Antilipemics- Chapter 27.pptx

Chapter 27 Antilipemic Drugs  Overview  Key to understanding use of antilipemic drugs is a working knowledge of the pathology of lipid abnormalities and their contributions to CHD  Important to understand, at the cellular level, the transporting and use of ch...

Chapter 27 Antilipemic Drugs  Overview  Key to understanding use of antilipemic drugs is a working knowledge of the pathology of lipid abnormalities and their contributions to CHD  Important to understand, at the cellular level, the transporting and use of cholesterol and triglycerides  Lipoproteins, apolipoproteins, receptors, and enzyme systems are integral parts of these processes. 2  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 apolipoprotein. 3  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” 4  Atherosclerotic Plaque Formation  Lipids and lipoproteins form athrosclerotic plaque leading to development of CHD.  When serum cholesterol levels are elevated, circulating monocytes adhere to smooth endothelial surfaces of coronary vasculature.  Macrophage cells are formed and fill with fat.  Foam cells develop.  Precursor lesion of atherosclerosis 5 Cholesterol and Coronary Heart Disease  The risk of coronary heart disease 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.  Benefits of cholesterol reduction are well documented. 6  Hyperlipidemias and Treatment Guidelines  National Cholesterol Education Program Adult Treatment Panel III of the National Institutes of Health  Antilipemic drugs  Drugs used to lower lipid levels  Used as an adjunct to diet therapy  Drug choice based on the specific lipid profile of the patient (phenotyping) 7  Hyperlipidemias Treatment and Guidelines (Cont.)  All reasonable nondrug 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. 8  Antilipemics  ACC/AHA Guideline on the Treatment of Blood Cholesterol to Reduce Atherosclerotic Cardiovascular Risk in Adults (2018)  Hydroxymethylglutaryl–coenzyme A (HMG–CoA) reductase inhibitors (HMGs, or statins)  Bile acid sequestrants  B vitamin niacin (vitamin B3, nicotinic acid)  Fibric acid derivatives (fibrates)  Cholesterol absorption inhibitor (Zetia)  Combination drugs (Vytorin) 9  Newer Drugs  Mipomersen: once-weekly subcutaneous injection  Microsomal triglyceride transfer protein inhibitor  Lomitapide (Juxtapid)  Proprotein convertase subtilisin kexin 9 (PCSK9) inhibitors  Alirocumab (Praluent)  Evolocumab (Repatha)  ATP-citrate lyase inhibitor  Bempedoic acid (Nexletol) 10  Antilipemics: HMG-CoA Reductase Inhibitors (Statins)  Statins  Patients with clinical atherosclerotic cardiovascular disease (CVD)  Patients with LDL cholesterol levels >190 mg/dL  Patients with diabetes age 40 to 75 years with LDL levels of 70 to 189 mg/dL and without evidence of CVD  Patients without evidence of CVD or diabetes but who have LDL levels between 70 and 189 mg/dL and a 10- year risk of CVD > 7.5% 11  Antilipemics: HMG-CoA Reductase Inhibitors (Statins) (Cont.)  Most potent LDL reducers  Lovastatin (Mevacor)  Pravastatin (Pravachol)  Simvastatin (Zocor)  Atorvastatin (Lipitor)  Fluvastatin (Lescol)  Rosuvastatin (Crestor)  Pitavastatin (Livalo) 12  HMG-CoA Reductase Inhibitors: Mechanism of Action  Inhibit HMG-CoA reductase, which is used by the liver to produce cholesterol  Lower the rate of cholesterol production 13  HMG-CoA Reductase Inhibitors: Indications  First-line drug therapy for hypercholesterolemia  Treatment of types IIa and IIb hyperlipidemias  Reduces LDL levels by up to 50%  Increases HDL levels by 2% to 15%  Reduces triglycerides by 10% to 30% 14 HMG-CoA Reductase Inhibitors: Adverse Effects  Mild, transient gastrointestinal (GI) disturbances  Rash  Headache  Myopathy (muscle pain), possibly leading to the serious condition rhabdomyolysis  Elevations in liver enzymes or liver disease 15  Rhabdomyloysis  Breakdown of muscle protein  Myoglobinuria: urinary elimination of the muscle protein myoglobin  Can lead to acute renal failure and even death  When recognized reasonably early, rhabdomyolysis is usually reversible with discontinuation of the statin drug.  Instruct patients to immediately report any signs of toxicity, including muscle soreness or changes in urine color. 16  HMG-CoA Reductase Inhibitors: Interactions  Oral anticoagulants  Drugs metabolized by CYP3A4  Erythromycin  Azole antifungals  Verapamil  Diltiazem  Human immunodeficiency virus protease inhibitors  Amiodarone  Grapefruit juice 17  Audience Response System Question #1 A patient with a new prescription for a HMG-CoA (statin) drug is instructed to take the medication with the evening meal or at bedtime. The patient asks why it must be taken at this time of day. What is the nurses’ best response? A. “The medication is better absorbed at this time.” B. “This timeframe correlates better with the natural diurnal rhythm of cholesterol production.” C. “There will be fewer adverse effects if taken at night instead of with the morning meal.” D. “This timing reduces the incidence of myopathy.” NOTE: No input is required to proceed. 18  Answer to System Question #1 ANS: B All statins are generally dosed once daily, usually with the evening meal or at bedtime to best coincide with the body’s natural diurnal rhythm of cholesterol production. 19  Atorvastatin (Lipitor)  One of the most commonly used drugs in this class of cholesterol-lowering drugs  Lowers total and LDL cholesterol levels as well as triglyceride levels and raises “good” cholesterol, the HDL component  Dosed once daily, usually with the evening meal or at bedtime to correlate with diurnal rhythm 20  Simvastatin (Zocor)  One of the first statins to become generic and one of the most commonly used drugs in this class  Used to primarily lower total and LDL cholesterol levels as well as triglyceride levels  Can moderately raise levels of HDL  Many drug interactions which may require dosing adjustments 21  Bile Acid Sequestrants  Cholestyramine (Questran)  Colestipol (Colestid)  Tablet form  Colesevelam (Welchol)  Also called bile acid–binding resins and ion-exchange resins  Powdered form may not be convenient or well tolerated 22  Bile Acid Sequestrants: Mechanism of Action  Considered second line choice after statins  Prevent resorption of bile acids from small intestine  Bile acids are necessary for absorption of cholesterol. 23 Bile Acid Sequestrants: Indications  Type II hyperlipoproteinemia  Relief of pruritus associated with partial biliary obstruction (cholestyramine)  May be used along with statins 24  Bile Acid Sequestrants: Adverse Effects  Constipation  Heartburn, nausea, belching, bloating  These adverse effects tend to disappear over time.  Increasing dietary fiber intake or taking a fiber supplement such as psyllium (Metamucil and others), as well as increasing fluid intake, may relieve constipation and bloating.  May also cause mild increases in triglyceride levels 25  Bile Acid Sequestrants: Considerations  Overdose can cause obstruction because the bile acid sequestrants are not absorbed.  Treatment of overdose includes restoring gut motility.  Drug interactions  All drugs must be taken at least 1 hour before or 4 to 6 hours after the administration of bile acid sequestrants.  High doses of a bile acid sequestrant decrease the absorption of fat-soluble vitamins (A, D, E, and K). 26  Bile Acid Sequestrants: Cholestyramine (Questran)  Contraindications: known hypersensitivity or phenylketonuria  Pregnancy and lactation considerations  Treatment of loose bowel movements  Caution when administering dry powder 27  Audience Response System Question #2 A patient has been ordered the powdered form of the bile acid sequestrant colestipol. Which of the following does the nurse identify as true? A. The nurse should have the patient swallow the dose of the colestipol powder one teaspoonful at a time. B. The powder should be dissolved and immediately administered. C. The colestipol should be administered 1 hour before or 4 to 6 hours after any other oral medication. D. The colestipol should be administered with meals. NOTE: No input is required to proceed. 28  Answer to System Question #2 ANS: C It is important that colestipol and any bile acid sequestrant be taken 1 hour before or 4 to 6 hours after any other oral medication or meals because of the high risk for drug-drug and drug-food interactions. The powder should be dissolved for 1 full minute before administration and should not be taken in dry form. 29  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 30  Niacin: Mechanism of Action  Thought to increase activity of lipase, which breaks down lipids  Reduces the metabolism or catabolism of cholesterol and triglycerides 31  Niacin: 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 32  Niacin: Adverse Effects  Flushing (caused by histamine release)  Small dose aspirin or NSAIDS 30 minutes before Niacin may help cutaneous flushing  Pruritus  GI distress 33  Audience Response System Question #3 A patient will be taking niacin as part of antilipemic therapy. What is the best way to avoid problems with flushing or pruritus? A. Take the medication at bedtime. B. Take the medication with a small dose of a steroid. C. Take the medication with a full glass of water on an empty stomach. D. Start with a low initial dose and then increase it gradually. NOTE: No input is required to proceed. 34  Answer to System Question #3 ANS: D Cutaneous flushing may be minimized if the niacin is started at a smaller dose and gradually increased. Premedication with a small dose of aspirin or a nonsteroidal antiinflammatory drug 30 minutes before taking the niacin, as well as taking the niacin with meals, may help to minimize these undesirable effects. 35  Fibric Acid Derivatives  Primarily affect the triglyceride levels but may also lower the total cholesterol and LDL levels and raise the HDL  Also known as fibrates  Gemfibrozil (Lopid)  Fenofibrate (Tricor) 36  Fibric Acid Derivatives: Mechanism of Action  Believed to work by activating lipase, which breaks down cholesterol  Also suppress the release of free fatty acid from adipose tissue, inhibit synthesis of triglycerides in the liver, and increase secretion of cholesterol in the bile 37 Fibric Acid Derivatives: Indications  Treatment of type III, IV, and V hyperlipidemias  The fibric acid derivatives gemfibrozil and fenofibrate decrease the triglyceride level and increase the HDL cholesterol level by as much as 25%. 38 Fibric Acid Derivatives: Contraindications  Known drug allergy  Severe liver or kidney disease  Cirrhosis  Gallbladder disease 39  Fibric Acid Derivatives: Adverse Effects  Abdominal discomfort, diarrhea, nausea  Blurred vision, headache  Increased risk of gallstones  Prolonged prothrombin time  Liver studies may show increased enzyme levels. 40  Fibric Acid Derivatives: Interactions  Oral anticoagulants  Statins  Risk of myositis, myalgias, and rhabdomyolysis is increased.  Laboratory test reactions  Decreased hemoglobin level, hematocrit value, and white blood cell count  Increased activated clotting time, lactate dehydrogenase level, and bilirubin level 41  Miscellaneous Antilipemic Drugs: Cholesterol Absorption Inhibitor  Ezetimibe (Zetia)  Inhibits absorption of cholesterol and related sterols from the small intestine  Results in reduced total cholesterol, LDL, and triglyceride levels  Also increases HDL levels  Often combined with a statin drug  Can be used as monotherapy 42  Herbal Product: Garlic  Used as an antispasmodic, antihypertensive, antiplatelet, lipid reducer  Adverse effects: dermatitis, vomiting, diarrhea, flatulence, antiplatelet activity  Possible interactions with warfarin, diazepam  May enhance bleeding when taken with nonsteroidal antiinflammatory drugs (NSAIDs) 43  Audience Response System Question #4 A patient wants to take garlic tablets to improve his cholesterol levels. Which condition would be a contraindication? A. Hypertension B. Bowel obstruction C. Sinus infection D. Scheduled surgery NOTE: No input is required to proceed. 44  Answer to System Question #4 ANS: D Garlic has antiplatelet activity and is contraindicated in patients who will undergo surgery within 2 weeks and in patients with human immunodeficiency virus infection or diabetes 45  Herbal Product: Flax  Both the seed and oil of the plant are used.  Uses: atherosclerosis, hypercholesterolemia, GI distress, menopausal symptoms  May cause diarrhea and allergic reactions  Possible interactions: antidiabetic drugs, anticoagulant drugs 46  Herbal Product: Omega-3 Fatty Acids  OTC Fish oil products  Prescription products  Lovaza  Vascepa  Used to reduce cholesterol  May cause rash, belching, allergic reactions  Potential interactions with anticoagulant drugs 47  Nursing Implications  Before beginning therapy, obtain a thorough health and medication history.  Assess dietary patterns, exercise level, weight, height, vital signs, tobacco and alcohol use, and family history.  Assess for contraindications, conditions that require cautious use, and drug interactions. 48  Audience Response System Question #5 Which patient would benefit from administration of simvastatin (Zocor) 80 mg? A. A patient newly diagnosed with hyperlipidemia B. A patient with muscle aches who was taking another antilipidemic drug C. A patient who is taking verapamil D. A patient who has already been taking simvastatin (Zocor) for 12 months with no evidence of myopathy NOTE: No input is required to proceed. 49  Answer to System Question #5 ANS: D In 2011, the Food and Drug Administration imposed new prescribing restrictions on simvastatin, stating: “Physicians should limit using the 80-mg dose unless the patient has already been taking the drug for 12 months and there is no evidence of myopathy. Simvastatin 80 mg should not be started in new patients, including patients already taking lower doses of the drug.” In patients taking verapamil, the dose of simvastatin is not to exceed 10 mg. 50  Nursing Implications  Contraindications include biliary obstruction, liver dysfunction, and active liver disease.  Obtain baseline liver function studies.  Patients on long-term therapy may need supplemental fat-soluble vitamins (A, D, K).  Refer to guidelines regarding administration times and meals. 51  Nursing Implications (Cont.)  Counsel patient concerning diet and nutrition on an ongoing basis.  Instruct patient on proper procedure for taking the medications.  Powder forms must be taken with a liquid, mixed thoroughly but not stirred, and never taken dry. 52  Nursing Implications (Cont.)  Other medications should be taken 1 hour before or 4 to 6 hours after meals to avoid interference with absorption.  To minimize adverse effects of niacin, start on low initial dose and gradually increase it, and take with meals. 53  Audience Response System Question #6 What patient history would the nurse recognize as a contraindication for beginning Niacin therapy? A. Allergy to erythromycin B. Gout C. Coronary artery disease D. Hypothyroidism NOTE: No input is required to proceed. 54  Answer to System Question #6 ANS: B With niacin, patient assessment includes noting contraindications such as liver disease, peptic ulcer disease, gout, hypertension, and any active bleeding. Although a thorough assessment of all patient conditions is helpful, the other conditions do not preclude use of niacin. 55  Nursing Implications  Small doses of aspirin or NSAIDs may be taken 30 minutes before niacin to minimize cutaneous flushing.  Provide teaching regarding use of NSAIDs and aspirin.  Inform patients that these drugs may take several weeks to show effectiveness. 56  Nursing Implications (Cont.)  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 57