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Yr 2 Sem 2 CPT > 3.2 Cholesterol Pharmacology > Flashcards

3.2 Cholesterol Pharmacology Flashcards

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1
Q

What is the relationship between cholesterol and CHD risk?

A

Positive

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2
Q

What is the primary target to prevent CHD?

A

LDL cholesterol

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3
Q

What are the pro-atherogenic effects of Ox-LDL?

A

Inhibits macrophage motility
Induces T cell activation and VSMC division
Toxic to endothelial cells
Enhances platelet aggregation

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4
Q

Effect of obesity on cholesterol, triglycerides and HDL cholesterol

A

Cholesterol and triglycerides increase

HDL cholesterol decrease

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5
Q

What do statins do?

A

Inhibit cholesterol synthesis in hepatocytes
Increase clearance of IDL and LDL
Decrease production of VLDL and LDL

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6
Q

What enzyme do statins block?

A

HMG-CoA reductase

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7
Q

What are the indications for statins?

A

CV risk prevention

Familial hypercholesterolaemia

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8
Q

What is a mechanism of action of statins?

A

Increased synthesis of LDL receptor

Decreases serum cholesterol

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9
Q

What are some ADRs of statins?

A

Liver function - Increased transaminase levels

Muscle - Myopathy, diffuse muscle pain
Can sometimes have elevated CK can lead to rhabdomyolysis
Seen when statins used in higher doses and in combination with cyclosporin, gemfibrozil and erythromycin and niacin

GI complaints, arthralgias and headaches

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10
Q

What are some secondary benefits of statin treatment?

A

Anti-inflammatory
Plaque reduction
Improved endothelial cell function
Reduced thrombotic risk

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11
Q

What is a problem with cerivastatin?

A

Its structure caused drug-drug interaction

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12
Q

What is the receptor that fibrates act on?

A

Peroxisome Proliferator-Activated Receptor agonist

Increases production of lipoprotein lipase

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13
Q

What do fibrates do?

A

Reduces triglyceride production

Some reduction in LDL, may increase HDL

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14
Q

What is the mechanism of action of fibrates?

A

Increases fatty acid uptake and oxidation
Reduces triglyceride levels
Increases LDL particle size and HDL-C levels
Direct vascular effects

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15
Q

What are the indications for fibrates?

A

Adjunctive therapy to diet

Hypertriglyceridmia

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16
Q

Side effects of fibrates?

A

GI upset, cholelithiasis, myositis

Abnormal liver function test

17
Q

Contraindications of fibrates?

A

Hepatic of renal dysfunction

Pre-existing gall bladder disease

18
Q

What does nicotinic acid do?

A

Reduces VLDL
Increases HDL
Reduces coronary events

19
Q

How does nicotinic acid exert its lipid lowering effects?

A

Inhibition of lipoprotein a synthesis

20
Q

Adverse effects of nicotinic acid

A

Flushing, itching and headache
Hepatotoxicity, GI
Activation of peptic ulcer
Hyperglycaemia and reduced insulin sensitivity

21
Q

Contraindications for nicotinic acid

A

Active liver disease or unexplained raised LFTs

Peptic ulcer disease

22
Q

What type of drug is ezetimibe?

A

Cholesterol lipase inhibitor

23
Q

What is the main mechanism of action of ezetimibe?

A

Selectively inhibits intestinal cholesterol absorption

Decreases intestinal delivery of cholesterol to liver
Increase expression of hepatic LDL receptors (so remove more LDL cholesterol)
Decrease cholesterol content of atherogenic particles

24
Q

Why does ezetimibe have less adverse side effects?

A

Ezetimibe and active metabolite circulate enterohepatically
Delivers agents back to site of action
Limits systemic exposure

25
Q

What are some ADRs for ezetimibe?

A

Headache
Abdominal pain
Diarrhoea

26
Q

What is a problem with combination statin and fibrate therapy?

A

Increased risk for myopathy and rhabdomyolysis

Fibrates may impair statin metabolism so higher concentrations of statins in blood can lead to more side effects

27
Q

What is a new type of lipid lowering drug?

A

PCSK9 inhibitors - monoclonal antibodies

Stops LDL receptors from being internalised

28
Q

What could someone who didn’t want to take drugs do to lower lipids?

A

Plant sterols

Positive: Fish oils, fibre, vit C and E, alcohol (HDL)

Negative: Dietary cholesterol and fat, alcohol (TG)

29
Q

What should be given to all people that have had an MI?

A

Statin

30
Q

How can cardiovascular risk be calculated?

A

Internet calculator eg Qrisk2

31
Q

What are some lifestyle changes for prevention of CVD?

A 
Cardioprotective diet
Physical activity 
Weight management 
Alcohol consumption 
Smoking cessation
32
Q

What drug is usually prescribed for primary prevention of CVD?

A

Atorvastatin

Yr 2 Sem 2 CPT (9 decks)

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