Analogues of bismuth tripotassium dicitrate: a review of substitutes for action and active substance. Visitor Report on Side Effects
Colloidal bismuth subcitrate belong to the group antacids And adsorbents . The substance is usually found in film-coated tablets. Its molecular weight is 704 g per mole.
pharmachologic effect
Enveloping, antibacterial, gastroprotective, antiulcer.
Pharmacodynamics and pharmacokinetics
The substance has a pronounced astringent and anti-inflammatory effect. Getting into the acidic environment of the stomach bismuth oxychloride And bismuth citrate precipitate and form chelate complexes in the form of a protective film on the surface of the damaged mucosa. The agent stimulates the synthesis PgE2 , selection bicarbonate and mucus, activates the protective properties of the gastric mucosa, thereby protecting gastrointestinal tract from the effects of aggressive acids, salts and enzymes. In the area where the damage to the mucous membrane occurred, accumulates epidermal growth factor . Activity pepsin And pepsinogen starts to decline.
Bismuth Dicitrate Accumulates Inside Bacteria Helicobacter and leads to their destruction. cytoplasmic membrane and death. Due to the ability of the substance to penetrate under the layer duodenal mucus , where the concentration Helicobacter pylori the greatest, its effectiveness in the eradication of bacteria Helicobacter significantly higher than similar products.
The medicine is not absorbed by the walls gastrointestinal tract and does not enter the systemic circulation. The unchanged substance is excreted in the feces. A small amount of the drug that enters the bloodstream is metabolized and excreted in the urine.
Indications for use
The drug Bismuth Tripotassium Dicitrate is used:
- with, accompanied by seizures;
- for treatment, including those caused by bacteria Helicobacter ;
- during exacerbation chronic And gastroduodenitis ;
- in patients with, which is not caused by organic lesions gastrointestinal tract .
Contraindications
The drug can not be prescribed:
- during breastfeeding;
- pregnant women;
- for this substance;
- patients with renal insufficiency.
Side effects
During treatment with the drug may occur:
- vomiting, constipation or nausea;
- skin rashes, itching, other allergic reactions.
With prolonged use of this substance in the central nervous system may accumulate bismuth , which leads to development.
Bismuth Tripotassium Dicitrate, instructions for use (Method and dosage)
Depending on the disease, it is advisable to use different treatment regimens.
Bismuth Tripotassium Dicitrate tablets are taken orally with water.
As a rule, adults are prescribed 480 mg per day, divided into 4 doses, half an hour before meals or at bedtime. You can also take 240 mg, 2 times a day.
Children from 4 to 8 years old are prescribed 8 mg per kg of body weight per day, the daily dosage should be divided into 2 doses. The course of treatment is prescribed by the attending physician and, as a rule, it is 1-2 months.
Within 2 months after the course, you can not take drugs bismuth .
Bismuth Tripotassium Dicitrate is used in various treatment regimens Helicobacter pylori . The drug is combined with proton pump inhibitors ( , or ) and antibiotics ( , , ).
Overdose
With prolonged use of overdoses of the drug, there are observed: disturbances in the functioning of the kidneys,.
The treatment is: gastric lavage, enterosorbents And saline laxatives means, symptomatic therapy.
In case of violations in the work of the kidneys, which are accompanied by a high level of bismuth in the blood, are shown: complexing agents — dimercapto-propanesulfonic acid And dimercapto-succinic acid,
Bismuth tripotassium dicitrate (trade name - the drug "De-Nol") is an effective antiulcer drug with a pronounced bactericidal activity against microorganisms of the species Helicobacter pylori. In addition, this medicine has antacid, anti-inflammatory and astringent effects. Taking this remedy significantly improves the protective characteristics of the mucous surface of the gastrointestinal tract, forming a special insoluble coating directly at the site of the ulcer. Also, bismuth tripotassium dicitrate increases the resistance of the stomach and intestines to the negative effects of enzymes, pepsin and hydrochloric acid, increases mucus production, bicarbonate secretion and the synthesis of prostaglandin type E. In addition to all of the above, experts note its ability to stimulate the activity of cytoprotective mechanisms.
As for the pharmacokinetics of this antiulcer agent, as a result of its course use, equilibrium concentrations in the blood are reached after four to five days, and the half-life is about five days. In this case, the fully active component is excreted from the body only twelve weeks after the start of taking such a remedy as bismuth tripotassium dicitrate. Analogues of this tool - capsules "Bismay", "Desmol" and "Novobismol" - have a similar mechanism of action.
This is produced mainly in the form of conventional coated medicinal dragees. Taking tablets "De-Nol" (bismuth tripotassium dicitrate), the price of which is very affordable, the manufacturer recommends exclusively for the treatment of duodenal ulcers or stomach ulcers. People suffering from chronic gastritis should also start taking this drug regularly. In addition, bismuth tripotassium dicitrate will quickly help in case of dyspepsia not associated with organic diseases of the gastrointestinal tract.
Doctors categorically prohibit taking this antiulcer drug in severe forms of impaired renal function, as well as during pregnancy. Hypersensitivity and the period of breastfeeding a newborn baby are similarly included in the list of strict contraindications. Patients who have not reached the age of twelve should also not start taking drugs that include bismuth tripotassium dicitrate. In addition, it must always be remembered that in people with various kinds of abnormalities in the functioning of the kidneys, as a result of prolonged use of high dosages of this agent, encephalopathy may develop.
If we consider the most common adverse reactions that may be caused by taking this antiulcer drug, then vomiting, nausea and diarrhea should be highlighted first. In addition, there is a rather high risk of skin rash, itching, flushing of the skin and angioedema.
caps. 120 mg: 30 or 60 pcs.
Reg. No: 16/11/2629 dated 11/08/2016 - Valid
Capsules hard gelatin, No. 0, cylindrical shape with hemispherical ends, white; contents of capsules - powder of white or almost white color; the presence of particles in the form of a compacted powdery mass is allowed.
Excipients: magnesium stearate, anhydrous colloidal silicon dioxide, potato starch.
The composition of the gelatin capsule: gelatin, purified water, titanium dioxide (E171).
10 pieces. - cellular contour packings (3) - packs of cardboard.
10 pieces. - cellular contour packings (6) - packs of cardboard.
Description of the medicinal product DE-BISMUT based on the officially approved instructions for use of the drug and made in 2017. Date of update: 02/21/2018
Antiulcer drug with bactericidal activity against Helicobacter pylori. It also has anti-inflammatory and astringent properties. In the acidic environment of the stomach, insoluble bismuth oxychloride and citrate are precipitated, chelate compounds with a protein substrate are formed in the form of a protective film on the surface of ulcers and erosions. By increasing the synthesis of prostaglandins E, the formation of mucus and the secretion of bicarbonate, it stimulates the activity of cytoprotective mechanisms, increases the resistance of the gastrointestinal mucosa to the effects of pepsin, hydrochloric acid, enzymes and bile salts. Leads to the accumulation of epidermal growth factor in the area of the defect. Reduces the activity of pepsin and pepsinogen.
Suction
Bismuth potassium citrate is practically not absorbed from the gastrointestinal tract, the drug acts locally. The minimum amount of bismuth is absorbed (less than 0.2% of the dose taken).
Distribution
Bismuth is mainly found in the kidneys, other organs also contain traces of bismuth.
Metabolism
Insoluble bismuth compounds precipitate in the stomach, in particular bismuth oxychloride and bismuth citrate.
breeding
The main part of bismuth taken orally is excreted in the feces.
The renal clearance of a small amount of absorbed bismuth is approximately 50 ml/min. T 1/2 most of the absorbed bismuth is from 5 to 11 days.
The drug is taken orally. Capsules should be taken 30 minutes before meals with a small amount of water.
Adults and children over 12 years old the drug is prescribed 1 caps. 4 times / day 30 minutes before meals and at night or 2 caps. 2 times / day 30 minutes before meals.
Children aged 6 to 12 the drug is prescribed at the rate of 8 mg / kg / day. Depending on the weight of the child, 1-3 capsules / day are prescribed (respectively, 1-3 doses / day). In this case, the daily dose should be as close as possible to the calculated dose (8 mg/kg/day).
The duration of the course of treatment is 4-8 weeks. For the next 8 weeks, preparations containing bismuth should not be used.
For the eradication of Helicobacter pylori, it is advisable to use De-Bismuth in combination with other antibacterial agents with anti-Helicobacter pylori activity.
From the digestive system: very often (≥1 / 10) - blackening of the feces can occur due to the formation of bismuth sulfide, but it can be easily distinguished from melena;
From the skin and subcutaneous tissue: rarely (≥1/1000,<1/100) - легкие кожные аллергические реакции.
From the immune system: very rarely (<1/10 000), неизвестная частота (невозможно оценить по имеющимся данным) - анафилактические реакции.
With prolonged use in high doses - encephalopathy associated with the accumulation of bismuth in the central nervous system.
The drug should not be used for more than 8 weeks, it is also not recommended to exceed the established daily doses for adults and children during treatment.
During the period of treatment with De-Bismuth, other drugs containing bismuth should not be used, because. increases the risk of side effects.
At the end of the course treatment with the drug in recommended doses, the concentration of the active active substance in the blood plasma does not exceed 3-58 μg / l, and intoxication is observed only at a concentration above 100 mg / l.
When using the drug De-Bismuth, it is possible to stain the feces in a dark color due to the formation of bismuth sulfide. Sometimes there is a slight darkening of the tongue.
Prolonged use of large doses of bismuth-containing compounds is not recommended, since in some cases this can lead to reversible encephalopathy. The risk of encephalopathy, however, is minimal if De-Bismuth is used at recommended doses.
Pediatric use
The drug is not used in children under the age of 6.
Influence on the ability to drive vehicles and control mechanisms
Data on the effect of the drug De-Bismuth on the ability to drive vehicles and work with mechanisms are not available.
Symptoms: acute massive overdose can lead to renal failure with a delayed onset of up to 10 days.
Treatment: after a single dose of a very high dose, treatment should include gastric lavage followed by activated charcoal and osmotic laxatives. This reduces the absorption of bismuth, so additional therapeutic measures are not required.
The concentration of bismuth in the blood and urine should be determined in the case of acute and chronic intoxication to determine the relationship of symptoms with increased exposure to bismuth. Chelation therapy with dimercaptosuccinic acid (DMSA) or dimercaptopropane sulfonic acid (DMPS) is used when symptoms are known to be caused by acute or chronic bismuth overdose.
In severe renal failure after chelation therapy, hemodialysis should be performed.
Bismuth tripotassium dicitrate is the active ingredient in many drugs, the most famous of which is De-Nol. This drug is familiar to many patients of gastroenterologists. Bismuth tripotassium dicitrate is one of the effective antiulcer drugs. It has the ability to increase the functional activity of the mucous membranes of the digestive organs and restore their damage.
Specific causative agents of peptic ulcer and gastritis, the Helicobacter pylori bacteria, die much faster if, together with antibiotics and antimicrobials, patients take medicines with bismuth tripotassium dicitrate. The undoubted advantages of the drugs include the absence of the development of resistance of microorganisms when it is taken repeatedly.
Bismuth tripotassium dicitrate destroys the pathogens of peptic ulcer and gastritis Helicobacter pylori bacteria
Preparations
Based on the combined antiulcer action of a chemical compound, many pharmacological preparations have been synthesized. Tablets for internal use contain the main substance in the optimal therapeutic dosage - 120 mg. What medicines contain bismuth:
- Tribimol - manufactured by Torrent Pharmaceuticals (India);
- - releases ASTELLAS PHARMA EUROPE B.V. (Netherlands);
- Ventrisol - produces the Poznan pharmaceutical plant SA Polf (Poland);
- Trimo - manufacturers Rantakos Bret and Co Ltd (India);
- Bisnol - produced by Wave International (India);
- Novobismol - produced by Pharmproekt (Russia);
- Pilocid - the drug is produced by Merck KGaA (India).
The drugs differ from each other only in excipients that are necessary for the complete dissolution of the tablets, as well as the formation of the main dosage form.
Warning: "Despite the seeming minority of auxiliary components, they are of no small importance and significantly affect the effectiveness of drugs."
Consumer opinions about the therapeutic effect of drugs can vary significantly: some patients prefer drugs from an Indian manufacturer, others - Russian or Dutch.
pharmachologic effect
Under the action of the acidic gastric juice of bismuth tripotassium dicitrate decomposes into citrate and bismuth oxychloride, which are not able to dissolve in water. Inorganic substances enter into chemical reactions with high-molecular proteins with the formation of cyclic complex compounds. The acidic environment of the stomach in this case acts as a catalyst. As a result, a strong film is formed in the area where ulcerative lesions are located. Under the influence of this polymer glycoprotein complex, the mucous membrane of the gastrointestinal tract is under reliable protection from the negative effects of:
- of hydrochloric acid;
- digestive enzymes;
- bile.
Medicines containing bismuth are able to enlarge proteins and destroy microorganisms. The undoubted advantages of bismuth tripotassium dicitrate include its inability to be absorbed by the mucous membranes of the digestive organs. The minimum amount penetrates into the bloodstream, and the main part of the conglomerate is released with each bowel movement.
Bismuth tripotassium dicitrate is used in the treatment of gastric and duodenal ulcers.
Antibacterial properties of the compound
What is bismuth tripotassium dicitrate is a chemical compound that exhibits bactericidal activity against spiral gram-negative bacteria. Under its influence, the production of enzymes important for pathogenic pathogens of ulcers and gastritis is reduced. The course of reactions important for the vital activity of microorganisms begins to change, as a result of which they die. A chemical compound can disrupt:
- cell membrane permeability;
- cell membrane structure.
This significantly reduces its viability and prevents bacteria from attaching to the walls of the gastrointestinal tract.
Bismuth tripotassium dicitrate limits the free movement of spiral bacteria in the digestive tract. Other antimicrobials used to treat ulcers lose their effectiveness with repeated use. And bacterial strains are not able to develop resistance to drugs containing bismuth tripotassium dicitrate.
The chemical compound is characterized by a high degree of solubility, so it penetrates into the deepest layers of the walls of the stomach and inactivates the microorganisms located there.
Gastrocytoprotective effect
In addition to the bactericidal and protective effect of preparations containing bismuth, the list of useful properties of the chemical compound complements the gastrocytoprotective effect. They increase the resistance of the walls of the stomach to the negative effects of aggressive hydrochloric acid. This is based on the following mechanisms:
- the compound stimulates the synthesis of prostaglandins, which leads to the formation of an increased amount of mucin and the production of bicarbonate ions. As a result, a mucosal-bicarbonate barrier is formed;
- microcirculation improves in the antrum of the stomach and duodenum. Significantly increases the metabolic rate in cells, accelerates their regeneration. There is a rapid recovery of the damaged lining of the stomach;
- fundic cells of the mucous membrane reduce the production of caustic hydrochloric acid and the acidity of gastric juice is significantly reduced.
In addition to the above useful properties, preparations of bismuth tripotassium dicitrate affect the production of enzymes, which becomes an additional protection for the mucous membrane of the gastrointestinal tract.
De-Nol - the most famous drug with bismuth tripotassium dicitrate
Indications and contraindications
Gastroenterologists prescribe bismuth tripotassium dicitrate to patients who, under the influence of excessive production of enzyme substances and acids, have been diagnosed with damage to the mucous or submucosal layer of the stomach walls. The duration of treatment depends on the stage of the peptic ulcer. The drugs are used in the treatment of the following pathologies:
- during the period of relapse;
- dyspeptic disorders.
Bismuth tripotassium dicitrate is indicated for the treatment of gastric pathologies, regardless of whether Helicobacter pylori is detected during laboratory tests. There are certain restrictions on the use of a chemical compound:
- the period of bearing a child or breastfeeding;
- children's age up to 4 years;
Bismuth tripotassium dicitrate is not intended or restricted for use in certain categories of patients with liver disease.
Warning: "The drug should be used only after diagnosis and in accordance with medical recommendations."
When prescribing therapy, the gastroenterologist evaluates the risks and benefits of the substance, chooses which drugs contain bismuth and auxiliary ingredients in the safest doses for humans.
Pharmacological group of drugs - Antacids and adsorbents, regenerants and reparants. Names of drugs - Ventrisol, De-Nol, Tribimol.
Composition and form of release
Composition of Bismuth Subgalat
Amorphous powder of lemon-yellow color, odorless and tasteless. Practically insoluble in water and alcohol. Let's dissolve at heating in mineral acids (with decomposition). Easily soluble in sodium hydroxide solution to form a yellow solution that quickly turns red in air. Contains 52-54% bismuth oxide.
Composition of Bismuth Subnitrate
A mixture of BiNO3(OH)2, BiONO3 and BiOOH, which is a white amorphous or finely crystalline powder. Practically insoluble in water and alcohol, freely soluble in hydrochloric acid.
pharmachologic effect
Forming compounds with proteins, covers the ulcerative surface, protecting it from aggressive influences. Causes the death of Helicobacter pylori. Promotes healing of ulcers.
Indications for use of Bismuth
With peptic ulcer of the stomach and duodenum, gastritis, duodenitis, dyspeptic disorders.
Contraindications
Hypersensitivity, severe renal dysfunction, pregnancy.
Restrictions: breastfeeding (should stop breastfeeding).
Side effects
When taking high doses - the development of renal failure. Possible - nausea, vomiting, frequent stools. Rarely, allergic reactions in the form of skin rash and itching
Instructions for use
Method and dosage
Inside, drinking water (but not milk) - 1 table. 3-4 times a day 30 minutes before breakfast, lunch and dinner and at bedtime. Course - 4-8 weeks. , repeated after 8 weeks.
Start of action unknown
Duration of action unknown
If the medication is missed Take Bismuth as soon as you remember it. If it is shortly before the next dose, skip the previous one and go back to your regular schedule. Do not double the next dose.
Overdose
With the frequent use of large doses, the development of renal failure is possible. Contact your doctor. Treatment-gastric lavage, the appointment of activated charcoal and saline laxatives, symptomatic therapy.
special instructions
Long-term use of large doses of the drug is not recommended. Within 30 min. after taking, you should refrain from drinks, solid food, milk, antacids. Colors feces black.
Precautionary measures
Over 60 years old Special problems with the use of the drug are not expected.
Driving a car and operating machinery does not affect the ability to perform such work.
Alcohol alcohol intake is contraindicated.
Interaction with other drugs
Reduces the absorption of tetracycline. Simultaneous administration of drugs containing bismuth (vikalin, vikair, roter) increases the risk of systemic side effects (increases the concentration of the drug in the blood). Milk interferes with the absorption of the drug.
Domestic and foreign analogues
The main active ingredient is part of the drugs: Novobismol, De-Nol.
Price in pharmacies
The price of Bismuth in different pharmacies can vary significantly. This is due to the use of cheaper components and the pricing policy of the pharmacy chain.
Read the official information about the drug Bismuth, the instructions for use of which include general information and a treatment regimen. The text is provided for informational purposes only and is not a substitute for medical advice.
