Autonomic Nervous System Drugs

Drugs Acting on the
Autonomic Nervous
System
Ms. Cres P. Quinzon
Salalah Nursing Institute
1
st
Semester 2014-2015

Objectives
By the end of this session, the students will be
able to:

Explain the mechanisms of action, uses, and
adverse effects.

Identify the common sympathomimetic and
parasympathomimetic drugs used in the
Sultanate of Oman

Objective 1

Explain the mechanisms of action,
uses, and adverse effects.

Contents
A. Sympathomimetic drugs
B. Asthma drugs (bronchodilators, corticosteroids,
sodium cromoglicate)
C. Adrenergic Blocking Agents
D. Parasympathomimetic drugs
E. Anticholinesterases
F. Synthetic atrophine like drugs
G. Drugs to prevent migraine
Autonomic Nervous System
Autonomic
Nervous System
Sympathetic
Nervous System
Parasympathetic
Nervous System
viscera
Gastrointestinal Tract
Respiratory and Urogenital
Heart and Blood vessels
Muscles of the eyes
Various secretory glands
Effects of Sympathetic and Parasympathetic Activity
Sympathetic Activity Parasympathetic Activity

Heart Rate increased Slowed
Blood Vessels constricted Dilated
Stomach / Intestine Decreased activity and
secretion
Increased activity and
secretion
Salivary / Bronchial glands Decreased secretion Increased secretion
Urinary bladder Body relaxed, sphincter
contracted
Body contracted, sphincter
relaxed
Bronchial muscle relaxed Contracted
Blood sugar raised
Eye Pupils dilated Pupils constricted,
accommodates for near
vision
Chemical Transmission of Nerve Impulses
Neurotransmitter- a substance liberated
through a stimulation of a nerve ending,
which activates a receptor in the organ
supplied or in another nerve cell.
Acetylcholine (ACh) in parasympathetic
Noradrenaline in sympathetic

Receptor - proteins that occur at the
surface of the cell or inside it.
Purpose is to bind the bodys chemical
messengers and transmit the binding event into
a signal that the cell can recognize and respond
to.
Nicotinic and Muscarinic in Parasympathetic
alpha 1, alpha 2, beta 1, beta 2 and beta 3 in
Sympathetic

Parasympathetic System
Acetylcholine Receptors: (Cholinergic)
After stimulation of the neurotransmitter,
acetylcholine (ACh), it acts on a cholinergic
receptor on the organ supplied by the nerve.
To prevent the effect of acetylcholine (ACh) being
too prolonged and powerful,
acetylcholineseterase, which is also present at the
nerve endings, rapidly breaks down the
acetylcholine and terminates its effect.
Sympathetic System
Adrenergic Receptors:

a1 receptors- these receptors are
stimulated by noradrenaline and adrenaline
produces constriction of blood vessels, causing
rise in blood pressure and reflex slowing of the
heart and dilatation of the pupil

Effects of adrenoreceptors: (Cont)
a2 receptors- when noradrenaline binds
with them, they limit further release of
noradrenaline, thus, forming a release
control mechanism to inhibit further
release of noradrenaline, and therefore,
useful to treat hypertension.
Effects of adrenoreceptors: (Cont)
b1 and b2 receptors- these receptors are
stimulated by isoprenaline and adrenaline
(epinephrine);
The effects are:
b1 increase in rate and excitability of the heart
with increased cardiac output
b2 responses dilatation of bronchi and blood
vessels
B3 receptors - present in cardiac muscle;
inotropic (depress the rate and force of
contraction)
Autonomic Nervous
System
Neurotransmitter
Preganglionic
neuron
Neurotransmitter
Postganglionic
neuron

Receptors on
Target tissue
Sympathetic Acetylcholine (ACh) Noradrenaline Adrenergic
Receptor
(a and b )
Parasympathetic Acetylcholine (ACh)

Acetylcholine Cholinergic
Muscarinic
Receptor

Autonomic Nervous
System
Neurotransmitter
Preganglionic
neuron
Receptors on
Target tissue
Sympathetic Acetylcholine
(ACh)
Adrenergic
Receptor
(a and b )
Parasympathetic Acetylcholine
(ACh)

Cholinergic
Muscarinic
Receptor

Sympathomimetic Drugs
Sympathomimetic drugs have similar effects to
those produced by activity of the sympathetic
nervous system and comprise:
Adrenaline
Noradrenaline
Isoprenaline
Selective b
2
agonists

1. Adrenaline (epinephrine)
Mechanism of Action:
Released from the medulla of the adrenal gland
when sympathetic system is activated
Acts on the sympathetic receptors of the visceral
organs (alpha and beta)
It is prepared synthetically
Destroyed by gastric acid, not effective to be taken
orally
Adrenaline (epinephrine)
Given by subcutaneous or intramuscular injection
Effects are more pronounced via IM site
Adrenaline (epinephrine) (cont)
Uses/Effects:
b1 effects:
increase in the force and rate of contraction
of the heart
Rise in systolic blood pressure due to
increased cardiac output
Adrenaline (epinephrine) (cont)
Uses/Effects:
Relaxes smooth muscle, including that of
bronchial tree (b2 effect).
Raises blood sugar by mobilizing glucose
from tissues
Following injection, it is rapidly broken
down by the enzymes and effects last for
only a few minutes

Adverse Effects:
Adrenaline (epinephrine) is given as an
intravenous bolus in small doses as a
stimulant to the heart in cardiac arrest.
It is essential not to inject larger doses into a
vein by mistake for this can precipitate fatal
cardiac arrhythmia.

2. Noradrenaline (norepinephrine)
Chemically closely related to adrenaline
(noradrenaline)
Noradrenaline acts on both alpha-1
and alpha-2 adrenoreceptors to cause
vasoconstriction

2.Noradrenaline (norepinephrine)
Uses/Effects:
Widespread vasoconstriction and thus, a rise in
both systolic and diastolic blood pressure (alpha-1
effect)
It is given by intravenous infusion

Uses/Effects:
Used in the treatment of various forms of
shock, which is usually associated with a
very low blood pressure

Adverse Effects:
Opinion has moved against using noradrenaline to
raise blood pressure except in extreme
circumstances, for although a satisfying rise in
blood pressure can be obtained due to
vasoconstriction, this also reduces the blood flow
to essential organs, esp. the kidney, with
troublesome results.

Adverse Effects: Nursing Point
A patient receiving noradrenaline (norepinephrine)
requires careful nursing monitoring and
assessment because blood pressure may fluctuate
widely with small changes in the rate of infusion.
Care should be taken to avoid extravasation, which
can cause necrosis.

3. Isoprenaline
Synthetic drug related to adrenaline
Well absorbed from the oral mucosa and following
inhalation
It is rapidly inactivated after absorption and its
effects are short lived.
Can also be given by infusion in severe bradycardia

3.Isoprenaline
isoprenaline stimulates beta-1 and beta-2
receptors but not alpha receptors

3. Isoprenaline
Uses:
Relaxes smooth muscle, including that of the
bronchial tree
stimulates the heart, but has little or no
effect on the blood pressure

3.Isoprenaline
Adverse Effects:
Avoid overdose as it can cause dangerous cardiac
arrythmias
Palpitation, nausea, headaches and tremors

4. Selective beta-2 Agonists
Mechanism of Action
Stimulate predominantly beta-2 receptors,
results in relaxation of bronchial smooth muscles.
- although they are effective bronchodilators, they
have minimal effects on the heart

4. Selective beta-2 Agonists (cont)
A. Salbutamol (short-acting)
The most widely used beta-2 agonist
Powerful bronchodilator
Action lasts about 4 hours
Can be given in various routes, but if given orally,
a considerable proportion is broken down in the
liver (first pass effect).

A. Salbutamol
Inhalation most common route
Maximum effect on the bronchi than elsewhere
Even so, only 10% of the dose reaches the
bronchial tree because the rest is being
swallowed

A. Salbutamol
Orally 3-4 times daily
Large dose should be given because of the first
pass effect (metabolize in the liver)

A. Salbutamol
Slowly by IV route
Treat severe asthma attack, though it is rare
because as a nebulizer is usually very effective
Salbutamol IV requires careful monitoring for
cardiac arrythmias

Salbutamol
Uses / Effects:
Treat bronchospasms due to asthma or bronchitis
It may be taken to relieve an attack or, on a
regular basis, control spasm.
It can also be used to inhibit premature labor and
treat hyperkalemia
Terbutaline, fenoterol, reproterol and babuterol
are other selective beta-2 agonists
4. Selective beta-2 Agonists(cont)
Salbutamol
Adverse Effects:
In large doses, it can cause tremor and
tachycardia and occasionally night cramps
Salmeterol and Eformeterol
Long-acting beta-2 agonists
Effective after about 30 mins and their action lasts
for about 12 hours; therefore, should not be used for
rapid effect in treating acute attack, but given 2x/day,
by inhalation, as a preventive
Salmeterol and Eformeterol
Claimed to have anti-inflammatory action as well as
relieving bronchospasm, but still is controversial
Can be combined with an inhaled steroid
Asthma Drugs
A. Bronchodilators
Inhaled beta-2 agonists
Oral beta-2 agonists
Methylxanthines
Anticholinergic drugs
B. Corticosteroids
C. Sodium Cromoglicate
Asthma Drugs
A. Bronchodilators
1. Inhaled beta-2 agonists
Widely prescribed
Given by inhalation to treat a developing attack
or prevent attack (exercise-induced asthma)
Dont control the inflammatory component of
asthma and there is evidence that regular use
can lead ultimately to more severe and
sometimes fatal attack
Corticosteroid can be added to a regular use of
beta-2 agonist to control asthma
Asthma Drugs
A. Bronchodilators
2. oral beta-2 agonists
Salbutamol tablets are not very efficient, but
salbutamol control-release tablets, at a dose of
one a night, have a prolonged action and are
useful in preventing nocturnal attacks of
asthma
3. Methylxanthines
relax and relieve spasm
Asthma Drugs
A. Bronchodilators
3. Methylxanthines (cont)
Aminophylline and theophylline , though they
are effective, they require careful use, as there
is only small difference between the
therapeutic and toxic dose.
Asthma Drugs
A. Bronchodilators
Aminophylline can be given slow IV to
terminate acute attack
Can be given as loading dose followed by an
infusion by pump
Plasma levels should be measured at intervals
if to be given prolonged as a guide to dosage
High plasma levels may result if oral and IV
administration are combined and this can be
dangerous

Asthma Drugs
A. Bronchodilators
Always ask if the patient is taking a
methylxanthine orally before giving
intravenous
Adverse Effects:
Dose related and include nausea, anxiety,
tachycardia, arrhythmias and convulsions

Asthma Drugs
A. Bronchodilators

Interactions are common and effects are
increased by cimetidine, erythromycin and oral
contraceptives

Asthma Drugs
A. Bronchodilators
4. Anticholinergic Drugs
- Ipratropium bromide related to atropine
Anticholinergic agent, and acts as bronchodilator
Asthma Drugs
A. Bronchodilators
4. Anticholinergic Drugs
- Ipratropium bromide (cont)
- Given via inhaler or nebulizer
- Any of the drug that is swallowed is not absorbed
from the intestine
- It should be used for those patients who have not
responded to beta-2 agonists

Asthma Drugs
A. Bronchodilators
4. Anticholinergic Drugs (cont)
- Ipratropium bromide
- Effects begin after 45 minutes and lasts 3-4 hours;
therefore, has to be taken to prevent asthma attack
- Can be combined with a beta-2 agonist or
corticosteroid

Asthma Drugs
A. Bronchodilators
4. Anticholinergic Drugs (cont)
- Ipratropium bromide
- Adverse Effects:
- Unpleasant taste and dry mouth due to blocking of
salivation

Asthma Drugs
B. Corticosteroids (Steroids)
- Reduce inflammation and allergic aspects of asthma
and decrease bronchospasm in severe and
persistent asthma
- Beclamethasone (steroid that is well absorbed from
mucous surfaces) can be given by inhalation

Asthma Drugs
B. Corticosteroids (Steroids) cont
- Fluticasone has the same benefits with less
systemic effects
- Occasional candida infection of the mouth may
occur, presumably due to the lowering of local
resistance by the steroid
- Hoarse voice may occur due to weakening of voice
chords

Candida albicans in mouth
Asthma Drugs
B. Corticosteroids (Steroids) cont
- These effects usually disappears when the drug is
stopped or the dose is reduced.
- In a few resistant case of asthma, oral prednisone
will be required, at the minimal effective dose

Asthma Drugs
- Mechanism of Action:
- Prevents asthmatic attack by stopping the release
of histamine from bronchial mast cells that are
responsible for bronchospasm.

Pressurized aerosol or rotahaler
Asthma Drugs
- Given regularly by pressurized aerosol or rotahaler.
- Usual dose is four inhalations daily
- Most effective in young patients with an allergic
history of asthma and is of some use in non-allergic
asthma
Asthma Drugs
- Nedocromil also a mast cell stabilizer and anti-
inflammatory drug, and is very similar to sodium
cromoglicate
- Given as a pressurized aerosol and is used to
prevent rather than treat attacks
Asthma Drugs
D. Leukotrienes Modifiers
- Leukotrienes are substances produced by leucocytes
involved in the inflammatory response and which
cause spasm of the bronchial muscle
Asthma Drugs
- Leukotriene modifiers prevent spasm either by
blocking the action of leukotrienes or by preventing
inflammation.
Asthma Drugs
- They also diminish hyperactivity of the bronchial
mucosa and reduce inflammation.
- Zileuton, Montelukast and Zafirlukast (block
leukotriene receptors)
Asthma Drugs
Montelukast, can be given orally to adults and
children over age 6.
At present it is used as a continuous treatment for
mild-to-moderate asthma and may reduce the need
for other drugs.
It is also useful in preventing exercise-induced
asthma
Adrenergic Blocking Agents

it is possible to block alpha and beta- adrenergic
receptors selectively
Alpha-1 adrenergic blocker
uses: hypertension and bladder neck
obstruction

Adrenergic Blocking Agents (cont)
Hypertension : blocks the vasoconstrictor action of
noradrenaline causing dilatation of arterioles and
lowering blood pressure

Bladder Neck Obstruction:
-Alpha-1 adrenergic receptors control the smooth
muscle round the neck of the bladder

Bladder Neck Obstruction: cont
- By blocking these receptors it is possible to relax this
muscle and partially relieve bladder neck obstruction
due to an enlarged prostate

Beta Adrenergic Blockers
block the effects of adrenaline and noradrenaline
on beta-adrenergic receptors

Beta Adrenergic Blockers
-Widely used and more important than the
alpha-blocking drugs
-have the same effects and uses but with minor
differences:

Some beta-blocking drugs block predominantly
beta-1 adrenoreceptors (ex. cardiac beta
receptors) and are called selective beta-blockers
Others block both beta-1 and beta-2 receptors (ex.
Cardiac + bronchi + peripheral blood vessel
receptors) and are called non-selective beta-
blockers
General Actions of Beta-blockers
Cardiovascular Actions:
When 1 receptors in the heart are blocked, the
heart rate is slowed, the cardiac output is reduced
and the work done by the heart is thus
decreased.

Cardiovascular Actions:
In addition, the excitability of heart muscle is
reduced.
-Blockers lower blood pressure

Respiratory Actions:
Blocking 2 receptors with -blockers cause
bronchospasm, particularly in patients with
asthma.
This is particularly marked with non-selective
-blockers such as propanolol.
This is usually of little consequence in healthy
people, but in patients with asthma it may
make bronchospasm worse and increase
dyspnea.
Respiratory Actions: cont
Selective 1-blockers have less effect on 2
receptors.
Metabolic Actions:
Some -blockers prevent the rise in blood
glucose which normally follows increased
sympathetic activity.
CNS Actions:
Some sedation is fairly common in patients
receiving -blockers and occasionally this may
be severe.
In addition, vivid dreams and, more rarely,
hallucinations may occur.
Uses:
Angina of effort because they reduce the work
of the heart, especially on effort or
excitement.
Cardiac arrhythmias, because they reduce the
excitability of the heart.
Hypertension, as they lower blood pressure,
perhaps by setting the regulation of blood
pressure at a lower level.
Uses:
Thyrotoxicosis and anxiety, because they
reduce the increased sympathetic activity
which occurs in these disorders.
Essential tremor, a rare familial condition
characterized by severe intention tremor.
Prevention of migraine attacks
Adverse Effects:
exacerbation of heart failure
Occasionally cause vivid dreams and
hallucinations,
decreasing cardiac output, they reduce the
blood flow to the extremities, causing the
patient to feel cold, and are best avoided in
peripheral vascular disease.
Adverse Effects:
They mask the usual warning symptoms of
hypoglycemia and can be dangerous in
patients with diabetes who are taking insulin.
Active people may feel less energetic whilst
taking these drugs
Parasympathomimetic
Drugs
Parasympathomimetic drugs have effects
similar to those produced by activity of the
parasympathetic nervous system. Examples
are:
Acetylcholine
Carbachol
Bethanechol
Pilocarpine

Parasympathomimetic
Drugs
Acetylcholine
acetylcholine activates voluntary muscle when a
motor nerve is stimulated and is essential for all
voluntary movements.
Its action is very short lived, as it is quickly
broken down by cholinesterase to choline and
acetate, so it is not used therapeutically.

Parasympathomimetic
Drugs
Acetylcholine cont
However, a prolonged effect can be produced either
by giving an acetylcholine-like drug which is not
broken down or by using a drug which inhibits the
action of cholinesterase, thus prolonging and
intensifying the actions of naturally occurring
acetylcholine.
This type of drug is called an anticholinesterase

Parasympathomimetic
Drugs
Carbachol
Carbachol is a synthetic substance chemically related
to acetylcholine.
Its actions resemble those of parasympathetic
stimulation.
It is not broken down by the body cholinesterases
and its actions are therefore much more prolonged
than those of acetylcholine.

Parasympathomimetic
Drugs
Carbachol Uses:
The most important therapeutic use of carbachol is
in the treatment of urinary retention following
surgical operation or childbirth when there is no
mechanical obstruction.
It causes contraction of the bladder muscle, resulting
in the passage of urine
Parasympathomimetic
Drugs
Administration and Effects of carbachol after
injection
Carbachol may be given by subcutaneous injection or
by mouth.
After subcutaneous injection, flushing and sweating
appear in about 20 minutes, followed by increased
intestinal peristalsis, sometimes with colic, and
contraction of the bladder muscle.
These actions last up to an hour.
Parasympathomimetic
Drugs
Adverse Effects
include colic, diarrhoea and a marked fall in blood
pressure.
These adverse effects are controlled by atropine.
Parasympathomimetic
Drugs
Bethanechol
Bethanechol is another acetylcholine-like drug,
which, like carbachol, is not broken down by
cholinesterase.
Parasympathomimetic
Drugs
Pilocarpine
Pilocarpine is used only as eye drops, where it
causes constriction of the pupil
Anticholinesterases
These drugs prevent the breakdown of acetylcholine
by cholinesterase produced at nerve endings
throughout the body.
Anticholinesterases
Important Effects
The eye: absorbed through the conjunctiva and
following application to the eye cause constriction
of the pupil and spasm of accommodation.
Gastrointestinal tract: cause increased tone and
motility.
Urinary tract: cause contraction of the bladder.
Anticholinesterases
Clinically-used anticholinesterases
Several anticholinesterases are used to treat a
variety of disorders, depending on where their
actions are most pronounced:
neostigmine
physostigmine
pyridostigmine
edrophonium
distigmine.
Anticholinesterases
Clinically-used anticholinesterases (cont)
Neostigmine is a synthetic anticholinesterase with
actions very similar to those of physostigmine, but
with an effect on the neuromuscular junction of
voluntary muscle and less on the eye and
cardiovascular system.
It is rapidly effective following subcutaneous or
intramuscular injection and is also absorbed after
oral administration, although this route requires
larger doses.
Anticholinesterases
Uses of Neostigmine:
Neostigmine is used widely in the treatment of
disorders of the voluntary muscle (e.g. myasthenia
gravis*), and has been used in cases of paralytic
ileus and atony of the bladder.
*Myasthenia gravis a form of muscular
paralysis through Ach receptor failure

Anticholinesterases
Uses of Neostigmine:
Pyridostigmine and edrophonium are
anticholinesterases used in the treatment of
myasthenia gravis.
Edrophonium has a very short-lived action.
Distigmine has widespread actions and may also
be used for urinary retention and myasthenia
gravis.
It can be given orally or by injection.
Anticholinesterases
Adverse Effects:
intestinal colic and diarrhoea
sweating and salivation
pupils are constricted
pulse slow
blood pressure low.

Treatment: The immediate treatment is atropine
given intravenously
Synthetic Atropine-like
Drugs
shorten the duration of action of the drug, e.g.
tropicamide for use in the eye, or to target certain
specific subtypes of the muscarinic receptor.
For example, trihexyphenidyl is used clinically to
treat Parkinson's disease since it is claimed
selectively to target M1 muscarinic receptors in the
brain.
Synthetic Atropine-like
Drugs
Among those available are:
dicycloverine
mebeverine
propantheline
oxybutynin
flavoxate
Drug to Prevent Migraine
Drugs used to prevent migraine attacks:
-blockers
pizotifen
sodium valproate
antidepressants
methysergide
-Blockers prevent or reduce attacks in about half of
the patients.
They probably act by reducing vasodilation
When they are prescribed, their contraindications
must be remembered and they should not be
combined with ergotamine.
Pizotifen
prevents migraine attacks by reducing the
constriction and dilatation of blood vessels.
It can cause drowsiness and the initial dose should
be given at night.
Its main adverse effect is weight gain and it may take
up to a month to be effective.
Sodium valproate
is an antiepileptic agent that can also be used to
prevent migraine attacks.
It should not be used in pregnancy, owing to the risk
of fetal malformation
Antidepressants
Dosulepin and amitriptyline are effective, even if the
patient is not suffering from depression
Methysergide
Methysergide blocks the effects of 5-HT (serotonin)
on receptors in smooth muscle leading to
vasoconstriction.
It is effective but has serious adverse effects and
should only be used when safer treatment has failed.
Anti-Migraine Drugs Used in Oman

Major Classification Sub
classification
Examples or Drugs Used in
Oman
Anti-migraine Ergotamine tartrate and
caffeine
Flunarizine hydrochloride
Naratriptan
Rizatriptan
Sumatriptan succinate
zolmitriptan
Anti-Migraine Drugs Used in Oman

Major
Classification
Sub classification Examples or Drugs
Used in Oman
Antiepileptic For grandmal and
partial
seizures
Carbamazine
Clonazepam
Ethosuximide
Gabapentin
Leveitracetam
Phenobarbital /
phenobarbitone
Phenytoin sodium
Sodium valproate
Topiramate
Patient and Family Education
Migraine Drugs
1. Take medication at onset of pain, when
possible, to prevent development of more
severe symptoms
2. With triptans, take oral drugs with fluids. If
symptoms recur, a second dose may be taken.
However, do not take a second dose of
sumatriptansooner than 2 hours after the first
dose. Do not take more than 300mg of
sumatriptanin any 24 hour period.
Patient and Family Education
Migraine Drugs
3. Sumatriptan can be taken by mouth,
injection, or nasal spray. Do not take more than
40 mg of nasal spray in any 24-hour period. If
self-administering injectable sumatriptan, be
sure to give in fatty tissue under the skin.
4. With ergot preparation, reports signs of
vascular insufficiency, such as tingling sensation
or coldness, numbness, or weakness of the
extremities. These are symptoms of ergot
toxicity.

Autonomic Nervous System Drugs

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