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CV Exam 4 Drugs and Treatments
Drugs and Treatments for CV Exam 4
39
Medical
Professional
10/12/2011

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Term
Nitrates
Definition
metabolized by mtALH2 to NO and S-nitrothiols, activate gualylyl cyclase to dephosphorylate myosin light chains, not affected by K+/NE, no direct effect on cardiac/skeletal muscle, dilate venules/veins at low doses and arterioles/arteries at high doses, dilates coronary arteries to reduce coronary vasospasm and decrease resistance, cause headache/flushing/hypotension/light-headedness, contraindicated if currently taking PDE5 inhibitors (-afils) for erectile dysfunction
Term
Nitrostat (Nitrates)
Definition
sublingual, for acute attacks/prophylaxis, 2-5min onset, heat/light sensitive
Term
Nitromist/nitrolingual (Nitrates)
Definition
spray, 3 sprays in 15min, 2-3yr shelf life
Term
Nitrodur/minitran (Nitrates)
Definition
trasndermal, 30min onset, long-last, use 12h on and then 12h off to avoid nitrate tolerance
Term
Isosorbide dinitrate (Nitrates)
Definition
oral, 15-30min onset, limited effectiveness due to tolerance, dose-dependent increase in exercise tolerance
Term
Isosorbide mononitrate (Nitrates)
Definition
oral, longer half-life due to no first-pass metabolism
Term
Beta Blockers
Definition
decrease myocardial O2 demand (decreased HR/contractility/LV wall stress), avoid ISA due to increases in HR, increases exercise tolerance and survival, decreases ST depression/frequency of angina/necessity for nitrates
Term
Amlodipine/nicardipine (CCBs)
Definition
more selective for smooth m (less negative inotropy and bradycardia), vasodilation, decreased coronary resistance, increase perfusion, long-lasting forms to avoid reflex tachycardia
Term
Verapamil (CCBs)
Definition
decreases contractiliy/HR/afterload, less vasodilation causes less headache/flushing/edema, can exacerbate HF/AV block, DO NOT COMBINE WITH A BB
Term
Diltiazem (CCBs)
Definition
potent coronary dilator, improves blood flow, may cause bradycardia/AV block
Term
Ranolazine
Definition
inhibits late inward sodium channels (INa), prevents electrical instability/mechanical dysfunction/O2 imbalance due to excess Ca2+, decreases angina symptoms and improves exercise capacity, can cause increased QT interval, contraindicated in pre-existing long QT/liver and kidney disease/CYP3A4 inhibitors
Term
Nitrates, BBs, CCBs, antiplatelets, ranolazine
Definition
treatment for stable angina
Term
Nitrates, CCBs, Low dose aspirin
Definition
treatment for variant angina
Term
Morphine
Definition
causes venodilation and increased vagal tone, can cause severe respiratory depression
Term
Aldosterone antagonists, ACEI
Definition
treatment for unstable angina if MI/LV systolic dysfunction/diabetes
Term
Nitroglycerin/morphine/BBs/CCBs/antiplatelets/anticoagulants
Definition
treatment for unstable angina
Term
Statins
Definition
inhibit HMG-CoA Reductase, activate SREBP to upregulate LDL-R, DECREASE LDL, decrease triglycerides, increase HDL, decrease coronary events/CHD mortality/procedures/stroke, improve endothelial function with NO, decrease CRP/platelet aggregation, stabilize plaques, cause GI/hepatic/neural/myopathic side-effects, cause myaliga/myositis/rhabdomyolysis, MONITER CK AND ALT, contraindicated in liver disease/pregnancy/CYP3A4 inhibitors, 20-30% CV risk after 10yr therapy
Term
Statins, bile acid sequestrant, niacin
Definition
initial treatment for dyslipidemia, decrease LDL
Term
Red Yeast Rice (monacolins
Definition
inhibit HMG-CoA reductase, contain plant sterols/isoflavones/monounsaturated fatty acids, content varies with strain of rice, can cause myalgia/myopathy
Term
Fish oil
Definition
highly unsaturated omega-3 fatty acids, found in cold-water fish and plant sources, decrease triglycerides, increase HDL, reduced hepatic TG production and increased TG clearance, alternative to fibrinates, does not prevent pancreatitis
Term
Cholestyramine, colestipol, colesevelam (Bile Acid Sequestrants)
Definition
bind bile acids in intestine, liver converts cholesterol to replace bile acids, decrease LDL, increase triglycerides, reduce coronary events/CHD mortality, cause constipation/heartburn/nausea/gas/bloating, not for biliary obstruction/hypertriglyceridemia
Term
Ezetemibe
Definition
inhibits intestinal absorption of dietary and biliary cholesterol, decreased delivery/storage of cholesterol in liver, increased cholesterol clearance in blood, causes abdominal pain/diarrhea/arthralgia/myalgia/rhabdomyolysis/hepatitis, can cause allergic reactions, INCREASE TRIGLYCERIDES
Term
Niacin
Definition
water-soluble vitB3, mechanism not understood, blocks fatty acid release, inhibits hepatic fatty acid synthesis, decreases triglycerides, decreases VLDL, INCREASES HDL, reduces coronary events/mortality, causes flushing/hyperglycemia/hyperuricemia/upper GI distress/hepatoxicity, not for liver disease/gout/peptic ulcer
Term
Fenofibric acid (Fibric Acid)
Definition
active metabolite of fenofibrate
Term
Gemfibrozil (Fibric Acid)
Definition
inhibits statin metabolism
Term
Fenofibrate (Fibric Acid)
Definition
micronized and non-micronized forms
Term
Fibric Acid
Definition
activate transcription factor for PPAR-a, decrease liver triglyceride synthesis/VLDL secretion, DECREASE TRIGLYCERIDES, increase HDL, reduce coronary events/lesion progression, cause GI/hepatitis/myositis/cholelithiasis, not for renal/hepatic disease
Term
Niacin (+fibrate)
Definition
treatment if HDL<40 (TG>200)
Term
Thrombolytics
Definition
act on thrombotic and anti-fibrinolytic components, MAJOR TOXICITY IS HEMORRHAGE, for acute MIs/pulmonary embolism/venous catheters/strokes/occlusive disease, improve neurological outcome (but not survival) of strokes, prevent future R. ventricular dysfunction in pulmonary emboli, improved clinical response to pleural effusions, 50-70% salvage of digits in frostbite
Term
Streptokinase (Thrombolytic)
Definition
produced by B-hemolytic streptococci, non-covalent 1:1 complex with plasminogen, conformational change cleaves Arg560 and activates plasmin, systemic lytic state due to activation of circulating plasminogen, not inhibited by a-antitrypsin, renal excretion, 80min half-life, 1.5M units/60min (MI), 250K units/30min (pulmonary embolism), used worldwide due to low cost, causes systemic bleeding/antigenic reaction, pre-existing antibodies require a higher dose, can only be used once
Term
Urokinase (u-PA)
Definition
two-chain serine protease, directly activates plasminogen, non-antigenic, causes systemic lytic state, hepatic metabolism, renal/fecal excretion, 13min half-life, for pulmonary embolism, loading does over 10min, 12h infusion
Term
tPAs
Definition
high fibrin affinity, high plasminogen conversion at site of thrombus, more efficacy, less bleeding
Term
Alteplase (tPA)
Definition
hepatic metabolism, 3-6min half-life, weight-adjusted loading dose
Term
Reteplase (tPA)
Definition
deletion 1-172, missing EGF domain (not targeted to liver), missing kringle-1 domain, missing fibronectin finger (less affinity for fibrin), hepatic metabolism, hepatic/renal excretion, , 13-16min half-life, for acute MI
Term
Tenectaplase (tPA)
Definition
Thr103Asn increases half-life, Asn117Gln decreases hepatic clearance, KHRR296-299AAAA decreases PAI-1 inhibition, hepatic metabolism, 22min half-life, for acute MI
Term
Direct fibrinolytic agents
Definition
degrade fibrin without requiring plasminogen activation, not more effective than indirect fibrinolysis
Term
Carboxypeptidase U
Definition
may increase effectiveness of lower doses of tPA, potent anti-fibrinolytic enzyme, activated by thrombin/thrombomodulin
Term
Aminocaproic Acid
Definition
inhibitor of fibrinolysis, similar structure to lysine, competitive plasminogen inhibitor, thrombi formed during therapy are not lysed
Term
PGE1
Definition
used to maintain ductal patency for TGA/Common ventricle
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