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23 Cards in this Set
- Front
- Back
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Chylomicrons
- composition - transport pathway |
- triglycerides
- transport triacylglycerols from intestine to other tissues (except kidneys) |
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What do chylomicron remnants do?
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transport cholesterol to liver
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What do IDL do?
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transport cholesterol to LDL or liver
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VLDL
- composition - transport pathway |
- cholesterol & triglycoids
- transport triacylglycerol to fat tissue |
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LDL
- composition - transport pathway |
- cholesterol
- transport cholesterol to peripheral tissues |
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HDL
- composition - transport pathway |
- protein
- transport cholesterol to liver |
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What are the two apoproteins and what lipoproteins are they found in?
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B-100 - one per LDL
A-1 - 2-5 per HDL particle |
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What are B-100 apoproteins?
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responsible for lipid recognition & binding
- one per LDL - only "non-exchangeable" apoprotein |
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What are A-1 apoproteins?
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promote cholesterol efflux from tissue to liver
- 2-5 per HDL |
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How is HDL involved in cholesterol efflux?
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1. HDL binds to B1 receptor in hepatocytes
2. HDL transfers associated cholesterol & cholesterol esters to liver for digestion 2b. HDL changes cholesterol to cholesterol ester for transport |
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How is losartan metabolized?
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oxidation to EXP-3174 (15x more potent than losartan)
- adds =o to carboxyl |
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What are the hyperlipidemia strategies for:
- statins - exetimbe - fibrates - bile acid sequestriants |
statins: biosynthesis
exetimbe: diet fibrates: lipoprotein catabolism bile acid sequestriants: reabsorption |
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What is the moa of bile acid sequestriants?
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pos. charge N sequesters bile acid reabsorption
→ excretion after ion exchange → ↓ serum LDL |
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What is the moa of ezetimbe?
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inhibits NPCILI (sterol influx transporter - takes chol. from diet into blood)
→ prevents absorption of cholesterol from diet |
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What is the moa of statins?
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HMGCoA reductase inhibitors
→ prevent formation of mevalonic acid |
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Which statins are
- fungal metabolites? - totally synthesized? |
fungal: lova, simva, prava
synth: fluva atorva, ceriva |
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Define:
rhabdomyolysis - what is it's significance in this class? |
weakening of skeletal muscle
- it is the main side effect of statin drugs that causes them to be withdrawn from the market |
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What are the classes of steroid hormones according to number of carbons?
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18- estranes
19- androstanes 21- pregnanes 24- cholanes 27- cholestanes |
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What is meant by "G" and "M" in regards to steroid activity?
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G - glucocorticoid activity (↓ immune activity)
M - mineral corticoid activity (not desired for anti-inflammatory) dexmethasone is the most active anti-inflammatory steroid with no mineralcorticoid activity |
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What is the main chemical modification of synthetic estrogens vs. estradiol?
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Block C17 to prevent oxidation
→ 15-20 x more potent than estradiol |
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What are the structural requirements for non-steroidal estrogens?
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1. flat, rigid structure
2. fixed distance for two OH/OMe |
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What are the main structural requirements for anabolic and androgenic activity?
What are 19-norandrogens and their main activity? |
1. steroid skeleton
2. C17 ketone = androgenic 17α alkyl = anabolic 3. 19-norandrogens: removal or 19- Me group = ↓ androgenic while retaining anabolic |
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What is the major metabolite of aspirin and salicylic acid?
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salicyluric acid
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