Antihyperlipidemics Flashcards
HMG CoA reductase inhibitors
atorvastatin
rosuvastatin
decrease liver cholesterol
increase LDL receptors
decrease plasma LDL
decrease VLDL synthesis: decrease tags
HMG CoA inhibitors “statins”
myalgia
myopathy
rhabdomyolysis
hepatotoxicity
SE of HMG CoA inhibitors
drug interactions with HMG CoA inhibitors
Gemfibrozil
cytochrome p450 inhibitors enhance toxicity of statin
avoid in chronic alcohol drinkers and hepatitis pts
what enzyme is decreased?
that decreases ATP and leads to myocyte damage
CoQ
statin contraindications
pregnant and lactating women
kids under 8
because the need cholesterol
increase bile acid synthesis
resin
Bile Acid sequestrants
cholestyramine
colestipol
decrease recirculation of bile salts increase synthesis of new bile salts decrease liver cholesterol increase LDL receptors decrease blood LDL
Bile acid sequestrants
decrease blood cholesterol by 50-65%
Statins
decrease cholesterol by 20%
bile acid sequestrants
increase VLDL and tags
increase cholesterol in gall bladder = gall stones
constipation
Malabsorption of lipid soluble vitamins (A,D,E,K & folic acid)
bile acid sequestrants
drug interaction with bile acid sequestrants
orally administered drugs (warfarin, thiazides, digoxin, etc)
hypertriglyceridemia
Contraindication of bile acid sequestrants
inhibits VLDL synthesis decreases plasma VLDL decreased plasma LDL (20-30%) increase plasma HDL (30-40%) decreases lipoprotein (a)
Niacin (B3)
flushing pruritus burning pain hepatotoxicity hyperglycemia
SE of niacin
can take aspirin to avoid increase in PG
bind to PPARa and increase expression of lipoprotein lipases
Gemfibrozil
Fenofibrate (Fibrates)
decrease VLDL (35%) and IDL modest decrease LDL (10%) increased HDL (10%)
gemfibrozil
fenofibrate
used in hypertriglyceridemia
gemfibrozil
fenofibrate
gallstones
myositis
myopathy
gemfibrozil
fenofibrate
most effect at increasing HDL
niacin
removing cholesterol from fatty streak in blood vessels and activates LCAT to esterize cholesterol (transferred to IDL and LDL by CETP)
increasing Apo A1 and A2
directly blocks NPC1L1 receptor - increases LDL receptor - decreasing LDL in blood stream
Ezetimibe
GIT distress
SE of Ezetimibe
decreases cytosolic cholesterol and increases HDL 4-9%
Ezetimibe
weight loss drug
orlistat
inhibits pancreatic lipase - decreasing tags breakdown in intestine
orlistat
oily stool
diarrhea
decrease absorption of lipid soluble vitamins
orlistat
PCSK9 inhibitors
alirocumab
evolocumab
decrease hepatic tags synthesis and increase tags clearance
omega 3 fatty acid
indication: hypertriglyceridemia
Contraindications: fish allergy
omega 3 fatty acid
are monoclonal antibody - bind to PCSK9 to inhibit LDL receptor degradation and increase LDL receptors; decreasing LDL (48-71%) and APO B (42-55%) in blood stream
PCSK 9 inhibitors
Indications
1) heterozygous familial hypercholesterolemia
2) clinical atherosclerotic cardiovascular disease
PCSK 9 inhibitors
ADR: allergy, nasopharyngitis, injection site reaction
PCSK 9 inhibitors