Dyslipidemia

Question 1

Statins

Answer 1

Structural analog of HMG-COA and inhibit HMG-COA reductase (r8 limiting step of cholesterol synth)

Causes the cell to increase the number os specific cell-surface LDL receptors that bind and internalize LDL

Atorvastatin=Rosuvastatin>Simva>pitava=lova=prava>fluvastain

Question 2

Niacin (Vit B3)

Answer 2

Inhibits the lypolysis of triglycerides on adipose tissue. reducing FFA=liver procuding less VLDL and LDL levels decrease. Catabolic rate of HDL is decreased

Cutaneous flushing (use NSAID)

Question 3

Fibrates

Answer 3

Gemfibrozil and Fenofibrate

agonist for peroxisome proliferator-activated receptor alpha (PPARa). PPARa binds DNA and regs expression of proteins in lipoprotein struct and funct.

Major effect is increase oxidation of fatty acids in liver and muscle.

Question 4

Bile acid resins

Answer 4

Colestipol, cholestyramine, colesevelam

Bind to bile acids and increase bile excretion. increase cholesterol conversion to bile by 7a-hydroxylation and uptake of cholesterol from blood by liver via LDL receptor

Impairs absoprtion of fat soluble vits (ADEK)

Question 5

Ezetimibe

Answer 5

Cholesterol absorption inhibitors

Selectively inhibits GI absoption of cholest. (inhibits NPC1L1). Even in absence of dietary cholest, it inhibs reabsorption of chole in bile.

Question 6

Lomitapide

Answer 6

Binds and inhibs microsomal triglyc transf protein (MTP). Prevents assembly or apo-B=reduced VLDL=reduced LDL

Sunstrate and inhibitor of CYP3A4

Homozygous Familial Hypercholesterolemia

Question 7

Mipomersen

Answer 7

Antisense oligonucleotide that targets apo-B mRNA and disrupts it

Familial Hypercholesterolemia

Question 8

PCSK9

Answer 8

Alirocumab and evolocumab

Ab that bind to PCSK9 and inhib LDL receptor metabolism. 70%LDL decrease