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					Cardiovascular System ANTILIPEMICS LILLEY, READING & WORKBOOK: CHAP 28 Antilipemics Drugs used to lower lipid levels Triglycerides and Cholesterol  Two primary forms of lipids in the blood  Water-insoluble fats that must be bound to apolipoproteins, specialized lipid-carrying proteins  Lipoprotein is the combination of triglyceride or cholesterol with a polipoprotein Lipoproteins  Very-low-density lipoprotein (VLDL)  Produced by the liver  Transports endogenous lipids to the cells  Low-density lipoprotein (LDL)  High-density lipoprotein (HDL)  Responsible for “recycling” of cholesterol  Also known as “good cholesterol” Coronary Heart Disease The risk of CHD in patients with cholesterol levels of 300 mg/dL is three to four times greater than that in patients with levels less than 200 mg/dL Coronary Heart Disease Positive Risk Factors  Age  Male 45 years or older  Female 55 years or older, or women with premature menopause not on estrogen replacement therapy  Family history: history of premature CHD  Current cigarette smoker  Hypertension  BP 140/90 or higher, or on antihypertensive medication  Low HDL levels: less than 35 mg/dL  Diabetes mellitus Treatment Guidelines  Antilipemic drugs are used as an adjunct to diet therapy  Drug choice based on the specific lipid profile of the patient  All reasonable non-drug means of controlling blood cholesterol levels (e.g., diet, exercise) should be tried for at least 6 months and found to fail before drug therapy is considered Antilipemics  HMG-CoA reductase inhibitors      (HMGs, or statins) Bile acid sequestrants Niacin (nicotinic acid) Fibric acid derivatives Cholesterol absorption inhibitor Combination drugs Antilipemics: HMG-CoA Reductase Inhibitors (HMGs, or statins) Most potent LDL reducers  lovastatin (Mevacor)  pravastatin (Pravachol)  simvastatin (Zocor)  atorvastatin (Lipitor)  fluvastatin (Lescol) HMG-CoA Reductase Inhibitors (statins) Indications  First-line drug therapy for hypercholesterolemia  Treatment of types IIa and IIb hyperlipidemias  Reduce LDL levels by 30% to 40%  Increase HDL levels by 2% to 15%  Reduce triglycerides by 10% to 30% HMG-CoA Reductase Inhibitors (statins) Adverse effects  Mild, transient GI disturbances  Rash  Headache  Myopathy (muscle pain), possibly leading to the serious condition rhabdomyolysis  Elevations in liver enzymes or liver disease Bile Acid Sequestrants  cholestyramine (Questran)  colestipol hydrochloride (Colestid)  colesevelam (tablet form)  Also called bile acid–binding resins and ion-exchange resins Bile Acid Sequestrants Mechanism of action  Prevent resorption of bile acids from small intestine  Bile acids are necessary for absorption of cholesterol Indications  Type II hyperlipoproteinemia  Relief of pruritus associated with partial biliary obstruction (cholestyramine)  May be used along with statins Bile Acid Sequestrants Adverse effects  Constipation  Heartburn, nausea, belching, bloating  These adverse effects tend to disappear over time Niacin (Nicotinic Acid)  Vitamin B3  Lipid-lowering properties require much higher doses than when used as a vitamin  Effective, inexpensive, often used in combination with other lipid-lowering drugs Niacin (Nicotinic Acid) Mechanism of action  Increases activity of lipase, which breaks down lipids  Reduces the metabolism of cholesterol and triglycerides Indications  Effective in lowering triglyceride, total serum cholesterol, and LDL levels  Increases HDL levels  Effective in the treatment of types IIa, IIb, III, IV, and V hyperlipidemias Niacin (Nicotinic Acid) Adverse effects  Flushing (due to histamine release)  Pruritus  GI distress Fibric Acid Derivatives Also known as fibrates  gemfibrozil (Lopid)  fenofibrate (Tricor) Fibric Acid Derivatives Mechanism of action  Activate lipase, which breaks down cholesterol  Suppress release of free fatty acid from the adipose tissue, inhibit synthesis of triglycerides in the liver, and increase the secretion of cholesterol in the bile Indications  Treatment of types III, IV, and V hyperlipidemias Drug Effects  Decrease the triglyceride levels  Increase HDL by as much as 25% Fibric Acid Derivatives Adverse effects  Abdominal discomfort, diarrhea, nausea  Blurred vision, headache  Increased risk of gallstones  Prolonged prothrombin time  Liver studies may show increased function Cholesterol Absorption Inhibitor ezetimibe (Zetia)  Inhibits absorption of cholesterol and related sterols from the small intestine  Results in reduced total cholesterol, LDL, triglylceride levels  Also increases HDL levels  Works well when taken with a statin drug Nursing Implications Patient Education  Before beginning therapy, obtain a thorough health and medication history  Assess dietary patterns, exercise level, weight, height, VS, tobacco and alcohol use, family history  Assess for contraindications, conditions that require cautious use, and drug interactions Nursing Implications Patient Education  Contraindications include biliary obstruction, liver dysfunction, active liver disease  Obtain baseline liver function studies  Patients on long-term therapy may need supplemental fat-soluble vitamins (A, D, K)  Take with meals to decrease GI upset Nursing Implications Patient Education  Patient must be counseled concerning diet and nutrition on an ongoing basis  Instruct on proper procedure for taking the medications  Powder forms must be taken with a liquid, mixed thoroughly but not stirred, and NEVER taken dry Nursing Implications Patient Education  Other medications should be taken 1 hour before or 4 to 6 hours after meals to avoid interference with absorption  Clofibrate often causes constipation; instruct patients to increase fiber and fluid intake to offset this effect Nursing Implications Patient Education  To minimize adverse effects of niacin, start on low initial dose and gradually increase it, and take with meals  Small doses of aspirin or NSAIDs may be taken 30 minutes before niacin to minimize cutaneous flushing  Inform patients that these drugs may take several weeks to show effectiveness Nursing Implications Patient Education  Instruct patients to report persistent GI upset, constipation, abnormal or unusual bleeding, and yellow discoloration of the skin  Monitor for adverse effects, including increased liver enzyme studies  Monitor for therapeutic effects  Reduced cholesterol and triglyceride levels Review In addition to drug therapy, the patient should be encouraged to do which of the following to treat hyperlipidemia? (Select all that apply.) 1. Reduce cholesterol and fats in diet. 2. Reduce weight. 3. Decrease exercise. 4. Increase use of polyunsaturated and monounsaturated fats. Review Before initiating a statin drug, the premedication assessment should include: 1. complete blood count (CBC). 2. liver function studies. 3. bleeding time. 4. gastrointestinal (GI) series. Review Ezetimibe (Zetia) acts by: 1. an unknown mechanism of action. 2. binding bile acids in the intestines. 3. removing fat-soluble vitamins. 4. blocking absorption of cholesterol by the small intestines.
 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
									 
                                             
                                             
                                             
                                             
                                             
                                             
                                             
                                             
                                             
                                             
                                            