Pharmacology of Hyperlipidaemia.

1. DRUGS FOR
HYPERLIPIDAEMIA
PRESENTED BY,
Mr. Jithin Mathew,M.Pharm.,
Assistant Professor
Dept of Pharmacology
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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
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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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CLASSIFICATION
•HMG CoA reductase inhibitors (statins)
•Bile acid sequestrants(resins)
•Lipoprotein lipase activators(fibrates)
•Lipolysis and triglyceride synthesis inhibitors
•Sterol absorption inhibitors

8. HMG-CoA Reductase inhibitors
 Atorvasatatin
 Simvastatin
 Lovastatin
 Pravastatin
 Rosuvastatin
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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.

12. Bile acid sequestrants( resins )
 Cholestyramine
 Colestipol
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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

15. Activators of lipoprotein lipase (Fibrates)
 Gemfibrozil
 Bezafibrate
 Fenofibrate
 Clofibrate
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16. FIBRIC ACID DERIVATIVES
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 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.

17. Inhibitors of lipolysis and triglyceride
synthesis
 Niacin (Nicotinic acid)
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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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 Contraindication:
During pregnanacy, and in children
 Dose:
2.6gm/day in daily divided dose
 Use:
most effective in reducing plasma TG level.

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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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Hypolipidemic Drugs

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