Anticholinergic and Antispasmodic Drugs

  • Pharmacy Author:
    Omudhome Ogbru, PharmD

    Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

  • Medical and Pharmacy Editor: Jay W. Marks, MD
    Jay W. Marks, MD

    Jay W. Marks, MD

    Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.

woman with abdominal pain

What are anticholinergic drugs?

Anticholinergic and antispasmodic drugs include a broad class of medications that are used to treat various medical conditions that involve contraction and relaxation of muscles. Examples of these conditions includeoveractive 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 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 diseases and conditions do anticholinergic and antispasmodic drugs treat?

Quick GuideDigestive Disorders: Common Misconceptions

Digestive Disorders: Common Misconceptions

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.

Anticholinergic activity drugs

  • Parkinson's medications
  • diphenhydramine (Benadryl)
  • trihexyphenidyl (Artane)
  • benztropine mesylate (Cogentin)
  • biperiden (Akineton) (This drug is no longer available in the US)
  • 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)

Antispasmodic medications

  • belladonna
  • chloridiazepoxide (Librium)
  • dicyclomine (Bentyl)
  • hyoscyamine (Levsin) (This drug is no longer available in the US)

Anticholinergic activity drugs

Antispasmodic medications

Overactive bladder (OAB) medications

Quick GuideDigestive Disorders: Common Misconceptions

Digestive Disorders: Common Misconceptions

Antidepressant medications

Motion sickness medications

  • meclizine (Antivert-Discontinued brand
  • scopolamine (Transderm Scope)

Gastrointestinal medications

  • atropine
  • belladonna
  • dicyclomine (Bentyl)
  • hyoscyamine (Levsin) (This drug is no longer available in the US)
  • loperamide (Imodium)
  • promethazine (Phenergan)

Quick GuideDigestive Disorders: Common Misconceptions

Digestive Disorders: Common Misconceptions

Respiratory medications

  • ipratropium (Atrovent, Combivent, Duoneb)
  • tiotropium (Spiriva)
  • aclidinium (Tudorza Pressair)
  • umeclidinium and vilanterol (Anoro Ellipta)

What are the side effects of anticholinergic and antispasmodic drugs?

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 use of anticholinergic medications can worsen their conditions:

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.

REFERENCES:

Clinical Pharmacology [database online]. Tampa, FL: Gold Standard, Inc.; 2009.

Drugs with Anticholinergic Activity. Prescriber's Letter 2011; 18 (12):271233.

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Reviewed on 8/30/2017
References
REFERENCES:

Clinical Pharmacology [database online]. Tampa, FL: Gold Standard, Inc.; 2009.

Drugs with Anticholinergic Activity. Prescriber's Letter 2011; 18 (12):271233.

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