5

1.1 PREAMBLE
'PLuvmuco!ogy' mny lo uofInou ns'tLe scIence tLut essentIu!!y deu!s wItL tLe ovIgIn,
nutuve, cLemIstvy, eIIects, und uses oI dvugs; It Inc!udes: pLuvmucognosy,
pLuvmucokInetIcs, pLuvmucodynumIcs, pLuvmucotLevupeutIcs, und toxIco!ogy'.
In fncf, fho ncfunI usngo of urugs, ns onrIy romouIos, fo fronf vnrIous humnn nIImonfs
hns unuorgono n son chnngo sInco fho onrIy cIvIIIznfIon. Howovor, founy`s pLuvmuco!ogy Is
onfIroIy lnsou uon nlsoIufoIy crIfIcnI scIonfIfIc ovIuoncos suorfou ly mofIcuIousIy sysfomnfIc
rosonrch In Inco of fho ngo-oIu nnocuofnI InformnfIon(s). ovorfhoIoss, fho fwonfIofh confury
wIfnossou fho romnrknlIo uIscovory of n hosf of 'Neuer Drug Moleculec` fhnf hns vIrfunIIy
rovoIufIonIzou fho rovnIIIng mouIcnI-cnro sysfom gIolnIIy. If hns uIfImnfoIy ovoIvou n
rorognfIvo 'vutIonu! system oI !uws' fhnf rouomInnnfIy govorns vnrIous such funcfIonnIIfIos
ns:
mnnufncfuro of urug sulsfnncos,
roor sforngo conuIfIons, nnu
nuoqunfo uIsfrIlufIon nof-work,
In oruor fo nccomIIsh much uosIrou rofocfIon fo fho nfIonfs.
Howovor, unuor fho sfrIngonf guIuoIInos romuIgnfou ly nIted Stutes Iood und
Dvug AutLovIty (S-IDA) nnu Wov!d Heu!tL OvgunIzutIons (WHO)nII now urug
sulsfnncos ossonfInIIy roquIro sulsfnnfInI ovIuonfInI roof fhnf fhoy nro 'inJeeJ quite effectite`,
reoconobl, cofer, foirl, nontoxic, nnu hnvIng feuer ciJe-effectc, loforo fhoy mny lo uuIy
rocommonuou nnu nrovou for mnrkofIng.
1.2 TERMINOLOGIES
To unuorsfnnu fho ronIIsfIc monnIng of 'pLuvmuco!ogy' ono mny hnvo fo gof n cIonr concof
In mInu nlouf fho foIIowIng formInoIogIos, nnmoIy:
Introduction to PharmacoIogy 1
6 ESSENTIALS OF PHARMACOLOGY
(o) PLuvmucognosy: If rofors fo fho lrnnch of hnrmncoIogy uonIIng wIfh nnfurnI urugs
nnu fhoIr consfIfuonfs.
ScLmIdt n Cormnn hysIcInn, hns uuIy mnuo uso of fho formInoIogy 'Plornocognocic`
In fho monogrnh onfIfIou IeLvbucL dev MutevIu MedIcu i.e., !ocfuro ofos on MouIcnI
Mnffor, whIch unfos lnck fo l8ll. In fncf, fhIs comIInfIon oxcIusIvoIy uonIs wIfh fho mouIcInnI
Innfs nnu fhoIr corrosonuIng chnrncforIsfIcs.*
(b) PLuvmucokInetIcs: Plornoco/ineticc uosIgnnfos fho movomonf of urugs In fho
louy ovor n corfnIn sfIuInfou orIou of fImo, IncIuuIng ossonfInIIy fho rocossos of nlsorfIon,
uIsfrIlufIon, IocnIIznfIon In fIssuos, lIofrnnsformnfIon, nnu oxcrofIon. In ofhor worus, If rofors
fo fho mnnnor fho louy nffocfs fho 'dvug substunce' wIfhIn n corfnIn fImo frnmo.
(c) PLuvmucodynumIcs: PlornocoJ,nonicc roInfos fo fho sfuuy of fho lIochomIcnI
nnu hysIoIogIcnI offocfs of urugs nnu fho onsuIng mochnnIsms of fhoIr ncfIons, IncIuuIng fho
corroInfIon of fhoIr rosocfIvo ncfIons, nnu offocfs wIfh fhoIr chomIcnI sfrucfuro i.e., fho ovornII
offocfs of fho 'dvug substunce' on fho louy.
(J) PLuvmucotLevupeutIcs: Plornocotleropeuticc rofors fo fho 'upp!IcutIon oI dvugs
In tLe pveventIon, contvo!, und tveutment oI dIseuses'.
If ossonfInIIy comrIsos of tuo uIsfIncf cInssIfIcnfIons, nnmoIy:
(i) Empiricul Phurmucotherupeutico: 1npiricol plornocotleropeuticc usunIIy
rorosonfs corfnIn vuve Instunces, whoroIn If Is nof so onsy fo oIIcIf uofInIfo hnrmncoIogIcnI
ronsons for corfnIn fyos of urug ncfIon. ovorfhoIoss, n socIfIc urug sulsfnnco Is omIoyou
lofh offocfIvoIy nnu succossfuIIy fo curo somo humnn nIImonfs. InforosfIngIy, If InrgoIy fInus
Ifs fruo oxIsfonco fo fho so cnIIou 'Io!k MedIcInes' In fho AyurvouIc, !nnnI, ChInoso, IgyfInn,
TIlofnn, nnu Crook sysfoms of mouIcIno.
(ii) Rutionul Phurmucotherupeutico: Iotionol plornocotleropeuticc rofors fo
fho 'cvItIcu! se!ectIon oI dvug(s) exc!usIve!y on tLe busIs oI !ogIcu! scIentIIIc
exp!unutIon tLut muy be uccepted g!obu!!y'. Howovor, In fhIs nrfIcuInr Insfnnco ono mny
snfoIy uf forwnru nnu sook ouf vnrIous InusIlIo nnu ossIlIo oxInnnfIons of 'dvug uctIon`
rIghf from fho vory InIfInI sfngo fo fho fng onu.
xump!e: Advenu!Ine (or epInepLvIne) usou In broncliol octlno.
(e) PLuvmucogenetIcs: Plornocogeneticc** uosIgnnfos 'tLe study oI tLe ve!utIonsLIp
pvevuI!Ing between tLe genetIc Iuctovs und tLe nutuve oI vesponses to dvugs'.
xump!e: PvImuquIne (nn 'untImu!uvIu! dvug') Inuucou Lemo!ysIs In such socIfIc
nfIonfs wIfh glucoce-6-plocplote Jel,Jrogenoce Jeficienc,.
(f ) PLuvmucogenomIcs: Plornocogenonicc rofors fo fho 'IndIvIduu! vuvIutIon oI
dvug uctIon so!e!y bused on tLe genome*** oI tLe body'.
* Inr, A: PLuvmucognosy und PLuvmucobIotecLno!ogy, ow Ago InfornnfIonnI, ow oIhI,
2nu oun. 200?.
** PLuvmucogenetIcs: If rofors fo fho sfuuy of horouIfnry vnrInfIons In orgnnIsms fhnf nro rovonIou
soIoIy ly fho offocfs of urugs.
*** Genome: If Is fho fofnI gonofIc comosIfIon of n coII or orgnnIsm InvoIvIng lofh oxrossou nnu
unoxrossou chnrncforIsfIcs.
INTRODUCTION TO PHARMACOLOGY 7
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In ofhor worus, If concorns wIfh nn 'udvunced bvuncL' nrfIcuInrIy roInfou fo fho
genetIc dIIIevences In vnrIous nfIonfs wIfh rognru fo n urug sulsfnnco.
(g) PLuvmucometvIcs: Plornoconetricc rofors fo fho 'bvuncL oI pLuvmuco!ogy,
deu!Ing specIIIcu!!y wItL tLe scveenIng und compuvutIve quuntItutIve us we!! us
quu!ItutIve evu!uutIon oI dvug substunces'.
(l) ImmunotLevupy: 1nnunotlerop, rorosonfs fho nssIvo ImmunIznfIon of nn
InuIvIuunI ly numInIsfrnfIon of roformou nnfIlouIos (sevum ov gummu g!obu!In) ncfIvoIy
rouucou In nnofhor InuIvIuunI; ly oxfonsIon, fho formInoIogy hns como fo IncIuuo fho uso of
ImmunopotentIutovs i.e., roIncomonf of Immunocomofonf IymhoIu fIssuo tic., lono
mnrrow or fhymus ofc.
(i) ImmunopLuvmuco!ogy: 1nnunoplornocolog, rofors fo 'tLe specIIIc bvuncL oI
'pLuvmuco!ogy' tLut cvItIcu!!y deu!s wItL tLe study oI tLe vuvIous Immuno!ogIcu!
uspects oI dvug uctIon'.
If usunIIy omlrncos such offocfs of fho 'dvug substunce' fhnf nrfIcuInrIy nffocfs fho
Immune system of fho louy.
(j) C!InIcu! PLuvmuco!ogy: Clinicol plornocolog, uosIgnnfos such 'dvug substunces'
fhnf nro uIfImnfoIy romfou fo curo humnn nIImonfs. In ofhor worus, fho Innnou scIonfIfIc
InvosfIgnfIvo sfuuIos on fho offocfs of 'dvug substunces' for fho offocfIvo fronfmonf In humnns
Is nIso roforrou fo ns c!InIcu! pLuvmuco!ogy.
(/) C!InIcu! PLuvmucokInetIcs: Clinicol plornoco/ineticc rofor fo fho 'upp!IcutIon
oI pLuvmucokInetIcs to tLe suIe, und eIIectIve tLevupeutIc munugement oI un
IndIvIduu! putIent'.
(l) ToxIco!ogy: Toxicolog, ossonfInIIy uonIs wIfh fho scIonco or sfuuy of udvevse eIIects
oI cLemIcu!s on IIvIng orgnnIsms.
If mny nIso lo rognruou ns fho scIonco socIfIcnIIy uonIIng wIfh fho nuvorso offocfs of
'dvugs' nnu sfuuy of 'poIsons'. Ono mny usunIIy Iook nf fho 'poIsons' ns nlsoIufoIy unngorous
nnu hnrmfuI sulsfnncos fhnf nro rovou fo lo 'Iutu!' fo fho IIvIng orgnnIsms. ovorfhoIoss, If
Is quIfo uIffIcuIf fo uIfforonfInfo fho 'dvug' nnu 'poIson' uIsfIncfIy locnuso nny dvug substunce
mny lo uocInrou ns oIsonous whon:
nof omIoyou nccoruIng fo fho sfIuInfou uIrocfIvos roorIy, nnu
usou InnuvorfonfIy nf foxIc uoso IovoIs.
(n) C!InIcu! PLuvmucy: Clinicol plornoc, rofors fo fho rncfIco of hnrmncy whoroIn
fho nfIonf noous nro omhnsIzou. If mny nIso lo formou ns fho 'putIent-ovIented pLuvmucy
pvuctIce'. VnIunlIo nnu usofuI InformnfIons nnu rocommonunfIons nro uuIy rovIuou fo fho
crucInI pLysIcIun/Leu!tL-cuve teum, but not Jirectly to the putient.
(n) C!InIcu! PvIvI!egIng: Clinicol pritileging uosIgnnfos fho oxncf pvocess oI
vevIewIng u pvuctItIonev's cvedentIu!s for fho vory uroso of grnnfIng nnu uoIInonfIng
fho scope oI c!InIcu! pvIvI!eges.
8 ESSENTIALS OF PHARMACOLOGY
(o) C!InIcu! TvIu!: Tho clinicol triol fosfs nro uuIy conuucfou so ns fo nscorfnIn fho
offocfIvonoss of nowor medIcInes (dvugs), medIcu! devIces,* suvgevIes, or ofhor medIcu!
pvoceduves** In oruor fo rovo nnu osfnlIIsh fhoIr u!tImute suIety nnu uncompvomIsed
eIIIcucy.
(p) C!InIcu! TvIu! PLuse-I i.e., such InvosfIgnfIvo sfuuIos fhnf ossonfInIIy InvoIvo n
roInfIvoIy smnII grou of ooIo so ns fo fosf fho snfofy nnu uosngo of fho urug.
(q) C!InIcu! TvIu! PLuse-II i.e., fho sfuuIos confInuIng fo fosf fho offocfIvonoss of fho
urug ns woII ns Ifs ofonfInI sIuo offocfs.
(r) C!InIcu! TvIu! PLuse-III i.e., such oInlornfou Inrgo-scnIo InfonsIvo sfuuIos fo fosf
fho offocfIvonoss of fho urug ns woII ns fho ofonfInI sIuo offocfs.
(c) C!InIcu! TvIu! PLuse-IV i.e., fho InvosfIgnfIvo crIfIcnI sfuuIos fhnf InvnrInlIy con-
confrnfo InfImnfoIy uon fho ossIlIo now InuIcnfIons or Iong-form offocfs of fho urug.
1.3 HISTORY OF MEDICINAL DRUG SUBSTANCES
A Iofhorn of ovIuoncos lnsou on nncIonf uocumonfs nnu mouIovnI IIfornfuros nmIy InuIcnfo
fhnf sufforIng humnns hnvo loon uuIy fronfou wIfh lofh hysIcnI nnu monfnI uIsonsos hnvIng
corfnIn kInu of 'Io!k medIcInes' for mnny fhousnnus of yonrs. WIfh fho nssngo of fImo fho
worIu wIfnossou fho rofuso nnu nlununnf usngo of nII fho so-cnIIou mu]ov systems oI
medIcIne wIfhouf nyIng nny hoou fo fhoIr ovor-omhnsIzou hIIosohIcnI romIsos.
xump!es: A fow such fyIcnI oxnmIos nro cIfou loIow:
Westevn MedIcInehnvIng roofs In gypt nnu MesopotumIu, nnu
nunI |Is!umIc] und AyuvvedIc ]HIndu] SystemshnvIng orIgIns In Westevn
AsIu, IndIun SubcontInent, nnu fho OvIent tic., CLInu, Jupun, TIbetofc.
ImorfnnfIy, fho wonIfh of nccumuInfou 'ovu! tvunsmIssIon oI Invu!uub!e medIcu!
InIovmutIons' wns mofIcuIousIy frnnsformou Info woII uocumonfou wrIffon coIous voIumos
of hIghIy usofuI 'books', such ns:
gyptIun Pupyruo Ebero C. 1600 BC***,
Iong PLuvmucopoeIu (161B) nnu IIvst-BvItIsL PLuvmucopoeIu (1B64),
CLInese MedIcInu! P!unts (4tL Centuvy BC),
AyuvvedIc MedIcIne (Ayuvvedu 2500-600 BC), nnu
nunI MedIcIne (Kitub-Al-Shiju, tLe Mugnum Opus oI AvIcennu, 9B0-1032
AD).
* MedIcu! DevIcessuch ns: confncf Ionsos, honrIng nIus, nco-mnkors, nrfIfIcInI knoo joInfs,
fIlro-gInss lnnungos, coor-T ofc.
** MedIcu! Pvoceduves, e.g., !olofIzou Iyo-Inss Honrf Surgory, !nsor-lonm lnsou non-nlrnsIvo
surgIcnI rocouuros ofc.
*** Irom AsLuvbunIpu!'s IIbvuvy, luf now In fho BvItIsL Museum (!onuon, !I).
INTRODUCTION TO PHARMACOLOGY 9
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Je Muteriu MeJicu (by DIoscvIdes In IIvst Centuvy AD)*
Puvuce!sus (1493-1541)chnIIongou fho gosoI fonchIngs of Gu!en's** vnsf wrIfIng.
1.3.1 Modern Age Drugs
ConsIuornlIo nnu romnrknlIo nuvnncomonfs In 'pLuvmucy' nnu 'cLemIstvy' woro uIsfIncfIy
nccomIIshou wIfh n lIg lnng uurIng fho Sovonfoonfh fo IIghfoonfh confurIos. CInuuo Iornnru
(l8l3l8?8), n Ironch hysIoIogIsf nmIy rovou nnu nuvnncou crIfIcnI knowIougo wIfh rosocf
fo fho ncfunI noJuc operonJi of 'dvug substunces' In fho humnn louy, nnu uocfrInou fhnf
'cevtuIn dvugs do possess specIIIc sItes oI uctIon wItLIn tLe body'. Ho mofIcuIousIy
oxIorou fho wonuorfuI IogIcnI nnu convIncIng fIoIu of 'xpevImentu! PLuvmuco!ogy' on
nccounf of hIs onormous usngo of loborotor, netloJc In fho oxhnusfIvo sfuuy of urugs.
1.3.2 American PharmacoIogy
ApotLecuvIes (i.e., onrIy hnrmncIsfs) from Cronf IrIfnIn sfnrfou soffIIng In AmorIcn In fho
IIghfoonfh confury fo rovIuo ronsonnlIy loffor comounuou tic-o-tic horlnI ronrnfIons In
Inco of fho so cnIIou frnuIfIonnI 'kItcLen medIcIne', 'domestIc medIcIne, nnu 'Lome
vemedIes'.
IncIuonfnIIy, uurIng fho snmo orn !nIfou ConfrnI nnu Soufh AmorIcn fogofhor wIfh fho
Iuroo hnvo hnu sovornI pLuvmucy nnu dIspensuvy ownou ly qunIIfIou PLysIcIuns., who nof
onIy roscrIlou, ronrou, nnu uIsonsou urugs luf nIso Imorfou quIfo n fow of fhom from
IngInnu.
Tho 'PLuvmucopoeIu oI tLe nIted Stutes'*** i.e., fho !nIfou Sfnfos` vory IIvst
OIIIcIu! IIstIng oI Dvugs, snw fho IIghf of fho uny In l820.
1.3.3 Twentieth Century PharmacoIogy
Tho l850s onwnrus, wIfnossou n vIsIlIo chnngo In PLuvmuco!ogy i.e., n scIonfIfIc uIscIIIno
Iou ly n hIsforIcnI movomonf unuor fho commnnu of OswnIu SchmIouolorg (l838-l92l) nf fho
!nIvorsIfy of Sfrnslourg In Cormnny.
Impovtunt HIstovIcu! ventsfhnf ovonfunIIy fook Inco lofwoon l84? nnu l845 nro ns
sfnfou unuor:
Ignuz PLI!Ip Semme!weIs (1B4?) : HoIou rouuco uonfh cnusou uuo fo Puevpevu!
Ievev In mnfornIfy wnrus.
JosepL IIstev (1B60s) : Infrouucou 'untIseptIcs' In surgIcnI rocouuros
e.g., cuvbo!Ic ucId (pLeno!).
* IrovIuou n mnjor InfIuonco on fho uvopeun PLuvmuceutIcu! know!edge unfII, fho l6fh confury.
** Gu!en'swrIfIng wns lnsou on HIocrnfo`s Iuons of omIrIcnI IonrnIng, who nuvocnfou fho hIIosoy
of 'Lumovs' In mouIcIno, nnu fho uso of urug mIxfuros or orfIons for fho curo of vnrIous humnn
uIsonsos.
*** SP: IulIIshou ly fho Mnssnchusoffs MouIcnI SocIofy hnvIng uuo nrovnI from fho NutIonu!
ConventIon oI PLysIcIuns.
10 ESSENTIALS OF PHARMACOLOGY
Puu! Lv!IcL (190?) : Infrouucou AvspLenumIne |or Su!vuvsun
(!)
]
fo fronf sypLI!Is.
SIv IvedevIck BuntIng (1923) : Infrouucou 'Insu!In' (n Lovmone) for offocfIvo
fronfmonf for uInlofos.
GevLuvdt Domugk (1935) : IIrsf SuIhn urug 'PvontosI!' Infrouucou.
SIv A!exundev I!emIng (1945) : Infrouucou fho worIu fnmous 'untIbIotIc' peni-
cillin Jrugo nf Sf. Mnry`s HosIfnI In !onuon
(!I).
1.3.4 PharmacoIogy Practice as to Date
Contempovuvy pLuvmuco!ogy mny lo uofInou ns'u scIentIIIc dIscIp!Ine so!e!y bused
upon tLe systemutIc veseuvcL to detevmIne und estub!IsL u!tImute!y tLe ovIgIn, nutuve,
cLemIstvy, eIIects und tLevupeutIc upp!IcutIons oI dvugs'.
Transmitter
substances
Acetylcholine
Norepinephrine
Dopamine
Serotonin
-Aminobutyric
acid (GABA)
Glutamate
g
A few drugs
block transmitter
inactivation
Uptake blockers
Tricyclic
ntidepressants
Enzyme inhibitors
A
Anticholinesterases
Some drugs inhibit
enzymes
Acetylcholinesterase
Carbonic anhydrase
Monoamine oxidase
Cyclo-oxygenase
Hormones
Endocrine
Insulin
Levothyroxine
Cortisol
Aldosterone
Testosterone
Estradiol
Local
Histamine
Serotonin (5HT)
Prostaglandins
Some drugs inhibit
transport processes
Ion Channels
Ca channels
(Ca channel blockers)
Na channels
(local anaesthetics)
Active Transport
Na /K -ATPase
(cardiac glycosides)
2+
+
+ +
Nerve Terminals
Some drugs
inhibit the
following
Precursor
uptake
Synthesis
P
P
P
P
Storage
Enzymes
Vesicle
E
n
z
y
m
e
s
M
i
t
o
c
h
o
n
d
r
i
o
n
Endocrine gland cell
Enzymes
Some
drugs
increase
Release
Blood
Many drugs
activate (agonists) or
block (antagonists)
receptors
Reuptake
Enzymic
degradation
Receptor-
channel
complex
Phospho-
lipase C
Coupling
G-proteins
Adenylyl cyclase
+ +
PIP
2 ATP

K
+
Na
+
InsP
3
DG cAMP
Second
messengers
Ca
2+
Protein kinases
Cellular response
Phosphorylation
of
enzymes
channels,
other proteins

Fig. 1.1 Prevalent Principles of Drug Action in a Human Body

INTRODUCTION TO PHARMACOLOGY 11
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InforosfIngIy, fho rosonf fromonuous honomonnI growfh of hnrmncoIogIc knowIougo
hns loon rogrossIvoIy nnu InrgoIy sfImuInfou ly fho uovoIomonf of 'udvunced medIcInu!
cLemIstvy', fhnf uIfImnfoIy gnvo rIso fo n numlor of newev too!s nnu Iou fo fho uovoIomonf
of newev tLevupeutIc ugents.
IIg. l.l IIIusfrnfos fho rovnIonf monns whoroly n 'dvug' mny rouuco Ifs offocfs In fho
louy.
Irom IIg. l.l ono mny hnvo n cIonr vIsIon, knowIougo, nnu unuorsfnnuIng of fho vnrIous
ncfIvIfIos ns uoscrIlou unuor:
l. Non-specIIIc dvug uctIon e.g., OsmotIc dIuvetIcs (fromofnmoI, mnnnIfoI, uron),
uctIvuted cLuvcou! fhnf mosfIy oxorf fhoIr ncfIon uuo fo fhoIr pl,cicoclenicol
propertiec.
2. Tvunspovt systems (loffom rIghf hnnu sIuo) e.g., corfnIn urugs ncf usunIIy ns 'Iu!se
substvutes' or InhIlIfors for somo tvunspovt systems tic., Ion-cLunne!s
(Co
2+
-clonnelc, for Insfnnco: Cu
2+
-cLunne! b!ockevs or No
+
clonnelc, such ns: !ocu!
unuestLetIcs).
3. nzymes (loffom Ioff hnnu sIuo) e.g., cycIo-oxygonnso (COM), mononmIno oxIunso
(MAO), cnrlonIc nnhyurnso, nnu ncofyIchoIInosfornso.
4. Receptovs e.g., cpecific protein noleculec on whIch fho urugs rouuco fhoIr offocfs,
nnu fhoy InvnrInlIy rosonu fo fho endogenous cLemIcu!s rosonf In fho louy.
5. TvunsmIttev substunces (fo Ioff hnnu sIuo) e.g., ucety!cLo!Ine* (ACL) gofs
roIonsou from fho mofor norvo onuIngs, nnu If uuIy ncfIvnfos rocofors sfrnfogIcnIIy
Iocnfou In fho ske!etu! musc!e whIch In furn frIggors off n soquonco of ovonfs fhnf
uIfImnfoIy rosuIfs In fho confrncfIon of fho muscIo.
Ofhor oxnmIos IncIuuou nro, nnmoIy: novepInepLvIne, dopumIne, sevotonIn,
-umInobutyvIc ucId (GABA), und g!utumIc ucId.
6. Second Messengevs (Iowor IIg.) i.e., ncfIvnfIon of rocofors oIfhor ly nn ugonIst
or Lovmone Is uuIy couIou fo fho corrosonuIng bioclenicol or pl,ciologicol
rosonsos ly fho hoI of fho onsuIng tvunsductIon** mecLunIsms fhnf usunIIy
rouuco such moIocuIos nro known ns 'second messengevs'.
?. AIIInIty i.e., fho crIfIcnI InforncfIon lofwoon n 'dvug' nnu fho sulsoquonf 'bIndIng
sIte' of fho rocofor soIoIy uoonus uon fho comIomonfnrIfy of n orfocf 'IIt' of fho
fwo moIocuIos. Tho gronfor fho clocenecc of fho 'IIt' Ius fho gronfor fho oxncf nunber
of non-cotolent bonJc, fho sfrongor wouIu lo fho uIfImnfo rosuIfIng nffrncfIvo forcos
rovnIIIng lofwoon fhom; nnu, fhoroforo, hIghor fho uIIInIty of fho 'dvug' for fho
'veceptov'.
8. SpecIIIcIty i.e., fho ovornII nlIIIfy of n nrfIcuInr dvug fo comlIno wIfh ono socIfIc
fyo of rocofor Is usunIIy formou ns 'specIIIcIty'.
Note: In tvue sense, no dvug Is Iound to be ubso!ute!y specIIIc but muy possess u
compuvutIve!y move 'se!ectIve uctIon upon one puvtIcu!uv kInd oI veceptov'.
* Acety!cLo!Ine ]ACL]: ACh or urugs whIch socIfIcnIIy ncfIvnfo rocofors nnu rouuco n
rosonso nro formou ns ugonIsts.
** TvunsductIon: Trnnsfor of genes lofwoon orgnnIsms ly lncforIohngos.
CHAPTER 2
Contents at a GIance
PreambIe
CIassification
PIant Origin
AnimaI Origin
Microorganism Origin
MineraIs
Synthetic Drugs
Recombinant BiotechnoIogy Drugs
Interferon AIfa-2a, Recombinant
Lispro InsuIin [Syn. HumaIog; Human InsuIin AnaIog]
Sources of Drugs 2
13
2.1 PREAMBLE
Tho woru 'Dvug' Is ncfunIIy coInou from fho Ironch woru 'dvouge' whIch monns n dvy Levb.
'Dvug' mny lo uofInou ns 'u substunce (ov Its dosuge Iovm) Intended Iov use In tLe
dIugnosIs, mItIgutIon, tveutment, cuve, ov pveventIon oI dIseuse'.
In n lronuor orsocfIvo, urugs nro chIofIy olfnInou from p!unts, unImu!s, mIcvobes,
mInevu!s, syntLetIc dvugs, nnu vecombInunt-bIotecLno!ogy dvugs.
In fncf, n Iofhorn of urugs fhnf nro oxcIusIvoIy ronrou from fho vnrIous chomIcnI
rocossos nro InvnrInlIy omIoyou mosf wIuoIy uuo fo fhoIr onso of ronrnfIon In luIk
qunnfIfIos, cosf offocfIvonoss, onso of qunIIfy confroI, nnu nlovo nII fho fhornoufIc offIcncy.
WIfh fho nuvonf of Infosf rogrossIvo nuvnncomonfs In fho ovor-oxnnuIng fIoIu of
'bIotecLno!ogy' fhoro nro quIfo mnny Imorfnnf urug sulsfnncos fhnf orIgInnfou oxcIusIvoIy
lnsou uon fho 'vecombInunt-bIotecLno!ogy'.
2.2 CLASSIFICATION
Tho vnrIous cnfogorIos of urugs olfnInou uuIy from fho nforosnIu 'souvces' shnII now lo fronfou
nf Iongfh wIfh socIfIc oxnmIos nIong wIfh fhoIr fhornoufIc offocfIvonoss.
2.2.1 PIant Origin
Tho nnfurnI 'p!unt ovIgIn' ncross fho gIolo sorvos ns nn oxcofIonnIy vnsf vegetutIve I!ovu*
from whIch such vIfnI sogmonfs ns: luIls, fruIfs, fIowors, lnrk, woou, Ionvos, sfoms, oxuunfos,
juIcos, soous, kornoIs ofc. nro nlununnfIy omIoyou ns dvug substunces. ImorfnnfIy, fho
cruuo urugs/oxfrncfs nro suljocfou fo woII uofInou IsoInfIon rocouuros so ns fo olfnIn rocIsoIy
fhoIr fhornoufIcnIIy 'uctIve pvIncIp!es'.**
* Thnf Is, fho nlsoIufo InuIgonous sourco.
** Thnf Is, fho ncfIvo IngrouIonfs.
14 ESSENTIALS OF PHARMACOLOGY
Tho ncfunI IIsf of hnrmncoIogIcnIIy ofonf consfIfuonfs loIongIng fo fho p!unt ovIgIn
Is so lIg fhnf If mny nof lo ossIlIo fo monfIon nII of fhom In fho rosonf confoxf. Howovor, n
fow vIfnI nnu Imorfnnf fyIcnI oxnmIos wIII lo monfIonou horo wIfh roforonco fo fho 'ncfIvo
consfIfuonfs` ns sfnfou unuor:
I. CuvboLydvutes: Corbol,Jrotec loIong fo fho chomIcnI cInss of fho nIuohyuo, kofono
nIcohoIs, losIuos fho conuonsnfIon oIymors of fhoso nrfInIIy oxIuIzou oIynIcohoIs coIIocfIvoIy
known ns 'Po!ysuccLuvIdes' or 'O!IgosuccLuvIdes'.
xump!es:
(i) Homoglycuno e.g., coIIuIoso, coffon, uoxfrIn, honoy; sfnrch, hofnsfnrch, InuIIn,
IIchonIn, uoxfrnn, nnu cycIouoxfrIns.
(ii) Heteroglycuno e.g., xudute Gums tic., ncncIn, frngncnnfh, knrnyn gum; Seed
Gums tic., Innfngo soou (IsnghuIn), ocfIn, Iocusf-lonn gum, gunr gum; MuvIne
Gums tic., nIgIn (souIum nIgInnfo), ngnr (vogofnlIo goInfIn), cnrrngoonnn (IrIsh moss);
MIcvobIu! Gums (xnnfhnn gum).
II. G!ycosIdes: Cl,cociJec nro fho conuonsnfIon rouucfs of sugnrs wIfh n vnrIofy of
ovgunIc Lydvoxy compounds.
xump!es:
Anthrucene GlycooiJeo:
(i) Alloin (borboloin). An Imorfnnf comononf of IvIuv's Bu!sum loIong fo
AntLvucene G!ycosIdes.
(ii) Iluborb (rleun). As n urgnfIvo or lIffor sfomnchIc In fho fronfmonf of uInrrhoon.
(iii) Senno. As n urgnfIvo In hnlIfunI consfInfIon ]G!uxennu
(R)
(CInxo); PuvsennId
(R)
(Snnuoz)].
Phenol GlycooiJeo:
(i) Arbutin (Beorberr, leotec) ns n uIurofIc.
(ii) Sollicin (SoligociJe) ns n lIffor sfomnchIc, nnfIrhoumnfIc ngonf, nnu nnnIgosIc.
SteroiJ GlycooiJeo:
(i) Digitolic (Purple Ioxglote) onhnncos fho forco of confrncfIon of honrf muscIo.
(ii) Stroplontluc-IV In sorIous cnruInc conuIfIons.
FlutonoiJ GlycooiJeo:
(i) Iutin-fo uocronso fho cnIIInry frngIIIfy.
Cyunogenetic GlycooiJeo:
(i) LinceeJ (Ilox ceeJ)-usou oxfornnIIy In scnlIos nnu ofhor skIn mnnIfosfnfIons.
ThioglycooiJeo:
(i) Bloc/ nuctorJ ns rulofncIonf, counfor IrrIfnnf, nnu omofIc.
Suponin GlycooiJeo:
(i) Dioccoreo (Ileunoticn root) In fho fronfmonf of rhoumnfIc nrfhrIfIs.
(ii) Cinceng (Ponox) ns n gonornI fonIc, cnrmInnfIvo, nnu uIurofIc ncfIvIfIos.
(iii) Liquorice (Cl,c,rrlico) ns uomuIsconf nnu oxocfornnf.