Anti hyperlipidemic agent medicinal chemistry 5th semester unit 3

MEDICINAL CHEMISTRY 5TH SEM. NOTES

1. gent

2. 1
•
Introduction
• Cil
1
assificatiion
1
•
SAR of H
1
ypolip'idemic drrugs
1
•
MOA of Hlyp10
1lipidemic drugs
1
•
Drug stru1ctures
1
•
Uses

3. ••

4. c.1 assifica tior1
•'.-! HMG CoA redu:ctas,e i:nhibitor [ s,tat
1rn]
1
E~g, L,ovastatiin, p,rav,astati1n
• LiiP}~~tot1i@f lip,ase act1iv:at,Q:r
~g~Ci,o;fj br,ate ,f e:n,ofi bratet .
. . -- . ... -
~-
\'
·•• I -
lRiho ::.,, ~ •. ~f; I ~
~ ;JD ~tfillJifiK©
~~
I[· .. · ,.e]1

5. HMG COA Reductase enzyme is essential
tor cholesterol synthesis pathway
.J1 statin
Inhibit the HMG
COA reductase enzyme so
decrease cholesterol level
J1 Slatin
Anti-inflamatory effect
on the blood vessel
= wall fl
less Athetoscl,e
1ro
1s1is
fpptcom]

6. SAil
Comman famra li,r· all HfdGJUS
2. · •
11:Dnta•ntna. pradna reqalN In •
1lwu
Lydral,-1&1 HO ~•--....._ ·--
, H ,,
H
H
fPO com

7. • This is first choise drug for
dyslipidaemia
in diabetics
• Stain
are first choise drug for primery
hyperlipidaemias with raised LDL & CH
level
• Statins reduce
the risk of heart attack,
stroke & even de
1ath for fhe
1art diseases

8. CH~
I ,a
[Aromatic rin&)~(Spaecr.· group,] --c ............ --C~
I ......_OH
, .lsobutyric acid gro~p ·is essential fur activiay~ cH
3
CoqkJunds containing an rester. s.11:h as clafibralc and fenofibratc are
prodrugs and n:quirc in vivo
1 hyd~olysis.
• 1 S11b1titulion. at the p.-a position of the aromai.c ring with a chlor10 group
or a
chlorine· c.ontainin.g isof»opy·II ring ~ucc:· ,c,ompomd w.itb
significant.ly Ions~ half Ii re*
, :Most: of dn1gs
1
1C'OAlain a phenoxyimbutyric acid. lhe addi ti
1on of an ~
propyl spacs. as seen in gemfibrozil1 results in an acliv,e drug,~
-

9. • Headache, nausea, bowel upset, rashes
• Rise,s in serum transaminase
• Myopathy Disease
fppt oom

10. MOA OF FIBRAT
USES
Fenofibrate is used along with a proper diet to
help lower 'bad' cholesteFiol &fats
S1D
1
E EFFECT
Cause gallstones, liver problems,nausealvomiting
Stomach pain

11. In mtaal hype{tipkfania
ltli:im■ld Fil dlinl lt■g • MMJ1n111•1 ~ rff1g Cip1
Ix •N!llt1. •
11E-
I
1 P--• e PINII.,...,.

12. 11_
I f
Llpnar
1
2P mg ifldllldJI
Atorvasratbl
~ 11 ll!lilll
L.......-111.a.lii
lltllMvl■n- -3515
I !!i,f r,,,r r, '• ! ::,. ,;.. 1 ,F', 1 ~ ,
-- ---- --------------
: 'H :.. mlt·!f 00 TA». f I ~ I
- -
IIIIIIC' -• <PH • •
.· ~· .......
-•
II O llftQ • _,.