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PCol I - Exam 4
antidyslipidemic drugs
| Question | Answer |
|---|---|
| Ezetimibe (Zetia) | selectively inhibits intestinal absorption of cholesterol (inhibits more than >50% of absorption); lowers LDL by 15-20% but NO EFFECT on triglycerides |
| Ezetimibe (Zetia) monotherapy dose | 10 mg daily |
| % increase in cholesterol lowering by adding ezetimibe to statins | 15-20% greater lowering of cholesterol; reduction to 60% with 10 mg ezetimibe + 80 mg simvastatin |
| Ezetimibe (Zetia)'s only drug interaction | : bile acid resins inhibit absorption & action – thus, do not administer together (space apart) |
| high EPA/AA ratios (high fish oil) leds to increases in these plasma lipids | 3-series PGs and TX, 5-series LTs |
| high EPA/AA ratios (high fish oil) leds to decreases in these plasma lipids | 2-series PGs and TX, 4-series LTs |
| only FDA approved EPA/DHA (fish oil) supplement | Lovaza (formerly Omacor) from Reliant |
| TG level required in Lovaza's indication | >500 mg/dL |
| Lovaza dosage form (total; EPA; DHA) | 1 g capsules containing ~465 mg EPA & 375 mg DHA |
| Lovaza daily dosage | 4 g daily (combined EPA + DHA) |
| Lovaza SEs and interactions | mainly dyspepsia, loose stools, fishy taste; caution w/anticoagulants, blood thinners (okay with aspirin) |
| what is the risk of rhabdomyolysis when combining Lovaza and statins | none |
| decreased risk of overall mortality and CV mortality when omega-3 increases | 23% decrease in overall mortality; 32% decrease in CV mortality |
| lovastatin, simvastatin, atorvastatin - CYP metabolism | CYP 3A4 metabolism |
| fluvastatin - CYP metabolism | 2C9 |
| rosuvastatin - CYP metabolism | 2C9 & 2C19 |
| pravastatin - CYP metabolism | NOT METABOLIZED BY CYP450s |
| what is the warning for Simvastatin (Zocor) – amiodarone (Cordarone) interaction? | increased risk of severe muscle injury at dose greater than 20 mg/daily simvastatin along with amiodarone (anti-arrhythmic) |
| which 2 statins do not need to be given at night (long-acting statins) | Atorvastatin & rosuvastatin |
| 1st OTC statin in world | (Simvastatin) Zocor Heart Pro – 10 mg |
| dose related statin efficacy (%s increase/decrease) | LDL - decreased by ~ 20 – 60%HDL - raised by ~ 5 - 8%TGs - decreased by ~ 10 – 25% (due to decreased VLDL synthesis) |
| Atorvastatin (lipitor) usual daily dose | 10-80 mg qd |
| Fluvastatin (Lescol) usual daily dose | 20 mg once - 40 mg bid |
| Lovastatin (Mevacor) usual daily dose | 20 - 80 mg once |
| Lovastatin ER (Altocor) usual daily dose | 20 - 60 mg once |
| Pravastatin (Pravachol) usual daily dose | 40 - 80 mg once |
| Rosuvastatin (Crestor) usual daily dose | 10 - 40 mg |
| Simvastatin (Zocor) usual daily dose | 20 - 80 mg |
| safest fibrate to use with statin | fenofibrate |
| % improvement in LDL by combining Statins + bile acid-binding resins | 20 - 30% greater decrease |
| when combining statins + Niacin, how must the statin dose be adjusted | need to cut statins to 1/4 of maxium (or risk increased chance of myopathy) |
| when combining statins + fibrate, how must the statin dose be adjusted | need to cut statins to 1/4 of maxium (or risk increased chance of myopathy) |
| MOA for Cholestyramine & Cholestipol | Bile Acid Sequestrants - inhibits reabsorption of bile acids; decreased hepatic cholesterol levels results in enhanced synthesis of LDL-R on liver cells; promotes clearance of LDL-C & VLDL remnants |
| Bile Acid Sequestrants - drug interactions | (Cholestyramine & Cholestipol) decrease absorption of fat-soluble vitamins; interfere with absorption of some anionic drugs (e.g. thiazides, warfarin, thyroxine, digoxin) |
| Cholestyramine & Cholestipol (Bile Acid Sequestrant) efficacy | 8-24% decrease in LDL-C; some increase in VLDL so avoid in ptns w/hyperTGs |
| gemfibrozil (Lopid), fenofibrate (TriCor) MOA | PPAR-alpha agonist --> results in lower TG levels (decrease 25-50%) and raising of HDL levels (up to 15%) |
| fibrate uses | hypertriglyceridemia, combined hyperlipidemia, hyperlipidemia with decreased HDL |
| Fenofibrate dosing | once daily |
| Gemfibrozil dosing | two times a day |
| fibrate interactions | protein binding displacement; displaces warfarin, sulfonylureas |
| fibrate adverse events | myositis and rhabdomyolysis; dose-related effects; bigger problem with gemfibrozil |
| Niacin (nicotinic acid) MOA and results | inhibits major source of FA for TG synthesis; results --> decrease TG levels (~ 50%), decrease LDL-C formation (~ 25% decrease), increasing HDL-C levels (~ 15-40%) |
| therapeutic doses of Niacin | 1500-3000mg/day |
| niacin metabolism associated with flushing | conjugative pathway with glycine to form nicotinuric acid; low affinity, high capacity |
| niacin metabolism associated with hepatotoxity | amidation pathway, producing pyrimidine metabolites; high affinity, low capacity |
| niacin form that causes the most flushing | immediate release niacin (niacor) |
| niacin form with less flushing; increased liver toxicity | Long-acting niacin – Slo-niacin (dietary supp) |
| niacin form with less flushing, less hepatoxicity | Niaspan (extended-release; prescription only) |
| statins that are prodrugs | simvastatin (Zocor), lovastatin (Mevacor); hydrolyzed in GI tract to active drug |
| statin MOA | inhibits conversion of HMG-CoA to mevalonic acid (HMG CoA reductase inhibitors) |
| statin efficacy for high TGs (and req'd dose) | High triglyceride levels (>250 mg/dl) are decreased 35-45% by highest doses of most potent statins (simvastatin & atorvastatin, 80 mg/day; rosuvastatin, 40 mg/day) |
Created by:
Krafty
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