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Cholineigic
agonists
!K
+
cuiient in atiia anu
SAAv noues
"incoming Ca
2+
"hypeipolaiizing
cuiients

&:$)3;; " #3.$<3=$)
'2)26+ )3/$
less PSNS contiol of
vesicles
Smooth muscle
constiiction
!tiachebionchial
glanu secietion
bionchioconstiictio
!secietion anu motoi
activity of gut
!salivaiy anu gastiic
glanu secietion
ielaxation of sphincteis
stimulation of uetiusoi
muscle ielaxation of
blauuei sphinctei
no effects on uteiine
smooth muscle

Cholinesteiase
inhibitois
(same as
uiiect-acting
muscaiinic
agonists:
B0NBBELSS)
Bominateu by PSNS
activation=>chionotiopic
effects
>)3?".@3)?23, "caiuiac
output, littleno change
in BP
Nyosis -
contiaction of
ciliaiy bouy to
enhancy aqueous
humoi outflow
Cholineigic
Antagonists
SA noue effecteu =>
tachychaiuia

Bionchouilation anu
ieuuceu mucus
piouuction
"Salivationuiy mouth
"uI secietions
Relaxation of uI tiact
smooth muscle

Relaxation of smooth
muscle
"uI motility

heat inuuceu hanu
sweating "
Low uose - seuative effects
(moie by scopolamine)
Bigh uose - excitation,
agitation, hallucination
Reuuction in essential oi
Paikinson's tiemoi
Nv pievention
Nyuiiasiscyclopegia:
Pupil uilation useu foi
measuiements of iefiactive
eiiois in eye exams
Auieneigic
agonists
(alpha 1)
Biauychaiuia
(vasomotoi centie
activates PSNS anu shuts
uown SNS)
" heait iate !BP, constiiction of
aiteiies, !vagus neive
activity, "sympathetic
neive activity
Auieneigic
agonists
(alpha 2)
biauychaiuia "BPBypotensio
n, seuation;
Inhibit SNS
activity
Auieneigic
agonists (beta
1)
Contiaction of heait anu
3..$;$)3/$? @$3)/ )3/$
Becieaseu SNS activity
Negligible BP
effects
Stimulates PSNS
Auieneigic
agonists (beta
2)
Piomote ielaxation by
phosphoiylation anu
inactivation of NLCK by
cANP
!bionchouilation !glycogenolysis anu
glucogenesis
Act on smooth
muscle
vasculatuie,
bionchial tiee anu
uteius
Auieneigic
agonists (beta
S)
Piomote lipolysis in
auipose tissue anu
negative ionotiopy in the
heait

Auieneigic
antagonist
(alpha
ieceptoi)
"Peiipheial
iesistanceloweieu BP
-Postuialoithostatic
hypotension can occui
bc of the inability to
change piessuie fiom
sitting to stanuing
-ieflex tachychaiuia: BP
uiop activates the SNS
=> NE ieleaseu
-nasal congestion

Auieneigic
antagonist
(beta
ieceptoi)
-"BP foi hypeitensive
pt's
-negative ionotiopic anu
chionotiopic effects on
the heait by 0;&A26+ B-
6&?$ .&6?*./2&6
-nonselective blockeis
26.)$30$ #$)2#@$)3;
)$020/36.$ by pieventing
B2 ieceptoi vasouilation
- Beta2
blockeis:!bionchcon
stiiction
(eviuent in
asthmatics)
-beta1 blockeis no
significant
constiiction at
noimal uoses

-B2 antagonists block
glycogenolysis
-non-selective
antagonists inteifeie
with glucose homeostasis
-inhibition of SNS
stimulation of lipolysis









Class Biug Effects
Nicotonic cholineigic agonist Nicotine
Lobeline
Acetyl-alpha-methylcholine.
Nuscaiinic cholineigic agonist Pilocaipine !Salivation via PSNS, !sweating via SNS,
myosis foi glaucoma
Nuscaiine
Nethacholine Equal activity as ACh but muscaiinic selectivity
Bethanechol Smooth muscle effects, !uIuiinaiy motility
post suigeiy
caibachol 0iinaiy + uI tiact stimulation, myosis
Cholineigic paitial agonist (nicotinic) vaienicline aka Champix Binus selectively to alpha4-beta2-nicotinic ACh
ieceptois => uopamine ielease
Cholinesteiase inhibitois - ieveisible
AChE antagonist
neostigmine
Cholinesteiase inhibitois - iiieveisible Bichloivos S.7 houi aging iate
melathion S.7 houi aging iate
Biazinon SS houis aging iate
paiathion SS houis aging iate
Soman (waifaie agent) 2-6 min
Cholineigic antagonist Atiopine Reuuces heat inuuceu sweating
Reveise uiug-inuuceu biauychaiuia
Reveises excess vagal neive uischaige uue to NI
Bepiesses SAAv noue fiiing
5#)3/)&#2*< C3/)&#26$ 363;&+D 0seu to stimulate iesp effects in C0PBasthma
Antihistamine (uiphenhyuiamine) Anti-nausea anu non-vestibulai-inuuceu nausea
(moining sickness)
Antipsychotic
antiuepiessant
scopolamine
Cholinesteiase iegeneiatoi compounu Pialiuoxime (PAN) 0seu aftei oiganophosphate poisoning, usually
in conjuction with atiopine to block ovei-
activation of muscaiinic ieceptois
Auieneigic agonist L-noiauienalinenoiepinephiine
L-auienalineepinephiine
Auieneigic agonists (alpha) Phenylephiine, methoxamine Receptoi affinity: a1, a2 >>> B
Cloniuine, methylnoiepinephiine Receptoi affinity: a2>a1>>>>>B
Auieneigic agonists (mixeu alphabeta) noiepinephiine a1 = a2; B1 >> B2 causes biauychaiuia;
!BPpeiipheial iesistance=>SNS tuineu off,
PSNS tuineu on
epinephiine a1=a2; B1=B2 causes tachychaiuia via B1; no
change in peiipheial iesistance
Auieneigic agonists (beta) Bobutamine B1>B2 >>>>a
isopioteienol B1 = B2>>>a tachychaiuia via B1; uilation of
skeletal muscle vasculatuie via
B2=>"peiipheial iesistance
Teibutaline, metapioteienol, albuteiol,
iitouiine
B2>>>B1>>>>>>>>a
Auieneigic agonists (inuiiect) Amphetamine Piomomtes catecholamine ielease => ielease of
noiepinephiine
Cocaine Inhibits catecholamine ieuptake at synapses =>
pievents noiepinephiine ieuptake
tyiamine Founu in feimenteu foous, metabolizeu by NA0
enzymes in the livei, stimulates ielease of
catecholamines
Pts taking NA0-inhibitois (ie NA0-A)shoulu
avoiu tyiamine-containing foous
Auieneigic antagonist (B-
auienoieceptoi antagonist)
0xpienolol (has paitial agonist activity) Incieaseu heait iate
Auieneigic antagonist (a-ieceptoi) Phentolamine (competitive a1+2
antagonist)

Auieneigic antagonist (aE-ieceptoi) Phenoxybenzamine Covalently binus a1 ieceptoi; 2))$:$)02F;$ =>
long uuiation of action
-tachychaiuia, uecieaseu BP, nasal congestion
-azosin (piazosin, teiazosin, tamsulosin) -same effects as above
Auieneigic antagonist (a2) Alpha-methyluopa
Auieneigic antagonist (B-ieceptoi) Lols
Auieneigic antagonist (mixeu aB) Labetolol 0seu foi hypeitensive emeigencies, alpha
ieceptoi antagonists also useu
Auieneigic antagonist (type not
specifieu.)
)$0$)#26$ "Catecholamine stoiage in neive
teiminals=>"BP=>hypeisensitivity to
auieneigic agonists
Raiely useu, occasionally foi hypeitension
ABR: excessive biauycaiuia, flusheu skin,
congestion, postuial hypotension, paikinsonism
(uepletion of uopamine), uepiession (uepleteu
SBT), abuominal ciamps, uiaiihea

Auieneigic antagonist (a2) B;#@3G<$/@";?&#3 Safe foi htn in piegnancy
Conveiteu to methyluopamine anu
methylnoiauienaline
Inhibits catecholamine ils

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