Antihyperlipidemic drugs rahul sharma

Antihyperlipidemic drugs.

1. ANTIHYPERLIPIDEMIC DRUGS

SUBMITTED BY: DR.RAHUL SHARMA

DEPARTMENT OF VETERINARY
PHARMACOLOGY AND TOXICOLOGY

2. INTRODUCTION
• Hypolipidaemic agents, or antihyperlipidaemic
agents
• A diverse group of pharmaceuticals used in T/t
of high levels of fats (lipids), such as cholesterol,
in the blood (hyperlipidaemica).
• They are also called lipid-lowering drugs.

3. LIPID TRANSPORT AND METABOLISM
• Lipids originate from two sources:

▫
Endogenous lipids : synthesized in the liver,

▫
Exogenous lipids: ingested and processed in
the intestine.
• Dietary cholesterol & triglycerides : packaged into
chylomicrons in the intestine into bloodstream via
lymphatics.
• Liver synthesizes TG and cholesterol packages them as
VLDLs before releasing them into the blood

4. •• During this process, the VLDLs become progressively
more dense
•and turn into LDLs
•• Most LDLs taken up by Liver for disposal,
•• some circulate and distribute cholesterol to the rest of
the body
•tissues.
•• HDLs, which are also secreted from the liver and
intestine, have the
•task of preventing lipid accumulation.
•• They remove surplus cholesterol from tissues and
transfer it to
•LDLs that return it to the liver.

5. DIAGRAM

7. Hyperlipidaemia
Elevated concentrations of lipid i.e, Hyperlipidaemia ->
development of atherosclerosis and CAD.
• Dyslipidaemia can be primary or secondary.
• Primary forms : genetically determined
• Secondary forms : Consequence of other conditions such
as Diabetes mellitus,
Alcoholism,
Nepherotic syndrome,
Chronic renal failure,
Administration of drug…

8. Management of Dyslipidaemia
• Drug therapy to lower plasma lipids is only one
approach
to treatment
• Used in addition to dietary management
And
• Correction of other modifiable cardiovascular risk
Factors
• Several drugs are used to decrease plasma LDL-CHO

9. CLASSIFICATION 1
HMG - Co A Reductase inhibitors ( Statins ) :
Atorvastatin, Simvastatin,
Lovastatin, Pravastatin,
Fluvastatin, Rosuvastatin
• Bile acid binding resins :
Cholestyramine, Colestipol, Colesavelam.
• Inhibitors of intestinal absorption of cholesterol
: Stanol esters , Ezetemibe

10. CLASSIFICATION 2
• Activators of Lipoprotein lipase(Fibrates):
Gemifibrozil, Bezafibrate, Fenofibrate, and
Ciprofibrate
• Inhibitor of VLDL secretion and lipolysis :
Niacin (Nicotinic acid)
• New drugs (CETP Inhibitors) :
Torcetrapib, Anacetrapib

11. Class: HMG-CoA reductase inhibitors
• Mechanism: ↓rate-limiting step in cholesterol
synthesis.
• Clinical use: ↓ LDL, ↓ triglycerides
• Side effects: H : Hepatotoxicity
M : Myositis,rhabdoMyolysis
G : ↑ FPG
C : ↑ Creatinine phosphokinase
A : HeadAche, Joint pain
R : Rash

12. Diagram how statins work

15. Class: Fibrates
•• Mechanism: binds with PPAR α
•↑ lipoprotein lipase → ↓ VLDL
•↓TG
•• Clinical use: Elevated TG and remnants.
•• Side effects: GI upset (dyspepsia),
•Cholelithiasis,
•Myositis
•Hepatitis Rare
•• Drug interaction: Warfarin ,OHA

17. Interactions
• Increased risk of myopathy when combined with
statins.(fenofibrate)
• Displace drugs from plasma proteins( e.g. oral
anticoagulants and oral hypoglycemic drugs).
Contraindications:
• 1- Patients with impaired renal functions.
• 2- Pregnant or nursing women.
• 3-Preexisting gall bladder disease

18. Class : Nicotinic Acid
• Mechanism: ↓ fatty acid release from adipose
tissue, ↓ hepatic synthesis of LDL
• Clinical use: ↑ HDL, ↓ LDL, ↓TG
• Side effects: Skin flushing, paresthesias,
pruritus, GI upset, ↑LFTs, hyperglycemia,
hyperuricemia
• Prevention of side effects: Aspirin

21. Class: Bile acid resins
• Mechanism: Bind intestinal bile acids → ↓bile acid
stores & ↑ catabolism of LDL from plasma.
• Clinical use: ↓ LDL
• Side effects: Constipation,
↑ Gallstone formation,
GI upset,
LFT abnormalities,
Myalgias.
↓ Absorption of drugs
ADEK vitamins from the small intestine.
k

22. Dose : 4 to 8 g OD/BD, max dose 24 g/d.
• Contraindication

▫
1- Complete biliary obstruction( because bile is not
secreted into the intestine).

▫
2- Chronic constipation.

▫
3-Severe hypertriglyceridemia(TG >400 mg/dL)