Antilipemic DrugsTriglycerides 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 livero Transports endogenous lipids to the cellso Normal 5 - 40- Low-density lipoprotein (LDL)o Normal 62 - 100- High-density lipoprotein (HDL)o Responsible for “recycling” of cholesterolo 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 drugso Drugs used to lower lipid levelso 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 consideredAntilipemics- 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 reducerso 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 Actiono Inhibit HMG-CoA reductase, which is used by the liver to produce cholesterolo Lower the rate of cholesterol production- Indicationso First-line drug therapy for hypercholesterolemiao 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 Effectso Mild, transient GI disturbanceso Rasho Headacheo Myopathy (muscle pain), possibly leading to the serious condition rhabdomyolysis – breakdown of muscle protein myoglobino Elevations in liver enzymes or liver disease  Yellow sclera first – “icteric sclera” - Interactionso Oral anticoagulantso 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 Actiono Prevent reabsorbtion of bile acids from small intestineo Bile acids are necessary for absorption of cholesterol- Indicationso Type II hyperlipoproteinemiao Relief of pruritus associated with partial biliary obstruction (cholestyramine)o May be used along with statins- Adverse Effectso Constipationo Heartburn, nausea, belching, bloating These adverse effects tend to disappear over timeNiacin (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 Actiono Thought to increase activity of lipase, which breaks down lipidso Reduces the metabolism or catabolism of cholesterol and triglycerides- Indicationso Effective in lowering triglyceride, total serum cholesterol, and LDL levelso Increases HDL levelso Effective in the treatment of types IIa, IIb, III, IV, and V hyperlipidemias- Adverse Effectso Flushing (caused by histamine release)o Take with NSAIDS or allegra o Prurituso GI distressFibric Acid Derivatives - Also known as fibrates- gemfibrozil (Lopid)- fenofibrate (Tricor)- Both are important to know – patients with triglyceride problems - Mechanism of Actiono Believed to work by activating lipase, which breaks down cholesterolo 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- Indicationso Treatment of types III, IV, and V hyperlipidemiaso The fibric acid derivatives gemfibrozil and fenofibrate decrease the triglyceride level and increase the HDL cholesterol level by as much as 25%- Adverse Effectso Abdominal discomfort (very common – take with food), diarrhea, nauseao Blurred vision, headacheo Increased risk of gallstones o Prolonged prothrombin timeo Liver studies may show increased enzyme levels- Interactionso Oral anticoagulantso Statins Risk for myositis, myalgias, and rhabdomyolysis is increasedo Laboratory test reactions Decreased hemoglobin level, hematocrit value, and white blood cell count Increased activated clotting time, lactate dehydrogenase level, and bilirubin levelHerbal 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 NSAIDsHerbal 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 drugsHerbal Product: Omega-3 Fatty Acids- Fish oil products- Used to reduce cholesterol- May cause rash, belching, allergic reactions- Potential interactions with anticoagulant drugsNursing 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