adrenergicsystem-110126105226-phpapp02.ppt

8/19/2019 adrenergicsystem-110126105226-phpapp02.ppt

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Adrenergic System

Dr. D. K. Brahma

Department of Pharmacology

NEIGRIHMS, Shillong, Meghalaya


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Neurotransmission in ANS


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Noradrenergic transmission

Nor-arenaline i! the ma"orne#rotran!mitter of theSympathetic !y!tem

Norarenergic ne#ron! are

po!tganglionic !ympatheticne#ron! $ith cell %oie! inthe !ympathetic ganglia

&hey ha'e long a(on!$hich en in 'arico!itie!

$here N) i! !ynthe!i*ean !tore


4/73

Adrenergic transmission

Catecholamines:

Natural: )renaline, Norarenaline, Dopamine

Synthetic+ I!oprenaline, Do%#tamine

Non-Catecholamines: Epherine, )mphetamine!, Phenylepherine, Metho(amine,

Mephentermine

)l!o calle sympathomimetic amines a! mo!t of themcontain an intact or partially !#%!tit#te amino NH

gro#p


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/ Catecholamines:

0ompo#n! containing

a catechol nucleus

Ben*ene ring $ith

a"acent 1H gro#p!an an amine

containing !ie chain/ Non-catecholamines

lac2 hyro(yl 1H

gro#p


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Biosynthesis of

CatecholaminesPhenylalanine

PH

Rate limiting Enzyme

5-H! al"ha #ethyldo"a

Al"ha-methyl-"-

tyrosine


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Storage of Noradrenaline


8/73

Release of NA $ %eed&ac' Control


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Regulators of NA release


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("ta'e of Catecholamines


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Reu"ta'e

Sympathetic ner'e! ta2e #p amine! an relea!ethem a! ne#rotran!mitter!

("ta'e ) i! a high efficiency !y!tem more !pecific

for N) 3ocate in ne#ronal mem%rane Inhi%ite %y 0ocaine, &0)D, )mphetamine!

("ta'e * i! le!! !pecific for N)

3ocate in !mooth m#!cle4 cariac m#!cle Inhi%ite %y !teroi!4 pheno(y%en*amine No Phy!iological or Pharmacological importance


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#eta&olism of CAs

#ono Amine +,idase #A+. Intracell#lar %o#n to mitochonrial mem%rane Pre!ent in N) terminal! an li'er4 inte!tine M)1 inhi%itor! are #!e a! antiepre!!ant!

Catechol-o-methyl-transferase C+#. Ne#ronal an non-ne#ronal ti!!#e

)ct! on catecholamine! an %ypro#ct! 5M) le'el! are iagno!tic for t#mo#r!


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#eta&olism of CAs

Homo/anillic acid. 0anillylmandelic acid.


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Adrenergic neurotransmission


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) r e n

e r g i c R e c

e p t o r

!


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Adrenergic Rece"tors

Adrenergic rece"tors or adrenoce"tors are a cla!! of G-protein co#ple receptor! that are the target of catecholamine!

)renergic receptor! !pecifically %in their enogeno#! ligan! 6

catecholamine! arenaline an norarenline Increa!e or ecrea!e of n me!!enger! c)MP or IP74D)G

Many cell! po!!e!! the!e receptor!, an the %ining of anagoni!t $ill generally ca#!e the cell to re!pon in a flight-fightmanner.

8or in!tance, the heart $ill !tart %eating 9#ic2er an the p#pil!$ill ilate


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Ho1 #any of them 2222

Al"ha 3. Beta 4.

Adenorece"tors

: ;


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7ifferences - Adrenergic

Rece"tors 3 and 4. 8

)lpha 3 an Beta 4 )goni!t affinity of alpha 3+ arenaline = norarenaline = i!oprenaline )ntagoni!t+ Pheno(y%en*amine IP74D)G, c)MP an K> channel opening

)goni!t affinity of %eta 4+

i!oprenaline = arenaline = norarenaline Propranolol c)MP an 0a> channel opening


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Potency of catecholamines on

Adrenergic Rece"tors

)r N)

I!o

I!o )r

N)

3og 0oncentration

Aortic stri" contraction Bronchial rela,ation

3 4


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#olecular Effector 7ifferences

- 3 0s 4

3 Rece"tors: IP74D)G

c)MP

K> channel opening

4 Rece"tors: c)MP

0a> channel opening


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Recall: Adenylyl cyclase: cA#P

"ath1ay

PK A Phospholamban

IncreasedInteraction withCa++

Fasterrelaxation

Troponin

Cardiaccontractility

OtherFunctionalproteins

PK ) alter! the f#nction! of manyEn*yme!, ion channel!,

tran!porter!

an !tr#ct#ral protein!.

8a!ter !e9#e!tration of

0a>> in SR


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PKc

Also Recall: Phos"holi"ase C:

)P-7A9 "ath1ay


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Beta rece"tors

)ll < receptor! acti'ate aenylate cycla!e, rai!ing the intracell#lar c)MPconcentration

y"e 46: &he!e are pre!ent in heart ti!!#e, an ca#!e an increa!e heart rate %y

acting on the cariac pacema2er cell!

y"e 4*: &he!e are in the 'e!!el! of !2eletal m#!cle, an ca#!e 'a!oilatation, $hich

allo$! more %loo to flo$ to the m#!cle!, an reduce total peripheralre!i!tance

Beta- receptor! are al!o pre!ent in %ronchial !mooth m#!cle, an ca#!e%ronchoilatation $hen acti'ate

Stim#late %y arenaline, %#t not norarenaline

Bronchoilator !al%#tamol $or2 %y %ining to an !tim#lating the


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7ifferences &et1een 46! 4* and 4

Beta-6 Beta-* Beta-

3ocation Heart an ?G cell! Bronchi! uterus,Bloo 'e!!el!,

li'er, #rinary tract,eye

Adi"osetissue

)goni!t Do%#tamine Sal%#tamol -

)ntagoni!t Metoprolol, )tenolol )lpha-methylpropranolol

-

)ction onN)

Moerate @ea2 Strong


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Clinical Effects of 4-rece"tor

stimulation 46: Adrenaline! NA and )so"renaline:

&achycaria

Increa!e myocarial contractility

Increa!e 3ipoly!i!

Increa!e Renin Relea!e

4*: Adrenaline and )so"renaline not NA. Bronchi 6 Rela(ation

SM of )rteriole! !2eletal M#!cle 6 Dilatation

Ater#! 6 Rela(ation

S2eletal M#!cle 6 &remor

Hypo2alaemia

Hepatic Glycogenoly!i! an hyperlactiaciemia

4: )ncreased Plasma free fatty acid $ increased +* consum"tion -

increased heat "roduction


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Adrenergic rece"tors - al"ha

y"e 36 Bloo 'e!!el! $ith alpha-; receptor! are pre!ent in the

!2in an the genito#rinary !y!tem, an #ring the fight-or-flight re!pon!e there i! ecrea!e %loo flo$ to the!e

organ! )ct! %y pho!pholipa!e 0 acti'ation, $hich form! IP7 an

D)G In %loo 'e!!el! the!e ca#!e 'a!ocon!triction

y"e 3*

&he!e are fo#n on pre-!ynaptic ner'e terminal! )ct! %y inacti'ation of aenylate cycla!e, cyclic )MP le'el!

$ithin the cell ecrea!e c)MP


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7ifferences &et1een 36 and 3*

Al"ha-6 Al"ha-*

3ocation Po!t "#nctional 6 %loo 'e!!el!of !2in an m#co#!mem%rane, Pilomotor m#!cle !$eat glan, raial m#!cle!of Iri!

Pre"#nctional

8#nction Stim#latory 6 GA,5a!ocon!triction, glan!ecretion, G#t rela(ation,Glycogenoly!i!

Inhi%ition of tran!mitterrelea!e, 'a!ocon!triction,ecrea!e central !ymp.1#tflo$, plateletaggregation

)goni!t Phenylephrine, Metho(amine 0loniine

)ntagoni!t Pra*o!in Cohim%ine


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36 adrenoce"tors

Clinical effects

Eye -- Myria!i! )rteriole! 6 0on!triction ri!e in BP Ater#! -- 0ontraction

S2in -- S$eat Platelet - )ggregation Male e"ac#lation Hyper2alaemia

Blaer 0ontraction : arenoceptor! on ner'e ening! meiate negati'e

fee%ac2 $hich inhi%it! norarenaline relea!e


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#olecular Basis of Adrenergic

Rece"tors

)l!o glycogenoly!i!

in li'er

Inhi%ition of

In!#lin

relea!e an

Platelet

aggregation

Gl#coneogen

e!i!


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7o"amine rece"tors

D;-receptor! are po!t !ynaptic receptor!

locate in %loo 'e!!el! an 0NS

D-receptor! are pre!ynaptic pre!ent in 0NS,

ganglia, renal corte(


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Summary of agents modifying

adrenergic transmissionSte" Actions 7rugSynthe!i! of N) Inhi%ition : - methyl-p-tyro!ine

)(onal #pta2e Bloc2 0ocaine, g#anethiine,epherine

5e!ic#lar #pta2e Bloc2 Re!erpine

5e!ic#lar N) Di!placement G#anethiine

Mem%rane N) pool E(change iff#!ion &yramine, Epherine

Meta%oli!m M)1-) inhi%itionM)1-B inhi%ition01M& inhi%ition

Moclo%emieSelegiline&olcapone

Receptor! : ;: 46 4*46

Pra*o!inCohim%inePropranololMetoprolol


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Adrenaline as "rototy"e

Potent !tim#lant of alpha an %eta receptor!

0omple( action! on target organ!


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Heart

Beta-; meiate action - Po$erf#l 0ariac !tim#lant - >'echronotropic, >'e inotropic

)ct! on %eta-; receptor! in myocari#m, pacema2er cell! ancon#cting ti!!#e Heart rate increa!e! %y increa!ing !lo$ ia!tolic epolari*ation of cell! in

S)N High o!e! ca#!e mar2e ri!e in heart rate an BP ca#!ing refle(

epre!!ion of S)N 6 #nma!2ing of latent pacema2er cell! in )5N an P8 6 arrhythmia !en!iti*ation of arrhythmogenic effect! %y Halothane

0ariac !y!tole i! !horter an more po$erf#l

0ariac o#tp#t i! enhance an 1(ygen con!#mption i! increa!e 0ariac efficiency i! mar2ely ecrea!e

0on#ction 'elocity in )5N, atrial m#!cle fi%re, 'entric#lar fi%re anB#nle of Hi! increa!e 6 %enefit in partial )5 %loc2 Re#ce refractory perio in all cariac cell!


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Blood 0essels

Seen mainly in the !maller 'e!!el! 6arteriole! 6 5a!ocon!triction alpha an'a!oilatation %eta 6 epen! on the r#g

Decrea!e %loo flo$ to !2in an m#c#!mem%rane! an renal %e! 6 alpha effect ;an -

Increa!e %loo flo$ to !2eletal m#!cle!,coronary an li'er 'e!!el! - Beta- effectco#nter%alance %y a 'a!ocon!trictor effectof alpha receptor!


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Blood Pressure

Depen! on the 0atecholamine in'ol'e

N) ca#!e! ri!e in Sy!tolic, ia!tolic an mean BP

no %eta- action 6 #noppo!e alpha action

I!oprenaline ca#!e! ri!e in !y!tolic %#t fall in

ia!tolic BP 6 mean BP fall! %eta-; an %eta-

)r ca#!e! ri!e in !y!tolic BP, %#t fall in ia!tolic

BP 6 mean BP generally ri!e! !lo$ in"ection Decrea!e peripheral re!i!tance at lo$ conc. Beta

receptor! are more !en!iti'e to )r than alpha

receptor!


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Blood Pressure $ contd;

Rapi I5 in"ection of )renaline mar2e ri!e in

Sy!tolic an ia!tolic BP

3arge concentration alpha action preominate! 6

'a!ocon!triction e'en in !2eletal m#!cle B#t BP ret#rn! to normal in fe$ min#te!

) !econary fall in mean BP occ#r!

Mechani!m 6 rapi #pta2e an i!!ipation of )r 6

at lo$ conc. )lpha action lo!t %#t %eta action

preominate! 6 7ale


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7ale


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Actions of Adrenaline

Res"iratory: Po$erf#l %ronchoilator Rela(e! %ronchial !mooth m#!cle not N) Beta- meiate effect

Phy!iological antagoni!t to meiator! of %ronchocon!trictione.g. Hi!tamine 9) : Rela(ation of g#t m#!cle! alpha an %eta an con!tricte

!phincter! 6 re#ce peri!tal!i! 6 not clinical importance

Bladder: rela(e etr#!or m#!cle %eta m#!cle %#t con!triction of

&rigone 6 %oth are anti-'oiing effect

(terus: )r contract! an rela(e! Ater#! alpha an %eta action %#tnet effect epen! on !tat#! of #ter#! an !pecie! 6 pregnant rela(e!%#t non-pregnant - contract!


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Actions of Adrenaline $ contd;

S'eletal #uscle: 8acilitation of )ch relea!e in NM "#nction alpha -;

Beta- act! irectly on M#!cle fi%re!

)%%re'iate acti'e !tate an le!! ten!ion in !lo$con#cting fi%re! an enhance m#!cle !pinle firing 6

tremor

CNS: No 'i!i%le clinical effect in normal o!e! 6 a! lo$

penetration e(cept re!tle!!ne!!, apprehen!ion antremor )cti'ation of alpha- in 0NS ecrea!e! !ympathetic o#tflo$ an

re#ction in BP an %raycaria - cloniine


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#eta&olic effects

Increa!e! concentration of gl#co!e an lactic aci

0alorigene!i! 4-* and 4-.

Inhi%it! in!#lin !ecretion 3-*.

Decrea!e! #pta2e of gl#co!e %y peripheral ti!!#e

Sim#late! glycogenoly!i! - Beta effect

Increa!e! free fatty aci concentration in %loo

Hypo2alaemia 6 initial hyper2alaemia


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A7#E

)ll 0atecholamine! are ineffecti'e orally

)%!or%e !lo$ly from !#%c#taneo#! ti!!#e

8a!ter from IM !ite Inhalation i! locally effecti'e

Not #!#ally gi'en I5

Rapily inacti'ate in 3i'er %y M)1 an01M&


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Clinical =uestion8

=uestion: ) N#r!e $a! in"ecting a o!e of penicillin

to a patient in Meicine $ar $itho#t prior !2in te!t

an patient !#enly e'elope immeiate

hyper!en!iti'ity reaction!. @hat $o#l yo# o Ans1er: )! the patient ha! e'elope )naphylactic

reaction, the only $ay to re!#!citate the patient i!

in"ection of )renaline

.F mg .F ml of ;+; IM an repeat after F-; min#te! )ntihi!taminic!+ 0hlorpheniramine ; 6 mg IM or I5

Hyrocorti!one ; 6 mg


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Adrenaline $ Clinical uses

In"ecta%le preparation! are a'aila%le in il#tion!

;+;, ;+; an ;+;

A!#al o!e i! .7-.F mg !c of ;+ ; !ol#tion

A!e in+ )naphylactic !hoc2

Prolong action of local anae!thetic!

0ariac arre!t

&opically, to !top %leeing

Hyper2inetic chilren 6 )DHD, minimal %rain y!f#nction

)norectic


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CPR - )mage


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A7Rs

Re!tle!!ne!!, &hro%%ing heaache, &remor,

Palpitation!

0ere%ral hemorrhage, cariac arrhythmia!

0ontrainicate in hyperten!i'e!,

hyperthyroi an angina poctori!

Halothane an %eta-%loc2er! 6 not inicate


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+ther Adrenergic 7rugs


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Noradrenaline

Ne#rotran!mitter relea!e from

po!tganglionic arenergic ner'e ening!

1rally ineffecti'e an poor S0 a%!orption

I5 amini!tere

Meta%oli*e %y M)1, 01M&

Short #ration of action


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Actions and uses

)goni!t at :;preominant, : an


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Noradrenaline - A7Rs

)n(iety, palpitation, re!piratory iffic#lty

)c#te Ri!e of BP, heaache

E(tra'a!ation! ca#!e! necro!i!, gangrene0ontract! gra'i #ter#!

Se'ere hyperten!ion, 'iolent heaache,

photopho%ia, anginal pain, pallor an

!$eating in hyperthyroi an hyperten!i'e

patient!


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)so"renaline

0atecholamine acting on %eta-; an %eta- receptor! 6 negligi%le

action on alpha receptor

&herefore main action on Heart an m#!cle

'a!c#lat#re Main )ction!+ 8all in Dia!tolic pre!!#re, Bronchoilatation an

rela(ation of G#t

)DME+ Not effecti'e orally, !#%ling#al an inhalation ;mg ta%. S3

1'erall effect i! 0ariac !tim#lant %eta-;

Increa!e in SBP %#t ecrea!e in DBP %eta- Decrea!e in mean BP

A!e a! Bronchoilator an for treatment of )5 %loc2, Sto2e!-)am

Synrome etc. 6 %#t not preferre anymore

Adrenaline NA and


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Adrenaline! NA and

)so"renaline - Summary


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7o"amine

Immeiate meta%olic prec#r!or of

Norarenalin

High concentration in 0NS - %a!al ganglia,

lim%ic !y!tem an hypothalam#! an al!o in

)renal me#lla

0entral ne#rotran!mitter, reg#late! %oy

mo'ement! ineffecti'e orally, I5 #!e only,Short & ;4 7-Fmin#te!


54/73

7o"amine

#ECHAN)S#:

Agonists at do"aminergic 76! 7* rece"tors

Agonist at adrenergic 36 and 46


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7o"amine

In !mall o!e! -F g42g4min#te, it !tim#late! D;-receptor! in renal, me!enteric an coronary 'e!!el!

leaing to 'a!oilatation Increa!e in c)MP Recall+ Renal 'a!ocon!triction occ#r! in 05S !hoc2 #e to

!ympathetic o'er acti'ity

Increa!e! renal %loo flo$, G8R an ca#!e! natri#re!i! Interaction $ith D receptor! pre!ent in pre!ynaptic arenergic

ne#rone! 6 !#ppre!!ion of N) relea!e no alpha effect


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7o"amine $ cond;

Moerate o!e F-; g42g4min#te, !tim#late!


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>hy renal and mesenteric

/asodilatation is useful in Shoc'2

Increa!e! renal %loo flo$, G8R an

ca#!e! natri#re!i!

In 05S !hoc2 6 e(ce!!i'e !ympatheticacti'ity leaing to i!chemia of g#t,

!lo#ghening an entry of Bacteria to

!y!temic circ#lation - !epticemia

7 & t i 7 i ti f


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7o&utamine - 7eri/ati/e of7o"amine

#+A: )ct! on %oth alpha an %eta receptor! %#t more prominently in %eta-;

receptor 6 increa!e in contractility an 01 Doe! not act on D; or D receptor! 6 No relea!e of N) an there%y

hyperten!ion

Preominantly a %eta-; agoni!t $ith $ea2 %eta- an !electi'e alpha-;acti'ity Racemic mi(t#re con!i!ting of %oth > an L i!omer! - the > i!omer

i! a potent


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Adrenergic agonists

Selecti'e )lpha-; )goni!t!+ Phenylepherine, Epheerine, Metho(amine,

Metaraminol, Mephentermine

Selecti'e )lpha- )goni!t!+ 0loniine, :-methylopa, G#anfacine an

G#ana%en*- )renergic agoni!t!+

Sal%#tamol, &er%#taline, Salmeterol, Reproterol,1(iprenaline, 8enoterol, I!o(!#prine, Rimiterol,Ritorine, Bitolterol an I!oetharine

Adrenergic 7rugs


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Adrenergic 7rugs $

hera"eutic Classification

Pre!!or agent!+ N), Phenylephrine, epherine, Metho(amine, Dopamine

0ariac Stim#lant!+ Adr! 7o&utamine an I!oprenaline, Dope(amine

Na!al Deconge!tant!+ Phenylepherine, ylometa*oline, 1(ymeta*oline, Napha*oline an

&etrahyra*oline an Phenylpropanolamine an P!e#oephirine Bronchoilator!+

)so"renaline! Sal&utamol! Salmeterol! er&utaline, 8ormeterol Aterine Rela(ant!+

Ritodrine! Sal&utamol! )so,su"rine )norectic!

8enfl#ramine, De(fenfl#ramine an Si%#tramine 0NS Stim#lant!+

)mphetamine, Methamphetamine


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E"hedrine

Plant al2aloi o%taine from Ephera '#lgari! 6 Mi(e acting r#gal!o metaraminol 6 effecti'e orally

0ro!!e! BBB an 0entrally 6 Increa!e alertne!!, an(iety,in!omnia, tremor an na#!ea in a#lt!. Sleepine!! in chilren

Effect! appear !lo$ly %#t la!t! longer t;4-Jh 6 ; time! le!!potent

&achyphyla(i! on repeate o!ing lo$ ne#ronal pool A!e a! %ronchoilator, myriatic, in heart %loc2, m#co!al

'a!ocon!triction in mya!thenia gra'i! Not #!e commonly #e to non-!pecific action A!e!+ Mil Bronchial a!thma, hypoten!ion #e to !pinal anae!the!ia A/aila&le as ta&lets! nasal dro" and in?ection

S


62/73

Phenyle"herine - Selecti/e!synthetic and direct 36 agonist

)ction! 9#alitati'ely !imilar to norarenaline 3ong #ration of action Re!i!tant to M)1 an 01M& Doe! not cro!! BBB, !o no 0NS effect! Peripheral 'a!ocon!triction lea! to ri!e in BP %#t Refle(

%raycaria Pro#ce! myria!i! an na!al econge!tion A!e+

hypo'olaemic !hoc2 a! pre!!or agent Sin#!iti! Rhiniti! a! na!al econge!tant common in oral preparation! Myriatic in the form of eye rop! an lo$er! intraoc#lar pre!!#re

)DR!+ Photo!en!iti'ity, con"#ncti'al hyperemia an hyper!en!iti'ity )mini!tere parenteraly topically eye, no!e


63/73

>hat are #ucosal 7econgestants2

Na!al an %ronchial econge!tant! are the r#g! #!e inallergic rhiniti!, col!, co#gh! an !in#!iti! a! na!alrop! - Sympathomimetic 'a!ocon!trictor! $ith :- effect!are #!e

Dr#g!+ Phenylepherine, (ylometa*oline, 1(ymeta*oline,PP), P!e#oephirine etc. Dra$%ac2!+

Re%o#n conge!tion #e to o'er#!e Ho$e'er, m#co!al i!chaemic amage occ#r! if #!e e(ce!!i'ely

more often than 7 hrly or for prolonge perio! =7$ee2! 0NS &o(icity 8ail#re of antihyperten!i'e therapy 8atal hyperten!i'e cri!i! in patient! on M)1I!

A!e only a fe$ ay! !ince longer application re#ce! ciliary action


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Nasal 7econgestants

Pseudoe"hedrine to E"hedrine %#t le!! 0NS an 0ariaceffect! Poor Bronchoilator

Gi'en in com%ination $ith antihi!taminic!, antit#!!i'e! an NS)ID!in common cold an, allergic rhiniti!, %loc2e E#!tachian t#%e etc.

Ri!e in BP inhyperten!i'e!

Phenyl"ro"anolamine PPA. i! !imilar to epherine an #!ea! econge!tant! in many col an co#gh preparation! )l!o a! $eight loo!ing agent

ylometa*oline, 1(ymeta*oline etc.


65/73

Am"hetamine Synthetic compo#n !imilar to Epherine Pharmacologically

Kno$n %eca#!e of it! 0NS !tim#lant action 6 p!ychoacti'e r#g an

al!o performance enhancing r#g

)ction!+ alertne!!, e#phoria, tal2ati'ene!! an increa!e $or2 capacity 6 fatig#e

i! allaye act! on D) an N) ne#rotran!mitter! etc. 6re$ar path$ay increa!e phy!ical performance $itho#t fatig#e 6 !hort la!ting Banne

r#g an incl#e in the li!t of r#g! of ODope &e!t 6 eterioration

occ#r!

R)S Stim#lation 6 $a2ef#lne!!, !leep epri'ation then phy!ical

i!a%ility

Ho$e'er, an(iety, re!tle!!ne!!, tremor an y!phoria occ#r!

1ther action!+ Stim#lation of re!piratory centre, H#nger

!#ppre!!ion, al!o anticon'#l!ant, analge!ic an antiemetic action!


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Am"hetamine $ contd;

Dr#g of a%#!e 6 mar2e p!ychological effect %#t little

phy!ical epenence

Generally, &eenage a%#!er! - thrill or 2ic2

High Do!e 6 E#phoria, e(citement an may progre!! toeliri#m, hall#cination an ac#te p!ychotic !tate )l!o peripheral effect! li2e arrhythmia, palpitation, 'a!c#lar

collap!e etc.

Repeate Do!e 6 3ong term %eha'io#ral a%normalitie!

Star'ation 6 aciic #rine

(ses: Hyper2inetic 0hilren )DHD, Narcolep!y,

Epilep!y an Par2in!oni!m


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Anorectics

Dr#g! #!e for !#ppre!!ion of appetite

M1)+ Inhi%ition of N)4D) or F-H& #pta2e 6

enhancement of monoaminergic tran!mi!!ion N) agent! affect the appetite centre an

Serotonergic! act on !atiety centre 8enfl#ramine, e(fenfl#ramine an

!i%#tramine 6 )33 )RE B)NNED N1@ Rea!on!+ Heart 'al'e efect!, fi%ro!i! an

p#lmonary hyperten!ion etc.


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Clonidine

0entrally acting+ )goni!t to po!t!ynaptic :)arenoceptor! in %rain 6 'a!omotor centre in%rain!tem pre!ynaptic 0a>> le'el 6 increa!e N)relea!e

Decrea!e in BP an cariac o#tp#t Peripherally action+ High o!e acti'ate! peripheral

pre!ynaptic a#toreceptor! on arenergic ner'e eningmeiating negati'e fee%ac2 !#ppre!!ion of

norarenaline relea!e 1'ero!e !tim#late! peripheral po!t!ynaptic :;arenoceptor! ca#!e hyperten!ion %y'a!ocon!triction


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Clonidine $ contd;

A!e!+ )DHD in chilren, opioi $ithra$al re!tle!! leg!, "itter! anhyperten!ion, alcohol $ithra$al .7 to .Q mg

)%r#pt or gra#al $ithra$al ca#!e! re%o#n hyperten!ion 1n!et may %e rapi a fe$ ho#r! or elaye for a! long a! ay! an

!#%!ie! o'er -7 ay!

Ne'er #!e %eta-%loc2er! to treat

)'aila%le a! ta%let!, in"ection! an patche! Seation, ry mo#th, i**ine!! an con!tipation etc. &0)! antagoni*e antihyperten!i'e action increa!e re%o#n

hyperten!ion of a%r#pt $ithra$al 3o$ o!e 0loniine F-;g4l i! #!e in migraine prophyla(i!,

menopa#!al fl#!hing an chorea Mo(oniine, Rilmeniine 6 Ne$er Imia*oline!

4* Adrenergic Agonists $


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4* Adrenergic Agonists

discussed else1here8

Short acting + Sal%#tamol, Metaproterenol, &er%#taline,pir%#terol

Selecti'e for


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(terine Rela,ants discussed

else1here8

)ntio(ytocic! or tocolytic agent!


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Remem&er 2

Step! of Bio!ynthe!i! of 0atecholamine

Di!tri%#tion of arenergic receptor!

Ini'i#al 8#nction! of )renergic receptor!

)ll a!pect! of arenaline 6 Dale!

Phenomenon

Dopamine4Do%#tamine action!

Na!al econge!tant! - Phenylephrine

)mphetamine an 0loniine - De!ira%le


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ध नय व द @Ahu&lei

adrenergicsystem-110126105226-phpapp02.ppt

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