Antilipemic Agents

Antihyperlipedemic Drugs
Drugs used to lower lipid levels

Hyperlipedemia
Abnormal elevation of cholesterol and triglycerides in the blood A primary cause of atherosclerosis

Atherosclerosis
Characterized by accumulation of fatty deposits on the inner walls of arteries and arterioles throughout the body that reduces the blood supply to vital organs resulting to strokes, angina pectoris , myocardial infarction and peripheral vascular disease

Triglycerides and Cholesterol
Two primary forms of lipids in the blood WaterWater-insoluble fats that must be bound to apoproteins, specialized lipidlipid-carrying proteins Lipoprotein is the the combination of triglyceride or cholesterol with apoprotein

Types of Lipoproteins
Lipid Lipoprotein Classification Most chylomicron ProteinContent ProteinContent Content Least

veryvery-low density lipoprotein (VLDL) Intermediate-density lipoprotein Intermediate(IDL) Least High-density lipoprotein (HDL) HighMost

Hyperlipidemia is a major risk factor for atherosclerosis. Most of the evidence specifically implicates hypercholesterolemia. hypercholesterolemia. Elevated levels of serum cholesterol are sufficient to stimulate lesion development.

Coronary Heart Disease
The risk of CHD in patients with cholesterol levels of 300 mg/dL is 3 to 4 times greater than that in patients with levels less than 300 mg/dL

Antilipemics
Bile acid sequestrants HMGHMG-CoA reductase inhibitors (HMGs or statins) Fibric acid derivatives Niacin (nicotinic acid)

Antilipemics: Bile Acid Sequestrants
cholestyramine (Questran) colestipol hydrochloride (Colestid) Also called bile acid-binding resins acidand ionion-exchange resins

Antilipemics: Bile Acid Sequestrants
Mechanism of Action
Prevent resorption of bile acids from small intestine Bile acids are necessary for absorption of cholesterol

Antilipemics: Bile Acid Sequestrants
Therapeutic Uses
hyperlipoproteinemia Relief of pruritus associated with partial biliary obstruction (cholestyramine) (cholestyramine)

Antilipemics: Bile Acid Sequestrants
Side Effects Constipation
± Heartburn, nausea, bloating These adverse effects tend to disappear over time

Antilipemics: HMG-CoA Reductase HMGInhibitors (HMGs or statins)
lovastatin (Mevacor) pravastatin (Pravachol) simvastatin (Zocor) atorvastatin (Lipitor) cerivastatin (Baycol) fluvastatin (Lescol)
Most potent LDL reducers

Antilipemics: HMGHMG-CoA Reductase Inhibitors
Mechanism of Action
Inhibit HMG-CoA reductase, which is used HMGby the liver to produce cholesterol Lower the rate of cholesterol production

Antilipemics: HMGHMG-CoA Reductase Inhibitors
Therapeutic Uses
Treatment of hyperlipidemias
± Reduce LDL levels by 30 to 40% ± Increase HDL levels by 2 to 15% ± Reduce triglycerides by 10 to 30%

Antilipemics: HMGHMG-CoA Reductase Inhibitors
Side Effects
Mild, transient GI disturbances Rash Headache Myopathy (muscle pain) Elevations in liver enzymes

Antilipemics: Fibric Acid Derivatives
clofibrate gemfibrozil (Lopid) fenofibrate (Tricor)

Antilipemics: Fibric Acid Derivatives
Mechanism of Action ‡ Increase the activity of lipoprotein lipase thereby increasing th removal of VLDL from the plasma. Believed to work by activating lipase, which breaks down cholesterol Also suppress release of free fatty acid from the adipose tissue, inhibit synthesis of triglycerides in the liver, and increase the secretion of cholesterol in the bile

Antilipemics: Antilipemics: Fibric Acid Derivatives
Therapeutic Uses Treatment of hyperlipemias Treatment of hyperlipidemias
Decrease the triglyceride levels and increase HDL by as much as 25%

Antilipemics: Fibric Acid Derivatives
Side Effects
Abdominal discomfort Diarrhea Nausea Blurred vision Increased risk of gallstones Prolonged prothrombin time Liver studies may show increased function

Antilipemics: Niacin (Nicotinic Acid)
Vitamin B3 LipidLipid-lowering properties require much higher doses than when used as a vitamin Effective, inexpensive, often used in combination with other lipid-lowering lipidagents

Triacylglycerol (-) Niacin Adipose Tissue Fatty Acids Liver Fatty Acids Triacylglycerol VLDL

Antilipemics: Niacin (Nicotinic Acid)
Mechanism of Action
Thought to increase activity of lipase, which breaks down lipids Reduces the metabolism or catabolism of cholesterol and triglycerides Inhibit lipolysis in the adipose tissue,resulting in decreased hepatic VLDL synthesis.

Antilipemics: Niacin (Nicotinic Acid)
Therapeutic Uses
Effective in lowering triglyceride, total serum cholesterol, and LDL levels Increases HDL levels Effective in the treatment of hyperlipidemias

Antilipemics: Niacin (Nicotinic Acid)
Side Effects
Flushing (due to histamine release) Pruritus GI distress

Antilipemics: Nursing Implications
Before beginning therapy, obtain a thorough health and medication history. Assess dietary patterns, exercise level, weight, height, VS, tobacco and alcohol use, family history. Assess for contraindications, conditions that require cautious use, and drug interactions.

Antilipemics: Nursing Implications
Contraindications include biliary obstruction, liver dysfunction, active liver disease. Obtain baseline liver function studies. Patients on long-term therapy may longneed supplemental fat-soluble fatvitamins (A, D, K). Take with meals to decrease GI upset.

Antilipemics: Nursing Implications
Pati nt tb n l n rnin i t an n triti n n an n in basis. Instr t n r r r r f r takin t i ati ns. Powder for s st be taken wit a li id, i ed t oroughl but not stirred, and thoroughl taken dr . ther edi ations should be taken hour before or to 6 hours after eals to avoid interferen e with absor tion.

Antilipemics: Nursing Implications
Clofibrate often causes constipation; instruct patients to increase fiber and fluid intake to offset this effect. To minimize side effects of niacin, start on low initial dose and gradually increase it, and take with meals. Small doses of aspirin or NSAIDs may be taken 30 minutes before niacin to minimize cutaneous flushing.

Antilipemics: Nursing Implications
Inform patients that these agents may take several weeks to show effectiveness. Instruct patients to report persistent GI upset, constipation, abnormal or unusual bleeding, and yellow discoloration of the skin.

Antilipemics: Nursing Implications
Monitor for side effects, including increased liver enzyme studies. Monitor for therapeutic effects:
± Reduced cholesterol and triglyceride levels

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