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75 Cards in this Set
- Front
- Back
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three sources of cholesterol for the liver
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chol absorbed by sm intestine--diet
de nevo synthesis lipoproteins circulating in bloodstream |
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what is the rate limiting enzyme involved in the synthesis of cholesterol
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HMG-CoA reductase
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name HMG-Coa reductase inhibitors
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lovastatin
pravastatin simvastatin fluvastatin atovastatin rosubastin |
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lovastatin
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HMG-CoA reductase inhibitor
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rosuvastatin
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HMG-CoA reductase inhibitor
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HMG-CoA reductase inhibitors lead to
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decrease in chol synthesis
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decrease in chol synthesis leads to
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up regulation for LDL receptors
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up regulation of LDL receptors leads to
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removal of LDL from circulation
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what clears LDL out of the blood when using statins
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up regulation of LDL receptors
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what effect will statins have on triglycerides
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large decrease in LDL
modest decrease TG modest increase HDL |
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when is the greatest LDL lowering effect seen with statins
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at the usual starting dose
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doubling statins does what
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lowers LDL by 6%
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pharmokinestics of HMG-CoA reductase inhibitors
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first past hepatic metabolism
major effect on liver |
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what is metabolized cytochrome P450 3A4
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lovastatin
simvastatin atorvastatin |
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metabolized by P450 2C9
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fluvastain
rosuvastatin |
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metabolized by P450 non-cytochrome metabolism
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pravastatin
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half life of most HMG CoA reductase inhibitors
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< 4 hours
atorvastatin 20 hours---lipitor rovsuvastatin 19 hours--crestor |
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does HMG CoA reductase inhibitors reduce mortality
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yes
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clinical uses for HMG CoA reductase inhibitors
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hypercholesterolemia
mixed hyperlipidemia hypertriglyceridemia |
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why is simvastatin(zocor) taken at night
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hepatic cholesterol synthesis is maximal between 12-2 am
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adverse reactions in HMG CoA reductase inhbitors
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GI
elevation of hepatic transminases myalgia myopathy rhabdomyolysis |
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clinical sequence of rhabdomyolysis
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hypovolemia
hyperkalemia met acidosis ARF DIC |
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HMG CoA reductase inhibitors drug interactions
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increase incidence of myopathy with fibrates, niacin, and other CYP3A4 inhibitors
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what is most likely to interact with HMG CoA reductase inhibitors
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gemfibrizol
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which statins are less likely to be involved in drug interactions
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pravastain
fluvastatin rosuvastatin (not metabolized by CYP 3A4) |
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what was taken off market due to myopathy and death
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baycol
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contraindications for HMG inhibitors
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active hepatic disease
pregnancy and lactation |
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name bile acid binding resins
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cholestyramine
colesevelam |
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what is cholestyramine
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bile acid binding resins
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what drug class stops enterohepatic recirculation
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bile acid binding resins
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bile acid binding resins exchange ___ for bile acid
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cl
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reduced bile recirculation leads to
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increased need for bile synthesis
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increse demand for chol stimulates
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synthesis and increases the activity of HMG CoA reductase
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what other drug up regulates the LDL receptors
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HMG CoA reductase inhibitors
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would you combine bile acid binding resin with statin
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yes, further lowers LDL
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end result with bile acid binding resins
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modest decrease in LDL
increase in TG sm increase in HDL |
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would cholestyramine be indicated for hypertriglyceridemia
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no, it raises TG
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pharmacokinetics of bile acid binding resins
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not systemically absorbed
needs large doeses major problem-poor compliance take before meals gradually increase dose |
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clinical use for bile acid binding resins
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hypercholesterolemia
not for hypertriglyceridemia |
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what is the rationale for taking resin before meals
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eating stimulates bile acid release and synthesis
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adverse reactions of bile acid binding resins
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GI
impaired absorption of anionic drugs impaired absorption of Vit A, D, and K |
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when should you take other drugs in relation to taking cholestyramine
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1 hour before and 4 hours after the resin
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what is ezetimide
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cholesterol absorption inhibitors
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name cholesterol absorption inhibitors
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ezetimide
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MOA for ezetimide
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prevents chol absorption thru intestinal villa------
decreases delivery of intestinal chol to the liver |
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ezetimide does what to hepatic chol stores
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decreases
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how does ezetimide affect clearance of chol from the blood
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increases
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ezetimide does not alter
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intestinal TG or fat-soluble vit absorption
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end result of chol absorption inhibitors
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mod decrease LDL
decrease in TG increase HDL |
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chol absorption inhbitors with statin
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reduces statin and decreases myopathy side effects
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clinical use for chol absorption inhibitors
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hypercholesterolemia
in combo with statins |
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adverse reactions of chol absorption inhibitors
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GI upset
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Niacin is what vitamin
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B
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MOA with Niacin
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decreased lipolysis in adipocyte
decreased delivery of FFA to liver decreased TG synthesis in liver decreased release in VLDL fall in plamsa conc of LDL |
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with niacin
increase in lipoprotein lipase activity leads to |
increase clearance of VLDL
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end result of niacin
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modest decrease in LDL
large decrease in TG large increase in HDL |
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clinical use of niacin
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hypertriglyceridemia
mixed hyperlipidemia hypercholesterolemia |
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dose instructions with niacin
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used at high doses
titrate dose over several weeks to build tolerance to S/E |
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is niacins good for lowering LDL
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modest reduction
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what will happen if statins are combined with niacin
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good combo
larger reduction in TG and LDL larger increase in HDL |
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what would happen if you combine cholestyramine with nicacin
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large decrease in TG and LDL
large increase in HDL |
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adverse reactions with Niacin
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GI irritation
flushing abnl liver fx tests hepatotoxicity hyperglycemia hyperucemia |
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which lipid drug stimulates release of histamine
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niacin
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which lipid drug causes prostaglandin mediated dialtion of skin capillaries
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niacin
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when is niacin contraindicated
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chronic liver dx
active peptic ulcer gout high dose with type 2 DM |
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name fibric acid derivatives
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gemfibrizol
fenofibrate |
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what is gemfibrizol
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fibric acid derivative
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MOA with fenfibrate
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activates peroxisome proliferator activated receptor a
increases extrahepatic lipoprotein lipase activity increases VLDL catabolism |
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end result of fibric acid derivatives
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lg decrease TG
increase in HDL variable change in LDL |
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clinical use with fibric acid derivative
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hypertriglyceridemia
hypercholesterolemia |
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adverse reaction with fibric acid derivatives
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GI
gall stone formation myopathy rhabdomyolysis |
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what drug class good for hypercholesterolemia, mixed hyperlipidemia, and hypertriglyceridemia
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HMG CoA reductase inhibitors
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which drug class avoided with pregnancy
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HMG CoA reductase inhibitors
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which ones have major compliance issues
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bile acid binding resins
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which drug causes increased insulin resistance, can you use with diabetics
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niacin
yes, in low doses |
