Antilipemic Drugs

Question 1

What’s the difference between Low-density lipoprotein (LDL_ and High-Density lipoprotein (HDL)

Answer 1

LDL is less desired and is cholesterol-rich

HDL is highly desired and is responsible for recycling of cholesterol

Question 2

What are the non-modifiable (2) and modifiable (5) factors for Coronary Artery Disease?

Answer 2

Non-modifiable

• Age: Male 45+ years, female 55+ years or postmenopausal
• Family history: strong history of premature CHD

Modifiable Factors

• Current cigarette smoker
• Abdominal obesity
• Hypertension: BP 140/90, or on antihypertensive medication
• Diabetes mellitus
• LDL/HDL ratio

Question 3

What is the most common group of drugs for lipid lowering?

Answer 3

HMG-CoA reductase Inhibitors

HMG is one of the metabolites in cholesterol synthesis pathway
HMG-CoA Reductase is a critical enzyme for liver cholesterol production

Question 4

How do HMG-CoA reductase inhibitors work?

Answer 4

They inhibit HMG CoA reductase, the liver enzyme that produces cholesterol

Lower’s the rate of cholesterol production

Causes increased liver LDL receptors which increases the plasma clearance of LDL

Question 5

What is an example of a HMG-CoA reductase inhibitor?

Answer 5

Atorvastatin

Question 6

How do statins influence the LDL:HDL ratio?

Answer 6

It increased HDL, which improves the ratio

Question 7

When should HMG-CoA reductase inhibitors be used?

Answer 7

First-line drug therapy for hypercholesterolemia

Treatment of types IIa and IIb hyperlipidemias
- High LDL levels

Question 8

What are the adverse effects of HMG-CoA reductase inhibitors?

Answer 8

• Mild, transient GI disturbances
• Headaches
• Myalgia (muscle pain)
• Liver injury due to elevation in liver enzymes

Question 9

Considerations with Statins

Answer 9

Grapefruit and grapefruit juice impacts some statins (lovastatin, simvastatin, atorvastatin)

Do not use while pregnant

Question 10

Drug Interactions with Statins

Answer 10

Drug inhibitors of CYP3A4

• Warfarin (Coumadin)
• Erythromycin (Macrolide antibacterial)
• Ritonavir (HIV protease inhibitor)

Question 11

Why are Bile Acid Sequestrants important?

Answer 11

Examples are cholestyramine and colestipol and they are taken before meals to prevent reabsorption of bile acids from the small intestine

Question 12

When should you use Bile Acid Sequestrants ?

Answer 12

Type II hyperlipoproteinemia

For relief of pruritus associated with partial biliary obstruction (cholestyramine)

Question 13

What is the main adverse effect for Bile Acid Sequestrants

Answer 13

Can decrease absorption of fat soluble vitamins (A, D, E, K)

GI
- Constipation, heartburn, nausea, belching, bloating

Question 14

How do Fibric Acid Derivatives function and what are some adverse effects (4)?

Answer 14

Activate lipoprotein lipase which reduces plasma TG’s and increases fatty acid use in tissues. Increases HDL by 10-25%

Prolonged prothrombin time*
Increased risk for gallstones
Blurred vision
GI: abdominal discomfort, diarrhea, nausea

Question 15

What is Nicotinic Acid, how does it work, and what are the adverse effects?

Answer 15

Vitamin B3

Reduces a carrier of TG’s (VLDL) which breaks down lipids and less fatty acids for TG production.

Effective, inexpensive, and often used in combination

Adverse effects: flushing, (prevented by aspirin 30 min before), pruritus (especially anal itchiness), GI distress