it will provide information regarding pharmacology of lipid lowering drugs and pathogenesis of atherosclerosis

1. .
Lipid-Lowering Drugs
and
Atherosclerosis
By
N.Sharada
Assistant professor
Palamuru university

6. Classification:
• HMG CoA reductase inhibitors
(statins):Atovastatin, pravastatin, and simvastatin
• Bile-acid-binding resins: Colestyramine and
colestipol
• Fibrates : bezafibrate, ciprofibrate, and gemfibrozil
• Inhibits lipolysis and TGLsyntesis: nicotinic acid
• Others: probucol

7. Treatment (lipid-lowering drugs):
• HMG CoA reductase inhibitors ( ‘statins’)
• Atovastatin, pravastatin, and simvastatin are
examples of 3-hydroxy-3methylglutary coenzyme A
(HMG CoA ) reductase inhibitors. These drugs have
been shown to reduce blood cholesterol by up to 35%
in some patients.
• HMG CoA reductase inhibitors can reduce the risk of
dying from a coronary events by up to nearly half.
• Mechanismofaction:Statins reversibly inhibit the enzyme
HMGCoA reductase, which catalyses the rate-limiting
step in the synthesis of cholesterol.
• Adverseeffects:Reversible myositis (rare);
constipation or diarrhea; abdominal pain and
flatulence; nausea and headache; fatigue and
insomnia; and rash.

9. Bile-acid-binding resins
• Colestyramine and colestipol have been shown to
decrease the rate of mortality from coronary artery
disease.
• Mechanism of action: Basic anion exchange resins act
by binding bile acids in the intestine, thus preventing
their reabsorption and promoting hepatic conversion
of cholesterol into bile acids.
• Adverseeffects:Side effects include nausea and
vomiting, constipation, heartburn, abdominal pain
and flatulence, and aggravation of
hypertriglyceridaemia. They may interfere with the
absorption of fat-soluble vitamins and certain drugs.

11. Fibrates
• Fibrates include bezafibrate, ciprofibrate, and
gemfibrozil. These are broad-spectrum lipid
modulating agents that are ineffective in patients
with elevated cholesterol but normal triglyceride
concentrations.
• Mechanismofaction:Fibrates work in several
ways……… (Multiple action drug?)
• Adverseeffects: Side effects of fibrates include:
• Myositis-like syndrome ( especially if renal
function is impaired ).
• Gastrointestinal disturbances.
• Dermatitis, pruritus, rash, and urticaria.
• Impotence.
• Headache, dizziness, blurred vision.

12. Effects of Fibrates on Lipid
Metabolism
Peroxisome
proliferator
activated receptor  (Transcription factor)

13. Nicotinic acid
• The side effects of nicotinic acid limit its use in
the treatment of hyperlipidaemias. Nicotinic
acid has been shown to reduce the incidence of
coronary artery disease.
• Mechanismofaction:It inhibits VLDL and LDL
synthesis; it increases HDL- cholesterol.
• Adverseeffects:Flushing, dizziness, headache,
palpitation, nausea and vomiting, and
pruritus.

14. Effects of Niacin on Lipid
Metabolism