HLD drugs

Question 1

Rate limiting step of cholesterol synthesis inhibited by statins

Answer 1

HMG-CoA reductase

Question 2

Result in liver from blocking intrinsic cholesterol synthesis

Answer 2

Upregulation of hepatic LDL receptors resulting in decreased plasma LDL

Question 3

Therapeutic effect of statins

Answer 3

Decrease in LDL, VLDL, and triglycerides
Mild increase in HDL

Question 4

Secondary prevention of heart disease by statins

Answer 4

Improve endothelial function
Modulate inflammatory response
Maintain plaque stability
Increase NO and decrease mRNA for endothelin-1 –> vasodilation

Question 5

Drug interactions of statins

Answer 5

Inhibitors of CyP450 –> grapefruit juice and red yeast rice

Question 6

Adverse effects of statins

Answer 6

Myopathy
Hepatoxicity

Question 7

Risk of myopathy in statins increases with what?

Answer 7

Concurrent therapy of gemfibrozil and/or nicotinic acid (niacin/vit B3)

Question 8

Types of bile acid sequestrants used for HLD

Answer 8

Cholestyramine
Colestipol
Colesevelam

Question 9

Secondary use of cholestyramine (not HLD)

Answer 9

Used in pruritis due to biliary obstruction

Question 10

Mechanism of bile acid sequestrans

Answer 10

Bind bile acids in GIT to form insoluble complex that is excreted in the feces

Cholesterol used to make more bile –> results in lowered LDL

Question 11

Contraindication of bile acid sequestrants

Answer 11

Hypertriglyceridemia –> increases VLDL and triglycerides

Question 12

Adverse effects of bile acid sequestrants

Answer 12

Fat malabsorption –> steatorrhea
Malabsorption of fat soluble vitamins

Question 13

Vitamin with lipid lowering effect at high doses

Answer 13

Niacin/nicotinic acid/vit B3

Question 14

Mechanism of high dose niacin in HLD

Answer 14

Inhibit hepatic production of VLDL and LDL
Decreases HDL clearance
Increases lipoprotein lipase activity

Question 15

Catalyzes hydrolysis of triacylglycerol component of circulating chylomicrons and VLDL

Answer 15

Lipoprotein lipase

Question 16

Therapeutic effects of high dose niacin

Answer 16

Lower VLDL, LDL, and triglycerides
Increases HDL

Question 17

Fibrates used for HLD

Answer 17

Fenofibrate
Gemfibrozil

Question 18

Peroxisome proliferator-activated receptor alpha (PPAR-alpha) agonists that regulates gene transcription controlling carbohydrate and fat metabolism to increase activation of lipoprotein lipase.

Answer 18

Fibrates

Question 19

Therapeutic effect of fibrates for HLD

Answer 19

Decrease VLDL, triglycerides, and LDL
Mild increase in HLD

Question 20

Clinical indication for use of fibrates

Answer 20

Hypertriglyceridemia (>500 mg/dL)

Question 21

Adverse effects of fibrates

Answer 21

Myositis (with statin)
Hepatitis
Cholelithiasis

Question 22

Cholesterol uptake inhibitor that inhibits Niemann Pick C1 like protein, a cholesterol transporter, in the intestine

Answer 22

Ezetimibe

Question 23

Used effectively with statin to reach LDL goals in pts post MI

Answer 23

Ezetimibe

Question 24

Therapeutic effect of ezetimibe

Answer 24

Moderate decrease in LDL

Question 25

Adverse effects of ezetimibe

Answer 25

HA Myalgia Sinusitis and pharyngitis

Question 26

Antisense oligonucleotide against Apo B-100 mRNA used for homozygous familial hypercholesterolemia

Answer 26

Mipomerson (subQ injection)

Question 27

Adverse effects of Mipomerson

Answer 27

Hepatic fat accumulation Pain at injection site

Question 28

PCSK9 inhibitors that decrease recycling of LDL

Answer 28

Evolocumab (Repatha) Alirocumab (Praluent)

Question 29

Indications for use of PCSK9 inhibitors

Answer 29

Heterozygous familial hypercholesterolemia Adjunct to statin In pts who cannot tolerate statin

Question 30

Adverse effects of PCSK9 inhibitors

Answer 30

Injection site reaction Hypersensitivity reaction Increase in ALT and AST Musculoskeletal pain

Question 31

Amphetamine derivatives that increase norepinephrine release. They have an anorexiant effect used for weight loss

Answer 31

Phentermine Diethylpropion

Question 32

Mechanism of Orlistat

Answer 32

Blacks gastric and pancreatic lipases to decrease fat absorption

Question 33

Mechanism of Lorcaserin

Answer 33

5-HT2c agonist with anorexiant effect