This document discusses hypolipidemic drugs used to treat high cholesterol and triglyceride levels. It describes the different classes of drugs, including statins, bile acid sequestrants, niacin, fibrates, ezetimibe, and omega-3 fatty acids. For each class, it covers the mechanism of action, examples of drugs, indications, effects on lipid levels, adverse effects and interactions. Nursing implications for administration and monitoring of these drugs are also reviewed.

1. HYPOLIPIDEMIC
DRUGS
Dr. Resu Neha Reddy
2nd year Post Graduate
MD Pharmacology
Osmania Medical College

3. Triglycerides and Cholesterol
• Lipoprotein is the combination of triglyceride or
cholesterol with apolipoprotein

5. Lipoproteins
• Very-low-density lipoprotein (VLDL)
• Produced by the liver
• Transports endogenous lipids to the cells
• Low-density lipoprotein (LDL)
• High-density lipoprotein (HDL)
• Responsible for “recycling” of cholesterol
• Also known as “good cholesterol”

7. Cholesterol and Coronary Heart Disease
(CHD)
• The risk of CHD in patients with cholesterol levels of
300 mg/dL is three to four times greater than that in
patients with levels less than 200 mg/dL.

8. Coronary Heart Disease
Positive Risk Factors
• Age
Male 45 years or older
Female 55 years or older
Family history of premature CHD
• Current cigarette smoker

9. Coronary Heart Disease
Positive Risk Factors (cont’d)
• Hypertension
BP 140/90 or higher, or on antihypertensive medication
• Low HDL levels: less than 40 mg/dL
• Diabetes mellitus

10. Coronary Heart Disease
Negative (Beneficial) Risk Factor
• High HDL (“good” cholesterol): 60 mg/dL or higher

11. Hyperlipidemias and Treatment Guidelines
• Antilipemic drugs
Drugs used to lower lipid levels
Used as an adjunct to diet therapy
• Drug choice based on the specific lipid profile of the
patient

12. Treatment Guidelines (cont’d)
• All reasonable non-drug means of controlling blood
cholesterol levels (e.g., diet, exercise) should be tried
for at least 6 months and found to fail before drug
therapy is considered

17. Hypolipidemic drugs
• HMG-CoA reductase inhibitors (HMGs, or statins)
• Bile acid sequestrants
• B vitamin niacin (vitamin B3, nicotinic acid)
• Fibric acid derivatives (fibrates)
• Cholesterol absorption inhibitor (Zetia)
• Combination drugs (Vytorin)

22. HMG-CoA Reductase Inhibitors: Mechanism
of Action
• Inhibit HMG-CoA reductase, which is used by the liver
to produce cholesterol
• Lower the rate of cholesterol production

23. HMG-CoA Reductase Inhibitors (HMGs, or statins)
• Most potent LDL reducers
• lovastatin (Mevacor)
• pravastatin (Pravachol)
• simvastatin (Zocor)
• atorvastatin (Lipitor)
• fluvastatin (Lescol)
• rosuvastatin (Crestor)
• pitavastatin (Livalo)

24. HMG-CoA Reductase Inhibitors: Indications
• First-line drug therapy for hypercholesterolemia
• Treatment of types IIa and IIb hyperlipidemias
• Reduces LDL levels by 30% to 40%
• Increases HDL levels by 2% to 15%
• Reduces triglycerides by 10% to 30%

25. HMG-CoA Reductase Inhibitors: Adverse
Effects
• Mild, transient GI disturbances
• Rash
• Headache
• Myopathy (muscle pain), possibly leading to the serious condition
rhabdomyolysis
• Elevations in liver enzymes or liver disease

26. HMG-CoA Reductase Inhibitors: Interactions
• Oral anticoagulants
• Drugs metabolized by CYP3A4
• erythromycin
• Azole antifungals
• verapamil
• diltiazem
• HIV protease inhibitors
• Amiodarone
• Grapefruit juice

27. Classroom Response Question
A patient with a new prescription for a HMG-CoA (statin) drug is instructed to
take the medication with the evening meal or at bedtime. The patient asks why it
must be taken at this time of day. The reason is:
A. The medication is better absorbed at this time.
B. This timeframe correlates better with the natural diurnal rhythm of cholesterol
production.
C. There will be fewer adverse effects if taken at night instead of with the
morning meal.
D. This timing reduces the incidence of myopathy.

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

30. Bile Acid Sequestrants
• cholestyramine (Questran)
• colestipol (Colestid)
• colesevelam (Welchol)
• Also called bile acid–binding resins and ion-exchange resins

31. Bile Acid Sequestrants: Indications
• Type II hyperlipoproteinemia
• Relief of pruritus associated with partial biliary obstruction
(cholestyramine)
• May be used along with statins

32. Bile Acid Sequestrants:
Adverse Effects
• Constipation
• Heartburn, nausea, belching, bloating
 These adverse effects tend to disappear over time

35. Niacin (Nicotinic Acid)
• Vitamin B3
• Lipid-lowering properties require much higher doses
than when used as a vitamin
• Effective, inexpensive, often used in combination with
other lipid-lowering drugs

36. Niacin: Mechanism of Action
• Thought to increase activity of lipase, which breaks
down lipids
• Reduces the metabolism or catabolism of cholesterol
and triglycerides

37. Niacin: Indications
• Effective in lowering triglyceride, total serum
cholesterol, and LDL levels
• Increases HDL levels
• Effective in the treatment of types IIa, IIb, III, IV, and
V hyperlipidemias

38. Niacin: Adverse Effects
• Flushing (caused by histamine release)
• Pruritus
• GI distress

39. Classroom Response Question
A patient will be taking niacin as part of antilipemic therapy. The best
way to avoid problems with flushing or pruritus would be to:
A. take the medication at bedtime.
B. take the medication with a small dose of a steroid.
C. take the medication with a full glass of water on an empty stomach.
D. start with a low initial dose, and then increase it gradually.

42. Fibric Acid Derivatives: Mechanism of
Action
• Believed to work by activating lipase, which breaks
down cholesterol
• Also 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

43. Fibric Acid Derivatives
• Also known as fibrates
• gemfibrozil (Lopid)
• fenofibrate (Tricor)

44. Fibric Acid Derivatives: Indications
• Treatment of types III, IV, and V hyperlipidemias
• The fibric acid derivatives gemfibrozil and fenofibrate
decrease the triglyceride level and increase the HDL
cholesterol level by as much as 25%

45. Fibric Acid Derivatives:
Drug Effects
• Decrease the triglyceride levels
• Increase HDL by as much as 25%

46. Fibric Acid Derivatives:
Adverse Effects
• Abdominal discomfort, diarrhea, nausea
• Blurred vision, headache
• Increased risk of gallstones
• Prolonged prothrombin time
• Liver studies may show increased function

47. Fibric Acid Derivatives:
Interactions
• Oral anticoagulants
• Statins
• Risk for myositis, myalgias, and rhabdomyolysis is increased
• Laboratory test reactions
• Decreased hemoglobin level, hematocrit value, and white blood cell count
• Increased activated clotting time, lactate dehydrogenase level, and bilirubin
level

50. Cholesterol Absorption Inhibitor
• Ezetimibe (Zetia)
• Inhibits absorption of cholesterol and related sterols from the small
intestine
• Results in reduced total cholesterol, LDL, and triglyceride levels
• Also increases HDL levels
• Often combined with a statin drug
• Clinical usefulness has been questioned; new trials underway
 Currently recommended only when patients have not responded to other therapy

51. Herbal Product: Garlic
• Used as an antispasmodic, antihypertensive, antiplatelet, lipid
reducer
• Adverse effects: dermatitis, vomiting, diarrhea, flatulence,
antiplatelet activity
• Possible interactions with warfarin, diazepam
• May enhance bleeding when taken with NSAIDs

52. Classroom Response Question
A patient wants to take garlic tablets to improve his cholesterol
levels. Which condition would be a contraindication?
A. Hypertension
B. Bowel obstruction
C. Sinus infection
D. Scheduled surgery

53. DOCOSAHEXAENOIC ACID
EICOSAPENTAENOIC ACID

54. Herbal Product: Omega-3
Fatty Acids
• Fish oil products
• Used to reduce cholesterol
• May cause rash, belching, allergic reactions
• Potential interactions with anticoagulant drugs

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

57. Nursing Implications (cont’d)
• Contraindications include biliary obstruction, liver dysfunction,
active liver disease
• Obtain baseline liver function studies
• Patients on long-term therapy may need supplemental fat-soluble
vitamins (A, D, K)
• Take with meals to decrease GI upset

58. Nursing Implications (cont’d)
• Counsel patient concerning diet and nutrition on
an ongoing basis
• Instruct patient on proper procedure for taking
the medications

59. Nursing Implications (cont’d)
• Other medications should be taken 1 hour before or
4 to 6 hours after meals to avoid interference with
absorption
• To minimize adverse effects of niacin, start on low
initial dose and gradually increase it, and take with
meals

60. Classroom Response Question
Before administering niacin, it is most important for the nurse to
assess the patient for
A. allergy to erythromycin.
B. gout.
C. coronary artery disease.
D. hypothyroidism.

61. Nursing Implications (cont’d)
• Small doses of aspirin or NSAIDs may be taken
30 minutes before niacin to minimize cutaneous
flushing
• Inform patients that these drugs may take several
weeks to show effectiveness

62. Nursing Implications (cont’d)
• Instruct patients to report persistent GI upset, constipation,
abnormal or unusual bleeding, and yellow discoloration of the
skin
• Monitor for adverse effects, including increased liver enzyme
studies
• Monitor for therapeutic effects
• Reduced cholesterol and triglyceride levels

63. THANK YOU