverse effects: bleeding disorders; HS since streptokinase is a foreign protein that is antigenic
