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Pharmacology - Block 2 - Part 2

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davidwurbel7's version from 2016-07-03 00:12

Anticoagulant Drug

Question Answer
This enzyme converts phospholipids into arachidonic acidPhospholipase A2
The fibrinogen receptor on platelets is thisGP IIb/IIIa
This drug acetylates a serine residue in the active sites for both COX-1 & COX-2, which irreversibly inhibits these enzymesAspirin
Low doses aspirin (81-325 mg/d) selectively inhibits this enzymeCOX-1
At high doses, aspirin inhibits this enzymeCOX-1 and COX-2
These drugs irreversibly blocks the ADP receptor on platelets, thereby reducing platelet aggregation. It has no effect on prostaglandin metabolism (unlike aspirin)Clopidogrel and Ticlopidine
This drug is a prodrug that must be metabolized by CYP 2C19 to be effectiveClopidogrel
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Question Answer
Codeine is metabolized by this enzymeCYP 2D6
Clopidogerel is metabolized by this enzymeCYP 2C19
Warfarin is metabolized by this enzymeCYP 2C9
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Question Answer
The mechanism of action of Clopidogrel and Ticlopidine irreversibly blocks these on plateletsADP Receptors
This drug can cause severe neutropenia and thrombocytopenic purpura requiring regular monitoring of blood counts (hence has limited value as an antiplatelet)Ticlopidine
This drug has less incidence of neutropenia or thrombocytopenia and therefore is the preferred ADP Receptor AntagonistClopidogrel
This drug reversible P2Y12 inhibitor that inhibits ADP-induced platelet aggregation It is not a prodrug, and does not require metabolic conversion to an active metabolite as a result it produces an immediate effect when infused, and its therapeutic effects can be maintained with continuous infusion. Side effect has potential for autoimmune reactions manifesting as dyspneaCangrelor
This drug is only used in patients that are undergoing percutaneous coronary intervention (PCI) for anti-coagulationCangrelor
This drug is a monoclonal antibodies directed against gpIIb/IIIa receptor complexAbciximab
This drug is given along with aspirin and heparin during coronary angioplasty. Use has shown markedly reduce the incidence of re-stenosisAbciximab
The Mechanism of Action of this drug is a protease-activated receptor-1 (PAR-1) antagonist. Blocks thrombin-mediated platelet activation without interfering with thrombin-mediated cleavage of fibrinogen. Decreases the tendency of platelets to clump together to form a clotVorapaxar
These drugs are GP IIb/IIIa receptor antagonistsEptifibatide and Tirofiban
Eptifibatide and Tirofiban inhibiting the final, common pathway of platelet aggregation by binding to thisGP IIb/IIIa Receptor
The indiction for these drugs is given along with aspirin and heparin during coronary angioplasty (PTCA)Eptifibatide and Tirofiban
The mechanism of action of this drug is a protease-activated receptor-1 (PAR-1) antagonist. Blocks thrombin-mediated platelet activation without interfering with thrombin-mediated cleavage of fibrinogen. Decreases the tendency of platelets to clump together to form a clot. It is Indicated for recent MI, or established peripheral artery diseaseVorapaxar
Fibrinolytic obtained from streptococciStreptokinase
Fibrinolytic derived from human tissue and is no longer is common useUrokinase
Fibrinolytics that are recombinant DNA technologyAlteplase and Reteplase
The mechanism of this drug is a protein (not an enzyme) synthesized by streptococci that combines with plasminogen and increases its conversion to active plasmin. The side effects: Bleeding, allergic reactions, hypotension, feverStreptokinase
The mechanism of this drug binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin. This initiates local fibrinolysis with limited systemic proteolysis.tPA
The indications for this drug are acute myocardial infarction (STEMI) in adults for the improvement of ventricular function following acute myocardial infarction, acute massive pulmonary embolism and acute ischemic stroke (must be given within 3 hours) tPA
The contraindications for this drug is Non-ST elevated myocardial ischemia (NSTEMI) that result from incomplete blockage of a coronary artery by platelet aggregationtPA
This fibrinolytic drug binds to circulating plasminogen preventing further thrombus formationStreptokinase
This fibrinolytic drug binds to fibrin bound plaminogen converting the fibrin to plasmin breaking the thrombustPA
The mechanism of action is to inhibit plasminogen activation. Used to treat excessive bleeding due to overdose of fibrinolytic agentsAnti-Fibrinolytics
Aminocaproic acid and Tranexamic acid are examples of this class of drugAnti-Fibrinolytics
Unfractionated Heparin (UFH) and Low molecular weight heparins (LMWH) are this class of anticoagulantIndirect Thrombin Inhibitors
Lepuridin, argatroban, and dabigatran are this class of anticoagulantDirect Thrombin Inhibitors
Warfarin is this class of anticoagulantVitamin K Epoxide Reductase Inhibitors (Oral anticoagulant)
Rivaroxiban and apixaban are this class of anticoagulantDirect Factor Xa Inhibitors
A straight chain mucopolysaccharide with a large molecular weight. The mechanism of anticoagulant action is it activates antithrombin III and inactivates clotting factors in intrinsic pathway-thrombin (IIa), IXa, XaUnfractionated Heparin (UFH)
A strong acidic drug that can be neutralized by basic compounds like protamine. Highly ionised. Not absorbed orally Given i.v/ s.c. Dose monitored by aPTT (activated partial thromboplastin time)Unfractionated Heparin (UFH)
Heparin overdose/bleeding can be neutralized by thisProtamine
The normal aPTT (activated partial thromboplastin time) should be between25 seconds and 39 seconds
The aPTT (activated partial thromboplastin time) should be between45 seconds and 75 seconds
Has lower molecular weight. Selectively inhibits Factor Xa, less effect on thrombin and is given subcutaneous. Advantages - Less hemorrhagic complication, less thrombocytopenia. Equally efficacious. Increased bioavailability. Less frequent dosing..because of longer half life. Less effect on aPTTLow Molecular Weight (LMW) Heparins
Indications for this drug for the prophylaxis of deep vein thrombosis. Those undergoing abdominal surgery who are at risk for thromboembolic complication. Those undergoing hip replacement surgery, during and following hospitalization. Those undergoing knee replacement surgery. Those who are at risk for thromboembolic complications due to severely restricted mobility during acute illness for the prophylaxis of ischemic complications of unstable angina and non-Q-wave myocardial infarction, when concurrently administered with aspirinHeparin
Adverse effects of this drug Hemorrhage – nose bleeds, hematuria, tarry stools may be noted as the first sign of bleeding, petechial formations and easy bruising may precede frank bleeding close monitoring of activated partial thromoplastin time (aPTT), Heparin induced Thrombocytopenia and Osteoporosis- on prolonged useHeparin
If this occurs in a patient on heparin therapy - Stop heparin and give a direct thrombin inhibitor or FondaparinuxHeparin Induced Thrombocytopenia
Only anticoagulate that can be used in pregnancyLow Molecular Weight (LMW) Heparins
The mechanism of action of this drug is it avidly binds antithrombin with high specificity, resulting in inactivation of factor Xa. Does not cross react with pathologic HIT antibodies in most patientsFondaparinux
The indications for this drug include prophylaxis of Deep Vein Thrombosis, treatment of either acute deep vein thrombosis or acute pulmonary embolism when administered with warfarin and anticoagulation in patients with Heparin-induced-Thrombocytopenia (HIT)Fondaparinux
A recombinant form of Hirudin, which is a specific, irreversible inhibitor of thrombin found in the saliva of leeches. Inhibits thrombin directly. Its action is independent of antithrombinLepirudin
Inhibits thrombin directly. Its action is independent of antithrombin. Indication as alternatives to heparin in Heparin induced thrombocytopeniaArgatroban
Inhibits thrombin directly. Its action is independent of antithrombin. Indication to reduce the risk of stroke and embolism in patients with non-valvular atrial fibrillationDabigatran
Mechanism of Action is a direct Xa inhibitor. Use in prevention of venous thromboembolism following hip or knee surgeryRivaroxiban
Mechanism of Action is a direct Xa inhibitor. Used as prophylaxis for reduction of risk of stroke and systemic embolism in nonvalvular atrial fibrillationApixaban
The gamma carboxylation synthesis of clotting factors is effected by this drugWarfarin
Warfarin inhibits this enzyme in the gamma carboxylation synthesis of clotting factorsVitamin K Epoxide Reductase
The mechanism of action is by preventing the gamma carboxylation of glutamate residues of clotting factorsWarfarin
This test is used to monitor the dose of WarfarinInternational Normalized Ratio (INR)
The recommended International Normalized ratio (INR) is this2-3
Warfarin is contraindicated in thisPregnancy
These drugs interact with warfarin by reducing the synthesis of clotting factors by reducing Vitamin K productionBroad-Spectrum Antibiotics
These drugs interact with warfarin by inhibiting the metabolism of warfarinCYP Inhibitors
These drugs interact with warfarin by increasing the metabolism of warfarinCYP Inducers
Aspirin, phenytoin, Sulfonamides interact with warfarin by thisProtein Binding Displacement
Treatment for overdose fo this drug is to stop the drug, Vitamin K1, Fresh frozen plasmaWarfarin
A rare complication seen during first week of therapy with warfarin..due to reduced protein C synthesis. It manifests as dermal necrosis of extremities or breastSkin Necrosis
Used for long term anticoagulation- for maintenance for Deep vein thrombosis, Pulmonary embolism, Acute Myocardial infarction, Coronary angioplasty along with fibrinolytics, Atrial fibrillation, Cerebrovascular disease, Vascular surgery, prosthetic heart valvesWarfarin
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Anemia Treatment
Question Answer
This class of drugs reduce the absorption of ironTetracyclines
Adverse effects of this drug include Epigastric pain, Nausea, vomiting, Constipation, Staining of teeth and Metallic taste if taken orallyIron Supplements
Ferrous sulfate, Ferrous gluconate and Ferrous fumerate are of this type of iron supplementOral Iron Supplements
Iron dextran, Sodium ferric gluconate complex and Iron sucrose are of this type of iron supplementParenteral Iron Supplements
Indications for route include oral iron not tolerated, Severe deficiency, Malabsorption, Non complianceParenteral Iron Supplements
Common in infants and children. Manifestations include vomiting, haematemesis, bloody diarrhea followed by shock, Severe metabolic acidosis, coma, deathIron Poisoning
Iron chelating agent used for treatment of Iron poisoningDeferrioxamine
Cyanocobalamine or Hydroxocobalamine are used to treat these types of anemiasMegaloblastic Anemia and Pernicious Anemia
The neurological symptoms seen in B12 deficiency is due to thisImpairment of DNA Synthesis
Dihyrofolate reductase is inhibited by this drugMethotrexate
Long term use of phenytoin, sulfonamides, methotrexate, INH, and OCPs is associated with a deficiency of thisFolic Acid
This drug is used to treat folic acid deficiency in patients on methotrexate chemotherapyLeucovorin
A glycoprotein that stimulates red blood cell production. A 165 amino acid glycoprotein manufactured by recombinant DNA technologyErythropoietin (Epoetin alpha)
Indications for this drug is for any anemia due to chronic renal failure patients, zidovudine-treated HIV-infected patients (bone marrow suspression), cancer patients on chemotherapy, reduction of allogeneic blood transfusion in surgery patientsErythropoietin (Epoetin alpha)
Indications for this drug is to treat neutropenia with anticancer drugsMyeloid Growth Factors
Filgrastim and Sargramstim are examples of this type of drugsMyeloid Growth Factors
Granulocyte Colony Stimulating Factor (G-CSF)Filgrastim
Granulocyte/Macrophage Colony Stimulating Factor (GM-CSF)Sargramostim
Megakaryocyte Growth Factors. Stimulate the formation of megakaryocytes and increase their number in peripheral blood. Indications include thrombocytopenia after a cycle of cancer chemotherapyOprelvekin (IL-11)
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