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Loperamide

 
Drug Info: Loperamide

Brand names: Anti-DiarrhealDiamode®Imodium®Imodium® A-DImotil®K-Pek® IIKao-Paverin®Maalox® Anti-DiarrhealPepto-Bismol® Diarrhea ControlValu-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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Veterinary Dictionary: loperamide
Top

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

Wikipedia: Loperamide
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Loperamide
Systematic (IUPAC) name
4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]- N,N-dimethyl-2,2-diphenylbutanamide
Identifiers
CAS number 53179-11-6 34552-83-5 (with HCl)
ATC code A07DA03 A07DA05
PubChem 3955
DrugBank APRD00275
ChemSpider 3818
Chemical data
Formula C29H33ClN2O2 
Mol. mass 477.037 g/mol (513.506 with HCl)
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)
Excretion  ?
Therapeutic considerations
Pregnancy cat.

B[1] [2]

Legal status

?(CA) GSL(UK) OTC(US)

Routes oral, insufflation
 Yes check.svgY(what is this?)  (verify)

Loperamide, a synthetic piperidine derivative,[3] is a drug effective 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 and Pepto Diarrhea Control. It was discovered at Janssen Pharmaceutica.

Contents

Mode of action

Loperamide is an opioid-receptor agonist and acts on the μ-opioid receptors in the myenteric plexus large intestines; by itself it does not affect the central nervous system like other opioids.

It works by decreasing the activity of the myenteric plexus, which, like morphine, decreases the tone of the longitudinal smooth muscles but increases tone of circular smooth muscles (anal sphincter) 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.[4]

Loperamide molecules do not cross the blood-brain barrier in significant amounts, and, thus, it has no analgesic or euphoric properties. Any that do cross the blood-brain barrier are quickly exported from the brain by P-glycoprotein (Pgp), also known as multidrug resistance protein (MDR1). Tolerance in response to long-term use has not been reported.

However, loperamide can cause a mild physical dependence. Symptoms of mild opiate withdrawal have been observed in patients abruptly discontinuing long-term therapy with loperamide. For this reason, the drug was briefly classified as a Schedule V controlled substance upon its introduction.[citation needed]

Contraindications

Treatment should be avoided in the presence of fever or if the stool is bloody (dysentery).[5] It is of no value in diarrhoea caused by cholera, Shigella or Campylobacter.[5] 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.

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), P.P.I.'s like Omeprazole(Prilosec OTC), Venlafaxine(Effexor) & even black pepper(Piperine as the active ingredient) but only Quinidine with Loperamide was verified to have been found to produce respiratory depression, indicative of central opioid action. [6]

See also

References

  1. ^ loperamide medical facts from Drugs.com
  2. ^ SafeFetus.com
  3. ^ US National Cancer Institute, Drug Dictionary
  4. ^ Katzung, Bertram G. Basic and Clinical Pharmacology, 9th ed. (2004). ISBN 0-07-141092-9
  5. ^ a b Butler T (2008). "Loperamide for the treatment of traveler’s diarrhea: Broad or narrow usefulness?". Clin Infect Dis 47 (8): 1015–1016. doi:10.1086/591704. 
  6. ^ http://www.nature.com/clpt/journal/v68/n3/abs/clpt2000101a.html

External links


 
 

 

Copyrights:

Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
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. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Loperamide" Read more