Drugs for Lipid Disorders

Question 1

HMG-CoA reductase inhibitors

Answer 1

• Atorvastatin (Lipitor)
• Fuvastatin
• Lovastatin
• Pitavastatin
• Pravastatin
• Rosuvastatin (Crestor)
• Simvastatin

Question 2

Niacin

Answer 2

decreases catabolism of Apo-I, reduces VLDL secretion from the liver

Question 3

Fibric acid derivatives (fibrates)

Answer 3

• Fenofibrate

- Gemfibrozil

Question 4

Bile acid sequestrates (resins)

Answer 4

• Cholestyramine
• Colesevelam
• Colestipol

Question 5

Cholesterol absorption inhibitors

Answer 5

Ezetimibe (Zetia)

Question 6

Lomitapide MOA

Answer 6

directly binds and inhibits microsomal triglyceride transfer protein (MTP) in lumen of ER
- prevents assembly of apo-B lipoproteins -> reduced production of chylomicrons and VLDL

Question 7

Mipomersen MOA

Answer 7

antisense oligonucleotide that targets apolipoprotein B-100 and disrupts its function -> decreasing apoB and LDL

Question 8

Evolocumab, alirocumab

Answer 8

PCSK9 inhibitors

- antibodies bind to PCKS9 and inhibit LDL receptor metabolism -> reducing LDL up to 70%

Question 9

Which drug class reduces cholesterol synthesis and upregulates LDL receptors on hepatocytes?

Answer 9

Statins

- inhibit HMG-CoA reductase (*rate-limiting enzyme of cholesterol synthesis)

Question 10

Which drug class decreases secretion of VLDL, increases lipoprotein lipase activity, and increases HDL?

Answer 10

Fibrates

• agonist for peroxisome proliferator-activated receptor alpha (PPAR-a)
• inrease protein synthesis

Question 11

Which drug class decreases LDL?

Answer 11

Bile acid sequestrants

• binds bile acid in the gut preventing reabsorption
• increases cholesterol catabolism
• up-regulates LDL receptors

Question 12

Which drug class inhibits reabsorption of cholesterol excreted in bile, and decreases LDL and phytosterols?

Answer 12

Cholesterol absorption inhibitors

- blocks sterol transporter NPC1L1 in intestine brush border

Question 13

Which drug class increases HDL and decreases lipoprotein A and LDL?

Answer 13

Niacin

• incorporates into nicotinamide adenine dinucleotide
• decreases catabolism of Apo AI
• reduces VLDL secretion from liver

Question 14

What drug class inhibits catabolism of LDL receptors?

Answer 14

PCSK9 humanized monoclonal antibodies

- treatment for familial hypercholesterolemia (is expensive injection, not responsive to oral therapy)

Question 15

What are the effects of statins on LDL, HDL, TG?

Answer 15

• significant decrease in LDL ***
• increase HDL
• decrease TG

Question 16

What are the effects of fibrates on LDL, HDL, TG?

Answer 16

• slightly decrease LDL
• increase HDL
• significant decrease in TG ***

Question 17

What are the effects of niacin on LDL, HDL, TG?

Answer 17

• decrease LDL
• increase HDL
• decrease TG

Question 18

What are the effects of bile acid sequestrants on LDL, HDL, TG?

Answer 18

• decrease LDL
• slightly increase HDL
• minimal effect of TG

Question 19

What are the effects of cholesterol absorption inhibitors on LDL, HDL, TG?

Answer 19

• slight decrease in LDL
• slight increase in HDL
• slight decrease in TG
• ** most important MOA is inhibiting reabsorption of cholesterol