B / 9 : Drugs affecting the lipid metabolism

Question 1

How can you prevent artherosclerosis? (4)

Answer 1

• Physical exercise (increases HDL production)
• Healthy diet
• Estrogen
• Drugs

Question 2

What are the 3 statins?

Answer 2

• Simvastatin
• Atorvastatin
• Rosuvastatin

Question 3

Simvastatin, Atorvastatin, Rosusvastatin
- MOA
- Effect
- Indication
- Contraindication
- SE
- ROA

Answer 3

• HMG-CoA reductase inhibitors
• Decreases cholesterol synthesis, increases LDL receptor expression, decreases plasma LDL, HDL and TAG
• For prevention of atherosclerotic vascular disease, acute coronary syndrome
• Not in pregnancy or if sever liver failure
• Myopathy, myalgia, constipation, diarrhea
• Oral

Question 4

What reaction does HMG-CoA reductase catalyse?

Answer 4

The conversion of HMG-CoA to mevalonate, in the liver (which is inhibited by statins)

Question 5

What is a sterol absorption inhibitor?

Answer 5

Ezetimibe

Question 6

Ezetimibe
- MOA
- Effect
- Indication
- Contraindication
- SE
- ROA

Answer 6

• Inhibition of intestinal cholesterol absorption
• Decreased cholesterol content in chylomicron, increased expression of hepatic LDL receptor
• For reduction of elevated cholesterol
• No in pregnancy or if liver disease
• Increased liver enzymes
• Oral

Question 7

What are bile acid sequestrants?

Answer 7

Large, non-absorbable polymers that bind bile acids and steroids in the intestine and prevent their absorption (ex : colesevelam)

Question 8

Colesevelam
- MOA
- Effect
- Indication
- SE
- ROA

Answer 8

• Bile acid sequestrant
• Decreased bile acid reuptake, increased uptake of LDL from circulation via increased LDL receptor expression
• For isolated LDL-C increase
• Nausea, flatulence, malabsorption, can interfere with absorption of other drugs
• Oral

Question 9

Which lipid metabolism drugs can be used even in pregnancy?

Answer 9

• Colesevelam
• Fenofibrate

Question 10

Fenofibrate
- MOA
- Effect
- Indication
- SE
- ROA

Answer 10

• Agonist for PPR-alpha (transmission factor)
• Activate lipoprotein lipase, decreased VLDL and TAG, increased beta oxidation of TAG
• For hyperlipidemia
• Rhabdomyolysis, acute kidney failure, gallstones, hypoglycemia
• Oral