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Pharmacology > Hyperlipidaemias > Flashcards

Hyperlipidaemias Flashcards

1
Q

What is the mechanism of action for statins?

A

Competitive inhibition of HMG-CoA reductase

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2
Q

Statins cause an upregulation of what type of receptor?

A

Hepatic LDL receptor to increase clearance of circulating LDL

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3
Q

Name the two statins we have covered

A

Atorvastatin

Simvastatin

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4
Q

What is the half life of the active derivatives of Atorvastatin?

A

> 30hrs

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5
Q

Which statin is a prodrug activated by first pass metabolism?

A

Simvastatin

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6
Q

What is the half life of simvastatin?

A

2 hrs

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7
Q

What are the side effects associated with statins?

A 
GI disruption
Nausea
Headache
Myalgia
Rhabdomyolysis
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8
Q

When are statins contraindicated?

A

Renal impairment
Breast feeding
Pregnant

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9
Q

Which CYP450 is important when considering statins?

A

CYP3A4

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10
Q

If the patient required other drugs that interacted with the CYP450, then the statins would have to be temporarily withheld. What drugs does this apply to?

A

Amiodarone
Diltiazem
Macrolides
Amlodipine

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11
Q

How do statins improve vascular endothelial function?

A

Increase NO and VEGF

Decrease endothelin

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12
Q

How do statins improve plaque stability?

A

Increased collagen

Decreased smooth muscle cell proliferation

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13
Q

Statins have antioxidant effects, they prevent the formation of what?

A

Superoxide

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14
Q

When in the day should statins be taken?

A

At night due to the circadian rhythm of the LDL receptor synthesis and activity.

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15
Q

What is fenofibrate?

A

A fibric acid derivative

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16
Q

Fenofibrate activates which nuclear transcription factor?

A

PPARa

17
Q

PPARa regulates the expression of genes that control lipoprotein metabolism, the production of which enzyme gets upregulated as a result?

A

Lipoprotein lipase

18
Q

What are the warnings and contraindications associated with fenofibrate?

A

Gallbladder disease
Pancreatitis
Cholilithiasis
Myositis

19
Q

Fenofibrate does what to warfarin?

A

Potentiates it so there is an increased chance of bleeding.

20
Q

What is Alirocumab?

A

PCSK9 inhibitor

21
Q

What is the mechanism of action for Alirocumab?

A

PCSK9 normally binds internalised LDL receptors.

So the drug prevents the internalisation of the receptor.

22
Q

What is Ezetimibe?

A

Cholesterol absorption inhibitor

23
Q

Ezetimibe inhibits what?

A

NPC1L1 transporter in the small intestine, reducing gut absorption of cholesterol by 50%
And hepatic LDL receptor expression increases

24
Q

Is Ezetimibe a pro drug?

A

Yes

25
Q

In familial hypercholesterolaemia, what would be prescribed?

A

Statins and Ezetimibe as an adjunct.

26
Q

What is the dose of Ezetimibe?

A

10mg

It has no dose escalation

Pharmacology (11 decks)

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