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Pharmacology Term 6 > 7.2- Cholesterol drugs > Flashcards

7.2- Cholesterol drugs Flashcards

1
Q

Describe the infiltration and entrapment of LDL in the arterial wall

A
  • LDL enters endothelium–> gets OXIDISED,enabling it to:
  • inhibits macrophage motility
  • Induces T-cell activation and VSMC division/differentiation
  • Toxic to endothelial cells
  • Enhances platelet aggregation
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2
Q

State the 4 main classes of lipid lowering drugs

A
  • Statins e.g. Simvastatin
  • Cholesterol lipase inhibitors e.g. Ezetimibe
  • Nicotinic acid/niacin
  • Fibrates e.g. Fenofibrate
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3
Q

What are the indications for the use of statins?

A
  • CV risk prevention (CVD+DM)
  • Familial hypercholesterolaemia
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4
Q

Describe the mechanism of action of statins

A
  • Inhibits HMG-CoA reducatase in the pathway to cholesterol synthesis from Acetyl-Co-A
  • Thereore inhibits choleserol synthesis in hepatocytes
  • Increases clearance of LDL and IDL ( by increased synthesis of LDL receptor)
  • Decreases production of VLDL and LDL
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5
Q

Give 3 adverse drug reactions of statins

A
  1. Inreased transaminsase levels ( sign of liver damage)
  2. Myopathy
  3. Miscellaneous; GI complaints, anthralgias, headaches and memory loss
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6
Q

What is seen in Myopathy resulting as a statin ADR?

A
  • Diffuse muscle pain
  • CK> 10 x upper normal limit
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7
Q

With which statin drug combos is a myopathy seen?

A
  • Seen when HIGHER doses of statins are used in combination with
  • Cyclosporine

Erythromycin and niacin

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8
Q

What are some secondary benefits of statin treatment? ( APIR)

A
  • Anti-inflammatory
  • Plaque reduction
  • Improved endothelial cell function
  • Reduced thrombotic risk
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9
Q

What statin therapy is recommended as part of primary prevention of CVD in adults w a high QRISK2?

A

Atorvastatin 20mg

If high 10-year risk of developing CVD

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10
Q

How are statins used as part of secondary prevention?

A

Atorvastatin 80 mg

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11
Q

How is the level of CVD risk calculated?

A

using the QRISK2 risk calculator

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12
Q

What is the statin of choice?

A

Atorvastatin

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13
Q

What are are Fibric Acid Derivatives?

A
  • Ampipathic carboxylic acids
  • PPARalpha receptors agonist; increases production of lipoprotein lipase
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14
Q

Describe the mechanism of action of fibric acid derivatives

A
  • PPARalpha receptor agonist; increases production of lipoprotein lipase
  • Increases FA uptake and oxidation
  • Reduces triglyceride levels
  • Increases LDL particle size and HDL-C levels

Direct vascular effects

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15
Q

Name 3 indications for the use of FDA’s

A

Adjunctive therapy to diet

Hypertriglyceridaemia

Combined hyperliidemia with low HDL who not respond to NA

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16
Q

Describe the efficacy of FDA’s

A

Decreases trigyleride by up to 50%

LDL decreases but variably

Increases HDL up to 35% in Hypertriglyceridemia

17
Q

Name 4 side effects of FDA

A
  • GI upset
  • Cholelithiasis
  • Myositis
  • Abnormal LFT’s
18
Q

Name 2 contraindications for the use of FDA’s

A
  • Hepatic or renal dysfunction
  • Pre-existing gallbladder disease
19
Q

Describe the mechanism of action of nicotinic acid derivatives/ niacin?

A
  • Raises HDL cholesterol
  • INHIBITS lipoprotein-A synthesis —> lipid lowering effect
  • reduces coronary events
20
Q

Name 4 adverse effects of nicotinic acid ( niacin)

A

Hepatotoxicity, GI

Activation of peptic ulcer

Hyperglycemia and reduced insulin sensitivity

Flushing, itching, headache

21
Q

Name 2 contraindications for the use of Nicotinic acid

A

Peptic ulcer disease

Activ liver disease or unexplained LFT elevations

22
Q

Give an example of a cholesterol lipase inhibitor

A

EZETIMIBE

23
Q

How does Ezetimibe work?

A

selectively inhibits intestinal cholesterol absorption, therefore causing

  • DECREASED intestinal delivery of cholesterol to the liver
  • INCREASED expression of hepatic LDL receptors
  • DECREASED cholesterol content of atherogenic particles
24
Q

Describe the PK of ezetimibe

A

Ezetimibe and its active glucoronide metabolite circulate enterophepatically

  • delivers agent back to the site of action
  • therefore limits systemic exposure
25
Q

Give 3 ADR’s of ezetimibe

A

Headache

Abdominal Pain

Diarrhoea

26
Q

What drugs are given as part of combination therapy?

A

Statin plus any one of the following:

Fibrate ( not gemfibrozil

Nicotinic acid

Ezetimibe

omega-3 FA’s

27
Q

What 3 factors are considered when choosing drugs for combo therapy?

A

Benefit ( CV risk reduction)

Cost

ADRs

28
Q

Why are fibrates NOT used with statins?

A

Increased risk for myopathy and rhabdomyolysis

GEMFIBROZIL ( fibrate) may impair glucoronidation of statins

29
Q

Name 4 POSITIVE dietary factors for cholesterol

and 3 negative ones

A

Positive factors:

  • Fish oils
  • Fibre
  • Vitamin C/E
  • Alcohol (HDL)

Negative factors:

  • Dietary cholesterol/fat
  • Sugar
  • Alcohol (TG)

Pharmacology Term 6 (10 decks)

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