Lipid lowering agents
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Transcript of Lipid lowering agents
Lipid lowering agentsBy: Dr Israa Omar
MBBS, MRCP, MSc pharmacology
Reduces plasma concentration of LDL-Cholestrol by more than 30%.
Also cause a small reduction on plasma TGA and a small increase in plasma HDL
(statins)include simvastatin, pravastatin, atorvastatin.
REDUCE THE RISK OF CORONARY RTERY DISEASE BY 42%
HMG-CoA reductase inhibitors
Suppress HMG-COA reductase in the liver and therefore depress the production of cholesterol, which leads to increase synthesis of LDL receptors .
As a result, the clearance of LDL is enhanced
MOA
To treat patient with hyperlipidemia
Clinical uses
GIT disturbance Insomnia Rash More serious adverse effects (myositis,
hepatitis, angio-oedema )
Adverse effects
Include clofibrate, gemofibrate, fenofibrate. Mainly reduce VLDL and hence triglyceride . Also reduce LDL and increase HDL Gemofibrozil has been shown to reduce
coronary heart disease by one third compared to the placebo in male patients with primary hyperlipidaemia
fibrates
Stimulate the lipoprotien lipase in the peripheral tissues, and hence, increase hydrolysis of TGA in chylomicron and VLDL particles.
Also probably reduce hepatic VLDL production and increase LDL uptake
MOA
To treat patients with mixed hyperlipidemia (raised TGA and raised cholestrol)
Clinical uses
Myositis which can cause myoglobinuria and acute renal failure
Clofibrate can cause gallstone so its use is limited to patients who have had cholcystomy
Adverse effects
Cholestyramine and Colestipol They reduce the plasma concentration of
LDL-cholestrol by more than 10%
Bile acid-binding resins
They sequester the bile in the intestine and prevent their reabsorption and entero-hepatic recirculation.
This lead to increase expression of LDL receptors in the liver and hence removal of LDL from the blood
MOA
Used in addition to statins to treat hyperlipidemia
Clinical uses
N/V, abdominal pain , bloating, constipation or diarrhea are the commonest adverse effects
They interfere with absorption of fat- soluble vitamins and drugs like Digoxin and Warfarin
Adverse effect
Mechanism of action is poorly understood It is a water soluble vitamin Inhibit the production of hepatic triglyceride
and VLDL secretion with reduction of in TGA and LDL and increase HDL
It increase the blood sugar and causes flushing of the face an effect that can be reduced by taking Aspirin
Modified release prepartion are well tolerated
Nicotinic acid derivatives
Specifically inhibits absorption of cholesterol by blocking NPC1L1 in the brush border without affecting the absorption of bile salts or fat soluble vitamins
Combined with statins to treat patients with severe dyslipidemia
Generally well tolerated but can cause diarrhea, headache, rash and angioedema also reported
Ezetimibe
Thank you
RANGE AND DALE ,PHARMACOLOGY
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