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12 Cards in this Set
- Front
- Back
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-statin MoA
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inhibit HMG CoA reductase -> dec hepatic cholesterol synth, dec plasma VLDL, dec plasma LDL (20-55%), inc LDL-R on hepatocytes, inc plasma removal of LDLs
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-statin dosing
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optimal dosing hs (fasting) when cholesterol synth is upregulated
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-statin SEs + Contra
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well-tolerated: inc hepatic transaminase, rhabdomyolysis (fatal renal failure)
Contraindicated in pregnancy |
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bile acid binding resin MoA
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cholestyramine + cholestipol HCl: positively charged resins bind negatively charged bile secreted into the intestine to prevent their recirc
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cholestyramine + cholestipol Physio
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Inc bile excretion, dec pLDLs, inc LDL-R in hepatocytes, inc hepatic cholesterol synth (weakens tx), small inc in HDLs
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cholestyramine + cholestipol SEs + Interx
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Local only: bloating, ab discomf, constipation = compliance issues
Interx with other anionic cmpnds, dose other drugs 1 hr before or 3 after |
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niacin MoA
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water-soluble Vit B3: inhibits hepatic TIG synth (dec VLDL -> dec LDL) and inc lipase activity (dec chlyomicrons + VLDLs -> dec LDL)
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niacin tx
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adjunct tx to inc HDLs
Clinically proven to dec MI + mortality, slow atherosclerosis |
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niacin SEs + Contra
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~50% at therapeutic doses: intense flushing (prostaglandins, inc dose slowly), hepatic dysfunc, GI upset, hyperglycemia
Contra in hepatic dysfunc, PUD, diabetes, pregnancy |
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fibric acid derivative MoA
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gemfibrozil + clofibrate: stim PPARa -> transcription of genes which dec TIG synth; dec VLDL synth -> dec LDLs; inc HDLs
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gemfibrozil + clofibrate SEs + Cautions
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SEs: gallstones, GI upset, GI/hepatic tumors
Cautioned use in warfarin pts due to anti-coag fx |
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ezetimibe MoA
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Inhibits cholesterol transporter NPC1L1 @ brush border
Unlike bile resins, it does not affect absorption of vitamins, warfarin, OCs, etc. SEs (well-tolerated): rare allergies |
