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PHA321 > Antilipidaemics > Flashcards

Antilipidaemics Flashcards

1
Q

Classes of antilipidaemics

A

Statins
Bile acid sequestrants
Fibrates
Nicotinic acid
Ezetimibe
PCSK9 inhibitors
Omega 3 fatty acids
Lomitapide
Mipomersen

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2
Q

Effects of statins on TG, LDL, HDL

A
  • Significant LDL lowering and total cholesterol lowering effects
  • Modest triglyceride lowering
  • Modest HDL raising effect
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3
Q

Examples of statins based on potency

A
  • High potency - Rosuvastatin, Artovastatin
  • Intermediate potency - Simvastatin
  • Low potency - Pravastatin, Lovastatin, Fluvastatin
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4
Q

Statins MOA

A

Statins act in the liver to inhibit HMG CoA reductase, the enzyme responsible for the conversion of 3-hydroxy-3-methoxy glutaryl –CoA to mevalonate.

This is the rate limiting step in the synthesis of cholesterol in the liver. This leads to reduced endogenous production of cholesterol.

Reduction in cytoplasmic cholesterol levels leads to upregulation of LDL receptors in the liver. This results in enhanced uptake of LDL cholesterol in the circulation thus reducing plasma levels of LDL.

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5
Q

Why are statins administered at night?

A

The enzyme is more active at night

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6
Q

Which statins don’t necessarily need to be administered at night?

A

rosuvastatin and artovastatin, which are high potency statins.

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7
Q

Pleiotropic effects of statins

A

Regression of atherosclerosis
Anti-inflammatory
Plaque stabilizing effect
Improved endothelial function
Antioxidant

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8
Q

Adverse effects of statins

A
  • Major adverse effect include rhabdomyolysis, hepatitis, and angioedema
  • Others include headache, nausea, bowel upset, sleep disturbances and rashes.
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9
Q

Examples of bile acid sequestrants

A

Cholestyramine
Colestipol
Colsevelam

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10
Q

Bile acid sequestrants MOA

A

These are basic anion exchange compound.
They bind to bile acids in the intestine thus reducing the absorption of lipids. This leads to increased faecal excretion of bile salts and cholesterol.

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11
Q

Effects of BAS on TG, LDL, and HDL

A
  • Reduces LDL cholesterol
  • Small increase in HDL
  • Increase in triglyceride
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12
Q

DI and adverse effects of BAS

A

Reduces the absorption of statins and other drugs

Adverse effect – constipation, flatulence,

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13
Q

Niacin MOA

A
  • It reduces the production of VLDL in the liver by inhibiting triglyceride synthesis. This leads to reduced production of IDL and LDL cholesterol.
  • It also reduces the rate of lipolysis in adipose tissue, reducing the transport of free fatty acids to the liver and decreasing hepatic TG synthesis.
  • It increases the activity of lipoprotein lipase that clears triglycerides
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14
Q

Effects of niacin on TG, LDL, and HDL

A

TG - significantly reduced
LDL - significantly reduced
HDL - relatively increased

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15
Q

Adverse effects of niacin

A
  • Hepatotoxic, flushing, itching, rash, dyspepsia, nausea
  • Others are liver dysfunction, jaundice, hyperglycaemia
  • May increase risk of myopathy when used with statins
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16
Q

Examples of fibrates

A

Gemfibrozil, Fenofibrate, Benzafibrate

17
Q

Effects of fibrates on TG, LDL, and HDL

A
  • Lowers triglyceride
  • Increases HDL
  • Negligible LDL lowering effect
18
Q

Fibrates MOA

A
  • Interact with PPARs to reduce TG by stimulation of fatty acid oxidation
  • Stimulate lipoprotein lipase to reduce TG
19
Q

What is PPAR-alpha and how does it affect lipid metabolism?

A

It is the peroxisome proliferator-activated receptor, a nuclear receptor co-activator that regulates gene transcription for lipid metabolism. It also stimulates lipoprotein lipase.

20
Q

Adverse effects of fibrates

A

Increased risk of myositis with statins

21
Q

Ezetimibe MOA

A

Inhibits absorption of cholesterols at the brush border of the intestinal lumen

22
Q

Effect of ezetimibe on LDL, HDL, TG

A

Reduces LDL cholesterol
Reduces triglyceride
Small increase in HDL

23
Q

PCSK9 inhibitors examples

A

Alirocumab
Evolocumab

24
Q

PCSK9 meaning

A

Proprotein convertase subtilisin/kesin type 9)

25
Q

PCSK9 inhibitors MOA

A

They inhibit the PCSK9 enzyme that binds to LDL receptors on hepatocytes, leading to receptor degradation. Its inhibition means more receptors are available to clear plasma LDL.

26
Q

Mipomersen MOA

A

Inhibits apo B-100 synthesis, lowers LDL

27
Q

Lomitampide MOA

A

Inhibits microsomal TG transfer protein, essential for VLDL formation

28
Q

Fish oil MOA

A

Reduces VLDL triglycerides

PHA321 (12 decks)

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