Resins

&
Fibrates
NAME : SHEFALI RAWAT
SEMESTER : IV SEM { II YR }
HYPOLIPIDAEMIC DR
UGS
These are drugs which lower the
levels of lipids and lipoproteins i
n blood.

They prevent cardiovascular dis

ease by retarding
the accelerated atherosclerosis i
n hyperlipidaemic individuals.
 BILE ACID SEQUESTRAN
TS : resins
 EG: Cholestyramine and Colestipol : These
are basic ion exchange resins supplied in th
e chloride form.

 Resins have been shown to retard atheroscl

erosis

 Itbinds bile acids in the intestine interrupting

their enterohepatic circulation.

 Cholestrol is absorbed with the help of bile s

alts.
 This indirectly leads to enhanced hep
atic metabolism of CH to bile acids

 Faecal excretion of bile salts and CH i

s increased.

 More LDL receptors are expressed on

liver cells leading to increased clearan
ce of plasma IDL, LDL & VLDL.
USES
Treatment of hyperchole
strolemia

To relief itching in case o

f obstructive jaundice
ADVERSE EFFECTS
 Unpalatabilty
 Bloating
 Nausea
 Constipation
 Flatulence
 Bindto drugs and reduce its absorption eg.
Thiazides, digitalis, fat soluble vitamins, antic
oagulants, propranalol.
 FIBRATES: MECHANISM OF
ACTION
 The fibrates primarily activate paroxisome pro
liferator-activated receptor α (PPARα) expres
sed in liver, fat and muscles.

 Activation
of PPARα enhances lipoprotein lip
ase synthesis that increases the clearance of
VLDL and decreases plasma TG levels.
 It also increases fatty acid oxidation th
erby decreasing triglyceride level.

 PPARα may also mediate enhanced L

DL receptor expression in liver causing
increased uptake and degradation of L
DL.

Fibrates decrease hepatic TG synthesi

s as well.
Drugs in this class primarily lower

TG levels by 20–50%.

10–15% decrease in LDL-CH.
 10–15% increase in HDL-CH
ADVERSE EFFECTS
 Epigastric distress, loose motions.
 Skin rashes, body ache, eosinophilia, impo
tence,
 Headache and blurred vision have been re
ported.
 Gemfibrozil + statin :increases risk of myo
pathy.
 It is contraindicated during pregnancy.
 Gemfibrozil
 This fibric acid derivative effectively lowers plasma
TG level by enhancing breakdown and suppressing he
patic synthesis of TGs.

 Highly efficacious in type III hyperlipoproteinemia.

 Gemfibrozilhas shown action in subjects with raised bl

ood Cholestrol.

 Itdecreases the level of clotting factor VII-phospholipid

complex and promotes fibrinolysis providing antiathero
sclerotic effect.
Use

In a dose of 600 mg BD taken befo

re meals,
gemfibrozil is the drug of choice for
patients with
markedly raised TG levels, whether
or not CH
levels are also raised.
 BEZAFIBRATE
 This is a second generation fibric acid derivative
.
 It has also been indicated in hypercholesterolae
mia (type II).
 It has greater LDL-CH lowering action than ge
mfibrozil.
 Decreased level of circulating fibrinogen and gl
ucose has been demonstrated.
 Dose: 200 mg TDS with meals.
FENOFIBRATE
 Another 2nd generation prodrug fibric aci
d derivative which has greater HDL–CH rais
ing and greater LDL-CH lowering action tha
n other fibrates.

 No rise in LDL-CH has been observed in pa

tients with high TG levels.

 Dose: 200 mg OD with meals

THANK
YOU