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USMLE - Pharm

Kaplan Section 3 Chapter 7 Anti-Hyperlipidemics

QuestionAnswer
What is 7-a-hydroxylase (CYP7A1)? cholesterol ---(CYP7A1)---> bile acids (upregulated when cholesterol is high to reduce the level of cholesterol in hepatocytes, or when bile acids are low)
Cholestyramine Bile acid (BA) sequestrant. Complexes bile salts (BS)-->prevent recycling of BAs from GI-->dec BA levels in circulation-->dec inhib of CYP7A1-->inc synthesis of new BSs-->dec liver chol --> inc LDL receptors (to make more chol) --> dec LDL in plasma
Colestipol Bile acid (BA) sequestrant. Complexes bile salts (BS)-->prevent recycling of BAs from GI-->dec BA levels in circulation-->dec inhib of CYP7A1-->inc synthesis of new BSs-->dec liver chol --> inc LDL receptors (to make more chol) --> dec LDL in plasma
When would you NOT use bile acid sequestrants? in hypertriglyceridemias because they inc VLDL and TG's
Adverse effects of bile acid sequestrants 1. bloating, 2. constipation
Drug interactions of bile acid sequestrants Dec absorption of digoxin, thiazides, tetracyclines, warfarin, and vitamin K.
What is HMG CoA Reductase? Rate limiting enzyme in the synthesis of cholesterol
What are statins? Inhibit HMG-CoA Reductase --> decrease synthesis of cholesterol in liver --> inc LDL receptors --> dec LDL in circulation & dec hepatic synthesis of VLDL and ApoB
What is the effect of statins on HDL and TG's? small inc in HDL and small dec in TG's (atorvostatin)
What is the effect of statins on vessels? Inc in NO (vasodilator) and decreases mRNA for endothelin-1 (vasoconstrictor)
Adverse effects of statins 1. Diarrhea, 2. Myalgia/myopathy (watch CK), 3. rhabdomyolysis (gemfibrozil, nicotinic acid), 4. inc LFT's
What is nicotinic acid? anti-hyperlipidemic. 1. inhib VLDL and apoprotein synthesis in hepatocytes, 2. inc HDL --> dec plasma VLDL, LDL, and TG's, 3. activates lipoprotein lipases, 4. inc tPA, 5. dec serum fibrinogen
Adverse effects of nicotinic acid 1. flushing, 2. pruritis (use ASA), 3. rashes, 4. hyperuricemia, 5. hyperglycemia, 6. hepatotoxicity, 7. GI ulcer exacerbation.
Gemfibrozil anti-hyperlipidemic. 1. activates lipoprotein lipases --> inc catabolism of VLDL and LDL, 2. dec plasma VLDL, TG's, LDL, 3. small inc in HDL
Adverse effects of gemfibrozil 1. GI distress, 2. rash, 3. gallstones, 4. hypoK, 5. myositis
Drug interactions of gemfibrozil potentiates warfarin and sylfonylurea hypoglycemics
Ezetimibe anti-hyperlipidemic. 1. prevents intestinal absorption of cholesterol (used with statin to dec LDL)
Adverse effects of ezetimbe GI distress
Created by: christinapham
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