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5 - Pharmacology > Cholesterol lowering drugs > Flashcards

Cholesterol lowering drugs Flashcards

1
Q

Describe an atheroma

A

Fatty deposits in the tunica intima covered by a fibrous cap

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2
Q

What effects of oxidised LDLs have?

A

Inhibits macrophage motilityInduces T-cell activation Induces vascular smooth muscle cells divisions and differentiationIt is toxic to endothelial cellsEnhances platelet aggregation

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3
Q

Describe the effects of different types of lipids

A

HDLs - reduces CHD riskLDLs - links to coronary atherosclerosis

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4
Q

What are the different types of drugs which can be used to lower levels of lipids?

A

StatinsCholesterol absorption inhibtorsFibratesNiacinBile acid sequestrants

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5
Q

Describe the transport function of chylomicrons

A

Dietary TAGs from intestine to the tissues (adipose)

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6
Q

Describe the transport function of VLDLs

A

Dietary TAGs synthesised in the liver to adipose for storage

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7
Q

Describe the transport function of LDLs

A

Cholesterol synthesised in the liver to the tissues

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8
Q

Describe the transport function of HDLs

A

Excess tissue cholesterol to the liver so its can be disposed as biles salts

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9
Q

Which of the lipoproteins causes the worst clinical effects?

A

LDLs

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10
Q

Which is the most commonly used lipid lowering drug and why/

A

Statins- cheap- best tolerated for lowering LDLs- is very effective

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11
Q

What is the primary physiological action of statins?

A

Inhibits hepatic HMG CoA Reductase- involved in cholesterol synthesis

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12
Q

What happens when the hepatic cholesterol concentration decreases?

A

This stimulates LDL receptor production which increase the rate of removal of LDLs from the plasma

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13
Q

Describe simvastatin

A

Has a short half lifeMost commonly used statinGiven at night so have highest conc at time when cholesterol production is greatest

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14
Q

Describe atorvastatin

A

Half life = 20 hoursHas a superior efficacy to simvastatin

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15
Q

Describe rostuvastatin

A

Contains sulphurIs more potent than simvastatinHalf life = 20 hours

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16
Q

What is the indication for prescription for statins?

A

Hyperlipidaemia which has not responded to changes in diet or exercise

17
Q

When would you not give a statin?

A

Pregnant womenBreastfeeding womenPt with liver disease

18
Q

Give some adverse drug reactions which occur with statins

A

Increase transaminase levelsMyopathyGI disturbancesArthralgiaHeadaches

19
Q

Describe myopathy and when would you get it

A

Diffuse muscle pain- when combining statin use with cyclosporin, erythromycin, niacin- can test levels of creatinine kinase to confirm presence of myopathy

20
Q

What is the mechanism of action of fibrates?

A

Act as agonists on the Peroxisome Proliferator-Activated Receptor-α (PPAR-α).

21
Q

What actions do fibrates have?

A
  • LDL lowering (variable amount)- HDL increases of 15-25% in hypertriglyceridemia- Decreases Triglycerides 25-50%
22
Q

When would you prescribe fibrates?

A

Used as first line choice in hypertriglyceridemia

23
Q

Give some examples of fibrates

A

BezafibrateCiprofibrateGemfibrozil

24
Q

When would you not use fibrates?

A

PregnancyBreast feedingGall bladder diseaseSevere renal of hepatic impairmentHypoalbuminaemia

25
Q

What are some ADRs which occur with fibrates?

A

GI disturbancesDermatitisPruritisRashImpotenceHeadacheDizzinessBlurred vision

26
Q

Describe cholesterol absorption inhibitors

A

Inhibit cholesterol uptake by blocking NPC1L1 (cholesterol transport uptake protein) in the brush border. This decrease the hepatic cholesterol concentration.

27
Q

Give an example of a cholesterol uptake inhibitor

A

Ezetimibe

28
Q

What kind of effect does a dose of ezetimibe have?

A

A single 10mg dose reduces LDL levels by 15-20%.

29
Q

When would you use ezetimibe?

A

In statin intolerant patients- can give with a statin to reduce LDL levels by 40% and to reduce the side effects of statins

30
Q

What are some adverse drug reactions for cholesterol uptake inhibitors?

A

GI disturbances- diarrhoea- painHeadache

31
Q

Describe the mechanism of action of bile acid sequestrants

A

Bind to bile acids in the intestine and prevent their reabsorption which means that there will be lower cholesterol levels as bile acids are produced from cholesterol.

32
Q

Give some ADRs for bile acids sequestrants

A

GI disturbances- nausea- vomiting- constipation- abdominal pain- flatulence- heart burn

33
Q

When would you not use bile acid sequestrants?

A

Biliary obstruction

34
Q

Give the mechanism of action of niacin

A

Inhibits lipoprotein-a synthesis

35
Q

What are the effects of niacin?

A

Increases HDL levels- decreases risk of cardiovascular events

36
Q

Give some side effects of niacin

A

Skin flushingItchingDry skinEczema exacerbationsAcanthosis nigricans

5 - Pharmacology (17 decks)

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