Drugs Affecting The Autonomic Nervous System

Drugs Affecting the
Autonomic Nervous System

Cholinergic Agents and
Cholinergic Blocking Agents
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Cholinergic Agents
• Drugs that stimulate the

parasympathetic nervous system (PSNS)
• The PSNS is the opposing system to
the SNS

Cholinergic Agents
Also known as
• cholinergic agonists
or
• parasympathomimetics

Instructors may wish to use
EIC Image #56:
The Parasympathetic and

Sympathetic Nervous Systems
and
Their Relationships to One Another

Cholinergic Agents
• Mimic the effects of the PSNS

neurotransmitter
• Acetylcholine (ACh)

Cholinergic Receptors
Two types, determined by:

• Location
• Action once stimulated
Nicotinic receptors and Muscarinic receptors

Nicotinic Receptors
• Located in the ganglia of both the

PSNS and SNS
• Named “nicotinic” because can be stimulated
by the alkaloid nicotine

Muscarinic Receptors
• Located postsynaptically:
– Smooth muscle
– Cardiac muscle
– Glands of parasympathetic fibers
– Effector organs of cholinergic sympathetic fibers
• Named “muscarinic” because can be

stimulated by the alkaloid muscarine

Instructors may wish to
insert EIC Image #57:
The Sympathetic, Parasympathetic,

and Somatic Nervous Systems
This slide illustrates location of the nicotinic

and muscarinic receptors within the PSNS.

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• Direct-acting (agonist)
– Bind to cholinergic receptors, causing stimulation

Adrenergic Agents:
Mechanism of Action
• Indirect-acting
– Inhibit the enzyme “cholinesterase”
Result: more ACh is available at the receptors

Indirect-Acting Cholinergic Agents
(Cholinesterase Inhibitors)
• Reversible
– Bind to cholinesterase for a period of
minutes to hours
• Irreversible
– Bind to cholinesterase and form a permanent
covalent bond
– The body must make new cholinesterase

Drug Effects of Cholinergic Agents
• Effects seen when the PSNS is stimulated.

• The PSNS is the “rest and digest” system.

“SLUDGE”
• Salivation
• Lacrimation
• Urinary incontinence
• Diarrhea
• Gastrointestinal cramps
• Emesis
• Stimulate intestine and bladder

– Increased gastric secretions
– Increased gastrointestinal motility
– Increased urinary frequency
• Stimulate pupil
– Constriction (miosis)
– Reduced intraocular pressure
• Increased salivation and sweating

• Cardiovascular effects
– Decreased heart rate
– Vasodilation
• Respiratory effects
– Bronchial constriction, narrowed airways

• At recommended doses, the cholinergics

primarily affect the MUSCARINIC receptors.
• At high doses, cholinergics stimulate the
NICOTINIC receptors.

• DESIRED EFFECTS: from muscarinic

receptor stimulation
• Many undesirable effects are due to
stimulation of the nicotinic receptors

Cholinergic Agents:
Therapeutic Uses
Direct-Acting Agents
• Reduce intraocular pressure
• Useful for glaucoma and intraocular surgery
Examples: acetylcholine, carbachol, pilocarpine
Topical application due to poor oral absorption

Cholinergic Agents:
Therapeutic Uses
Direct-Acting Agent—bethanechol
• Increases tone and motility of bladder and GI tract
• Relaxes sphincters in bladder and GI tract, allowing
them to empty
• Helpful for postsurgical atony of the bladder
and GI tract
Oral dose or SC injection

Cholinergic Agents:
Therapeutic Uses
Indirect-Acting Agents
• Cause skeletal muscle contractions
• Used for diagnosis and treatment of
myasthenia gravis
• Used to reverse neuromuscular blocking agents
• Used to reverse anticholinergic poisoning (antidote)
Examples: physostigmine, pyridostigmine

Cholinergic Agents:
Therapeutic Uses
Indirect-Acting Agent—donepezil (Aricept)
• Used in the treatment of mild to moderate
Alzheimer’s disease.
• Helps to increase or maintain memory and
learning capabilities.

Cholinergic Agents: Side Effects
Side effects are a result of overstimulation
of the PSNS.
• Cardiovascular:
– Bradycardia, hypotension, conduction
abnormalities (AV block and cardiac arrest)
• CNS:
– Headache, dizziness, convulsions
• Gastrointestinal:
– Abdominal cramps, increased secretions,
nausea, vomiting
Cholinergic Agents: Side Effects
Side effects are a result of

overstimulation of the PSNS.
• Respiratory:
– Increased bronchial secretions, bronchospasms
• Other:
– Lacrimation, sweating, salivation, loss of
binocular accommodation, miosis

Cholinergic Agents: Interactions
• Anticholinergics, antihistamines,
sympathomimetics
• Antagonize cholinergic agents, resulting
in decreased responses

Cholinergic Agents:
Nursing Implications
• Keep in mind that these agents will stimulate
the PSNS and mimic the action of ACh.
• Assess for allergies, presence of GI or GU
obstructions, asthma, peptic ulcer disease,
or coronary artery disease.
• Perform baseline assessment of VS and
systems overview.

Cholinergic Agents:
• Medications should be taken as ordered
and not abruptly stopped.
• The doses should be spread evenly apart
to optimize the effects of the medication.
• Overdosing can cause life-threatening
problems. Patients should not adjust the
dosages unless directed by the physician.

Cholinergic Agents:
• Encourage patients with myasthenia gravis to
take medication 30 minutes before eating to
help improve chewing and swallowing.
• When donepezil is prescribed for Alzheimer’s
disease, be honest with caregivers and
patients that the drug is for management
of symptoms, not for a cure.
• Therapeutic effects of donepezil may not
occur for up to 6 weeks.
Cholinergic Agents:
• Atropine is the antidote for cholinergics.
It should be available in the patient’s room
for immediate use if needed.
• Patients should notify their physician if they
experience muscle weakness, abdominal
cramps, diarrhea, or difficulty breathing.

Cholinergic Agents:
Monitor for side effects, including:
Increased respiratory Abdominal cramping
secretions
Bronchospasms Dysrhythmias
Difficulty breathing Hypotension
Nausea and vomiting Bradycardia
Diarrhea Increased sweating
Increase in frequency and
urgency of voiding patterns

Cholinergic Agents:
Monitor for therapeutic effects:
• Alleviated signs and symptoms of myasthenia gravis
• In postoperative patients with decreased GI peristalsis,
look for:
– Increased bowel sounds
– Passage of flatus
– Occurrence of bowel movements
• In patients with urinary retention/hypotonic bladder,
urination should occur within 60 minutes of bethanecol
administration

• Drugs that block or inhibit the actions of

acetylcholine (ACh) in the parasympathetic
nervous system (PSNS)

Cholinergic Blocking Agents:
Mechanism of Action
• Competitive antagonists
• Compete with ACh
• Block ACh at the muscarinic receptors
in the PSNS
– As a result, ACh is unable to bind to the
receptor site and cause a cholinergic effect.

Mechanism of Action
• Once these drugs bind to receptors, they

inhibit nerve transmission at these receptors.

Instructors may wish to use
EIC Image #58:
Site of Action of Cholinergic Blockers

Within the PSNS

Chemical Class
Natural Synthetic/Semisynthetic
atropine anisotropine clidinium
belladonna dicyclomine glycopyrrolate
hyoscyamine hexocyclium homatropine
scopolamine ipratropium isopropamide
oxybutynin propantheline
tolterodine tridihexethyl

Drug Effects of
• Cardiovascular
– Small doses: decrease heart rate
– Large doses: increase heart rate
• CNS
– Small doses: decrease muscle rigidity
and tremors
– Large doses: drowsiness, disorientation,
hallucinations

Drug Effects of
• Eye
– Dilated pupils (mydriasis)
– Decreased accommodation due to paralysis
of ciliary muscles (cycloplegia)
• Gastrointestinal
– Relax smooth muscle tone of GI tract
– Decrease intestinal and gastric secretions
– Decrease motility and peristalsis

Drug Effects of
• Genitourinary
– Relaxed detrusor muscle
– Increased constriction of internal sphincter
– Result: urinary retention
• Glandular
– Decreased bronchial secretions, salivation, sweating
• Respiratory
– Decreased bronchial secretions
– Dilated bronchial airways

Therapeutic Uses
CNS
Decreased muscle rigidity and muscle tremors
• Parkinson’s disease
• Drug-induced extrapyramidal reactions

Therapeutic Uses
Cardiovascular
Affect the heart’s conduction system
• Low doses: slow the heart rate
• High doses: block inhibitory vagal effects on
the SA and AV node pacemaker cells
– Result: increased heart rate

Therapeutic Uses
Atropine
Used primarily for cardiovascular disorders
• Sinus node dysfunction
• Symptomatic second-degree heart block
• Sinus bradycardia with hemodynamic compromise
(advanced life support)

Therapeutic Uses
Respiratory
Blocking the cholinergic stimulation of the PSNS
allows unopposed action of the SNS.
• Results:
– Decreased secretions from nose, mouth,
pharynx, bronchi
– Relaxed smooth muscles in bronchi
and bronchioles
– Decreased airway resistance
– Bronchodilation
Therapeutic Uses
Respiratory agents are used to treat:
• Exercise-induced bronchospasms
• Chronic bronchitis
• Asthma
• Chronic obstructive pulmonary disease

Therapeutic Uses
Gastrointestinal
PSNS controls gastric secretions and smooth
muscles that produce gastric motility.
• Blockade of PSNS results in:
– Decreased secretions
– Relaxation of smooth muscle
– Decreased GI motility and peristalsis

Therapeutic Uses
Gastrointestinal agents are used to treat:
• Peptic ulcer disease
• Irritable bowel disease
• GI hypersecretory states

Therapeutic Uses
Genitourinary
• Relaxed detrusor muscles of the bladder
• Increased constriction of the internal
sphincter
• Reflex neurogenic bladder
• Incontinence

Side Effects
Body System Side/Adverse Effects
Cardiovascular Increased heart rate,
dysrhythmias
CNS CNS excitation, restlessness,
irritability, disorientation,
hallucinations, delirium

Side Effects
Eye Dilated pupils, decreased
visual accommodation,
increased intraocular pressure
Gastrointestinal Decreased salivation,

decreased gastric secretions,
decreased motility

Side Effects
Genitourinary Urinary retention
Glandular Decreased sweating
Respiratory Decreased bronchial secretions

Interactions
• Antihistamines, phenothiazines,
tricyclic antidepressants, MAOIs
• When given with cholinergic blocking
agents, cause ADDITIVE cholinergic
effects, resulting in increased effects

• Keep in mind that these agents will block
the action of ACh in the PSNS.
• Assess for allergies, presence of BPH,
glaucoma, tachycardia, MI, CHF, hiatal
hernia, and GI or GU obstruction.
• Perform baseline assessment of VS
and systems overview.

• Medications should be taken exactly as prescribed
to have the maximum therapeutic effect.
• Overdosing can cause life-threatening problems.
• Blurred vision may cause problems with driving

or operating machinery.
• Patients may experience sensitivity to light and

may want to wear dark glasses or sunglasses.

• When giving ophthalmic solutions, apply pressure to
the inner canthus to prevent systemic absorption.
• Dry mouth may occur; can be handled by chewing

gum, frequent mouth care, and hard candy.
• Check with physician before taking any other

medication, including OTC medications.
• ANTIDOTE for atropine is physostigmine salicylate

(Antilirium).

• Anticholinergics may lead to higher risk for
heat stroke due to effects on heat-regulating
mechanisms.
• Teach patients to limit physical exertion, and
avoid high temperatures and strenuous
exercise.
• Emphasize the importance of adequate fluid
and salt intake.

• Patients should report the following to their
physician: urinary hesitancy and/or retention,
constipation, palpitations, tremors, confusion,
sedation or amnesia, excessive dry mouth
(especially if they have chronic lung
infections or disease), or fever

Cholinergic Agents:
• Monitor for therapeutic effects:
• For patients with Parkinson’s disease:
fewer tremors and decreased salivation
and drooling
• For patients with peptic ulcer disease:
decreased abdominal pain

Monitor for side effects, including:
Constipation Tachycardia
Tremors Confusion
Hallucinations Sedation
Urinary retention Hot, dry skin
Fever
CNS depression (occurs with large doses of atropine)

Drugs Affecting The Autonomic Nervous System

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Drugs Affecting the

Autonomic Nervous System

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

• Drugs that stimulate the

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

The Parasympathetic and

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

• Mimic the effects of the PSNS

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Two types, determined by:

Nicotinic receptors and Muscarinic receptors

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

• Located in the ganglia of both the

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

• Named “muscarinic” because can be

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

The Sympathetic, Parasympathetic,

This slide illustrates location of the nicotinic

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Result: more ACh is available at the receptors

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

• Effects seen when the PSNS is stimulated.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

• Stimulate intestine and bladder

• Increased salivation and sweating

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

• At recommended doses, the cholinergics

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

• DESIRED EFFECTS: from muscarinic

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Topical application due to poor oral absorption

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Oral dose or SC injection

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Side effects are a result of

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

• Drugs that block or inhibit the actions of

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

• Once these drugs bind to receptors, they

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Site of Action of Cholinergic Blockers

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.