Drugs to treat dyslipidemias

Question 1

BL: What statins are used to lower cholesterol and triglycerides?

Answer 1

Atorvastatin and Rosuvastatin

Question 2

BL: What is the rate limiting enzyme of bile acid synthesis?

Answer 2

7alpha-Hydroxylase

Question 3

BL: What statins have a short half life? What is the most optimal time of day to take short half life statins?

Answer 3

Fluvastatin, Lovastatin, and Simvastatin are short half life statins and they are typically taken at night because endogenous cholesterol synthesis is highest at night.

Question 4

BL: Where does the mechanism of action for ezetimibe occur?

Answer 4

Ezetimibe inhibits cholesterol absorption at the enterocytes of the small intestine

Question 5

BL: What cholesterol lowering drug can be used for pregnancy and what is contraindicated?

Answer 5

During pregnancy, resins can be used. In addition, resins can be taken by children age 6 years or older. Statins are contraindicated in pregnancy. Statins are also contraindicated in nursing mothers and acute liver disease.

Question 6

BL: What fibrate is associated with increased risk of gallstones?

Answer 6

Clofibrate

Question 7

BL: What drug is associated with increased HDL

Answer 7

Niacin or Nicotinic Acid

Question 8

LB: What is the first line treatment for hyperlipidemia?

Answer 8

• Eat less fat
• Eat less sugar and alcohol to lower triglycerides
• Exercise to raise that HDL

Question 9

LB: What is the difference between primary and secondary hyperlipidemia?

Answer 9

Primary is caused by genetics or diet, secondary is caused by drugs or illness.

Question 10

BL: What drugs by themselves are related with myopathy? Explain what these drugs do to cause this?

Answer 10

Statins cause muscle weakness, mylagia and/or dark brown urine. It causes elevated creatine phosphokinase.

Fibrates cause myopathy. Worst with clofibrate by inhibiting OATP2 and competes with glucuronidation enzymes.

Question 11

BL: What drugs can cause secondary hyperlipdemia

Answer 11

thiazide diuretics, beta blockers (nonspecific), and oral contraceptives

Question 12

BL: What disease should you avoid treating with NIcotinic acid? Why? What is the recommended treatment?

Answer 12

Familial hypertriglyceridemia Type IV because nicotinic acid may exacerbate their glucose intolerance and hyperuricemia.

Fibrates

Question 13

What are the two Proprotein Convertase Subtilisin/Kexin 9 Inhibitors (PCSK9)? What is their MOA?

Answer 13

Alirocumab & Evolocumab

Promotes LDL receptor degradation at hepatocytes, which lowers LDL levels.

Question 14

What dyslipidemia drugs are injected sub cutaneously?

Answer 14

Proprotein Convertase Subtilisin/Kexin 9 Inhibitors (PCSK9)

Question 15

CYP3A4 affects which statins?

Answer 15

Lovastatin
Atorvastatin
Simvastatin

Question 16

What is the MOA of Ezetimibe?

Answer 16

It inhibits the NPC1L1 transporter protein, which is responsible for cholesterol absorption.

Question 17

Why is Ezetimibe given only once a day?

Answer 17

It undergoes hepatic recirculation.

Question 18

What statins do you avoid if a patient has a CYP2C9 polymorphism?

Answer 18

Rosuvastatin & Fluvastatin

Question 19

What resin drug has the least amount of side effects?

Answer 19

Colesevelam

Question 20

True or False? Statins lower HDL.

Answer 20

True. This is a side effect not a desired effect.