SISTEM SARAF OTONOM

ASISTENSI FARMAKOLOGI DAN TOKSIKOLOGI

 Nervous
system

Peripheral Central Nervous

Nervous system system

Efferent Afferent
Brain Spinal Cord
Division Division

Autonomic Somatic
Nervous System Nervous System

Parasympathetic Nervous System

2
Sympathetic Nervous System
Enteric Nervous System
DIFFERENCES
Comparisons
BETWEEN
Parasympathetic
PNS AND
Sympathetic
SNS

Sources of neurons

Neurotransmitter
(neuroeffector
transmitter)

Preganglionic fiber

Receptors

Response 3
DIFFERENCES
Comparisons
BETWEEN
Parasympathetic
PNS AND
Sympathetic
SNS

Sources of neurons Craniosacral Thoracolumbal

Neurotransmitter
Epinephrine/
(neuroeffector Acetylcholine
Norepinephrine
transmitter)

Preganglionic fiber Long Short

Muscarinic (M1-5) and nicotinic Adrenergic (α1-2 & β1-3)

Receptors
(Nn & Nm) receptors and nicotinic receptors

Response Rest & digest Fight or flight 4

 AUTONOMIC NERVOUS SYSTEM RECEPTORS
Sympathetic
• Alpha (α) receptors (α1-2)

• Beta (β) receptors (β1-2)

• Nicotinic receptors (Nn & Nm)

Parasympathetic
• Muscarinic receptors (M1-5)

• Nicotinic receptors (Nn & Nm)

5
NEUROTRANSMITT
ER
• SYNTHESIS
• STORAGE
• RELEASE
• INTERACTION
• REMOVAL/
DEGRADATION
• RECOVERY

Acetylcholine
6
NEUROTRANSMITT
ER
• SYNTHESIS
• STORAGE
• RELEASE
• INTERACTION
• REMOVAL/
DEGRADATION
• RECOVERY

Epinephrine
7
8
 OBAT-OBAT YANG BEKERJA SECARA AGONIS PADA SISTEM SARAF SIMPATIS (SIMPATOMIMETIK)

SYMPATOMIMETICS/ ADRENOMIMETICS/
ADRENERGIC AGONISTS

• HTTPS://WWW.YOUTUBE.COM/WATCH?V=KTMV-YMDYPI
 DIRECT – ACTING SYMPATOMIMETICS
α1 α2 β1 β2
(Post synaps) (Pre synaps) (Post synaps) (Post synaps)
Phenylephrine Salbutamol
Clonidine
Pseudoephedrine Dobutamine Terbutaline
Mehtyldopa
Tetrahydrozoline Denopamine Ritodrine
Guanabenz
Metaraminol Xamoterol Formoterol
Guanfacine
Midodrine Salmeterol
Guanethidine
Methoxamine Indacaterol

Oxymetazoline Isoproterenol
Naphazoline

Norepinephrine

Epinephrine

Highlight!! 12
Pseudoephedrine is an alpha-1 agonist and used as nasal decongestant. However,
it has property as a stimulant leading to special restriction by the government.
 INDIRECT – AND MIXED – ACTING
SYMPATOMIMETICS
Releasing • Amphetamine
Agents • Tyramine

Reuptake • Cocaine
Inhibitors Highlight!!!
Substances derived from AMPHETAMINE/
COMT • Pargyline METAMPHETAMINE is related to drug
Inhibitors • Entacapone abuses such as DOPING. It is caused by the
property of amphetamine that can enter blood
MAO • Moclobemide brain barrier leading to DECREASED SENSE
Inhibitors • Selegiline OF HUNGER OR FATIGUE.

Mixed - • Ephedrine
Acting • Dopamine 13
 MAO Inhibitors

COMT Inhibitors

Reuptake
Inhibitors

Releasing agents
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 14

used as ANTIDEPRESSANT and ANTIPARKINSON.

 OBAT-OBAT YANG BEKERJA SECARA ANTAGONIS PADA SISTEM SARAF SIMPATIS (SIMPATOLITIK)

SYMPATOLITICS/ ADRENOLITICS/
ADRENERGIC ANTAGONISTS

• HTTPS://WWW.YOUTUBE.COM/WATCH?V=KTMV-YMDYPI
 SYMPATOLITICS
α1 α2 β1 β2
(Post synaps) (Pre synaps) (Post synaps) (Post synaps)
Atenolol
Prazosin
Metoprolol
Doxazosin
Yohimbine Acebutolol Butoxamine
Terazosin
Bisoprolol
Bunazosin
Esmolol
Alfuzosin
Betaxolol
Tamsulosin
Nebivolol
Propranolol
Phenoxybenzamine Nadolol
Phentolamine Pindolol
Timolol
Penbutolol
Oxprenolol
16

Labetalol
Carvedilol
SYMPATHETIC SPECIFIC RESPONSES

α1
• Vasoconstriction (Vasodilation)
• Increased peripheral resistance (Decreased)
• Increased blood pressure (Decreased)
• Midriasis (Miosis)
• Increased closure of internal sphincter of the bladder

• Inhibition of norepinephrine release (Stimulation)

• Inhibition of acetylcholine release (Stimulation)
• Inhibition of insulin release (Stimulation) α2
β1
•Tachycardia (Bradycardia)
• Increased of lypolisis (Decreased)
• Increased myocardial contractility (Decreased)
• Increased release of renin (Decreased)

• Vasodilation

β2
• Slightly decreased peripheral resistance
• Bronchodilation
• Increased muscle and liver glycogenolisis 17

• Increased release of glucagon

• Relaxed uterine smooth muscle
SEVERAL SUBSTANCES ACTING ON NE
PRODUCTION

Methyltyrosine

Carbidopa
18
OBAT-OBAT YANG BEKERJA SECARA AGONIS PADA SISTEM SARAF PARASIMPATIS (PARASIMPATOMIMETIK)

PARASYMPATHOMIMETICS/ CHOLINOMIMETICS/ CHOLINERGIC AGONISTS

 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 20
NEUROTRANSMITTERS, GANGLIONIC
FIBERS AND RECEPTORS

21
PARASYMPATHOMIMETIC ACTING ON
Types NICOTINIC RECEPTORS
Neuromuscular Junction Autonomic Ganglia
ACh ACh

Agonists/ Nicotine Nicotine

Depolarizing
agents Suxamethonium
Decamethonium
Tubocurarine Trimetaphan
Antagonists/ Pancuronium Mecamylamine
Non –
depolarizing Vecuronium Hexamethonium
agents
Atracurium 22
 PARASYMPATHOMIMETIC ACTING ON
MUSCARINIC RECEPTORS

DIRECT – ACTING CHOLINOMIMETIC (CHOLINE ESTER)

• ACETYLCHOLINE
• METHACHOLINE
• BETHANECHOL
• CARBACHOL
• MUSCARINE
• PILOCARPINE
 PARASYMPATHOMIMETIC ACTING ON
MUSCARINIC RECEPTORS
INDIRECT – ACTING CHOLINOMIMETIC
(ANTICHOLINESTERASE)Reversible, intermediate-acting
anticholinesterases (carbamylating
Reversible, short-acting
agents)
anticholinesterases • Physostigmine
• Edrophonium • Neostigmine
• Tacrine • Pyridostigmine

Irreversible, long-acting anticholisterases

(phosphorylating agents)
Choline +
• Parathion ACh
• Malathion Acetate
• Diazinon Cholinesterase 24

• Sarin
OBAT-OBAT YANG BEKERJA SECARA ANTAGONIS PADA SISTEM SARAF PARASIMPATIS
(PARASIMPATOLITIK)

PARASYMPATHOLYTICS/ ANTICHOLINERGIC/ CHOLINERGIC ANTAGONISTS

ANTICHOLINERGIC
Highlight!!!
• ATROPINE Antimuscarinic agents were of plant
origin:
• HYOSCINE/ SCOPOLAMINE • Atropa belladonna  Atropine
• Datura stramonium  Atropine
• PIRENZEPINE • Hyoscyamus niger  Hyoscyamine
• PROPANTHELINE • Scopolia carniolica  Scopolamine

• BENZATROPINE
• IPRATROPIUM Highlight!!!
Several antihistamines have
• TIOTROPIUM anticholinergic effects.
• Diphenhydramine
• TRIHEXYPHENIDYL • Dimenhydrinate
26
• Doxylamine
• TROPICAMIDE
TERIMA KASIH