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Flashcards in Statins Deck (20):
1

What are statins?

Drug used to prevent coronary heart disease by improving the lipid profile of at risk patients.

Reversibly inhibitors of the hepatic enzyme HMG-CoA reductase.

2

Name 4 commonly used statins.

1. Atorvastatin
2. Simvastatin
3. Pravastatin
4. Rosuvastatin

3

How do statins work?

They prevent acetyl-CoA from forming Mevalonate, which would normally form cholesterol. SO they lower cholesterol levels.

Also:
- anti-inflam
- improve endothelial cell function
- plaque stability
- prevent thrombus formation

4

Are statins absorbed well?

Yes orally.

5

When do statins reach Cmax?

1-2 hours

6

When are therapeutic effects observed?

Within 1-2 weeks

7

What are a few dose-response issues with statins?

- plasma concentrations vary widely across individuals but therapeutic efficacy appears weakly related to plasma statin levels
- statins produce sigmoidal curve so dose above IC50 results in minor changes
- side effects increased with increased dose.

8

Of the 3 main statins, which is hydrophilic and which is lipophilic?

Atorvastatin - lipophilic
Simvastatin - lipophilic
Pravastatin - hydrophilic

9

Of the 3 main statins, which passively diffuses and which is actively pumped?

Atorvastatin - passive diff
Simvastatin - passive diff
Pravastatin - actively pumped

10

Of the 3 main statins, which is a prodrug that is metabolised in the liver to the active B-hydroxy FA form?

Simvastatin

11

Of the 3 main statins, which lowers the risk of myopathies and has a longer half life of 77 hours (yet lower protein binding profile)?

Pravastatin

12

Of the 3 main statins, which is a more potent lipid-lowering drug of the first generation of statins?

Atorvastatin

13

Which enzymes are involved in statin metabolism?

CYP3A4 and 2A9.

14

CYP inhibitors can cause what?

Elevated levels of statin and toxicity.

15

What is the effect of grapefruit juice on CYP3A4?

It is an inhibitor of the enzyme.

16

What enzyme polymorphisms can effect statin metabolism?

CYP2D6

17

What type of prevention is simvastatin?

secondary prevention

18

What relationship is there between LDL-cholesterol and frequency of CHD events?

Linear relationship.

19

What adverse effects are associated with statins?

Hepatotoxicty
Myositis
Angio-oedema
Dementia

20

What are other clinical uses of statins?

- prevents osteoporosis
- prevents alzheimer's
- anti-inflammatory
- lowers BP
- reduced DVT and stroke
- reduced bowel cancer