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PharmBlock 3
Antihyperlipidemics
| Question | Answer |
|---|---|
| Atorvastatin (lipitor) | HMG CoA reductase inhibitors; high potency; CYP3A4 substrate; standard for most dyslipidemic , post MI and diabetic pts |
| Fluvastatin (lescol, lescol XL) | HMG CoA reductase inhibitors; lowest potency; CYP2C9 substrate; standard for most dyslipidemic , post MI and diabetic pts |
| Lovastatin (mevacor, altoprev) | HMG CoA reductase inhibitors; CYP3A4 substrate; standard for most dyslipidemic , post MI and diabetic pts |
| Pravastatin (pravachol) | HMG CoA reductase inhibitors; NOT a CYP450 substrate = least # of interactions; standard for most dyslipidemic, post MI and diabetic pts |
| Rosuvastatin (crestor) | HMG CoA reductase inhibitors; most potent (use for pts that need significant reduction to dec side effects); 90% excreted in feces; interacts w/CYP2C9; standard for most dyslipidemic, post MI and diabetic pts |
| Simvastatin (zocor) | HMG CoA reductase inhibitors; CYP3A4 substrate; standard for most dyslipidemic, post MI and diabetic pts |
| Cholestyramine (questran) powder | Bile acid sequestrant; breaks cholesterol down into bile acid (does NOT dec cholesterol synthesis); ok in women considering pregnancy, young pts w/moderate LDL-C prob, and OK in combination therapy w/statins |
| Colestipol (colestid) powder, tablets | Bile acid sequestrant; breaks cholesterol down into bile acid (does NOT dec cholesterol synthesis); ok in women considering pregnancy, young pts w/moderate LDL-C prob, and OK in combination therapy w/statins |
| Colesevelam (WelChol) tablets | Bile acid sequestrant; *most potent and easier to administer/tolerate;* breaks cholesterol down into bile acid (does NOT dec cholesterol synthesis); ok in women considering pregnancy, young pts w/moderate LDL-C prob, and OK in combination therapy w/statin |
| Niacin (dietary supplement) | Nicotinic acid; *most effective for inc HDL-C* only drug to dec Lp(a); don't switch preparations; advise pt about OTC nicotinic acid; caution with diabetics |
| Niacin IR (niacor) prescription | Nicotinic acid; *most effective for inc HDL-C* only drug to dec Lp(a); don't switch preparations; advise pt about OTC nicotinic acid; caution with diabetics |
| Niacin SR (slo-niacin) dietary supplement | Nicotinic acid; *most effective for inc HDL-C* only drug to dec Lp(a); don't switch preparations; advise pt about OTC nicotinic acid; caution with diabetics |
| Niacin ER (niaspan) prescription | Nicotinic acid; *most effective for inc HDL-C* only drug to dec Lp(a); don't switch preparations; advise pt about OTC nicotinic acid; caution with diabetics |
| Gemfibrozil (lopid) | fibrate; greater reduction of TG in severely hypertriglyceridemics (prevents pancreatitis); treats atherogenic dyslipidemia w/nml LDL (dec non-HDL and inc HDL); inc risk of myopathy when used with statins (but can treat high LDL/atherogenic dyslipidemia) |
| Fenofibrate (antara, lofibra, TriCor, triglide) | fibrate; greater reduction of TG in severely hypertriglyceridemics (prevents pancreatitis); treats atherogenic dyslipidemia w/nml LDL (dec non-HDL and inc HDL); slight risk of myopathy when used with statins (to treat high LDL/atherogenic dyslipidemia) |
| Ezetimibe (zetia) | cholesterol absorption inhibitors; *dec LDL 18%* inhib absorption in gut/reabs from bile; dec hepatic chol stores; inc chol clearance; mono or combo w/statins (add'l 20% LDL dec); tolerated, GI effects, myopathy, don't take w/cholestyramine bc of binding |
| Omega-3 FA Ethyl Ethers (Omacor) | *dec TG 20-50%;* dec major coronary events/mortality; well tolerated, belching/dyspepsia, flu-like, prolonged bleeding time w/anticoagulants; no interactions; Asolute contra: fish allergy; Relative contra: coagulopathy or anticoag therapy |
| Omega-3 FAs (dietary supplements) | *dec TG 20-50%;* dec major coronary events/mortality; well tolerated, belching/dyspepsia, flu-like, prolonged bleeding time w/anticoagulants; no interactions; Asolute contra: fish allergy; Relative contra: coagulopathy or anticoag therapy |
| Niacin/Lovastatin (advicor) | combo therapy; **dec LDL, inc HDL;** used when LDL goal isn't met with statin monotherapy; avoid high doses of statin (side effects); Tx other dyslipidemia in addition to hi LDL; worry about rhabdomyopathies |
| Ezetimibe/simvastatin | combo therapy; **dec absorption and production of chol;** used when LDL goal isn't met with statin monotherapy; avoid high doses of statin (side effects); Tx other dyslipidemia in addition to hi LDL |
| Dyslipidemia | Hypercholesterolemias (inc LDL-C, inc non-HDL-C); Hypertryglyceridemias, HDL-C deficiency |
| What is the primary target of dyslipidemia therapy? | LDL-C |
| Normal levels for cholesterol | Normal (abnormal): TC <200 (>240); LDL <100-129 (>160-190); HDL >60 (<40); TG <150 (>200-500) |
| Therapy Options: Therapeutic lifestyle changes (TLC) | Use in combo with drug therapy to acieve **>40%** LDL reduction; diet (fiber; plant sterols; can dec LDL by 25-30%), wt reduction, inc physical activity, |
| Lipid modifying drugs | GOAL = dose for a 30-40% reduction in LDLs; HMG CoA reductase inhibitors (statins); bile acid sequestrants; nicotinic acid; fibrates; cholesterol absorption inhibitors; omega-3 FA |
| HMG CoA Reductase Inhibitors: STATINS | *most effective for lowering LDL (18-55%)* complete inhibition of rate limiting step in chol biosynth; inc expression of LDL-C receptors (less floating around for plaques); dec CHD (CRP), coronaries, stroke, mortality; stabilize plaques/prevent clots |
| Statins: adverse effects | risk of myopathy/rhabdomyolysis when used w/fibrates or nicotinic acid; inc aminotransferases (monitor LFTs for hepatotoxicity; d/c if >3xUNL); Monitor CK (get baseline; d/c if CK >10x normal) |
| Statins: absolute contraindications | pregnancy (category X); active or chronic liver disease |
| Statins: relative contraindications | concomitant use of certain drugs (ex: fibrates) |
| Bile acid sequestrants | used for LDL reduction (15-30%) NOT HDL elev; cation resins inc conversion of chol to bile acid and expression of LDL-C receptors; dec risk of coronaries and CHD deaths; GI distress; NO systemic toxicity; dec absorption of other drugs |
| Bile acid sequestrants: absolute contraindications | TG > 400mg/dL; may increase TGs more and cause acute pancreatitis |
| Bile acid sequestrants: relative contraindications | TG > 200mg/dL |
| Nicotinic acid | **Elevates HDL (15-35%)** (vit B3); inhibits hepatic secretion of VLDL-C and inc LPL activity; also dec TGs (20-50%); slows arthrosclerotic progression, dec coronary events and mortality; dec effect of oral hypoglycemics and inc myopathy when used with st |
| Nicotinic acid side effects | flushing of skin (resolve by taking it at night with aspirin); pruritis, rashes, dry skin; GI distress; hepatotoxicity (use smaller initial dose); hyperuricemia/gout; glucose intolerance/hyperglycemia |
| Nicotinic acid: absolute contraindications | chronic liver disease, severe gout |
| Nicotinic acid: relative contraindications | hyperuricemia, diabetes, peptic ulcer disease |
| Fibrates (fibric acid derivatives) | **Dec TG (20-50%);** unknown MOA; inc LPL activity; inhibits lipolysis and dec hepatic FA uptake; inhibit hepatic secretion of VLDL-C; GI symptoms, chol gallstones, hepatitis, myopathy (w/statins: gemfibrozil); binds ptns (displaces drugs; ie: warfarin) |
| Fibrates: absolute contraindications | severe renal or hepatic disease |
| Fibrates: relative contraindications | gallbladder disease or biliary cirrhosis |
| Cholesterol absorption inhibitors: absolute contraindication | hypersensitivity to ezetimibe |
| Cholesterol absorption inhibitors: relative contraindication | moderate to severe hepatic impairment |
Created by:
bscaryp