W4, 5 Control dyslipidemia (pharma) Flashcards

1
Q

Importance of cholesterol

A

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

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2
Q

From where we get cholesterol

A

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

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3
Q

Four major types of lipoproteins:

A
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4
Q

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

A

lipoproteins

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5
Q

Dyslipidemias can be classified into:

A
  1. Hypercholesterolemia
  2. Hypertriglyceridemia
  3. Mixed (i.e. hypercholesterolemia and hypertriglyceridemia).
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6
Q

What are THERAPEUTIC STRATEGIES of dyslipidemia

A
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7
Q

What is Dyslipidemia/ Hyperlipidemia

A
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8
Q

How does treatment of dyslipidemia work?

A
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9
Q

Main types of Lipid Lowering Drugs:

A
  1. Statins
  2. Fibrates
  3. Inhibitors of Cholesterol absorption (Resins and Ezetimibe)
  4. Nicotinic acid
  5. Omega-3-fatty acids
  6. PCSK9 Inhibitors
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10
Q

Statins drug examples

A

Statins eg lovastatin, Atorvastatin

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11
Q

MOA of statins

A
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12
Q

Other actions of statins unrelated to its actions on lipids:

A
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13
Q

Mean half-life in the plasma of statins is

A

14 hours

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14
Q

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

A

20 to 30 hours due to the contribution of active metabolites

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15
Q

Uses of statins

A
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16
Q

Adverse effects of statins

A

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

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17
Q

Fibrates drug exampls

A

Fibrates e.g. Clofibrate, gemfibrozil

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18
Q

Mechanism of Action of fibrates

A
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19
Q

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

A
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20
Q

Uses of fibrates

A

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

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21
Q

Adverse effects of fibrates

A
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22
Q

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

A
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23
Q

What are the uses of these drugs?

A

β€’ Treatment of hyperlipidemias.
β€’ Cholestyramine is the drug of choice for hypercholesterolemia.

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24
Q

What’s their Adverse effects:

A
  • Quite safe, because not absorbed in the intestine.
  • Abdominal pain, constipation, nausea.
  • Interfere with absorption of some drugs like warfarin and digitalis
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25
Q

What drugs inhibit Cholesterol Absorption

A

Ezetimibe, resins

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26
Q

Which is more potent? Ezetimibe or resins?

A

Ezetimibe

27
Q

MOA of Ezetimibe?

A

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

28
Q

Adverse effects of ezetimibe

A
  • Well tolerated, may cause fatigue, abdominal pain, diarrhea.
29
Q

MOA of Nicotinic Acid (Niacin)

A
30
Q

Therapeutic Uses of Nicotinic Acid:

A
  • Treatment of combined hyperlipidemia.
  • Most effective agent for increasing HDL.
31
Q

Adverse effects of Nicotinic Acid:

A
  • Weight gain due to inhibition of lipolysis
  • Hyperuricemia precipitates gout, intense cutaneous flush, nausea, abdominal pain, hyperglycemia, jaundice
32
Q

MOA of Probucol?

A
33
Q

Uses of probucol:

A
34
Q

Adverse effects of probucol:

A

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

35
Q

Omega-3-fatty acids MOA in dyslipidemia

A

β€’ Used for triglyceride (TG) lowering.
β€’ Inhibit VLDL and TG synthesis in the liver.

36
Q

Omega 3 fatty acids sources

A

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

37
Q

Uses of omega 3 FA

A

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

38
Q

Common side effects of omega 3 FA

A

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

39
Q

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

A

Statins

40
Q

Most effective agent for increasing HDL.

A

Nicotinic Acid

41
Q

drug of choice for hypercholesterolemia.

A

Cholestyramine

42
Q

What drugs are agonists at the Ξ± peroxisomal-proliferator activator receptors (PPARΞ±), which are nuclear transcription factors?

A

Fibrates

43
Q

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

A

Clofibrate

44
Q

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

A

Nicotinic Acid

45
Q

Miscellaneous Drugs (slide)

A
46
Q

Treatment of primary hypercholesterolemia associated with elevated LDL

A

probucol

47
Q

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

A

A. Statins

48
Q

Mcq: Which drug inhibits HMG coA reductase?

A

Statins

49
Q

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

A

A. PPAR Alpha / increase LPL activity

50
Q

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

A

A. Lovastatin

51
Q

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

A

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

52
Q

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

A

Lovastatin

53
Q

Mcq: Which drug affects PPAR-a?

A

A. Clofibrate

54
Q

Mcq: Which of the following drugs inhibit lipolysis?

A

A. Clofibrate

55
Q

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

A

A. Inhibiting Lipolysis

56
Q

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

A

C. Cholestyramine

57
Q

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

A

A. Increase the density of LDL receptors

58
Q

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

A

A. Nicotinic Acid

59
Q

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

A

A. Inhibition of lipolysis in lipid tissue

60
Q

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

A

A. Gout due to hyperuricemia

61
Q

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

A

A. Colestipol

62
Q

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

A

A. Decrease the LDL in the blood

63
Q

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

A

A. PPAR alpha agonist