Medications to Treat Lipid Disorders

Question 1

Biggest Strategy for lipid disorders

Answer 1

Decrease LDL

Question 2

“Statins” HMG-CoA Reductase Inhibitors

Answer 2

• 1st line of therapy for lipid disorders
• decrease mortality
• Most effective at lowering LDL and total cholesterol -> Raise HDL!

Question 3

Statins MOA:

Answer 3

• inhibit cholesterol synthesis in liver
• stimulate hepatocytes to produce more LDL receptors
• LDL receptors remove the LDL from the blood
• Most effective if given at night since cholesterol is made at night

Question 4

If a diabetic patient’s LDL level is normal do they still receive statin treatment?

Answer 4

Yes, because statins are very effective at preventing Cardiac events

Question 5

Common SE of Statins

Answer 5

Headache, rash, GI, memory loss, disturbance

-monitor for increased SE when statins are combined with other lipid-lowering agents

Question 6

Rare but serious SE of Statins

- Allergy on record

Answer 6

Hepatoxicity:

• Check LFTs before use
• Contraindicated in liver disease
• can use in steatohepatitis

Myopathy/ rhabdomyolysis:

• muscle aches, tenderness, weakness
• Elevated CK levels
• Can lead to Rhabdomyolysis

Increase in incidence of cataracts

Question 7

Food interactions

Answer 7

No grapefruit - causes toxicity

-CyP3A4 pathway

Question 8

Pregnancy Category

Answer 8

X should not be used in pregnant women

Question 9

Prototype for Statins

Answer 9

atorvastatin (Lipitor)

Question 10

Other Statins

Answer 10

Lovastatin ( Mevacor)

Pravastatin (Pravechol)

Question 11

Bile-Acid Sequestrants

Answer 11

• Biologically inert
• Bind to bile acids to form complexes that are excreted
• Since bile acids are made from cholesterol
• Work only in GI tract

Question 12

Side effects of Bile- Acid Sequestrants

Answer 12

• Gi side effects

- Constipation, bloating, indigestion

Question 13

Bile- Acid Sequestrant Prototype

Answer 13

colesevelam (Welchol)

-adminster with food + H2O

Question 14

Cholesterol Absorption Inhibitor

Answer 14

• Blocks cholesterol absorption in small intestine

- also blocks cholesterol secreted in bile

Question 15

Cholesterol Absorption Inhibitor SE:

Answer 15

equal placebo

- Watched for increased liver toxicity with statin

Question 16

Cholesterol Absorption Inhibitor Prototype

Answer 16

Ezetimibe (Zetia)

Question 17

Vytorin

Answer 17

ezetmibe+ sivastatin

• chlolesterol absorbed through food
• and what your body already blocks
• watch for liver toxicity

Question 18

Fibric Acid Derivatives (Fibrates)

Answer 18

MOA: accelerate the clearance of VLDLs

• Used for high tryglycerides
• Most effective for lowering TG levels
• little to no effect on LDL cholesterol

Question 19

Fibrates prototype

Answer 19

gemfibrozil (Lopid)

Question 20

Fibrates SE

Answer 20

Rash and GI upset, Increased risk of gallstones, myopathy, hepatotoxicity
-Supersize me

Question 21

Fibrates Drug-Drug

Answer 21

Warfarin: increased risk of bleeding
Statins: increased risk of rhabdo

Question 22

Monoclonal Antibodies PCSK9 Inhibitors

Answer 22

Prototype: evolocumab (Repatha)
Others: alirocumab (Praluent)

Question 23

Monoclonal Antibodies PCSK9 Inhibitors MOA:

Answer 23

binds to PCSK9 which block PCSK9 binding to LDL receptors. This increases LDL receptors, allowing LDL to bind to the receptors and be removed from the blood.

Question 24

Monoclonal antibodies indications

Answer 24

-approved for familial hypercholesterolemia or atherosclerotic heart problems who maxed out statins.

Question 25

Monoclonal antibodies route and SE

Answer 25

• adminstered SQ

SE: injection site reactions, vasculitis, rash ,uticaria. Antibody production can occur.

Question 26

Other cholesterol agents

Answer 26

Fish Oil - taken in pill form. Evidence doesn;t support that it prevents heart disease.
Plant sterols and Sterol esters: Benecol and promise brands
Cholestin: made from rice fermented yeast