Unit 5 Medicinal Chemistry by Chandu

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CAREWELL PHARMA - A FAMILY OF LEARNING
search CAREWELL PHARMA on Youtube, Watch free Video Lectures
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OWnd
lP
lP
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Phara
Pharma
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tor C
(AHAel
TUst
Tust
TUS
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Is holb
lP
lP
lP
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Note -If You have any Doubts

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in any thing in pdf

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Just Ask us in comment of any video,

Or confirm it from google
This Notes is Provided by Chandan MOCP

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Website For Notes & More :- www.carewellpharma.in

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Provided By - Chandu Brother

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Page 2 of 76
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iit
C
C
Orugsacting o entral. ervous
slem
a
a
rm
rm
eneral nae'sthelic3:
ha
ha
ha
lP
lP
lP
enesal vaesthetics are group of dnigs thot
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ew
ew
produces loss of Consciousne.s3 and therefoe
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of all Seations
C
C
las
She ass ot sensalion is teymed a

absolute
anacsthe3ia.
a
eneral onaesthe tics bring abaut descendng

rm
rm
of he CNS, 5tarting ith the Ceseba

ha
ha
ha
depres3ion
lP
lP
lP
thal4.
cortex, the basal ganglia, Cerebelum and
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spinal Cord
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Shese are nin Sugkal peraton

drlos Sad
C
therejore abolsh
to arnd
induce ulConsciousM¢ S5
4/
5ersation of Paln
a
a
rm
rm

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Page 3 of 76
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ages g generaAnaesthesia
C
adminlslesed
When an inhalatiovn ondes (heti i t
tollacng Lwell defined
palient Sonte ofthe
produce byincveSivg the blood
a
a
Jtaqes aye
rm
rm
Concantratim of the .agent heyase
.
ha
ha
ha
lP
lP
lP
- dhis
el
el
staqe is also Called as stage of onalgesia
ew
ew
ir
-Uhis period rom he begimming of

ot
is he
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C
C
anaesthetic acminishalion to he los of Corscious
nes5
-
he patient, Progressively looxe3 Paîn.
a
a
rm
rm
5tage
Ihis age also called as stage ofl
ha
ha
ha
lP
lP
delirium.
lP
extenas
el
el
vom
his pesiod extnds the l055
l0s3
ofonsiaisne
ew
ew
35 throuqh a stage irtegulosadh spechc

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ar
of
C
beathing the veestablishment

to qular bxeatg
-hespnaton 5 nomal and egular. iie.
potiemd May lough, Vomit ) saugale
a
a
rm
rm

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Page 4 of 76
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,
iagE
C
slag also callcd as Jtaqe o Jurqical
antacs
thesia
otage eitement i Jost and skeletal

his
a
a
rm
rm
muxle ela1atioti Produced
ha
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01 Suqesle s are done in this Jtoqe.
Mast ype
lP
lP
lP
Stage
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el
stage also stuge of me dullan
ew
ew
is called a5
hs
ar
ar
alcpession
e
C
C
Overdose of he ancaesthetic may brng
to his stoge
.
patie nt
espivatoy and Civculadony arlure occur 1inthis

a
a
rm
rm
sagg
ha
ha
ha
Classification ofGA
lP
lP
lP
-- eclassihicd aicotdng
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Meneral anacsthetics
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ew
to their.nature as llows,
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C
h Snhatotion nena oMaesthetiçs

3d
Stravenoussto qeneial :anaesthetics
a
a
rm
rm

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Page 5 of 76
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0 Jnhalotio anocsthelic
C
acdninisleve d by halofion
- fuvlher 3ubdided
a
a
D ases
rm
rm
Ntrous 0xide
ha
ha
ha
) Siquidb halatone, chlovobm, dichl ehe
lP
lP
lP
tveVenous a1OCthe
tics
el
el
.Jhey aye Odninisteved y ivtaveous 10
ew
ew
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ar
Jhey aye
C
C
) Bovbiturates thiopental Sodiun, methehe ital sodium
y Non- baubrierales- pnopenidid,popotol
Havacteinites: o A
a
a
rm
rm
An ideal
- genend ongesthe tic 5hauld passess he
the
ha
ha
ha
ollouaing chauacteriste
lP
lP
lP
) hould be inert
el
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e
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ew
should be potent and Mon- intlammable

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ar
oity 94 should be rol- isritating to nacous

Membiai
C
producephd and
shauld 1mooth anaesthesin
3hauld nst ProduceS¢vese:ypotension
y 9t t.
not produce rausea
0 9t Jhould f vamiting
a
a
rm
rm

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Page 6 of 76
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be
should CConomica.
C
Meckanim acdion
alacsthehes laret he ligand gated ion
enc 1a
produce be araeJthe lie action
a
a
channels and
rm
rm
eceptor cMoride
Jhe oA gted clharnvnels are
ha
ha
ha
impostant opens pertom
itcs ond de
lP
lP
lP
most
he
el
el
inlibito ac tan.
he
ew
ew
and ketamine do not affec? the nABA
-Ng0 (o)
ar
ar
C
C
alucine gaied
qaied cs-Channel, bul hey elechey
vhbit the cilatony NMDA,-pe of qlutome
seceptor, ohich belongs

lonqsto cakum-qated chanuels
a
in the NeuronsS andleads to eurtal hupespolar

rm
rm
ha
ha
ha
ization
lP
lP
lP
nhalation anaesthetics :
el
el
i t
ew
ew
alothonC
ar
ar
tructure
C
B
a
a
rm
rm

ha
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Page 7 of 76
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ythesv
C
icloroe hyene
a
a
rm
rm
ha
ha
ha
lP
lP
lP
el
el
F
ew
ew
hiflucaocthone
2- hloro- 1,1,1-
ar
ar
C
C
BY
F.
t
a
halotkone
rm
rm
Mechortom gt ACfion
ha
ha
ha
.actiornts on chames
-lalothane pro duces o multple
lP
lP
lP
depiession in
whick
theie
el
el
due to The Ne£TVE.

ew
ew
arnd Codiac (onttractithy*

Cornduc ton, breathng
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ar
-41 binds ith potasslum channeLs and pT0duces

C
jonnobihaing
effects
bind witha NMDA and

also calcium chans
-Jhcy
a
a
rm
rm

ha
ha
ha

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Page 8 of 76
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causes"hyparpolasizotion
C
. a, cleay,colausleas,heavy, no-4omnable. liguid
soluble in uuter, misibe with ethonel; ond,
slatly
a
a
rm
rm
trichloroethylene
idh
ha
ha
ha
lP
lP
lP
ptont elatvely 3afe 9eneral nholahor
tisa
el
el
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ew
:
Used i (onjuga to with ND
artaest he ti
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Aaveise ellecds
C
C
ineqular heart beals, halothane egatio
ivetproblems,
decieased efforts to breath
Methozytlurone
a
a
rm
rm
Atuctue
ha
ha
ha
lP
lP
lP
F
c
el
el
ew
ew
c
ar
ar
Meckonism of action
C
unction channel opein

-44 decxeO.se3 he 9ap
5 gnes junctor chomel cls
imes and ncreses 9
a
a
rm
rm

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time
ime Lohiclh inucc3 e dut tion in unctional Conduclon
C
svbunid
Melhofun also binds with D of h
of Avp
seceplo13, qlutonate veceptn3 qlcin

utthase, GiABA
Ttceptovs NADn dehydrbgeroe

a
a
rm
rm
Progestics .t.
ha
ha
ha
91 6 a cleor coelounless liqud
lP
lP
lP
Jt io Soluble in woles tt rom tempt1otuTe
el
el
.les , .
ew
ew
-1is the
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ar
mast potent of inhalational ongesthetiks
C
C
And Caus e liqht.anacsthesia hdeep ara lqese
and muscle elosaton. featne
Adverse effects
a
-Nephuotosicity, lo fotal hepatetesidy

rm
rm
scveie
luxane
ha
ha
ha
lP
lP
lP
uclure
el
el
ew
ew
ar
ar
-0 F
C
C i
Mechnism action
produces depressiveeffects by bnding oi

3t
a
a
rm
rm

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a1Bllpand gycne veceptors
C
cardio depae3sive elfeed isproduted due to
toilh calt ium channels

bding of he dug
a
a
-
rm
rm
4 a clear; colouless, volatle lquid wil
ha
ha
ha
pleasant hydhocas bon ike odour 5oluble in oter,
lP
lP
lP
mivcible oilh orqcnic solvents
el
el
ew
ew
as anaesthe tc
41 isuwed
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C
C
Advese
myoardkl foilure,
contrac tilky, kidney tailure
depre35hon of
myocasdial oxygen Cosumption, maligrant

decease i
a
Nephrotoricity, ei
rm
rm
ypesthemio,
ha
ha
ha
Devotlunane
lP
lP
lP
ructure
el
el
ew
ew
F F
ar
ar
C
CF3
Mecleibn
action
Pevelurone june don chonnel

decreases the 9P
a
a
rm
rm

ha
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ha

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Page 11 of 76
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opering tintes and
and inceas 9P Juneton Chonnc
C
TCductonin jinctional
clesmg tinme ohich induccs
Conductance
Aevoluane also bmas oith D subuait ef Ap su

a
a
rm
rm
ase GaABA WCeptors, qhutanate. recepteSyeine
ha
ha
ha
TOceptors, NADH dehyoroqenase.
lP
lP
lP
IOperties
-
el
el
i a lo beilng liqvid with a light Odous
ew
ew
miscible with most oqnic Solvents including ots
ar
ar
uter
C
C
(O1) oils piac fitally insouble in
Wses
.
-1 is uscd 4oT incucHon and maintainance of
general anaesthesia odull and peciatric patienb
a
a
rm
rm
Aave1se effects:
ha
ha
ha
B1adeardia, hypotension, achycondia,
- aqitalen; loiynasjp
lP
lP
lP
Sm, apea, tever Nause o, Vomiting, paim Confusion,
el
el
diy mauth, nsomnia

ew
ew
Ssoluaane
ar
ar
-1
C
Aiuc te
F
a
a
rm
rm

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ha

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Page 12 of 76
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Meckoncnl gtio
C
Aoorane decveascs the gap. juncton channcl
channel
Juntcion chonnel
openig
inmes and incie ase 9P
ime which induces. scduc tion, in junctoal
elosing
a
a
cotdut taace
rm
rm
ot
turane also bind uwithD Subunit P
ha
ha
ha
Isct
eceptos, 99e
lP
lP
lP
synathse, GnABA eceptos9lutompte
el
el
NAO dehychoqenase
eCeptors
ew
ew
soperties
ar
ar
liguid insoluble
C
C
colousles heovy in
41, is a clea
ater, Misxible wth, cthanol and ichlo1ecthylene.
Uses
4sofuräne i uSed,tor induc ton and: maintainance

a
a
rm
rm
pcdiotric
of genera
gene1a onacsthesia in.0dult and
ha
ha
ha
potienis
lP
lP
lP
Aaverse effecy
el
el
ew
ew
Yardot disorde13, hepato biliayy disotde1s

ar
ar
Desflurdde
C
tructure
a
a
rm
rm

ha
ha
ha

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P
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Page 13 of 76
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Mechonin
C
action
chonnol opeim
-
bestluranc decre ase he qap jungion open,
imes inctcase5 g0 junctian chamel closm

closmg
and
tme wkich induicesvedu ton in oee
junctional Conduco
a
a
rm
rm
-teslurone aso bin ds with D Subunit of ATp
ha
ha
ha
Synthase CnA BA
ece pto, qlutomote eceptors 9ycine
lP
lP
lP
Teceptois, NAOH dehydogenast
el
el
ew
ew
1Opettie
ar
ar
- 31 is
a ou bolhnq liquid with a sliaht odon
C
C
Mistible 01qanic Solventsinckuding olso)
oils psac icall insoluble in oter
a
a
rm
rm
pesfuoneis usedfor iMauchion of ona esthesia ts

ha
ha
ha
Inpatlnt and outpstend 3uqer
lP
lP
lP
Adverse effecis
el
el
on eqes, headoche
ew
ew
-kavdiovascukr effetts, etfec

ar
ar
di22iness Nasal congeštion, back ain lerqie i edeno

C
abdominal Pain dy mouth, diasrhea;

Nousea
Vomiring insomnia,
a
a
rm
rm

ha
ha
ha

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Page 14 of 76
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ar
hashoy acting 3bituate
C
Nethokexitol Odtum
uCture
a
a
rm
rm
1
ha
ha
ha
lP
lP
lP
el
el
ew
ew
ar
ar
ONa
C
C
acton
Meckorisn
of
- Me thohexital bindsatt a distinct binding site aJsiot
ionooie at
at lhe CABAA Teceptor,
witha The
a
inCICaStn lhe dura tion of time uahich the

rm
rm
ovopore isopen.
ha
ha
ha
opentea
lP
lP
lP
t uohide. to offwhie hygroopie pouder, essenkily
el
el
is
ew
ew
odousless and the solution

is alkaine soluble in
ar
ar
water
C
Ses
-is Used tos the inducdon o atoesthesia
hough he ntra venous adminlstraton.

a
a
rm
rm

ha
ha
ha

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Page 15 of 76
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urlhe
io
C
C
CHyooc
c +BYCH,cH=CH,
a
a
3-byomo pop -1-ene
rm
rm
dicthyl maloate
ha
ha
ha
H &7 CHONa
lP
lP
lP
CH00 C CH,CH = CH
el
el
ew
ew
CH00C H
ar
ar
) CHONo
C
C
li) Br-CH-CEc4NCH3
CH
CH,cHCH
CHo0C
CH-CEc-CH,CH
a
CH
rm
rm
Noo ci-methyl uvea

ha
ha
ha
-C21,OH|
lP
lP
lP
el
el
IN CHCH CH
ew
ew
CH-CE-CH,CH3
ar
ar
CH
C
Methohesital Jodium
Adveioe cffects
drowsiness, nausea, Vomitfng, Stomách
pain, shivering
a
a
rm
rm

ha
ha
ha

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Page 16 of 76
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ar
Hchinq, skin Yashe5 cta
Coghivg hictups,
C
hionylalOduen
tuclue '
a
a
rm
rm
ha
ha
ha
O.
lP
lP
lP
HN
el
el
ew
ew
sNat
ar
ar
Neckanism acfion
C
C
binding Jites assxiotedd
binds with dilfescnt
at the ABA
with chloride jatopote
the durrtion of
1esults in increaeI
a
Jhis
rm
rm
ionopoye
tne the opening of chlorlde
ha
ha
ha
ellect of
3moptiemibitony
-As a Tesult, the
past
lP
lP
lP
the halamus 1prolonged
el
el
nA BA in
ew
ew
JToperties
hydrophobit
ar
ar
'
and i a highi
asolid,
C
'4
.
tiooarbiturale hoving Spari ngy Soubili

a
a
rm
rm

ha
ha
ha

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Page 17 of 76
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ar
C
C
-41 ravenous5 onocshetic
USed as
aS
Advse ellector
los3 of c00sdinor
01 CO6sdno
Snsomnia, dizzinc33» droosines),
a
a
(ovtipation, VEstle sincs53, ebdoche,
rm
rm
Nauseo, Vonifing,
l055
ha
ha
ha
of appelite, pale ski
skin.
lP
lP
lP
hio penlal
Sochum
el
el
Aruclure
ew
ew
ar
ar
C
C
.
O.
H
a
a
rm
rm
3, Na
ha
ha
ha
NMecharisn
afo1
lP
lP
lP
31 binds with difleient binding sites assoctated
el
el
chloide onopove at aABAA

oith
ew
ew
-Jks FeSulis ininciease

ar
ar
in the dura tion of

C
me the opeinq the chloide onopore
inhisto
As a sesult, the potsynoglic inhidtory effect
in the halamus
of GaABA is prolorged
a
a
rm
rm

ha
ha
ha

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P
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Page 18 of 76
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ar
ar
C
C
a yellowish wite poder, hygre opic , fiely
oluble i wler ond prly Jouble in ethonol

a
a
rm
rm
USed as onocsthe tc ogent,for the
ha
ha
ha
of anaes theia o1 short
producion Conmpleie a
lP
lP
lP
duration
el
el
Sedotive, hypnotic
ew
ew
also used cis a
arficonvulsot
ar
ar
C
C
Auerse glfects
and espiraiong depsession, ypelension
-tovdiovaseular
heodoche, i Nausea, away obst ructbn, ete

Cpnca
a
Dissociative anaestheticg
rm
rm
ha
ha
ha
hudrochloride
ketaine
lP
lP
lP
tr lure
el
el
ew
ew
ar
ar
C
HCR
NH
H
a
a
rm
rm

ha
ha
ha

P
P
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Page 19 of 76
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ew
ar
ar
ytheis
C
Bs Mg
a
a
2-c hlovoben?onidiile (ye loenty magnrsium
rm
rm
lovice
ha
ha
ha
,
lP
lP
lP
el
el
ew
ew
ar
ar
C
C
.
a
a
rm
rm
,
ha
ha
ha
lP
lP
lP
el
el
Ho
ew
ew
12-
ar
ar
C
NHCH3
HCR
kelontne ydsochlanide
a
a
rm
rm

ha
ha
ha

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P
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Page 20 of 76
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Mechonisn of action
C
N-melhyl-o-spavtote (NamDA),
mterorls
ketanine
muscainic tecepbis, EValtage
ecpfors,
opiod ccptou3,
XNSItive Ca ion chonnels.

a
a
rm
rm
ke (onine does
doc
Llnlike other gencsal anacsletics
ha
ha
ha
oilh GaABA JCCeptors
1o inteat1
lP
lP
lP
Koperte
el
el
ew
ew
pounder
3t is a hitc
itc OY almost hite cnstalline wder
ar
ar
5oluble in water, ntethonol and ethano
huely
C
C
J1 a Tapidly acting non barbinurate gencral
- i
anacsthe tic ha procbes anaasthesia.
a
a
rm
rm
Advese gfecls
ha
ha
ha
- Confusion t-Voniing
-uo siness
lP
lP
lP
hallucinarto
oppette.y
el
el
Slouheart isate Aoso,

ew
ew
Weak a3halsa beothing ia

ar
ar
C
MCTCased uinationM
blusned
isen
-
Nousea
a
a
rm
rm

ha
ha
ha

P
P
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el
Page 21 of 76
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ar
C
C
Non -Novcotic fAoalgesi
Vavcotic and
Analgcsics o aqcns that 1elievVe pain by
actina to elevale pM thseshold, uoithot

centrally
a
a
rm
rm
dtstuubing alleinq olker
olher Scns0
O1)
CoiOSieJ3
ha
ha
ha
System
lP
lP
lP
-evtain 0nalgesics ke aminopyrinme ond phenglburrbre
el
el
ew
ew
alio outi intlamomatony proper tics
ar
ar
Avolacsics 1o
ac classitic
din 2 Catcgories
C
C
Opioid analqesicS oy nareotlc analqesics
di) Non oçicid analqesks
Opistd onaloesk5:
a
a
rm
rm
ugs that
-0 pioid onalesis, aTe drugs CTe naturalky
ha
ha
ha
3ymthetic
Semisynthetie dug3 ahch
lP
lP
OCCuim and
lP
Tke action
el
el
have "amorphine like - Manmely relieve hot

ew
ew
aud depie SsionM of CNS assoclarlcd uoih

pain he
ar
ar
depandence
C
drug
dask biouon
Ooum a sCSinos matevial,
ohoned rom he capsule

a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 22 of 76
ew
ew
ar
ar
has two upes of alkaloids
C
pheronthuene
y eriva:tve.
)Benzod0quiMo line deinvatives
Nortotic ginalsic cqens, quse 3lecp inorjuncion

a
a
rm
rm
their avnalqcsic effect
ha
ha
ha
Mechoriso actian:
lP
lP
lP
endogenous peptides found M CN3
Jhe ond
el
el
ew
ew
qastvointestinal Aact Con deciese paih-produce
ar
ar
Cuphonia dousincss dlepress
euphcvia, Espireion,depic55
C
C
cough eflex, tastrointestinal Mucle activi
he ve are S categoies ofopioicd receptor5,1

a
on
mo (u)
rm
rm
dy kappa (K)
ha
ha
ha
ii) Sigma ()
lP
lP
lP
(ivi delta (5)
el
el
ew
ew
epsilon (¢)
s. available
ar
ar
Ihe actions of heMaxotic analaesie nod

C
Con bedehned their. activh

.
at; thee
Peciic oplate Tecepto ypesmu(u), kappa(k)f
delta &
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 23 of 76
ew
ew
ar
ar
ve ceptors ieciote analqcoio, Cuphoria Tapira
C
depciiov miosis andedauced gastrointo.
,
Matih .
cceptoi subclasihe as
a
a
rm
rm
me shate analqesia
ha
ha
ha
me diote cspisateny depiesslon '
lP
lP
lP
d secepio13 meciaté pmal Supaspinal analges,
el
el
ew
ew
ysphoni. paychotomimelie effecis a0isafoiy Va3oml
ar
ar
OY stimulation
1
C
C
-hese aTe Dubtyped. as d
-k 3accptos me diote pentazocine ike

ike spinal
Cnolgesia, Sedatlon, miosis, iespmatoy depression

a
dypkosia.
rm
rm
-Jhese urther
ha
ha
ha
ae 3ubyped
lP
lP
lP
K mediate pina) analocsio
el
el
R3 me diate Supraspinal analqesia

ew
ew
sla tunction is unkauon

ar
ar
C
Cla3siticaion of arcotic andlgesics
Narcotic analqesicS are classiie

d as
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 24 of 76
ew
ew
ar
ar
Notunal alkaloids of opiumMophine, codeime
Notunal
C
i
Semisynthetë annloqs - hydronmorphone, oymerphane, oXycoe
in il
3ynthete
synthe tC aqents- mepeiidine, methadore Aentangl ele"
di
ji)
deivatives
a
a
Morphve and
rm
rm
Morphine
ha
ha
ha
SAR
lP
lP
lP
studied
AR ot movphime b
el
el
onedificati of alicyclic T
ew
ew
ch
ci modi
be ation of aromatic Tng
ar
ar
1
C
C
iy modihication of
3 nrlvogen
vy cpoxide bridge
a
tertlorytarynihaqen
rm
rm
ha
ha
ha
2 aliyclic unsaturaied inkaye
lP
lP
lP
el
el
S
Ho 0 oaleoholic hydoxy
ew
ew
ether bidg
ar
ar
phenonc hydoxjl gioup :

C
Mbdifcation on liralicycli g
-he alcoholic Aydrony I7oup at CH6hen mehylat
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 25 of 76
ew
ew
ar
ar
d,esterhed o1idized. enoved ploCed
C
Malogen, ac tivly as ocl 03 toxicily
analgesic
Compound increastd
' t
-he
*Ohe ieduction of keto qvoup to
c-6
6 P*ydeng
a
a
rm
rm
An Nalbupime
0umos phone ives it Sho03 onfagni
ha
ha
ha
ic acton of cceptons
lP
lP
lP
Jhe
el
el
Saturation of he double
bond of c-7
ew
ew
position mone potent
gives Con1paincd
ar
ar
5icing of
of C-6 and
-l through elhylene ukoge
C
C
gives potent deivaiives.
) Wlodihcotion pheny ing

a
An avomatic pheau C3sential

-
ing is toy
acti
actvi
rm
rm
ModiicatonM phenolic hudi0 a1up decteases

ha
ha
he
ha
lP
lP
achvity
lP
on phanu vinq dimishes
othrSubstution
el
el
Any
ew
ew
actividy
ar
ar
tnogcn*
id Moditication
C
terto amine U5ually necesar: fo g

-A
opiotdnsrac iviy
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 26 of 76
ew
ew
ar
ar
can dietate the
the N Jubstitulion
C
Size of
:-Jhe
Castpound olenty and ts agonist ond ls
Tevese ata qanisti proety

leads lo narcote
N yelo alky 910ups
a
a
and
-allyl
rm
rm
antagonistikpopety
ha
ha
ha
briege
o potide
lP
lP
lP
morphine struch
3truchr
el
el
Removal of 3,4 cpoxidebidge in
ew
ew
rCsult
result in he Conpoind that is efered to
ye
ar
ar
morphinans
C
C
as
preparcd:ynthetikally
Morpkirons ate
butorphanol
eq- levorphanol,
Moxphine analoques
a
a
rm
rm
Morphie
ha
ha
ha
sulphate,
lP
lP
lP
trucure-
el
el
ctt
ew
ew
ar
ar
H
C
Ho oH
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 27 of 76
ew
ew
ar
ar
.I
C
ottls
ot tla NH
a
a
Ho
rm
rm
CH m-ne thoy phenglclkyl mine
ha
ha
ha
CooH
3,u- cimethoxy phenlacete atid

lP
lP
lP
el
el
AlH ordcasatin
THF
ew
ew
ar
ar
C
oH
C
Ho
a
Codeine
rm
rm
sHN/H demethlaton
ha
ha
ha
lP
lP
lP
el
el
ew
ew
ar
ar
C
Ho OH
"maphinme
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 28 of 76
ew
ew
ar
ar
Mechonisni ofhon
C
opioidTeeplor aqmist broin
Mouphine acts a
-
by Coupling ih
th col
coln
Jhere by,i 3houos
attio:
with he he preteins
a
a
chones
rm
rm
chonne
the calciuM
his Esuls
eSu lS in pyoducing
ha
ha
ha
morphine
cntaqortist Proper fes of
lP
lP
lP
ope
el
el
rties
ew
ew
white oystolve
exists as a hide oy) almost
St
ar
ar
CololorlessSilk nee dles co) Cubial masies
on
C
C
poder
oudder
ethnol
- Soluble in walrsiqhtly 3olubeM
i
m taulene
and imsoluble
a
a
rm
rm
ToT the educton of boih, arute

-Morpkine is Used
ha
ha
ha
lP
lP
lP
oMd ckroric pai
the 3mpbms of shoshess
el
el
Educinq
-
Sti Used in
ew
ew
as an oplate ubstitrton,
of beath. and ed
ar
ar
heropj
C
Ave1se stfecis
anstipatlon, hoimone imboloce, addictiovn,.( tmparment

a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 29 of 76
ew
ew
ar
ar
C
C
a
a
rm
rm
ha
ha
ha
lP
lP
lP
el
el
ew
ew
ar
ar
pers beconve
of tolexonce
C
C
human pertovmance,
dependent he moyphine
a
a
rm
rm
ha
ha
ha
lP
lP
lP
el
el
ew
ew
ar
ar
C
C
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 30 of 76
ew
ew
ar
ar
C
C
a
a
rm
rm
ha
ha
ha
Codeine
lP
lP
lP
el
el
CH
ew
ew
ar
ar
N
C
C
a
a
rm
rm
-0 OH
ha
ha
ha
lP
lP
lP
el
el
ew
ew
ar
ar
C
C
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 31 of 76
ew
ew
ar
ar
Mechanisnn of actian
C
or opioid Yeceptor
eleche aqonist
t i a
SCceptots esponsible for

he transin
Cau
Opold
siqma thsaughd the bd, codeine bind
an
a
a
of
rm
rm
and produces effec
these ecertbrs
th
ha
ha
ha
td Conversion
due
lP
lP
lP
odeme anolaesic Propeity
el
el
in to
mMoxphine inside
he d
ew
ew
Mopetis
ar
ar
C
C
i (olosless to hitecstokine olid
-9t
Soluble in water
-3t is
a
Jt i used to selievetYom mild to

to modetotrly
rm
rm
poin
ha
ha
ha
Scvese
lP
lP
eftecis
lP
dverse
el
el
hock, espivatoy irculoto deprevbn, cardioc arest,

ew
ew
droasmess, Nausea, Vomi ting, Suoeatnq, Je daton, dizzine

ar
ar
C
Costipation, viCuphoia, diayThoea, anoueia, dy mauth,
oniety, innia et
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 32 of 76
ew
ew
ar
ar
Meperidme onaloque 5:
C
onaloques
SAR of neperidine
a
a
rm
rm
ha
ha
ha
N-R
lP
lP
lP
Ru
el
el
ew
ew
Placement. o qoup on the phenl
m-Iudrol
ar
ar
C
C
nccasesS activitu
he pie sence of phenyl andster 9To4p at, " ,
opfimum
Posiclon of 1-methulpipe s eine Tesulis in
a
a
rm
rm
of mepevide
pheng qalp
ha
ha
ha
-Jhe seplbcemen? of (-4
lP
lP
lP
atalkql and helen
ydronen alkyl, other anl,
el
el
TCduces analqesle actvity.

ew
ew
Cycic9ups
g to he rolidine
the olidine
ar
ar
ontrac ton of pipeidine

C
mote active Copound, D Causes

gives
ause Iabihiy
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 33 of 76
ew
ew
ar
ar
ubotitution of carbelhoy 910up in 1meperidme
ubotitufion b
C
axloy g10upprovides betler analqesi as rlas
Spumolyti acdudy
talargement6f pperiene ring to a me mbeted
a
a
rm
rm
louw
hesahydroazepine yield active Compounds wilh
ha
ha
ha
incide of side e ftects
lP
lP
lP
Anileicneydiahoide
el
el
ew
ew
tudure
ar
ar
C
c-H C
a
a
rm
rm
:
ha
ha
ha
1e
NH2
lP
lP
lP
Mechonism
gton
el
el
-
ew
ew
receptor Produer
binds uwith
protein and
ar
ar
negotive naptic transmiss'ns Via pro

and
C
the effecor proteins

whch acto tes
indracellutar CAMP
Drug also decse ases the
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 34 of 76
ew
ew
ar
ar
rihbtnq adenylole clase 6nyne
C
heve drea çasc in hedelease Vasepre s sin
Sonalostam , iksuln and qucagn and the xelease
Sme
ome
t.e
a
a
neutotanaille15 - are also inhbitcab
rm
rm
Topeitle
ha
ha
ha
lP
lP
lP
yellaoish white CIyptalhine
der
el
el
shghly 3oluble in uner, soluWe
in
ew
ew
Vey
ar
ar
alcohol omd chovotoim
C
C
ses
- is USed in the reotment and
and manaqement
of Systeic ain.
a
a
rm
rm
a used nocotic anolge sic

ha
ha
ha
Adverse efects-
lP
lP
lP
-Respiratory depresion, dizzim depession,
el
el
coma,
ew
ew
weakness, fointness visual proble ms

Sedation,
ar
ar
Dipkerolateydiochloside -
C
tructure
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 35 of 76
ew
ew
ar
ar
C
C
O
N
C-H
a
a
rm
rm
-CEN
ha
ha
ha
lP
lP
lP
el
el
ew
ew
action
Mechorisn of
ar
ar
which
acts as opiale
opiate Cceptor aqonist decieaes
C
C
the peristalsis ie
and Consrict. the sphinctre y
stimularting the mu receptor in C
- 42
also ha a divect effect OM circular Imooth
a
of bouwel ahich Tesulis in seqmentatio

rm
rm
muscles f
of the I tansit time

ha
ha
ha
prolo nga tion
lP
lP
lP
1oPeyties-
el
el
poudar
ohite almostwite Cnstalime
3 isa er)
ew
ew
paringlu Solublein: alcohol, Ve Slightly Soluble in

ar
ar
chloride
C
methylene
C
Dater4reely Sduble im
Uses
s Usedas analgesic9et
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 36 of 76
ew
ew
ar
ar
teatmet of djoyrhoea
-t the
C
wed in
Advetse effects
(Orfusion, headache,
-Nousca, Vomtitiutq, estlesshe,
chanqes in moocd, X055 o ape
tomock
a
a
dsotout,
rm
rm
shorthe33 of
of breath ett
eic
rashes, hives, tcng
itching,
ha
ha
ha
erlanl itote
lP
lP
lP
el
el
tructue
ew
ew
ar
ar
C
C
oH
CooH C0oH
CooH
a
a
rm
rm
ha
ha
ha
lP
lP
lP
Mechortism of acton
el
el
the opioid receptors

binds wth
ertonl J
ew
ew
are oupled with -proteins this sesub

ar
ar
ohich
C
actnotion of the opioid Teptos Causes GTP

iN
to be
exchanged b COP on the piotein
vequlates adenylate
usther down clase
Jhs
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 37 of 76
ew
ew
ar
ar
which iM tum duces the cAMP Concertroho
ie
C
cANMP
ArMP deperndontinflux., of calciumons into the
-
cel b educed
3 due to
uhibition o the neve otivity
a
a
rm
rm
hypeipoloizaton of the cell betouse of e1ckange
erchange
ha
ha
ha
(TP tox GDP
lP
lP
lP
ot
adynthesi
el
el
ew
ew
ar
ar
+HN
C
C
-estaylpiperidin-y-one ani line
a
a
rm
rm
N-
ha
ha
ha
lP
lP
lP
el
el
ew
ew
ar
ar
C
Hentanyl
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 38 of 76
ew
ew
ar
ar
0perties
C
-34 isa white (O)
almost hite solube
pauvdeSolub,
n oales ieely Joluble in mcthanol and spa

and Jpoi,
Jolube alcohol
a
a
rm
rm
a
ha
ha
ha
ond
. USe
potent naucotic.analgesic da
lP
lP
lP
On adjunci os qCnesal Tegionalanaethesia
el
el
Adverse
ew
ew
fecs
ar
ar
Siarhea,
Diairhea, Noweg,Nomiinq, dy mouth, Conusion,
C
C
Constipation, di2zines nevousness, oniety deptesin,
artigue, head oche ete
Lope ramide hyorochloride

a
a
rm
rm
iruetuE
ha
ha
ha
lP
lP
HO
lP
el
el
ew
ew
N
CA-H
ar
ar
C
N
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 39 of 76
ew
ew
ar
ar
Mechonidn acorn
C
(alcium chanel blocke
operamide is Movi- Jclective
intestinal motilitq ond ofecis wter
sloas the,
,,
clectolyte nmovemnt hr ough the kouel
a
a
d
and
rm
rm
inhibited
Jeistaltic tivity b direct actinq
ha
ha
ha
chmulos and dongitudimal
chu on the
of he
lP
lP
lP
of he intestol ui
el
el
Mustles
ew
ew
Yopeakies
ar
ar
white almost ohite poutdes, Jliqlrtly
-ib a or)
C
C
and
Soluble inwater, teelyJoluble inalcohol
mecthanol
',)
a
treatment of ciaarhea
9t Used to the
rm
rm
i
diarrhea in
,
patients with
ha
ha
ha
treatment of on-qol
lP
lP
lP
nflmmatoy bowel dbcase
el
el
Advese effecs
ew
ew
D22zines5
Mziness, diouasmess3, constipation, Nouseo, thedhe,
ar
ar
C
Vomiting,it abdominal pain, tainting, allegie actions,

ash etc
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 40 of 76
ew
ew
ar
ar
C
C
Meperidine hydhochloide
a
a
tucture
rm
rm
ha
ha
ha
,
lP
lP
lP
el
el
ew
ew
C-H
/
ar
ar
C
C
N
Mechonism ot acton
a
a
rm
rm
ceptor. aqonist
-32i a kappa -opiarte ie
ha
ha
ha
reLcptoy and produces
-Ahnds wth apsotein ,
lP
lP
lP
el
el
tansmission Via apro-

negativeJnaptie
ew
ew
positive arld
ald
ar
ar
he effector proteins
actvates he
C
teim whikh
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 41 of 76
ew
ew
ar
ar
C
C
- Binding also timulotes
enchange o1
of G7p
GTP
Uof drug
Complex
(n DP on C protein
a
a
rm
rm
OPesties
ha
ha
ha
pscsent he
the fom ofsolid nd
lP
lP
lP
in
el
el
oater
Joluble in
ew
ew
ar
ar
Ases
C
C
-St used relieve roM mode rato to
Sevese poîn
-3t
a
eryt
rm
rm
used becbre amd afle. 3urqer

ha
ha
ha
Ad effects rti
lP
lP
lP
-Repatong
el
el
depresolon, Shock dradsMe55, Nausea,t

ew
ew
arest, 3weating, Jedation, dizzine:

ar
ar
Vomitmg,
Vomitin Cardiac
C
Consipation, euphoria, diohea aniety dy mouth et

a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 42 of 76
ew
ew
ar
ar
C
C
M
ethodone arnaloque5
met hadone analoques

AR
ace tylation ot tesul
keto 0nd
e ductiono
a
a
acetyl mcthodot
rm
rm
hudaoxy oup qiVeS he
shorpy
ha
ha
ha
Shorply
an o e
phenyl qToup
Kemovol of an
lP
lP
lP
deceases he ativit
el
el
phenl ding
ew
ew
Place mend of m- hyesory 9roup in he
ar
ar
dectcases Onalaesic activity
C
C
he levo -isomer ot methacdone and isome thodone
ATe twice as effechve as heir 10cemíc mi tute

a5
-ubotiduton of teminal dimethylanino goup

poup
a
decie ases ac tividy

rm
rm
Pigerdne gTOup
ha
ha
ha
Metbadonelgduochlaide
lP
lP
lP
true luse
el
el
ew
ew
ar
ar
C
H -H
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 43 of 76
ew
ew
ar
ar
ayrhesis
C
-Ht N
C
a
a
CN
rm
rm
2-chloro-N,N-timethyl popas
2,2- diphenylacetontitile
-amime
ha
ha
ha
1.NaNtiz
lP
lP
lP
el
el
ew
ew
ar
ar
C
C
,
CN
cg &
a
a
rm
rm
ha
ha
ha
lP
lP
lP
el
el
-N
ew
ew
4i{
ar
ar
wmetha dome
C
acharism action
Methadone full agmist activity at the
the
hous
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 44 of 76
ew
ew
ar
ar
Opioid Teccpor ohich is he mcthanom
puimay mehanis
C
0r the thcatme nt
o pain
agonis tos kappa and
dctS aS 0
Sigma opiold irccpious wth in, tha pesipheral and
a
a
rm
rm
CNS
ha
ha
ha
- Methodote for N-methy-D
also an
attoist
lP
lP
lP
sportorte
Cceptos
el
el
ew
ew
TOpestics
ar
ar
31 b a ahite almost shile.cstalline puddeo
C
C
Arecly Soluble ethonol and Joluble in ates
t io wed in the theatment of Voviouus

pins
a
a
rm
rm
the tre athnent ofaddklion to opioids

and
ha
ha
ha
Juch he1oin
0s
lP
lP
lP
AdveiseHecis
el
el
Kightheadedness, Vomirtina Constipat

ew
ew
-bi22încss, Nausea,
ar
ar
mouth, droasiness, drouasines5 Confusion, Maod

dy
C
tircdness, eiqh los5 alleg oc tons,

changes
appetite inf
Joss
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 45 of 76
ew
ew
ar
ar
yogoxyphete ydrochloride
C
K
a
a
rm
rm
ha
ha
ha
C-H
lP
lP
lP
el
el
ew
ew
Mechonise acion
ar
ar
C
C
octs a weak avntaqonist oP, 0Pf
of3 eccptoi5 with in he CNS
binds with -proleín' eceptor and produces

- Jt
a
ond eqative Jyna pte tansnisions Via G-poten

poi five
rm
rm
uhich acdvates he
he effecdor pro ten
ha
ha
ha
Stimulates echange
lP
lP
Binding of drug aluo of

lP
el
el
GTP for CDP on he a-prote'm,: complex.

ew
ew
1OPe des
ar
ar
C
-St is white (OT) almost white Ctalline poudn
So veiy soluble nn atey 0ndreely Soluble in
alcokol
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 46 of 76
ew
ew
ar
ar
Uses
C
mild to modealtpain
is Used o Cortrol
other oMalqes5 kovina

having
a used to olo
with
Propeadles
Gmtiintlommoton nd antipyietic
a
a
rm
rm
has Hte ontitussive- activit
ha
ha
ha
Adyese effects
lP
lP
lP
Dizzmes5, comstipation, itchinq, Naue
el
el
diousnes5,
ew
ew
Nonvong impolied "alestness tt
Jove throat,
ar
ar
9Morpha
C
C
deivotives
AR enzomorphan deivotuesen2azoctnes)
a
2R2
rm
rm
)3
ha
ha
ha
lP
lP
lP
cH3
Ho
el
el
he timethy Conounc is moi octive hon. dinme

ew
ew
Contpound
ar
ar
C
-ocement of Nphenyl ethyl Tesults

L
n mose activ
N-methyl Conpound
hon
Placement of meth 91oup in 9h position

iio
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 47 of 76
ew
ew
ar
ar
ac ivity however O qTup deneases thc acb
the acbvi
he
C
N-allyl 0 N-ychopopl methl gioup tonfeis alaqoisde
andogai,
octid
ettozocine
a
a
rm
rm
dtuctuve
ha
ha
ha
,
lP
lP
lP
el
el
ew
ew
-CH3
ar
ar
C
C
CH3
Ho
Mecharis action
antagonizes the opioio
Pentozocine elftts
a
a
rm
rm
Compe ting at the seceptor site, mainly Compete

ha
ha
ha
he
dhe opioid eceplos site
lP
lP
lP
opesties
el
el
-St a
ew
ew
white coy almost hite puoderpoing

ar
ar
Soluble in toatev, Solube in etovol and patingy

C
Soluble in methlene chloside
Uses
t 1 a synthetc analgesic 2gent
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 48 of 76
ew
ew
ar
ar
Rdvese elHcis
C
tizzmcs5 Castipation, tirrdnes, xosk
neS5, dhousinc 33,
Stomoch
ock poin, upue lighlheadrdnes ond
stonach
chongc3
ete
a
a
rm
rm
evophanol artarale
ha
ha
ha
irucduse
lP
lP
lP
el
el
OH
ew
ew
OH
Ho
ar
ar
DH
O
C
C
OH
Mechanom
o1 actit
ike other M-agonit opioids, b belive b
a
a
rm
rm
act ot Keceptos i the Peiiventiculor and

ha
ha
ha
perioquedurtal qroy motte in both the "bo in f
perceptv
lP
lP
lP
spinal coTd to alter he tranamiion ond
el
el
pain
0t
ew
ew
ropesties
ar
ar
Rgt 15prEsentin the oum

otstals and is
and
C
i
water spotng soluble alcohol,
soluble in,,
insoluble
p1octcally in ether
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 49 of 76
ew
ew
ar
ar
C
C
a
a
rm
rm
ha
ha
ha
lP
lP
lP
-J b wed o treot
el
el
Modeiae to SCVe Te
ew
ew
ar
ar
pain
C
C
Adve1se effecls
-Nousca emesis, di2ziness, Tespixatory depiessi on,

a
a
rm
rm
hypotension urnan setenton, cardac arhythmias

ha
ha
ha
alleiqic Teattons, skin ash, Futtoria.
lP
lP
lP
el
el
ew
ew
ar
ar
C
C
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 50 of 76
ew
ew
ar
ar
Norcotic antagonists
C
Novcolics se lieve prin 0nd ofle
of.
or diug hat
nduce
lcep
Noicotic wheh black the
a
a
antaqonists are diugs
rm
rm
elferts of nodotics
ofher
ha
ha
ha
o1nd
ymptoms in he
he
lP
lP
lP
-Ohey olso
precipitate toithdiowl
el
el
Marcotic
addict
ew
ew
Valoxone hydhochloride
ar
ar
ucure
C
Ct C
a
a
rm
rm
Ho HCA
ha
ha
ha
lP
lP
lP
Ho
el
el
Mechenism ofachon
ew
ew
-4t shoiusantogonistie etfecds bindin

k
ar
ar
C
opioid sceptoss
he
- moinly
binels uoth -opiofd Teteptos, ut
also binds kappa and gamma leceptors

Can
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 51 of 76
ew
ew
ar
ar
oper tieg
C
white co almost white hyg1030 opc custaline
i
wate1, Jolube in cthanol,
de Soluble i in
insoluble im Toulee
a
a
rm
rm
ha
ha
ha
wed in'diagnosing an oVeidose of qpioid
is
lP
lP
lP
Advesse effecis
el
el
ye
ew
ew
nose, oteig
- body aches, evet, Suea tinq,
ar
ar
weakness, Mousea, dianr hea, Vomitinq, Spasms eezig,
C
C
Nervousness c0
Nolovphne kydockoide
tuctone
a
a
rm
rm
:
ha
ha
ha
lP
lP
lP
CR-H
el
el
ew
ew
OH
ar
ar
Mec honism of action

C
opiod
-3t acts on Teccptos
on -reccpto antaqonistie elfects

a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 52 of 76
ew
ew
on
ar
ar
shous high efkoy 0qorist
on kappa eceplos, it
C
eerts
.
T0pe T ies
-tis odouless, tolline poader

a
a
whrle co love d,
rm
rm
and is Solube in ate dilte alkoli
h droxide
ha
ha
ha
Solution in.chlorotoam and ether
olufion but insoluble
lP
lP
lP
el
el
ew
ew
St ed to ieot Monotic induced Tespiratonu
ar
ar
depiesson
C
C
Advesse
effecis-
-Artiely, hallucinoton, (onduson, dyphona
Levallorphon tortorate
a
a
rm
rm
tructure
ha
ha
ha
lP
lP
lP
el
el
4
ew
ew
ON
HO
ar
ar
Ho
C
lechanicm of action
Jevolorphan antoq oni2es opioid etfecs b
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 53 of 76
ew
ew
ar
ar
Conpe tvng SaMe eceptis" Jites
C
Jiopeties
J4 i hite Colored ,odourleas Custalinc Pauder s
slightly Joluble
inun er,, but, injoluble, in
a
a
rm
rm
ethe and chloiofoum.
ha
ha
ha
-t
lP
lP
lP
is used in, the yeatmentof Ttspiratory depes
el
el
ion duc to narote overdoses
ew
ew
Advense effects
ar
ar
C
C
dysphosia, ethorqydizziness,, drassine35, gastric, upsc
Sueating Mouseo, ett
Anti- Irflommatony ggents i.

a
a
rm
rm
-Non-uteroidal ati-intlam ntatoy drugs NSM0) are

ha
ha
ha
he treotme nt paw
widcly Wed ofminoi
lP
lP
lP
ovld the manaqement of edema aindfisue
el
el
a
ew
ew
from itlamnatony joint diseae

danaqe xesuldng
t1
ar
ar
(ondhrrts).
C
Classrication of NTATD
.
o alicylic acid derivotives -ospirin, Salsolate

a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 54 of 76
ew
ew
ar
ar
MP-Amino phenol deiivatives5paiacetampl, pheacein
/mino
C
Yqo2obdinc dione deivalivespheag biloone, 0jenb
Antkioikeacid derivaitves- metencmic acid 20e

meclefenon
A alkandc adddeinrve
a
a
rm
rm
a Indole acetic acid indomethacin
ha
ha
ha
Sndone acelic atid Sulindac
lP
lP
lP
acetic ocid- tolmein, Zo1mipirot
Pyriole
el
el
ew
ew
phengl acetic rie-ibupnol en, iclofenot, ketornl
Oxicamg piroxicam meloxicam, cnotiom

ar
ar
C
C
Vl Sclectve Cox2 inhibltots ofecosib
iii) Cnolu Compounds - aurono in
4) MscelaneousNob mebne
a
)arug used ingout- allopurinol.

rm
rm
odium
ha
ha
ha
saliculote
lP
lP
lP
tructune -
el
el
irdfniC00 Nat
ew
ew
iv
OH
ar
ar
C
Mechanism ot chon-
inhibits he eleose t on
4 iasta qlondin
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 55 of 76
ew
ew
ar
ar
logether leukin p
withnter
added
C
mibiton of
also cQUses a Coridentation deprndent
3t
Cox-2 ativity
opestics-
a
a
5oluble in uotex,
rm
rm
a white Cngstalhne Prvde,
-9t is
ha
ha
ha
Soluble in alcolol
3pain
lP
lP
lP
USIS
el
el
to fever and tos the elief f
ew
ew
St b used
ar
ar
,
i
C
C
actoms
posses5 anti-inilemmatony
olso ,
Advese effcts
cromps allergic
- Nousea,.Yotng heartbum Stomath
onemia, hives ho _spasm,
bioncho
bronc span,
a
nVes,
eac to,g Maysea ,tchinq,
rm
rm
redne35, Stomach ulceis ele

ha
ha
ha
Skin
lP
lP
lP
Apinn
el
el
ructure
ew
ew
yOH
ar
ar
C
achon
Mechanism of
aceyl qroup 'ot aceyl salcule ad binds
Ohe
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 56 of 76
ew
ew
ar
ar
kreveisiblu Icdure of (o
wjth; Stine CNm
C
dhich ineversible hibition, due
inhibition,
de.
Meads to, ls
kis paim produt ing prastoqlonhs pridu ction is
Prevented
a
a
rm
rm
opestics
a
ha
ha
ha
ukide cnstaline uodes,ligktly.3oluble. n
0oter
lP
lP
lP
and 3olu ble ih alcohol
el
el
ew
ew
-t used fo e ehef of minor aches and
ar
ar
mil to maderate pain
C
C
-t Stdin myocatdial
focfon
Advesog
lfecd
heort buan, Jtmoth upset, Nousco,
hi ting, tirednes
a
dizziness, dark uine abdominal 'palh.vi

rm
rm
pole Skim,
Metenomic acid
ha
ha
ha
lP
lP
lP
Atrucluve-
el
el
ew
ew
ar
ar
C
Mechanism tacton
binds wth Cox-1 ond
cox-2 and inh bit
inhbipi
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 57 of 76
ew
ew
ar
ar
Hhe ar tion f prosiglndin ynthetase
C
ue to tis the level of prosoqlordns decaeaser
and the synptoms of pain a tempo1oil iedu ced
dunthesis-
a
a
rm
rm
OK.I
ha
ha
ha
lP
lP
lP
+
CH3
el
el
potassium 2-branobenzarte Ct3
ew
ew
2,3- dimethyl benzanomine
ar
ar
C
C
ChCocu
OH
o
a
a
rm
rm
N
ha
ha
ha
lP
lP
lP
metenoni acid
el
el
0peuties
ew
ew
-9t is white o-off white nstallime paisder 5oluble

ar
ar
C
of alka hydhozides, spariqly Joluble

in 3olution
elhetshghdhy 3olyble ethonol.
Mses
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 58 of 76
ew
ew
ar
ar
ancd onti indbmatony,
ano lqeoic.
C
31 b sed aS
Advese efeeis
Jkin Yayh, changes

shosine
sofbreatk
breah,
Taundice, pale skin

Jkin
Nouseo,
ACight qam, Suoel
a
a
rm
rm
Anenia, tremos, drvoSihes di2zines5 ct
ha
ha
ha
Meclefenomate
lP
lP
lP
lructuxe
el
el
ew
ew
ONa
ar
ar
C
C
Mechanism action
-inhibits he snthesi of prostaqlancin and o
a
Competes br bindng: at heprosoglandin ecepbr

rm
rm
Site
ha
ha
ha
roperies:
lP
lP
lP
he
el
fom
el
pesent in Jolid
ew
ew
41 isouble in OTqanic 3olvents Such as elhas

ar
ar
DMSOl
C
Usrd as analacSond anti-mflammaby
agent
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 59 of 76
ew
ew
ar
ar
Aavese"feei 1
C
diorqheo, speh
9an, NouUea, skin Tashy anemid,)
0
.
Conluson dito sines
oundit e Pale iskiMCAshpatin
1dneligeipgthe
d hess head athes ollcge eocion3,
a
a
rm
rm
4Hdowmethatin .ui,
ha
ha
ha
.
lP
lP
lP
str.
1 Coo
el
el
C
ew
ew
ar
ar
C
C
Machanim action
a
a
rm
rm
-Sndome thacin onspacitic and T2VeTsible inhoitor

ha
ha
ha
of he
of cyeloo1ygenuse (Cox) enzine
lP
lP
lP
Jndome thacin inhbts both the bofomof cox:
el
el
dhuyha
ew
ew
GO1-Land Cox 2, brt hiher

ar
ar
Selecdnhj r he cox- Tecaptors oich isb

esponsb
assti
C
e oT the increase advase elfects of dug

t
OPertie5
St 15
t13 a wte ellow
o)yellow cayallme pouder obvde
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 60 of 76
ew
ew
,
ar
ar
woter ond paglyoluble alceho
C
ti9 uwedir as
ian ti- ntlardnätoy an
and onl
anb
eiseeffeciyja l
a
a
gatric dbdders, "headochey
rm
rm
"laad ider th
allerqie
allerqic
ha
ha
ha
YEactonsavet, dizaines, Nousedo itng
Ving,
lP
lP
lP
pale skin, anemid dianhea, Cokne3, soe wat
wat eic
ele
el
el
ulindae
ew
ew
Hucdre
ar
ar
C
.C
a
vS
rm
rm
Mechoriam
o action ())
ha
ha
ha
simgarl
inhibtsbothco
lP
lP
and
lP
CoL-2 enzumes whic
futher leads to the
el
el
nhibiton of protaglondin
ew
ew
Synthesis
synthesis th isesponsibieo he anti-intlom
ar
ar
action o drug
C
e Cnipyvetic actin ofdrug

hypothalamus
is due ocn acion
whick
dug esut increase
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 61 of 76
ew
ew
ar
ar
og tpu ,Wasoliloton ànd iurquent hegt adoaipoi,
C
ie- ti i
LSt is a iyelo caystallie derNEr
poud aligatiy
soluble in water 3oluble in, melhylene. thoride

a
a
rm
rm
ytonsof olkalhydotide s,' parinl
on3
eil
ha
ha
ha
cohol,
de al
lP
lP
lP
el
el
mog t poten lantinfiammn actv
L4tn hasil
ew
ew
f
- also havng anclgesic, antipyretc PTopeit
is
ar
ar
C
C
Advese gfecis
-Nauseo
reactuns;
dvease
digcae uperten šion, modd 1choresalegic
stomach kicney probleds
a
upset
rm
rm
Jolme ton
ha
ha
ha
truture
lP
lP
lP
el
el
ew
ew
Cop
ar
ar
CH
C
CH3
Mechaniom
of action
TOStuglondw yrthelasË" entue i1 mhidtea i

a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 62 of 76
ew
ew
ar
ar
oetin shidk, lowero the pladmlevel1of p
C
Ahis
veophnisible fo
he anti inflammacbjiu act
of
a
a
3t is a, crestaline) podet
rm
rm
lihtb yellouo Jolele
in water, shdtlyolube
ha
ha
ha
ho A
lP
lP
lP
Uses
,
el
el
ontyacbe, onalqes. jondyinant:inthmai,
ew
ew
octionu
ar
ar
dvese elects
C
C
Nausea, i VoMitng, hegsllunin,djarhkd dizzihes
headathe, hypertertsinj modi kne ver diene
A\le1qic seactions
a
a
rm
rm
omepriac
ha
ha
ha
vuclure
lP
lP
lP
el
el
HO
ew
ew
ar
ar
O
C
of action
Mechanism
h 1
A irwbts prostaglandin Jynthetasdi enzumehich
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 63 of 76
ew
ew
ar
ar
MunCoultsin deerease] poduchin proto
C
Pglaglondiy.)
Sanals thyaugh out 1he
bd
a
a
rm
rm
ha
ha
ha
-t piegent i in the tonRf.i olid p0nd
lP
lP
lP
in methonol ethoroli,gnd hot p
opropi
heloluble,
el
el
Cetone, chlororbi m sigtl' solue
ew
ew
M
inJoluble in taulene et
ar
ar
in ethe and praLtikcally
:
C
C
Uses
(
wed as an analqesieand attinhlammoto
N
drug
a
Aavetse ettects
rm
rm
Naused, Vomitinq, alleqie Tealtions, suria, uríd,

ha
ha
ha
Jumptoms.
lP
lP
roqein tal
lP
el
el
Dicloferac
ew
ew
tructuae
ar
ar
C
NH
oH
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 64 of 76
ew
ew
ar
ar
lechori of atton:i t
C
inhibita caloggenase" (cöt-iand
ic lofenac cox-)
of pras
okich
tu derea hepduc bo
"
dins
a
a
-rasaglaind
rm
rm
trarnmasano
ave épon'sible for' the
ha
ha
ha
paiynand
andintlanimaton ond thi ieduc the
lP
lP
lP
Omount ot pros tagqlandinu iel in1edue thelp
el
el
and
ew
ew
ilammatn he "bd
ar
ar
3pesties
C
C
t isa white or) 3liyhtl yellbtsish erstoline
sliahtk hyqr0.3t.opic puode 5parg 3oluble in
nter Solube inmethanal and alcool shqtly

a
a
rm
rm
Jolubde,, n
ha
ha
ha
sdenfnts
lP
lP
lP
-t is uGed in he theatmentof Theumatic
el
el
Carhitis D1Sol
ew
ew
Advee effect
ar
ar
aiarhea 1
C
- Nausea JArowsiness
Vormi fing
upsetstomqch head ache
buin dizness
heart Alletqic reacdos
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 65 of 76
ew
ew
ar
ar
Kotorla " 'a
C
Hucture
HO
a
a
rm
rm
N
ha
ha
ha
lP
lP
lP
MechoriSm
of action
el
el
-
ew
ew
non sele ctively inhibits co F. cos-2 enymes
ar
ar
whch ase Yesponsible fos the 3yntheJi, oprotam
C
C
ondins
ee duced leveofprogtàglondns TSponsibe for
Controling theh. Mfohmation and
.
pain in the bo
a
a
rm
rm
Operties
ha
ha
ha
-9t ia a white cnystalline pawdeSoluble in ter
lP
lP
lP
ad n methanol, slighty! i cthongpractal iwolude
el
el
chloride
in methlene
ew
ew
Mocs
ar
ar
treatmeat
C
gotent ana lqesic nased in the
of modesateSevee and acutC pal
Adverse gffeclstu
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 66 of 76
ew
ew
ar
ar
Skin weiqht nain eling
kn bash,
ash, chonges sin Vision
.
C
Nausca, pale skin, anemia, dzzines
dizzines,
Ca,Jundice,
hcadache, Suendng,CtusinVomiting etuj
bupolen
a
a
tuctue
rm
rm
ha
ha
ha
ctly
lP
lP
lP
CH3
el
el
ew
ew
,y
ar
ar
unihe sis
C
C
J-soutyl benzene
a
a
rm
rm
s q
ha
ha
ha
.
lP
lP
lP
el
el
ew
ew
-4-isbrl phengl ) eihanane

ar
ar
NaCN
C
Supiolen
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 67 of 76
ew
ew
ar
ar
opertes
C
white cHstaltine powder co1) colorles st
tisa in acetone,
Joluble
prattalky mduble in water
'
methatol methylené' chonde

a
a
rm
rm
scs
ha
ha
ha
avni-inladinm aiou, antpyede
- 3t 13 ued 'as
lP
lP
lP
ara loesic diug
el
el
ew
ew
Meckarism acton
that me
ar
ar
se lectve I'nhi bitor,
-Jhupsoten 15 a,, Mon Co
C
C
itiwhibtb both Cox- aMdT CoX-2 Cnzymes
- Co-2 .
inhibitionleads todecre ase inproducten o
'
of prastuqlandinswhich 5 repansile he
a
signels in the body and

rm
rm
transrnicslonM of pain
ha
ha
ha
inflammatoM
me diartimg teveri and Sueling.
lP
lP
lP
Adveiseeltecis
si
el
el
-
Rlerai Teactons oss of appebte
ew
ew
i
- Skin Taactons Taundice Constipotio
ar
ar
pale Skin
- MiSion, di2zmess
C
chonqes
- Nausea
ane mia head ache
4C1 l:
Nausea
upsetstomach i
diarhea Vomit 'eil i Si
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 68 of 76
ew
ew
ar
ar
NapioXen
C
tructule
a
a
rm
rm
ha
ha
ha
Mechorism
of acton
lP
lP
lP
JNopio1en,
el
el
inhibits C0 2 Cnzume ichi vesults
ew
ew
decnaase ofpros taqlondins ohich
in productiono i
ar
ar
-
Tesponsible
fo Conveyimqopainand intlomai
intlammarion
C
C
STqnals M the
d, ,
t olso mhibis Cox Cozume which 15 Sespo
ble he side effects at drug ike ChI

a
a
rm
rm
ulce rabon
ha
ha
ha
Y1opetiey
lP
lP
lP
Custalnepandepiac
-Jt is a ohite
tital
el
el
insoluble in wateT
inthano
ew
ew
Joluble and in
ar
ar
methanol.
C
Ises
pasSess analgesid
ni
"ontinflantmaton and
antipyredc actions
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 69 of 76
ew
ew
ar
ar
C
C
-Aleale ieoc tions, Skin eattiois heenfburn,
eiht g
Voofiting, one
aneri,
vi ehangcs, "indijesbon ple3k
dizzines, headathe, ele
Vomitinq,
a
a
Nausea,
rm
rm
Proxicom
ha
ha
ha
pTruC ture
lP
lP
lP
el
el
N t o'H i
ew
ew
NH
ar
ar
C
C
Mechanism action
.i
-4t
t veveisibly inhibits Cycbo1yjenare enume ohich
a
a
rm
rm
inhibition otprostaglandin 3nthesis

Cases perieral
ha
ha
ha
also pievenis the gga to due to platelets
lP
lP
lP
through inhibtng the iqrator of the Deukayles
el
el
into site of intlammotói " whicH prvënt

the the
ew
ew
fDImaton "ofthromboxòne A
ar
ar
C
ope ties
a wnlte ol slighily yellociystolline ,
pouder pracd ally iniokle mates, 3qlub in
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 70 of 76
ew
ew
ar
ar
hethylene chlarlde andhahilu' sol be, metha
C
ses
Jtsse d "
i"heik tieamentb of oeoaslhiti

heumatid ,
arlhviris
i 3i
a
a
-
rm
rm
also posses urido3urit cachon) cndhas e
ha
ha
ha
Used in thetreament o, acute geyt y
lP
lP
lP
Aveise elfects-
el
el
Nausea, upsetstomag; drbuasine
drou)hes3 33,
Nauea, dizziness,
ew
ew
heod
heod acke,
ache, hyperiension, Yomitina, pale skin, dark uing
ar
ar
C
C
allerq eochons, mood,choncset,d
henacetin*
tructure
a
a
rm
rm
ha
ha
ha
N
lP
lP
lP
' Hinu
el
el
Mechanism,w,
gAto o
ew
ew
-Jt produces acton ons Sensontracts of he

ar
ar
coTd and producesanalgesigeffact

phal
C
proouces epressanta
-1also acthons on the heat
y acting inotropieagent
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 71 of 76
ew
ew
ar
ar
produe effecb'"od the hedt-conroling
sd
olso"
C
centen he br d
ars onp1 Tu
Pioeste
te der with oi ter

|- t csiss as a qlisterim
,
a
a
rm
rm
tastePgyplule iMate end50ke
ha
ha
ha
clMorofnm
lP
lP
lP
el
el
as an arnalqesic(and attirešc
ew
ew
Jtis uscd
ar
ar
Advese effecis
C
C
- Naisea Vomitinq, allerqic tactons, cólon Cance, blado r
gilc 1
iteistitial nephitis
Cance
Acctomino phen
a
a
rm
rm
ha
ha
ha
lP
lP
lP
el
el
ew
ew
ar
ar
Mechanis action
C
-t inhbits cyclooygenase coxi scox-1)?Gih in

PToduchionM of prastaqlonsins
tATM deCicases the
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 72 of 76
ew
ew
ar
ar
Prastanlon dins hard sprsble or thetroaamiss,a
C
of Painadd tlommation, dhus Yeduc
Yeducing
imq
Amousrt
ofppotoqlandint
h"
TeducMq
th i
andInommadn hebg
a
a
rm
rm
Aceloninophenalso selicdrely inhibits A
Co
ha
ha
ha
Anrtipuiete I
actionn. a dru is dug to cliectoci
lP
lP
lP
ofthe drug
druq o the hent - 1aqulatinq Cantres
i
el
el
he brain
ew
ew
ic
OPeite
ar
ar
C
C
1iot as
hie ystalme,. padesSpatin
oluble n water Joluble in alcohol 0Md ve
li.
Joluble meulene chloide
,
a
a
rm
rm
-Abused for he tyeatwmenrt

of
mildt moca
ha
ha
ha
and
is ued
pains to seduce" ever
lP
lP
lP
Advese gllect
el
el
Vontring
ew
ew
-
Nause0, cilevc TCacions inamnid
Antpyrine
ar
ar
C
bucue o
-
,
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 73 of 76
ew
ew
ar
ar
Meckonioe action
f
C
thev:NŠ, ete
ašing
-Antipyrine artpritmail tin
'of
thresold by nhibmg bothh idofofns
ther pitl
enzyne
CyclooxygcAase, Co-1,coM- codgsl
a
a
rm
rm
involved posq landi synthesty
. 1p!i
ha
ha
ha
ogerhe 1 1
lP
lP
lP
Coloyless (ustollime powder (01)
availoble as
-4t i
el
el
i Hovinglighly"pl
ew
ew
white pouo der oduufless
'e
ar
ar
bittersie i
C
C
Areely
treely Soluble atei, altohol ati* chodoforn-
3t
analqesis," onliinhf lammiartopyi and antipreHe

-Jthoas
a
a
rm
rm
activides
ha
ha
ha
Advese eHects
lP
lP
lP
buining tingmg' TCdhes, Me aMl 1,in und
el
el
heears Huish skin 3evere firedne5, eakoey.

ew
ew
henlbutazone
ar
ar
C
tuc tur
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 74 of 76
ew
ew
ar
ar
Mechon acton"
echonln of 1
C
henlbutadonebindstnond jnattvatesi prsto
din H oM
dlt pratarujc iM yathasd., thyovi
ynthdse
a
a
PeToxide mediateddegctvar tion1 N
rm
rm
he veduced of. pióatogbndi lends
ha
ha
ha
lP
lP
lP
seduced in lomma tion of tissue
Suroundingtisue
el
el
ropeties , iola
ew
ew
ar
ar
-
S isit a whte, cusalhde poloderpgctieal
C
C
.
soble M water paiingly 3olube ni,.alcoho,
and Soluble Iali akalme Soy R
ses
a
a
rm
rm
-Jt, has iartipy rcdoyilañalqesiie ci antjintlomnt

ha
ha
ha
lP
lP
lP
ac
hons
el
el
Advase effecto
ew
ew
ar
ar
- Nausea, Vomitin dasThacay, edema Skin ,,1ashe

V
C
izziness arolsfnasoheadadhe
lured vision
aplastic anemia.
a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 75 of 76
ew
ew
ar
ar
Kle ot nzume JHlaation
C
COX
Cox iderrbfied
-Jwo isoenymes have boen
COX Cox-2
tunchiors ot
a
a
Cox-1 intluences the house keepin
rm
rm
prostaqlandins
ha
ha
ha
axe
invalved
lP
lP
lP
|-Cox-2 M inflommatos process that
prastoglandins
el
el
mediated by
ew
ew
Ae major mechanim by ohich the NSAT D, ali«t
ar
ar
C
C
their the rapeutic effecb (onipyrete, analqesic
anti jntlom madoy a tvities) is inhibition ot prastaqlan-
din (Pa) sunthesis

a
-4enerally. the NsATD mabit both and

rm
rm
CoX-1
ha
ha
ha
COx-2
,
lP
lP
are
lP
-Most, NsATD mdimly Co-1Jelectve.
el
el
-Other mechoniss That mayConti ute to NsATO

ew
ew
avti-infbmnmarb'y actvty include the reduetion of

ar
ar
C
Supe io xide radicals nducton of agoptosis, inhibrhon
of adhesin molec ule epiesionM nodiiciaton of
yonphayte ot tvity, decrease of pro-infbnmatoy

a
a
rm
rm

ha
ha
ha

P
P
l
l
el
el
Page 76 of 76
ew
ew
ar
ar
C
C
a
a
rm
rm
ha
ha
ha
lP
lP
lP
el
el
Cytokine levels deciease of nirit 0ide 3jnthae
ew
ew
ri
ar
ar
function.
Ond alteo thon o celular membrane
C
C
a
a
rm
rm
ha
ha
ha
lP
lP
lP
el
el
ew
ew
ar
ar
C
C
a
a
rm
rm

ha
ha
ha

P

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This Notes is Provided by Chandan MOCP

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Provided By - Chandu Brother

She ass ot sensalion is teymed a

eneral onaesthe tics bring abaut descendng

of he CNS, 5tarting ith the Ceseba

Shese are nin Sugkal peraton

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Provided By - Chandu Brother

-Uhis period rom he begimming of

35 throuqh a stage irtegulosadh spechc

beathing the veestablishment

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Provided By - Chandu Brother

otage eitement i Jost and skeletal

espivatoy and Civculadony arlure occur 1inthis

h Snhatotion nena oMaesthetiçs

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Provided By - Chandu Brother

y Non- baubrierales- pnopenidid,popotol

should be potent and Mon- intlammable

oity 94 should be rol- isritating to nacous

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Provided By - Chandu Brother

vhbit the cilatony NMDA,-pe of qlutome

seceptor, ohich belongs

in the NeuronsS andleads to eurtal hupespolar

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Provided By - Chandu Brother

due to The Ne£TVE.

arnd Codiac (onttractithy*

-41 binds ith potasslum channeLs and pT0duces

bind witha NMDA and

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Provided By - Chandu Brother

unction channel opein

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Provided By - Chandu Brother

seceplo13, qlutonate veceptn3 qlcin

Ttceptovs NADn dehydrbgeroe

and muscle elosaton. featne

-Nephuotosicity, lo fotal hepatetesidy

produces depressiveeffects by bnding oi

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toilh calt ium channels

myocasdial oxygen Cosumption, maligrant

Pevelurone june don chonnel

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Provided By - Chandu Brother

Aevoluane also bmas oith D subuait ef Ap su

diy mauth, nsomnia

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ater, Misxible wth, cthanol and ichlo1ecthylene.

4sofuräne i uSed,tor induc ton and: maintainance