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63 Cards in this Set
- Front
- Back
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Ticlopidine is activated in what organ?
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Liver
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What does ticlopidine inhibit?
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Purinergic receptors
(P2Y12 type, Gi-protein coupled) |
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How long does it take to see the effect of Ticlopidine?
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4-11 days (check??????)
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Is ticlopidine more or less safe than clopidogrel?
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less safe
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Ticlopidine uses
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Secondary prevention of thrombotic strokes in patients in tolerant of ASA
(something else) |
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What is clopidogrels MoA?
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Same as ticlopidine
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What are the adverse effects of clopidogrel?
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Same as ticlopidine
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What is clopidogrel used for?
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Secondary prevention for recent MI, stroke, or peripheral vascular disease pt
ACS that are treated with either percutaneous coronary intervention or coronary artery bypass grafting |
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What form does prasugrel come in?
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Oral tablet
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What must be monitored in a pt on prasugrel?
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Bleeding or unusual
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How fast is prsugrel absorbed?
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Fast!
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What CYP does prasugrel use to convert to its active metabolite?
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CYP3A4 CYP2B6
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Prasugrel MoA
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Active metabolite binds to platelet P2Y12 adenosine diphosphate (ADP) receptors
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Adverse effects of Prasugrel
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● Bleeding, hypertension, hypotension, headache, hyperlipidemia
● Thrombotic thrombocytopenic purpura (postmarketing) - May occur after short-term (less than 2 wk) exposure |
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Prasugrel uses
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Reduction of thrombotic cardiovascular events (including stent thrombosis)
- Patients with acute coronary syndrome who are to be managed with PCI |
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What are the precautions fofr a pt on Prasugrel
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● Do not use in patients with pathological bleeding or a history of TIA or stroke
● Use is not recommended in patients 75 y of age and older - Exception: high-risk situations like diabetes or a history of MI ● Discontinue at least 7 days prior to any surgery. ● Discontinuing in the first few weeks after ACS increases the risk of CV events |
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Ticagrelor dosage form?
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Oral twice daily
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Are ticagrelor and it's active metabolite bound or unbound to plasma proteins?
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bound
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What metabolizes Ticagrelor?
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CYP3A4
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Is ticagrelor and it's active metabolite weak or strong substrates for P glycoprotein?
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Weak
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Half life of ticagrelor and half life of its active metabolite?
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7 hours and 9 hours
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How do you adjust the dose of ticagrelor for renal impairment, mild hepatic impairment, age?
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You don't adjust it!
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Ticagrelor MoA
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Reversibly binds to the P2Y12 adenosine diphosphate (ADP) receptors on platelets
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Adverse Effects of Ticagrelor
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Bleeding, ventricular pause, atrial fibrillation, hypertension, hypotension
● Headache, dyspnea, increased serum creatinine |
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Ticagrelor Precautions
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● Do not use with active pathological bleeding or history of intracranial hemorrhage
● Discontinue at least 5 days prior to any surgery ● Discontinuing ticagrelor increases the risk of subsequent CV events ● Maintenance doses of aspirin above 100 mg reduce the effectiveness of ticagrelor ● Avoid use with strong inducers or inhibitors of CYP3A ● Avoid simvastatin and lovastatin doses greater than 40 mg |
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Ticagrelor Uses
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● Reduce the rate of thrombotic CV events in acute coronary syndrome (ACS) - Unstable angina, non-ST elevation MI or ST elevation MI
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Abciximab MoA
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● Chimeric Fab fragment of a monoclonal antibody against fibrinogen αIIbβ3 receptor
● Also binds vitronectin receptor ● Receptor binding blocks the binding of fibrinogen ● Binding is essentially irreversible |
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Is abciximab binding reversible or irreversible?
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irreversible
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Adverse effects of Abciximab
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Bleeding, hypoTN, thrombocytopenia
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Abiciximab Uses
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● Adjunct to percutaneous coronary intervention or atherectomy
- Prevent acute cardiac ischemic complications ● Unstable angina not responding to conventional therapy in patients scheduled for PCI |
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Tirofiban MoA
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Small molecule, nonpeptide against fibrinogen αIIbβ3 receptor
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Tirofiban Uses
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Acute coronary syndromes in patient undergoing angioplasty or atherectomy
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Tirofiban adverse effects
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Bleeding, hypoTN, thrombocytopenia
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Eptifibatide MoA
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● Cyclic peptide against fibrinogen αIIbβ3 receptor
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Eptifibatide Adverse effects
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Bleeding! (about 10%), hypoTN, thrombocytopenia
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Eptifibatide Uses
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● Given as a bolus followed by up to 96 hour infusion
● Treat acute coronary syndrome for angioplastic interventions ● Less benefit than abciximab, used with aspirin and heparin |
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Streptokinase MoA
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● Interacts with proactivator (plasminogen)
● Forms equimolar complexes with plasminogen ● Complex converts "free" plasminogen to plasmin ● Releases plasmin |
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What drug is a single chain protein of β-hemolytic streptococci
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Streptokinase
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What is streptokinase used for?
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● ST elevation myocardial infarction
● Arterial thrombosis, deep vein thrombosis, pulmonary embolism ● Intra-arterial or intravenous catheter occlusion ● Thrombi occluding vessels are difficult to lyse - 3 to 7 day old clot usually do not resolve with thrombolytic therapy - Complete dissolution is more difficult with massive clots |
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Streptokinase adverse reactions
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● Hemorrhage
● Allergic reactions ● Febrile response (fever, shivering) |
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Streptokinase Contraindications
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1. Surgery within 10 days, including organ biopsy, puncture of noncompressible vessels, serious trauma, cardiopulmonary resuscitation
2. Serious gastrointestinal bleeding within 3 months 3. History of hypertension (diastolic pressure >110 mm Hg) 4. Active bleeding or hemorrhagic disorder 5. Previous cerebrovascular accident or active intracranial process 6. Aortic dissection 7. Acute pericarditi |
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Which fibrinolytic is administred as a bolus?
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Reteplase, TNK t-PA
(don't know if we need to know..) |
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What fibrinolytic agent is most likely to have an allergic reaction (hypoTN most common)
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Streptokinase
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Which fibrinolytic agent binds fibrin?
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Altaplase, Reteplase, TNK-t-PA
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Which fibrinolytic agent is the least specific?
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Streptokinase
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Which fibrinolytic agent is antigenic?
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Streptokinase
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Which fibrinolytic is the most specific and least specific?
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Most specific : TNK-t-PA
Least specific: Streptokinase |
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Recombinant t-PA (Alteplase) Use
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- Acute myocardial infarction - Acute cerebrovascular thrombosis - Pulmonary embolism - Central venous catheter occlusion
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Alteplase adverse effects
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Cardiac arrhythmia, cholesterol embolus
syndrome, gastrointestinal hemorrhage |
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Tenecteplase comparison and differences to alteplase
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- Recombinant mutant variant of tPA
- Higher affinity for fibrin - Longer half-life than alteplase (can be given as a single bolus) - More resistant to plasma activator inhibitor-1 |
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Tenecteplase use
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Acute MI
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Tenecteplase adverse effects
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Cardiac arrhythmia, cholesterol embolus syndrome, gastrointestinal hemorrhage
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Reteplase comparison to alteplase
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- Recombinant mutant variant of tPA
- Higher affinity for fibrin - Longer half-life than alteplase (can be given as a double bolus) |
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Reteplase Use
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Acute MI
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Reteplase adverse effects
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Cardiac arrhythmia, cholesterol embolus syndrome, gastrointestinal hemorrhage
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Lysine Analogues (aminocaproic acid and tranexamic acid) MoA
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a. Analogues of lysine that bind plasminogen and plasmin
b. Competitive antagonist of activators of plasminogen c. Prevents conversion of plasminogen to plasmin |
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Lysine analogues (aminocaproic acid and tranexamic acid) Uses
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a. Disorder involving the fibrinolytic system
● Hemophilia |
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Lysine analogues adverse effects
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a. Bradyarrhythmia, hypotension, thrombotic disorder, rare renal failure (less than aprotinin)
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Does aprotinin have more or less renal failure than the lysine analogues
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Aprotinin has more renal failure than lysine analogues
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Dipyridamole primarily blocks the action of..?
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adenosine
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Serine Protease Inhibitors (aprotinin) MoA
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a. Peptide of 58 amino acids administered by injection only
b. Inhibitor of a wide variety of protease enzymes c. More potent competitive inhibitor of plasmin than aminocaproic acid |
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Serine protease inhibitors (aprotinin) Uses
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a. Reduce perioperative bleeding during coronary artery bypass graft surgery
b. FDA and Bayer suspended use (severely restricted to research-related work) |
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Serine Protease Inhibitors (aprotinin) Adverse effects
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a. Heart failure, myocardial infarction, shock, thrombotic disorder, renal failure
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