BISMUTH SUBSALICYLATE

Absorption

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.

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.

Description

Bismuth subsalicylate was originally used in a formula developed 100 years ago by a doctor in his home to combat cholera infantum. A staple of many medicine cabinets, bismuth subsalicylate, in the form of Pepto-Bismol, is be taken by countless people during the holiday season to help reverse the effects of overindulging.

Chemical properties

White or almost white powder.

The Uses of BISMUTH SUBSALICYLATE

To impart pearly surface to cellulose-base, polystyrene, and phenolformaldehyde resins. Typical tap bulk density 0.43g/cm^3Bismuth subsalicylate is used to treat temporary discomforts of the stomach and gastrointestinal tract, such as diarrhea, indigestion, heartburn and nausea. It also acts as an antacid. It is practiced to decrease the number of bowel movements and to make the stool firmer. It is also used to reduce inflammation within the intestine. It is further used in growth media for selective isolation of microorganisms.

The Uses of BISMUTH SUBSALICYLATE

anticoagulant

The Uses of BISMUTH SUBSALICYLATE

Used to treat nausea, heartburn, indigestion, upset stomach, diarrhea, and other temporary discomforts of the stomach and gastrointestinal tract.

Indications

Bismuth subsalicylate is indicated to temporarily relieve diarrhea, travelers' diarrhea, and upset stomach due to overindulgence in food and drink, including heartburn, indigestion, nausea, gas, belching, and fullness.
Bismuth subsalicylate is a component of HELIDAC Therapy (bismuth subsalicylate, metronidazole, and tetracycline), which is a treatment regimen indicated for the eradication of H. pylori for treatment of patients with H. pylori infection and duodenal ulcer disease.

Background

Bismuth subsalicylate is an antacid and anti-diarrheal agent. Exhibiting antibacterial and gastroprotective properties, bismuth subsalicylate is an insoluble salt of salicylic acid linked to trivalent bismuth cation. Each molecule of bismuth subsalicylate contains 58% bismuth and 42% salicylate by weight. Bismuth subsalicylate has been around for over 100 years: it was originally developed in 1901 for hygienic use and sanitation for cholera infection.
Bismuth subsalicylate was first approved by the FDA in 1939 and is now mainly used to relieve nausea, diarrhea, and gastrointestinal discomfort. It is an active ingredient found in Pepto-Bismol, a common over-the-counter medication that is used to temporarily treat discomforts of the stomach and gastrointestinal tract. Bismuth subsalicylate is a component of HELIDAC Therapy (bismuth subsalicylate, metronidazole, and tetracycline), which is a treatment regimen indicated for the eradication of H. pylori for treatment of patients with H. pylori infection and duodenal ulcer disease.

What are the applications of Application

Bismuth(III) subsalicylate is an antiinflammatory

Indications

Bismuth subsalicylate (Pepto-Bismol) also binds intestinal toxins and may coat irritated mucosal surfaces.

Definition

ChEBI: Bismuth subsalicylate is a bismuth salt of salicylic acid. It is a member of salicylates and a bismuth coordination entity.

General Description

White crystalline powder or fluffy white solid.

Air & Water Reactions

Insoluble in water.

Reactivity Profile

BISMUTH SUBSALICYLATE is stable in air but is sensitive to light. BISMUTH SUBSALICYLATE is unstable in alkaline solutions. BISMUTH SUBSALICYLATE decomposes in boiling water and alkalis into a more basic salt.

Hazard

A poison by ingestion. Human systemic effects.

Health Hazard

SYMPTOMS: Symptoms of exposure to BISMUTH SUBSALICYLATE may include headache, nausea, foul breath, blue-black line on the gums and stomatitis.

Fire Hazard

Flash point data for BISMUTH SUBSALICYLATE are not available, but BISMUTH SUBSALICYLATE is probably combustible.

Flammability and Explosibility

Non flammable

Pharmacokinetics

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.

Side Effects

This compound is a salicylate and may therefore produce signs of salicylate toxicity (e.g., ringing of the ears) if taken chronically, especially with aspirin. Bismuth is radiopaque and may interfere with radiological examinations. Its use may cause temporary gray-black discoloration of the stool and brown pigmentation of the tongue. High dose Pepto-Bismol (8 tablets/day) has been efficacious in some patients with diarrhea secondary to collagenous or lymphocytic colitis.

Veterinary Drugs and Treatments

In veterinary medicine, bismuth subsalicylate products are used to treat diarrhea and as a component of “triple therapy” for treating Helicobacter GI infections. The drug is also used in humans for other GI symptoms (indigestion, cramps, gas pains) and in the treatment and prophylaxis of traveler’s diarrhea.

Metabolism

Bismuth subsalicylate undergo hydrolysis at pH levels lesser than three. It is largely hydrolyzed in the stomach to bismuth oxychloride and salicylic acid. In the small intestine, unchanged bismuth subsalicylate reacts with other anions such as bicarbonate and phosphate to form insoluble bismuth salts. In the colon, unchanged bismuth subsalicylate and other bismuth salts react with hydrogen sulfide produced by anaerobic bacteria to form bismuth sulfide, a highly insoluble black salt responsible for the darkening of the stools.