Hello everyone.....I shared a pdf file containing the deep knowledge about HYPERLIPIDEMIA AND THE PHARMACOLOGY OF ANTI-HYPERLIPIDEMIC DRUGS . In the B.pharma 5th semester...there is an most important topic ANTI-HYPERLIPIDEMIC DRUGS in the subject Pharmacology -II so i uploaded this file to help the students about this most important topic.....if u want this assignment in any format....feel free to DM me on my gmail id.....careof22@gmail.com.....THANK YOU

1. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 1
-ANTI-HYPERLIPIDEMIC DRUGS-
These are those agents or drugs which are used in the treatment of
HYPERLIPIDEMIA.
Also known as –
 Lipid lowering agents
 Hypolipidaemic drugs
-HYPERLIPIDEMIA-
 Hyperlipidemia a broad term, also called Hyperlipoproteinemia, is
a common disorder in developed countries and is the major cause
of coronary heart disease.
 It results from abnormalities in lipid metabolism or plasma lipid
transport or a disorder in the synthesis and degradation of plasma
lipoproteins.
Causes of Hyperlipidemia-
 Mostly hyperlipidemia is caused by lifestyle habits or treatable
medical conditions.
 Obesity, not exercising and smoking, diabetes, obstructive
jaundice, and an under active thyroid gland inherit hyperlipidemia.

2. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 2
-LIPIDS-
 Lipids are the heterogenous mixtures of fatty acids and alcohol that
are present in the body.
 The major lipids in the bloodstream are CHOLESTEROL and it’s
ESTERS, TRIGLYCERIDES and PHOSPHOLIPIDS.
Cholesterol-
 It is necessary for new cells to form and for older cells to repair
themselves after injury.
 Cholesterol is also used by the adrenal glands to form hormones
such as cortisol, by the testicles to form testosterone, and by the
ovaries to form estrogen and progesterone.
Triglycerides- It supply energy for the body. Tryglycerides either
meet immediate energy needs in muscles or stored as fat for future
energy requirments.

3. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 3
Phospholipids- These are the compounds that are used to make
cell membranes, generate second messengers, and store fatty acids for
the use in generation of prostaglandis.
-LIPOPROTEINS-
 Since blood and other body fluids are watery, so fats needs a
special transport system to travel around the body.
 They carried from one place to another mixing with protein
particles, called LIPOPROTEINS.
Types of Lipoproteins-
Lipoproteins further divide into four major types-
1) Chylomicrons
2) Very low density lipoprotein {VLDL}
3) Low density lipoprotein {LDL}
4) High density lipoprotein {HDL}

4. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 4
1). Chylomicrons-
o Produced in GIT {Gastrointestinal Tract} from dietary lipids.
o It composed of mostly triglycerides and small ammout of
cholesterol.
Functions- Deliver energy rich glycerides to cell throughout the body.
2.) VLDL-
o Produced in liver and composed primarily of triglycerides and
small amount of cholesterol {More than chylomicrons}.
Functions- Deliver energy rich triglycerides to body.
3.) LDL-
o Produced from VLDL.
o Contain higher percentage of cholesterol compare to others.
Functions- Deliver cholesterol to cells throughout the body.
4.) HDL-
o Produced in liver (70-80%) and also in small intestines.
o Mostly composed of phospholipids, cholesterol and proteins.

5. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 5
Functions- Transport excess cholesterol from the peripheral cells to
the liver.
NOTE- HDL refered as a GOOD CHOLESTEROL and LDL refered
as a BAD CHOLESTEROL.
CLASSIFICATION OF
ANTI-HYPERLIPIDEMIC DRUGS
Several different classes of drugs are used to treat hyperlipidemia. These
classes differ not only in their mechanism of action but also in the type
of lipid reduction and the magnitude of the reduction.
1) HMG CoA Reductase inhibitors – Lovastatin, Simvastatin etc
2) Bile acid sequestrants - Cholestyramine, Colestipol etc
3) Fibric acid derivatives – Clofibrate, Fenofibrate etc
4) Lipolysis and triglyceride synthesis inhibitors – Nicotinic acid/ Niacin
5) Cholesterol absorption inhibitors – Ezetimide

6. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 6
1.) HMG CoA REDUCTASE INHIBITORS
 Also known as STATINS.
 Introduced in 1980, and used as a first line drugs for
HYPERLIPIDEMIA.
Mechanism of action-

7. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 7
Pharmacokinetic-
 Mostly given at bedtimes (Night) for maximum response (HMG
CoA max. at night).
 Absorption of the statins is variable (30-85%) following oral
administration.
 All statins metabolized in liver.
 Excretion through bile and faeces and some urinary elimination
also occurs.
Adverse Drug Reaction-
 Mild – Headache, GIT disturbance.
 Risk for liver toxicity.
 Myopathy (Disintegration of skeletol muscles) in some cases.
 Contraindicated in pregnancy.
Uses-
Used to treat hyperlipidemia by lowering plasma cholesterol levels.
Drugs-
o Lovastatin
o Simvastatin
o Metastatin
o Pravastatin
o Fluvastatin
o Rosuvastatin
o Pitavastatin
o Atorvastatin

8. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 8
2.) -BILE ACID SEQUESTRANTS-
 These drugs also give their effect by lowering cholesterol in blood
circulation.
 But these are less effective than statins.
Mechanism of action-
Pharmacokinetic-
 Not metabolized and Not absorbed.
 Excreted through faecs.

9. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 9
Adverse Drug Reaction-
o Nausea, GIT disturbance.
o Less absorption of fat soluble vitamins.
Uses-
 In the treatment of hyperlipidemia.
 Cholestyramine can also relieve pruritis caused by accumulation of
bile acids.
 Colesevelam is also used for type -II diabetes for its glucose
lowering effects.
Drugs-
Cholestyramine
Colestipol……etc

10. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 10
3.) FIBRIC ACID DERIVATIVES (FIBRATES)
 These drugs are derivatives of fibric acid and these drugs give their
action by decreasing the triglyceride and by increasing HDLlevel.
Mechanism of action-
Pharmacokinetic-

11. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 11
o Completely absorbed throgh oral administration.
o Fenofibrates (Pro-drug) converts to active moety fenofric acid.
o Excreted in urine.
Adverse Effect-
 Nausea, liver toxicity, muscle pain, GIT disturbance.
 Not used with statins.
Uses-
 Used in the treatment of hypertriglyceridemias.
 Also used in hyperlipidemia.
Drugs-
 Fenofibrates
 Gemfibrozil
 Bezafibrate…..etc

12. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 12
4.) LIPOLYSIS AND TRIGLYCERIDE
SYNTHESIS INHIBITORS
 These drufs give their effects by decreasing triglyceride in liver.
 Also these drugs can increase HDL.
Mechanism of action-
Pharmacokinetic-
 Administrated orally.
 Excreted in the urine.
Adverse Effect-
o Flushing.
o Risk of hyperurecemia, gout.
o Cause liver toxicity.
Uses-
Treat hyperlipidemia and also effective in hypercholesterolemias.
Reduce LDL by 10 - 20%, increasing HDL.
Drugs- Nicotinic acid/ Niacin.

13. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 13
5.) CHOLESTEROL ABSORPTION
INHIBITORS
 also known as Sterol absorption inhibitors.
 These drugs give their action by inhibiting dietary and biliary
cholesterol in small intestine.
Mechanism of action-

14. ANTIHYPERLIPIDEMIC DRUGS
ANSHIK SRIVASTAVA
ROLL NO.-2008880500016 Page 14
Pharmacokinetic-
 Poor aqueous solubility (Less absorption).
 Plasma t1/2 = 22 hours approx..
 Metabolised in small intestine liver.
 Excretion = Biliary & renal excretion.
Adverse effect- Mild & Tolerated.
Uses- Good choice for patient in combination for hyperlipidemia.