Lipid lowering part 4 Flashcards
What are statins contraindicated in
pregnacy
What type of risk factor is pregnancy and for what drug
statins; risk factor X
What can ethanol and statins do to the body
increases risk of liver damage w/ HMG-CoA reductase inhibitor
What happens when you take statins with grape fruit juice
statin serum concentrations go up if you take more than 1 quart per day
What does st.johns work do to statins
decrease statins levels
What is the argument behind why healthy people should take cholesterol drugs to prevent heart disease
need to give to patients who have high levels of bad cholesterol as well as other risk factor, but who are health because it prevents heart disease and is preventative
What are fibrates and what do they do
amphipathic carboxylic acid; used to treat triacylglycerol levels by activating PPAR (perioxisome proliferator activated receptors) esp. PPAR alpha
What are peroxisome proliferation activated receptors (PPAR-alpha)
intracellular receptors that control carbohydrate, fat metabolism and adipose tissue differentiation.
What statins are safer to use with fibrates
less lipoophilic statins
What are some side effects of fibrates
stomach upset
myopathy- muscle pain w/ creatine kinase elevating
rhabdomyolysis- if combined with statins
lithiasis- predispolistion to form gallstones
How do fibrates help the body with lipids
gene expression of fibrates-decrease triacylglycerol concentration by increasing lipoprotein lipase
increase HDL by increasing production of ApoI and II
What is fenofibrate
its a type of fibrate, it starts as a prodrug producing an active metabolite, fenofibric acid which is responisble for the primary effects of the drug
What are fibrates used for
in combination with statins to treat hypercholesterolemia
fibrate improve HDL and triglyceride levels and improve insulin resistance when abnormal amounts of lipids are associated with metabolic syndrome
What are some drug interactions of fibrates
fibrate + warfarin= compete for binding sites; too much anticoagulation activity,. watch with INR
elevate levels of sulfonylureas- used for diabetes
this will lower glucose levels=sulfonylureas=hypoglycemia
What is niacin and what is its function with lipids
niacin is nicotinic acid or vitamin B3 (water soluble)
its derivatives play a role in energy metabolism of the cell
Niacin inhibits triacylglycerols from coming out of adipose tissue—and from the liver fatty acids broken down in triacylclycerol–> VLDL—> LDL
What does lack of niacin cause
a deficiency disease of pellagra—mild deficiency slow metabolism(lower cold tolerance and increases obesity)
What can niacin be synthesis from but what is the problem with this
body can synthesize niacin from amino acid trytophan, but its slow–need to consume niacin
serotonin synthesis relies on tryptophan availability—> inadequate vitamin B3 can lead to depression
What does niacin inhibit
VLDL secretion in liver
and free fatty acid release from adipose tissue
What does niacin increase
increase the activity of lpl
What does niacin decrease
triglycerol systhesis and lipolysis
What is a bad side effect of niacin and will tolerance develop
flushing, esp with the immediate release form; up to 20% can take it and discontinue therapy was a result- vasodilation
tolerance does not develop
What are the benefits and down sides of sustained release niacin
with sustained release you don’t get as much flushing but its associated with high rate of adverse hepatic effects, leading to hepatic failure and because of this the patient can experience fatigue, anorexia, and nausea.
Why is niacin a bad choice for diabetics
because studies have suggested that niacin at high doses lead to higher glucose levels; and can increase cardiovascular risk
In large doses what are niacin other effects
vasodilator- in large doses (note found in meet to enhance color) can cause unpleasant short term symptoms such as skin flush, itching, gastric disturbances, and lowering of blood pressure
What is ezetimibe (zetia)
its a cholesterol absorption inhibitor; blocks the intesinal absorption of cholesterol; its has enterohepatic circulation and a half life of 22 hours
How often should ezetimibe be dose and what is its effect on LDL
give it once a day; the max effective dose is 10mg
it reduces LDL-c by 19%
What is vytorin
its a combination with simvastatin 10/ 20, 40, or 80 mg provides an LDL-c reduction of 52%
What is advicor and how should it be taken
its a combination of niacin and lovastatin–for an additive effect(absorption lower with food); only take with a low fat snack (can still cause flushing)
What is simcor and how should it be taken
its niacin extended release with simvastatin @
ratios:
1,000/20 and 500/20 and 750/20
What is caduet
its a combination atorvastin with amlopidine which a blood pressure medication
Understand lipid panel
see back of notes
What adverse effects can patients have while on statis
hepatotoxicity in 1% incidence elevations of hepatic transaminase- values are three times higher but with how rare it is FDA doesn’t make doctors check it as ofter
What adverse drug reaction can occur with statins
fibrates and niacin can inhibit sterol synthesis in skeletal muscle leading to a build up of creatininine-
myopathy—its the major adverse effect only in 0.1% statins
drugs that are metabolized by cytochrome P450 (CYP34a)
macrolides antifungals cyclosporine phenylpeperazine antidepressants nefazodone protease inhibitors amidoarone verapamil ditizem amidoipine warfarin
