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Flashcards in Cholesterol Drugs Deck (25)
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1
Q

What are some examples of Statin drugs?

A
  • Simvastatin

* Atorvastatin

2
Q

What is the effect of statin on the cholesterol synthesis and lipoproteins?

A
  • Inhibit cholesterol synthesis
  • Increase clearance of IDL and LDL
  • Decrease production of VLDL and LDL so less in serum
3
Q

What is the mechanism of action demonstrated by Statins?

A
  • Antagonising HMG-CoA reductase

- Increase in synthesis of LDL receptor

4
Q

What are the uses of Statins?

A
  • Cardiovascular risk prevention

* Familial hypercholesterolemia

5
Q

What are the side effects of Statins?

A
  • Increased transaminase levels (reversible)
  • Myopathy resulting in muscle pain.
  • Increase in creatinine phosphokinase levels with higher dose
  • GI complaints
  • Arthralgia
  • Headaches
6
Q

What are some examples of cholesterol lipase inhibitors?

A

•Ezetimibe

7
Q

What are the effects of ezetimibe on cholesterol?

A

Selectively inhibits intestinal cholesterol absorption

  • Decreased intestinal delivery of cholesterol to the liver
  • Increased expression of hepatic LDL receptor
  • Decreased cholesterol content of atherogenic particles
8
Q

What are the uses of cholesterol lipase inhibitors?

A

-Cardiovascular risk prevention

9
Q

What are the side effects of Ezetimibe?

A
  • Headache
  • Abdominal pain
  • Diarrhoea
10
Q

What are the classes of cholesterol drugs?

A
  • Statin
  • Cholesterol lipase inhibitors
  • Nicotinic Acid
  • Fibrates
11
Q

What are the effect of nicotinic acids on cholesterol?

A
  • Reduce VLDL

* Increases HDL at high doses. Best agent to raise HDL-C

12
Q

What is the mechanism of action of nicotinic acids?

A

•Lipid lowering by inhibition of lipoprotein synthesis

13
Q

What are the uses of Nicotinic acid?

A

-Reduces coronary events

14
Q

What are the side effects of Nicotinic acids?

A
  • Flushing, Itching, Headache
  • Hepatoxicity, GI
  • Activation of peptic ulcer
  • Hyperglycaemia and reduced insulin sensitivity
15
Q

What are the contraindications of nicotinic acids?

A
  • Peptic ulcer disease

- Active liver disease or unexplained LFT elevations

16
Q

What are effects of fibrates on cholesterol?

A

PPAR-alpha agonist which increases production of lipoprotein lipase

  • Reduces triglyceride production
  • Some reduction in LDL but variable
17
Q

What is the mechanism of action of Fibrates?

A
  • Increase in fatty acid uptake and oxidation
  • Increase LDL particle size and HDL-C levels
  • Direct vascular effects
18
Q

What are some key messages about combination therapies to lower cholesterol?

A

Statins are used in combination with:

  • Fibrate
  • Nicotinic Acid
  • Ezetimibe
  • Omega-3 Fatty acids
  • Resins
19
Q

What are some risk of using fibrates and statins?

A
  • Increased risk of myopathy and rhabdomyolysis
  • Gemfibrozil in particular may impair glucorinidation of statins.
  • Fenofibrate appears to have less potential for impairment of statin metabolism and thus this may account for the reduced reports
20
Q

What are examples of fibrates?

A
  • Fenofibrate
  • Bezafibrate
  • Gemfibrozil
21
Q

How is Ezetimibe delivered?

A

Ezetimibe and its active glucuronide circulate entero-hepatically

  • Delivers agents back to the site of action
  • Limited systemic exposure
22
Q

When are fibrates used?

A
  • Adjunctive therapy to diet
  • Hypertriglyceridemia
  • Combined hyperlipidaemia with low HDL who do not respond to NA
23
Q

What are some side effects of fibrates?

A
  • GI upset
  • Cholelithiasis
  • Myositis
  • Abnormal LFTs
24
Q

What are some contraindications to consider when using fibrates?

A
  • Hepatic or renal dysfunction

* Pre-existing gallbladder disease

25
Q

What are secondary benefits of statin?

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