W4, 5 Control dyslipidemia (pharma)

Question 1

Importance of cholesterol

Answer 1

Cholesterol is a necessary component of cell membranes and is a precursor of steroid hormones.

Question 2

From where we get cholesterol

Answer 2

Cholesterol is derived from both exogenous (dietary)
and endogenous (synthesized in the liver) sources.

Question 3

Four major types of lipoproteins:

Answer 3

Question 4

Lipids including cholesterol and triglycerides are transported in the plasma as ………….

Answer 4

lipoproteins

Question 5

Dyslipidemias can be classified into:

Answer 5

1. Hypercholesterolemia
2. Hypertriglyceridemia
3. Mixed (i.e. hypercholesterolemia and hypertriglyceridemia).

Question 6

What are THERAPEUTIC STRATEGIES of dyslipidemia

Answer 6

Question 7

What is Dyslipidemia/ Hyperlipidemia

Answer 7

Question 8

How does treatment of dyslipidemia work?

Answer 8

Question 9

Main types of Lipid Lowering Drugs:

Answer 9

1. Statins
2. Fibrates
3. Inhibitors of Cholesterol absorption (Resins and Ezetimibe)
4. Nicotinic acid
5. Omega-3-fatty acids
6. PCSK9 Inhibitors

Question 10

Statins drug examples

Answer 10

Statins eg lovastatin, Atorvastatin

Question 11

MOA of statins

Answer 11

Question 12

Other actions of statins unrelated to its actions on lipids:

Answer 12

Question 13

Mean half-life in the plasma of statins is

Answer 13

14 hours

Question 14

Half-life of inhibitory activity for HMG-CoA reductase is …. hours & why?

Answer 14

20 to 30 hours due to the contribution of active metabolites

Question 15

Uses of statins

Answer 15

Question 16

Adverse effects of statins

Answer 16

• Long treatment may cause a rise in serum levels of the liver
enzyme, transaminase.
• Other adverse effects include myopathy and ocular damage
(cataract)

Question 17

Fibrates drug exampls

Answer 17

Fibrates e.g. Clofibrate, gemfibrozil

Question 18

Mechanism of Action of fibrates

Answer 18

Question 19

Pharmacokinetics of fibrates
a. Route of administration
b. Half life
c. Metabolism & excretion

Answer 19

Question 20

Uses of fibrates

Answer 20

• Clofibrate is used to treat hyperlipidemias of various etiologies in
which there is an increase in VLDL levels.
• It has mild antidiuretic action in individuals with mild or moderate
diabetes insipidus (ADH not produced in diabetes insipidus = increased urine production)

Question 21

Adverse effects of fibrates

Answer 21

Question 22

What DRUGS AFFECT PLASMA CHOLESTEROL? What’s their MOA?

Answer 22

Question 23

What are the uses of these drugs?

Answer 23

• Treatment of hyperlipidemias.
• Cholestyramine is the drug of choice for hypercholesterolemia.

Question 24

What’s their Adverse effects:

Answer 24

• Quite safe, because not absorbed in the intestine.
• Abdominal pain, constipation, nausea.
• Interfere with absorption of some drugs like warfarin and digitalis

Question 25

What drugs inhibit Cholesterol Absorption

Answer 25

Ezetimibe, resins

Question 26

Which is more potent? Ezetimibe or resins?

Answer 26

Ezetimibe

Question 27

MOA of Ezetimibe?

Answer 27

Inhibits intestinal absorption of cholesterol, specifically in the brush border of enterocytes in the duodenum.

Question 28

Adverse effects of ezetimibe

Answer 28

- Well tolerated, may cause fatigue, abdominal pain, diarrhea.

Question 29

MOA of Nicotinic Acid (Niacin)

Answer 29

Question 30

Therapeutic Uses of Nicotinic Acid:

Answer 30

- Treatment of combined hyperlipidemia. - Most effective agent for increasing HDL.

Question 31

Adverse effects of Nicotinic Acid:

Answer 31

- Weight gain due to inhibition of lipolysis - Hyperuricemia precipitates gout, intense cutaneous flush, nausea, abdominal pain, hyperglycemia, jaundice

Question 32

MOA of Probucol?

Answer 32

Question 33

Uses of probucol:

Answer 33

Question 34

Adverse effects of probucol:

Answer 34

• Adverse effects are usually mild and of short duration. • They include nausea, diarrhea, flatulence, abdominal pain, Nausea, Vomiting.

Question 35

Omega-3-fatty acids MOA in dyslipidemia

Answer 35

• Used for triglyceride (TG) lowering. • Inhibit VLDL and TG synthesis in the liver.

Question 36

Omega 3 fatty acids sources

Answer 36

Found in marine sources & available as over-the–counter fish oil capsules.

Question 37

Uses of omega 3 FA

Answer 37

Can be used as adjunct to other lipid-lowering therapies for individuals with elevated TG.

Question 38

Common side effects of omega 3 FA

Answer 38

GI effects (nausea & vomiting) & a fishy aftertaste.

Question 39

First-line drug for patients at high risk of myocardial infarction due to hypercholesterolemia.

Answer 39

Statins

Question 40

Most effective agent for increasing HDL.

Answer 40

Nicotinic Acid

Question 41

drug of choice for hypercholesterolemia.

Answer 41

Cholestyramine

Question 42

What drugs are agonists at the α peroxisomal-proliferator activator receptors (PPARα), which are nuclear transcription factors?

Answer 42

Fibrates

Question 43

used to treat hyperlipidemias of various etiologies in which there is an increase in VLDL levels & has mild antidiuretic action

Answer 43

Clofibrate

Question 44

This drug can’t be given to a patient with diabetes

Answer 44

Nicotinic Acid

Question 45

Miscellaneous Drugs (slide)

Answer 45

Question 46

Treatment of primary hypercholesterolemia associated with elevated LDL

Answer 46

probucol

Question 47

Mcq: 1. What is given to a patient with high risk of MI due to hypercholesteremia?/ What is the suggestive prevention for a patient at risk of myocardial infarction because of his hypercholesterolemia? A. Statins B. Resin C. Fibrates

Answer 47

A. Statins

Question 48

Mcq: Which drug inhibits HMG coA reductase?

Answer 48

Statins

Question 49

Mcq: What is the MOA of clofibrate? A. PPAR Alpha / increase LPL activity B.PCSK9 C. Inhibits cholesterol absorption in GI

Answer 49

A. PPAR Alpha / increase LPL activity

Question 50

Mcq: Which drug causes myopathy as an adverse effect? A. Lovastatin B. Clofibrate

Answer 50

A. Lovastatin

Question 51

Mcq: A drug that causes elevated liver enzymes as a side effect?

Answer 51

A. Lovastatin Note (they also mention that it is a statin in Q)

Question 52

Mcq: What is the suggestive prevention for a patient at risk of myocardial infarction because of his hypercholesterolemia? A. Aspirin B. Lovastatin

Answer 52

Lovastatin

Question 53

Mcq: Which drug affects PPAR-a?

Answer 53

A. Clofibrate

Question 54

Mcq: Which of the following drugs inhibit lipolysis?

Answer 54

A. Clofibrate

Question 55

Mcq: Weight gain when using Clofibrate is due to? A. Inhibiting Lipolysis B. Activating lipolysis

Answer 55

A. Inhibiting Lipolysis

Question 56

Mcq: Which of the following decrease bile acid salt absorption in the intestine? A. Simvastatin B. Clofibrate C. Cholestyramine D. Nicotinic Acid

Answer 56

C. Cholestyramine

Question 57

Mcq: Consequences of using a drug that prevent absorption of cholesterol into gastrointestinal tract like Cholestyramine?

Answer 57

A. Increase the density of LDL receptors

Question 58

Mcq: What is the best drug for increasing HDL levels?

Answer 58

A. Nicotinic Acid

Question 59

Mcq: What is the mechanism of weight gain in a patient receiving nicotinic acid?

Answer 59

A. Inhibition of lipolysis in lipid tissue

Question 60

Mcq: Which of the following may be an adverse effect of Nicotinic acid? A. Gout due to hyperuricemia B. Weight loss C. Myalgia D. Arthralgia

Answer 60

A. Gout due to hyperuricemia

Question 61

Mcq: Which of the following drugs complex with bile salts to prevent their reabsorption?/ which of the following drugs prevents the absorption of bile acids by intestine by forming insoluble complex with bile acid salt? A. Colestipol B. Ezetimibe C. Niacin

Answer 61

A. Colestipol

Question 62

Mcq: What is the mechanism of action of lovastatin? A. Decrease the LDL in the blood B. Increase the LDL in the blood

Answer 62

A. Decrease the LDL in the blood

Question 63

Mcq: What is the mechanism of action of clofibrate? A. PPAR alpha agonist B. PPAR gamma agonist C. PPAR gamma antagonist D. HMG CoA reductase inhibitors

Answer 63

A. PPAR alpha agonist