50 Drugs that Help Normalize Cholesterol & Triglyceride Levels AKA: Antilipemic Agents

Lipids and Cardiovascular Disease Hyperlipidemia High levels of lipids in blood major risk factor Most patients asymptomatic until cardiovascular disease produces symptoms May be inherited or acquired Diets high in saturated fat and lack of exercise contribute Genetics determines ability to metabolize lipids 2

Types of Hyerlipidemia Hypercholesterolemia Elevated blood cholesterol Dyslipidemia Abnormal levels of lipoproteins Can refer to excess or deficit of different lipoproteins 3

Types of Lipids Triglycerides Phospholipids Steroids Most common 90% of lipids Major storage form of fat in body Provide fuel for body Phospholipids Builds plasma membranes (lecithins most common) Steroids Cholesterol Building block for biochemicals Vitamin D, bile acids cortisol, estrogen, testosterone

Lipid Proteins Lipids must be packaged for transport throught he blood Protein carrier (apoprotein) attached to the lipid Classified as to weight, size, composition Three types VLDL (LDL synthesized from VLDL) LDL HDL

LDL LDL transports cholesterol from liver to tissues and organs Used to build plasma membranes and synthesize other steroids Carries highest amount of cholesterol Known as bad cholesterol Contributes to plaque deposits and coronary artery disease VLDL: Primary carrier of triglycerides in blood 6

HDL ”H” is for happy Manufactured in liver and small intestine Reverse cholesterol transport Assists in transport of cholesterol away from body tissues and back to liver Known as good cholesterol ***Transports cholesterol for destruction and removal from body 7

Therapeutic Lifestyle Changes Monitor blood-lipid levels Maintain weight; exercise Reduce dietary saturated fats and cholesterol Increase soluble fiber in diet Reduce or eliminate tobacco use 8

Metabolic Syndrome High TG Low HDL Hyperglycemia High Blood Pressure > 40 inches waist circumference for men or 35 inches for women

Five Main Classes HMG CoA reductase inhibitors (Statins) Bile Acid Sequestrants Nicotinic Acid Fibrates Cholesterol Absorption Inhibitors *** Table 50-5 page 565

HMG-CoA Reductase Inhibitors (Statins) Works by interfering with critical enzyme (HMG-coA reductase in the synthesis of cholesterol First line of treatment for lipid disorders Drop LDL, lower triglycerides and increase HDLs Reduces cardiovascular events by 25% to 30%

HMG-CoA Reductase Inhibitors (Statins) Prototype drug: atorvastatin (Lipitor) Mechanism of action: inhibits HMG-CoA reductase Primary use: Reduces serum-lipid levels Adverse effects: headache, fatigue, muscle or joint pain, and heartburn, rarely rhabdomyolysis See Table 50-8 page 571 12

Nursing Care and Statins Watch for muscle pain and rhabdomyolysis Administer at night (cholesterol synthesis highest then) Avoid macrolides (i.e., erythromycin) azole antifungals*** (i.e., ketoconazole - Nizoral) , fibric acid agents, immunosuppressants (can cause rhabdomyolysis) Often given in conjunction with cholesterol absorption inhibitors*** Watch for hepatotoxicity and myopathy Pregnancy Risk X

Bile Acid Sequestrants Work by increasing excretion of cholesterol in the stool They bind bile acids which contain a high amount of cholesterol making them unable to be absorbed in the small intestine promoting their excretion used in primarily in conjunction with statins These used to be primary way to treat lipid disorders before statins discovered

Bile-Acid Resins Prototype drug: cholestyramine (Questran) Mechanism of action: bind with bile acids increasing cholesterol excretion in stool Primary use: to lower serum-lipid levels Adverse effects: GI tract, such as bloating and constipation Can bind other drugs, increasing potential for drug interactions Bind with bile acids to increase excretion of cholesterol in stool Used in combination with statins Examples: Welchol, Colestid 15

Nursing Care and Bile Acid Resins Main adverse effects will be GI ***Assess bowel sounds Avoid constipation with high fiber foods, fluids Can decrease fat soluble vitamins May need supplement Interfers with absorption of digoxin, warfarin, thiazides and tetracyclines Advise to take other medications 1 hour before or 4 hours after taking bile sequestrants

Nicotinic Acid (Niacin) B complex vitamin Much larger doses required for antilipid effect Decreases LDL and triglyceride levels Increases HDL

Nicotinic Acid Prototype drug: niacin Mechanism of action: acts in the liver and adipose tissue to inhobit synthesis of TGs and thereby decreasing VLDL, how it increases HDL is unclear. Primary use: to reduce triglycerides; increase HDL levels Adverse effects: intense flushing, hot flashes, nausea, excess gas, diarrhea; more serious effects like hepatotoxicity and gout possible B-complex vitamin Decreases VLDL and LDL levels 18

Nursing Care and Nicotinic Acid Almost all patients will experience flushing ***Advise to take one aspirin 325 mg 30 minutes before niacin to reduce flushing symptoms GI effects common Nausea, gas, diarrhea Hepatotoxicity and gout (elevation of uric acid) are possible , hyperglycemia May give 3 times a day, or extended release at nighttime

Fibric-Acid Agents Not used as frequently since statins developed Drug of choice for treating high triglyceride levels Mechanism of action (see page 574)

Fibric-Acid Agents Prototype drug: gemfibrozil (Lopid) Mechanism of action: unknown Primary use: treating severe hypertriglyceridemia Adverse effects: GI distress, rash, watch for bleeding with clients on anticoagulants, gallstones, myopathy, liver injury Drugs of choice for treating severe hypertriglyceridemia Examples: Atromid-S, Tricor 21

Nursing Care and Fibric-Acid Agents Increase likelihood of gallstones GI related side effects most common Dyspepsia, diarrhea, nausea and cramping Give with meals to decrease GI symptoms Fatty foods may decrease absorption Avoid with severe renal or hepatic dysfunction Avoid with gallstones

Cholesterol Absorption Inhibitors Inhibits absorption of cholesterol secreted in the bile and from food Cholesterol is normall abslored in jejunum of small intesting Meds block 50% of absorption Unfortunately, body responds by manufacturing more cholesterol; thus, a statin may be given also

Cholesterol Absorption Inhibitor Prototype drug: ezetimibe (Zetia) Mechanism of action: inhibits absorption of cholesterol Primary use: modest reduction in LDL Adverse effects: No serious side effects New class of drug Inhibits the absorption of cholesterol Example: ezetimibe (Zetia) 24

Nursing Care and Cholesterol Absorption Inhibitor Note: ezetimibe (Zetia) is the only drug in this class! Watch for side effect of hepatitis Monitor liver function Observe for liver dysfunction Avoid alcholol Watch for myopathy Educate patient to report signs