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Autonomic Drugs Two

Autonomic Drugs Two

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Published by jslum

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Published by: jslum on Jul 05, 2011
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05/27/2012

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uonomc rugsDefinition
COMT  Catechol O-methyltransferase(at synaptic space, metabolize noradrenalin)MAO  Monoamine oxidase(located at neuronal mitochondria, oxidize noradrenalin)
Adrenergic Receptors
Receptors stimulated by Noradrenalin, Adrenaline
Groups
1
y
 
Atpost-synapticeffector organs
y
 
S
timulation cause smooth musclecontraction (eg.vasoconstriction)2
y
 
I
nhibitoryin nature
y
 
L
ocated atpre-synapticnerveendings, other cells
y
 
S
timulation causes feedbackinhibition of NA release1
y
 
Causecardiac stimulation 2
y
 
P
roducevasodilatation (Relax vascular smooth muscle)
y
 
B
ronchiolar relaxation
Distribution & Functional Response of Adrenoceptors1 receptors
Contractionof majority of vascular smooth muscleContractionof trigone &sphincter  Ejaculationof male sex organsContraction of pupillary dilator muscle (dilates pupils)Erect hairof pilomotor smooth muscle
2 receptors
 Central sympathetic outflow (CN
S
)
I
nhibit NA release (Adrenergic nerve terminals)
1 receptors
 Force of contraction,  Contraction rate of heart Reninrelease in juxtaglomerular apparatus
2 receptors
Relaxation of bronchial smooth muscle (bronchodilation)Relaxation of uterine smooth muscle Relaxation of vascular smooth muscleGlycogenolysis, Gluconeogenesisin liverGlycogenolysisin skeletal muscle
IV Infusion of Adrenaline, Noradrenalin, IsoprenalineTherapeutic Uses of DrugsDrug Uses Receptor
Adrenaline Acute asthmaAnaphylactic shock1, 2,1, 2Noradrenalin
S
hock 1, 2, 1Dopamine
S
hockHeart failureD, 1Dobutamine Heart failure 1
P
henylephrine Nasal congestion 1Clonidine Hypertension 2
S
albutamolRitodrineTerbutalineAsthma
P
remature labour2Ephedrine Nasal decongestion 1
 
renergc gonss ympaommecsCatecholamines Non-Catecholamines
Adrenaline, Noradrenalin, Dopamine, Dobutamine Ephedrine, Amphetamine
S
hort durationof actionNot given orallyDo not penetrate
BBB
 Rapidly inactivatedby (short period of action)
y
 
COMT(post-synaptically)
y
 
MAO
I
neffective orally (inactivated by G
I
T enzymes)
P
olar substance (poor CN
S
penetration)
L
onger durationof actionNot inactivated by COMT
P
oor substrates for MAO
L
ipid solubility (better penetration CN
S
)
Adrenaline(SC, IV, ETT, Inhalation, Eye-topical)NoradrenalinDirect Acting(1 selective, 2 selective)(Oral, Inhaled)Indirect Acting
Act on ,  receptors (1-2)
Effects
CV
S
()
y
 
+
ve inotropic,
+
ve chronotropic
y
 
 CO,  O2 demandVascular (, )
y
 
Constricts arterioles in skin,mucous membranes, viscera
y
 
Dilates vessels to liver, skeletalmuscle (2)
y
 
S
ystolic
BP
(
SBP
) Diastolic
BP
(D
BP
)Respiratory
y
 
B
ronchodilation(direct action bronchial smooth muscle (2))
y
 
U
seful anaphylactic shock,acute asthmaMetabolic
y
 
Hyperglycemic ( Glycogenolysis in liver)( Glucagon release, 2 effect)
S
mooth muscle G
I
T
y
 
 Tone & Motility (2, )
y
 
S
phincter constriction ()
S
mooth muscle uterus
y
 
Relaxation (2)
B
ladder
y
 
Detrusor muscle relaxation (2)
y
 
Contraction trigone, sphincter(1)Act on , 1 receptors(little effect on 2 receptor)Neurotransmitter of postganglionicadrenergic neuron10-20% of catecholamine secreted byadrenal medulla(during sympathetic stimulation)
Effects
CV
S
 
y
 
P
eripheral resistance (due to vasoconstriction of vascular beds incl. kidney (1))
y
 
S
ystolic
BP
(
SBP
)
y
 
 Diastolic
BP
(D
BP
)
BP
 
 
I
nduce reflex rise vagal activity(stimulate baroreceptors)
 
B
radycardia
2 selective agonists
S
albutamol(albuterol),Terbutaline  Action
y
 
Relax bronchial smooth muscle(bronchodilatation)
y
 
U
terine relaxationTherapeutic use
y
 
B
ronchialasthma 
y
 
P
remature labour(2)Adverse Effects
y
 
S
keletal muscle tremor
y
 
Tachycardia
y
 
HyperglycemiaAmphetamine,Methamphetamine 
Effects
NA release from pre-synaptic terminals(potentiate effects of endogenous NA)CN
S
 
y
 
 Wakefulness
y
 
P
sychomotoractivity
y
 
Respiratorystimulation
y
 
 Appetite
2 agonist
Clonidine,Methyldopa  Action
y
 
Act centrally to inhibitsympathetic vasomotor centerTherapeutic use
y
 
S
ymptoms of opiate,benzodiazepine withdrawal
y
 
Hypertension
1 selective agonists
P
henylephrine,pseudoephedrine  Therapeutic use
y
 
Nasal decongestant(topically)
K
inetics
Metabolized by COMT, MAOOral ineffective(inactivated by intestinal enzymes)
Therapeutic Uses
B
ronchospasm (bronchoconstriction)
y
 
Acuteasthma 
y
 
Anaphylactic shock
Therapeutic Uses
S
hock
BP
 Not used for  asthma, hypersensitivity
Adverse Effects
ArrhythmiasAngina pain (
I
HD patient)HeadacheTremorCN
S
disturbances
y
 
Anxiety
y
 
FearTension
 Adverse Effects
Cardiac arrhythmiasHeadacheHyperactivity
I
nsomniaNauseaTremors

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