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Autonomic Nervous

System
Sukamto S M

Nervous
system
Peripheral
Nervous
system

Central
Nervous
system

Efferent
Division

Afferent
Division

Brain

Autonomic
Nervous
System

Somatic
Nervous
System

Parasympathetic Nervous
System
Sympathetic Nervous
System

Spinal Cord

Nervous
System
2

CNS
Preganglionic
neurons

Cell body

Ganglionic
transmitter

Efferent
Neurons

Postganglionic
neurons
Neuroeffector
transmitter

Effector
organ

Differences between PNS


and SNS
Comparisons

Parasympathetic

Sympathetic

Sources of
neurons
Neurotransmitt
er
(neuroeffector
transmitter)
Preganglionic
fiber
Receptors
Response
4

Differences between PNS


and SNS
Comparisons

Parasympathetic

Sympathetic

Sources of
neurons

Craniosacral

Thoracolumbal

Neurotransmitt
er
(neuroeffector
transmitter)

Acetylcholine

Epinephrine/
Norepinephrine

Preganglionic
fiber

Long

Short

Receptors

Muscarinic (M1-5) and


nicotinic (Nn & Nm)
receptors

Adrenergic (1-2 & 13) and nicotinic


receptors

Response

Rest & digest

Fight or flight
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Sources of Neurons

Neurotransmitters, ganglionic fibers and


receptors

Neurotransmitters, ganglionic fibers and


receptors

Autonomic Nervous System


Sympathetic
Receptors
Alpha () receptors (1-2)
Beta () receptors (1-2)
Nicotinic receptors (Nn &
Nm)
Parasympathetic

Highlights!!

Alpha receptors have


subtypes: 1A 1B 1D 2A 2B
2C
Another beta receptor has
been identifies as 3
located in fat tissue

Muscarinic receptors (M1-5)


Nicotinic receptors (Nn &
Nm)
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Neurotransmitt
er

Synthesis
Storage
Release
Interaction
Removal/
Degradatio
n
Recovery
Acetylcholin
e
10

Neurotransmitt
er

Synthesis
Storage
Release
Interaction
Removal/
Degradatio
n
Recovery
Epinephrine
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Receptor Bindings

12

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Agents Acting on
Sympathetic Nervous System
(Sympatomimetics/ Adrenomimetics/ Adrenergic
agonists)
(Sympatolytics/ Adrenolitics/ Adrenergic
antagonists)

14

Sympatomimetics/ Adrenomimetics/
Adrenergic Agonists
Direct acting
(The drugs bind directly to
the receptors leading to
responses)
Indirect acting
(The drugs stimulate the
release of norepinephrine
rather than binding to the
receptors)
Mixed acting
(The drugs have both
direct- and indirect
acting mechanisms)

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Direct Acting
Sympatomimetics
2
1
2

1
(Post
Phenylephrine
synaps)

(Pre
synaps)

Pseudoephedri
Clonidine
ne
Mehtyldopa
Tetrahydrozoli
Guanabenz
ne
Guanfacine
Metaraminol
Guanethidine
Midodrine
Methoxamine
Oxymetazolin
e
Naphazoline
Norepinephrin
e

(Post
synaps)

(Post
synaps)

Dobutamine
Denopamine
Xamoterol

Salbutamol
Terbutaline
Ritodrine
Formoterol
Salmeterol
Indacaterol

Isoproterenol

Epinephrine

Highlight!!

Pseudoephedrine is an alpha-1 agonist and used as nasal


decongestant. However, it has property as a stimulant leading
16
to special restriction by the government.

Sympathetic Specific Responses

1
2
1
2

Vasoconstriction
Increased peripheral resistance
Increased blood pressure
Midriasis
Increased closure of internal sphincter of the bladder

Inhibition
Inhibition
Inhibition

of
of
of

norepinephrine release
acetylcholine release
insulin release

Tachycardia
Increased of lypolisis
Increased myocardial contractility
Increased release of renin

Vasodilation
Slightly decreased peripheral resistance
Bronchodilation
Increased muscle and liver glycogenolisis
Increased release of glucagon
Relaxed uterine smooth muscle

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Indirect and Mixed Acting


Sympatomimetics
Substances derived from
AMPHETAMINE/ METAMPHETAMINE
is related to drug abuses such as
DOPING. It is caused by the
property of amphetamine that can
enter blood brain barrier leading to
DECREASED SENSE OF HUNGER OR
FATIGUE.

Moclobemide
Selegiline
Ephedrine
Dopamine

Mixed Acting

Pargyline
Entacapone

Inhibitor
s
MAO
Inhibitor
s

Cocaine

e
Inhibitor
s
COMT

Amphetamine
Tyramine

Releasin
g
Agents
Reuptak

Highlight!!!

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MAO
Inhibitors
COMT
Inhibitors

Highlight!!!

The use of MAO inhibitors not only


increases the concentration of
NOR/EPINEPHRINE in synapse but also
SEROTONIN and DOPAMIN leading to
potency to be used as
ANTIDEPRESSANT and
ANTIPARKINSON.

Reuptak
e
Inhibitor
s

Releasing
agents

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Clinical Use of
Sympatomimetics

Phenylephrine
Decongestant
Midriaticum

Clonidine
Along with other alpha-2
agonists, Clonidine has been
used clinically as
antihypertensive agent.
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Clinical Use of
Sympatomimetics

Dobutamine
Cardiogenic shock
Heart failure

Salbutamol
Like other beta-2
agonists, this drug is an
asthma therapy
Short acting drug

21

Clinical Use of
Sympatomimetics

Oxymetazoline
Nasal decongestant

Epinephrine
Anaphylactic shock
Cardiac arrest
Local anaesthetic
preparation

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Sympatolitics/ Adrenolitics/
Adrenergic Antagonists

23

1
(Post
synaps)
Prazosin
Doxazosin
Terazosin
Bunazosin
Alfuzosin
Tamsulosin

Sympatolitics

(Pre
synaps)
Yohimbine

(Post
synaps)
Atenolol
Metoprolol
Acebutolol
Bisoprolol
Esmolol
Betaxolol
Nebivolol

2
(Post
synaps)
Butoxamine

Propranolol
Nadolol
Pindolol
Timolol
Penbutolol
Oxprenolol

Phenoxybenzam
ine
Phentolamine

Labetalol
Carvedilol

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Sympathetic Specific Responses

1
2
1
2

Vasoconstriction (Vasodilation)
Increased peripheral resistance (Decreased)
Increased blood pressure (Decreased)
Midriasis (Miosis)
Increased closure of internal sphincter of the bladder

Inhibition
Inhibition
Inhibition

of
of
of

norepinephrine release (Stimulation)


acetylcholine release (Stimulation)
insulin release (Stimulation)

Tachycardia (Bradycardia)
Increased of lypolisis (Decreased)
Increased myocardial contractility (Decreased)
Increased release of renin (Decreased)

Vasodilation
Slightly decreased peripheral resistance
Bronchodilation
Increased muscle and liver glycogenolisis
Increased release of glucagon
Relaxed uterine smooth muscle

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Several Substances Acting on NE


Production

Methyltyrosin
e
Carbidopa
26

Clinical Use of Sympatolitics


Alpha 1 blocker

Hypertension

Alpha 2 blocker

Libido
performance. Not
widely used.

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Clinical Use of Sympatolitics


Beta 1
blocker

Hypertension,
angina, myocardial
infarction &
cardiac

Glaucoma
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Parasympathomimetics/
Cholinomimetics/ Cholinergic Agonists

29

Parasympathetic Receptors
Nicotinic
Neuromuscular junction
at skeletal muscle
Autonomic ganglia

Muscarinic (M1 - M5)


M1 ganglia and
secretory glands
M2 myocardium and
smooth muscles
M3 smooth muscles
and secretory glands
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Parasympathetic Responses

Miosis
Copious; watery salivation
Bronchoconstriction; increased secretion
Bradycardia
Gastric acid secretion
Increased gastric motility
Diuresis
Erection
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Parasympathomimetic Acting on
Nicotinic Receptors
Types

Neuromuscular
Junction
ACh

Agonists/ Nicotine
Depolarizi
ng agents Suxamethonium
Decamethonium
Tubocurarine
Antagonis
Pancuronium
ts/ Non
depolarizi Vecuronium
ng agents
Atracurium

Autonomic Ganglia
ACh
Nicotine

Trimetaphan
Mecamylamine
Hexamethonium
32

Clinical Use of Drugs Acting on


Nicotinic Receptors

Muscle relaxant

Muscle relaxant
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Parasympathomimetic Acting
on Muscarinic Receptors
Direct Acting Cholinomimetic (Choline
ester)

Acetylcholine
Methacholine
Bethanechol
Carbachol
Muscarine
Pilocarpine

Glaucoma

Urine retention/
increase GIT
motility
Mioticum/
Glaucoma

34

Parasympathomimetic Acting on
Muscarinic Receptors
Indirect Acting Cholinomimetic
(Anticholinesterase) Reversible, intermediateReversible, shortacting
anticholinesterases
Edrophonium
Tacrine

Irreversible, long-acting
anticholisterases
(phosphorylating agents)

Parathion
Malathion
Diazinon
Sarin

acting anticholinesterases
(carbamylating agents)
Physostigmine
Neostigmine
Pyridostigmine

Choline
ACh
+
Cholinestera Acetate
se

35

Clinical Use of Drugs Acting on


Muscarinic Receptors

Myasthenia gravis

Alzheimer disease

Anticholinergic toxicity/
Glaucoma

36

Parasympatholytics/ Anticholinergic/
Cholinergic Antagonists

37

Anticholinergic
Highlight!!!

Antimuscarinic agents were of


Atropine
plant origin:
Atropa belladonna Atropine
Hyoscine/ Scopolamine
Datura stramonium
Atropine
Pirenzepine
Hyoscyamus niger
Propantheline
Hyoscyamine
Scopolia carniolica
Benzatropine
Scopolamine

Ipratropium
Tiotropium
Trihexyphenidyl
Tropicamide

Highlight!!!

Several antihistamines have


anticholinergic effects.
Diphenhydramine
Dimenhydrinate
Doxylamine
38

Clinical Uses of
Anticholinergics

Midriaticum

Sinus bradycardia/
premedication in
surgery

Antispasmodic

Asthma

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Thank You

40

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