(Cholinergics and Anti-cholinergics)

Prof Dr M.T. Kamaluddin

Bagian Farmakologi FK Unsri
2012

Divisions of human
nervous system

Nervous system

ANS / SNS
Autonomic nervous system controls
involuntary activities of smooth muscle,
secretory glands and the visceral organs of
the body such as the heart (involuntary
activities of smooth muscle)
Somatic nervous system innervates the
skeletal muscles and controls voluntary
movement

Autonomic Nervous
System Sympathetic Nervous System
Para sympathetic System
Enteric System

Sympathetic Nervous System

Parasympathetic Nervous
System
75% of all parasympathetic nerve fibers are in

the vagus nerves

These nerves supply the thoracic and
abdominal organs, which innervate the heart,
lungs, esophagus, stomach, small intestine,
proximal half of the colon, liver , gallbladder,
pancreas and upper portions of the ureters

Parasympathetic Nervous
System
Also supply the muscles of the eyes, lacrimal,

nasal, submaxillary, and parotid glands;

descending colon and rectum; lower portions
of the ureters, bladder and genitalia
All are regulated by acetylcholineexerts
excitatory effects at nerve synapses and
neuromuscular junctions; and inhibitory
effects at peripheral sites e.g. heart

Neurotransmitters
Neurotransmitters
Acetylcholine: skeletal muscle
Norepinepherine: stress response

Body Responses
Dilation of blood vessels in skin
Decrease heart rate (bradycardia)
Increase secretion of digestive enzymes
Constriction of smooth muscle of bronchi
Increase in sweat glands
Contraction of smooth muscles of urinary
bladder
Contraction of smooth muscle of skeletal
system

Cholinergic Agents
Direct acting - act on the receptors to
activate a tissue response
Indirect acting - inhibit the action of the
enzyme cholinesterase
(acetylcholinesterase - ACH)
: Major uses
, Stimulate bladder & GI tone
, constrict pupils (miosis)
neuromuscular transmission

Cholinergic Receptors
:Two types, determined by
Location
Action once stimulated

Nicotinic receptors
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

Cholinergic Agent
(Parasympathomimetics)
Bethanechol (Urecholine) selective to
muscarinic receptors, mimic action of
acetylcholine
Use - For urinary retention
Take on an empty stomach d/t inc. peristalsis *
Alert- Never give IM or IV circulatory
*
collapse, hypotension, shock & cardiac arrest
.poss
Pilocarpine (Pilocar) - Ophthalmic - direct
acting

Parasympathetic Nervous
System
: Functions stimulated by PNS
, Resting
, reparative
vegetative function

Autonomic Drugs
Drugs used due to their ability to stimulate or
block activity of the sympathetic or
.parasympathetic nervous system

Effect of Drugs
Drugs that act of ANS usually affect
.the entire body
Effects depend on whether you are
.trying to stimulate or inhibit function

Receptor Activity
Drugs are developed to stimulate or inhibit
.particular subtypes of receptors
.More selective on particular body tissues
Decrease adverse effects on other body
.tissues side effects

Cholinergic Drugs
Parasympathomimetics or cholinomimetics
Stimulate parasympathetic nervous system in

same manner as does acetylcholine

May stimulate cholinergic receptors directly or
slow acetylcholine metabolism at synapses
(affect the enzyme acetylcholinesterase)

Cholinergic Drugs
Useful in treating
Alzheimers Disease,
Myasthenia gravis,
atony of the smooth muscle of the GI system or
urinary system

Cholinergic Drugs
Normal neuromuscular function, acetylcholine

binds to nicotinic receptors on cell

membranes of muscle cells to cause
contraction
Myasthenia gravis autoantibodies presumably
destroy nicotinic receptors; thus, acetylcholine
less able to stimulate muscle contraction.
Results in severe muscle weakness.

Cholinergic Drugs
Acetylcholine important neurotransmitter

affecting cognitive functioning, memory

storage and retrieval
In Alzheimers disease (AD), abnormalities of
the cholinergic, serotonergic, noradrenergic,
and glutaminergic neurotransmission systems
In cholinergic system, patient with AD found to
have loss of neurons that secrete acetylcholine

Cholinergic DrugsGI
effects
Acetylcholine stimulates cholinergic receptors in the

gut to promote normal secretory and motor activity

Cholinergic activity in the gut will increase peristalsis
and facilitates movement of flatus and feces
The secretory functions of the salivary and gastric
glands also stimulated

Cholinergic DrugsGU
effects
Acetylcholine stimulates cholinergic receptors

in the urinary system to promote urination

Results in contraction of the detrusor muscle
and relaxation of the urinary sphincter to
facilitate emptying of the urinary bladder

Acetylcholine
One of the main neurotransmitters of the ANS is

acetylcholine
Acetylcholine is released at preganglionic fibers
of both the sympathetic and parasympathetic
nervous system
Also released from postganglionic sympathetic
neurons that innervate the sweat glands and
from motor neurons that innervate the skeletal
muscles

Acetylcholine
Sympathetic and parasympathetic divisions of

the ANS are antagonistic to each other

When acetylcholine acts on body cells that
respond to parasympathetic stimulation, it
interacts with two types of cholinergic
receptors: nicotinic and muscarinic

Acetylcholine
Nicotinic receptors are located in motor

nerves and skeletal muscle

Stimulation results in muscle contraction

Acetylcholine
Muscarinic receptors are located in :
most internal organs.
This includes the cardiovascular, respiratory,
gastrointestinal, and genitourinary. Stimulation of the
muscarinic receptors may result in either excitation or
inhibition, depending on the organ involved.

Mechanisms of ActionDirect
Acting Cholinergics
Direct acting cholinergics are lipid insoluble
Do not readily enter the CNS so effects are peripheral
Resistant to metabolism by acetylcholinesterase
Effects are longer acting than with acetylcholine

Direct Acting Cholinergic Drugs

.cont
Widespread systemic effects when they

combine with muscarinic receptors in :

cardiac muscle,
smooth muscle,
exocrine glands
the eye

Direct-acting Cholinergic Drugs

Effects
Decreased heart rate, vasodilation, variable

BP effects
Increased tone and contractility in GI smooth
muscle, relaxation of sphincters, increased
salivary gland and GI secretions
Increased tone and contractility of smooth
muscle in urinary bladder and relaxation of
the sphincter

Direct Acting Cholinergic Drugs

.cont
Increased tone and contractility of bronchial

smooth muscle
Increased respiratory secretions
Constriction of pupils (miosis) and contraction
of ciliary muscle

Direct Acting Cholinergics

Bethanecol (Urecholine)given orally. Not

given IM or IV.
Used to treat urinary retention due to bladder
atony and for postoperative abdominal
distention due to paralytic ileus

Indirect-Acting Cholinergic
Drugs
Action is by decreasing the inactivation of

acetylcholine in the synapse by the enzyme

acetylcholinesterase
Accumulation of acetylcholine then occurs
which enhances the activation of the nicotinic
and muscarinic receptors

Indirect-Acting or
.Anticholinesterase Drugs cont
Anticholinesterase drugs are either reversible

or irreversible inhibitors of
acetylcholinesterase
Reversible agents are such drugs
as:edrophodium (Tensilon). Used to diagnose
myasthenia gravis and for reversal of nondepolarizing neuromuscular blockers

Indirect-acting agents
.cont
Neostigmine (Prostigmine)prototype

anticholinesterase agent. Used for long-term

tx of myasthenia gravis and as an antidote for
tubocurarine and other non-depolarizing
agents in surgery.
Poorly absorbed orally so requires larger
doses than when given parenterally.
Can develop resistance to its action over time

Indirect Acting Agents

Pyridostigmine (Mestinon) is the maintenance

drug of choice for patients with Myasthenia

gravis. Slow release.

Indirect ActingReversible
.cont
Physostigmine (Antilirium)only

anticholinesterase capable of crossing the

blood brain barrier. Is more lipid soluble. Used
as an antidote for overdosage of
anticholinergics such as: atropine,
antihistamines, TCA, phenothiazines. May also
be used in tx of glaucoma.

Indirect Acting Agents used to treat

Alzheimers disease
Donepezil (Aricept)said to delay

progression of the disease by up to 55

weeks. Does not cause liver toxicity.
Galantamine (Reminyl)newest kid on the
block
Rivastigmine (Exelon) long acting. Twice a
day dosing.
Tacrine (Cognex)hepatoxic. Elevated liver
enzymes usu. Within 18 wks. > in women.

Specific Conditions
Distinction between cholinergic crisis and a

myasthenic crisis
Difficult to ascertain as both are characterized
by respiratory difficulty or failure
Need to distinguish as require opposite
treatment measures

Specific ConditionsCholinergic vs.

Myasthenic Crisis
Myasthenic crisis requires more

anticholinesterase drug whereas cholinergic

crisis requires discontinuation of the
anticholinesterase drugs
Diagnosis can be made by evaluating
patient patient response to their medication
(s/s one hour after medication often is
cholinergic crisis, s/s 3 or more hours after
medication often is myasthenic crisis

Myasthenia Gravis
If s/s not clearly indicative of the problem,

may have to intubate patient, inject dose of IV

edrophonium. If dramatic improvement in
breathing, diagnosis is myasthenic crisis. If
edrophonium makes s/s worse, the diagnosis
is cholinergic crisis. Patient must be intubated
and assisted with mechanical ventilation to
perform this test.

Toxicity of Cholinergic
Drugs
Atropine is the specific antidote to cholinergic
agents
Atropine reverses only the muscarinic effects
of cholinergic drugs; heart, smooth muscle,
and glands.
Atropine cannot reverse the nicotinic effects
of skeletal muscle weakness or paralysis due
to overdose of indirect cholinergic drugs.

Toxicity of Irreversible
Anticholinesterase Agents
These agents are lipid soluble
Can enter the body by the eye,skin,

respiratory system and GI tract.

Case in point, organophosphate insecticides
(malathion, parathion) or nerve gases (sarin,
tabun, soman)
These agents cause excessive cholinergic
stimulation (muscarinic) and neuromuscular
blockade

.Toxicity cont
Cholinergic crisis occurs because the

irreversible anticholinesterase poison binds to

the enzyme acetylcholinesterase and
inactivates it. Thus, acetylcholine remains in
cholinergic synapses causing excessive
stimulation of muscarinic and nicotinic
receptors.

.Toxicity cont
Emergency tx includes:
1. Decontamination of clothing
2. Flushing poison from skin and eyes
3. Activated charcoal and lavage for GI

ingestion
4. Atropine to counteract the muscarinic
effects

.Toxicity cont
To relieve the neuromuscular blockade by

nicotinic effects, give pralidoxime

(Protopam), a cholinesterase reactivator.
Pralidoxime causes the anticholinesterase
poison to release the enzyme
acetylcholinesterase.
Give Pralidoxime as soon as possible as if
too much time passes, the poison bond
becomes too strong for the pralidoxime to
work.

(Cholinergics and Anti-cholinergics)

Prof Dr M.T. Kamaluddin

Bagian Farmakologi FK Unsri
2012

Nervous system

Nervous system

Neurotransmitter systems

System
Noradrenaline
system

Dopamine
system

Origin
locus coeruleus
Lateral tegmental field

arousal
reward

dopamine pathways:
mesocortical pathway
mesolimbic pathway
nigrostriatal pathway
tuberoinfundibular pathway

motor system, reward,

cognition, endocrine, nausea

caudal dorsal raphe nucleus

Serotonin
system

Cholinergic
system

Effects

rostral dorsal raphe nucleus

pontomesencephalotegmental
complex
basal optic nucleus of Meynert
medial septal nucleus

Increase (introversion), mood,

satiety, body temperature and
sleep, while decreasing
nociception.
learning
short-term memory
arousal
reward

Common neurotransmitters

Abbreviation

Category

Name

Small: Amino
acids

Aspartate

Neuropeptides

N-Acetylaspartylglutamate

NAAG

Small: Amino
acids

Glutamate (glutamic acid)

Glu

Small: Amino
acids

Gamma-aminobutyric acid

GABA

Small: Amino
acids

Glycine

Small:
Acetylcholine
Small:
Monoamine (
Phe/Tyr)

Metabotropic

Ionotropic

Metabotropic glutamate receptors;

selective agonist of mGluR3

Metabotropic glutamate receptor

NMDA receptor,
Kainate receptor,
AMPA receptor

GABAB receptor

GABAA, GABAC

Gly

Glycine receptor

Acetylcholine

Ach

Muscarinic acetylcholine receptor

Nicotinic acetylcholine
receptor

Dopamine

DA

Dopamine receptor

Small: Monoamine (Phe/Tyr)

Norepinephrine (noradrenaline)

NE

Adrenergic receptor

Small: Monoamine (Phe/Tyr)

Epinephrine (adrenaline)

Epi

Adrenergic receptor

Small: Monoamine (Phe/Tyr)

Octopamine

Small: Monoamine (Phe/Tyr)

Tyramine

Small: Monoamine (Trp)

Serotonin (5-hydroxytryptamine)

Small: Monoamine (Trp)

Melatonin

Small: Monoamine (His)

Histamine

PP: Gastrins

Gastrin

PP: Gastrins

Cholecystokinin

PP: Neurohypophyseals

5-HT

Serotonin receptor, all but 5-HT3

5-HT3

Mel

Melatonin receptor

Histamine receptor

Cholecystokinin receptor

Vasopressin

Vasopressin receptor

PP: Neurohypophyseals

Oxytocin

Oxytocin receptor

PP: Neurohypophyseals

Neurophysin I

PP: Neurohypophyseals

Neurophysin II

PP: Neuropeptide Y

Neuropeptide Y

NY

Neuropeptide Y receptor

PP: Neuropeptide Y

Pancreatic polypeptide

PP

PP: Neuropeptide Y

Peptide YY

PYY

PP: Opioids

Corticotropin (adrenocorticotropic
hormone)

Corticotropin receptor

PP: Opioids

Dynorphin

PP: Opioids

Endorphin

PP: Opioids

Enkephaline

PP: Secretins

Secretin

Secretin receptor

PP: Secretins

Motilin

Motilin receptor

PP: Secretins

Glucagon

Glucagon receptor

CCK

ACTH

PP: Secretins

Vasoactive intestinal peptide

VIP

Vasoactive intestinal peptide

receptor

PP: Secretins

Growth hormone-releasing factor

GRF

PP: Somtostatins

Somatostatin

Somatostatin receptor

SS: Tachykinins

Neurokinin A

SS: Tachykinins

Neurokinin B

SS: Tachykinins

Substance P

PP: Other

Bombesin

PP: Other

Gastrin releasing peptide

GRP

Gas

Nitric oxide

NO

Gas

Carbon monoxide

CO

Other

Anandamide

AEA

Cannabinoid receptor

Other

Adenosine triphosphate

ATP

P2Y12

P2X
receptor

Drug Effects of Cholinergic Agents

SLUDGE
Salivation
Lacrimation
Urinary incontinence
Diarrhea
Gastrointestinal cramps
Emesis

Anticholinergics
Also called cholinergic blocking agents or

parasympatholytics
Again, focus is on the parasympathetic
nervous system
Parasympathetic system acts as a resting and
reparative function
Functions include digestion, excretion, cardiac
decelertion, anabolism and near vision

Anticholinergics
Most anticholinergic drugs interact with the

muscarinic receptors in the brain, secretory

glands, heart, and smooth muscle
A few can also affect the nicotinic receptors.
Ex : Glycopyrrolate (Robinul)
Drugs that block or inhibit the actions of acetylcholine (ACh)
in
the parasympathetic nervous system (PSNS)

Mechanism of Action and

Effects
Act by occupying receptor sites at

parasympathetic nerve endings, thereby

leaving fewer receptor sites free to respond to
acetylcholine
Distribution of receptors is broad so effects of
anticholinergics will be diffuse.

Parasympatholytic - inactivate cholinergic

receptors

Cholinergic Blocking
Agents: Mechanism of
Competitive antagonists
Action
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

Once these drugs bind to receptors, they

.inhibit nerve transmission at these receptors

Drug Effects of
Cholinergic Blocking

Cardiovascular
Agents
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
Cholinergic
Blocking
Eye

Dilated
pupils
(mydriasis)
Agents
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
Cholinergic
Blocking
Genitourinary
Agents
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: Nursing
Anticholinergics may lead to higher risk for
Implications

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

Effects on Body Tissues

CNS stimulation followed by depression, can
result in coma and death (atropine,
antiparkinsons)
2. Decreased cardiovascular response to vagal
stimulation resulting in tachycardia. Increases
vagal tone. (Atropine), acts as sympathetic
effects.
3. Bronchodilation and decreased respiratory tract
secretions.
1.

Effects on Body Tissues

Antispasmotics of GI tract due to decreased

tone and motility.

Mydriasis and cyclopegia. Normally do not
increase IOP but caution as can precipitate
acute glaucoma.
Can cause decreased oral secretions, decreased
sweating, relaxation of urinary bladder

Indications for Use

Uses include GI, GU, ophthalmic and

respiratory disorders, bradycardia and in

Parkinsons disease.
Used preoperatively

Use In GI Disorders
Helpful in treating irritable colon or colitis
Useful in gastritis, pylorospasm and ulcerative

colitis as they slow motility

Use in GU disorders
Antispasmotic effects seen in overactive

bladder and in urinary incontinence

Ophthalmology
Mydriatic and cycloplegia for examinations

and surgery

Meiosis

Mydriasis

Respiratory
In bronchospasm whether related to asthma

or COPD
Atrovent very useful for its bronchodilating
effects

Cardiology
Atropine is used to increase heart rate in

symptomatic bradycardias and higher blocks

Parkinsons Disease
Useful in those with minimal side effects
Those who cannot take Levodopa
Helpful in decreasing salivation, spasticity and

tremors

Preop
Help prevent vagal stimulation and potential

bradycardia
Reduce respiratory secretions as well

Contraindications
BPH
Myasthenia gravis
Hyperthyroidism
Glaucoma
Tachydysrhythmias
Not in situations whereby delaying of gastric

emptying is a concern

Individual Anticholinergic
Drugs
Atropineprototype. Antidote. Belladonna
alkaloid.
Ipratropium (Atrovent). Useful in
rhinorrhea. Also excellent bronchodilator.
Scopolamine, similar to atropine.
Depresses CNS and causes amnesia,
drowsiness, euphoria, relaxation and sleep.
Also good for motion sickness. Given
parenterally, orally and transdermally.

Centrally Acting
Anticholinergics

Benztropine (Cogentin)temporary use in

Parkinsons disease. Useful for dystonic
reactions caused by antipsychotics.
Trihexyphenidyl (Trihexy)also used for txing
EPS by some antipsychotics. Contraindicated
in glaucoma.

Urinary Antispasmotics
Flavoxate (Urispas)relieves dysuria, urgency,

frequency, and pain with GU infections

Oxybutynin (Ditropan) has direct
antispasmodic effects on smooth muscle and
anticholinergic effects. Decreases frequency of
voiding.
Tolterodine (Detrol) is competitive,
antimuscuranic anticholinergic that inhibits
contraction. More selective for this area than
elsewhere in the body.

Toxicity of
Anticholinergics
Anticholinergic overdose syndrome is
characterized by: Hyperthermia, delirium, dry
mouth, tacycardia, ileus, urinary retention.
Seizures, coma and respiratory arrest may
occur.
Txactivated charcoal, Antilirium, cooling
agents (ice bags, cooling blankets, tepid
baths).

Cholinergic Blocking
Agents: Chemical Class
Typical anticholinergic (cholinergic blocking) agents include :
Atropine sulfate
Benztropine mesylate
Biperiden hydrochloride
Dicyclomine hydrochloride
Ipratropium bromide
Propantheline bromide
Scopolamine hydrobromide
Scopolamine transdermal therapeutic system
Trihexyphenidyl hydrochloride

Cholinergic Blocking
Agents: Therapeutic
CNS
Uses
Decreased muscle rigidity and muscle
tremors
Parkinsons disease
Drug-induced extrapyramidal reactions

Cholinergic Blocking
Agents: Therapeutic
Cardiovascular
Uses
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

Cholinergic Blocking
Agents: Therapeutic
Atropine
Uses

Used primarily for cardiovascular disorders

Sinus node dysfunction
Symptomatic second-degree heart block
Sinus bradycardia with hemodynamic
compromise (advanced life support)

Cholinergic Blocking
Agents: Therapeutic
Respiratory
Uses
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

Cholinergic Blocking
Agents: Therapeutic Uses
:Respiratory agents are used to treat

Exercise-induced bronchospasms
Chronic bronchitis
Asthma
Chronic obstructive pulmonary disease

Cholinergic Blocking
Agents: Therapeutic
Gastrointestinal
Uses
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

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

Cholinergic Blocking
Agents: Therapeutic
Genitourinary
Usesdetrusor muscles of the bladder
Relaxed
Increased constriction of the internal
sphincter
Reflex neurogenic bladder
Incontinence

Cholinergic Blocking
Agents:
Side/Adverse Effectson Body System
Side Effects
CNS : excitation, restlessness, irritability, disorientation, hallucinations, delirium
Increased heart rate
Cardiovascular dyrrhytmias -

Cholinergic Blocking
Agents:
Side Effects
EYE :

dilated pupils, decreased eye visual and accommodation, increased

intraocular pressure
G I tract :
Decreased salivation, decreased gastric secretions dan decreased
gastrointestinal motility.

Cholinergic Blocking
Agents:
Genito-Urinary
retention
Side
Effects
Glandular : decreased sweating
Respiratory : 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
Keep in mind that these agents will block
Implications

.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

Cholinergic Blocking
Agents: Nursing
Medications should be taken exactly as prescribed
Implications
.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

Cholinergic Blocking
Agents: Nursing
When giving ophthalmic solutions, apply pressure to
Implications
.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)

Drug interactions
Amantadine / Additive anticholinergic side effects
Antacids / Lowered absorption of anticholinergics from GI tract
Antidepressants, tricyclic / Additive anticholinergic side effects
Antihistamines / Additive anticholinergic side effects
Atenolol / Anticholinergics increase effects of atenolol
Benzodiazepines / Additive anticholinergic side effects
Corticosteroids / Additive increased intraocular pressure
Cyclopropane / Increased chance of ventricular arrhythmias
Digoxin / Increases effect of digoxin due to increased absorption from GI tract
Disopyramide / Potentiation of anticholinergic side effects
Guanethidine / Reversal of inhibition of gastric acid secretion caused by
anticholinergics
Haloperidol / Additive increased intraocular pressure
Histamine / Reversal of inhibition of gastric acid secretion caused by
anticholinergics
Levodopa / Possible decreased effect of levodopa due to increased breakdown
of levodopa in stomach (due to delayed gastric emptying time)

MAO inhibitors / Increased effect of anticholinergics due to reduced

breakdown by liver
Meperidine / Additive anticholinergic side effects
Methylphenidate / Potentiation of anticholinergic side effects
Metoclopramide / Anticholinergics block action of metoclopramide
Nitrates, nitrites / Potentiation of anticholinergic side effects
Nitrofurantoin / Increased bioavailability of nitrofurantoin
Orphenadrine / Additive anticholinergic side effects
Phenothiazines / Additive anticholinergic side effects; also, effects of
phenothiazines may lower effect
Primidone / Potentiation of anticholinergic side effects
Procainamide / Additive anticholinergic side effects
Qutnidine / Additive anticholinergic side effects
Reserpine / Reversal of inhibition of gastric acid secretion caused by
anticholinergics
Sympathomimetics / Increases bronchial relaxation
Thiazide diuretics / Increased bioavailability of thiazide diuretics
Thioxanthines / Potentiation of anticholinergic side effects

Contralndicatlons:
Glaucoma, adhesions between iris and lens of the eye, tachycardia, myocardial
ischemia, unstable CV state in acute hemorrhage, partial obstruction of the GI
and biliary tracts, prostatic hypertrophy, renal disease, myasthenia gravis,
hepatic disease, paralytic ileus, pyloroduodenal stenosis, pyloric obstruction,
intestinal atony, ulcerative colitis, obstructive uropathy. Cardiac clients,
especially when there is danger of tachycardia; older persons suffering from
atherosclerosis or mental impairment. Lactation.
Special Concerns:
Use with caution in pregnancy. Infants and young children are more susceptible
to the toxic side effects of anticholinergic drugs. Use in children when the
ambient temperature is high may cause a rapid increase in body temperature
due to suppression of sweat glands. Geriatric clients are particularly likely to
manifest anticholinergic side effects and CNS effects, including agitation,
confusion, drowsiness, excitement, glaucoma, and impaired memory. Use with
caution in hyperthyroidism, CHF, cardiac arrhythmias, hypertension, Down
syndrome, asthma, spastic paralysis, blonde individuals, allergies, and chronic
lung disease.

Overdose Management:
Symptoms ("Belladonna Poisoning"): Infants and children are especially
susceptible to the toxic effects of atropine and scopolamine. Poisoning (dosedependent) is characterized by the following symptoms: dry mouth, burning
sensation of the mouth, difficulty in swallowing and speaking, blurred vision,
photophobia, rash, tachycardia, increased respiration, increased body
temperature, restlessness, irritability, confusion, muscle incoordination, dilated
pupils, hot dry skin, respiratory depression and paralysis, tremors, seizures,
hallucinations. and death.
Treatment ("Belladonna Poisoning"):
Gastric lavage or induction of vomiting followed by activated charcoal. General supportive
measures.
Anticholinergic effects can be reversed by physostigmine (Eserine), l 3 mg IV
(effectiveness uncertain; thus use other agents if possible). Neostigmine methylsulfate, 0.52 mg IV, repeated as necessary.
If there is excitation, diazepam, a short-acting barbiturate, IV sodium thiopental (2%
solution), or chloral hydrate (100-200 mL of a 2% solution by rectal infusion) may be given.
For fever, cool baths may be used. Keep client in a darkened room if photophobia is
manifested.
Artificial respiration should be instituted if there is paralysis of respiratory muscles.