Term
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Definition
| cholesterol absorption inhibitors; MoA: inhibits absorption of dietary & biliary cholesterol in brush border of small intestine, inhibits specific protein-mediated transport system --> reduces delivery of cholesterol to liver --> liver increases # of LDL receptors --> increases uptake of LDL, increases HDL very slightly; Uses: alone or in combo to treat high LDL-hyperlipoproteinemias; ADRs: few side effects, increases liver enzymes w/ statins; fibrates INCREASE availability of drug, bile acid binding resins DECREASE availability of drug |
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Term
| cholestyramine (Questran), colestipol (Colestid), colesevelam (WelChol) |
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Definition
| bile acid binding resin; large copolymers that have ion-exchange; MoA: exchange Cl for bile acids --> more cholesterol converted to bile acids secreted into intestine --> increases # of LDL receptors --> decreases serum LDL; serum VLDL increases for a time; HDL slightly increased; Uses: w/ diet & other drug for tx of mostly high LDL hyperlipoproteinemias; ADRs: NO systemic toxicity, GI: bloating, nausea, constipation, fecal impartation, epigastric distress (less with colesevelam (WelChol), not very palatable; Drug-Nutrient Interactions: inhibits absorption of other drugs (thiazide diuretics, antibiotics, barbiturates, statins), interferes with fat soluble vitamin & iron absorption; may cause weight loss due to malabsorption |
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Term
| lovastatin (Mevachor), pravastatin (Pravachol), simvastatin (Zocor), atorvastatin (Lipitor), rosuvastatin (Crestor) |
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Definition
| HMG-CoA reductase inhibitors; MoA: inhibits HMG-CoA reductase in liver from converting HMG-CoA to mevolonate (rate-limiting step in biosynthesis of cholesterol) --> reduce systemic cholesterol --> induces liver to increase # of LDL receptors --> decrease in LDL along with VLDLs & IDLs, may increase HDLs; MOST POWERFUL LDL-lowering agents; Uses: indicated alone or as adjunct to diet & other drugs for reducing elevated LDLs; may have anti-inflammatory action; PKs: oral, extensive "first pass" effect; inhibited by other drugs & lots of grapefruit juice; one is active, others are prodrugs; ADRs: well tolerated, mild & transient constipation, diarrhea, abdominal pain, HA, dizziness, rash, blurred vision, nausea; Increases serum transaminase; rhabdomyolysis (muscle weakness, pain); C/Is: active liver dx, pregnancy & lactation |
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Term
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Definition
| inhibits intracellular lipolysis in fat cells --> inhibits intracellular lipase activity in adipocytes --> reduces fatty acids --> reduces VLDL --> increases VLDL catabolism --> increases HDL (most effective drug); Uses: primary types of hyperlipidemia, isolated HDL deficiency; PKs: oral, with each meal, metabolized to nicotinamide (vitamin B3) --> no lipid lowering action; short duration of action; ADRs: flushing, itching or burning feeling in skin (take 300 mg aspirin 30 min before taking); hypotension in pts taking antihypertensive drugs, moderately increased liver enzymes, mild hyperglycemia & glucose intolerance in diabetics, GI disturbances, peptic ulcers, elevated plasma uric acid (enahnces Gout attacks) |
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Term
| gemfibrozil (Lopid), fenofibrate (Tricor, Triglide) |
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Definition
| fibrates; MoA: increased clearance of VLDL by increased lipoprotein lipase activity --> increased activity of PPAR-alpha --> oxidation of FFAs (free fatty acids) --> decreases VLDLs --> increased HDL moderately; Uses: tx primary hyperlipidemias w/ high VLDL, hypertriglyceridemia 2ndary to a defect in apolipoprotein E; Pk: oral, one is a prodrug, one is recycled enterohepatically; ADRs: gallstone formation, GI upset & nausea, risk of myopathy when combined with statins |
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Term
| omega-3-ethyl esters (Lovaza) |
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Definition
| contains 2 main omega-3-fatty acids found in high amounts of certain fish; MoA: inhibits hepatic synthesis of triglycerides from endogenous free fatty acids (eFFAs) --> increased beta-oxidation of eFFA, decreased eFFA delivery to liver, decreased synthesis of eFFA, & decreased activity of triglyceride-synthesizing enzymes; may slighltly increase HDL; Uses: adjunct to diet to reduce high triglyceride levels --> decreases VLDL; used in combo w/ statins to treat pts w/ both high LDL & VLDL; Pks: take 4 caps per day; ADRs: flu & infectious symptoms, mild GI distress, taste perversion, "fishy" belching, inhibits platelet aggregation; D-D interaction --> prolonged bleeding time with warfarin |
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