Lipid lowering medications

Question 1

What are the 2 classes of lipid lowering drugs that reduce absorption of fats?

Answer 1

Bile acid binding resins and ezetimide (reduce intestinal sterol reabsorption)

Question 2

What are the 2 classes of lipid lowering drugs that increase peripheral clearance of cholesterol?

Answer 2

1. ** Statins (HMG-CoA reductase inhibitors)
2. Fibrates

Question 3

What is the class of lipid lowering drugs that reduce LDL receptor degradation?

Answer 3

PCSK9 inhibitors

Question 4

Which class of lipid lowering drugs reduces triglyceride synthesis?

Answer 4

Omega-3-acid ethyl esters

Question 5

Name at least 2 statins

Answer 5

Atorvastatin
Pravastatin
Simvastatin
Lovastatin

Question 6

What is the MOA of statins?

Answer 6

Inhibits HMG-CoA reductase, an enzyme which is involved in the rate limiting step in cholesterol synthesis.

Upregulates LDL receptors to internalize more LDL

Question 7

What is the unique property of statins?

Answer 7

Advised to be taken in the evening
- Peak endogenous cholesterol synthesis is in the night
- Synchronisation of statin peak concentration with the peak synthesis

Question 8

What are the adverse effects of statins?

Answer 8

1. Liver abnormalities
2. Myopathy & rhabdomyolysis
3. Urine turns tea colour

Question 9

Which groups of patients are contraindicated to take statins?

Answer 9

1. Pregnant
2. Nursing mothers
3. Children
4. Teenagers

Affects neurodevelopment of fetus and child

Question 10

What is the class of drug recommended if patients are intolerant to statins?

Answer 10

PCKS9 inhibitors

Question 11

Name 2 PCKS9 inhibitors

Answer 11

Evolocumab
Alirocumab

Question 12

What is the MOA of PCKS9 inhibitors?

Answer 12

Inhibits PCKS9 which is an enzyme that catalyses the degradation of LDL receptors.

Reduce LDL receptor degradation, more LDL receptors that can bind to and internalise circulating LDLs

Question 13

What is the ROA of PCKS9 inhibitors?

Answer 13

Injection! because they are monoclonal antibodies

Question 14

What are the adverse effects of PCKS9 inhibitors?

Answer 14

1. Serum sickness - contraindicated in patients with previous hypersensitivity reactions
2. Injection site inflammatory reaction
3. Nasopharyngitis and sinusitis

Question 15

Name 2 fibrates

Answer 15

Gemfibrozil, fenofibrate

Question 16

What is the MOA of fibrates?

Answer 16

Increase peripheral clearance by increasing activity of lipoprotein lipase (break down triglycerides)

More used in treatment of hypertriglyceridemias

Question 17

What is a unique adverse effect of fibrates?

Answer 17

Gall stones

Question 18

What is the drug name of omega 3 acid ethyl ester?

Answer 18

Omacor

Question 19

What is the MOA of omega 3 acid ethyl esters?

Answer 19

Reduce triglyceride production and increase free fatty acid breakdown via beta oxidation.

Question 20

What are the contraindications and adverse effects of omega 3 acid ethyl ester?

Answer 20

Contraindicated in patients who are allergic to fish.

1. GIT symptoms
2. Reduced production of thromboxane A2 (coagulant) -> increased bleeding time

Question 21

Name a resin

Answer 21

Cholestyramine

Question 22

What is the MOA of resins?

Answer 22

Bile acids bind to bile salts leading to a decrease in bile acid concentration.

This causes hepatocytes to increase conversion of cholesterol to bile acids

Intracellular cholesterol concentration decreases.

Question 23

What is the unique adverse effect of bile acid binding resins?

Answer 23

Impaired absorption of vitamin A, D, E, K

Question 24

What is the MOA of ezetimibe?

Answer 24

Reduces cholesterol absorption at the small intestine

Question 25

What is Vytorin?

Answer 25

Ezetimibe + simvastatin

Question 26

What is the unique adverse effect associated when ezetimibe is combined with statins?

Answer 26

Rhabdomyolysis