Lositala

Lositala 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.

Simethicone is used as an antiflatulent to relieve symptoms commonly referred to gas including upper GI bloating, pressure, fullness or stuffed feeling. The clinical use of Simeticone is based on its antifoaming properties. Its antifoaming action relieves flatulence by dispersing and preventing the formation of mucous surrounded gas pockets in the GI tract. Simeticone acts in the stomach and intestines to change the surface tension of gas bubbles, enabling them to coalesce; thus gas is freed and eliminated more easily by belching or passing flatus. Simeticone aids in the elimination of gas from the GI tract and can be used to reduce postoperative gas pains. Simeticone can also be used prior to gastroscopy to enhance visualization and prior to radiography of the intestine to reduce gas shadows.

Simethicone decreases the surface tension of gas bubbles in the gastrointestinal tract, facilitating their expulsion. It has a short duration of action as it is generally given as needed, and a wide therapeutic index as it is not systemically absorbed.

Lositala
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Lositala
Generic	loperamide + simethicone
Type
Therapeutic Class
Manufacturer
Available Country	Poland
Last Updated:	September 19, 2023 at 7:00 am

Uses

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

Flatulence, abdominal distention, fullness, gas and windy colic: Simethicone is an excellent and effective antiflatulent. It is used for relief of the painful symptoms of excess gas in the digestive tract. Such gas is frequently caused by excessive swallowing of air or by eating foods that disagree. Simethicone drop is especially used in infants, acts in the stomach and intestines. Thus Simethicone enables freeing and eliminating the gas more easily by belching or passing flatus.

Large bowel preparation: Addition of Simethicone to a polyethylene glycol bowel preparation produces symptomatic improvement prior to investigation in the management of accidental ingestion of foaming detergents.

Treatment of poisoning: Simethicone has an anecdotal use as an antifoaming agent in the management of accidental ingestion of foaming detergents.

Lositala is also used to associated treatment for these conditions: Chronic Functional Diarrhea, Diarrhoea, Intestinal stoma leak, Traveler's DiarrheaAbdominal Cramping, Abdominal Pain, Abdominal distension, Acid Reflux, Bloating, Colic, Diarrhoea, Distention, Dyspepsia, Flatulence, Gastric Ulcer, Gastritis, Heartburn, Hiatus Hernia, Hyperacidity, Pain, Pancreatic Insufficiency, Peptic Esophagitis, Peptic Ulcer, Stomach ache, Gastrointestinal cramps, Gastrointestinal cramps caused by Gas, Gastrointestinal spasms, Stomach cramps, Antacid therapy, Bowel preparation therapy

How Lositala 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.

Simethicone is a surfactant that decreases the surface tension of gas bubbles in the gastrointestinal tract, more easily allowing gas to exit the body.

Dosage

Lositala 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

Take after meals and at bedtime. Can be given with infant’s feeds. Shake the bottle well before each use.

Children less than 2 years of age: 20 mg (0.3 ml Simethicone Paediatric Drops) 4 times daily up to 240 mg/day (3.6 ml Simethicone Paediatric Drops).
Children 2-12 years of age: 40 mg (0.6 ml Simethicone Paediatric Drops) 4 times daily.
Adults: 40-125 mg or 1-3 Simethicone chewable tablets; 4 times daily, up to 500 mg/day (12 Simethicone chewable tablets).

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.

Simethicone is physiologically inert and no adverse effect has been noted after oral ingestion.

Toxicity

Oral, mouse: LD₅₀ = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, lethargy, and nausea.

Data regarding overdoses with simethicone are rare due to the fact that it is not systemically absorbed.. In the case of an overdose stop the drug and initiate symptomatic and supportive care.

Precaution

It should be used with caution in patients with defective hepatic function as this might result in a relative overdose.

Do not exceed 12 doses per day except under the advice and supervision of a physician.

Interaction

No drugs are known to be incompatible with Loperamide

There is no evidence that Simethicone modifies the effect of other drugs. The defoaming effect of Simethicone is reduced by antacids such as Aluminium Hydroxide and Magnesium Carbonate, which absorb the Silicone.

Volume of Distribution

Simethicone is not systemically absorbed and so these data are not readily available.

Elimination Route

Not significantly absorbed from the gut

Simethicone is not systemically absorbed and so these data are not readily available.

Half Life

9.1 to 14.4 hours (average 10.8 hours)

Simethicone is not systemically absorbed and so these data are not readily available.

Clearance

Simethicone is not systemically absorbed and so these data are not readily available.

Elimination Route

Excretion of the unchanged loperamide and its metabolites mainly occurs through the feces.

Simethicone is eliminated in 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.

Pregnant women: No data are available to suggest any harmful effects.

Lactating mother: Excretion of simethicone in breast milk has not been established, and would be most unlikely.

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.