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137 Cards in this Set
- Front
- Back
Where do thiazide diuretics work?
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distal convoluted tubule
|
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where do loop diuretics work?
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ascending loops of henle
|
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where do potassium sparing diuretics work?
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collecting duct
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Where do carbonic anhydrase inhibitors work?
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Proximal convoluted tubule
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Where does mannitol (osmotic diuretic) work?
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Descending loop of henle
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Indications for thiazide diuretics.
(3) |
1. HTN
2. Heart failure 3. Nephrolithiasis due to idiopathic hypercalcemia |
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Adverse effects of thiazide diuretics
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hypo(k,mg)
hyper (Ca, uric acid, Gl, lipids), sexual disfunction caution with sulfa allg. |
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Are thiazide diuretics effective in patients with severe fluid overload?
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NO
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What disease are thiazide diuretics first line treatment?
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HTN
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MOA of thiazide diuretics
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Inhibit NA and Cl reabsorption
loss of K, Na, Cl causes increased urination decreases BP and CO |
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MOA of loop diuretics
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Inhibits Cl reabsorption in ascending loops of henle
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Indications for loop diuretics
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Pulmonary edema
large fluid volume acute hypercalcemia |
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Side effects of loop diuretics
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Hypo (Na, K, Ca, Mg, volemia)
Hyper (uric acid) ototoxicity |
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Are loop diuretics derived from sulfa?
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yes, except ethacrinic acid (but it's the most ototoxic)
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What is the most potent loop diuretic?
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Bumex
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MOA of potassium sparing diuretics
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Increase Na excretion and decreased K secretion in collecting duct
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Name the aldosterone receptor blockers
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spironolactone
eplerenone |
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Which aldosterone receptor blocker is more selective?
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eplerenone (doesn't cause androgen syndrome)
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Name a carbonic anhydrase inhibitor
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Acetazolamide
|
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What are the indications for a carbonic anhydrase inhibitor?
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Glaucoma
urinary alkalization metabolic alkalosis acute mountain sickness |
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What are the SE of carbonic anhydrase inhibitors?
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metabolic acidosis (mild)
K depletion renal stones drowsiness |
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What is a contraindication to the use of carbonic anhydrase inhibitors?
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hepatic cirrhosis - can lead to decreased excretion of ammonia and hepatic encephalopathy
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What is the MOA of mannitol?
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osmotically inhibits Na and water reabsorption, promotes diuresis
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What are the indications for mannitol?
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toxic ingestion
increased ICP decreased occular pressure before eye procedure |
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What are the SE for mannitol?
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Decreased Na, headache, N/V
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What are the 1st choice for LDL lowering?
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Statins
|
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What is the MOA of statins?
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increased LDL catabolism
inhibit LDL synthesis |
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What are the SE of statins?
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myopathy, rhabdo, hepatotoxicity
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How are statins metabolized?
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Hepatic
P450 3A4 - Atorva/lova/simvastatin increased chance of rhabdo with azoles, macrolides, protease inhib, grapefruit juice, amiodarone, cyclosporin |
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When are statins contraindicated?
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active or chronic liver disease
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What are the lipid outcomes with statin treatment?
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Decreased LDL 18 - 55%
decreased TG 7 - 30 % increased HDL 5 - 15% |
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Name the bile acid sequestrants
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cholestyramine (4-16 gm/day)
colestipol (5-30 gm/day) colesvelam 3 tabs BID |
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What 2 things make bile acid sequestrants not frequently used?
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GI upset
decreased absorption of other drugs. |
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What is MOA of bile acid sequestrants?
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Increased LDL catabolism, decreased chol. absorption,
decreased LDL and VLDL synthesis |
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What is a contraindication to bile acid sequestrants?
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biliary obstruction
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What are the lipid outcomes with bile acid sequestrants?
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decreased LDL 15 - 30%
TG 0 change or increased Increased HDL 3 -5% |
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What are the 2nd most powerful diuretics?
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Thiazides
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Which diuretics are very effective in patients with poor renal function?
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Loops
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If you are converting your patient from IV to PO furosemide and the dose is currently 10mg IV - what is your PO dose?
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20 MG
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Name 2 potassium sparing diuretics (not aldosterone receptor blockers).
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Amiloride
Trianterene |
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What are some indications for Spironolactone?
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secondary hyperaldosteronism, cirrhosis, nephrotic syndrome heart failure
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What is the best agent to increase HDL?
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Nicotinic acid
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What are absolute contraindications to nicotinic acid? (2)
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chronic liver disease
severe gout |
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What are relative (caution) contraindications to nicotinic acid?
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diabetes
peptic ulcer disease hyperuricemia |
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What is the MOA of nicotinic acid?
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Decrease LDL and VLDL synthesis and catabolism of HDL
|
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What are the SE of nicotinic acid?
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Flushing (take ASA or NSAID before dose)
hyperglycemia**(DM?) hyperuricemia**(gout?) GI distress hepatotoxicity |
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Nicotinic Acid
Effect on lipid profile |
Decrease LDL 5-25%
decrease TG 20-50% **Increase HDL 15-35%** |
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What are 2 fibric acid products available?
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Gemfibrozil 600 BID (lopid)
Fenofibrate 48-145 QD (tricor) |
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What is a drug class used to treat metabolic syndrome?
(assoc. with high TG and low HDL?) |
Fibric acid
|
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What are contraindications of fibric acid?
(gemfibrozil and fenofibrate) |
severe renal dz
severe hepatic dz pre-existing gallbladder dz |
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What is the MOA of fibric acid? (gemfibrizil and fenofibrate)
|
decrease synthesis of VLDL and release of fatty acids from peripheral adipose tissue.
increase lipoprotein activity and remove TG from plasma. |
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Fibric acid SE?
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GI (abd pn, nausea, diarrhea)
gallstones myopathy rhabdo (esp combo with statin) |
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Fibric acid
Effect on lipid profile |
decrease LDL 5-20%
decrease TG 20-50% increae HDL 10-20% |
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Name a cholesterol absorption blocker
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Ezetimibe (zetia) 10MG QD
|
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MOA of cholesterol absorption blocker (ezetimibe)
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inhibits absorption of cholesterol at the brush border of the small intestine to reduce LDL
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SE of cholesterol absorption blocker (ezetimibe)
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GI effects
Headache slight increase LFT's when combo with statins |
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cholesterol absorption blocker (ezetimibe)
Effects on lipid profile |
Decrease LDL 17%
Decrease TG 12-34% Increase HDL 8-10% |
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Which drugs decrease LDL?
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statins (DOC)
Nicotinic acid cholesterol absorption blocker |
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Which drugs increase HDL?
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Nicotinic acid (DOC)
Fibrates |
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Which drugs decrease TG?
|
fibrates (DOC)
Nicotinic acid |
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What drug class is ASA?
|
platelet aggregation inhibitor
|
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Name 2 thienopyridines
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Ticlopidine (ticlid)
Clopidogrel (plavix) |
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MOA of ASA?
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Inhibits thromboxane A2 synthesis from arachadonic acid in platelets, inhibits COX-1 resulting in inhibition of platelet aggregation
|
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SE of ASA?
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GI bleeding
prolonged bleeding time |
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How long does platelet inhibition last with ASA?
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7-10 days (lifespan of the platelet)
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MOA of thienopyridines (Ticlopidine (ticlid)
Clopidogrel (plavix) |
inhibit ADP pathway of platelet aggregation
irreversibly block ADP pathway on plt - thus inhibiting activation of GP IIb/IIIa receptor |
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SE of ticlopidine (ticlid)
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neutropenia** most serious
thrombocytopenia, N/V/D |
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Which of the thienopyridines is preferred agent?
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Clopidogrel (rarely assoc. with neutropenia)
|
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What are indications for thienopyridines?
(Ticlopidine (ticlid) Clopidogrel (plavix) |
Prevent CV, Cerebrovascular, and PVD.
prevention of thrombosis in pts undergoing coronary stent placement |
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Name 3 Glycoprotein Inhibitors (GP IIb/IIIa).
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Abciximab (reopro)
Eptifibatide (integrillin) Tirofiban (aggrastat) |
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What does GP IIb/IIIa receptor of platelet do?
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final common pathway for platelet aggregation
|
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Indication for GP IIb/IIIa inhibitor?
Abciximab (reopro) Eptifibatide (integrillin) Tirofiban (aggrastat) |
Unstable angina
NSTEMI undergoing PCI (abciximab) NSTEMI/UA not undergoing PCI |
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SE of GP IIb/IIIa inhibitors?
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Bleeding
Thrombocytopenia (more with abciximab) |
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Which GP IIb/IIIa inhibitor is not renally excreted, has short half life but stong affinity for the receptors, and is contraindicated in pts with high risk of bleeding?
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Abciximab (reopro)
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What drug is a vasodilator that inhibits platelet function, used in combo with ASA to prevent cerebrovascular ischemia?
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Dipyridamole
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Which drug binds to antithrombin III and irreversably inactivates clotting factors II (thrombin) and Xa?
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Unfractionated Heparin
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Which clotting factor does heparin have more affinity for?
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Factor II (thrombin)
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What are indications for heparin?
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Prophylaxis and tx of DVT, PE, ACS, PCI.
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What anticoagulant is used during pregnancy?
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Heparin
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What are SE of heparin?
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Bleeding, Hyperkalemia, Osteoporosis, HIT, hematomas
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What inactivates Heparin?
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protamine sulfate
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What is goal of heparin therapy?
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1.5 - 2.5 times patient PTT baseline
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Name the low molecular weight heparins
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Enoxaparin (lovenox)
Deltaparin (fragmin) |
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What factor does LMW heparin inactivate?
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X
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Can LMW heparin be used during pregnancy?
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Yes
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Is a renal adjustment necessary for LMW heparin in renal failure?
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yes
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Name a pentasaccharide that binds selectively to antithrombin III which inhibits factor X.
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Fondaparinux (arixtra)
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Name 3 direct thrombin inhibitors
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Argatroban (acova)
Lepirudin (Angiomax) Bivalirudin (refludan) |
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Which direct thrombin inhibitor can only be used in PCI?
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Bivalirudin
|
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Indications for direct thrombin inhibitor.
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Prophylaxis and tx of thrombosis in pt's with HIT
alternative anticoag during PCI |
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Which drug inhibits vitamin K dependent clotting factors (II, VII, IX, X) and protein C and S?
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Warfarin
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Which drug is given for pts with a fib or artificial heart valves?
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Warfarin
|
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What is antidote to warfarin?
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Vitamin K
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Which test is used to monitor warfarin?
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INR
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Which 2 fibrinolytics require weight adjustment?
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Alteplase
Tenctaplase |
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Which fibrinolytic has antigenicity?
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Streptokinase
|
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What drug class is used to lyse thrombi in ischemic coronary arteries after MI?
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Fibrinolytics
[Streptokinase Altepase Reteplase Tenecteplase] |
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What is the time window for use of fibrinolytics
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within 12 hrs of symptoms
preferably within 6 hrs and ideally within 30 min of arrival to hospital |
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Are all fibrinolytics hepatically eliminated?
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all except Reteplase which is both hepatic and renal
|
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What is SE of fibrinolytics?
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Major bleeding, allergic rxn and hypotension (greater with streptokinase)
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Which drug class inhibits the enzyme that cleaves ANG I to ANG II; decreases adrenergic stimulation and causes vasodilation; and decreases the breakdown of bradykinin?
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ACE inhibitors
|
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1) Which drug class causes arterial and venous dilation?
2) What does that do to preload and afterload? |
1) ACE inhibitors
2) decrease preload and afterload |
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Which drug is the cornerstone of treatment for heart failure?
|
ACE inhibitors
|
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Have ACE inhibitors been shown to improve symptoms and survival in heart failure?
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YES
|
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ACE inhibitors prevent development of HF in patients with asymptomatic LV disfunction.
TRUE/FALSE |
TRUE
|
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Contraindications for ACE inhibitors
|
SBP <90
Hyperkalemia Pregnant B renal artery stenosis |
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SE of ACE inhibitors
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Hypotension
Hyperkalemia angioedema cough leukopenia renal insufficiency taste disturbance |
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Which ACE inhibitor has SE of angioedema, cough, leukopenia, and taste disturbance more commonly?
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Captopril (which is short acting - by the way)
|
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What is MOA of ARB's?
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Antagonist at ANG II receptor of vascular tone
|
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What are the ACE inhibitors actions on the heart?
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Decrease vascular resistance, venous tone, and blood pressure = increased CO
|
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Which drug class is standard therapy for pt's with stable mild to severe HF and has been shown to slow progression, decrease hospitalizations and increase survival?
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Beta Blockers
|
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Which drug class blocks adrenergic stimulation; decreases release of renin which attenuates RAAS?
|
Beta Blockers
|
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What are SE of Beta Blockers?
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Bradycardia
AV abnormalities mask hypoglycemia abnormal lipid profile fatigue depression sexual disturbance |
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At high doses B1 selective BB can become less selective and block B2 receptors in lung.
TRUE/FALSE |
TRUE
|
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Contraindications of Beta Blockers?
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Bradycardia
2nd and 3rd degree HB SBP <90 Decompensated HF |
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Relative contraindications of Beta Blockers?
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COPD, asthma, poorly controlled DM
PVD - but coreg may be used (has alpha properties which cause vasodilation and doesn't increase lipids) |
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Which drug is an arterial direct acting vasodilator?
|
Hydralazine
(Decreases afterload) |
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What drug can be considered for a patient that cannot take ACEI or ARB?
|
Hydralazine/Isosorbide
|
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Are Nitrates venodilators?
[NTG, isosorbide dinitrate or mononitrate] |
yes
(decrease preload) |
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Which drug causes arterial and venous dilation, enhances Na excretion, diuresis, and suppresses the RAAS?
|
Nesiritide (BNP)
|
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SE of vasodilators
|
hypotension
tachycardia headache lupus (long term hydralazine) |
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Name a synthetic catecholamine that has B1>b2>alpha1.
|
Dobutamine
|
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When are IV positive inotropes used in HF?
|
As a bridge to transplant
|
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What is the MOA of milrinone?
|
PDE inhibitor
(phosphodiesterase) |
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Does Milrinone require renal adjustment?
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Yes
|
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SE of IV positive inotropes
|
arrthymias
Increased HR Increased or decreased BP palpitations CP |
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Can milrinone cause severe hypotension?
|
Yes!
|
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1) Which drug inhibits Na/K ATPase pump?
2) What does this cause? |
1) Digoxin
2) influx of Ca++ which increases cardiac contractility and decreases HR; also enhances diastolic filling time. |
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Which drug slows ventricular rate in a fib/a flutter?
|
Digoxin
|
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Does digoxin have beneficial impact on mortality?
|
Nope
|
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Does digoxin improve symptoms of HF and frequency of hospitalizations?
|
Yes
|
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Non-cardiac SE of digoxin
|
N/V
abdominal pain visual disturbances |
|
Cardiac SE of digoxin
|
Ventricular arrythmias
AV block Atrial arrythmias Sinus brady |
|
these drugs increase or decrease digoxin conc?
amiodarone, erythromycin, quinidine, tetracycline, verapamil |
Increase
|
|
these drugs increase or decrease digoxin conc?
antacids, metocloperamide, cholestyramine |
Decrease
|
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A decreased K level enhances toxicity of which drug?
name 3 drugs that decrease K level |
Digoxin
(corticosteroids, thiazide and loop diuretics) |
|
Increased survival and decreased hospital rates in pt's with systolic disfunction is seen with adding this drug...(in HF)
|
Aldosterone Antagonists
(spironolactone, eplerenone) |