Antimotility agent explained

Antimotility agents are drugs used to alleviate the symptoms of diarrhea. These include loperamide (Imodium), bismuth subsalicylate (Pepto-Bismol),[1] diphenoxylate with atropine (Lomotil), and opiates such as paregoric, tincture of opium, codeine, and morphine. In diarrhea caused by invasive pathogens such as Salmonella, Shigella, and Campylobacter, the use of such agents has generally been strongly discouraged, though evidence is lacking that they are harmful when administered in combination with antibiotics in Clostridium difficile cases.[2] Use of antimotility agents in children and the elderly has also been discouraged in treatment of EHEC (Shiga-like toxin producing Escherichia coli) due to an increased rate of hemolytic uremic syndrome.[3]

Loperamide (Imodium)

See main article: Loperamide.

Mechanism of action

Loperamide is a μ-opioid receptor agonist.[4] By binding to μ-opioid receptors, loperamide inhibits acetylcholine release and decreases excitation of neurons in the myenteric plexus, which leads to a decrease in peristalsis. Decreasing intestinal motility prolongs the transit time of food content through the digestive tract, which allows for more fluid absorption; thereby alleviating diarrhea symptoms and improving stool consistency and frequency.

Unlike other opiates, loperamide does not cross the blood brain barrier, so there is minimal risk for abuse.[5]

Adverse effects

Side effects of use of anti-motility agents include:

Contraindications

Contraindications include:

Drug interactions

CYP3A4 inhibitors, such as erythromycin, fluconazole, ketoconazole, quinidine, and ritonavir, increase plasma levels of loperamide

Bismuth subsalicylate (Pepto-Bismol)

See main article: Bismuth subsalicylate.

Mechanism of action

Bismuth subsalicylate (BSS) has both antibacterial and anti-secretory actions that help with diarrhea. Once in the gut, BSS gets broken down into bismuth and salicylic acid. Bismuth produces other bismuth salts, which blocks the binding and proliferation of bacteria in stomach mucosal cells, leading to a decrease in inflammation in the intestine.[9] Also, BSS inhibits cyclooxygenase enzyme and leads to a decrease in the production of prostaglandins, which are compounds that increase intestinal inflammation and motility. Lastly, this antidiarrheal agent enhances fluid reabsorption, which helps improve diarrhea symptoms and stool consistency.

Adverse effects

Adverse effects include:

Contraindications

Contraindications include:

Drug interactions

Drug interactions may occur with:

See also

Notes and References

  1. Book: Budisak P, Abbas M . Bismuth Subsalicylate . 2024 . StatPearls . http://www.ncbi.nlm.nih.gov/books/NBK560697/ . 2024-04-22 . Treasure Island (FL) . StatPearls Publishing . 32809532 .
  2. Koo HL, Koo DC, Musher DM, DuPont HL . Antimotility agents for the treatment of Clostridium difficile diarrhea and colitis . Clinical Infectious Diseases . 48 . 5 . 598–605 . March 2009 . 19191646 . 10.1086/596711 . free .
  3. Bae WK, Lee YK, Cho MS, Ma SK, Kim SW, Kim NH, Choi KC . A case of hemolytic uremic syndrome caused by Escherichia coli O104:H4 . Yonsei Medical Journal . 47 . 3 . 437–439 . June 2006 . 16807997 . 2688167 . 10.3349/ymj.2006.47.3.437 .
  4. Schiller LR . Antidiarrheal Drug Therapy . Current Gastroenterology Reports . 19 . 5 . 18 . May 2017 . 28397130 . 10.1007/s11894-017-0557-x .
  5. Schiller LR, Pardi DS, Sellin JH . Chronic Diarrhea: Diagnosis and Management . Clinical Gastroenterology and Hepatology . 15 . 2 . 182–193.e3 . February 2017 . 27496381 . 10.1016/j.cgh.2016.07.028 .
  6. Web site: Forrester A . August 1, 2018 . Diarrhea . April 27, 2024.
  7. Regnard C, Twycross R, Mihalyo M, Wilcock A . Loperamide . Journal of Pain and Symptom Management . 42 . 2 . 319–323 . August 2011 . 21703817 . 10.1016/j.jpainsymman.2011.06.001 . free .
  8. Leung AK, Leung AA, Wong AH, Hon KL . Travelers' Diarrhea: A Clinical Review . Recent Patents on Inflammation & Allergy Drug Discovery . 13 . 1 . 38–48 . 2019-08-05 . 31084597 . 6751351 . 10.2174/1872213X13666190514105054 .
  9. O'Malley PA . Pink Prescribing: Bismuth Subsalicylate; History, Actions, Risks, and Future Use . Clinical Nurse Specialist CNS . 34 . 2 . 45–47 . March 2020 . 32068631 . 10.1097/NUR.0000000000000509 .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Antimotility agent".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.