Gastro-Bismol/Gastro-Bismol L

Gastro-Bismol/Gastro-Bismol L

Manufacturer:

Farmaline

Distributor:

Farmaline
Full Prescribing Info
Contents
Bismuth subsalicylate.
Action
Pharmacology: Pharmacodynamics: Bismuth subsalicylate is an insoluble salt of trivalent bismuth and salicylic acid, with each molecule containing 42% salicylate and 58% bismuth. Bismuth compounds have been demonstrated to exert numerous actions in the gastrointestinal tract, including antibacterial activity, protective effects on the gastric mucosa, binding of the ulcer base and mucus, and binding of bile acids.
Bismuth subsalicylate appears to have antisecretory and antimicrobial effects in vitro and may give some anti-inflammatory effects. The salicylate moiety provides the antisecretory and anti-inflammatory effects, while the bismuth moiety may exert direct antimicrobial effects against bacterial and viral enteropathogens.
Therapeutic effects of bismuth subsalicylate in gastritis and gastric and duodenal ulcer have been primarily attributed to demulcent and cytoprotective properties. Bismuth subsalicylate interferes with the integrity of the Helicobacter pylori cell and prevents adhesion of the organism to the gastric epithelium. Another mechanism by which bismuth compounds interferes with H. pylori is by inhibiting its urease, phospholipase and proteolytic activity. By eliminating H. pylori associated with peptic ulcers, the esophageal lesion healing rate is improved and the chance of recurrence is decreased. The in vitro minimum inhibitory concentration (MIC) of bismuth subsalicylate for H. pylori ranges from 2-32 mcg/mL, and these concentrations are achieved locally in the gastric mucosa.
The antidiarrheal effects of bismuth subsalicylate appear to be mediated via both antimicrobial and antisecretory properties. Direct antimicrobial activity against numerous diarrheal pathogens has been reported, including E. coli, salmonella, Clostridium difficile, Campylobacter jejuni and shigella. Other aerobic and anaerobic bacteria in the normal microflora are also inhibited in vitro, although the overall composition of normal flora of the stomach or feces does not appear altered.
Pharmacokinetics: Time to peak concentration (tmax): Oral: 1.8-5 hrs. With a dose regimen of 524 mg bismuth subsalicylate (30 mL suspension) every 30 min for a total of 8 doses in 3.5 hrs, peak salicylate serum level of 137 mcg/mL were observed; peak levels occurred 5 hrs after administration of the 1st dose. Steady-state salicylate plasma level of 24 mcg/mL were reported after 2 weeks of therapy during administration of bismuth subsalicylate 30 mL (1 tablet) 4 times daily for 3 weeks (daily dose 2.1 g).
Absorption: Bioavailability: Gastro-Bismol: Less than 1% (bismuth), >80% (salicylic acid) bismuth serum level following oral administration of bismuth subsalicylate are characteristically low due to poor gastrointestinal absorption. Normal bismuth plasma levels are <10 mcg/L.
In contrast, the salicylate moiety of bismuth subsalicylate is almost completely absorbed, with 95% of salicylate in each dose being recovered in the urine after 72 hrs.
Gastro-Bismol L: Bismuth subsalicylate undergoes chemical dissociation in the gastrointestinal tract. One (1) tablet of Gastro-Bismol L yields salicylate 408 mg. Following ingestion, salicylate is absorbed with >90% recovered in the urine; plasma levels are similar to levels achieved after a comparable dose of aspirin. Absorption of bismuth is negligible.
Distribution: Bismuth is 90% bound to plasma proteins. Absorbed bismuth is sequestered in multiple tissue site and slowly excreted over a period of several months. Bismuth has a half-life (t½) ranging from 5-11 days.
Metabolism: Bismuth subsalicylate is hydrolyzed in the stomach to form bismuth oxychloride and salicylic acid. A portion of unchanged bismuth subsalicylate passed into the duodenum, and reacts with other anions; salicylate continues to be released from these reactions. Salicylate is primary absorbed in the small intestine.
In the colon, bismuth oxychloride, undissociated bismuth subsalicylate, bismuth subcarbonate and bismuth phosphate react with hydrogen sulfite to form bismuth sulfide; this salt is black and insoluble and accounts for the harmless darkening of the stool associated with the use of bismuth subsalicylate.
Excretion: Salicylate absorbed from bismuth subsalicylate appears in breast milk. Renal excretion (in urine): Salicylate 95%. Greater than 99% of bismuth present in a dose of bismuth subsalicylate is excreted in the feces.
Toxicology: Salicylate plasma levels of 200-390 mcg/mL are associated with adverse effects (eg, tinnitus, hyperventilation, dehydration), and acute salicylate toxicity occurs with levels exceeding 400 mcg/mL.
"Safe" serum bismuth levels during bismuth salt therapy are considered to be <50 mcg/L. Most patients with bismuth encephalopathy have had blood bismuth level in excess of 100 mcg/L (more commonly, >500 mcg/L). In one case of encephalopathy associated with bismuth salicylate administration, the blood bismuth level on admission was 72 mcg/mL; this declined to 10 mcg/mL after 2 weeks.
Indications/Uses
Treatment of indigestion occurring after food or alcohol ingestion. Treatment of diarrhea and controlling associated complaints eg, cramping, heartburn, nausea and stomach upset when administered following the occurrence of diarrhea, a significant reduction in the number of unformed stools. Treatment and prevention of traveler's diarrhea. Treatment of acute or chronic diarrhea of childhood. Bismuth subsalicylate alone has been effective in the treatment of gastritis and peptic ulcer associated with Helicobacter pylori infection. Bismuth subsalicylate in combination with proton pump inhibitor (PPI) or antimicrobial use is effective in the treatment of Helicobacter pylori-associated active duodenal ulcer disease.
Dosage/Direction for Use
Gastro-Bismol: Adults: Treatment of Diarrhea Including Traveler's Diarrhea: 30 mL (1 tab) every 30 min to 1 hr up to a maximum of 8 doses daily and continued for 2 days.
Treatment of Gastritis: 30 mL (1 tab) 4 times daily for 3 weeks effective in treating H. pylori-associated gastritis.
Treatment of H. pylori Infections: Bismuth salicylate 524 mg twice daily with 2 antibiotics (eg, amoxicillin 1 g, metronidazole 500 mg, clarithromycin 500 mg) twice daily and proton-pump inhibitor (eg, omeprazole 200 mg) twice daily, with treatment duration of 10-14 days.
Treatment of Indigestion (Stomach upset, Nausea and Other Symptoms of Dyspepsia): 30 mL (1 tablet) every 30 min to 1 hr up to a maximum of 8 doses.
Treatment of Peptic Ulcer: 30 mL (1 tablet) 3 times daily.
Children 9-12 years: For Treatment of Diarrhea, Nausea, Stomach Upset: Use 15 mL; 6-9 years: Use 10 mL; 3-6 years: Use 5 mL. All doses may be repeated every 30 min to 1 hr up to a maximum of 8 doses in a 24-hr period.
Acute Diarrhea of Childhood: Children 4-6 months: 100 mg/kg/day.
Sachet: Adults: 1-2 sachets four times daily before meals and at bedtime. Children 9-12 years: 1 sachet four times daily before meals and at bedtime, 6-9 years: 10 mL four times daily before meals and at bedtime, 3-6 years 5 mL four times daily before meals and at bedtime, under 3 years as directed by physicians.
Gastro-Bismol L:
Recommended Dose: Adults: 1 tablet twice daily. Children 9-12 years: ½ tablet twice daily. Dose may be repeated every 1 hr if needed but a maximum of 4 doses/day (4.2 g) should not be exceeded.
Anti-Ulcer Regimen: OBMT Quadruple Therapy (>90% Efficacy): Omeprazole 20 mg once daily, bismuth subsalicylate 1 tablet twice daily, metronidazole 250 mg 4 times daily, tetracycline 500 mg 4 times daily for 7 days.
BMT Triple Therapy (85% Efficacy): Bismuth subsalicylate 1 tablet twice daily, metronidazole 250 mg 4 times daily, tetracycline 500 mg 4 times daily for 7-10 days.
Administration: Gastro-Bismol: Shake well before use.
Gastro-Bismol L: Should be taken with lots of water.
Overdosage
Patients who have received doses higher than the recommended dose should be carefully monitored.
In salicylate toxicity, the event of clinically significant tinnitus, hyperventilation, dehydration may occur.
Contraindications
Hypersensitivity to bismuth preparation, aspirin or salicylates. Histories of severe gastrointestinal bleeding and coagulopathy.
Use in Pregnancy: Salicylates cross placenta. Concern only goes with high doses and long-term therapy bacause of salicylates effects. Thus, it is contraindicated during 3rd trimester of pregnancy.
Special Precautions
Bismuth subsalicylate may cause a temporary and harmless darkening of the tongue and/or black stool.
Concomitant administration of drugs for anticoagulation, gout or diabetes.
Previous hypersensitivity to nonsteroidal anti-inflammatory agents. Patients with gout, diabetes, bleeding ulcers, hemophilia or other hemorrhagic conditions, or renal insufficiency (due to salicylate component). Patients with colitis or other gastrointestinal mucosa abnormalities which may enhance bismuth absorption. Rare reports of neurotoxicity with excessive dose of bismuth subsalicylate.
Bismuth may interfere with radiologic examinations in gastrointestinal tract.
Impactation may occur in debilitated patients.
Patient with renal impairment.
Use in Lactation: Concern only goes with high doses and chronic use because salicylate intake of infant may occur.
Use in Children: Caution in use of bismuth subsalicylate in infants and children (greater risk of impaction and salicylate toxicity). Children and teenagers who have or are recovering from influenza or varicella.
Use In Pregnancy & Lactation
Use in Pregnancy: Salicylates cross placenta. Concern only goes with high doses and long-term therapy bacause of salicylates effects. Thus, it is contraindicated during 3rd trimester of pregnancy.
Use in Lactation: Concern only goes with high doses and chronic use because salicylate intake of infant may occur.
Adverse Reactions
Tinnitus, encephalopathy has occurred only rarely with bismuth subsalicylate, nausea, vomiting, constipation, diarrhea, melena. The risk of constipation or impaction is greater in infants, children and debilitated elderly patients. Grayish-black discoloration of the feces. Grayish-black discoloration of the tongue may also occur.
Drug Interactions
Combination with methotrexate decreases methotrexate elimination. Combination with probenecid or sulfinpyrazone decreased uricosuric effects of probenecid or sulfinpyrazone. Although there are no reports of a warfarin-bismuth subsalicylate interaction in the literature, there appears to be potential for such interaction. Concurrent use of warfarin and salicylates should be avoided. Bismuth subsalicylate increases risk of bleeding.
Aspirin: Bismuth subsalicylate contains salicylate. If taken with aspirin and ringing of the ears occurs, discontinue use.
Tetracycline: Bismuth subsalicylate may decrease gastrointestinal absorption and bioavailability of tetracycline reducing its efficacy.
Storage
Store below 30°C in a dry place. Protect from light.
ATC Classification
A07BB - Bismuth preparations ; Used as intestinal adsorbents.
Presentation/Packing
Gastro-Bismol Tab 524 mg x 10 x 10's, 20 x 10's. Susp 262 mg/15 mL (orange and original flavor) x 240 mL x 24's; (sachet; original flavor) 262 mg x 20's. Gastro-Bismol L Tab 1048 mg (oblong, biconvex, pink) x 10 x 10's, 20 x 10's.
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