Chapter 6 λ Antihyperlipidemics
λSide effects:
−Flushing, pruritus, burning pain (use aspirin)
−Hepatotoxicity
−Hyperglycemia
GEMFIBROZIL, FENOFIBRATE (FIBRATES)
λMechanism: bind to the PPARα and increase expression of lipoprotein lipases, results in:
−↓ VLDL and IDL
−Modest ↓ LDL
−↑ HDL in most patients
–In some patients with combined hyperlipidemias, can ↑ LDL
–Used in hypertriglyceridemia
λSide effects: − Gallstones − Myositis
EZETIMIBE
λMechanism: prevents intestinal absorption of cholesterol, results in ↓ LDL
λSide effect: gastrointestinal distress
Table III-6-1. Summary of Antihyperlipidemic Uses
Lab Findings |
|
Drugs |
↑ Cholesterol |
Cholestyramine, colestipol, ezetimibe |
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↑ Triglycerides |
Gemfibrozil, fenofibrate |
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↑ Cholesterol and triglycerides |
Statins, niacin, ezetimibe |
|
ORLISTAT
λTherapeutic use: weight loss
λMechanism: inhibits pancreatic lipase → ↓ triglyceride breakdown in the intestine
λSide effects: oily stools (steatorrhea), diarrhea; ↓ absorption of lipidsoluble vitamins
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Section III λ Cardiac and Renal Pharmacology
Chapter Summary
λAn aberrant serum lipid profile is associated with increased risk of atherosclerosis and cardiac heart disease.
λAtorvastatin and the other statins inhibit the rate-limiting step in cholesterol synthesis, HMG-CoA reductase. This lowers liver cholesterol, plasma LDL, and the hepatic synthesis of VLDL and apo B. Statins also cause a small increase in HDL, and atorvastatin lowers triglycerides (TGs). The adverse effects are listed.
λCholestyramine and colestipol are bile acid sequestrants that enhance cholesterol loss into the feces, thereby stimulating new bile salt synthesis, which lowers liver cholesterol levels and consequently plasma LDL levels. Their adverse effects are also listed.
λNicotinic acid inhibits the hepatic synthesis of VLDL and apoprotein. It also increases HDL levels and decreases plasma VLDL, LDL, and TG levels. The adverse effects are listed.
λGemfibrozil activates lipoprotein lipase, thus decreasing VLDL, TG, and LDL levels. The adverse effects are listed.
λEzetimibe prevents cholesterol absorption.
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Cardiac and Renal Drug List |
7 |
and Practice Questions |
Table III-7-1. The Major Cardiovascular and Renal Drugs
Antiarrhythmics |
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Antihypertensives |
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Antianginals |
1A quinidine, procainamide |
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Thiazide diuretics |
Nitrates: nitroglycerin, |
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isosorbide |
1B lidocaine |
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ACEIs: captopril, etc., |
CCBs: verapamil, |
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and ARBs: losartan, etc. |
nifedipine |
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Renin inhibitor: aliskiren |
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1C flecainide |
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CCBs: verapamil, |
β blockers: |
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|
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nifedipine, etc |
atenolol, etc. |
|
II propranolol, acebutolol |
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β blockers: atenolol, |
|
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(ISA), esmolol |
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metoprolol, acebutolol, |
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etc. |
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||
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||
III amiodarone, sotalol |
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α blockers: prazosin, |
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doxazosin, etc. |
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IV verapamil, diltiazem |
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α2 agonists: clonidine, |
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methyldopa |
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Adenosine |
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Vasodilators: hydralazine, |
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nitroprusside, diazoxide, |
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minoxidil |
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Pulmonary hypertension: |
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|
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bosentan, epoprostenol, |
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sildenafil |
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Diuretics |
|
Drugs for Heart Failure |
|
Antihyperlipidemics |
CA inhibitors: acetazolamide |
|
ACEI or ARBs |
Statins l |
|
Loops: ethacrynic acid, |
|
Beta blockers |
Resins: cholestyr- |
|
furosemide |
|
|
|
amine, colestipol |
Thiazides: hydrochlorothia- |
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Diuretics |
Other: nicotinic acid, |
|
zide, indapamide, |
|
|
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ezetimibe, gemfibro- |
chlorthalidone |
|
|
|
zil, fenofibrate |
K+ sparing: amiloride, |
|
Digoxin, bipyridines: |
Weight loss: Orlistat |
|
triamterene, spironolactone, |
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inamrinone, milrinone; |
|
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eplerenone |
|
β agonists: dobutamine, |
|
|
|
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dopamine, nesiritide |
|
|
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Section III λ Cardiac and Renal Pharmacology
1.A patient has a genetic polymorphism such that they cannot rapidly metabolize drugs by acetylation. You would be most concerned about this polymorphism if the patient was taking which drug?
A.Sotalol
B.Clonidine
C.Nitroglycerin
D.Hydralazine
E.Prazosin
2.Which side effect is associated with spironolactone?
A.Alkalosis
B.Hirsutism
C.Hyperkalemia
D.Hypercalcemia
E.Hyperglycemia
3.Lidocaine is an effective antiarrhythmic because it
A.suppresses excitability in hypoxic areas of the heart
B.prolongs the QT interval
C.prolongs the PR interval
D.depresses the slope of phase 0 in slow response tissues
E.acts on inhibitory G-protein coupled receptors
4.Sildenafil has been prescribed for years to treat erectile dysfunction. Recently, this drug is also being used for what condition?
A.vasospastic angine
B.supraventricular tachycardia
C.cyanide poisoning
D.Raynaud disease
E.pulmonary hypertension
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Chapter 7 λ Cardiac and Renal Drug List and Practice Questions
5.A patient with hypertension also suffers from essential tremor. Optimal treatment of the patient should include management with
A.prazosin
B.clonidine
C.metoprolol
D.lidocaine
E.propranolol
6.Selective β-1 blockers are preferred over nonselective beta blockers in some patients because they
A.cause less cardiodepression
B.are less likely to cause bronchoconstriction
C.are more effective for migraine prophylaxis
D.are more effective as an antiarrhythmics
E.have greater prophylactic value post-MI
7.Which drug will utilize the same signaling pathway as endogenous bradykinin on smooth muscle?
A.minoxidil
B.nitroprusside
C.theophylline
D.phenylephrine
E.cocaine
8.A 75-year-old patient suffering from congestive heart failure accidentally ingests a toxic dose of digoxin. Clinical consequences due to the toxic effects of cardiac glycosides are likely to include
A.seizures
B.hypercalcemia
C.bicarbonaturia
D.intermittent claudication
E.visual disturbances
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