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72 Cards in this Set
- Front
- Back
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Aspirin MOA
Acetasalicylic acid ASA |
Irreversible acetylation of cyclooxygenase (COX) --> stop TXA2 synthesis
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Ibuprofen (NSAID) MOA
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Reversibly inhibit COX
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Aspirin Drug Interference
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Ibuprofen
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Acute Therapeutic Uses of Aspirin
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Acute STEMI
Unstable angina or NSTEMI During Pericutaneous Intervention |
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Prophylaxis Uses of Aspirin
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Unstable angina or NSTEMI
Afib PCI Venous thrombosis & pulm embolism Ischemic stroke & Transient ischemic attacks (TIAs) Heart valve replacement |
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Aspirin a/a
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Profound bruising/bleeding
Risk of heartburn & PUD due to inhibited gastric prostaglandin synthesis (cytoprotective) |
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Aspirin pharmacokinetics
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PO
Plasma half life 15-30m; enteric 3-4hr Therapeutic effect 7-10 days |
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Thienopyridine examples
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Clopidogrel
Prasugrel (Ticlopidine) |
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Thienopyridine MOA
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Irreversible antagonists of ADP receptor, P2Y12:
Prevents ADP induced drop in cAMP and subsequent platelet aggregation |
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Clopidogrel Therapeutic Uses: FDA approved
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Acute STEMI - Thrombosis; Prophylaxis
Arteriosclerotic vascular disease - T; P Cerebrovascular accident - T; P MI - T; P NSTEMI, acute - T; P Peripheral arterial occlusive disease - T; P |
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Clopidogrel Therapeutic Uses: Non-FDA
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Afib - Thrombosis; Prophylaxis
Heart Failure - T; P Percutaneous Coronary Intervention - T; P |
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Prasugrel Therapeutic Uses
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Acute coronary syndromes (unstable angina, STEMI, or NSTEMI) with Percuteneous coronary intervention - T; P
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Clopidogrel Adverse Effects
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Profound bruising/bleeding
Rare: Neutropenia, TTP |
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Prasugrel Adverse Effects
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Profound bruising/bleeding
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Thienopyridine PK
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PO
Therapeutic half life 7-10 days Prodrugs activated by CYP2C19 |
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CYP2C19 inhibitor
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Omeprazole (proton pump inhibitor)
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Dipyridamole MOA
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Inhibits phosphodiesterase activity and blocks adenosine uptake --> increases cAMP in smooth muscle and platelets --> vasodilation & reduced platelet activation
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Cilostazol MOA
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Selective for PDE 3 inhibition
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Cilostazol use
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Intermittent claudication
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Dipyridamole Therapeutic Uses
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Secondary prevention of stroke in combo with Aspirin
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Dipyridamole Adverse Effects
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Minor effects that cause 15% of patients to discontinue use
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Dipyridamole PK
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PO
2-3/day |
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Abciximab MOA
(monoclonal antibody) |
Antagonist of integrin receptor (gpIIbIIIa receptor) --> prevents fibrinogen & vWF from binding to platelets, consolidating the platelet plug --> blocks platelet adhesion & aggregation by any stimulus
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Abciximab Therapeutic Uses
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MI
Myocardial ischemia PCI |
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Abciximab Adverse Effects
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Bleeding (major in 1-10%)
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Abciximab PK
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IV
Half life of 30m GP IIb/IIIa bound is 18-24hr |
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Antiplatelet Drugs
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Aspirin
Clopidogrel Prasugrel Dipyridamole Abciximab |
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Indirect Thrombin Inhibitors
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Heparin
Low Molecular Weight Heparins Enoxaparin Fondaparinux |
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Direct Thrombin Inhibitors - Parenteral
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Lepirudin
Bivalirudin |
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Direct Thrombin Inhibitors - Oral
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Dabigatran
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Indirect Oral Anticoagulants
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Warfarin
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Thrombolytic or Fibrinolytic Drugs
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Streptokinase
Alteplase |
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Heparin MOA
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Forms a complex with Antithrombin III and accelerates ATIII inactivation of IIa, IXa, & Xa.
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Heparin PK
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IV or SC
Half life 0.5-2.5hr |
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Heparin Monitoring
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aPTT (goal 1.5-2.5x normal)
Protamine titration |
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Low molecular weight heparin drug
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Enoxaparin
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Enoxaparin MOA
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Accelerates ATIII to inactivate Factor Xa
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Heparin & Enoxaparin Therapeutic Uses
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Venous thromboembolism
Pulmonary embolism DVT prophylaxis (orthopedic and abdominal surgery, spinal cord trauma, immobilized) ACS: unstable angina, STEMI, NSTEMI with antiplatelet therapy During and after PCI Cardiopulmonary bypass surgery |
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Enoxaparin PK
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IV or SC
3-6 hr Greater bioavailability SC Less dosing More predictable No monitoring Factor Xa levels |
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Fondaparinux MOA
(pentasaccharide) |
Accelerates the AT III Fondaparinux complex
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Fondaparinux PK
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SC
Half life 17hr |
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Fondaparinux Therapeutic Uses
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DVT prophylaxis for hip & knee replacement
HIT VTE & Pulmonary Embolism |
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Parenteral Anticoagulant Adverse Effects
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Bleeding
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Heparin and LMWH Adverse Effects
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HIT
HAT Hypersensitivity (heparin) Osteoporosis (rare) |
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Heparin Antidote
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Protamine Sulfate (1mg/100units heparin remaining in pt)
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Parenteral Anticoagulant Contraindications
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Active bleeding
Surgery within 10 days Hemophilia Bleeding peptic ulcer Threatened abortion TTP or previous HIT Advanced hepatic dz (factors) Advanced renal dz (elimination) |
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Lepirudin
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Direct Thrombin Inhibitor
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Bivalirudin
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Direct Thrombin Inhibitor
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Lepirudin Therapeutic Uses
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Patients who need heparin but have had HIT
PCI Microvascular surgery to reattach digits |
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Bivalirudin Therapeutic Uses
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Patients who need heparin but have had HIT
PCI Microvascular surgery to reattach digits |
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Lepirudin MOA
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Direct irreversible inhibition of circulating or clot-bound thrombin
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Bivalirudin MOA
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Direct irreversible inhibition of circulating or clot-bound thrombin
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Lepirudin PK
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IV
Half life 25m |
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Bivalirudin PK
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IV
Half life 25m |
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Dabigatran Etexilate MOA
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Competitive inhibitor of thrombin activity on fibrinogen and platelets, decreasing both coagulation and platelet activity
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Dabigatran Etexilate Therapeutic use
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Prevent thromboembolism in patients with Afib
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Dabigatran Etexilate Adverse Effects
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Bleeding
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Dabigatran Etexilate PK
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PO
Prodrug cleaved by esterases Glucoronidated without CYP450 Dose adjustment with renal disease Half life 12-17hr |
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Warfarin MOA
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Antagonist of Vit K epoxide reductase (II, VII, IX, X, protein C & S)
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Warfarin Time of Action
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8-12 hours
Full effect 3 days |
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Warfarin Therapeutic Uses
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Venous thrombosis following initial parenteral anticoagulant
Pulmonary embolism following "" Long term prophylaxis of VTE Prosthetic valves |
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Warfarin PK
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PO
Half life LONG 99% plasma protein bound - HIGH Hepatic metabolism via CYP Drug interactions common |
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Warfarin Adverse Effects
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Bleeding (monitor INR)
Skin Necrosis Purple Toe Syndrome Teratogenic |
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Warfarin Antidotes
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Vitamin K (Phytonadione)
FFP Prothrombin complex concentrate Recombinant Factor VIIa - severe toxicity or bleeding |
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Warfarin Interactions
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- Drugs which displace from plasma protein & inc bleeding : Aspirin in high doses
- Drugs which inhibit metabolism & inc bleeding: Amiodarone, Clopidogrel, Fluconazole, Ketoconazole, Erythromycin, Omeprazole, Cimetidine |
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Warfarin Warnings
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Pregnancy Category X
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Alteplase MOA
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Binds to fibrin and activates plasminogen conversion to plasmin, permitting fibrin degradation
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Streptokinase MOA
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Binds to fibrin and activates plasminogen conversion to plasmin, permitting fibrin degradation
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Alteplase & Streptokinase Therapeutic Indications
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- Multiple pulm emboli with hemodynamic instability
- Central DVT of ascending thrombophlebitis of iliofemoral vein or superior vena cave syndrome - MI - Acute Ischemic Stroke |
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Alteplase & Streptokinase Adverse Effects
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Hemorrhagic toxicity
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Alteplase & Streptokinase Antidotes
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Epsilon Aminocaproic acid PO, IV
- inhibits plasminogen activation |
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Alteplase & Streptokinase Contraindications
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- Surgery Biopsy, serious trauma, CV resuscitation within 10 days
- Serious GI bleeding in last 3 months - History of HTN (diastolic > 110mmHg) - Active bleeding or threat (CVA, aortic dissection, acute pericarditis) |
