Peptolite
Peptolite Uses, Dosage, Side Effects, Food Interaction and all others data.
Antacid action: Peptocid coats ulcer surface, protecting it from acid and pepsin. It stimulates mucus and bicarbonate secretion and also reacts with HCl, producing bismuth oxychloride and salicylic acid. Thus it reduces HCl.
Anti-diarrheal action: Peptolite stimulates absorption of water and electrolytes across the intestinal wall. In infectious diarrhea it binds with toxin produced by E.coli and disrupts cell, causing lysis of H.pylori and prevents adhesion of H.pylori in the cell wall of intestine.
Anti-inflammatory action: Salicylic acid from hydrolyzed Peptolite inhibits prostaglandin G/H synthase. Thus reduces inflammation and coats irritated tissue to retard the expulsion of fluid.
Bismuth subsalicylate is an antacid and antimicrobial, gastroprotective, anti-secretory, and anti-inflammatory actions. It works to reduce the severity and incidence of flatulence and diarrhea, and consequently relieving gastrointestinal discomfort. In one study, bismuth subsalicylate was prevented traveler's diarrhea with a protection rate >60%.
Organobismuth compounds, formed by the breakdown of bismuth subsalicylate in the gastrointestinal tract, inhibit the growth of Helicobacter pylori and other bacteria implicated in gastrointestinal disorders, and some fungi. In one study, bismuth subsalicylate was shown to eradicate up to 90% of H. pylori infection when used as part of a quadruple therapy regimen containing a proton pump inhibitor, tetracycline, and metronidazole. Bismuth subsalicylate exhibited antimicrobial activity against Clostridium difficile, enterotoxigenic Escherichia coli O157:H7, norovirus, and other common enteric pathogens such as Salmonella and Shigella.
Trade Name | Peptolite |
Generic | Bismuth Subsalicylate |
Bismuth Subsalicylate Other Names | Bismuth oxide salicylate, Bismuth oxysalicylate, Bismuth subsalicylate, Pink bismuth, Wismutsubsalicylat |
Type | |
Formula | C7H5BiO4 |
Weight | Average: 362.0926 Monoisotopic: 361.999166889 |
Protein binding | Salicylic acid is about 90% plasma protein bound. Bismuth is about >90% bound to plasma proteins. |
Groups | Approved, Vet approved |
Therapeutic Class | Anti-dyspeptic/Carminatives |
Manufacturer | |
Available Country | Israel |
Last Updated: | September 19, 2023 at 7:00 am |
![Peptolite Peptolite](https://www.medicinesfaq.com/media/png/peptolite.png)
Uses
Peptocid is used for indigestion, gastric fullness, bloating, belching, growling stomach, sour stomach and diarrhea.
Peptolite is also used to associated treatment for these conditions: Diarrhoea, Dyspepsia, Flatulence, Heartburn, Helicobacter Pylori Infection, Nausea, Traveler's Diarrhea, Upset stomach, Belching, Gastrointestinal fullness
How Peptolite works
The exact mechanism of bismuth subsalicylate is not fully understood. Bismuth subsalicylate is an insoluble complex that constitutes salicylic acid and trivalent bismuth. Once orally administered, bismuth subsalicylate hydrolyzes in the stomach into bismuth oxychloride, which is minimally absorbed into the bloodstream, and salicylic acid, which is almost completely absorbed. Bismuth interacts with other anions and compounds, such as hydrochloric acid, bicarbonate, phosphate, and hydrogen sulfide, in the gastrointestinal tract to form bismuth salts such as bismuth oxychloride, bismuth subcarbonate, bismuth phosphate, and bismuth sulfide. Bismuth salts possess bactericidal and antimicrobial activity, mainly by preventing bacteria from binding and growing on the mucosal cells of the stomach. It has no effects on normal gut flora. By preventing bacteria from binding to mucosal cells, bismuth subsalicylate prevents intestinal secretion and fluid loss, promotes fluid and electrolyte reabsorption, reduces gastrointestinal inflammation, and promotes the healing of pre-existing ulcer in the stomach. Salicylic acid from dissociated bismuth subsalicylate adds to the anti-inflammatory actions of bismuth salts by inhibiting the cyclooxygenase enzyme and limiting the formation of prostaglandin, a pro-inflammatory mediator. Bismuth subsalicylate exhibits cytoprotective and demulcent activity, which makes it an effective drug in peptic ulcer disease. It blocks the adhesion of H. pylori to the gastric epithelial cells and blocks the bacteria's enzyme activities, including phospholipase, protease, and urease.
Dosage
Peptolite dosage
12 years and above: 30 ml at a time.Dose can be repeated after 1-2 hours if necessary. Daily maximum intake should not exceed 8 doses.Less than 12 years: Please contact with physician.
Side Effects
Black stool and black tongue are common with use of Peptocid. Peptocid should not be used if black stool and black tongue are severe or persist for more than 2 days.
Toxicity
Lowest Lethal Dose (LDLo) in humans is 700 mg/kg. LD50 in rats is 1200 mg/kg via oral route, 542 mg/kg via intraperitoneal route, and 980 mg/kg via subcutaneous route.
Overdose of bismuth subsalicylate over an extended period of time and consequently, bismuth toxicity, can lead to blackening of the tongue and teeth, fatigue, mood changes, deterioration of mental status, and neurotoxicity. Other signs and symptoms include impaired cognition, tremors, lethargy, somnolence, insomnia, delirium, myoclonus, seizures, depressed mood, anxiety, and a depressed mood. Salicylate toxicity can occur from chronic bismuth subsalicylate use : it mostly occurs from ingestion of more than 150 mg/kg of salicylates (or >6.5 g of aspirin equivalent). As there are no specific antidotes for bismuth salicylate toxicity, overdose should be managed with supportive care, with or without decontamination with activated charcoal. Hemodialysis may be considered in more severe cases and with the presence of altered mental status and metabolic acidosis.
Precaution
Do not take with aspirin or other salicylates. Caution should be exercised by patients taking medicines for anti-coagulation, diabetes or gout.For elderly patients suffering from renal insufficiency, caution should be taken.
Interaction
There are no known drug interactions and none well documented.
Food Interaction
No interactions found.Volume of Distribution
There is no information available.
Elimination Route
Following oral administration, bismuth subsalicylate hydrolyzes into bismuth and salicylic acid in the stomach. Salicylic acid is almost completely absorbed in the small intestine and reaches plasma peak levels one to two hours after dosing. In one study involving healthy male subjects, oral administration of 60 mL Pepto-Bismol, a common over-the-counter product of bismuth subsalicylate, equivalent to 1050 mg of bismuth subsalicylate, resulted in the peak plasma concentration of salicylate of 40.1 μg/mL, with a time to peak concentration (Tmax) of 1.8 hours.
Less than 1% of bismuth from bismuth subsalicylate is absorbed from the gastrointestinal tract into the systemic circulation. In one study, oral administration of 787 mg bismuth subsalicylate in the chewable tablet form for two weeks resulted in the mean trough blood bismuth concentration was 5.1 ± 3.1 ng/mL. In another study, the mean trough blood bismuth concentration ranged from five to 32 ng/mL following oral administration of 525 mg bismuth subsalicylate in the liquid suspension form.
Half Life
The terminal half-life of salicylic acid following a single oral dose of 525 mg bismuth subsalicylate is ranges from two to five hours. Bismuth has an intermediate half-life of 5 to 11 days and a terminal half-life of 21 to 72 days.
Clearance
The renal clearance of bismuth is 50 ± 18 mL/min.
Elimination Route
Following oral administration, salicylate dissociated from bismuth subsalicylate is excreted in the urine. Bismuth is primarily eliminated via urinary and biliary routes.
Pregnancy & Breastfeeding use
There are no adequate data concerning the use of Peptocid in pregnant women. Peptocid should be avoided during pregnancy and lactation.
Contraindication
Hypersensitivity to bismuth, aspirin, other salicylates, Infectious diarrhea, high fever, von Willebrand disease, hemorrhage, ulcer or Gl bleeding with black or bloody stool, hemophilia, chicken pox or influenza (risk of Reye syndrome); changes in behavior with nausea and vomiting may be early sign of Reye syndrome.
Acute Overdose
Bismuth intoxication may be present as an acute encephalopathy with confusion, myoclonic movements, tremor, dysarthria and walking and standing disorders. Bismuth intoxication may also cause gastrointestinal disturbance, skin reactions, discoloration of mucus membranes and renal dysfunction as a result of acute tubular necrosis. Treatments include gastric lavage, purgation and hydration. Overdose of Peptocid may also give symptoms of salicylate intoxication e.g. dizziness, tinnitus, sweating, nausea, headache. If symptoms occur, use of Peptocid should be avoided.
Storage Condition
Store in a cool (25 o C) and dry place.Keep out of the reach of children.Shake well before use.
Innovators Monograph
You find simplified version here Peptolite
Peptolite contains Bismuth Subsalicylate see full prescribing information from innovator Peptolite Monograph, Peptolite MSDS, Peptolite FDA label