Loperamide
Loperamide Uses, Dosage, Side Effects, Food Interaction and all others data.
Loperamide inhibits the peristaltic activity of longitudinal and circular smooth muscle in the intestine by interacting with cholinergic and noncholinergic neuronal mechanisms responsible for producing the peristaltic reflex.
Loperamide binds to the opiate receptor in the gut wall, reducing propulsive peristalsis, and increase intestinal transit time.Loperamide is orally administered capsule. After administration absorption is more than 65% which occurs at a modest rate, with peak serum levels of 2-3 µgm/litre occurring at about 4 hours later after oral administration. The rest 35% is excreted unchanged in the faeces. Loperamide undergoes an extensive presystemic first pass metabolism in the gut wall and in the liver. Loperamide does not act centrally due to its high affinity for the gut wall and its presystemic metabolism. This is why it reaches the systemic circulation in very minute amount. The route of elimination is 0.63-1.4% in urine as unchanged drug, 58% is excreted in the bile and 15-23% appears in the faeces.
Loperamide is a synthetic anti-diarrheal indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. Loperamide is also indicated for reducing the volume of discharge from ileostomies. In man, Loperamide prolongs the transit time of the intestinal contents. It reduces the daily fecal volume, increases the viscosity and bulk density, and diminishes the loss of fluid and electrolytes. Tolerance to the antidiarrheal effect has not been observed. Loperamide is an opioid receptor agonist and acts on the mu opioid receptors in the myenteric plexus large intestines; it does not affect the central nervous system like other opioids. It works specifically by decreasing the activity of the myenteric plexus which decreases the motility of the circular and longitudinal 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.
| Trade Name | Loperamide |
| Availability | Rx and/or OTC |
| Generic | Loperamide |
| Loperamide Other Names | Loperamid, Loperamida, Lopéramide, Loperamide, Loperamidum |
| Related Drugs | ciprofloxacin, sulfamethoxazole / trimethoprim, Bactrim, sulfasalazine, Lomotil, Imodium, neomycin, Pepto-Bismol, bismuth subsalicylate, atropine / diphenoxylate |
| Weight | 2mg, 1mg/5ml, 1mg/7.5ml, |
| Type | Oral Capsule, Oral Liquid, Oral Suspension, Oral Tablet, Chewable, Oral Solution, Tablet, Capsule |
| Formula | C29H33ClN2O2 |
| Weight | Average: 477.038 Monoisotopic: 476.223056017 |
| Protein binding | 97% |
| Groups | Approved |
| Therapeutic Class | Anti-diarrhoeal, Anti-motility drugs |
| Manufacturer | Flamingo Pharma (uk) Ltd, Ifars, Harsen, Combiphar, Holi Pharma, First Medifarma, Jay Formulations Limited |
| Available Country | United Kingdom, United States, Indonesia, India, Nigeria |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Loperamide is used for a symptomatic treatment of acute and chronic diarrhoea
Loperamide is also used to associated treatment for these conditions: Chronic Functional Diarrhea, Diarrhoea, Intestinal stoma leak, Traveler's Diarrhea
How Loperamide works
In vitro and animal studies show that Loperamide acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide inhibits peristaltic activity by a direct effect on the circular and longitudinal muscles of the intestinal wall. It is a non-selective calcium channel blocker and binds to opioid mu-receptors. Evidence also suggests that at higher concentrations it binds to calmodulin.
Dosage
Loperamide dosage
Acute diarrhoea-
The initial dose is 2 capsules for adults and 1 capsule for children older than eight; in addition 1 capsule should be taken at any subsequent loose stool. The daily dose, however should not exceed 8 capsules for adults, for children 4-6 capsules according to age.
Chronic diarrhoea-
Initial dose:
- Adults: 2 capsules daily.
- Children older than eight: 1 capsule daily.
Maintenance dose: One should aim at obtaining normal stools (e.g., one or two stools of good consistency a day). For this it may be necessary to adjust the initial dose (by increasing or decreasing it as required). Maintenance dose as a rule will vary from 1 to 6 capsules daily
Side Effects
On occasions paralytic ileus, abdominal cramps and bloating have been reported. Other side effects observed are skin reactions including urticaria, nausea, vomiting, constipation, tiredness, drowsiness, dizziness and dry mouth.
Toxicity
Oral, mouse: LD50 = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, lethargy, and nausea.
Precaution
It should be used with caution in patients with defective hepatic function as this might result in a relative overdose.
Interaction
No drugs are known to be incompatible with Loperamide
Food Interaction
- Drink plenty of fluids.
- Take with or without food.
[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.
Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.
Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Loperamide Drug Interaction
Moderate: diphenhydramine, acetaminophen / hydrocodone, ondansetron, cetirizineUnknown: aspirin, duloxetine, apixaban, omega-3 polyunsaturated fatty acids, furosemide, atorvastatin, pregabalin, metoprolol, polyethylene glycol 3350, esomeprazole, acetaminophen, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, alprazolam
Loperamide Disease Interaction
Major: infectious diarrheaModerate: fluid/electrolytes, hepatic/renal dysfunction, toxic megacolon
Elimination Route
Not significantly absorbed from the gut
Half Life
9.1 to 14.4 hours (average 10.8 hours)
Elimination Route
Excretion of the unchanged loperamide and its metabolites mainly occurs through the feces.
Pregnancy & Breastfeeding use
Safety of use of Loperamide during pregnancy has not been established, although studies in animal did not demonstrate any teratogenic effects. Therefore, it should not be administered to the patients during pregnancy. Although the fraction of loperamide secreted in the human milk is very low, caution is advised if it is to be administered to nursing mothers.
Contraindication
It should not be used in children less than 4 years of age. It must not be used when inhibition of peristalsis is to be avoided in particular when constipation are present or when abdominal distension develops particularly severely dehydrated children or in patients with acute ulcerative colitis or pseudomembranous colitis associated with broad spectrum antibiotics. It should not be used alone in acute dysentery associated with blood in stools and elevated temperature.
Acute Overdose
Symptoms: CNS depression; constipation, urinary retention and ileus may occur.
Management: Employ gastric lavage followed by admin of activated charcoal. Naloxone HCl may be given as antidote.
Storage Condition
Store between 20-25°C.
Innovators Monograph
You find simplified version here Loperamide
Loperamide contains Loperamide see full prescribing information from innovator Loperamide Monograph, Loperamide MSDS, Loperamide FDA label
FAQ
What is Loperamide used for?
Loperamide to treat diarrhoea . It can help with short-term diarrhoea or irritable bowel syndrome (IBS). Loperamide is also used for recurring or longer lasting diarrhoea from bowel conditions such as Crohn's disease, ulcerative colitis and short bowel syndrome.
How safe is Loperamide?
Loperamide is a safe drug when used as directed.Taking too much Loperamide can causes serious heart problems or death. Serious heart problems may also happen if you take loperamide with other medicines. Ask a doctor or pharmacist about safely using medications together.
How does Loperamide work?
Loperamide works on mu-opioid receptors in the gut wall to slow down the movement of the gut. This slows the contractions of the intestine, allowing more water to be absorbed back into the body through the intestinal wall, this makes the stool less watery and decreases the number of bowel movements.
What are the common side effects of Loperamide?
The common side effects of Loperamide are include:
- dizziness,
- drowsiness,
- tiredness,
- constipation,
- stomach pain,
- skin rash, or.
- itching.
Is Loperamide safe during pregnancy?
Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.Loperamide should not be used during pregnancy unless the benefit outweighs the risk to the fetus.
Is Loperamide safe during breastfeeding?
Loperamide can be taken by breastfeeding mothers as it is poorly absorbed from the gut and minimal amounts reach breastmilk.
Can I drink alcohol with Loperamide?
It's best not to drink alcohol while you're taking Loperamide. Alcohol makes you more likely to have side effects such as feeling sleepy or dizzy and having difficulty concentrating.
Can I drive after taking Loperamide?
Avoid becoming overheated or dehydrated while taking Loperamide. Do not drive or operate machinery if Loperamide makes you drowsy or dizzy.
Does loperamide make you sleepy?
Talk to your doctor about using Loperamide safely.Loperamide may make you dizzy or drowsy.
Who should not take Loperamide?
You should not use Loperamide if you have ulcerative colitis, bloody or tarry stools, diarrhea with a high fever, or diarrhea caused by antibiotic medication.
How much Loperamide take daily?
You should not take more than eight tablets (16mg) per day unless instructed otherwise by your doctor.
Does Loperamide affect the liver?
Loperamide has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury.
When is the best time to take Loperamide?
Loperamide usually is taken immediately after each loose bowel movement but not more than the 24-hour maximum amount described on the label.
How many times a day should I take Loperamide?
Loperamide usually means taking three or four tablets/capsules a day. Never take more than eight tablets/capsules a day.
Is Loperamide good for stomach cramps?
This combination Loperamide is used to treat diarrhea and symptoms of gas (e.g., cramps, bloating, pressure). Loperamide works by slowing down the movement of the gut.
Does Loperamide raise blood pressure?
Yes. There are both prescription and non-prescription strengths of Imodium. Abnormal heart rhythms, a sudden drop in heart rate and blood pressure, and heart attack can all be caused by high doses of Imodium.
Can I take Loperamide for a long time?
If you've bought Loperamide for short-term diarrhoea, do not take it for longer than 48 hours without talking to a doctor.
What happen if I overdose of Loperamide?
An overdose of loperamide can be fatal.Overdose symptoms may include fast or irregular heartbeats, or fainting. A person caring for you should seek emergency medical attention if you pass out and are hard to wake up.
What happens if you stop taking Loperamide?
If you develop a dependence, you might experience withdrawal symptoms if you suddenly stop taking the drug.
What happens if I miss a dose of Loperamide?
Since Loperamide is used when needed, it does not have a daily dosing schedule. Call your doctor if your symptoms do not improve after using Loperamide.
