Drugs Affecting The Autonomic Nervous System: Cholinergic Agents and Cholinergic Blocking Agents

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.
Lisa L. HHS: Hernandez: HHS: Is there copy missing at the end? Inhibiting what?
Adrenergic Agents: Mechanism of Action

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

Direct-Acting Agentbethanechol
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

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

Indirect-Acting Agentdonepezil (Aricept)
Used in the treatment of mild to moderate Alzheimers 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.

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.

Encourage patients with myasthenia gravis to take medication 30 minutes before eating to help improve chewing and swallowing.
When donepezil is prescribed for Alzheimers 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.

Atropine is the antidote for cholinergics. It should be available in the patients room for immediate use if needed.
Patients should notify their physician if they experience muscle weakness, abdominal cramps, diarrhea, or difficulty breathing.

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

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
Cholinergic Blocking Agents

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.
Cholinergic Blocking Agents: 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
Cholinergic Blocking Agents: Chemical Class

Natural
atropine belladonna hyoscyamine scopolamine
Synthetic/Semisynthetic
anisotropine dicyclomine hexocyclium ipratropium oxybutynin tolterodine clidinium glycopyrrolate homatropine isopropamide propantheline tridihexethyl
Drug Effects of Cholinergic Blocking Agents

Cardiovascular
Small doses: decrease heart rate Large doses: increase heart rate
CNS
Small doses: decrease muscle rigidity and tremors Large doses: drowsiness, disorientation, hallucinations

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

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
Cholinergic Blocking Agents: Therapeutic Uses

CNS
Decreased muscle rigidity and muscle tremors Parkinsons disease Drug-induced extrapyramidal reactions

Cardiovascular
Affect the hearts 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

Atropine
Used primarily for cardiovascular disorders
Sinus node dysfunction
Symptomatic second-degree heart block

Sinus bradycardia with hemodynamic compromise (advanced life support)

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

Respiratory agents are used to treat:
Exercise-induced bronchospasms Chronic bronchitis Asthma Chronic obstructive pulmonary disease

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

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

Genitourinary
Relaxed detrusor muscles of the bladder Increased constriction of the internal sphincter Reflex neurogenic bladder Incontinence
Cholinergic Blocking Agents: Side Effects

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

Body System
Eye
Dilated pupils, decreased visual accommodation, increased intraocular pressure Decreased salivation, decreased gastric secretions, decreased motility
Gastrointestinal

Body System
Genitourinary Glandular Respiratory
Urinary retention Decreased sweating Decreased bronchial secretions
Cholinergic Blocking Agents: Interactions

Antihistamines, phenothiazines, tricyclic antidepressants, MAOIs
When given with cholinergic blocking agents, cause ADDITIVE cholinergic effects, resulting in increased effects
Cholinergic Blocking Agents: Nursing Implications

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

Monitor for therapeutic effects:
For patients with Parkinsons disease: fewer tremors and decreased salivation and drooling For patients with peptic ulcer disease: decreased abdominal pain

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

Drugs Affecting The Autonomic Nervous System: Cholinergic Agents and Cholinergic Blocking Agents

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Drugs Affecting the Autonomic Nervous System

Cholinergic Agents and Cholinergic Blocking Agents

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.

Nicotinic receptors and Muscarinic receptors

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

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

Named muscarinic because can be stimulated by the alkaloid muscarine

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

Adrenergic Agents: Mechanism of Action

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

Adrenergic Agents: Mechanism of Action

Result: more ACh is available at the receptors

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

Indirect-Acting Cholinergic Agents (Cholinesterase Inhibitors)

The body must make new cholinesterase

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

Drug Effects of Cholinergic Agents

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

Drug Effects of Cholinergic Agents

Drug Effects of Cholinergic Agents

Increased salivation and sweating

Drug Effects of Cholinergic Agents

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

Drug Effects of Cholinergic Agents

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

Drug Effects of Cholinergic Agents

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

Cholinergic Agents: Therapeutic Uses

Topical application due to poor oral absorption

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

Cholinergic Agents: Therapeutic Uses

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

Cholinergic Agents: Therapeutic Uses

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

Cholinergic Agents: Therapeutic Uses

Helps to increase or maintain memory and learning capabilities.

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

Cholinergic Agents: Side Effects

Bradycardia, hypotension, conduction abnormalities (AV block and cardiac arrest)

Headache, dizziness, convulsions

Cholinergic Agents: Side Effects

Increased bronchial secretions, bronchospasms

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

Cholinergic Agents: Interactions

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

Cholinergic Agents: Nursing Implications

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

Cholinergic Agents: Nursing Implications

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

Cholinergic Agents: Nursing Implications

Cholinergic Agents: Nursing Implications

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

Cholinergic Agents: Nursing Implications

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

Cholinergic Agents: Nursing Implications

Occurrence of bowel movements

Cholinergic Blocking Agents

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

Cholinergic Blocking Agents: Mechanism of Action