What are anticholinergic and antispasmodic drugs? How do they work (mechanism of action)?
Anticholinergic and antispasmodic drugs include a broad class of medications that are used to treat various medical conditions that involve the contraction and relaxation of muscles. Examples of these conditions include overactive bladder, muscle spasms, breathing problems, diarrhea, gastrointestinal cramps, movement disorders, and others. Anticholinergics work by blocking the action of acetylcholine in the brain and at nerves. Neurotransmitters are chemicals made and released by nerves that travel to nearby nerves or, in the case of acetylcholine, nearby muscles and glands where they attach to receptors on the surface of the nerve, muscle, or glandular cells. The attachment of the neurotransmitter can stimulate or inhibit the activity of the receptor-containing cells. Anticholinergic drugs affect the function of many organs by preventing acetylcholine from binding to its receptors.
Anticholinergic drugs decrease the activity of muscles in the gut and reduce the production of sweat, saliva, digestive juices, urine, and tears. Additionally, anticholinergic drugs help to balance the production of dopamine, another neurotransmitter that plays an important role in maintaining mood, movement, memory, attention, problem-solving, motivation, and pleasure.
In addition to drugs that are primarily anticholinergic, there are drugs used for purposes other than nerve, muscle, or glandular problems which have some anticholinergic effects that are considered side effects, for example, antipsychotic and antidepressant drugs
What are anticholinergic and antispasmodic drugs used for?
- Overactive bladder
- Movement problems in Parkinson's disease
- Diarrhea
- Motion sickness
- Nausea and/or vomiting
- Muscle spasms
- Chronic obstructive pulmonary disease (COPD)
- Asthma
What are examples of prescription anticholinergic and antispasmodic agents available in the US?
A variety of medications with anticholinergic properties are available for the treatment of various medical conditions.

SLIDESHOW
Super Tips to Boost Digestive Health: Bloating, Constipation, and More See SlideshowDrugs that have anticholinergic activity
- Parkinson's medications
- diphenhydramine (Benadryl)
- trihexyphenidyl (Artane -- discontinued brand)
- benztropine mesylate (Cogentin)
- biperiden (Akineton) (This drug is no longer available in the U.S.)
- antipsychotics
- clomipramine (Anafranil)
- chlorpromazine (Thorazine -- discontinued brand)
- clozapine (Clozaril, Fazaclo ODT, Versacloz)
- fluphenazine (Prolixin -- discontinued brand)
- loxapine (Adasuve; Loxitane -- discontinued brand)
- olanzapine (Zyprexa, Symbyax)
- perphenazine (Trilafon -- discontinued brand)
- pimozide (Orap)
- quetiapine (Seroquel)
- thioridazine (Mellaril -- discontinued brand)
- thiothixene (Navane -- discontinued brand)
- trifluoperazine (Stelazine -- discontinued brand)
Overactive bladder (OAB) medications
- oxybutynin (Ditropan XL; Ditropan -- discontinued brand)
- darifenacin (Enablex)
- solifenacin (Vesicare)
- fesoterodine (Toviaz)
- tolterodine (Detrol)
- trospium (Sanctura)
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Antispasmodic medications
- belladonna
- chloridiazepoxide (Librium)
- dicyclomine (Bentyl)
- hyoscyamine (Levsin) (This drug is no longer available in the U.S.)

QUESTION
Pancreatitis is inflammation of an organ in the abdomen called the pancreas. See AnswerAntidepressant medications
- amitriptyline (Elavil, Endep)
- amoxapine (Asendin)
- clomipramine (Anafranil)
- desipramine (Norpramin)
- doxepin (Silenor)
- imipramine (Tofranil)
- nortriptyline (Pamelor)
- protriptyline (Vivactil)
- trimipramine (Surmontil)
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Muscle relaxants
- cyclobenzaprine (Amrix; Flexeril-Discontinued brand)
- dantrolene (Dantrium, Revonto, Ryanodex)
- carisoprodol (Soma)
- methocarbamol (Robaxin)
- orphenadrine (Norflex-Discontinued brand)
- tizanidine (Zanaflex)
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Gastrointestinal medications
- atropine
- belladonna
- dicyclomine (Bentyl)
- hyoscyamine (Levsin) (This drug is no longer available in the US)
- loperamide (Imodium)
- promethazine (Phenergan)
Respiratory medications
What are the side effects of anticholinergic and antispasmodic drugs?
- Blurred vision
- Dry mouth
- Dry eyes
- Decreased urine production
- Decreased sweat production
- Constipation
- Memory impairment
- Delirium
- Confusion
When possible, the use of anticholinergics should be avoided in the elderly because anticholinergic side effects are particularly common and problematic in older individuals.
Who should not use anticholinergic and antispasmodic medications?
Patients with the following medical conditions should not use medications with anticholinergic properties since the use of anticholinergic medications can worsen their conditions:
- Benign prostate hyperplasia (enlarged prostate)
- Glaucoma
- Urinary bladder neck obstruction
- Myasthenia gravis
- Alzheimer's disease
What drugs interact with anticholinergic and antispasmodic drugs?
The use of multiple drugs with anticholinergic properties may be problematic because of their cumulative anticholinergic side effects. Examples of medications with anticholinergic properties that should not be combined include:
- Antipsychotics
- Certain antidepressants
- Histamine 1-receptor blockers (H1RA)
- Antispasmodics
- Anti-diarrheal medications
- Parkinson's medications
- Overactive bladder (OAB) medications
- Motion sickness medications
- Certain antiemetics
Patients are advised to consult with their doctor or pharmacist for more information regarding potential drug interactions.
What about taking anticholinergics and antispasmodic during pregnancy or while breastfeeding?
Pregnancy
Most of the available anticholinergic medications have not been adequately studied in pregnant women. Patients who are pregnant or plan on becoming pregnant should consult with their doctor before starting a regimen that contains anticholinergic medications.
Breastfeeding
Many drugs can enter human milk and cause unwanted side effects in the nursing baby. Therefore, all medications should be used cautiously in nursing mothers. The prescribing information for each drug should be consulted for recommendations about use while breastfeeding.
Summary
Anticholinergic or antispasmodic drugs include prescription medications used to treat a variety of medical conditions. Review anticholinergic drug side effects, drug interactions, storage, dosing, and pregnancy and safety information prior to taking this medication.
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Related Disease Conditions
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Muscle Spasms
Muscle spasms are involuntary muscle contractions that come on suddenly and are usually quite painful. Dehydration, doing strenuous exercise in a hot environment, prolonged muscle use, and certain diseases of the nervous system may cause muscle spasms. Symptoms and signs of a muscle spasm include an acute onset of pain and a possible bulge seen or felt beneath the skin where the muscle is located. Gently stretching the muscle usually resolves a muscle spasm.
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Peptic Ulcer (Stomach Ulcer)
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Parkinson's Disease
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Nausea and Vomiting
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COPD (Chronic Obstructive Pulmonary Disease)
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Asthma
Asthma is a condition in which hyperreactive airways constrict and result in symptoms like wheezing, coughing, and shortness of breath. Causes of asthma include genetics, environmental factors, personal history of allergies, and other factors. Asthma is diagnosed by a physician based on a patient's family history and results from lung function tests and other exams. Inhaled corticosteroids (ICS) and long-acting bronchodilators (LABAs) are used in the treatment of asthma. Generally, the prognosis for a patient with asthma is good. Exposure to allergens found on farms may protect against asthma symptoms.
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Motion Sickness
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Treatment & Diagnosis
Medications & Supplements
- Antidepressants (Depression Medications)
- scopolamine - transdermal, Transderm-Scop
- olanzapine - oral, Zyprexa
- diphenhydramine
- loperamide
- ipratropium bromide inhaler (Atrovent)
- quetiapine (Seroquel)
- methocarbamol (Robaxin)
- meclizine, Antivert, Bonine, Meni-D, Antrizine
- cyclobenzaprine (Flexeril, Amrix, Fexmid)
- Side Effects of Flexeril (cyclobenzaprine)
- promethazine, Phenergan, Phenadoz, Promethegan
- tizanidine
- dicyclomine, Bentyl
- amitriptyline (Elavil, Endep)
- promethazine and codeine, Phenergan with Codeine
- benztropine (Cogentin)
- olanzapine (Zyprexa, Zydis)
- chlorpromazine - oral, Thorazine
- atropine eye drops
- nortriptyline (Pamelor)
- orphenadrine (Norflex)
- oxybutynin (Ditropan, Oxytrol, Anturol, Gelnique)
- chlorpromazine-injection, Thorazine
- atropine (Atreza)
- clomipramine (Anafranil)
- carisoprodol (Soma)
- clozapine (Clozaril, Fazacio ODT, Versacloz)
- desipramine (Norpramin)
- imipramine (Tofranil)
- doxepin (Sinequan and Adapin are discontinued brand in the US; Silenor)
- scopolamine, Transderm-Scop
- tolterodine (Detrol)
- dantrolene - oral, Dantrium
- hyoscine (scopolamine)-injectable
- fluphenazine (Permitil, Prolixin)
- trospium - oral, Sanctura
- loxapine - oral, Loxitane
- fluphenazine liquid - oral, Prolixin
- pimozide - oral, Orap
- thioridazine (Mellaril [discontinued])
- trimipramine (Surmontil)
- hyoscyamine - disintegrating oral tablet, Nulev
- fluphenazine concentrate - oral, Prolixin
- thiothixene - oral, Navane
- ipratropium solution - inhalation, Atrovent
Prevention & Wellness
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Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
Drugs with Anticholinergic Activity. Prescriber's Letter 2011; 18 (12):271233.