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Anti-lipemic Agents
Module 3 Drug Classifications
Question | Answer |
---|---|
What is the action of Bile Acid Sequestrants (BAS)? | They are drugs that bind bile acids in the intestine, allows excretion in the feces instead of reabsorption, causes cholesterol to be iodized in the liver, and serum cholesterols levels to fall. |
Name the three Bile Acid Sequestrangs drugs | Begin in "chole-" or "cole-" Cholestyramine, Colestipol, and Colesevelam. C(h)ole BAS |
What are the indications for Bile Acid Sequestrants | Decrease plasma cholesterol levels in primary hypercholesterolemia, and pruritic (itching) associated w/ partial biliary obstruction. |
What are the contraindications for Bile Acid Sequestrants? | Allergy, complete biliary obstruction; abnormal intestinal function and pregnancy and lactation |
What are the adverse effects for Bile Acid Sequestrants | Headache, anxiety, fatigue, and drowsiness. Nausea & constipation. Vitamin A, D, E, and K deficiencies (fat soluble vitamins), which increases bleeding times. |
Name the prototype for Bile Acid Sequestrants | Cholestyramine |
What is the action of HMG-CoA Reductase Inhibitors (statins)? | Blocks HMG–CoA reductase (an enzyme) causing serum cholesterol and LDLs to decrease since the liver cannot produce cholesterol. Thus, HDL levels increases. |
Name 5 HMG-CoA Reductase Inhibitors (statins) | “-statin” Atorvastatin, Lovastatin, Pravastatin, Rosuvastatin, and Simvastatin |
What are the indications for statins? | Along with diet, treats elevated cholesterol, triglycerides, and LDL. Increase in HDL in patients with primary hypercholesterolemia. Treat familial hypercholesterolemia with 2+ risk factors for CAD |
What are the contraindications for statins? | Known allergy, pregnancy/lacation (pregnancy X catergory). Acute liver disease/alcoholic liver disease. |
What should you be cautious for when administering statins? | Renal impairment which can be worsened if rhabdomyolysis occurs and impaired endocrine function |
What are the adverse effects of statins? | GI system: flatulence, abdominal pain, cramps, N/V, constipation. CNS effects: HA, dizziness, blurred vision, insomnia, fatigue, cataracts. Liver: elevated liver enzymes and acute liver failure. Rhabdomyolysis: breakdown of muscles which releases waste |
What are the drug-drug interactions for statins? | Erythromycin, cyclosporine, gemfibrozil, niacin, or antifungal drugs (increased risk of rhabdomyolysis). Digoxin or warfarin: increased serum levels and possible toxicity. Monitor Digoxin levels and clotting times. Grapefruit juice: increased risk of t |
Name the prototype for HMG-CoA Reductase Inhibitors (statins) | Atorvastatin |
How do cholesterol absorption inhibitors (CAIs) function? | They work in the small intestine to decrease absorption of dietary cholesterol. Less cholesterol is circulated to the liver. Liver clears more cholesterol from the blood which results in less circulating cholesterol. |
What are the indications for cholesterol absorption inhibitors (CAIs)? | Lower serum cholesterol levels; treat homozygous familial hypercholesterolemia; treat homozygous sitosterolemia to lower sitosterol and campesterol levels |
Which drug is a cholesterol absorption inhibitor (CAI)? | Ezetimibe |
Which drug class can be an adjunct with Ezetimibe? | A statin can be an adjunct with Ezetimibe to help lower LDLs & decrease risk of CV events. |
What are the contraindications for cholesterol absorption inhibitors? | Known allergy to CAIs. Take caution with pregnancy/lacation, older adults, and liver disease. |
What are the adverse effects for CAIs? | GI: abdominal pain and diarrhea. CNS: HA, dizziness, fatigue. Upper respiratory infection. Muscle aches and pains, back pain |
What are the drug-drug interactions for CAIs? | Cholestyramine, fenofibrate, gemfibrozil, or antacids: Increase in ezetimibe levels. Take ezetimibe at least 2 hours priors or 4 hours after the other drug. Cyclosporine: Increase in toxicity risk. Fibrates: Increased risk for cholelithiasis. Warfarin: In |
What are the actions for PCSK 9 inhibitors? | Monoclonal antibodies that bind to free PCSK9 enzyme inhibiting it from attaching to the LDL receptors on the liver cell allowing for the liver to process more LDL, which decreases circulating LDL levels. |
What drugs are PCSK 9 inhibitors? | End in “-ocumab”. Alirocumab and Evolocumab |
What are the indications for PCSK 9 inhibitors? | Treatment of high cholesterol levels with statin therapy or if statins are not tolerated or contraindicated |
What are the contraindications and cautions for PCSK 9 inhibitors? | Hx of serious hypersensitivity reactions |
What are the adverse effects PCSK 9 inhibitors? | Risk of infection, injection site reactions, and allergic reaction |
Are there any drug-drug interactions with PCSK 9 inhibitors? | Unknown drug-drug interactions. |
What are other-lipid lowering agents? | Fibrates, Vitamin B, Omega-3 Fatty Acids and Other Therapies |
Which other-lipid lowering agents lower triglycerides and LDL levels? | Fibrates & Vitamin B3 (aka Niacin) |
What are fibrates? | Fenofibrate, Gemfibrozil, and Fenofibric acid |
What are the indications for Omega-3 fatty acids? | For treatment of hypertriglyceridemia |
What are other therapies for hypercholesterolemia? | Mipomersen and Lomitapide. No effect on CV morbidity and mortality. Available only through a limited access program d/t black box warnings for potential for serious hepatotoxicity |
What are the indications for combination therapies? | Combination therapy is tried if patient shows no response to strict dietary modification, exercise, and lifestyle changes with the use of one lipid-lowering agent. Goal is to achieve lowered LDL and cholesterol levels. |
What are the adverse effects for combination therapies? | Rhabdomyolysis with certain combinations |
What is rhabdomyolysis? | Breakdown of muscle tissue that releases a damaging protein into the blood |