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Obesity drug - Coggle Diagram
Obesity drug
Mechanism
Bile acid-binding resin
Lower reabsorption of BA @ small intestine
Drugs
Colestipol
Same as Cholestyramine
Cholestyramine
TID, PC
Low vit. K
Hypoprothrombinemia
Constipation
Poor app.
Lower cholesterol intake
Interfere NPC1L1 protein @ GI epi.
Ezetimibe
Always w/ statin
Compete cholesterol-Receptor
β-Sitosterol
AC
HMG-CoA reductase inhibitor
Lower 70% endogenous cholesterol synthesis
LDLR expression increases
LDL decreases
Type
Prodrug
Mevastatin
Lovastatin
Simvastatin
HS
Active from
Pravastatin
Fluvastatin
lactone-included
HS
Long HF
Rosuvastatin
Atorvastatin
Adverse eff.
Hepatic
CPK (creatinine phosphate kinase) increases
Rash
Constipation/ N/ V
PCSK9 monoclonal antibody
Proprotein convertase subtilisin/kexin type 9(PCSK9)
Binds LDLR @ Liver
LDLR degradation
Drugs
Evolocumab
Alirocumab
Good for familial hypercholesterolemia
Lower lipoprotein synthesis
Nicotinic acid (Niacin = Vit. B3)
Mechanisms
Bind nicotinic acid receptor @ adipocyte
Lower TG @ blood and liver
Lower VLDL synthesis
Inhibit diacylglycerol acyltransferase-2 @ liver
TG synthesis decrease
VLDL syn. decreases
Activate lipoprotein lipase @ blood
Clearance of VLDL increases
Increase apoA-1 @ liver
HDL increase
Adverse eff.
angiotelectasia
Hepatic
Stomach
Fibrate
Mechanism
Activate PPARα
Heterodimerize w/ RXR
(retinoid X receptor)
Bind PPREs @ gene
peroxisome proliferator response elements
TG / LDL decrease
HDL increases
(peroxisome proliferator-activated receptor α)
Common w/ lower dosage of coumadin
Adv eff.
AST /ALP increase
Myopathy
Renal
Others
Fenofibrate
Bezofibrate
Gemfibrozil