Cholesterol Lowering Drugs

Question 1

Name the 4 main classes of cholesterol lowering drugs.

Answer 1

HMG Co-A reductase inhibitors
Fibrates
Bile acid binding resins
Ezetimibe

Question 2

What is the MOA of Ezetimibe?

Answer 2

Decreases the absorption of dietary and biliary cholesterol by inhibiting its transport across the intestinal wall. This causes increased demand for cholesterol, increased LDL uptake and removal from plasma.

Question 3

Name a precaution to ezetimibe use.

Answer 3

Treatment with fenofibrate. May increase risk of gall bladder disease.

Question 4

What is the daily dose of ezetimibe?

Answer 4

10mg daily

Question 5

Name 1 counselling point for ezetimibe.

Answer 5

Watch for signs of myalgia especially if using combination therapy with a statin.

Question 6

What is the MOA of statins?

Answer 6

Competitively inhibit HMG Co-A reductase causing increased hepatic cholesterol uptake from the blood, decreasing concentration of total cholesterol, LDL, TGs and slight increase in HDL.

Question 7

Name 3 indications for the use of statins.

Answer 7

Hypercholesterolaemia
High risk of coronary artery disease
Heterozygous familial hypercholesterolaemia in children

Question 8

Name 3 adverse effects of statins.

Answer 8

Myalgia
Transient GI upset
Sleep disturbance
High aminotransferases

Question 9

What is the dose range for statins?

Answer 9

10-40mg daily. Maximum 80mg/day.

Question 10

List 2 counselling points for statins.

Answer 10

Avoid grapefruit juice.
Watch for unexplained muscle pain.
Monitor creatinine kinase.

Question 11

What is the MOA of fenofibrate?

Answer 11

Modulates lipoprotein synthesis and catabolism causing decreased plasma TG and moderately increases HDL levels.

Question 12

Name 3 indications for the use of fenofibrate.

Answer 12

Severe hypertriglyceridaemia
Dyslipidaemia associated with T2DM
Hypercholesterolaemia (2nd line)

Question 13

Name 3 precautions to fenofibrate use.

Answer 13

Photosensitivity
Pancreatitis
Treatment with ezetimibe (may worsen gall bladder disease).

Question 14

What is the daily dose of fenofibrate?

Answer 14

145mg daily
CrCl: 20-60ml/min = 96mg daily
CrCl: 10-20ml/min = 48mg daily

Question 15

What is the MOA of cholestyramine?

Answer 15

Binds bile acids in the intestinal lumen preventing reabsorption and increasing bile acid excretion in the faeces.

Question 16

Name 3 indications for use of cholestyramine.

Answer 16

Hypercholesterolaemia
Itch associated with biliary tract obstruction
Diarrhoea following ill resection or disease.

Question 17

What is the dose of cholestyramine?

Answer 17

Initially 4g bd, increasing to 12-16g per day.

In combination with other lipid-lowering therapy, 4g once-twice daily.

Question 18

Name 2 practice points for cholestyramine.

Answer 18

Mix with water or juice.

Decrease gritty texture by mixing and allowing to stand in the fridge for at least 4 hours.