Chapter 29 Antilipemic Drugs

Question 1

Antilipemics

Answer 1

• Used for primary prevention of cardiac event in patients with risk factors (cholesterol level of 5.2 mmol/L)
• Used for secondary prevention of subsequent cardiac events in individuals who have previously suffered a heart event (i.e. MI)

Question 2

HMG CoA Reductase Inhibitors

Answer 2

• Also called “statins”
• Atorvastatin (most effective)
• Lower blood cholesterol levels by decrease rate of production. When less cholesterol is produced, the liver increases the number LDL receptors to recycle LDL from circulation. Increases HDLs.
• Combined therapy with other statins, fibrates or niacin may be necessary for desired results
• Contraindicated with known allergy, pregnancy and possibly liver disease
• Adverse effects: GI distrubances, rash, headache are most common. Increased liver enzymes including CPK. Rhabdomyolysis (muscle pain) is rare but an urgent, serious condition to know and understand before it becomes fatal
• Interactions: Use cautiously with oral anticoagulants, oral hypoglycemics, erythormucin, gemfibrozil, insulin, niacin, and grapefruit juice; added risk of rhabdomyolsis

Question 3

Bile Acid Sequestrants

Answer 3

• Bile acid binding resins
• Cholestyramine
• Prevent resorption of bile acids from small intestine so it is excreted in bowel movement. The more the bile acids are excreted, the more the liver converts cholesterol to bile acids, reducing cholesterol in liver and circulation
• Commonly used as an adjunct to statin therapy
• Do not use if allergic or bowel obstruction present
• Adverse Effects: constipation is common & heartburn, bloating, belching, nausea
• Interactions: All drugs should be taken at least one hour before or 4-6 hours after these drugs. Decreases absorption of fat soluble vitamins A,D,E,K

Question 4

Nicotinic Acid (Vitamin B3)

Answer 4

• Also known as niacin
• Often given as adjunct to statins
• Inhibit lipolysis in adipose tissue, decrease esterification of triglycerides in the liver, and increase the activity of lipoprotein lipase. Resultant effect: decreased triglyceride levels, decreased LDL and increased HDL levels. Causes histamine release which increases acid secretion
• Therapeutic effects noticed after 1-4 days of therapy
  Maximum effects in 3-5 weeks of continuous therapy
• Contraindicated in peptic ulcer disease, hypertension, active hemorrhagic process
• Adverse effects: Flushing (cutaneous, superficial - take NSAIDs 30 minutes before), Pruritis, GI distress

Question 5

Fibric Acid Derivatives (Fibrates)

Answer 5

• Activate lipoprotein, the enzyme responsible for breaking down cholesterol. Resultant effect is reduction of triglycerides and VLDL & LDL concentrations. Also noted to increase HDL levels
• Can also induce changes in blood coagulation including decreased platelet adhesion and increased fibrinolysis
• Gemfibrozil
• Contraindicated in drug allergy, severe liver, kidney disease, cirrhosis and gallbladder disease
• Adverse effects: Abdominal discomfort, diarrhea, nausea, Headache, blurred vision, Increase risk of gallstone, Prolonged bleeding time
• Interactions: Gemfibrozil can enhance the action of oral anticoagulants, Risk of rhabdomyolysis is increased when fibrates are used with statins