Antihyperlipidemics

Question 1

What is the suffix to remember for HMG-CoA reductase inhibitors?

Answer 1

“statins”

Question 2

What are the S/E of HMG reductase inhibitors?

Answer 2

rhabdomyolysis
hepatotoxicity
myalgia, myopathy

Question 3

What are some tests you should run before giving HMG-CoA inhibitors?

Answer 3

check creatine kinase
check liver function tests

Question 4

What are some important drug interactions to remember when taking HMG-CoA inhibitors?

Answer 4

• Gemfibrozil (inc. rhabdomyolysis)
• Cytochrome P450 inhibitors enhance toxicity of statins (exception Pravastatin because it isn’t metabolized through this pathway)

Question 5

How is HMG-CoA reductase inhibition beneficial for patients with dyslipidemia?

Answer 5

• dec liver cholesterol
• inc LDL receptor expression
• dec. plasma LDL
• dec VLDL synthesis result in: dec triglyceridemia

Question 6

Name some important HMG-CoA reductase inhibitors to remember.

Answer 6

atorvastatin, rosuvastatin

Question 7

What are some bile acid sequestrant drugs that are important to remember?

Answer 7

cholestyramine and colestipol

Question 8

What is the MOA of bile acid sequestrants? Benefits?

Answer 8

complexation of bile salts in the gut resulting in

• dec. enterohepatic recirculation of bile salts
• inc. in new bile salt synthesis by the liver
• dec. liver cholesterol
• inc. LDL receptor expression
  *dec blood LDL

Question 9

S/E of bile acid sequestrants.

Answer 9

• Increase VLDL and triglycerides
• GI disturbances
• Malabsorption of lipid-soluble vitamins

Question 10

What are some important drug interactions to remember with bile acid sequestrants?

Answer 10

warfarin
thiazides
digoxin

Question 11

Contraindications to remember with bile acid sequestrants? ( What people shouldn’t be taking them?

Answer 11

those with hypertriclyceridemia

Question 12

How do the nicotinic acid drugs work to affect persons with dyslipidemias?

Answer 12

decrease cAMP and inhibits lipolysis in adipose tissue; with fewer free fatty acids hepatic TG and VLDL synthesis dec.

Question 13

Name the nicotinic acid drugs that are useful in treating dyslipidemia.

Answer 13

Niacin (Vit. B3)

Question 14

What are the S/E of the Nicotonic acid drugs?

Answer 14

flushing, pruritis, burning pain (use aspirin)

hepatoxicity

hyperglycemia

Question 15

Name the important fibrate drugs that you need to remember.

Answer 15

Gemfibrozil, Fenofibrate

Question 16

What is the MOA of fibrates?

Answer 16

binds to the PPARα and increases expression of lipoprotein lipases

Question 17

What are the benefits of using fibrates to treat dyslipidemias?

Answer 17

• dec VLDL and IDL (intermediate density lipoprotein)
• modest dec LDL (however in some patients with combined hyperlipidemia in inc. LDL
• inc HDL (most patients)

Question 18

Main indication for use of fibrates?

Answer 18

hypertriglyceridemia

Question 19

What are the S/E of fibrates?

Answer 19

gallstones, myositis

Question 20

MOA of Ezetimibe

Answer 20

prevents intestinal absorption of cholesterol resulting in dec. LDL

prevents absorption by targeting Niemann-Pick C1-Like 1 (NPC1L1) which is a sterol transporter located on the brush border of the SI

Question 21

S/E of Ezetimibe.

Answer 21

GI distress

Question 22

Name the important PCSK9 inhibitors to remember.

Answer 22

Alirocumab, Evolocumab

Question 23

What is PCSK9?

Answer 23

proprotein convertase subtilisin kexin 9 is a hepatic protease that promotes the destruction of LDL receptors

Question 24

MOA of PCSK9 inhibitors and benefit.

Answer 24

block PCSK9 which can lower LDL 50-60% above that achieved by statin therapy alone

Question 25

Orlistat indication?

Answer 25

weight loss

Question 26

MOA of Orlistat?

Answer 26

inhibits pancreatic lipase > dec. triglyceride breakdown in the intestine

Question 27

S/E of Orlistat?

Answer 27

oily stools (steatorrhea), diarrhea; dec absorption of lipid soluble vitamins

Question 28

ROA for PCSK9 inhibitors?

Answer 28

subQ

Question 29

What are monoclonal antibodies?

Answer 29

antibodies produced by a cell line “cell clone” derived from a single B lymphocyte

Question 30

Are PCSK9 inhibitors monoclonal antibodies?

Answer 30

yes