PHARMACOTHERAPEUTIC

S
Drugs Affecting the ANS

Katherine Kyra D. Alonday, RPh

The Graduate School
University of Santo Tomas

OUTLINE OF REPORT
AUTONOMIC NERVOUS SYSTEM
SYMPATHETIC ANS (SANS)
PARASYMPATHETIC ANS (PANS)

DRUGS AFFECTING SANS

ADRENERGIC AGONISTS
ADRENERGIC ANTAGONISTS

DRUGS AFFECTING PANS

CHOLINERGIC AGONISTS
CHOLINERGIC ANTAGONISTS

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 CENTRAL NERVOUS SYSTEM (CNS)

PERIPHERAL NERVOUS SYSTEM (PNS)

Sensory Division sends stimuli to PNS

Motor Division elicits response from PNS

The PNS receives stimuli from the CNS & initiates responses

Under the Motor Division

A.Autonomic involuntary
- acts on smooth muscles & glands
- person has little or no control
B. Somatic voluntary
- acts on skeletal muscles
- person has control

What happens when you accidentally

touch a very hot object?

HIGH TEMPERATURE SENDS PAIN

STIMULI
(Sensory Division PNS CNS PNS
Motor Division ANS)
ANS elicits the Withdrawal Reflex in
just about split seconds through the
pathway shown.

AUTONOMIC NERVOUS SYSTEM

(ANS)
Definition:
Major involuntary, unconscious, automatic
portion of the nervous system that can be
divided into the SANS, PANS and in some
references, ENS.
Roles:
Fight/Flight & Rest/Digest
2 Major Divisions of ANS:
Sympathetic (SANS) & Parasympathetic
(PANS)

TRIVI
A

DID YOU KNOW THAT

Hypothalamus is the major control and
integration center of the ANS?
The ENS (Enteric Nervous System) is a
semi autonomous part of the ANS
located in the GIT

ANS has 2 Sets of Neurons:

1. Afferent (sensory) - sends
impulses to the CNS for
interpretation
2. Efferent (motor) - receives
impulses (information) from the
brain & transmits from the spinal
cord to the effector organ cells
*Efferent Branches SANS and PANS

SYMPATHETIC DIVISION

SANS (Adrenergic)

Also called thoraco-lumbar system

Leads to every part of the body (unlike
parasymp.)
Norepinephrine is the neurotransmitter
released by most postganglionic fibers
ADRENERGIC

Sympathetic Response
SANS (Adrenergic)

Stress fight-or-flight response

production of ATP
Dilation of the pupils
heart rate and blood pressure
Dilation of the airways
Constriction of blood vessels that supply the
kidneys and gastrointestinal tract.
11

Sympathetic Response
continued..
SANS (Adrenergic)
blood supply to the skeletal muscles,
cardiac muscle, liver and adipose tissue
glycogenolysis blood glucose
lipolysis
Sympathetic Response = ENERGY
EXPENDITURE
12

SYMPATHETIC RESPONSES

S (Adrenergic)

PARASYMPATHETIC
DIVISION
PANS (Cholinergic)
Also called the cranio-sacral system
Only innervate internal organs (not
skin)
Acetylcholine is neurotransmitter at
end organ as well as at preganglionic
synapse
CHOLINERGIC

Parasympathetic
Responses
PANS (Cholinergic)
Rest-and-digest response
digestive and urinary function
body functions that support physical
activity
Parasympathetic = ENERGY
CONSERVATION

15

Parasympathetic
Responses

PANS (Cholinergic)

COMPARISON
(Sympathetic vs.
Parasympathetic)
STANDARD

SYMPATHETIC
(SANS)

PARASYMPATHETIC
(PANS)

Other Name

Fight/Flight
Thoraco-lumbar

Rest&Digest
Cranio-sacral

Receptors

Alpha: a1,a2,a3
Beta: b1,b2

Nicotinic
Muscarinic

Considered as

ADRENERGIC

CHOLINERGIC

Major
Neurotransmit
ter

Epinephrine (E)

Acetylcholine (ACh)

Function/(s)

Uses energy

Conserves energy

SANS (Adrenergic)
4 TYPES OF ADRENERGIC RECEPTOR
ORGAN CELLS:
Alpha-1 : Vasoconstriction of Peripheral Blood
Vessels
Alpha-2 : inhibits NE release; Vasodilation
Beta-1 : Increase in HR and Force of contraction
Beta-2 : Relaxes smooth muscle in Bronchi, Uterus,
Peripheral BV

Adrenergic Agonists
(Sympathomimetics)
Drugs that Stimulate the Sympathetic Nervous
System (adrenergics, adrenergic agonists,
sypathomimetics, or adrenomimetics)
Mimic the neruotransmitters norepinephrine and
epinephrine
Act on one or more adrenergic receptor sites
located on the cells of smooth muscles - heart,
bronchioles, GI tract, bladder, eye
4 main receptors alpha 1, alpha 2, beta1, beta2

ADRENERGIC AGONISTS
I. Centrally-Acting
II. Indirect-Acting Sympathomimetics
A. Releasers
B. Reuptake-Inhibitors
III. Direct-Acting
NON-SELECTIVE : Catecholamines
SELECTIVE:
A. Alpha agonists (Alpha 1, Alpha2)
B. Beta agonists (Beta1, Beta2, Non-S)
C. Dopa agonist

ADRENERGIC AGONISTS
I. Centrally-Acting Sympathomimetics
Risk for Addiction and Hemorrhagic Stroke
A (Amphetamine)
M (Methylphenidate) DOC for ADHD
M (Modafinil) DOC for Narcolepsy
P (Pemoline)
P (Phenmetrazine) Anorexiant; CI in HTN
P (Phentermine) Anorexiant; CI in HTN

ADRENERGIC AGONISTS
II. Indirect-Acting Sympathomimetics:
A. Releasers
Amphetamine derivatives&Tyramine
Pseudoephedrine
Ephedrine I: Hypotension &Bronchospasm
B. Reuptake-Inhibitors
TCAs
Cocaine

ADRENERGIC AGONISTS
III. Direct-Acting (Non-Selective)
E (Epinephrine) First line heart stimulant
DOC for Anaphylaxis
N (Norepinephrine) DOC for Septic
Shock
D (Dopamine) DOC for Cardiogenic
Shock

ADRENERGIC AGONISTS
Direct-Acting (Selective)
A. Alpha agonists (Alpha 1, Alpha2)
ALPHA-1 SELECTIVE Causes Vasoconstriction
Causes Urinary retention
X (Xylometazoline) I: Nasal congestion/Hypotension
Do not use more than 3 days (nasal)
Do not use more than 5 days (IV/PO)
P (Phenylephrine)
M (Methoxamine)
O (Oxymetazoline)
M (Midodrine) I: Orthostatic Hypotension

ADRENERGIC AGONISTS
Direct-Acting (Selective)
A. Alpha agonists (Alpha 1, Alpha2)
ALPHA-2 SELECTIVE
Causes Sedation and/or Depression
C (Clonidine) I: ADHD (next to Methylphenidate)
Combined with Labetalol to avoid rebound HTN
M (Methyldopa) DOC for HTN Pregnancy
G (Guanfacine)
B (Brimonidine)
A (Apraclonidine)
G (Guanabenz)

ADRENERGIC AGONISTS
Direct-Acting (Selective)
B. Beta agonists (Beta1, Beta2, Nonselective)
BETA-1 SELECTIVE
Dobutamine DOC: Cardiogenic
Shock

ADRENERGIC AGONISTS
Direct-Acting (Selective)
B. Beta agonists (Beta1, Beta2, Non-selective)
BETA-2 SELECTIVE Causes Tremor
> SABA (Relievers)
PAT-terols
(Prenalterol, Albuterol, Terbutaline)
> LABA (Controllers)
FS-terols
(Formoterol, Salmeterol)

ADRENERGIC AGONISTS
Direct-Acting (Selective)
B. Beta agonists (Beta1, Beta2, Nonselective)
NON-SELECTIVE
Isoproterenol I: Asthma
Obsolete use (Tolerance)
C. Dopa agonist
Fenoldopam

END OF ADRENERGIC
AGONISTS

Adrenergic Antagonists
(Sympathoplegics)
I. INDIRECT SYMPATHOPLEGICS
II. DIRECT SYMPATHOPLEGICS
A. Alpha Antagonists
Non-Selective Alpha Antagonist
Selective Alpha-1 Antagonist
Selective Alpha-2 Antagonist
B. Beta Antagonists
Non-Selective Beta Antagonist
Selective Beta-1 Antagonist
C. Mixed Alpha/Beta Antagonists

Adrenergic Antagonists
(Sympathoplegics)
I. INDIRECT SYMPATHOPLEGICS
G (Guanidine)
R (Reserpine)
II. DIRECT SYMPATHOPLEGICS
A. Alpha Antagonists
B. Beta Antagonists
C. Mixed Alpha/Beta Antagonists

DIRECT SYMPATHOPLEGICS
A. Alpha Antagonists

NON-SELECTIVE ALPHA ANTAGONISTS

PHEN (Phenoxybenzamine) I: Anti5HT
PHEN (Phentolamine) Vasodilator
SELECTIVE ALPHA ANTAGONISTS
>Selective Alpha-1 Antagonists
>Selective Alpha-2 Antagonists

DIRECT SYMPATHOPLEGICS
A. Alpha Antagonists

SELECTIVE ALPHA ANTAGONISTS

>Selective Alpha-1 Antagonists
INDICATION: Pheochromocytoma and HTN
T (Terazosin)
I (Indoramin)
T (Tamsulosin)
P (Prazosin)
A (Alfusozin)
D (Doxazosin)

DIRECT SYMPATHOPLEGICS
A. Alpha Antagonists

SELECTIVE ALPHA ANTAGONISTS

>Selective Alpha-2
Antagonists(Investigational)
R (Raunuolscine)
Y (Yohimbine)

DIRECT SYMPATHOPLEGICS
B. Beta Antagonists

NON SELECTIVE BETA ANTAGONISTS

AS LOCAL ANESTHETICS
L (Labetalol)
A (Acebutolol)
M (Metoprolol)
P (Propranolol)
P (Pindolol)

DIRECT SYMPATHOPLEGICS
B. Beta Antagonists

NON SELECTIVE BETA ANTAGONISTS

AS PARTIAL ANTAGONISTS
T (Timolol)
C (Carteolol)
L (Labetalol)
A (Acebutolol)
P (Penbutolol)
P (Pindolol)

DIRECT SYMPATHOPLEGICS
B. Beta Antagonists

NON SELECTIVE
SELECTIVE
Beta-1 Selective Antagonists
B (Bisoprolol)
B (Betaxolol)
E (Esmolol)
A (Atenolol)
A (Acebutolol)
M (Metoprolol)

DIRECT SYMPATHOPLEGICS
C. Mixed Alpha/Beta Antagonists

C (Carvedilol)
L (Labetalol)

END OF ADRENERGIC ANTAGONISTS

Cholinergic Agonists
(Cholinomimetics)

Cholinergic Agonists
(Cholinomimetics)
I. DIRECT-ACTING CHOLINOMIMETICS
II. CENTRALLY-ACTING
CHOLINOMIMETICS
III. INDIRECT-ACTING
CHOLINOMIMETICS

Cholinergic Agonists
(Cholinomimetics)
I. DIRECT-ACTING CHOLINOMIMETICS
A. Choline Esters
M (Metacholine)
A (Acetylcholine)
C (Carbachol)
Beth (Bethanechol)

Cholinergic Agonists
(Cholinomimetics)
I. DIRECT-ACTING CHOLINOMIMETICS
B. Alkaloids
Nico (Nicotine)
Lo (Lobeline)
Pi (Pilocarpine)
Mu (Muscarine)

Cholinergic Agonists
(Cholinomimetics)
II. CENTRALLY-ACTING
CHOLINOMIMETICS
I: Alzheimers
Don (Donepezil)
Galanta (Galantamine)
Tac (Tacrine)
Rivas (Rivastigmine)

Cholinergic Agonists
(Cholinomimetics)
II. INDIRECT-ACTING CHOLINOMIMETICS
>Carbamates
Neo (Neostigmine)
Phy (Physostigmine)
Py (Pyridostigmine)
Car (Carbaryl)
>Organophosphates
Mapa (Mala/Parathion)
Soman
Echo (Echothiopate)
>Edrophonium

End of Cholonergic Agonists

Cholinergic Antagonists

Cholinergic Antagonists
I. MUSCARINIC ANTAGONISTS
II. NICOTINIC GANGLIONIC
ANTAGONISTS
III. MIXED MUSCARINIC/NICOTINIC
ANTAGONISTS
A. Non-Depolarizing
B. Depolarizing

IV. CHOLINESTERASE REGENERATORS

Cholinergic Antagonists
I. MUSCARINIC ANTAGONISTS
C (Cyclopentolate)
A (Atropine)
S (Scopolamine)
H (Homatropine)
I (Ipratropium)
T (Tiotropium)
D (Dicyclomine)
O (Oxybutinin)
T (Tolterodine)
S (Solifenacin)

Cholinergic Antagonists
II. NICOTINIC GANGLIONIC
ANTAGONISTS
T (Trimethaphan)
T (Triethylammonium)
H (Hexamethonium)
M (Mecylamine)

Cholinergic Antagonists
I. MIXED MUSCARINIC/NICOTINIC
ANTAGONISTS
A. Non-Depolarizing
M (Mivacurium)
R (Rocuronium)
P (Pancuronium)
T (Tubocurarine)
M (Metocurine)
A (Atracurium)
D (Doxacurium)

Cholinergic Antagonists
I. MIXED MUSCARINIC/NICOTINIC
ANTAGONISTS
B. Depolarizing
Succinylcholine

END OF PRESENTATION

THANK
YOU!