Antilipemic Drugs 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 Organ meats smoking alcohol contributes Lipoproteins Very low density lipoprotein VLDL o Produced by the liver o Transports endogenous lipids to the cells o Normal 5 40 Low density lipoprotein LDL o Normal 62 100 High density lipoprotein HDL o Responsible for recycling of cholesterol o Also known as good cholesterol o Normal 35 75 Cholesterol normal 150 200 TRIG 40 150 Cholesterol and Coronary Heart Disease CHD 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 Hyperlipidemias and Treatment Guidelines Antilipemic drugs o Drugs used to lower lipid levels o Used as an adjunct to diet therapy Drug choice based on the specific lipid profile of the patient phenotyping 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 Antilipemics 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 HMG CoA Reductase Inhibitors HMGs or statins Most potent LDL reducers o pravastatin Pravachol o simvastatin Zocor o atorvastatin Lipitor o fluvastatin Lescol o rosuvastatin Crestor o pitavastatin Livalo Potent at total cholesterol All bioequivlent At bedtime with meal Medication error if given in the AM Mechanism of Action o Inhibit HMG CoA reductase which is used by the liver to produce cholesterol o Lower the rate of cholesterol production Indications o First line drug therapy for hypercholesterolemia o Treatment of types IIa and IIb hyperlipidemias Reduces LDL levels by 30 to 40 Increases HDL levels by 2 to 15 Reduces triglycerides by 10 to 30 Adverse Effects o Mild transient GI disturbances o Rash o Headache o Myopathy muscle pain possibly leading to the serious condition rhabdomyolysis breakdown of muscle protein myoglobin o Elevations in liver enzymes or liver disease Yellow sclera first icteric sclera Interactions o Oral anticoagulants o Drugs metabolized by CYP3A4 erythromycin Azole antifungals verapamil diltiazem HIV protease inhibitors amiodarone Grapefruit juice Greater risk for developing rhabdo Bile Acid Sequestrants chole cholestyramine Questran colestipol Colestid colesevelam Welchol o Also called bile acid binding resins and ion exchange resins Mechanism of Action o Prevent reabsorbtion of bile acids from small intestine o Bile acids are necessary for absorption of cholesterol Indications o Type II hyperlipoproteinemia o Relief of pruritus associated with partial biliary obstruction cholestyramine o May be used along with statins Adverse Effects o Constipation o Heartburn nausea belching bloating These adverse effects tend to disappear over time Niacin Nicotinic Acid Vitamin B3 Number 2 choice Excellent lipid lowering qualities Lipid lowering properties require much higher doses than when used as a vitamin Effective inexpensive often used in combination with other lipid lowering drugs Mechanism of Action o Thought to increase activity of lipase which breaks down lipids o Reduces the metabolism or catabolism of cholesterol and triglycerides Indications o Effective in lowering triglyceride total serum cholesterol and LDL levels o Increases HDL levels o Effective in the treatment of types IIa IIb III IV and V hyperlipidemias Adverse Effects o Flushing caused by histamine release o Take with NSAIDS or allegra o Pruritus o GI distress Fibric Acid Derivatives Also known as fibrates gemfibrozil Lopid fenofibrate Tricor Both are important to know patients with triglyceride problems Mechanism of Action o Believed to work by activating lipase which breaks down cholesterol o 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 Indications o Treatment of types III IV and V hyperlipidemias o The fibric acid derivatives gemfibrozil and fenofibrate decrease the triglyceride level and increase the HDL cholesterol level by as much as 25 Adverse Effects o Abdominal discomfort very common take with food diarrhea nausea o Blurred vision headache o Increased risk of gallstones o Prolonged prothrombin time o Liver studies may show increased enzyme levels Interactions o Oral anticoagulants o Statins Risk for myositis myalgias and rhabdomyolysis is increased o Laboratory test reactions Decreased hemoglobin level hematocrit value and white blood cell count Increased activated clotting time lactate dehydrogenase level and bilirubin level 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 NSAIDs 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 Herbal Product Omega 3 Fatty Acids Fish oil products Used to reduce cholesterol May cause rash belching allergic reactions Potential interactions with anticoagulant drugs 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 family history Assess for contraindications conditions that require cautious use and drug interactions 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 Refer to guidelines regarding administration times and meals 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 Other medications should be taken 1 hour before or 4 to 6 hours after meals to avoid interference with absorption To