Chapter 27: Antilipemic Drugs Flashcards
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.
What is an indication for fibric acid derivatives?
hyperlipidemia
What are the adverse effects of fibric acid derivatives?
- abdominal discomfort, diarrhea, nausea
- blurred vision, headache
- increased risk of gallstones
- prolonged prothrombin time
- liver studies may show increased enzyme levels
- myopathy
Cholesterol Absorption Inhibitor
inhibits absorption of cholesterol and related sterols from small intestine
What are the select cholesterol absorption inhibitors?
ezetimibe
Inhibition of the absorption of cholesterol and related sterols from the small intestine results in:
- reduced total cholesterol, LDL, and triglyceride levels
- increased HDL levels
- often combined with a statin drug
Clinical trials continue
currently recommended only when patients have not responded to other therapy
Nursing Process
discuss the nursing process focus on patient-centered care pgs 446-449.
