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5: Y5 - ESA 5 - Pharmacology > Cholesterol Pharmacology > Flashcards

Cholesterol Pharmacology Flashcards

1
Q

What effect does a 10% reduction in cholesterol have on CHD mortality?

A

It reduces it by 15%

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2
Q

What effect does a 10% reduction in cholesterol have in total mortality?

A

11% reduction

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3
Q

What is the primary target to prevent CHD?

A

LDL cholesterol

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4
Q

What does the intensity of cholesterol intervention depend on?

A

Total CV risk

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5
Q

What are the pro-atherogenic effects of oxidated LDL?

A
  • Inhibits macrophage motility
  • Induces T-cell activation and VSMC divison/differentiation
  • Toxic to endothelial cells
  • Enhances platelet aggregation
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6
Q

What are the classes of lipid lowering drugs?

A
  • Statins
  • Cholesterol lipase inhibitors
  • Nicotinic acid
  • Fibrates
  • Resins
  • Omega-3 fatty acids
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7
Q

Give a statin

A

Simvastatin

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8
Q

Give a cholesterol lipase inhibitor

A

Ezetimibe

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9
Q

Give a fibrate?

A

Fenofibrate

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10
Q

Give a resin

A

Colestyramine

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11
Q

Give an omega-3 fatty acid

A

Omacor

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12
Q

What are the actions of statins?

A
  • Inhibits cholesterol synthesis in hepatocytes
  • Increase clearance of IDL and LDL
  • Decreases production of VLDL and LDL
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13
Q

What are the indications for the use of statins?

A
  • CV risk prevention in CVD and diabetes
  • Famlial hypercholesterolaemia
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14
Q

What are the potential adverse drug reactions of statins?

A
  • Increased transaminase levels
  • Myopathy
  • Gastrointestinal complaints
  • Arthralgia
  • Headaches
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15
Q

What % of patients treated with statins develop increased transaminase levels?

A

0.1-2.5%

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16
Q

By how much can statins increase transaminase levels?

A

Can increase >3x the upper normal limit, especially at higher doses

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17
Q

Can increased transaminases due to statin use be reversed?

A

Yes, rapidly reversible

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18
Q

Does increased transaminase levels due to use of statins cause liver disease?

A

No

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19
Q

What myopathies can be caused by statins?

A
  • Diffuse muscle pain
  • CPK > 10x upper normal limit
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20
Q

When are myopathies due to statin use primarily seen?

A

When higher doses of statins are used in combination with cyclosporine, gemfibrozil, and occassionally erythromycin and niacin

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21
Q

What are some secondary benefits of statin treatments?

A
  • Anti-inflammatory
  • Plaque reduction
  • Improved endothelial cell functions
  • Reduced thrombotic risk
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22
Q

When is statin therapy recommended?

A

As part of the management strategy for the primary prevention of CVD for adults who have a 20% or greater risk of developing CVD

23
Q

How should the level of CVD risk a patient has be calculated?

A

Using an appropriate risk calculator, or by a clinical assessment for people whom an appropriate risk calculator is not available

24
Q

What kind of molecules are fibric acid derivatives?

A

Ampipathic carboxylic acids

25
Q

How do fibric acid derivatives act to reduce cholesterol?

A

They are PPAR-alpha agonists, which increase the production of lipoprotein lipase and so reduce triglyceride production

26
Q

By how much can fibric acid derivatives reduce cholesterol?

A

10-20%, but variable depending on specific drug

27
Q

What are the effects of fibric acids?

A
  • Increase fatty acid uptake and oxidation
  • Reduces triglyceride levels
  • Increases LDL particle size and HDL-C levels
  • Direct vascular effects
28
Q

What are the indications for fibric acid derivatives?

A
  • Hypertriglyceridema
  • Combined hyperlipidaemia with low HDL, who do not respond to NA
29
Q

Is fibric acid derivative therapy used alone, or as an adjuct?

A

It is an adjuctive therapy to diet

30
Q

What is the efficacy of fibric acid derivatives?

A
  • Decreases TG by 25-50%
  • LDL increases, but variable
  • Increases HDL 15-25% in hypertriglycaemia
31
Q

What are the side effects of fibric acid derivatives?

A
  • GI upset
  • Cholelithiasis
  • Myositis
  • Abnormal LFTs
32
Q

What are the contraindications for fibric acid derivatives?

A
  • Hepatic or renal dysfunction
  • Pre-existing gallbladder disease
    *
33
Q

What is the best agent to raise HDL-C?

A

Nicotinic acid

34
Q

What is the effect of nicotinic acid?

A
  • Reduces VLDL
  • Increases HDL at high doses

​

35
Q

How does nicotinic acid have a lipid lowering effect?

A

By inhibition of lipoprotein (a) synthesis

36
Q

What effect does nicotonic acid have on the incidence of coronary events?

A

It reduces the incidence

37
Q

What are the adverse effects of nicotinic acid?

A
  • Flushing
  • Itching
  • Headache
  • Hepatotoxicity
  • GI toxicity
  • Activation of peptic ulcer
  • Hyperglycaemia and reduced insulin sensitivity
38
Q

How can the side effects of flushing, itching and headache due to nicotinic acid be reduced?

A
  • Using immediate release Niaspan form
  • Using in combination with low dose aspirin
39
Q

What form of nicotinic acid causes hepatotoxicity and GI toxicity?

A

Sustained release

40
Q

What are the contraindications for nicotinic acid?

A
  • Active liver disease
  • Unexplained LFT elevations
  • Peptic ulcer disease
41
Q

What is the mechanism of action of ezetimibe?

A

It selectively inhibits intestinal cholesterol absorption, which;

  • Decreases intestinal delivery of cholesterol of the liver
  • Increased expression of hepatic LDL receptors
  • Decreased cholesterol content of atherogenic particles
42
Q

What do ezetimibe metabolise to?

A

An active glucuronide metabolite

43
Q

How does ezetimibe and its metabolite circulate?

A

Enterohepatically

44
Q

What is the result of the enterohepatic circulation of ezetimibe?

A

It delivers the agent back to the site of action, and limits systemic exposure

45
Q

What are the adverse drug reactions of ezetimibe?

A
  • Headache
  • Diarrhoea
  • Abdominal pain
46
Q

What can statins be used in combination with?

A
  • Fibrate
  • Nicotinic acid
  • Ezetimibe
  • Omega-3 FAs
47
Q

What should be considered when thinking about giving a patient combination therapy to reduce cholesterol?

A
  • Benefit
  • Cost
  • ADRs
48
Q

What is the advantage of combination fibrate and statin therapy?

A

It may significantly improve triglyceride, LDL-C and HDL-C levels

49
Q

What is the disadvantage of combination fibrate and statin therapy?

A

Fibrates plus statins are associated with increased risk of myopathy and rhabdomyolosis

50
Q

What effect might gemfibrozil have on statins?

A

May impair glucuronidation of statins, with cervistatin being more susceptible than other statins

51
Q

Which fibrate seems to have less potential for impairment of statin metabolism?

A

Fenofibrate

52
Q

What dietary factors may have a positive effect on statin metabolism?

A
  • Plant sterols
  • Fish oils
  • Fibre
  • Vitamin C/E
  • Alcohol (HDL)
53
Q

What dietary factors may have a negative effect on cholesterol metabolism?

A
  • Dietary cholesterol/fat
  • Alcohol (TG)

5: Y5 - ESA 5 - Pharmacology (28 decks)

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