2. • These are the drugs which lower the levels of
cholesterol and fats( lipids and lipoproteins )in
blood.
Hyperlipoproteinaemia
(elevaed lipids and lipoproteins in blood)
Primary Secondary
HYPOLIPIDAEMIC DRUGS
1-2
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Cholesterol
Fundamental building block of steroid hormones
Essential for building cell membranes, the myelin
sheath, and the brain
Core component of bile salts, which helps in digest
dietary fats
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Lipoproteins
There are different
lipoproteins:
Low-density lipoprotein (LDL)
Very-low-density lipoprotein (VLDL)
High-density lipoprotein (HDL)
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Triglycerides
Main form of fat from diet
Provide body with energy
Chylomicrons:
Very large lipoproteins that deliver triglycerides to muscle
and fat tissue
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Also referred to as statins
decrease total serum and LDL cholesterol,raise HDL.
Effective in secondary hypercholesterolaemia.
MOA—inhibit enzyme that causes cholesterol synthesis
by inhibiting the conversion of HMG CoA to mevalonate
by HMG CoA reductase enzyme.
HMG CoA reductase activity is maximum at midnight ,so
administered at bed time to get maximum effectiveness.
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Adverse effects:
Headache,
dizziness,
alteration of taste,
insomnia,
abdominal cramping
photosensitivity
myalgias,
leg ache,
muscle weakness
Contraindicated during pregancy
Uses:
Treatment of primary and secondary hyperlipidaemias.
First choice of drug for dyslipidemia in diabetes.
Treatment of primary secondary hyper cholesteraemia.
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They are basic ion exchange resins supplied in chloride
ion form.
Neither absorbed or digested in gut.
MOA:
They bind with bile acid in intestine and interupt their
enterohepatic circulation and increase bile acid ,faecal
excretion.
They are not popular clinically because they are
unpalatable,inconvinient and exhibit GI
symptoms,interfere with absorption of other drugs.
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Adverse effects:
include GI disturbances,
severe constipation,
acidosis,
worsening of piles.
Most serious adverse effect is intestinal
obstruction.
Uses:To releive itching ,obstructive jaundice and in
certain bile salt mediated diarrhoea
Dose: cholestyramine 4g TDS
16. FIBRIC ACID DERIVATIVES
16
All fibrates are isobutyric acid derivatives.
Drugs in these class lowers TG level 20-25%,LDL 10-15%,HDL 10-
15%.
MOA:They activate lipoprotein lipase enzyme which is a key
enzyme in the degradation of VLDL resulting in lowering of
circulating triglycerides.
ADR:
Epigastric problem,
loosed stool,
skin rashes,
blurred vission
,myopathy,
Eosinophilia
Uses:Used in patients with raised triglyceride levels.
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•It is a group of B complex vitamins.
•They reduce the level of cholesterol on higher doses
TG,VLDL level decreases rapidly followed by fall in LDL and
total cholesterol.
MOA:
It reduces production of VLDL in liver by inhibiting TG
synthesis.Indirectly the degradation products such as IDL
and LDL also reduced.
But have no role in cholesterol and bile acid metabolism.
ADR:
Cutaneous vasodilation,dryness of
skin,hyperpigmentation,liver dysfunction
high doses are intolerated.
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Others
Ezetimibe:
MOA—blocks absorption of cholesterol in
the intestines
Decreases VLDL
Decreases circulating LDL cholesterol
IND—treatment of hyperlipidemia along
with diet alteration.
Used along with statin for a synergestic
action.
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Adverse effects:abdominal pain, fatigue,
hepatic dysfunction.
Uses:ezetimibe +low dose statin =much
effective than high dose statin.
22. Gugulipid
Consists of Z and E gugulsterone,obtained from gum
guggul.
MOA: Inhibit cholestrol biosynthesis and also
enhance rate of cholesterol excretion
Dose 25 mg 3 times a day
Reduced total CH, LDL-C with an elevation of HDL-C
Adverse effect: well tolerated except loose stool
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