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Loperamide

 
Drug Info:

Loperamide

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Brand names: Anti-Diarrheal, Diamode®, Imodium®, Imodium® A-D, Imotil®, K-Pek® II, Kao-Paverin®, Maalox® Anti-Diarrheal, Pepto-Bismol® Diarrhea Control, Valu-Rite Anti Diarrheal

Chemical formula:



Loperamide Hydrochloride Oral tablet

What is this medicine?

LOPERAMIDE (loe PER a mide) is used to treat diarrhea.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•a black or bloody stool
•bacterial food poisoning
•colitis or mucus in your stool
•currently taking an antibiotic medication for an infection
•fever
•liver disease
•severe abdominal pain, swelling or bulging
•an unusual or allergic reaction to loperamide, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take your doses at regular intervals. Do not take your medicine more often than directed.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•alosetron

This medicine may also interact with the following medications:
•quinidine
•ritonavir
•saquinavir

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Do not take this medicine for more than 1 week without asking your doctor or health care professional. If your symptoms do not start to get better after two days, you may have a problem that needs further evaluation. Check with your doctor or health care professional right away if you develop a fever, severe abdominal pain, swelling or bulging, or if you have have bloody/black diarrhea or stools.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can increase possible drowsiness and dizziness. Avoid alcoholic drinks.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe. Drinking plenty of water can also help prevent dehydration that can occur with diarrhea.

Elderly patients may have a more variable response to the effects of this medicine, and are more susceptible to the effects of dehydration.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•bloated, swollen feeling in your abdomen
•blurred vision
•loss of appetite
•stomach pain

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•constipation
•drowsiness or dizziness
•dry mouth
•nausea, vomiting

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 25 degrees C (59 and 77 degrees F). Keep container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Saunders Veterinary Dictionary:

loperamide

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Home > Library > Animal Life > Veterinary Dictionary

A butyramide derivative; the hydrochloride is used as an antiperistaltic in the treatment of diarrhea.

Wikipedia on Answers.com:

Loperamide

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Home > Library > Miscellaneous > Wikipedia
"Imodium" redirects here. For the song by Nirvana, see Breed (song).
Loperamide
Systematic (IUPAC) name
4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]- N,N-dimethyl-2,2-diphenylbutanamide
Clinical data
Trade names Imodium
AHFS/Drugs.com monograph
MedlinePlus a682280
Pregnancy cat. B[1]
Legal status  ? (CA) GSL (UK) OTC (US)
Routes oral, insufflation
Pharmacokinetic data
Bioavailability Not significantly absorbed from the gut
Protein binding 97%
Metabolism hepatic
Half-life 9.1 to 14.4 hours (average 10.8 hours)
Identifiers
CAS number 53179-11-6 YesY
34552-83-5 (with HCl)
ATC code A07DA03
A07DA05 (oxide)
PubChem CID 3955
DrugBank DB00836
ChemSpider 3818 YesY
UNII 6X9OC3H4II YesY
KEGG D08144 YesY
ChEBI CHEBI:6532 N
ChEMBL CHEMBL841 YesY
Chemical data
Formula C29H33ClN2O2 
Mol. mass 477.037 g/mol (513.506 with HCl)
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Loperamide (play /loʊˈpɛrəmaɪd/; R-18553[clarification needed]), a synthetic piperidine derivative,[2] is an opioid drug used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. In most countries it is available generically and under brand names such as Lopex, Imodium, Dimor, Fortasec, and Pepto Diarrhea Control. It was developed at Janssen Pharmaceutica.[3]

Contents

Medical uses

Loperamide is effective for the treatment of a number of types of diarrhea.[4]

Mechanism of action

Loperamide is an opioid-receptor agonist and acts on the μ-opioid receptors in the myenteric plexus of the large intestine; by itself it does not affect the central nervous system like other opioids, unless extremely high doses are taken (in which case it can produce psychoactive effects on its own[citation needed]).

It works by decreasing the activity of the myenteric plexus, which, like morphine, decreases the tone of the longitudinal smooth muscles but increases the tone of circular smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.[5]

Many physicians and pharmacists believe that loperamide does not cross the blood–brain barrier. In fact, however, loperamide does cross this barrier, although it is immediately pumped back out into non–central nervous system (CNS) circulation by P-glycoprotein. While this mechanism effectively shields the CNS from exposure (and thus risk of CNS addiction) to loperamide, many drugs are known to inhibit P-glycoprotein and may thus render the CNS vulnerable to opiate agonism by loperamide.[6]

Only when very high doses are taken does enough accumulate in the brain to produce typical opioid effects, lasting for a number of hours (just as typical opioids would).[7][8] Tolerance in response to long-term use has not been reported.

However, loperamide has been shown to cause a mild physical dependence during preclinical studies, specifically in mice, rats, and rhesus monkeys. Symptoms of mild opiate withdrawal have been observed following abrupt discontinuation of long-term therapy with loperamide.[9][10]

Contraindications

The use of loperamide (Imodium) in children under 2 years is not recommended. There have been rare reports of fatal paralytic ileus associated with abdominal distention. Most of these reports occurred in the setting of acute dysentery, overdose, and with very young children less than two years of age.[11] In 1990, all pediatric formulations of the antidiarrheal loperamide (Imodium and others) were banned in Pakistan.[12]

Treatment should be avoided in the presence of fever or if the stool is bloody (dysentery).[13] It is of no value in diarrhea caused by cholera, Shigella or Campylobacter.[13] Treatment is not recommended for patients that could suffer detrimental effects from rebound constipation. If there is a suspicion of diarrhea associated with organisms that can penetrate the intestinal walls, such as E. coli O157:H7 or salmonella, loperamide is contraindicated.

Loperamide treatment is not used in symptomatic C. difficile infections, as it increases the risk of toxin retention and precipitation of toxic megacolon.

Adverse effects

Adverse drug reactions (ADRs) associated with Loperamide include abdominal pain and bloating, nausea, vomiting and constipation. Rare side-effects associated with Loperamide are paralytic ileus, dizziness and rashes.[14]

Hepatic

It is not recommended for use in hepatic failure since it can precipitate hepatic encephalopathy.[14]

Marketing in the developing world

In Pakistan, seven infants died in 1989 and 1990 after parents treated their babies' diarrhea with Imodium, a medicine sold by a subsidiary of Johnson & Johnson.

Since 1980, the World Health Organization has warned doctors of developing countries not to use Imodium because it can paralyze a child's intestines. For months a local doctor begged the company to pull the product from stores, but it didn't do so until a British television program broadcast footage of dying babies.[15]

Crossing the blood-brain barrier

Concurrent administration of P-glycoprotein inhibitors such as quinidine and its other isomer quinine (although much higher doses must be used), PPIs like omeprazole (Prilosec OTC) and even black pepper (piperine as the active ingredient) could potentially allow loperamide to cross the blood-brain barrier. It should however be noted that only quinidine with loperamide was found to produce respiratory depression, indicative of central opioid action.[16]

See also

References

  1. ^ "Loperamide Hydrochloride." DailyMed.
  2. ^ US National Cancer Institute, Drug Dictionary
  3. ^ Stokbroekx, R. A.; Vanenberk, J.; Van Heertum, A. H. M. T.; Van Laar, G. M. L. W.; Van der Aa, M. J. M. C.; Van Bever, W. F. M.; Janssen, P. A. J. (1973). "Synthetic Antidiarrheal Agents. 2,2-Diphenyl-4-(4'-aryl-4'-hydroxypiperidino)butyramides". Journal of Medicinal Chemistry 16 (7): 782–786. doi:10.1021/jm00265a009. 
  4. ^ Hanauer, S. B. (2008 Winter). "The Role of Loperamide in Gastrointestinal Disorders". Reviews in Gastroenterological Disorders 8 (1): 15–20. PMID 18477966. 
  5. ^ Katzung, B. G. (2004). Basic and Clinical Pharmacology (9th ed.). ISBN 0-07-141092-9. [page needed]
  6. ^ Upton, R. N. (2007). "Cerebral Uptake of Drugs in Humans". Clinical and Experimental Pharmacology and Physiology 34 (8): 695–701. doi:10.1111/j.1440-1681.2007.04649.x. PMID 17600543.  edit
  7. ^ Litovitz, T.; Clancy, C.; Korberly, B.; Temple, A. R.; Mann, K. V. (1997). "Surveillance of Loperamide Ingestions: An Analysis of 216 Poison Center Reports". Journal of Toxicology. Clinical Toxicology 35 (1): 11–19. PMID 9022646. 
  8. ^ Sklerov, J.; Levine, B.; Moore, K. A.; Allan, C.; Fowler, D. (October 2005). "Tissue Distribution of Loperamide and N-desmethylloperamide Following a Fatal Overdose". Journal of Analytical Toxicology 29 (7): 750–754. PMID 16419413. 
  9. ^ Yanagita, T.; Miyasato, K.; Sato, J. (1979). "Dependence Potential of Loperamide Studied in Rhesus Monkeys". NIDA Research Monograph 27: 106–113. PMID 121326. 
  10. ^ Nakamura, H.; Ishii, K.; Yokoyama, Y. et al. (November 1982). "[Physical Dependence on Loperamide Hydrochloride in Mice and Rats]" (in Japanese). Yakugaku Zasshi 102 (11): 1074–1085. PMID 6892112. 
  11. ^ "Imodium (Loperamide Hydrochloride) Capsule". DailyMed. NIH. http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6651. 
  12. ^ "E-DRUG: Chlormezanone". Essentialdrugs.org. http://www.essentialdrugs.org/edrug/archive/199708/msg00056.php. 
  13. ^ a b Butler, T. (October 2008). "Loperamide for the Treatment of Traveler's Diarrhea: Broad or Narrow Usefulness?". Clinical Infectious Diseases 47 (8): 1015–1016. doi:10.1086/591704. PMID 18781871. 
  14. ^ a b Bichner, F., ed (2010). Australian Medicine Handbook. Adelaide: Australian Medicine Handbook Pty Ltd. 
  15. ^ Scanlan, Christopher (1991-06-09). "America's Deadly Exports -- Trade Of Toxic Products Abroad Is A Windfall For U.S. Companies". The Seattle Times. http://community.seattletimes.nwsource.com/archive/?date=19910609&slug=1288069. 
  16. ^ Sadeque, A. J.; Wandel, C.; He, H.; Shah, S.; Wood, A. J. (September 2000). "Increased Drug Delivery to the Brain by P-glycoprotein Inhibition". Clinical Pharmacology and Therapeutics 68 (3): 231–237. doi:10.1067/mcp.2000.109156. PMID 11014404. 

External links
Rehydration
Intestinal anti-infectives
Intestinal adsorbents
Antipropulsives (opioids)
Intestinal anti-inflammatory agents
Antidiarrheal micro-organisms
Other antidiarrheals

This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)

 
 

 

Copyrights:

Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Saunders Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia on Answers.com. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article Loperamide.  Read more