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Anticholinergic Drugs
Objectives
AFTER STUDYING THIS CHAPTER, THE STUDENT WILL BE ABLE TO:
Reflect on:
Important assessments to detect anticholinergic effects.
How anticholinergic side effects can be especially significant for the elderly.
DESCRIPTION cross cell membranes readily. They are well absorbed from
the gastrointestinal (GI) tract and conjunctiva and they cross
Anticholinergic drugs, also called cholinergic blocking and the bloodbrain barrier. Tertiary amines are excreted in the
parasympatholytic agents, block the action of acetylcholine on urine. Some belladonna derivatives and synthetic anticholin-
the parasympathetic nervous system (PNS). Most anticholin- ergics are quaternary amines. These drugs carry a positive
ergic drugs interact with muscarinic cholinergic receptors in charge and are lipid insoluble. Consequently, they do not read-
the brain, secretory glands, heart, and smooth muscle and are ily cross cell membranes. They are poorly absorbed from the GI
also called antimuscarinic agents. A few anticholinergic drugs, tract and do not cross the bloodbrain barrier. Quaternary
when given at high doses, are also able to block nicotinic re- amines are excreted largely in the feces. Table 211 lists com-
ceptors in autonomic ganglia and skeletal muscles. Glycopyr- mon tertiary amine and quaternary amine anticholinergic drugs.
rolate (Robinul) is an example of such a medication. The
prototype anticholinergic drug is atropine, and this drug class
includes belladonna alkaloids, their derivatives, and many syn- Mechanism of Action and Effects
thetic substitutes.
Most anticholinergic medications are either tertiary These drugs act by occupying receptor sites at parasympa-
amines or quaternary amines in their chemical structure. Ter- thetic nerve endings, thereby leaving fewer receptor sites free
tiary amines are uncharged lipid-soluble molecules. Atropine to respond to acetylcholine (Fig. 211). Parasympathetic re-
and scopolamine are tertiary amines and therefore are able to sponse is absent or decreased, depending on the number of
308
CHAPTER 21 ANTICHOLINERGIC DRUGS 309
orders, bradycardia, and Parkinsons disease. They also are Contraindications to Use
used before surgery and bronchoscopy. Drugs at a Glance:
Selected Anticholinergic Drugs describes the therapeutic use, Contraindications to the use of anticholinergic drugs include
dosage and route of administration of selected anticholiner- any condition characterized by symptoms that would be ag-
gic medications. gravated by the drugs. Some of these are prostatic hypertrophy,
GI disorders in which anticholinergics have been used myasthenia gravis, hyperthyroidism, glaucoma, tachyarrhyth-
include peptic ulcer disease, gastritis, pylorospasm, di- mias, myocardial infarction, and heart failure unless bradycar-
verticulitis, ileitis, and ulcerative colitis. These condi- dia is present. They should not be given in hiatal hernia or other
tions are often characterized by excessive gastric acid conditions contributing to reflux esophagitis because the drugs
and abdominal pain because of increased motility and delay gastric emptying, relax the cardioesophageal sphincter,
spasm of GI smooth muscle. In peptic ulcer disease, and increase esophageal reflux.
more effective drugs have been developed, and anti-
cholinergics are rarely used. The drugs are weak inhibitors
of gastric acid secretion even in maximal doses (which INDIVIDUAL
usually produce intolerable adverse effects). Although ANTICHOLINERGIC DRUGS
they do not heal peptic ulcers, they may relieve abdom-
inal pain by relaxing GI smooth muscle. Belladonna Alkaloids and Derivatives
Anticholinergics may be helpful in treating irritable
colon or colitis, but they may be contraindicated in Atropine, the prototype of anticholinergic drugs, produces
chronic inflammatory disorders (eg, diverticulitis, ulcer- the same effects, has the same clinical indications for use, and
ative colitis) or acute intestinal infections (eg, bacterial, has the same contraindications as those described earlier. In
viral, amebic). Other drugs are used to decrease diarrhea addition, it is used as an antidote for an overdose of choliner-
and intestinal motility in these conditions. gic drugs and exposure to insecticides that have cholinergic
In genitourinary disorders, anticholinergic drugs may effects.
be given for their antispasmodic effects on smooth mus- Atropine is a naturally occurring belladonna alkaloid that
cle to relieve the symptoms of urinary incontinence and can be extracted from the belladonna plant or prepared syn-
frequency that accompany an overactive bladder. In thetically. It is usually prepared as atropine sulfate, a salt that
infections such as cystitis, urethritis, and prostatitis, the is very soluble in water. It is well absorbed from the GI tract
drugs decrease the frequency and pain of urination. The and distributed throughout the body. It crosses the bloodbrain
drugs are also given to increase bladder capacity in barrier to enter the CNS, where large doses produce stimulant
enuresis, paraplegia, or neurogenic bladder. effects and toxic doses produce depressant effects. Atropine is
In ophthalmology, anticholinergic drugs are applied also absorbed systemically when applied locally to mucous
topically for mydriatic and cycloplegic effects to aid membranes. The drug is rapidly excreted in the urine. Phar-
examination or surgery. They are also used to treat macologic effects are of short duration except for ocular
some inflammatory disorders. Anticholinergic prepa- effects, which may last for several days.
rations used in ophthalmology are discussed further in Belladonna tincture is a mixture of alkaloids in an aqueous-
Chapter 65. alcohol solution. It is most often used in GI disorders for anti-
In respiratory disorders characterized by bronchocon- spasmodic effect. It is an ingredient in several drug mixtures.
striction (ie, asthma, chronic bronchitis), ipratropium Homatropine hydrobromide (Homapin) is a semisyn-
(Atrovent) may be given by inhalation for bronchodi- thetic derivative of atropine used as eye drops to produce my-
lating effects (see Chap. 47). driasis and cycloplegia. Homatropine may be preferable to
In cardiology, atropine may be given to increase heart atropine because ocular effects do not last as long.
rate in bradycardia and heart block characterized by Hyoscyamine (Anaspaz) is a belladonna alkaloid used
hypotension and shock. in GI and genitourinary disorders characterized by spasm,
In Parkinsons disease, anticholinergic drugs are given increased secretion, and increased motility. It has the same
for their central effects in decreasing salivation, spas- effects as other atropine-like drugs.
ticity, and tremors. They are used mainly in clients who Ipratropium (Atrovent) is an anticholinergic drug chemi-
have minimal symptoms, who do not respond to lev- cally related to atropine. When given as a nasal spray, it is use-
odopa, or who cannot tolerate levodopa because of ad- ful in treating rhinorrhea due to allergy or the common cold.
verse reactions or contraindications. An additional use When given as an inhalation treatment or aerosol to patients
of anticholinergic drugs is to relieve Parkinson-like with chronic obstructive pulmonary disease (COPD), it is ben-
symptoms that occur with older antipsychotic drugs. eficial as a bronchodilator. An advantage of administration of
Before surgery, anticholinergics are given to prevent anticholinergic drugs by the respiratory route over systemic ad-
vagal stimulation and potential bradycardia, hypoten- ministration is less thickening of respiratory secretions and re-
sion, and cardiac arrest. They are also given to reduce duced incidence of mucus-plugged airways.
respiratory tract secretions, especially in head and neck Scopolamine is similar to atropine in uses, adverse
surgery and bronchoscopy. effects, and peripheral effects but different in central effects.
CHAPTER 21 ANTICHOLINERGIC DRUGS 311
(continued )
312 SECTION 3 DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM
Centrally Acting Anticholinergics Oxybutynin (Ditropan and Ditropan XL) has direct anti-
spasmodic effects on smooth muscle and anticholinergic ef-
Used in Parkinsons Disease
fects. It increases bladder capacity and decreases frequency
of voiding in clients with neurogenic bladder. Oxybutynin is
Older anticholinergic drugs such as atropine are rarely used to
treat Parkinsons disease because of their undesirable periph- now available in an extended-release form for once a day
eral effects (eg, dry mouth, blurred vision, photophobia, con- dosing.
stipation, urinary retention, and tachycardia). Newer, centrally Tolterodine (Detrol and Detrol LA) is a competitive anti-
acting synthetic anticholinergic drugs are more selective for muscarinic, anticholinergic agent that inhibits bladder con-
muscarinic receptors in the CNS and are designed to produce traction, decreases detrusor muscle pressure, and delays the
fewer side effects. urge to void. It is used to treat urinary frequency, urgency, and
Trihexyphenidyl (Trihexy) is used in the treatment of urge incontinence. Tolterodine is more selective for muscarinic
parkinsonism and extrapyramidal reactions caused by some receptors in the urinary bladder than other areas of the body,
antipsychotic drugs. Trihexyphenidyl relieves smooth mus- such as the salivary glands, and therefore anticholinergic side
cle spasm by a direct action on the muscle and by inhibiting effects are less marked. Reduced doses (of 1 mg) are recom-
the PNS. The drug supposedly has fewer side effects than at- mended for those with hepatic dysfunction. Tolterodine is also
ropine, but approximately half the recipients report mouth available in an extended-release form.
dryness, blurring of vision, and other side effects common to
anticholinergic drugs. Trihexyphenidyl requires the same
precautions as other anticholinergic drugs and is contraindi-
cated in glaucoma. Biperiden (Akineton) and procyclidine Nursing Process
(Kemadrin) are chemical derivatives of trihexyphenidyl and
have similar actions. Assessment
Benztropine (Cogentin) is a synthetic drug with both an-
Assess the clients condition in relation to disorders for
ticholinergic and antihistaminic effects. Its anticholinergic
which anticholinergic drugs are used (ie, check for brady-
activity approximates that of atropine. A major clinical use is
cardia or heart block, diarrhea, dysuria, abdominal pain,
to treat acute dystonic reactions caused by antipsychotic
and other disorders). If the client reports or medical records
drugs and to prevent their recurrence in clients receiving
indicate a specific disorder, assess for signs and symptoms
long-term antipsychotic drug therapy. It also may be given in
of that disorder (eg, Parkinsons disease).
small doses to supplement other antiparkinson drugs. In full
dosage, adverse reactions are common.
Assess for disorders in which anticholinergic drugs are
contraindicated (eg, glaucoma, prostatic hypertrophy, re-
flux esophagitis, myasthenia gravis, hyperthyroidism).
Urinary Antispasmodics Assess use of other drugs with anticholinergic effects,
such as antihistamines (histamine-1 receptor antagonists
Flavoxate (Urispas) was developed specifically to counter- [see Chap. 48]), antipsychotic agents, and tricyclic anti-
act spasm in smooth muscle tissue of the urinary tract. It has depressants.
anticholinergic, local anesthetic, and analgesic effects. Thus,
the drug relieves dysuria, urgency, frequency, and pain with Nursing Diagnoses
genitourinary infections, such as cystitis and prostatitis. Impaired Urinary Elimination: Decreased bladder tone
and urine retention
Constipation related to slowed GI function
Disturbed Thought Processes: Confusion, disorientation,
Nursing Notes: Apply Your Knowledge especially in older adults
Deficient Knowledge: Drug effects and accurate usage
Scott Andrews is scheduled for a bronchoscopy. Before this Risk for Injury related to drug-induced blurred vision and
procedure, you have been ordered to give him Valium and at- photophobia
ropine. Explain the rationale of giving an anticholinergic agent Risk for Noncompliance related to adverse drug effects
as a preoperative medication. Risk for Altered Body Temperature: Hyperthermia
314 SECTION 3 DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM
Gastrointestinal Disorders
Planning/Goals
The client will: When anticholinergic drugs are given for GI disorders, larger
doses may be given at bedtime to prevent pain and awaken-
Receive or self-administer the drugs correctly
ing during sleep.
Experience relief of symptoms for which anticholinergic
drugs are given
Be assisted to avoid or cope with adverse drug effects on Parkinsonism
vision, thought processes, bowel and bladder elimination,
and heat dissipation When these drugs are used in parkinsonism, small doses are
given initially and gradually increased. This regimen decreases
Interventions adverse reactions.
Use measures to decrease the need for anticholinergic drugs.
For example, with peptic ulcer disease, teach the client to
Extrapyramidal Reactions
avoid factors known to increase gastric secretion and GI
motility (alcohol; cigarette smoking; caffeine-containing When used in drug-induced extrapyramidal reactions
beverages, such as coffee, tea, and cola drinks; ulcerogenic (parkinson-like symptoms), these drugs should be prescribed
drugs, such as aspirin). Late evening snacks also should be only if symptoms occur. They should not be used routinely to
avoided because increased gastric acid secretion occurs ap- prevent extrapyramidal reactions because fewer than half the
proximately 90 minutes after eating and may cause pain and clients taking antipsychotic drugs experience such reactions.
awakening from sleep. Although milk was once considered Most drug-induced reactions last approximately 3 months and
an ulcer food, it contains protein and calcium, which pro- do not recur if anticholinergic drugs are discontinued at that
mote acid secretion, and is a poor buffer of gastric acid. Thus, time. (An exception is tardive dyskinesia, which does not re-
drinking large amounts of milk should be avoided. spond to anticholinergic drugs and may be aggravated by them.)
Evaluation
Interview and observe in relation to safe, accurate drug Muscarinic Agonist Poisoning
administration. Atropine is the antidote for poisoning by muscarinic ago-
Interview and observe for relief of symptoms for which nists such as certain species of mushrooms, cholinergic ag-
the drugs are given. onist drugs, cholinesterase inhibitor drugs, and insecticides
Interview and observe for adverse drug effects. containing organophosphates. Symptoms of muscarinic poi-
soning include salivation, lacrimation, visual disturbances,
bronchospasm, diarrhea, bradycardia, and hypotension.
Atropine blocks the poison from interacting with the mus-
PRINCIPLES OF THERAPY carinic receptor, thus reversing the toxic effects.
Physostigmine salicylate (Antilirium), an acetylcholineste- spasmodics, flavoxate is not recommended for children
rase inhibitor, is a specific antidote. It is usually given intra- younger than 12 years, oxybutynin is not recommended for
venously (IV) at a slow rate of injection. Adult dosage is 2 mg children younger than 5 years of age, and the safety and effi-
(no more than 1 mg/minute); child dosage is 0.5 to 1 mg cacy of tolterodine are not established in children.
(no more than 0.5 mg/minute). Rapid administration may The drugs cause the same adverse effects in children as in
cause bradycardia, hypersalivation (with subsequent respira- adults. However, they may be more severe because children
tory distress), and seizures. Repeated doses may be given if are especially sensitive to the drugs. Facial flushing is com-
life-threatening dysrhythmias, convulsions, or coma occur. mon in children, and a skin rash may occur.
Diazepam (Valium) or a similar drug may be given for ex- Ophthalmic anticholinergic drugs are used for cycloplegia
cessive CNS stimulation (delirium, excitement). Ice bags, and mydriasis before eye examinations and surgical proce-
cooling blankets, and tepid sponge baths may help reduce dures (see Chap. 65). They should be used only with close
fever. Artificial ventilation and cardiopulmonary resuscita- medical supervision. Cyclopentolate (Cyclogyl) and tropi-
tive measures are used if excessive depression of the CNS camide (Mydriacyl) have been associated with behavioral dis-
causes coma and respiratory failure. Infants, children, and the turbances and psychotic reactions in children. Tropicamide
elderly are especially susceptible to the toxic effects of anti- also has been associated with cardiopulmonary collapse.
cholinergic agents.
Older adults are especially likely to have significant ad- such a medication. In the presence of liver impairment,
verse reactions because of slowed drug metabolism and the dosages should be reduced and given less frequently.
frequent presence of several disease processes. Some com-
mon adverse effects and suggestions for reducing their im-
pact are: Use in Critical Illness
Blurred vision. The client may need help with ambula-
tion, especially with stairs or other potentially haz- Atropine is an important drug in the emergency drug box. Ac-
ardous environments. Remove obstacles and hazards cording to ACLS guidelines, atropine is the first drug to be ad-
when possible. ministered in the emergency treatment of bradyarrhythmias.
Confusion. Provide whatever assistance is needed to Atropine 0.5 to 1 mg should be administered IV every 5 min-
prevent falls and other injuries. utes and may be repeated up to 2 to 3 mg (0.03 to 0.04 mg/kg
Heat stroke. Help to avoid precipitating factors, such as total dose). For clients with asystole, 1 mg of atropine is ad-
strenuous activity and high environmental temperatures. ministered IV and repeated every 3 to 5 minutes if asystole
Constipation. Encourage or assist with an adequate in- persists, up to 0.04 mg/kg. Administration of atropine in doses
take of high-fiber foods and fluids and adequate exercise less than 0.5 mg should be avoided because this may result in
when feasible. a paradoxical bradycardia. Atropine may be administered by
Urinary retention. Encourage adequate fluid intake endotracheal tube in clients without an intravenous access.
and avoid high doses of the drugs. Men should be ex- The recommended dose is 2 to 3 mg diluted in 10 mL normal
amined for prostatic hypertrophy. saline.
Hallucinations and other psychotic symptoms.
These are most likely to occur with the centrally active
anticholinergics given for Parkinsons disease or drug- Abuse of Anticholinergic Agents
induced extrapyramidal effects, such as trihexyphenidyl
or benztropine. Dosage of these drugs should be carefully Anticholinergic drugs have potential intoxicating effects.
regulated and supervised. Abuse of these drugs may produce euphoria, disorientation,
hallucinations, and paranoia in addition to the classic anti-
cholinergic adverse reactions.
Use in Renal Impairment
NURSING
ACTIONS Anticholinergic Drugs
1. Administer accurately
a. For gastrointestinal disorders, give most oral anticholiner- To allow the drugs to reach peak antisecretory effects by the time
gic drugs approximately 30 min before meals and at bedtime. ingested food is stimulating gastric acid secretion. Bedtime ad-
ministration helps prevent awakening with abdominal pain.
b. When given before surgery, parenteral preparations of at- The primary reason for mixing medications in the same syringe is
ropine can be mixed in the same syringe with several other to decrease the number of injections and thus decrease client dis-
common preoperative medications, such as meperidine (De- comfort. Note, however, that extra caution is required when mixing
merol), morphine, oxymorphone (Numorphan), and promet- drugs to be sure that the dosage of each drug is accurate. Also, if any
hazine (Phenergan). question exists regarding compatibility with another drug, it is safer
not to mix the drugs, even if two or three injections are required.
c. When applying topical atropine solutions or ointment to the Atropine ophthalmic preparations are available in several concen-
eye, be sure to use the correct concentration and blot any ex- trations (usually 1%, 2%, and 3%). Excess medication should be
cess from the inner canthus. removed so the drug will not enter the nasolacrimal (tear) ducts
and be absorbed systemically through the mucous membrane of
the nasopharynx or be carried to the throat and swallowed.
d. If propantheline is to be given intravenously, dissolve the Parenteral administration is reserved for clients who cannot take
30-mg dose of powder in no less than 10 mL of sterile water the drug orally.
for injection.
e. Instruct clients to swallow oral propantheline tablets, not to The tablets have a hard sugar coating to mask the bitter taste of
chew them. the drug.
f. Parenteral glycopyrrolate can be given through the tubing
of a running intravenous infusion of physiologic saline or lac-
tated Ringers solution.
g. Do not crush extended-release forms of anticholinergic drugs Crushing long-acting medications may result in high blood levels
such as Detrol LA and Ditropan XL. of the medication and increased adverse effects.
2. Observe for therapeutic effects Therapeutic effects depend primarily on the reason for use. Thus,
a therapeutic effect in one condition may be a side effect or an ad-
verse reaction in another condition.
a. When a drug is given for peptic ulcer disease or other gastro- Relief of abdominal pain is due to the smooth muscle relaxant or
intestinal disorders, observe for decreased abdominal pain. antispasmodic effect of the drug.
b. When the drug is given for diagnosing or treating eye dis- Note that these ocular effects are side effects when the drugs are
orders, observe for pupil dilation (mydriasis) and blurring of given for problems not related to the eyes.
vision (cycloplegia).
c. When the drug is given for symptomatic bradycardia, observe These drugs increase heart rate by blocking action of the vagus
for increased pulse rate. nerve.
d. When the drug is given for urinary tract disorders, such Anticholinergic drugs decrease muscle tone and spasm in the
as cystitis or enuresis, observe for decreased frequency of uri- smooth muscle of the ureters and urinary bladder.
nation. When the drug is given for renal colic due to stones,
observe for decreased pain.
e. When the centrally acting anticholinergics are given for Decreased salivation is a therapeutic effect with parkinsonism but
Parkinsons disease, observe for decrease in tremor, salivation, an adverse reaction in most other conditions.
and drooling.
(continued )
318 SECTION 3 DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM
3. Observe for adverse effects These depend on reasons for use and are dose related.
a. Tachycardia Tachycardia may occur with usual therapeutic doses because anti-
cholinergic drugs block vagal action, which normally slows heart
rate. Tachycardia is not likely to be serious except in clients with
underlying heart disease. For example, in clients with angina pec-
toris, prolonged or severe tachycardia may increase myocardial
ischemia to the point of causing an acute attack of angina (chest pain)
or even myocardial infarction. In clients with congestive heart fail-
ure, severe or prolonged tachycardia can increase the workload of the
heart to the point of causing acute heart failure or pulmonary edema.
b. Excessive central nervous system (CNS) stimulation (tremor, These effects are more likely to occur with large doses of atropine
restlessness, confusion, hallucinations, delirium) followed by because atropine crosses the blood-brain barrier. Large doses of
excessive CNS depression (coma, respiratory depression) trihexyphenidyl (Trihexy) also may cause CNS stimulation.
c. Sedation and amnesia with scopolamine or benztropine This may be a therapeutic effect but becomes an adverse reaction if
(Cogentin) severe or if the drug is given for another purpose. Benztropine has
anticholinergic and antihistaminic properties. Apparently, drowsi-
ness and sedation are caused by the antihistaminic component.
d. Constipation or paralytic ileus These effects are the result of decreased gastrointestinal motility
and muscle tone. Constipation is more likely with large doses or
parenteral administration. Paralytic ileus is not likely unless the
drugs are given to clients who already have decreased gastro-
intestinal motility.
e. Decreased oral and respiratory tract secretions, which cause Mouth dryness is more annoying than serious in most cases and is
mouth dryness and thick respiratory secretions caused by decreased salivation. However, clients with chronic
lung disease, who usually have excessive secretions, tend to retain
them with the consequence of frequent respiratory tract infections.
f. Urinary retention This reaction is caused by loss of bladder tone and is most likely
to occur in elderly men with enlarged prostate glands. Thus, the
drugs are usually contraindicated with prostatic hypertrophy.
g. Hot, dry skin; fever; heat stroke These effects are due to decreased sweating and impairment of the
normal heat loss mechanism. Fever may occur with any age group.
Heat stroke is more likely to occur with cardiovascular disease,
strenuous physical activity, and high environmental temperatures,
especially in elderly people.
h. Ocular effects-mydriasis, blurred vision, photophobia These are adverse effects when anticholinergic drugs are given for
conditions not related to the eyes.
4. Observe for drug interactions
a. Drugs that increase effects of anticholinergic drugs: Anti- These drugs have anticholinergic properties and produce additive
histamines, disopyramide, phenothiazines, thioxanthene agents, anticholinergic effects.
tricyclic antidepressants and amantadine
b. Drugs that decrease effects of anticholinergic drugs: Cholin- These drugs counteract the inhibition of gastrointestinal motility
ergic drugs and tone induced by atropine. They are sometimes used in atropine
overdose.
CHAPTER 21 ANTICHOLINERGIC DRUGS 319