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Prof. Dr. Shah Murad
shahmurad655@yahoo.com
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As if we didn't have enough cholesterol
in our diet, our liver actually makes the
stuff!
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Ifyou can't bring down your
cholesterol with diet and exercise,
you may need a prescription for one
of the HYPOLIPIDEMIC DRUG
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The most frequently prescribed drugs
are generically called "statins",
because their chemical names all
end with…..statin! They reduce the
manufacture of cholesterol in our
liver.
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Thereare also other drugs used to lower
cholesterol that work by different
mechanisms.
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In1984 it was demonstrated for the first
time that there exists a link between
serum cholesterol levels and risk to CHD.
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Positive risk factors for CHD
include:
Age (men>45 yrs, women>55 yrs);
family history of premature CHD;
smoking;
hypertension (>140/90 mm Hg);
low HDL cholesterol (<35 mg/dl);
obesity (>30% overweight);
diabetes; and
high LDL (>160 mg/dl).
Negative risk factors include high
HDL levels (>60 mg/dl).
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The structure of Ch suggests a highly
non-polar nature indicating that it should
be reasonably insoluble in aqueous
solution.
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(5) Types of
hyperlipidemia
I (familial hypertriglyceridemia)
IIa (familial hyperlipidemia)
IIb (familial dysbetalipoproteinemia)
III (familial
hypoalphalipoproteinemia)
IV (familal hypercholesterolemia)
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Lipoprotein Particles
triglycerides
phospholipids
cholesterol
cholesterol esters
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Chylomicrons (TG >> C, CE )
VLDL (TG > CE )
IDL (CE > TG )
LDL (CE >> TG )
HDL (CE > TG )
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Mechanism of Lipid
Transport
Dietary fat including cholesterol and
triglycerides are absorbed in the intestine and
released in the blood stream as chylomicrons.
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A 15-30 point drop in LDL could be
reasonably expected with most
statins after a therapy of about 1
month.
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The antitriglycedemic effect of clofibrate
in human is related to the increased
catabolism of serum TG-rich proteins
(VLDL and VLDL remnants), but not to
any effect on hepatic TG or VLDL
synthesis and release from liver.
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Bile Acid Sequestering
(BAS) Agents
Colestipol
and cholestyramine are anion
exchange resins that are approved in
1970s for the reduction of elevated
serum cholesterol in patients with
hypercholesterolemia.
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BASagents may also lower the
amount of anticoagulants (warfarin,
coumadin) absorbed due to
sequestration
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Nicotinic Acid (Vitamin
Pharmacologic B-3)
doses of nicotinic acid
reduce serum cholesterol and TG levels in
types II, III, IV, and V
hyperlipoproteinemias.
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n Administered in large doses (0.5
to 6 grams daily)
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Abdominal cramps when taken in empty
stomach
Diarrhea
Nausea
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Very new Anti-hyperlipidemic Drug – Ezetimibe
• Approved in October 2002
• Reduces serum LDL, TC, and TG and increases HDL
• Prevents the absorption of cholesterol from diet
• Useful in Type IIa, IIb, III, IV and V hyperlipidemias
OH
OH
N
F O
F 46