Module C: Drugs for Hypercholesterolemia

Question 1

Lipids

Answer 1

-cannot be dissolved in plasma- must be transported in blood via. lipoproteins- either HDL or LDL

Question 2

Low-density Lipoproteins (LDLs)

Answer 2

-contain high % of cholesterol, some used in body into cell membranes and steroids, but also used in development of atherosclerosis

Question 3

High-Density Lipoproteins (HDLs)

Answer 3

• ratio of protein to lipid is high
• often referred to as “good” lipoproteins
• transport cholesterol from atheroma back to liver = reverse cholesterol transport
• require extra cholesterol from macrophages in blood
• this reverse transport lowers cholesterol and decreases risk of CHD

Question 4

Triglycerides

Answer 4

• composed of fatty acids and glycerol

- oxidized to generate energy for muscle contraction and metabolic reactions

Question 5

Cholesterol

Answer 5

precursor to steroid compounds that fulfill vital physiologic functions

Question 6

Hypercholesteremia

Answer 6

-contributes to development of atherosclerosis, coronary artery disease, and other atherosclerotic vascular diseases

Question 7

Risk factors associated with CHD

Answer 7

cigarette smoking
low level of HDL cholesterol
male gender
family history o premature CHD
aging
hypertension

Question 8

TLC

Answer 8

therapeutic lifestyle changes

• embrace dietary modifications, weight management, and physical activity
• exercise increases HDL levels
• diets should be low in cholesterol, saturated fat, and calories (these increase LDLs)

Question 9

Role of omega-3 fatty acids and CHD

Answer 9

omega-3 fatty acids (linolenic acid and those in fish oils) improve the ratio of LDL-C to HDL-C
-can also help reverse angiographic evidence of coronary atherosclerosis and reduce mortality rate in pt. with CHD

Question 10

How statins reduce hypercholesterolemia

Answer 10

-treat hypercholesterolemia, and also prevent CAD and reduce its risk of mortality

• they inhibit enzyme, HMG-CoA (involved in biosynthesis of cholesterol) = then limits production of very low-density lipoproteins (VLDLs) = more LDL taken back into liver reducing amount of LDL vs HDL
• typically decrease LDLs by 20-50% and increase HDLs by 10%
• relatively low bioavailability- extensive first pass metabolism
• relatively short half-lives

Question 11

Adverse effects of Statins

Answer 11

most serious effect is rhabdomyolysis (potentially fatal form of skeletal muscle toxicity - myopathy)
GI problems
liver damage
memory loss
Type-2 Diabetes

Question 12

examples of statins

Answer 12

Atorvastatin
Fluvastatin
Lovastatin
Pitavastatin
Pravastatin
Rosuvastatin
Simvastatin