Anti hyperlipidimidec drugs
Hypolipidemic drugs
: is a condition of excess fatty
substances called lipids ,largely cholesterol and triglycerides in the
blood .
It results from abnormalities in lipid metabolism or plasma lipid
transport , or a disorder in the synthesis and degradation of plasma
lipoprotiens.
Lipoproteins types: 4 types:
1- VLDL( very low density lipoproteins) ( N.R
2- LDL ( low density lipoprotein ) called bad lipoprotein (N.R less 130)
3- IDL ( intermediate density lipoprotein) . )
4- HDL( high density lipoprotein) called good lipoprotein. ( N.R above
60). Cholesterol serum ( N.R up to 200 ).
: is serum laboratory exam for lipoproteins
and other lipids as cholesterol and triglycerides.
Complications of Hyperlipidemia:
1- Hypertension ; specially if cholesterol level is increased.
2- IHD or atherosclerosis that may occur with ↑ level of cholesterol
and LDL and ↓ HDL level specially in obese patients.
3- Pancreatitis may be due very high plasma triglyceides . VDl and
chylomicrones.
4- Obstructive or cholestatic jaundice due to precipitation of
cholesterol in the bile duct in patients with cholecystitis ( Fч).
Antihyperlipidemic drugs : are drugs used to lower the conc. of
cholesterol ,phospholipids .triglycerides and chylomicrons in plasma.
Management of hyperlipidemia:
1- HMG- COA Reductase inhibitors :
Mechanism of action :
1- Inhibit HMG- COA ( 3- hydroxyl 3- methyl- glutaryl) coenzyme
found in the liver responsible for the conversion of HMG-COA to
mevalunae or mevalonic acid ( one of the steps of cholesterol
synthesis ) leading to ↓ conc. of cholesterol within the cell.
2- Low intracellular cholesterol stimulates the synthesis of LDL
receptors and ↓ secretion of VLDL.
3- ↑ number of LDL receptors promotes uptake of LDL from blood and
may ↑ HDL .
Uses:
1- Patients with CHD with or without hyperlipidemia .
2- Men with hyperlipidemia but no known CHD.
2- Men and women with ↑average total of LDL and cholesterol
Side effects:
Atorvastatin : ( Lipitor - Atorlip – Vasolip ) 10 – 20 – 40 – 80 mg
- Has a longer half-life than simvastatin, thus works for much longer.
- More effective thsn (SMT) at lowering cholesterol LDL ( bad) as
well as well as fibrinogen .
- Lower side effectscompared to (SMT) as muscle pain and drug
interactions.
- Could be a good oh choice in kidney disese as there is no need to
adjust the dosage , as others like SMTcanslows your kidneys when
given at the highest dosage 80mg per day.
Combinations of atorvastatin :
+ ( Ca channel blocker) :(Atorvee) for ttt of
HTN and angina.
+ :( Tinovas plus) : works by inhibiting the
activity of an enzyme called cyclooxygenase (COX) , specially COX-1,
which is involved in the production of thoromboxane A2 that
promotes pltelet aggregation→formation of clot.
3- + : ( Lipvas ) Gold
b) Rosuvastatin ( Crestor – Ultrox ) 5 - 10 – 20 – 40 mg
- Equally effective as atorvastatin at reducing heart attacks, strokes.
New study has found the finding s indicate that rosuvastatin lowers
cholestrol more than ator. But also carries a higher risk of developing
diabetes and cataract.
2- Lipoprotein lipase activators ( ):
- Less commonly used compared than statins, because it treats a
different type of cholesterol abnormality to statins , while statins
have strong evidence for reducing heart diseases and death.
- Prefered in people with elevated triglyceride levels and reduced
HDL.
- Its use is recommended together with dietary changes.
Mechanism of action:
Indications :
Fenofibrate: ( – - Fenolip ) 67 - 145- 160 - 200 300 mg
The Most commonly used drug among others because less side
effects and drug interaction.
Combination of fenofibrate with statins:
+ +
.
3- Sterol absorption Inhibitors:
*Ezetimibe:
Combination of Ezetimibe:
+ = 10mg + 20 mg respectively ( )
4- Bile acid sequestrans : - –
In chronic liver diseases such as cirrhosis or obstructive jaundice
,levels of bile salts become high and deposits in the skin , causing
pruritus ( itching ) ,bile acid sequestrans may be uses for this purpose
Mechanism of action:
Indications :
1- TTT of hyperlipidemia , but after statins introduced ,its use
becomes limited.
2- Controlling itching due to free bile salts .
3- Chronic diarrhea due to bile acid mal absorption.
Cholestyramin : ( )
Dose : 1 pouch ( 4 gms) or 1 level scoopful 9 4 gms) taken once or
twice per day , after one monthmay ↑ bases on ch. Level up to 2 to 4
pouchs.
5- Lipolysis and trigyceride synthesis inhibitor:
Nicotinic acid : ( vit B3)
Combination of Niacin ;
+ =
Dr. Ahmad Albabshi
Dr. Ahmad alhabshi
