Bismuth subcitrate

Bismuth subcitrate is a compound used in medicine, primarily as an antiseptic and antiemetic. This compound includes bismuth and citrate, which is a salt representative of citrate acid.

Bismuth subcitrate is commonly used to treat various gastrointestinal disorders such as heartburn, dyspepsia, and diarrhea. It acts protectively on the gastric mucosa, creating a protective layer and reducing irritation.

However, it is important to note that bismuth subcitrate should only be used under medical supervision, as improper use or overdosing can cause unwanted side effects such as bismuth deposition in tissues (including the brain), which can lead to toxic effects.

Indications Bismuth subcitrate

1. Dyspepsia: Including heartburn, nausea, vomiting, stomach pain and non-specific dyspepsia (functional digestive disorders).
2. Diarrhea: For short-term or acute diarrhea, especially when caused by infection or irritation of the intestinal mucosa.
3. Gastrointestinal ulcers: As a protective agent for the mucous membrane of the stomach and intestines in peptic ulcer disease.
4. Prevention of toxic effects of drugs: Including to protect the mucous membrane of the stomach and intestines from the irritating effects of certain drugs, such as nextradol, aspirin and some NSAIDs.
5. Other digestive disorders: Including irritable bowel syndrome and dysbiosis.

Release form

Bismuth subcitrate is usually available as a powder or crystals for the preparation of various dosage forms, such as suspensions or tablets. It can also be included in some medications intended for the treatment of various gastrointestinal disorders, including gastric ulcer and intestinal ulcer.

Pharmacodynamics

1. Antimicrobial action: Bismuth subcitrate has an antimicrobial action, helping to suppress the growth of various pathogenic microorganisms in the gastrointestinal tract. It may be effective in treating infections caused by Helicobacter pylori, a bacterium that can cause gastric ulcers and duodenal ulcers.
2. Anti-inflammatory action: Bismuth subcitrate also has the ability to reduce inflammation in the mucous membrane of the stomach and intestines. This helps reduce symptoms associated with irritation of the mucous membrane and inflammation, such as pain, discomfort and diarrhea.
3. Protective effect on mucosa: Bismuth subcitrate can form a protective coating on the mucosa of the stomach and intestines, which helps prevent further irritation and damage.
4. Toxin Binding: Bismuth subcitrate has the ability to bind and neutralize toxins that may be the cause of various gastrointestinal disorders such as irritable bowel syndrome.
5. Promoting Ulcer Healing: In addition to reducing inflammation and protecting the mucosa, bismuth subcitrate may also promote ulcer healing and improve the condition of the mucosa after injury.
6. Minimal Absorption: Since bismuth subcitrate has low absorption from the gastrointestinal tract, its action is limited primarily to the gastrointestinal mucosa, which minimizes systemic side effects.

Pharmacokinetics

The pharmacokinetics of bismuth subcitrate describe how the body takes up, metabolizes, and excretes this drug. However, given that bismuth subcitrate is commonly used in combination products, pharmacokinetic data may be limited or unavailable.

Dosing and administration

1. Tablets or capsules:

   • The dosage is usually 120-300 mg of bismuth subcitrate two or three times daily.
   • Take tablets or capsules after meals with a full glass of water.
   • Follow the directions on the package or your doctor's instructions regarding how often to take it and how long to take it.

2. Suspension:

   • If you are using the suspension, it is important to shake the bottle well before each use to ensure even distribution of the medication.
   • Measure the required amount of suspension using the dispenser or measuring spoon provided in the package.
   • Follow your doctor's instructions regarding dosage and frequency of administration.

3. Duration of treatment:

   • The duration of treatment with bismuth subcitrate is determined by your doctor and depends on the nature of your disease and your response to treatment. Treatment can usually last several days or weeks.

Use Bismuth subcitrate during pregnancy

The use of bismuth subcitrate during pregnancy should be discussed with a physician, as the safety of this drug in pregnant women has not been established. The use of bismuth subcitrate can only be justified if the benefits of its use outweigh the potential risks to the development of the fetus.

Contraindications

1. Individual intolerance: People with known individual intolerance to bismuth subcitrate or any other component of the drug should avoid using it.
2. Allergic reactions: In patients with a history of allergic reactions to bismuth or other bismuth-containing products, the use of bismuth subcitrate may be contraindicated.
3. Renal impairment: Since bismuth is partially excreted via the kidneys, the use of bismuth subcitrate may be limited or contraindicated in patients with severe renal disease or impairment of renal function.
4. Pregnancy and breastfeeding: There are limited data on the use of bismuth subcitrate during pregnancy and breastfeeding, so its use during these periods may be contraindicated without consulting a doctor.
5. Paediatric population: The use of bismuth subcitrate in children may be contraindicated due to insufficient data on efficacy and safety in this age group.
6. Unstudied conditions: The use of bismuth subcitrate may be contraindicated in patients with certain conditions, such as acute pancreatitis or acute bleeding diathesis, where the safety and efficacy of its use have not been adequately studied.

Side effects Bismuth subcitrate

1. Stool changes: Including black stool (melena), which is common with bismuth. This is due to the formation of bismuth compounds that turn the stool black. This is usually temporary and harmless, but may be important in differentiating it from gastrointestinal bleeding.
2. Systemic side effects: Including rare reactions such as allergic reactions, nausea, vomiting, diarrhea and other gastrointestinal disorders.
3. Bismuth deposition: Long-term or excessive use of bismuth can cause deposits in the body, which can lead to toxic effects. This can manifest as flu-like symptoms (e.g. fever, weakness, seizures) or more serious side effects such as kidney and nervous system damage.
4. Other side effects: May include anemia, taste disturbances, skin changes, and rarely arthritis or vasculitis.

Overdose

1. Bismuth Toxicity: Overdose can lead to bismuth toxicity, which manifests itself in a variety of symptoms including nausea, vomiting, diarrhea, anemia, disorientation, shaking, abdominal pain, headaches, impaired coordination, and even in extreme cases, more serious complications such as neurological disorders and kidney damage.
2. Activation of systemic inflammation: A systemic inflammatory response may develop, which can lead to damage to organs and body systems.
3. Kidney and Liver Damage: Bismuth can accumulate in the kidneys and liver, which can cause damage and dysfunction.
4. Electrolyte disturbances: Overdose may result in electrolyte disturbances in the body, including hyperkalemia and hypocalcemia.
5. Cardiac complications: In rare cases, overdose may cause cardiac arrhythmias and heart failure.
6. Convulsive syndrome: Development of convulsive syndrome is possible.

Interactions with other drugs

1. Tetracyclines and fluoroquinolones: Bismuth subcitrate may reduce the absorption of tetracyclines and fluoroquinolones due to the formation of complexes between them in the stomach.
2. Medicines containing iron or zinc: Bismuth subcitrate may reduce the absorption of iron and zinc due to the formation of insoluble compounds.
3. Salicylate preparations: Bismuth subcitrate may enhance the action of salicylates, which may lead to an increase in their toxic effect.
4. Antiulcer drugs: Bismuth subcitrate is often used in combination with antacids, proton pump inhibitors and prokinetics for the treatment of peptic ulcer and dyspepsia. In such combinations, the therapeutic effect can be enhanced.
5. Drugs that affect gastric pH: Drugs that alter gastric pH (eg, antacids) may affect the solubility of bismuth subcitrate and its ability to form complexes with other substances.