Chapter 50: prophylaxis of atherosclerotic CV disease Flashcards
drugs are only employed when what two things are tried first?
diet and exercise
lipoproteins serve as carriers for what two things in the blood?
cholesterol and triglycerides
what two lipoproteins contribute to arthersclerosis?
VLDL and LDL
the goal of therapy should be to do what?
decreases VLDL and LDL levels
what lipoprotein should be increased?
HDL
why do we want HDL levels to be increased?
it helps protect against atherosclerosis
what do all lipoproteins that deliver cholesterol and triglycerides to non hepatic tissues contain?
apolipoprotein B-100.
drug therapy alone is not enough to achieve the LDL goal which is to keep the level below what
less than 100 mg/dl
what are the two primary goals of treating dyslipidemia?
reducing the risk of atherosclerotic disease and reducing the risk of type 2 diabetes.
what are the most effective antilipedics?
statins
when being treated with a statin, one must avoid drinking what?
grapefruit juice, a cytochrome p-450 inhibitor
what class is the suffix “statin” for?
HMG-CoA Reductase Inhibitor
how does atorvastatin lower the blood cholesterol levels?
increase HDL, decrease LDL, decrease triglycerides
when are statins most effective
in the evening
why are statins most effective in the evening?
the drug will peak at the time that the most cholesterol is being synthesized
what else can statin drugs do other than lipid effects?
stabilize plaque within blood vessels to prevent emboli
what do statins decrease the risk of and how?
thrombus by inhibiting platelet deposition/aggregation and suppressing production of thrombin.
how do statins enhance the ability of blood vessels to dilate?
improving abnormal vascular endothelium
how do statins decrease LDL cholesterol?
increasing the number of LDL receptors on hepatocytes
what does increasing LDL receptors lead to?
increase of LDL being removed from the blood
what role does HMG-CoA reductase play in the cholesterol biosynthesis?
it is the final step in converting cholesterol
statins lower VLDL levels by decreasing the production of what protein?
apolipoprotein in B-100
the potential for statins to promote bone formation by enhancing activity of osteoblasts which will reduce the risk of what
osteoporosis
what are the 2 serious adverse effects of the statins?
hepatotoxicity, rhabdomyolysis
what two components are released from injured or inflamed muscles?
creatinine kinase and myoglobin
what is defined as muscle disintegration and marked elevated levels of CK
rhabdomyolysis
the elevation of CK is how many times the upper normal limit
greater than 10
what can result from the muscle leaking myoglobin?
renal failure
how often should liver function tests be done when using statins?
before starting treatment and every 6-12 months thereafter
when should you discontinue a statin?
when AST levels rise 3 times above the UNL.
what other lipid-lowering drug increases the risk of rhabdomyolysis when given concurrently with statins?
fibrates
what is a B3 vitamin that lowers LDL and triglyceride levels?
Nicotinic acid (Niacin)
what increases HDL levels better than any other drug?
Nicotinic Acid
The OTC dose to correct Niacin deficiency is the 25x the amount to reduce what?
reducing lipoprotiein levels
intense flushing of the face, neck and chest when taking statins is due to what?
peripheral vasodilation
how can you minimize the intense flushing?
taking 325 mg of Aspirin 30 minutes before each dose of a statin. or by using an XR form instead of an IR formulation.
what organ is nicotinic acid toxic to?
the liver
what two serum levels should be monitored since they are increased when taking nicotinic acid?
uric acid and glucose
what lipoprotein do bile acid sequestrates decrease?
LDL
bile acids contain a significant amount of what
cholesterol
what is bile acid cholesterol used to do?
emulsify fats
along with fat soluble vitamins, what else can bile acid sequestreants reduce?
iron, folic acid, B12
where do bile acid sequestrates work?
GI tract
what is the main ADR of bile acid sequestrates
constipation
what do bile acid sequestrates bind to
bile acid–>form large complexes which cannot be absorbed or recycled
what do bile acid sequestrates promote?
promote excretion via the feces
oral medications known to interact with bile acid sequestrates should be taken when
either 1 hour before or 4 hours after the sequestrate
what are the three main drugs that interact bile acid sequestrates?
digoxin, warfarin, and thiazide diuretics
where does ezetimibe block cholesterol absorption
small intestine
what can taking ezetimibe with a fibrate cause
increased risk of gallstones
what 2 other ADRS (besides liver issues) can ezetimibe cause?
pancreatitis and thrombocytopenia
what are the most effective drugs at lowering triglycerides?
fibrates
what effect do vibrates have on LDL levels?
little to no effect
how does gemfibrozil increase plasma TG levels?
lowering VLDL levels which transport TG
how does gemfibrozil increase the risk of gallstones
increases biliary cholesterol saturation
who should not take gemfibrozil
people who have pre-existing gall bladder diseases
what drug does gemfibrozil displace from albumin causing more free drug to be available in the body
warfarin
vibrates increase the synthesis of the enzyme lipoprotein lipase which does what
increase the breakdown and elimination of triglycerides
vibrates increase the production of what which in turn facilitates the production of HDL
both A-I and A-II
what prescription drug has been FDA approved as an Omega-3 fatty acid
Lovaza
what does Lovaza reduce
triglycerides
lovaza can also be purchased as what?
OTC fish oil
how is Pcska inhibitors administered?
SQ
pcska inhibitors are a class of drug that is used as what
an adjunct therapy when maximal amounts of statins have been reached.
why could someone develop antibodies against a pcska inhibitor
because it is composed of proteins
who is pcska inhibitors usually used for?
people with familial hypercholesteremia
