Chapter 27: Antilipemic Drugs Flashcards
(31 cards)
What are the 3 types of lipoproteins?
- Very-low-density lipoprotein (VLDL)
- Low-density lipoprotein (LDL)
- High-density lipoprotein (HDL)
Very-low-density lipoprotein
- produced by the liver
- transports endogenous lipids to the cells
High-density lipoprotein (HDL)
- responsible for “recycling” of cholesterol
- aka “good cholesterol”
Low-density lipoprotein (LDL)
…
Antilipemic drugs
- used to lower lipid levels
- used as an adjunct to diet therapy
Drug choice based on
the specific lipid profile of the patient
Name the Antilipemics
- hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors (aka statins)
- bile acid sequestrants
- Niacin (vitamin B3, nicotonic acid)
- fibric acid derivatives (fibrates)
- cholesterol absorption inhibitor
What are the most potent LDL reducers?
- pravastatin
- simvastatin
- atorvastatin
- fluvastatin
- rosuvastatin
- pitavastatin
Mechanism of Action for HMG-CoA Reductase Inhibitors
- liver requires HMG-CoA reductase to produce cholesterol
- these drugs inhibit HMG-CoA reductase = decrease cholesterol production
Adverse effects of HMG-CoA Reductase Inhibitors
- elevations in liver enzymes or liver disease
- myopathy (muscle pain), could lead to serious condition rhabdomyolysis
Interactions of HMG-CoA Reductase Inhibitors
- oral anticoagulants
- drugs metabolized by CYP3A4: erythromycin, azole antifungals, verapamil, diltiazem, grapefruit juice
What are the bile acid sequestrant drugs?
- cholestyramine
- colestipol
- colesevelam
Bile acid sequestrants are also known as
bile acid-binding resins and ion-exchange resins
What is the mechanism of action for bile acid sequestrants?
- prevent resorption of bile acids from small intestine
- bile acids are necessary for absorption of cholesterol
What are the indications for bile acid sequestrants?
- relief of pruritus associated with partial biliary obstruction (cholestyramine)
- may be used along with statins
What are the adverse effects of bile acid sequestrants?
- constipation
- heartburn, nausea, belching, bloating (these adverse effects tend to disappear over time)
Niacin (Nicotinic Acid)
- it is a vitamin B3.
- effective, inexpensive and often used in combination with other lipid-lowering drugs.
When using Niacin (Nicotinic Acid),
much lower doses are required for its lipid-lowering effects than are more commonly given when it’s used as a vitamin.
What is the mechanism of action for niacin?
- thought to increase activity of lipase (which breaks down lipids) and inhibit lipolysis in adipose tissue
- reduces the metabolism or catabolism of cholesterol and triglycerides
What is an indication of niacin?
hyperlipidemias
What are the adverse effects of niacin?
- flushing
- pruritus
- GI distress
Current fibric derivatives consist of
gemfibrozil (lopid) and fenofibrate (tricor)
Fibric Acid Derivatives are also known as
fibrates
What is the mechanism of action for fibric acid derivatives?
- activate lipase, which breaks down cholesterol
- suppress the release of free fatty acid from adipose tissue, inhibit synthesis of triglycerides in the liver, and increase secretion of cholesterol in the bile.
