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lipid-modifying pt1
pharm exam 2
| Question | Answer |
|---|---|
| increased LDL= | increased heart disease risk |
| LDL | bad cholesterol, potentially proinflammatory-> contribute to plaque formation |
| HDL | "good" cholesterol, cardioprotective, potentially anti-inflammatory |
| What filters cholesterol? | liver |
| LDL cholesterol <100 | optimal |
| LDL cholesterol 100-129 | near or above optimal |
| LDL cholesterol 130-159 | borderline high |
| LDL cholesterol 160-189 | high |
| LDL cholesterol >/= 190 | very high |
| total cholesterol <200 | desirable |
| total cholesterol 200-239 | borderline high |
| total cholesterol >/= 240 | high |
| low HDL cholesterol | <40 (men) or <50 (women) |
| high HDL cholesterol | >60 |
| how to raise HDL? | through exercise |
| normal triglycerides | <150 |
| borderline triglycerides | 150-174 |
| moderate triglycerides | 175-499 |
| severe triglycerides | >/= 500 |
| lipid lowering agents | HMG-CoA reductase inhibitors Fibric acid derivatives (fibrates) Niacin Bile acid sequestrants (bile acid resins) Selective cholesterol absorption inhibitors Omega-3 fatty acids PCSK9 inhibitors Small interfering RNA inhibitor Bempedoic acid |
| where do Gemfibrozil and niacin work? | where chylomicrons are absorbed into the lymphatic system and enter the heart |
| where do HMG-CoA reductase inhibitors work? | where chylomicrons are absorbed into the lymphatic system and enter the heart and where liver processes fats into LDLs and HDLs |
| where do PCSK9 inhibitors work? | where liver processes fats into LDLs and HDLs and enter circulation and reach periphery |
| where does ezetimibe work? | where micelles are absorbed into small intestine wall and packaged as chylomicrons |
| where do bile acid sequeastrants work? | where the gallbladder contracts and releases bile into the small intestine |
| HMG-CoA Reductase Inhibitors | Atorvastatin (Lipitor®) Fluvastatin (Lescol®, Lescol XL®) Lovastatin (Mevacor®, Altocor ®) Pravastatin (Pravachol®) Rosuvastatin (Crestor®) Simvastatin (Zocor®) Pitavastatin (Livalo®) |
| 2 most potent HMG-CoA Reductase Inhibitors | atorvastin and rosuvastin |
| where are statins metabolized? | liver |
| how do statins work? | used for "the long haul," strengthens outer cap of plaque and is used to prevent future events by stabling plaque so it is less likely to rupture |
| what are statins mostly metabolized through? | cytochrome P450 (CYP450) isoenzyme system |
| least potent statins | fluvastatin, pravastatin |
| when is the best time to take statins? | in the evening hours |
| why is it best to take statins in the evening hours? | because when in a fasting state the liver produces the most amount of cholesterol |
| how does a daily dose of high-intensity statin therapy affect LDL-C? | lowers it by approximately 50% |
| high intensity statins | atorvastatin- 80mg, rosuvastatin- 40mg |
| adverse effects of statins: liver | Hepatic transaminase (AST/ ALT) elevations- infrequent |
| when can you start/ continue with therapy if statins cause Hepatic transaminase (AST/ ALT) elevations? | if <3x normal |
| when administering statins what lab values are important to get? | AST, ALT |
| Adverse Effects of Statins: Muscle | Myalgias, Myositits/Myopathy, Rhabdomyolysis |
| Adverse Effects of Statins: Muscle- Myalgias | symptoms (muscle pain, weakness, discomfort) with normal creatine kinase (CK) -1-10% |
| Adverse Effects of Statins: Muscle- Myositis/Myopathy | symptoms with evidence of muscle injury (CK > normal) - rare |
| Adverse Effects of Statins: Muscle- rhabdomyolysis | symptoms w/ CK > 10x normal + renal injury - rare |
| What does CK indicate? | muscle breakdown |
| statin intolerance | Adverse effects that resolve or improve with statin dose reduction or discontinuation |
| how to determine statin intolerance? | A minimum of 2 statins should have been attempted, including at least one at the lowest dose |
| overall statin intolerance | about 5-30% |
| complete statin intolerance | < 5% and may related to nocebo effec |
| what to do when a patient is showing signs of statin intolerance? | Lower dose, switch statin, change regimen (qod or twice weekly), +/- addition of non-statin to maintain lipid goals |
| examples of statin drug-drug interactions | immunosuppressants, antibiotics |
| risks reduced on long term statins | reduced mortality, less likely to have future event such as MIor stroke |
| fibrates examples | Fenofibrate (Tricor®) Gemfibrozil (Lopid®) |
| what are fibrates primarily used for? | triglyceride lowering |
| what do fibrates do? | ↑ breakdown of VLDL in peripheral tissues ↓ VLDL from liver and ↑ HDL Potent triglyceride-lowering effect |
| fibrates adverse effects | Gastrointestinal Myopathy Transaminase elevations |
| how to minimize GI effects when taking fibrates? | take with food |
| what is niacin also known as? | nicotinic acid or vitamin B3 |
| What can prescription formulas of Niacin help with? | HDL-raising and TRG-lowering, plus modest effect on LDL-lowering |
| Are niacins well tolerated? | no, flushing, itching, liver and GI effects, can worsen glycemic and uric acid levels |
| Niacin | No longer a main modality for modification of atherogenic lipoproteins |
| When may niacin be used? | in some circumstances under the care of a lipid specialist |
| bile acid sequestrants | Cholestyramine (Questran®/ Prevalite®) Colesevelam (Welchol®) Colestipol (Colestid®) |
| what are bile acid sequestrants used mainly to do? | lower LDL-> not very effective alone |
| what to bile acid sequestrants do? | Interfere with reabsorption of bile acids in GI tract leading to less cholesterol delivery to liver (↑ LDL receptors) |
| How do bile acid sequestrants interfere with the reabsorption of bile acids in the GI tract? | help breakdown fat, by interfering with liver the liver has to make it up by making more LDL receptors |
| are bile acid sequestrants well tolerated? | no, not long term, they bind to other meds in the gut (need to stagger administration times |
| bile acid sequestrants adverse effects | Gastrointestinal - nausea, bloating, constipation Hypertriglyceridemia |
| Selective Cholesterol Absorption Inhibitors examples | Ezetimibe (Zetia®) Ezetimibe/ simvastatin (Vytorin®) |
| what does ezetimibe do? | prevents absorption of cholesterol in intestine |
| what may ezetimibe be used as? | monotherapy or for synergistic effect in combination with statins to achieve LDL goal |
| when to give ezetimibe? | oral, once daily |
| is ezetimibe well-tolerated? | yes, there are possible GI effects |
| drug interactions of ezetimibe | minimal |
Created by:
camrynfoster