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Lipid Lowering Drugs Lipid Lowering Drugs: HMG Coa Reductase Inhibitors (Statin)
Lipid Lowering Drugs Lipid Lowering Drugs: HMG Coa Reductase Inhibitors (Statin)
Drugs
Bile acid
binding
resins (BAR)
Niacin
Fibrates
(Fibric acid)
MoA
Effect on Lipid
MoA
Effect on Lipid
Bind to bile acid in the intestine insoluble complex feces the liver uses
cholesterol to make more bile which cholesterol levels
VLDL synthesis
TG
LDL
HDL GOOD
LDL
(may)TG
HDL
SE GI disturbance
activity of lipoprotein lipase
S/E pruritus
Flushing. Prevent by taking aspirin 30 min in advance
SE
Cholesterol
Absorption
Inhibitors
D/I
PK
powder form, taste "funny"
absorbtion of
NSAIDs, tetracycline, niacin, digoxin, warfarin, thyroxin, furosemide
& thiazide
Give the drugs at least 1 hr before Bile acid or 4 hrs after Bile Acid
A, D, E, K & folic acid need supplements
eg
Cholestyramine & Cholestipol
Little effect on levels of HDL-C and TG
C/I
diabetics
Gout, Peptic ulcer
C/I When there's a complete biliary obstruction
MoA LipoProtein Lipase activity TG
eg
Effect on Lipid
TG
HDL
Gemfibrozil & Fenofibrate
MoA
eg
Effect on Lipid
SE
PK
Ezetimibe
inhibits absorption of cholesterol from small intestine
Not absorbed, not metabolized, insoluble in water, huge molecule
Excreted - feces
PK
oral
Excreted - kidney
myositis-like syndrome
Oral
Metab - liver
HMG CoA
Reductase
inhibitors (Statin)
MoA Inhibit HMG-CoA Reductase
eg
Effect on Lipid
LDL
TG
HDL GOOD
S/E
Transaminases @ aminotransferase hepatotoxicity
Myopathy
(muscle ache&
weakness)
Myalgia
Myositosis
Rhabdomyolysis: muscle tissue breakdown (Creatine
kinase@phosphokinase) which can cause
myoglobinuria renal failure
Monitor lab value
liver functional enzymes
Muscle enzymes (creatine phosphokinase)
C/I
PK
Oral - take at night
Metab: Liver
GI upset, hyperglycemia, liver damage, uric acid
as result of peripheral vasodilator
Atorvastatin, Rosuvastatin
pregnancy & lactation
GI disturbance
nausea, flatulance
Constipation
Overcome: forcing fluids and encouraging diet
high in raw vegetables, fruit, and bran
Headache,Diarrhea
Headache
Excrete Bile, feces
C/I pregnancy & lactation
Lithiasis:biliary cholesterol excretion formation of gallstones
LDL
May LDL with pt TG
HDL
LDL
TG
safe for pregnancy & children
C/I hypertriglyceridemia
lovastatin, pravastatin, simvastatin, fluvastatin
potent
GI disturbance Constipation, nausea & flatulence
Normally: Well tolerate
Lipid Lowering
Drugs