Adrenergics and Antiadrenergics

Group Drug Physiologic Effects Therapeutic Uses Toxicities and Side Effects Notes:
Group Drug Physiologic Effects Therapeutic Uses Toxicities and Side Effects Notes:
Catecholamines Epinephrine *Heart (1): automaticity, HR,
conduction velocity, CO (1 stimulated
in contractility + relaxation in lood
vessels due to ! stimulation "
t#era$eutic dose), O! consum$tion,
e%%iciency
*&' (! ( )1): " lo* + , via ! dilation,
as + , ( )1 rece$tors ecome
occu$ied- .% ot# rece$tors occu$ied /
)1 res$onse $redominates- " lo* + ,
0&' is o%ten , " #ig# + , 0&' is
*Res$iratory tract (! ( )1):
ronc#ioles dilated via ! / most
$rominent *#en ronc#ial muscle is
constricted due to drugs1disease-
secretions via )1
0etaolism: glycogen rea2do*n (!)-
glycogen synt#esis ()1)- insulin
secretion ()!), %ree %atty acids (3)
*Ana$#ylactic 4#oc2 (drug o% c#oice):
! stimulation o$ens air*ays- !
stimulation su$$resses release o%
#istamine and leu2otrienes y in#iiting
antigen5induced degranulation o% mast
cells- )1 stimulation can &'
*Ast#ma: o$ens air*ays " !
*Hy$ersensitivity rxn: can occur to suc#
stimuli as ee stings, %oods, drugs /
reasons same as %or s#oc2
*6o$ical Hemostasis: s#rin2s mucosa in
nose, t#roat, larynx ()1) to im$rove
visuali7ation %or surgical $rocedure
*Cardiac arrest: resuscitate #eart via
1 stimulation
*4u$$ort &': not %irst line- try 8A %irst
*Arr#yt#mias- cereral
vascular accident- less serious,
ut $redictale side e%%ects
suc# as anxiety, %ear,
#eadac#es, $al$itations, and
tremors
Norepinephrine *Heart(1): direct e%%ects- same as e$i
*&' ()1): systolic, diastolic and mean
*Cardiac Out$ut: no c#ange or slig#tly
due to )1 mediated constriction o% lood
vessels
*0etaolism- glycogen synt#ase
activity via )1
*9o longer *idely used, ut goes in (
out o% %as#ion in :R %or s#oc2 / i% $t is
in s#oc2, sym$at#etics usually turned on
*9eurogenic s#oc2 associated *1 s$inal
anest#esia (sometimes)
4imilar to e$i
Isoproterenol *Heart (1) / direct e%%ects same as e$i
&' (!): &'
Res$iratory 6ract (!): relaxes ronc#i
*:mergencies to stimulate #eart in
$atients *1 #eart loc2 or to stimulate
rate, es$ecially to $re$are inserting a
$acema2er / myocardial e%%iciency
*Relax ronc#i, ut ! selective agonist
$re%erred
*;atal arr#yt#mias,
tac#ycardia, $al$itations,
anginal $ain
*4elective agonist also*
5not endogenous
Dopamine *Rece$tors activated (8A, 1, !, )1 "
+ ,)
Heart (1): HR
&': y 8A rece$tor activation in
*0anagement o% certain ty$es o% s#oc2
(i<e< cardiogenic) / $rolem *1 s#oc2 is
$oor $er%usion
*8ue to excessive sym$at#etic
stimulation, tac#ycardia,
anginal $ain, arr#t#mias) and
8A rece$tor o% c#emotrigger
1
Adrenergics and Antiadrenergics
Group Drug Physiologic Effects Therapeutic Uses Toxicities and Side Effects Notes:
renal1mesenteric eds- y !
rece$tor activation- y + , y )1
rece$tor activation
7one nausea1vomiting
*8A does not cross &&& / no
C94 e%%ects
Doutamine *Heart (1*) / greater inotro$ic
(contractility) t#an c#ronotro$ic (rate)
e%%ects- + , may also automaticity
*&': + , can &' via )1
*Heart %ailure associated *1 o$en #eart
surgery or acute cardiac in%arction
*Arryt#mias- does not cross
&&& / no C94 e%%ects
!" agonists
#stimulators$
Phenylephrine *9on5catec#olamine ) stimulators are
9O6 metaoli7ed y CO06
*8econgestion o%
mucus memranes-
&' ($ressor
agents)- dilate
$u$il, eye dro$s
=gets red out>
8econgestant,
$u$ilary dilator)-
no* limited sales
*:xcessive )1 stimulation can
&'
*9oncatec#olamine )5
stimulators are 9O6
metaoli7ed y CO06-
sustitution o% ) caron
loc2s 0AO metaolism
**.ncreases ? li%e**
Ephedrine @ea2 ) (
agonist- also a
releaser o% 9: /
C94 stimulant /
used as nasal
decongestant and
$ressor agent
**Also stimulator
!% agonists Clonidine *&rain: )! " rece$tors sites loc2
sym$at#etic out$ut / $ostsyna$tic
*'eri$#ery: )! act " $resyna$tic
rece$tors to in#iit 9: release
*:ssential #y$ertension
* un$leasant side e%%ects associated
*1 o$ioid *it#dra*al
*A8H8
*8ry mout#, sedation
*Hy$ertensive crisis may
occur u$on aru$t *it#dra*al
%rom clonidine
*@or2s directly " )!
rece$tors
!&'ethyldopa *:ssential #y$ertension *8ry mout#, sedation
*'roduces a incidence o%
autoimmune res$onse (+
Cooms test)
*0ust e metaoli7ed to )5
met#yl59:
**4A;: .9 'R:A9A9CB**
( stimulators Terutaline *&ronc#ial ast#ma
(! o$ens air*ays)
*Ana$#ylactic
s#oc2 (!
stimulation in#iits
release o%
mediators o% t#e
allergic res$onse
Relatively !5
selective agonists-
more use%ul t#an
non5selective 5
agonists %or
ast#ma *Csed to
delay $remature
laor
*Related to less t#an total
selectivity %or !
+ , can activate 1 rece$tors
on t#e #eart
2
Adrenergics and Antiadrenergics
Group Drug Physiologic Effects Therapeutic Uses Toxicities and Side Effects Notes:
%rom mast cells)
*Relaxation
$regnant uterus
)luterol Relatively !5
selective agonists-
more use%ul t#an
non5selective 5
agonists %or
ast#ma
*active enantomer o%
aluterol (levaluterol no*
availale)
CNS Stimulants )mphetamine *8is$laces 9: %rom terminal
sym$at#omimetic e%%ects
*4ustrate %or 9:6 and syna$tic 9:
via %acilitated exc#ange di%%usion
*9arcole$sy: release 9: %rom nerve
terminal y %acilitated exc#ange
di%%usion
*@eig#t reduction: su$$ress a$$etite
*:xcessive C94 stimulation
and $eri$#eral cardiovascular
e%%ects can occur
*Ris2 o% ause
'ethylphenidate *A8H8: availale oral1$atc#
Selecti*e !" loc+ers
#re*ersile$
Pra,osin *&loc2 )1 rece$tors only
*)1 loc2ade: &', get re%lex
tac#ycardia
*Hy$ertension
*&enign $rostatic #y$ertro$#y
*'ostural #y$otension caused
y )1 loc2ade
*Re%lex tac#ycardia occurs *1
ot# selective and non5
selective ) loc2ers (@OR4:
@1 9O954:D:C6.E:)
*9asal stu%%iness
*.n#iition o% eFaculation
*:$i reversal / ! e%%ects
last longer *#en ) loc2er is
given
5 *#en t#e $ressor e%%ect
o% e$i #as een converted
to a $ure de$ressor e%%ect
due to t#e $resence o% an )
loc2er
Selecti*e !" loc+ers
#irre*ersile$
Phenoxye,amine *&loc2 )1 rece$tors only
*8uration o% action G!H #rs
*0ust synt#esi7e ne* rece$tor to
recover )1 e%%ect
*'#enoxye7amine and $#entolamine (in
como *1 $ro$ranolol) %or
$#eoc#romocytoma management
*&enign $rostatic #y$ertro$#y
Non&Selecti*e !
loc+ers
Phentolamine *&loc2 )1 and )! rece$tors
*)1 loc2ade &'
*)! loc2ade $revents %eedac2
in#iition y released 9:, causing more
9: to e released onto rece$tors in
#eart, $roducing even AR:A6:R
6ACHBCAR8.A t#an *1 a selective
loc2er
*'#eoc#romocytoma / see aove
Non&selecti*e (
loc+ers
Propanolol *&loc2s 1 and !
*Cardiac e%%ects: HR due to 1 loc2-
CO (more $ronounced during
exercise)- conduction velocity,
myocardial O! demand, ( s$ontaneous
rate o% de$olari7ation
*Eascular ( &' :%%ects: ! may 6'R
slig#tly- $lasma rennin due to 1
loc2- net e%%ect &'
*0etaolic :%%ects: no e%%ect on $lasma
glucose in normal, ut does slo*
&loc2ers:
*Hy$ertension
*Cardiac arr#yt#mias
*Angina
*'ro$#ylaxis o% migraine
*:arly in 0. to reduce sym$at#etic
tone in some $atients
*'ro$#ylactic to mortality a%ter 0.
*'#eoc#romocytoma (*1 ) loc2ers)
*Alaucoma
*Heart %ailure
8ue to 1 loc2: CO, #eart
loc2, radycardia
! loc2: ronc#oconstriction
C94: de$ression, let#argy
**0ec#anism o% &' due
to:**
1< CO
!< $lasma renin
3< sym$at#etic tone via
e%%ects in C4
3
Adrenergics and Antiadrenergics
Group Drug Physiologic Effects Therapeutic Uses Toxicities and Side Effects Notes:
recovery %rom #y$oglycemia in diaetics
(less o% a $rolem *1 selectives)-
$lasma + , o% triglycerides (ED8D) and
+ , H8D
*Res$iratory 6ract (! loc2): air*ay
resistance - can e li%e t#reatening in
ast#matics
*'er%ormance anxiety
(" selecti*e loc+ers )tenolol *Cardiac e%%ects: similar to non5
selective loc2ers
*Dess danger o% res$iratory side
e%%ects t#an *1 non5selective
*At + , 9O loc2er is really
=selective>
Esmolol :mergency $rocedures *4#ort 11! li%e (I mins)
Timolol
#nonselecti*e$
Alaucoma ( aJueous #umor
$roduction t#ere%ore
$ressure)
-anthines:
#.produce effects
resemling
sympathetic
stimulation/ ut N0T
inding to adrenergic
receptors.$
Caffeine *C94: all cortical areas are sensiti7e-
+ , sensiti7e t#e res$iratory areas to
CO! ( res$iratory rate
*CE: HR and contractility- systemic
&E dilate- 6'R (loo2s li2e !
stimulation)- cereral lood vessels
constricted- net e%%ect &' ecause
ca%%eine releases catec#olamines
*Res$iratory tract: ronc#i relaxed
.n#iits $#os$#odiesterase
cA0'
Also antagonists "
adenosine rece$tors / C94
stimulating e%%ects
C94 Heart &ronc#i
Ca% 1 3 3
6#e ! 1 1
(1 #ig#est)
Theophylline *.ntractale ronc#ial ast#ma (in %orm
o% amino$#ylline / t#eo$#ylline
et#ylenediamine)
*'ro$#ylactic management / can e used
in como *1 in#aled ! agonists %or
management o% c#ronic ronc#ial
ast#ma
Drugs acting 1
presynaptic site
Guanethidine :nters via 9:6, uncou$les A' %rom Ca++
entry, and staili7es vesicular
memrane- sto$s 9: %rom eing stored-
&'
Anti5Hy$ertension *'ostural #y$otension,
diarr#ea, im$aired sexual
%unction all related to
$eri$#eral antiadrenergic
actions
0ec#< Only
2eserpine :nters t#e terminal (li$id solule),
staili7es vesicular memrane, causing
de$letion o% 9: over time- sto$s 9:
%rom eing stored
Anti5Hy$ertension *C94 de$ression
*'eri$#eral: ort#ostatic
#y$otension
0ec# Only
Tyramine Cause dis$lacement o% 9: %rom terminal
sy$at#omimetic e%%ects
*normally metaoli7ed y monamine
oxidase in t#e gut
*.n C94 metaoli7ed to octo$amine
*#ic# is stored in vesicles causing
0ec# Only
*;ound in c#eeses, eers,
*ine, %ava eans
*.% $atient on 0AO.
ingestion o% t#ese %ine
$roducts can lead to
4
Adrenergics and Antiadrenergics
Group Drug Physiologic Effects Therapeutic Uses Toxicities and Side Effects Notes:
dis$lacement o% 9: #y$ertensive crisis
Cocaine *&loc2s 9:6 syna$tic 9: 0ec# Only
Imipramine *&loc2s 9:6 syna$tic 9: 6ricyclic antide$ressants 0ec# Only
)tomoxetine *&loc2s 9:6 syna$tic 9:
(selective 9: reu$ta2e in#iitor)
A8H8 0ec# Only- C94 4timulant
*'o$ular ecause not
sc#eduled and no ris2 ause
5