7. Anti-hyperlipidemics

Question 1

Hyperlipidemias have been classified into ___ major subtypes.

Answer 1

5

Question 2

Coronary heart disease (CHD) causes ___ of all deaths in US

Answer 2

1/2

Question 3

The incidence of CHD correlates with elevated levels of ________& _________ and low levels of ________ cholesterol

Answer 3

LDL cholesterol, triacylglycerols, HDL

Question 4

T/F The most common types of hyperlipidemias involve elevated LDL (IIa) > VLDL (IV) or both LDL and VLDL (IIb)

Answer 4

False.

Other way around

Question 5

T/F Risk factors for CHD include cigarette smoking, hypertension, obesity, diabetes, and family history

Answer 5

True

Question 6

Anti-hyperlipidemic therapies aim to:

a. increase degradation
b. increase removal
c. decrease absorption
d. decrease carrier production
e. all of the above

Answer 6

e. all of the above

Question 7

What is the therapeutic goals of anti-hyperlipidemics?

Answer 7

LDL and HDL about the same amount in our body

Question 8

What are the anti-hyperlipidemic drug classes?

Answer 8

1. HMG CoA Reductase Inhibitors (Statins)
2. Fibrates
3. Niacin
4. Cholesterol Absorption Inhibitors
5. Bile Acid Sequestrants
6. Omega-3 Fatty Acids

Question 9

What are the HMG CoA Reductase Inhibitors (Statins)?

Answer 9

1. Atorvastatin [Lipitor®] "MOST COMMON"
2, Rosuvastatin [Crestor®]
3. Simvastatin [Zocor®]
4. Pravastatin [Pravachol®]
5. Lovastatin [Mevacor®]

Question 10

Which HMG CoA Reductase Inhibitors (Statins) has the highest percentage on Serum LDL chlesterol reduction produced?

Answer 10

Atorvastatin (50%) and Rosuvastin (50%)

Question 11

Which HMG CoA Reductase Inhibitors (Statins) has the lowest percentage on Serum LDL chlesterol reduction produced?

Answer 11

Fluvastatin (24%)

Question 12

Which HMG CoA Reductase Inhibitors (Statins) has the highest percentage on Serum triacylglycerol reduction produced?

Answer 12

Atorvastatin (29%)

Question 13

Which HMG CoA Reductase Inhibitors (Statins) has the lowest percentage on Serum triacylglycerol reduction produced?

Answer 13

Fluvastatin (10%)

Question 14

Which HMG CoA Reductase Inhibitors (Statins) has the highest percentage on Serum HDL cholesterol increase produced?

Answer 14

Pravastatin (12%) and Simvastatin (12%)

Question 15

Which HMG CoA Reductase Inhibitors (Statins) has the lowest percentage on Serum HDL cholesterol increase produced?

Answer 15

Atorvastatin (6%)

Question 16

Which HMG CoA Reductase Inhibitors (Statins) has the longest Plasma half-life (hr)?

Answer 16

Rosuvastatin (19hrs)

Question 17

Which HMG CoA Reductase Inhibitors (Statins) has the shortest Plasma half-life (hr)?

Answer 17

Fluvastatin, Pravastatin and Simvastatin

“all have 1-2 hrs half-life”

Question 18

Which HMG CoA Reductase Inhibitors (Statins) can penetrate the central nervous system?

Answer 18

Lovastatin and Simvastatin

Question 19

What is the indication for Atorvastatin?

Answer 19

Hyperlipidemia/CVD Prevention

Question 20

The mechanism of action of Atorvastatin is competitively inhibits ________ which is responsible for an early, rate-limiting step in cholesterol biosynthesis.
It also increases hepatic ______receptors, enhancing catabolism.

Answer 20

HMG-CoA Reductase, LDL

Question 21

What is the common adverse effect when taking Atorvastatin?

Answer 21

The 50% probability of cataract in statin users occurred at age 51.7 and 54.9 years in patients with type 2 diabetes and without diabetes, respectively, vs at age 55.1 and 57.3 years in non-statin users, respectively

Question 22

Which Statin drugs cause the least significant side effects?

Answer 22

Simvastatin and Pravastatin

Question 23

What is the drug interactions of Cyclosporin, Erythromycin, Azole antifungals in the presence of Atorvastatin?

Answer 23

Decrease metabolism —-> Myopathy exacerbation

Question 24

What is the contraindications/cautions when taking Atorvastatin?

Answer 24

Azole antifungals
-Production of endogenous steroids, whose activities or levels may be reduced by ketoconazole may be further blunted at adrenal and gonadal levels by statins

Question 25

What is Fibrates?

Answer 25

That’s a class of anti-hyperlipidemic drugs.

Question 26

What are the Fibrates (anti-hyperlipidemic) drugs?

Answer 26

1. Fenofibrate [Tricor®, Lofibra®, Triglide®] “MOST COMMON”

2. Gemfibrozil [Lopid®]

Question 27

1. The Mechanism of Action of Fenofibrate is to stimulates nuclear receptor ______ which modulates transcription of ______ genes in liver, muscle and adipose tissue
2. It also enhances ______ production; inhibits ______ synthesis and stimulates catabolism of ______.

Answer 27

PPAR, insulin sensitive

HDL, triglyceride, triglyceride-rich lipoproteins

Question 28

What is the drug interactions of Acyclovir, Aminoglycosdes, cyclosporine, and Ganciclovir with Fenofibrate?

Answer 28

Impaired renal elimination

Question 29

Fenofibrate impaired metabolism of ________.

Answer 29

Sulfonylureas

Question 30

What is Niacin?

Answer 30

It’s one of the anti-hyperlipidemic drug classes.

Question 31

What are the Niacin drugs?

Answer 31

Nicotinic Acid [Vitamin B3, Niacin, Niaspan®, Slo-Niacin®]

Question 32

What is the drug indication of Niacin?

Answer 32

Hypertriglyceridemia, Hypercholesterolemia and Mixed Dyslipidemia
Dosing [50-1000mg]
- 1500-3000mg/d

Question 33

The mechanism of action of Niacin is to Inhibits _____ in adipose tissue, resulting in reduced hepatic _____ synthesis and production of _____ in the plasma.

Answer 33

lipolysis, VLDL, LDLs

Question 34

Niacin induces prostaglandin D2 production which causes..

Answer 34

vasodilation (flushing) and hypothetically Mueller cell toxicity

Question 35

Ocular effects self-resolve in about ___ wks following discontinuation of therapy.

Answer 35

2

Question 36

What is the drug interactions of Alpha-blockers and beta-blockers in the presence of Niacin?

Answer 36

Additive

Question 37

What do you have to be cautious about when taking Niacin?

Answer 37

Diabetes because it elevates blood sugar

Surgery because it has anti-platelet effects