WEEK 2 ANTILIPEMICS Flashcards
Describe the action of HMG-CoA reductase inhibitors
Inhibits HMG-CoA reductase, a key enzyme in endogenous cholesterol synthesis, restricting lipoprotein production
What is the therapeutic effect of HMG-CoA reductase inhibitors?
Lowers total LDL cholesterol and triglycerides, slightly increases HDL cholesterol. Decreases plaque site inflammation and risk of thromboembolism.
Name 1 example of an HMG-CoA reductase inhibitor
Atorvastatin
Name 3 side effects of HMG-CoA reductase inhibitors
- Myopathy/rhabdomyolysis
- Hepatotoxicity/increased liver enzymes
- Peripheral neuropathy
Why should HMG-CoA reductase inhibitors be taken at night?
The liver produces the most cholesterol at night
What are 2 food/drug interactions with HMG-CoA reductase inhibitors?
- Fibrates
- Grapefruit
Describe the action of bile acid sequestrants
Binds bile acids in the GI tract, forming an insoluble complex, which is then cleared from the body
What is the therapeutic effect of bile acid sequestrants?
Decreased plasma cholesterol and LDL cholesterol
Name 1 example of a bile acid sequestrant
Cholestyramine
What time should bile acid sequestrants be taken?
1 hour before or 4 hours after other medications or vitamins (to prevent binding in GI tract)
When should bile acid sequestrants be held?
Bowel obstruction
What are 2 side effects of bile acid sequestrants?
- Constipation (take a fibre supplement)
- GI upset (take with meals)
Describe the action of nicotinic acid
Large doses decrease lipoprotein and triglyceride synthesis by inhibiting the release of free fatty acids from adipose tissue and decreasing hepatic lipoprotein synthesis
What is the therapeutic effect of nicotinic acid?
Adjunctive treatment (with bile acid sequestrants or fibrates) to decrease blood lipids
What are 3 side effects of nicotinic acid?
- Flushing (prevent with NSAIDs)
- Pruritis
- GI upset
What are 3 contraindications for nicotinic acid?
- Liver disease
- Hypertension
- Active bleeding
Describe the action of cholesterol absorption inhibitors
Inhibits absorption of cholesterol in the small intestine
What is the therapeutic effect of cholesterol absorption inhibitors?
Lowers cholesterol to lower the risk for atherosclerosis
What is the name of the only cholesterol absorption inhibitor?
Ezetimibe
Cholesterol absorption inhibitors should not be taken which which group of drugs?
Fibrates
Describe the 3 actions of fibric acid derivatives (fibrates)
- Inhibits peripheral lipolysis
- Decreases triglyceride production by liver
- Decreases production of triglyceride carrier protein
What is the therapeutic effect of fibrates?
Lowers triglycerides and increases HDL
Name 1 example of a fibrate
Gemfibrozil
When are fibrates used?
When patient not responsive to statins
What does fibrates not have an effect on?
LDL levels
What group of drugs should fibrates not be used with?
Statins
What drug should be used with caution in a patient on fibrates?
Warfarin, as fibrates bind to vitamin K which would normally inhibit warfarin
Name 2 side effects of fibrates
- Gallstones
- GI upset
Name 2 examples of platelet aggregation inhibitors
- Aspirin
- Clopidogrel
Describe the action of aspirin
Prevents platelet aggregation and vasoconstriction by blocking the production of thromboxane
Describe the action of clopidogrel
Prevents platelet aggregation by blocking adenosine diphosphate receptors on platelets
