Imodium Dual Action Relief (GSL)

Imodium Dual Action Relief (GSL) 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 Imodium Dual Action Relief (GSL)
Generic simeticone + Loperamide
Type
Therapeutic Class
Manufacturer McNeil Products Ltd
Available Country United Kingdom
Last Updated: September 19, 2023 at 7:00 am
Imodium Dual Action Relief (GSL)
Imodium Dual Action Relief (GSL)

Uses

Loperamide is used for a symptomatic treatment of acute and chronic diarrhoea

Imodium Dual Action Relief (GSL) is also used to associated treatment for these conditions: Chronic Functional Diarrhea, Diarrhoea, Intestinal stoma leak, Traveler's Diarrhea

How Imodium Dual Action Relief (GSL) 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

Imodium Dual Action Relief (GSL) 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

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

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