Cholesterol Drugs

Question 1

What are some examples of Statin drugs?

Answer 1

• Simvastatin

* Atorvastatin

Question 2

What is the effect of statin on the cholesterol synthesis and lipoproteins?

Answer 2

• Inhibit cholesterol synthesis
• Increase clearance of IDL and LDL
• Decrease production of VLDL and LDL so less in serum

Question 3

What is the mechanism of action demonstrated by Statins?

Answer 3

• Antagonising HMG-CoA reductase

- Increase in synthesis of LDL receptor

Question 4

What are the uses of Statins?

Answer 4

• Cardiovascular risk prevention

* Familial hypercholesterolemia

Question 5

What are the side effects of Statins?

Answer 5

• Increased transaminase levels (reversible)
• Myopathy resulting in muscle pain.
• Increase in creatinine phosphokinase levels with higher dose
• GI complaints
• Arthralgia
• Headaches

Question 6

What are some examples of cholesterol lipase inhibitors?

Answer 6

•Ezetimibe

Question 7

What are the effects of ezetimibe on cholesterol?

Answer 7

Selectively inhibits intestinal cholesterol absorption

• Decreased intestinal delivery of cholesterol to the liver
• Increased expression of hepatic LDL receptor
• Decreased cholesterol content of atherogenic particles

Question 8

What are the uses of cholesterol lipase inhibitors?

Answer 8

-Cardiovascular risk prevention

Question 9

What are the side effects of Ezetimibe?

Answer 9

• Headache
• Abdominal pain
• Diarrhoea

Question 10

What are the classes of cholesterol drugs?

Answer 10

• Statin
• Cholesterol lipase inhibitors
• Nicotinic Acid
• Fibrates

Question 11

What are the effect of nicotinic acids on cholesterol?

Answer 11

• Reduce VLDL

* Increases HDL at high doses. Best agent to raise HDL-C

Question 12

What is the mechanism of action of nicotinic acids?

Answer 12

•Lipid lowering by inhibition of lipoprotein synthesis

Question 13

What are the uses of Nicotinic acid?

Answer 13

-Reduces coronary events

Question 14

What are the side effects of Nicotinic acids?

Answer 14

• Flushing, Itching, Headache
• Hepatoxicity, GI
• Activation of peptic ulcer
• Hyperglycaemia and reduced insulin sensitivity

Question 15

What are the contraindications of nicotinic acids?

Answer 15

• Peptic ulcer disease

- Active liver disease or unexplained LFT elevations

Question 16

What are effects of fibrates on cholesterol?

Answer 16

PPAR-alpha agonist which increases production of lipoprotein lipase

• Reduces triglyceride production
• Some reduction in LDL but variable

Question 17

What is the mechanism of action of Fibrates?

Answer 17

• Increase in fatty acid uptake and oxidation
• Increase LDL particle size and HDL-C levels
• Direct vascular effects

Question 18

What are some key messages about combination therapies to lower cholesterol?

Answer 18

Statins are used in combination with:

• Fibrate
• Nicotinic Acid
• Ezetimibe
• Omega-3 Fatty acids
• Resins

Question 19

What are some risk of using fibrates and statins?

Answer 19

• Increased risk of myopathy and rhabdomyolysis
• Gemfibrozil in particular may impair glucorinidation of statins.
• Fenofibrate appears to have less potential for impairment of statin metabolism and thus this may account for the reduced reports

Question 20

What are examples of fibrates?

Answer 20

• Fenofibrate
• Bezafibrate
• Gemfibrozil

Question 21

How is Ezetimibe delivered?

Answer 21

Ezetimibe and its active glucuronide circulate entero-hepatically

• Delivers agents back to the site of action
• Limited systemic exposure

Question 22

When are fibrates used?

Answer 22

• Adjunctive therapy to diet
• Hypertriglyceridemia
• Combined hyperlipidaemia with low HDL who do not respond to NA

Question 23

What are some side effects of fibrates?

Answer 23

• GI upset
• Cholelithiasis
• Myositis
• Abnormal LFTs

Question 24

What are some contraindications to consider when using fibrates?

Answer 24

• Hepatic or renal dysfunction

* Pre-existing gallbladder disease

Question 25

What are secondary benefits of statin?

Answer 25

• Anti-inflammatory
• Plaque reduction
• Improved endothelial cell function
• Reduced thrombotic risk