Why are antacids prescribed in an hour. Features of the use of antacids: list and classification

Are medicines that neutralize hydrochloric acid, thereby reducing the acidity of gastric juice. These drugs remove pain and heartburn - the most common manifestations of diseases of the alimentary canal. For medicinal purposes, antacids have been used for over a century.

All agents are classified according to their chemical composition into water-soluble and water-insoluble. Medicines contain the following substances:

• sodium bicarbonate;
• calcium carbonate;
• aluminum hydroxide and phosphate;
• magnesium citrate, oxide, carbonate and hydroxide.

Substances soluble in water (sodium and calcium compounds), when combined with hydrochloric acid, act quickly, almost instantly, form a large amount of carbon dioxide, which stretches the stomach and stimulates the re-release of acid. This phenomenon is called ricochet syndrome. All drugs based on them are absorbable.

Sodium bicarbonate (baking soda) is especially "sinning" with this, funds based on it are completely absorbed and cause a systemic effect. If you take them for too long, then the acid-base balance of the internal media shifts to the acidic side (acidosis).

Compounds of magnesium and aluminum do not dissolve in water. Medicines based on them are non-absorbable, their action comes slowly. The funds act only in the intestinal lumen, they are not absorbed into the blood, but they can collect toxins on their surface. With an excess of magnesium salts, stool loosening occurs, aluminum - a blocking effect. Non-absorbable products can be taken for a long time, since they do not have ricochet syndrome. In addition, these agents adsorb pepsin, from which the production of hydrochloric acid is suppressed.

Modern antacids contain combinations of soluble and insoluble substances in different combinations, which allows you to change the time and quality of action. Also, the preparations contain additives that protect the gastric mucosa.

Antacids have the greatest effect when acidic gastric contents or backflow into the esophagus. This is practically the only remedy that allows such patients to prevent burns of the esophagus and improve the quality of life.

Absorbable antacids

You can use baking soda, but only once - when overeating, after consuming acidic foods, alcohol, occasionally in pregnant women. It is not suitable for systematic use, since with prolonged use it causes electrolyte disturbances and many complications - from edema and increased blood pressure to the formation of kidney stones.

Absorbable antacids should not be taken with milk. With prolonged use, this can lead to the formation of lactic-alkaline syndrome, which is manifested by nausea and vomiting, the release of large amounts of urine and a temporary increase in the concentration of nitrogen in the blood.

Non-absorbable antacids

Features of the use of antacids for various pathologies

The choice of an antacid agent is made by the doctor, based on the characteristics of a specific clinical picture. The use of this group of drugs has its own nuances for each disease.

Peptic ulcer

Non-absorbable antacids are used before use and on the first day after their appointment, while the size of ulcers should not exceed 1 cm. It is possible to use these drugs after removal for symptomatic treatment of heartburn, neutralize the "acid rebound" of some drugs, and also to prevent relapse. Almagel and its varieties have gained the greatest popularity for peptic ulcer disease.

Chronic and acute duodenitis, gastroduodenitis

Nonabsorbable antacids are used, but only as a complement to histamine blockers and proton pump inhibitors. Medicines help to suppress inflammation faster and prevent another exacerbation. When using NSAIDs, antacids are used as a protective agent. The most widely used in such a situation was the drug Talcid in the form of chewable tablets. The active ingredient is hydrotalcite, which has a crystalline layered-reticular structure, from which aluminum and magnesium ions are released in the stomach. For a long time and firmly binds hydrochloric acid, bile acids, stimulates the protective factors of the stomach.

After a single tablet dose, a sufficient concentration of anti-acid ions lasts up to 90 minutes. You can chew the tablets as needed, but not more than 12 per day.

Due to its sorbing effect, Talcid should be taken 1-2 hours before or after meals or other medications. It is advisable to continue taking the tablets for 4 weeks after the disappearance of all symptoms.

Recurrent stomach pains, heartburn of pregnant women

In cases where heartburn and other dyspeptic symptoms occur rarely and are caused by overeating, excessive consumption of coffee and other irritating substances, it is recommended to take absorbed antacids. The best drugs for this are Rennie, a mixture of Bourget, Tams, Andrews antacid.

Medicines are used in the "on demand" mode, their effect develops within 3-5 minutes, with episodic use, there are no side effects and complications.

Gastroesophageal reflux disease (GERD)

This is a constant reflux of gastric contents into the esophagus, in which its lower part is damaged.

This condition can occur in a healthy person with physical overstrain, stress, infections. However, if this occurs constantly, treatment is required.

Treatment for GERD is complex, but antacids should be taken regularly. International guidelines suggest using non-absorbable antacids in the following sequence: Phosphalugel → Maalox (Almagel) → Gaviscon (Topalkan).

The most effective in this case are antacids of the second generation or aluminum-magnesium: Maalox, Megalak, Almagel. The variety of trade names is due to marketing requirements, and the active ingredients are the same.

Contraindications

Only non-absorbable antacids have contraindications, and there are few of them.

Side effects

Absorbed antacids have practically no side effects, except for allergic reactions that occur during an overdose. After drug withdrawal or a significant dose reduction, these reactions stop.

The adverse effects of nonabsorbable drugs are extensive:

• constipation at high doses;
• nausea and vomiting (rare);
• a change in the taste of food;
• a significant increase in the level of magnesium in the serum, which, combined with a lack of phosphorus intake from food, can lead to softening of the bones (osteomalacia).

Such effects occur only with prolonged uncontrolled use in high doses. If you follow the dosage indicated in the instructions or be under the supervision of a doctor, then side effects can be avoided.

Natural antacids

With heartburn and it is important to establish nutrition, using natural products to extinguish acidity.

The best foods in this sense are milk and meat. A large amount of hydrochloric acid and pepsin is spent on their assimilation, and the duration of their presence in the stomach is several hours. To normalize acidity, it is useful to eat boiled or baked fish. Wheat bran works very well; in its structure, they resemble a sorbent.

Oatmeal works the same way, especially with raisins and fresh pineapple added. Any boiled porridge is useful, especially with milk.

During the season, it is advisable to eat as many watermelons and melons as possible, which are excellent at reducing acidity. At any time of the year, you need to eat as many starchy vegetables as possible - potatoes, bell peppers, cabbage, carrots, zucchini, legumes, which are best boiled.

E.A. Ushkalova
Moscow

Antacids are among the effective drugs for the treatment of acid-related diseases (peptic ulcer, gastroesophageal reflux disease). The mechanisms of action and the main pharmacological properties of antacids are considered, their classification is presented, and the characteristics of monocomponent drugs of this group are given. Data on combined and mixed preparations of antacids are given. The clinical pharmacology of the combined antacid Maalox is discussed. It is emphasized that Maalox is a modern effective and safe antacid drug that has a complex effect - acid-neutralizing, cytoprotective, enveloping, adsorbing (adsorbs bile acids, lysolecithin, pepsin); stimulates repair, and also increases the effectiveness of anti-Helicobacter therapy.

Acid-related diseases occupy a leading place in the morbidity structure. In particular, peptic ulcer (PU) of the stomach and duodenum (Duodenum) in Western Europe affects an average of 8.2% of the population, in the United States - from 7 to 10%, in Japan - 11%, in India - 25%. In Russia, according to official statistics, the proportion of patients with newly diagnosed duodenal ulcer in recent years has increased from 18 to 26%, and about 3 million people are under dispensary supervision with this diagnosis. Symptoms of gastroesophageal reflux disease (GERD) are found in half of the world's adult population, and endoscopic signs are found in 2-10% of the examined individuals.

Along with the “classic” acid-dependent diseases caused by excessive production of hydrochloric acid in the stomach, mediated and symptomatic disorders of the gastrointestinal tract (GIT; Table 1) are widespread. Complaints about dyspeptic (dyspeptic) phenomena are presented by 30-40% of the population of industrially developed countries. For example, in the United States, 25 million adults experience heartburn every day, and more than 50 million people experience heartburn twice a week. Dyspeptic symptoms are the cause of 5% of visits to general medical practitioners and 40-50% of visits to gastroenterologists.

Table 1. Acid-dependent diseases

The first pharmacological agents that began to be used for the treatment of acid-related diseases several centuries ago were antacids. They remained the main drugs for the treatment of these diseases almost until the middle of the 20th century, but then they were largely "supplanted" by drugs of new pharmacological groups, primarily by blockers of H2-histamine receptors and proton pump inhibitors. However, even today, antacids continue to be widely used drugs. This is evidenced by the number of drugs in this group on the pharmaceutical market (more than 30 trade names are registered in Russia) and the volume of their sales. For example, in 2003, the volume of pharmacy sales of antacids in Russia amounted to USD 25.2 million in wholesale prices and increased by 14% in comparison with 2002. In the United States, approximately 6 million people use antacids to prevent gastrointestinal side effects of drugs for treating arthritis.

The advantages of antacids over drugs of other pharmacological groups used to treat acid-related diseases is the rapid relief of pain and dyspepsia. Modern antacids also have a number of other beneficial properties, for example, adsorbent and cytoprotective, the ability to correct intestinal motility, improve the quality of ulcer scarring, etc.

Currently, antacids are used mainly in the following situations:

• to relieve symptoms of gastroduodenal ulcers, reflux esophagitis with self-medication;
• as a means of differential diagnosis ex juvantibus between cardiac and non-cardiac chest pain;
• as a means of differential diagnosis ex juvantibus of epigastric ulcerative and biliary pain;
• for relief of symptoms of ulcer, GERD, chronic pancreatitis in the first days of exacerbations before the appointment of standardized treatment;
• as a remedy taken by patients on demand for heartburn, ulcerative hunger pains, ulcerative dyspepsia, etc.

In recent years, antacids have again begun to attract the attention of gastroenterologists. In particular, in the works of ON Minushkin et al. it has been shown that they are very effective as agents for the treatment of peptic ulcer disease and, depending on the severity of the lesions, can be used in different patients both as monotherapy and as part of complex therapy. Researchers give a special place to antacids in pediatric practice, considering them as a means of basic therapy and prevention of acid-dependent gastrointestinal pathology in children. It should be emphasized that the conclusions of O.N. Minushkin. et al. based on an analysis of the use of modern aluminum / magnesium-containing antacids, primarily Maalox.

The pharmacological properties of a number of modern antacids allow us to consider them the drugs of choice for the treatment and prevention of reflux gastritis and can be successfully used for GERD and acid-dependent diseases occurring with impaired intestinal motility. However, in order to achieve favorable treatment outcomes, it is necessary to choose the right antacid drug, taking into account its pharmacological properties and the characteristics of a particular patient. The leading place in the treatment of acid-related diseases in adults and children belongs to one of the most widely used combined antacids in the world - Maalox.

Mechanism of action and main pharmacological properties of antacids

The mechanism of action of antacids is direct interaction with hydrochloric acid in the stomach, leading to its inactivation. Their main pharmacological properties are a decrease in the proteolytic properties of gastric juice, a decrease in the irritating effect of hydrochloric acid on the gastric mucosa, and an increase in the intragastric pH to 4.0–5.0. An increase in pH in the stomach is accompanied by a decrease in the activity of a number of proteolytic enzymes and a weakening of the action of aggressive factors. It also improves the tone of the lower esophageal sphincter, which is important in gastroesophageal reflux.

The strength of the action of antacids is determined by their acid-neutralizing activity (KNA), which is expressed in milliequivalents (the amount of 1N hydrochloric acid titrated to pH 3.5 with a certain dose of the drug for a specified time). KPA of different antacids varies widely. It is considered low if it is less than 200 meq / day; medium - in the range of 200-400 meq / day and high - more than 400 meq / day. An increase in KNA values \u200b\u200bover 600 meq / day does not lead to an increase in the antacid effect.

The rate of onset of the antacid effect is determined by the rate of dissolution of drugs. The rapid development of the buffering effect is characteristic primarily of sodium bicarbonate, calcium carbonate, and magnesium hydroxide, which dissolves quite easily in the stomach. The speed and duration of action of monocomponent antacids are presented in table. 2. The speed of the onset of the effect also depends on the dosage form: suspensions usually dissolve faster than solid dosage forms, and the duration of action of antacids is significantly influenced by the speed of their evacuation from the stomach, which is determined in turn by the presence or absence of food in the stomach. An antacid taken one hour after a meal lasts longer in the stomach and has the longest effect.

Table 2. The rate of onset and duration of action of monocomponent antacids

Classification of antacids and general characteristics of monocomponent drugs

The classification of antacids is based on their ability to absorb. Absorbed antacids can have systemic effects, non-absorbable - they act mainly in the gastrointestinal tract. It should be noted that this subdivision of antacids is relatively arbitrary and based on the degree of absorption, therefore, some drugs (for example, calcium carbonate and magnesium oxide) are included by different authors in different groups.

Sodium bicarbonate (sodium bicarbonate, baking soda) is certainly a well-absorbed antacid in the gastrointestinal tract. Usually, precipitated calcium carbonate is also referred to the group of absorbed antacids, which is absorbed by about 10%, and therefore, when using it, there is a rather high risk of developing systemic effects.

The most attractive property of sodium bicarbonate is its rapid onset of effect, but the duration of action of the drug is very short. Within 15–20 minutes, it leads to an increase in intragastric pH to 7 and above, which causes the development of a rebound syndrome with a secondary increase in the secretion of hydrochloric acid. An increase in acid secretion is also facilitated by the release of carbon dioxide during the neutralization reaction, which stretches the walls of the stomach and causes pain. In patients with a deep ulcerative defect, stretching of the stomach walls is fraught with perforation. Carbon dioxide also causes belching and flatulence, side effects that are especially undesirable for GERD patients.

The systemic effect of sodium bicarbonate can be manifested by the development of alkalosis, the clinical signs of which are weakness, headache, impaired appetite, nausea, vomiting, abdominal pain, muscle cramps and cramps. The risk of alkalosis is especially high in patients with impaired renal function. Against the background of alkalosis, hypokalemia may develop. In addition, sodium bicarbonate alkalizes urine and promotes the formation of phosphate stones. It also has a negative effect on water and electrolyte metabolism: 2 g of bicarbonate retains the same amount of fluid in the body as 1.5 g of sodium chloride, and therefore, in elderly patients with cardiovascular pathology, its use may increase blood pressure. increased edema and increased signs of heart failure.

Calcium bicarbonate reacts with hydrochloric acid more slowly than sodium bicarbonate. As a result of the interaction, carbon dioxide is also released. In addition, calcium ions have a direct stimulating effect on gastrin secretion by cells of the gastric mucosa and, as a result, stimulate the secondary secretion of hydrochloric acid to an even greater extent than sodium bicarbonate. With prolonged use, approximately 10% of the calcium bicarbonate taken is absorbed, which can lead to the development of hypercalcemia, especially in patients with impaired renal function. With prolonged use of calcium bicarbonate, constipation and the formation of kidney stones are possible. Hypercalcemia also inhibits the production of parathyroid hormone, causing a delay in phosphorus excretion and the accumulation of calcium phosphate, which in turn leads to tissue calcification and the development of nephrocalcinosis. When using calcium bicarbonate, alkalosis can develop. The combined intake of calcium-containing antacids with milk contributes to the development of "lactic-alkaline" syndrome, the signs of which are hypercalcemia, transient azotemia, nausea, vomiting, polyuria and mental disorders.

Along with monocomponent drugs, absorbed antacids include:

• a mixture of Bourget (sodium sulfate, sodium phosphate, sodium bicarbonate);
• rennie's mixture (calcium carbonate + magnesium carbonate);
• tams mixture (calcium carbonate + magnesium carbonate).

Due to the large number of side effects, absorbed antacids have practically lost their clinical significance and are used by the population mainly for self-medication.

The group of nonabsorbable antacids includes primarily aluminum and magnesium preparations. The main mechanism of action of non-absorbable antacids is associated with the adsorption of hydrochloric acid, so their effect develops more slowly than that of absorbed drugs, but lasts longer - 2.5-3 hours. They are superior to absorbed antacids and in terms of buffer (neutralizing) capacity. Non-absorbable antacids have additional beneficial properties:

• they can adsorb pepsin, helping to reduce the proteolytic activity of gastric juice;
• bind lysolecithin and bile acids, which have a damaging effect on the gastric mucosa;
• have an enveloping effect.

The results of numerous studies indicate that non-absorbable antacids have a cytoprotective effect associated with an increase in the content of prostaglandins in the gastric mucosa, stimulation of the secretion of bicarbonates, and an increase in the production of glycoproteins in gastric mucus. They are able to protect the endothelium of the capillaries of the submucosa from the damaging action of ulcerogenic substances, improve the processes of regeneration of epithelial cells and stimulate the development of the microvasculature of the gastric mucosa.

When using aluminum-containing products, be aware of the potential danger of serious side effects. In the small intestine, they can form insoluble aluminum phosphate salts, leading to impaired absorption of phosphates and the development of hypophosphatemia, manifested by malaise and muscle weakness. Severe phosphate deficiency causes osteomalacia and osteoporosis. Hypophosphatemia promotes increased calcium absorption, the development of hypercalcemia, hypercalciuria and the formation of calcium stones.

Long-term use of aluminum-containing antacids and / or their use in high doses can cause intoxication, accompanied by damage to bone tissue, brain and the development of nephropathy. It is assumed that aluminum directly violates the mineralization of bone tissue, has a toxic effect on osteoblasts, affects the function of the parathyroid glands and inhibits the synthesis of the active metabolite of vitamin D3 - 1,25-dihydrooxycholecalciferol. The accumulation of aluminum in the membranes of the glomeruli of the kidneys can cause the development of renal failure or its aggravation.

The most severe complication of aluminum-containing drugs is Alzheimer's encephalopathy. Severe side effects can be irreversible, especially in children, especially newborns, and the elderly. The risk of serious side effects arises when the concentration of aluminum in the blood is more than 100 μg / ml.

A number of magnesium compounds have pronounced antacid properties. The highest KNA is characteristic of magnesium oxide and magnesium hydroxide. Magnesium-containing antacids do not cause secondary hypersecretion of gastric juice and do not disturb the acid-base balance. Magnesium ions increase the secretion of cholecystokinin, which stimulates intestinal peristalsis, and increases the osmotic pressure in its lumen, therefore, all magnesium-containing antacids have a laxative effect. In patients with renal failure, with their use, the development of nephrological and cardiovascular disorders is possible.

Bismuth preparations (colloidal bismuth subcitrate, bismuth subnitrate, etc.) and the aluminum salt of sucrose octasulfate (sucralfate) also have weak antacid properties. Colloidal bismuth subcitrate and sucralfate are used as enveloping agents, and bismuth subnitrate is part of mixed antacid preparations (see below).

Combined and mixed preparations of antacids

Currently, the most widely used are combined antacid preparations containing two or more active ingredients. Rational fixed combinations of antacids can vary the rate of onset of the therapeutic effect and the duration of action, as well as reduce the number of side effects and improve tolerance.

Along with combined antacids, mixed preparations are isolated, which additionally contain bismuth salts and plant substances. Bismuth subnitrate, or basic nitrate, has an astringent and antibacterial effect; chamomile and fennel - antiseptic and anti-inflammatory; licorice - gastroprotective; rutin and kellin - anti-inflammatory (kellin also has antispasmodic properties); buckthorn bark powder - laxative; calamus rhizome powder improves digestion. Currently, drugs in this group have largely yielded to combined antacids, but sometimes they are used in combination.

Clinical Pharmacology of Maalox

The most widely used are combined antacid preparations containing aluminum and magnesium hydroxide. Maalox is one of the most well balanced combinations. It is one of the most well-studied and commonly used antacids worldwide and in Russia.

Maalox meets all the requirements for modern antacids. The optimal ratio of aluminum and magnesium hydroxides (0.9 in suspension and 1.0 in tablets) provides a complementary effect of the components of the drug, which determines a quick and long-lasting antacid effect and a slight laxative effect. Maalox not only actively neutralizes hydrochloric acid (Table 3), but is also able to adsorb it. The first contributes to the speed of onset of the antacid effect, the second - to increase its duration. After a single injection of Maalox, pH 4.5 in the stomach is maintained for at least 3 hours. The buffering action of the drug ensures the achievement of an intragastric pH of 3.0-5.0, which allows not only to prevent the undesirable consequences of a higher increase in pH (secondary hypersecretion), but also to use it in acid-dependent diseases in combination with antisecretory drugs, significantly accelerating the relief of pain and dyspeptic disorders.

Table 3. Acid-neutralizing activity of some commercial antacid preparations

Maalox possesses moderate pepsinoadsorbing activity, which, on the one hand, enhances its therapeutic effect, and on the other hand, does not “turn off” the stomach from the hydrolysis of chyme components. It also adsorbs bile acids and lysolecithin, which prevents peptic damage to the mucous membrane of the stomach and esophagus in patients with duodenogastric and duodenogastroesophageal reflux and in case of nonsynchronous ingestion of chyme, bile and pancreatic secretions in the duodenum in patients who have undergone endoscopic papilloscystectomy or cholecystectomy. These properties of the drug are useful for patients with chronic recurrent pancreatitis resulting from bilio- or duodenopancreatic reflux, since bile acids that have entered the pancreatic duct are involved in intrapancreatic activation of trypsinogen, and lysolecithin has a pronounced pancreatotoxic effect.

Maalox has a cytoprotective effect due to an increase in the synthesis of prostaglandin E2. It also stimulates the secretion of bicarbonates and protective mucopolysaccharide mucus, improves microcirculation. Thus, the drug increases the resistance of the gastric mucosa and duodenum to the action of various ulcerogenic factors, including non-steroidal anti-inflammatory drugs.

Maalox has the ability to bind epithelial growth factor and fix it in the zone of the ulcer, thereby stimulating local reparative-regenerative processes, cell proliferation and angiogenesis. A scar formed at the site of the former ulcer, when using Maalox, has better histological characteristics than when using omeprazole:

• absence of erosive changes in the periulcerous zone and the scar itself,
• an increase in the thickness of the stomach wall in the scarring area,
• reduction of glandular dilatation,
• normalization of differentiation of glandular cells,
• the development of the capillary network in the submucosa.

Maalox inhibits the multiplication of Helicobacter pylori in the gastric mucosa and reduces its urease activity.

Unlike antacids containing calcium, magnesium or sodium carbonates, Maalox does not contribute to gas formation and the occurrence of flatulence, belching. Unlike antacids containing calcium carbonate, it does not worsen steatorrhea in patients with pancreatitis.

Maalox does not contain sodium and does not increase the volume of circulating blood, and therefore it can be prescribed to patients with concomitant hypertension, circulatory failure and portal hypertension.

Unlike a number of other antacids, Maalox does not significantly affect the electrolyte composition and pH of urine and does not contribute to the occurrence of urolithiasis. Unlike preparations containing calcium carbonate, it does not cause hypercalcemia and a decrease in parathyroid hormone production. Unlike preparations containing bismuth salts, Maalox does not cause discoloration of feces and does not mask melena.

Maalox is well tolerated by patients of all ages, including the elderly and children. Its main side effect is a mild laxative effect, which usually does not necessitate discontinuation of the drug. The accumulation of aluminum and magnesium in the body when using Maalox is possible only in patients with renal failure.

The presence of Maalox dosage forms with different KNA allows you to select the form and dose of the drug, regulating its daily KNA from low to medium and high, depending on the level of gastric secretion of the patient. The Maalox suspension has additional enveloping properties. When using a solid dosage form of the drug, its effect can be prolonged if the tablets are chewed and kept in the mouth until they are completely absorbed.

Maalox has good organoleptic properties to enhance patient adherence to treatment, especially in pediatrics. It does not require special storage conditions and remains stable for a long time.

The effectiveness of Maalox in acid-dependent diseases (gastric ulcer and duodenal ulcer, gastroduodenitis, GERD) has been proven in numerous studies. In particular, they show that the incidence of scarring of gastroduodenal ulcers when using Maalox is 75%.

Maalox can be used for the treatment of ulcer not associated with Helicobacter pylori. This is due to both its high KNA and cytoprotective properties. The drug contributes not only to ulcer scarring, but also to the restoration of the functional activity of the mucous membrane of the stomach and duodenum, supplementing, and often correcting the effects of antisecretory drugs.

Analysis of the results of treatment of 250 patients (average age - 36.5 years) with YB Maalox, conducted by ON Minushkin. et al., allowed the authors to recommend it:

• 1) in the form of monotherapy - for patients with an uncomplicated course of an ulcer, a short ulcer history and an ulcer defect not exceeding 1.0 cm;
• 2) as part of complex therapy (as cytoprotective agents and to reduce doses of antisecretory drugs) - for patients with a long history, complicated course and ulcerative defect exceeding 1.0 cm.

The analysis included patients with ulcer sizes from 0.5 to 1.7 cm with a rare, moderate and often recurrent course of the disease. Maalox was used in the form of a suspension and tablets in medium therapeutic doses, endoscopic control of the treatment was carried out after 2, 4, 6 weeks. Ulcer healing was accompanied by a decrease in inflammation in 2/3 of patients. The treatment was well tolerated, practically without causing side effects (except for the relief observed in 0.5% of patients and did not require a change in therapy).

Maalox has been shown to be highly effective in GERD. The use of the drug not only led to the disappearance of clinical symptoms, but was also accompanied by positive dynamics of the morphological substrate of the disease, which is associated with its protective effect on the mucous membrane. In a number of studies, Maalox was not inferior in efficiency to H2-blockers. The good tolerance of Maalox, noted in all studies, should also be emphasized. The efficacy and safety allow Maalox to be recommended as monotherapy for patients with stages I and II of GERD, especially for elderly patients and children.

Maalox, along with other antacids that bind bile acids and lysolecithin, should be considered as the drug of choice for the prevention and treatment of reflux gastritis. Recently, data have appeared indicating the participation of bile acids in the formation of Barrett's esophagus, therefore, antacids that bind bile acids may be the drugs of choice in this category of patients.

The expediency of using Maalox in functional dyspepsia as both an antacid and a means that indirectly accelerates the opening of the pylorus sphincter, evacuation of the chyme from the stomach, and a decrease in pressure in the stomach and duodenum has been substantiated. The stimulating effect of Maalox on intestinal motility determines its beneficial effect in the pathology of the gastrointestinal tract, accompanied by constipation, including in irritable bowel syndrome.

The use of Maalox in exacerbation of chronic recurrent pancreatitis is due to both its direct (see above) and indirect action - the "protection" of enzyme preparations from inactivation by acid in the stomach. It is especially advisable to use Maalox in patients with chronic pancreatitis with severe exocrine pancreatic insufficiency, low gastric secretion and intestinal dysbiosis. In these situations, more powerful antisecretory drugs can aggravate the clinical course of the underlying disease.

The combination of efficacy and safety makes Maalox of great importance in the prevention and treatment of acid-related diseases in children. It was confirmed by an analysis of the results of treatment with combined aluminum / magnesium-containing antacids, including Maalox, 433 children aged 6 to 15 years with erosive gastritis, duodenitis, reflux esophagitis and ulcer.

Thus, Maalox is a modern, effective and safe antacid drug that has a complex effect - acid-neutralizing, cytoprotective, enveloping, adsorbing (adsorbs bile acids, lysolecithin, pepsin); stimulates reparation, and also increases the effectiveness of anti-Helicobacter pylori therapy. All this allows it to be successfully used for various acid-related diseases in patients of different ages.

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The possibility of a quick therapeutic effect, primarily in the elimination (reduction of intensity) of heartburn and pain, after taking antacids per os has long attracted the attention of doctors and researchers. This quality of antacid drugs compares favorably with drugs of other classes, including H 2 -blockers of histamine receptors and proton pump inhibitors, the use of which in the treatment of patients can significantly reduce acid production in the stomach, however, the effect of their action occurs somewhat later, and the financial cost is much higher ...

The main point of application of antacids is the neutralization of hydrochloric acid secreted by the parietal cells of the gastric mucosa. According to the observations of some researchers, when taking antacids in usual therapeutic dosages, the acidity level is no more than 5 (drugs neutralize only excess acidity of gastric juice), however, when the acidity level decreases to 1.3-2.3, these drugs neutralize 90% of the gastric juice, and with a value of 3.3 - 99% of gastric juice.

Antacids have been used for a long time in the treatment of patients suffering from various gastroenterological diseases, primarily acid-dependent diseases. Currently, a large group of diseases of the upper gastrointestinal tract is classified as acid-dependent, regardless of whether the factor of acid aggression is central or only additional, leading to the onset and progression of these disorders. Among acid-related diseases, the most common are gastric ulcer and duodenal ulcer, gastroesophageal reflux disease (GERD), non-ulcer (functional, essential) dyspepsia (NDF), pancreatitis, ulcers associated with non-steroidal anti-inflammatory drugs. Some researchers also refer to acid-related diseases as ulcers that can occur with hyperthyroidism. In our opinion, these disorders can also include an idiopathic hypersecretory state, peptic ulcers of gastroenteroanastomosis that occur in some patients after resection of the stomach, and, to some extent, Cushing's ulcers, as well as ulcers that appear with celiac enteropathy.

In the treatment of patients suffering from acid-related diseases, various antacids are used, which differ to a greater or lesser extent from each other, primarily in composition, speed of onset of the therapeutic effect, duration and effectiveness of the action. These qualities of drugs to some extent depend on their form (tablet, gel, suspension). However, most modern antacids have something in common - a decrease in the concentration of hydrogen ions in the stomach, resulting from the neutralization of hydrochloric acid; in addition, the neutralizing effect causes a decrease in peptic activity. In addition, in the stomach, antacids bind bile acids and lezolecithin, providing an enveloping effect. Some of the antacid preparations (in particular, those containing aluminum hydroxide) also have a cytoprotective effect, which consists in increasing the secretion of mucus and the synthesis of prostaglandins. It was also found that antacids are able to bind epithelial growth factor and fix it in the area of \u200b\u200bthe ulcer, stimulating cell proliferation, angiogenesis and tissue regeneration.

Taking into account the antagonistic effect of intravenously injected magnesium into the stomach on the hypersecretion of acid caused by calcium carbonate, agents containing a mixture of calcium carbonate and magnesium oxide hydrate have been created. However, these antacids do not reverse the stimulatory effect of calcium carbonate on gastric acid secretion. In addition, antacids containing calcium carbonate, when interacting in the stomach with hydrochloric acid, cause the formation of a significant amount of carbon dioxide, which leads to the appearance or intensification of flatulence, and in the presence of cardia insufficiency, including combined with a hiatal hernia, - belching.

The stimulating effect of some antacids on gastric acid secretion is partially associated with alkalization of the antrum, release of gastrin and possibly other neurohormonal factors, and partly with the direct effect of these antacids on parietal cells of the gastric mucosa.

Several attempts have been made to somehow classify antacids (absorbed and non-absorbable, local and systemic action, anionic and cationic, combined and monocomponent). The most common are absorbable and non-absorbable antacids. The absorbable group usually includes such drugs as sodium bicarbonate (soda), magnesium calcium carbonate basic - a mixture of Mg (OH) 2, 4MgCO 3, H 2 O, magnesium oxide (burnt magnesia), basic calcium carbonate - CaCO 3, Bourget mixture (Na sulphate, Na phosphate and Na bicarbonate), Rennie's mixture (calcium carbonate and magnesium carbonate), Tams' mixture (calcium carbonate and magnesium carbonate). These antacid drugs are characterized by the relative speed of the onset of the therapeutic effect (the disadvantage is the short duration of the neutralization of hydrochloric acid). Usually, these drugs, exerting a systemic effect, increase the alkaline reserves of plasma, changing the acid-base balance, and neutralize (with local action) hydrochloric acid in the stomach, which in some cases can lead to the syndrome of "acid rebound" due to the persistent appearance of acid hypersecretion in the stomach after taking such antacids. In particular, these antacid drugs include calcium carbonate, which soon after ingestion begins to stimulate the secretion of acid in the stomach - accelerated neutralization of hydrochloric acid in the stomach, activates the enhancement of its secretion by parietal cells of the gastric mucosa. In this regard, calcium carbonate is currently very rarely used in the treatment of patients.

The group of nonabsorbable antacids most often includes such drugs as phosphalugel (aluminum salt of phosphoric acid), the so-called aluminum-magnesium antacids (maalox, almagel neo, talcid, protab, magalfil, etc.) and aluminum-magnesium antacids with the addition of alginata (topalkan). A common feature of the primary action of this group of drugs (when it enters the stomach) is the adsorbing effect on hydrochloric acid, followed by its neutralization. Unlike absorbed antacids, nonabsorbable antacids have a longer antisecretory (neutralizing) effect (up to 2-3 hours), do not cause changes in acid-base balance and do not lead to an increase in the pH of gastric contents above neutral, without causing the syndrome of "acid ricochet ".

Modern antacids differ among themselves and in the composition of cations (magnesium, calcium, aluminum), which largely determines their main properties (neutralizing, adsorbing, enveloping, astringent and cytoprotective effect).

Unlike monocomponent antacids, combined antacids are composed of several constituent components and have different properties, depending on the composition. Sometimes aluminum-containing preparations are isolated (phosphalugel, maalox, almagel, gelusil lacquer, talcid, etc.), one of the essential advantages of which, along with neutralizing hydrochloric acid in the lumen of the stomach, is the protection of the mucous membrane of the esophagus and stomach from the action of the acid-peptic factor. Combined antacid preparations, especially those containing aluminum, have different mechanisms of action, including a combination that neutralizes hydrochloric acid and increases the protective properties of the mucous membrane, i.e., apparently also having a cytoprotective effect.

When assessing the effectiveness of antacid drugs, their acid-neutralizing ability and duration of action are most often taken into account. This fact is very important: the duration of the antacid effect is one of the main factors in assessing the therapeutic efficacy of antacid drugs used in the treatment of patients. It is known that antacids, due to their ability to be adsorbed on the gastric mucosa, cause a persistent acid-neutralizing effect, allowing them to exhibit buffering properties at 2.4 pH.

The acid-neutralizing activity of different antacids ranges from less than 20 mmol / 15 ml of the antacid preparation to 100 mmol / 15 ml. The acid-neutralizing ability (activity) of antacid drugs is usually understood as the amount of a particular antacid drug in grams or mmol / l required to reach a pH level of 50 ml of 0.1N hydrochloric acid solution to 3.5.

The shortest duration of action among antacid drugs is possessed by agents associated with the calcium carbonate group, somewhat longer with the magnesium group, even longer with the phosphorus group (up to 90 minutes). There are other data on the duration of action of antacid preparations, in particular, containing aluminum phosphate, which have an antacid effect due to their absorption on the gastric mucosa, which lengthens the duration of their buffering capacity at pH \u003d 2.4 to 120 minutes.

According to a number of researchers, combinations of aluminum and magnesium hydroxides, as well as calcium and magnesium carbonates, basically show only neutralizing activity, including the accelerated passage of food through the stomach. The study of the properties of some antacid drugs, according to the data of intragastric computer pH-metry, using a 3-electrode pH probe showed that the shortest time from the start of the administration of the antacid drug to an increase in pH (on average 8.9 minutes) was found in Maalox, the longest time - Almagel (on average 13.5 minutes) compared to Remagel, Phosphalugel, Megalak; the average duration of the alkalizing effect (alkaline time - from the beginning of the increase in pH to the return to the initial level) for antacids ranged from 28 minutes for Almagel to 56 minutes for Maalox. At the same time, remagel, phosphalugel and megalak occupied an intermediate position between almagel and maalox. Analysis of the pH-grams showed that the maximum pH values \u200b\u200bafter taking various antacids did not differ significantly.

Antacid therapy

Antacids can be successfully used in drug therapy for all acid-related diseases in the following cases: 1) as monotherapy in the initial stages of these diseases; 2) as additional agents (for example, in the treatment of patients with histamine H2-receptor blockers or prokinetics); 3) as symptomatic means to eliminate (reduce the intensity) of heartburn and pain behind the breastbone and / or in the epigastric region, both during the treatment of patients, combining their intake with other drugs, and during remission (including as therapy " on demand"); 4) during the screening phase before the start of the proposed treatment, when selecting patients for randomized studies to study the efficacy and safety of certain medications or regimens for their use (as a rule, taking antacids is allowed according to the protocols of these studies), as well as directly during the time of such studies as an emergency therapy in cases where the efficacy and safety of prokinetics, H 2 -blockers of histamine receptors, proton pump inhibitors or so-called cytoprotective drugs are studied.

In such cases, the undoubted advantage of antacid drugs is taken into account - the rapid elimination (decrease in intensity) of heartburn (burning) behind the breastbone and / or in the epigastric region and other gastrointestinal symptoms caused by the disease itself, about which patients are being treated, taking medications and intoxication ...

One of the antacids that periodically attracts the attention of researchers and doctors is phosphalugel (colloidal aluminum phosphate in the form of a gel for oral administration, containing 8.8 g in one sachet). Phosphalugel is often referred to as a group of nonabsorbable antacids. Most of the aluminum phosphate gel is insoluble, however, at pH less than 2.5, the phosphalugel transforms into water-soluble ammonium chloride, part of which is capable of dissolving, after which further dissolution of aluminum phosphate is suspended. A gradual decrease in the level of acidity of gastric contents to pH 3.0 does not lead to the occurrence of "acid rebound": the use of phosphalugel in the treatment of patients does not entail the appearance of secondary hypersecretion of hydrochloric acid.

One of the advantages of phosphalugel is its acid-neutralizing ability depends on the level of acidity: the higher the acidity, the more active the effect of this drug. An increase in pH under the action of the drug leads to a decrease in the proteolytic activity of pepsin. The drug does not cause alkalization of gastric juice, does not limit enzymatic processes and does not violate the physiological conditions of the digestion process. Long-term administration of the drug does not affect the metabolism of phosphorus. The actual effect of phosphalugel, which is in the form of hydrophilic colloidal micelles of the drug, is determined by colloidal aluminum phosphate, which has an antacid, enveloping and adsorbing effect. An insignificant part of phosphalugel precipitates in the intestine in the form of oxides and insoluble carbonates, which enhances its protective, adsorbing and antacid effect. One gram of aluminum phosphate gel micelles, consisting of aluminum phosphate, agar gel and pectin, has a contact surface of about 1000 m2, which provides an intensive connection with the walls of the digestive tract and adsorption of harmful substances. The pectin and agar gels, which are part of the preparation, participate in the formation of a mucoid, antipeptic protective layer in the gastrointestinal tract. Colloidal aluminum phosphate binds endogenous and exogenous toxins, bacteria, viruses, gases formed as a result of putrefaction and pathological fermentation throughout the gastrointestinal tract, normalizing their passage through the intestines and thereby facilitating their excretion from the body of patients. Under the action of the drug, pain is also weakened. Adults and children over 6 years old are usually prescribed 1-2 sachets 2-3 times a day immediately after meals and at night (with reflux esophagitis) or more often (with other diseases) - 1-2 hours after meals.

One of the antacids that has recently also attracted the attention of doctors is hydrotalcite (rutacid, talcid), a drug with a low content of aluminum and magnesium. Among the features of the mechanism of action of this drug is the gradual release of aluminum and magnesium ions, depending on the state of pH of the gastric contents. Other advantages of hydrotalcite are fast and long-term neutralization of hydrochloric acid while maintaining pH close to normal, protective effect on the gastric mucosa with a decrease in the proteolytic activity of pepsin, binding of bile acids, as well as the form of release of the drug - in the form of chewable tablets, which should be thoroughly chewed ... When treating adult patients, hydrotalcite is usually prescribed at 500-1000 mg (1-2 tablets) 3-4 times a day 1 hour after meals and before bedtime; after errors in the diet, accompanied by the appearance of symptoms of discomfort, as well as with alcohol abuse - 1-2 tablets once. For children aged 6-12 years, the dosage is reduced by 2 times. The duration of treatment is determined by the general condition of the patients. It is not recommended to take this drug at the same time as drinking acidic drinks (juices, wine).

It is known that along with dyspeptic disorders, usually associated with various diseases of the esophagus and stomach, a significant part of patients are worried about flatulence arising for various reasons, including in patients, according to our observations, who have been taking proton pump inhibitors for a long time. The appearance on the domestic market of Russia of a new antacid water-soluble preparation Almagel neo, containing in its composition the optimal amount of aluminum hydroxide and magnesium hydroxide (in comparison with the previously well-known suspension of Almagel, the content of the latter is increased by 3.9 times) and simethicone (antifoam) introduced into its composition , allows patients with preserved and increased gastric secretion to obtain a positive effect in eliminating symptoms of discomfort, including flatulence, in a short time (on average, on the fifth to seventh day); only in cases of severe symptoms of flatulence, treatment of patients with neo Almagel should be started with the use of 60 ml / day. The effectiveness of this drug is due to its high acid-neutralizing ability, the presence in its composition of simethicone (a surfactant that reduces the external tension of gas bubbles), which promotes the natural release of intestinal gases and their absorption, which to a certain extent prevents the appearance of stool retention (constipation) and flatulence , reduces the likelihood of belching. The presence of neo-sorbitol in the composition of almagel makes it possible to use it in the treatment of patients who, along with one of the acid-dependent diseases, have diabetes mellitus. The usual dosages of the appointment of this drug to patients: inside for adults 1 sachet or 2 dosing spoons 4 times / day 1 hour after meals and at night; for children over 10 years old, the dosage of the drug is determined by the attending physician (taking into account the body weight and condition of the child).

There are various options for prescribing antacids to patients for different diseases, but most often antacids are prescribed in the following cases: with the so-called "on demand" therapy for the rapid elimination (decrease in intensity) of dyspeptic symptoms, especially heartburn and pain (at any time of the day) ; in the course of treatment 30-40 minutes before or 30-60 minutes after a meal (if necessary and before bedtime) in the form of monotherapy or in complex treatment, in combination, first of all, with prokinetics and / or with H 2 -blockers of histamine receptors (the frequency and duration of taking antacid drugs are determined by the general condition of the patients). By itself, the positive effect of antacids in eliminating pain in the chest and / or in the epigastric region and / or heartburn (burning) indicates the presence of an acid-dependent disease in the patient. Most often, as observations show, antacids may be necessary in the treatment of patients suffering from peptic ulcer disease, chronic pancreatitis, GERD and / or NFD, which can both be combined with chronic hyperacid or normacid gastritis, and is possible in patients with NFD syndrome without morphological signs of gastritis.

As our observations have shown, it is more expedient to use antacids in the following cases. In case of peptic ulcer disease associated with Helicobacter pylori (HP), after eradication therapy in patients with pain and / or dyspeptic disorders, especially heartburn. However, due to the adsorbing ability of antacids, their use is not justified directly during the eradication therapy of Helicobacter pylori: during this period, patients take a lot of tablets or capsules - 6 times a day the basic drug (proton pump inhibitor, ranitidine or bismuth drug) in combination with 2 antibiotics (first-line therapy) or 4 drugs 13 times a day (second-line therapy), since the likelihood of a decrease in the effectiveness of both antibiotics and the basic (basic) drug (drugs) increases. Taking into account the number of drugs used by patients during the day and necessary to obtain an eradication effect, i.e., the destruction of Helicobacter pylori (HP), in the case of additional prescription of antacid drugs, the number of tablet forms of drugs will exceed the indicated number of drug doses (taking into account dosages), more than 6 and 13 times a day in first and second line therapy, respectively.

In case of peptic ulcer disease not associated with HP, antacids can be successfully used in the form of independent therapy for newly diagnosed, uncomplicated duodenal ulcer disease (with small ulcers), as well as as an additional therapy for gastric ulcer and duodenal ulcer to H 2-blockers of histamine receptors, either in therapy on demand or proton pump inhibitors. The success of treatment of patients largely depends on the depth of the ulcer.

When comparing the results of 4-week treatment of 2 groups of patients suffering from uncomplicated duodenal ulcer (one of the groups was treated with various antacid preparations in "liquid" form or in the form of tablets, 4-6 times a day, which had different neutralizing ability - from 120 to 595 mEq of H + anions per day, another group of patients was treated in therapeutic doses with H 2 -histamine receptor blockers), no significant differences were observed in the timing of the disappearance of clinical symptoms and ulcer healing. In another study, comparing the results of treatment of 42 patients treated with phosphalugel 11 g of aluminum phosphate gel 3 times a day (after meals) for 4 weeks, and treatment of 49 patients treated with ranitidine 150 mg 2 times a day, also for 4 weeks , showed the following: healing of duodenal ulcers was noted, respectively, in 60 and 55% of cases. According to another study, based on the analysis of the results of 6-week treatment of 153 patients who received aluminum phosphate (1 sachet \u003d 11 g of gel) 5 times a day, ulcer healing was found in 65% of cases.

Depending on the stage of the course in the treatment of GERD, antacids can be effectively used in the following cases: as the main drug in some patients with endoscopically negative GERD and in GERD in the stage of mild reflux esophagitis (with minimal symptoms); in combination with H 2 -blockers of histamine receptors in the course of treatment of patients with GERD in the stage of mild or moderate reflux esophagitis, as well as during therapy on demand; in the course of treatment of patients with GERD in the stage of erosive reflux esophagitis in combination with H 2 -blockers of histamine receptors, in therapy on demand in combination with constant treatment of patients with proton pump inhibitors (during an exacerbation of the disease); in the course of treatment of patients with GERD at the stage of peptic ulcer of the esophagus in combination with H 2 -blockers of histamine receptors or in therapy on demand (against the background of treatment of patients with proton pump inhibitors).

To improve the condition of patients, antacids should also be used in the treatment of patients suffering from other diseases: in particular, with erosive and ulcerative lesions of the stomach and duodenum associated with non-steroidal anti-inflammatory drugs, with erosive and ulcerative lesions of the upper gastrointestinal tract, the occurrence of which possibly with decompensated cirrhosis of the liver, with peptic ulcer disease, combined with celiac disease, and with Zollinger-Ellison syndrome.

In the course of treatment of patients with the listed diseases, it is advisable to use antacids during the course of therapy in combination with H 2 -blockers of histamine receptors (in therapy on demand and with proton pump inhibitors).

The use of antacids is useful, as shown by observations, and in the treatment of patients with acute gastritis (as an additional adsorbing agent in various variants of acute gastritis); as an additional therapy (to H 2 -blockers of histamine receptors or to proton pump inhibitors) for Cushing's ulcers; in the treatment of patients with peptic ulcers of gastroenteroanastomosis and patients with chronic pancreatitis. Antacids are used in combination with H 2 histamine receptor blockers or proton pump inhibitors as on-demand therapy.

It is advisable to use antacids in the treatment of patients with functional bowel diseases in order to eliminate pain and / or discomfort. It was shown that a single dose of aluminum phosphate gel with a volume of 100 to 300 ml, administered per os, just before taking a dose of radiostrontium 85Sr, reduced the absorption of the latter by 87.5%, while a dosage of 100 ml of aluminum phosphate gel was as effective as 300 ml, which indicates other possibilities of using antacids.

It is known that aluminum phosphate gel, which is a combination of an antacid and substances that cover and protect the mucous membrane from the pathological effects of acid and bile acids, helps to eliminate (reduce) their "irritating" (pathological) effect on the mucous membrane of the esophagus and stomach, which makes it possible to recommend a short-term use of this drug in pregnant women or during lactation after childbirth. The same advantages of phosphalugel (cytoprotective effect of the drug) protect the mucous membrane from damage and from the effects of alcohol.

As a symptomatic (additional) means to eliminate (reduce the intensity) of symptoms of dyspepsia, antacids can also be used in the treatment of patients with organic dyspepsia of various etiology (for example, before surgical treatment of patients, if necessary, and after it), as well as to eliminate symptoms of discomfort in people who consider themselves healthy.

Features of the appointment of antacids

When prescribing antacid drugs, it is necessary to take into account the mechanism (s) of their action and the symptoms of diseases observed in specific patients (constipation, diarrhea, etc.). In particular, in the presence of diarrhea (as additional funds, if necessary), it is advisable to treat patients with antacid preparations containing aluminum (almagel, phosphalugel, rutacid, talcid); for constipation - antacids, which include magnesium (gelusil varnish, gastal, etc.).

It is known that antacids (when they enter the body of patients) have an adsorbing ability, due to this, it is possible to reduce the activity and bioavailability of some medications taken by patients (for example, H 2 blockers of histamine receptors, non-steroidal anti-inflammatory drugs, antibiotics, etc.) ... Therefore, when prescribing antacids in combination with other drugs, it is advisable to recommend that patients observe the time interval between taking antacids and other drugs (before or after, about 2-2.5 hours), that is, indicate the time when patients take specific drugs during the day ...

According to our observations, the effect of taking antacids, produced in the form of gels or suspensions (compared to tablet forms), comes faster, although the tablet form seems to be somewhat more convenient for storage (especially when traveling).

When deciding on the use of antacids, especially long-term (in high dosages), it is necessary to take into account the possibility of side effects. Side effects, which are possible in some patients while taking antacid drugs, largely depend on the individual characteristics of patients, the dosage of antacid drugs and the duration of their use. Constipation or diarrhea (depending on the antacid drug used in the treatment of patients) are the most common side effects that occur in patients while taking antacid drugs. A significant increase in the dosage of antacids is the main cause of constipation or diarrhea, and prolonged, uncontrolled use is the appearance of metabolic disorders.

In particular, one of the features of the action of antacid preparations containing magnesium is an increase in the motor function of the intestines, which can lead to normalization of the stool, but if taken excessively, to the development of diarrhea. An overdose of antacid preparations containing magnesium (an increase in the patient's body of Mg +++ ions) contributes to an increase in the magnesium content in the patient's body, which can cause bradycardia and / or kidney failure.

In case of an overdose, antacids containing calcium cause an increase in Ca ++ in the patient's body (hypercalcemia), which can lead to the so-called "alkaline" syndrome in patients suffering from urolithiasis, which, in turn, increases the formation of calculi. A decrease in the production of parathyroid hormone can lead to a delay in the excretion of phosphorus, an increase in the content of insoluble calcium phosphate and, consequently, to calcification of the tissues of the patient's body and the occurrence of nephrocalcinosis.

The level of aluminum absorption can be different for different drugs, which must be taken into account when determining the possible risk of side effects due to the fact that antacids containing aluminum in some patients, especially with prolonged use, can cause hypophosphatemia, in renal failure - encephalopathy, osteomalacia (with an aluminum level of more than 3.7 μmol / l), clinical symptoms considered characteristic of poisoning (with an aluminum concentration of more than 7.4 μmol / l). It is necessary to take into account the fact that the lower toxicity of aluminum phosphate A1PO4, in comparison with aluminum hydroxide A1 (OH) 3, is due to its higher resistance to dissolution and the formation of neutral complexes in the presence of acids usually contained in food, which indicates a lower toxicity of phosphate aluminum.

As a rule, the appearance of side effects can be avoided if, when prescribing antacids, the mechanism of their action, the condition of specific patients are taken into account, and, in addition, if detailed explanatory work is carried out with patients before prescribing antacids.

For literature questions, please contact the editorial office.

Yu.V. Vasiliev, Doctor of Medical Sciences, Professor

Central Research Institute of Gastroenterology, Moscow

Antacids are medicines whose tasks include neutralizing hydrochloric acid in the stomach. The result of their use is manifested in a decrease in the irritating effect of gastric juice on the mucous membrane, elimination of pain in the stomach and the beginning of the recovery process.

The main advantage of antacids is:

• high speed of appearance of the effect of neutralizing hydrochloric acid (HCl);
• affordable cost;
• minimum side effects. Moreover, their appearance can be avoided if, when prescribing therapy, the mechanism of action of drugs and the condition of specific patients (allergic reactions, intolerance to components, weakened immunity) are taken into account;
• a wide range of dosage forms, allowing you to choose the appropriate option for any situation.

Among the disadvantages of antacids is the fact that their action, although quite effective, is not too long. Therefore, drugs are prescribed along with other drugs to reduce gastric secretion and motility.

Form of release of drugs

The most common forms of antacid release are tablets (regular and for resorption) and suspensions (for dissolving in sachets and ready-made in vials), each serving of which contains one dose of medication for an adult patient. Although a suspension is a more effective option due to the larger surface area of \u200b\u200bthe active substance, antacids in tablet form are most often used - primarily due to the possibility of taking them in public places.

Swallowing and chewing the tablets before swallowing helps better than the usual use of the medicine.

Indications for appointment

Doctors do not consider antacids to be the main remedy for stomach diseases. However, antacids are prescribed in such situations:

• at an early stage of acid-dependent disease (peptic ulcer, gastritis, gastroduodenitis);
• when prescribing therapy with antisecretory agents (H2-blockers) as the main drugs;
• with the appearance of severe heartburn and pain in the epigastric or retrosternal region.

They are used, although in combination with a number of other drugs, they are also used when the patient develops gastritis, reflux gastritis, functional dyspepsia, chronic diseases of the pancreas and Zollinger-Ellison syndrome. And some of the drugs, such as Maalox, are used to eliminate heartburn and belching.

Classification of drugs

Antacids are divided into two groups - absorbing and non-absorbing. The former provide the best and fastest effect, however, they act for a relatively short time (no more than half an hour), and the resulting carbon dioxide results in bloating and belching. Some suction antacids can dramatically increase the pressure in the bloodstream. However, due to side effects, they are rarely used.

The peculiarity of non-absorbable drugs is slow action. Although, at the same time, drugs have practically no side effects and retain their effect for up to 1.5 hours. They are also able to neutralize irritants without leading to an increase in HCl production. In addition, nonabsorbable antacids bind not only hydrochloric acid, but also a number of bile acids.

Absorbable medicines

Absorbable are antacids that can dissolve in the blood on their own (for antacids containing sodium) or by interacting with gastric juice (for calcium-containing drugs). As a result of a sharp decrease in acidity and a not too long duration of action, the appearance of the so-called "acid rebound" - acceleration of the production of HCl, is possible. When bicarbonates dissolve in the blood, systemic alkalosis (a violation of the acid-base balance, characterized by muscle tension and convulsions) is possible.

Long-term use of antacids, which contain calcium, can lead to hypercalcemia - and as a result, constipation, nausea, and excess urine production. If you use such drugs together with dairy products, it is possible that lactic-alkaline syndrome may appear, which is characterized by almost the same symptoms as an excess of calcium, and mental disorders added to them, loss of appetite and deposition of calcium salts in tissues.

Acidic ricochet

The name "acid rebound" is derived from the effect that occurs after the absorption-type antacids expire. The rapid increase in gastric alkalinity causes opposition from the body, which signals the stomach to increase the production of hydrochloric acid. As a result, the rate of formation of HCl can increase by up to 30% compared to the usual state.

Advice! Due to the increased production of acid, absorbable preparations with calcium as an active ingredient should not be taken at night.

In this case, the ricochet effect is not compensated for by food intake.

List of drugs

One of the major suction-type antacids is baking soda or sodium bicarbonate. Taking this agent reduces the HCl content, but after a while it leads to the formation of carbon dioxide and a short acid rebound. Another popular remedy that practically does not cause an acid ricochet is charred magnesia or magnesium oxide. Other drugs include:

• magnesium carbonate, which is part of such tablets as "Vikair" and "Vikalin";
• calcium carbonate (precipitated chalk), considered a good remedy for diarrhea;
• gafter mixture (active substance - calcium carbonate, additional - bismuth subnitrate and magnesium hydroxide);
• Rent, an antacid containing magnesium and calcium carbonates.

Non-absorbable drugs

Non-absorbable antacids are drugs whose effect on the body is determined by the presence in their composition of aluminum and magnesium hydroxides, aluminum phosphate and magnesium trisilicate. The duration of their effect reaches 3 hours, but it comes later than after taking absorbed antacids - as a rule, within an hour. During the entire period of action of non-absorbable antacids, they maintain the acidity of the stomach at 3-4 pH levels.

List of funds

Non-absorbable antacids are divided into several groups, according to their active ingredients:

1. Medicines, the main effect of which is achieved due to the content of aluminum phosphates. The most common drug in this group is Fosfalugel, whose neutralizing ability directly depends on the initial acidity value. The higher it is, the more effective the drug is. It should be noted that in this case there is no alkalization of the contents of the stomach and, accordingly, there are no "ricochets";
2. Magnesium and aluminum. The most commonly used and most effective means of this type is considered "Almagel". Its approximate counterparts in terms of efficiency and effectiveness are drugs such as "Maalox", "Gastracid" and "Gastala";
3. Combinations of active ingredients (the first is aluminum, magnesium and silicon, the second is sodium and calcium), the effectiveness of which is complemented by the inclusion of alginates in the drug. The combined action of antacids and alginic acid salts leads to the creation of a mechanical barrier that prevents gastric juice from entering the esophagus.

Features of drugs

The use of non-absorbable antacids is associated with several features. Thus, preparations with a high aluminum content are not recommended for pregnant women or nursing mothers. The main reason is the accumulation of this metal in the tissues of the fetus or infant, which causes developmental delays, increased bone fragility and neurological disorders. For the same reason, despite the almost complete absence of side effects in adult patients, one should not neglect the negative effect of nonabsorbable antacids on children.

Contraindications

Antacid drugs have no serious contraindications for adults - except for individual intolerance to individual components of the drug (depending on the specific drug). Among the few contraindications for antacids, kidney problems (such as renal failure) are also worth noting.

Taking antacids is not always contraindicated for children - most often the dose is simply halved. Although some of these drugs are not recommended for patients under the age of 14. Moreover, some of the antacids are prohibited for the treatment of children under 3 years of age.

Possibility of side effects

Long-term (for 2 weeks or more) therapy with antacids can lead to a number of adverse side effects, the specific symptoms of which depend on the type of drug and on the individual parameters of the body:

1. Medicines, the main active substance in which are magnesium salts, lead to an increase in the motor function of the intestines, and, as a result, to the appearance of diarrhea. And an overdose of such a drug causes hypermagnesia, and, as a result, renal failure;
2. In some patients, aluminum-containing preparations lead to a decrease in the level of phosphate in the body, as well as cause symptoms characteristic of poisoning - nausea, vomiting and heartburn;
3. Antacids with calcium as the main substance lead to hypercalcemia, and, in patients with urolithiasis, may increase the formation of kidney stones. An overdose of these drugs causes a delay in phosphorus excretion and increases the concentration in the body of calcium phosphate, a compound whose excess causes weakness, seizures, and loss of appetite.

Drug interactions

Taking antacids can weaken the medicinal effect of other drugs. For this reason, they should not be taken at intervals of less than 2 hours along with medications such as:

• benzodiazepines;
• non-steroidal anti-inflammatory drugs;
• antibiotics such as nitrofurantoin, tetracycline and metronidazole;
• anti-tuberculosis medicines (for example, isoniazid);
• H2 blockers;
• iron sulfates;
• phenytoin, digoxin, quinidine, and warfarin.

The use of antacids

Antacids are the best remedy for heartburn, which is a consequence of both pathologies and disorders in the diet. These same medications relieve other stomach problems by neutralizing hydrochloric acid and changing the pH of the stomach for 1 to 3 hours. It is heartburn in combination with belching that can become one of the main indications for the appointment of antacids. It is recommended to take them continuously (except in cases of side effects or allergic reactions to drug components) until the symptoms disappear completely.

This group includes agents that neutralize hydrochloric acid and reduce the acidity of gastric juice. These are anti-acid drugs. Usually these are chemical compounds with properties of weak bases, and they neutralize hydrochloric acid in the lumen of the stomach. Reducing acidity is of great therapeutic value, since the activity of pepsin and its digestive effect on the gastric mucosa depend on its amount. The optimum pH for pepsin activity is between 1.5 and 4.0. At pH \u003d 5.0, pepsin is inactive.

Therefore, it is desirable that antacids raise the pH to no higher than 4.0 (it is optimal that when antacids are taken, the pH of gastric juice is 3.0-3.5), which does not disrupt food digestion. Usually, however, the pH of gastric contents normally ranges from 1.5 to 2.0. The pain syndrome begins to subside when the pH rises above 2. In this sense, the role of antacids is twofold.

Distinguish between systemic and non-systemic antacids. Systemic antacids are agents that can be absorbed, and therefore not only give effects in the stomach, but can also lead to the development of alkalosis in the body as a whole. Non-systemic antacids are not absorbed, and therefore are able to neutralize acidity only in the stomach, without affecting the acid-base state of the body.

Antacids include SODIUM HYDROCARBONATE (drinking soda), CALCIUM CARBONATE, ALUMINUM and MAGNESIUM HYDROOXIDES, magnesium oxide. Usually these substances are used in different dosage forms and in different combinations.

Systemic antacids include sodium bicarbonate and sodium citrate, all the rest of the above agents are non-systemic.

Sodium bicarbonate (drinking soda) is a compound that is readily soluble in water and reacts quickly with hydrochloric acid in the stomach. This reaction takes place to produce sodium chloride, water and carbon dioxide. The drug acts almost instantly. Although sodium carbonate acts quickly, its effect is short and weaker than that of other antacids. The carbon dioxide formed during the reaction stretches the stomach, causing bloating, belching. In addition, recoil syndrome may occur with this drug. The latter consists in the fact that a rapid increase in pH in the stomach leads to the activation of parietal G-cells of the central part of the stomach, producing gastrin.

Gastrin stimulates the secretion of hydrochloric acid, which leads to the development of hyperacidity after the cessation of the action of the antacid. Typically, recoil syndrome develops in 20-25 minutes.

Due to its good absorption from the gastrointestinal tract, sodium bicarbonate can cause systemic alkalosis, which will clinically manifest as decreased appetite, nausea, vomiting, weakness, abdominal pain, cramps and muscle cramps. This is a rather dangerous complication that requires immediate discontinuation of the drug and assistance to the patient. Due to the severity of these side effects, sodium bicarbonate is rarely used as an antacid.

Non-systemic antacids, as a rule, are insoluble, act in the stomach for a long time, are not absorbed, and are more effective. When using them, the body does not lose either cations (hydrogen) or anions (chlorine), and there are no changes in the acid-base state. The action of non-systemic antacids develops more slowly, but it is more prolonged.

First of all, you should name:

1) aluminum hydroxide;

2) magnesium oxide.

ALUMINUM HYDROXIDE (aluminum hydroxide; Aluminii hydroxydum) - a drug with a moderate strength of antacid action, acts quickly and effectively, a significant effect appears after about 60 minutes.

The drug binds pepsin, reduces its activity, inhibits the formation of pepsinogen and increases mucus secretion.

One gram of aluminum hydroxide neutralizes 250 ml of decinormal hydrochloric acid solution to pH \u003d 4.0.

In addition, the preparation has an astringent, enveloping and adsorbing effect.

Side effects: not all patients tolerate the astringent effect of the drug well, which can be manifested by nausea; taking aluminum preparations is accompanied by constipation, therefore, aluminum-containing preparations are combined with magnesium preparations. Aluminum hydroxide helps to eliminate phosphates from the body.

The drug is indicated for diseases with increased secretion of gastric juice (hydrochloric acid): ulcer, gastritis, gastroduodenitis, food poisoning, flatulence. Assign aluminum hydroxide orally in the form of a 4% aqueous suspension, 1-2 teaspoons per dose (4-6 times a day).

Magnesium oxide (Magnesii oxydum; powder, gel, suspension) burnt magnesia is a strong antacid agent, more active than aluminum hydroxide, acts faster, longer and has a laxative effect.

Each of the listed antacids has a certain range of advantages and disadvantages. In this regard, their combinations are used.

The combination of aluminum hydroxide in the form of a special balanced gel, magnesium oxide and D-sorbitol made it possible to obtain one of the most widespread and effective antacids at present - ALMAGEL (Almagel; 170 ml; the drug was named from the words al-aluminum, ma-magnesium , gel-gel). The drug has an antacid, adsorbent and enveloping effect. The gel dosage form contributes to the uniform distribution of the ingredients over the mucous membrane surface and prolongs the effect. D-sorbitol promotes bile secretion and relaxation.

Indications for use: gastric and duodenal ulcers, acute and chronic hyperacid gastritis, gastroduodenitis, esophagitis, reflux esophagitis, Zollinger-Ellison syndrome, heartburn of pregnant women, colitis, flatulence, etc.

There is a drug called Almagel-A, in which, in addition to the composition of Almagel, anesthesin is added, which has both a local anesthetic effect and suppressing gastrin secretion.

Almagel is usually used 30-60 minutes before meals, and also within an hour after meals. The drug is prescribed individually, depending on the localization of the process, the acidity of gastric juice, etc.

Drugs similar to almagel:

Gastrogel (Czechoslovakia);

Phosphalugel (Yugoslavia) contains aluminum phosphate and colloidal gels of pectin and agar-agar, which bind and absorb toxins and gases, as well as bacteria, and reduce the activity of pepsin;

Megalak (Germany);

Milanta (USA) contains aluminum hydroxide, magnesium oxide and simethicone;

Gastal (Yugoslavia) - tablets, which include: 450 mg of aluminum hydroxide - magnesium carbonate gel, 300 mg of magnesium hydroxide.

Currently, the most popular drug from the group of antacids in many countries of the world is the drug MAALOX (Maalox) of the French company Rhone-Poulenc Rorer. The preparation contains aluminum hydroxide and magnesium oxide. Maalox is available in suspension and tablets; 5 ml of Maalox suspension contains 225 mg of aluminum hydroxide, 200 mg of magnesium oxide and neutralizes 13.5 mmol of hydrochloric acid; the tablets contain 400 mg of aluminum hydroxide and magnesium oxide, so they have a higher acid-neutralizing activity (up to 18 mmol of hydrochloric acid). Maalox-70 is even more active (up to 35 mmol of hydrochloric acid).

The drug is indicated for gastritis duodenitis, gastric ulcer and duodenal ulcer, reflux esophagitis.

There are practically no side effects. MEGALAK (Megalac) - German drug, analgesic antacid (silicic water aluminum-magnesium). It contains 0.2 aluminum oxide, 0.3 magnesium oxide and 0.02 oxetaine.

TOPALKAN (Topalkan) - French antacid preparation. It contains alginic acid, colloidal aluminum hydroxide, magnesium bicarbonate, hydrated silicon in a precipitated formless state. The drug has a foaming effect, forms a gel on the surface of the liquid contents of the stomach, covers the mucous membrane; acts quickly (6-14 minutes) and long-term (2-4 hours). Beneficial for esophagitis, reflux esophagitis.

MEANS PROTECTING THE MUCOSA OF THE STOMACH FROM ACID-PEPTIC EXPOSURE AND IMPROVING REPAIR PROCESSES

1. Preparations of bismuth (vikalin, vikair, de-nol).

2. Venter.

3. Preparations of prostaglandins.

4. Dalargin.

Bismuth preparations are used as astringent and antiseptic agents in the treatment of patients with peptic ulcer disease. Most often these are combined tablets - VIKALIN (basic bismuth nitrate, sodium bicarbonate, calamus rhizome powder, buckthorn bark, rutin and kellin). A related drug VICAIR (no rutin and no kellin).

In recent years, drugs have entered medical practice that more powerfully protect the mucous membrane from acid-peptic exposure. These are colloidal preparations of bismuth of the second generation, one of which is DE-NOL (De-nol; 3-potassium dicitrate bismuth; each tablet contains 120 mg of colloidal bismuth subcitrate). This drug envelops the mucous membrane, forming a protective colloidal-protein layer on it. They have no antacid effect, but exhibit antipeptic activity by binding to pepsin. The drug also has an antimicrobial effect, it is much more effective than bismuth-containing antacids, increases the resistance of the mucous membrane. De-nol cannot be combined with antacids.

The drug is used for any localization of the ulcer, it is highly effective for:

ü long-term non-scarring ulcers of the stomach and duodenum;

ü peptic ulcer disease in smokers;

ü prevention of recurrence of peptic ulcer disease;

ü chronic gastritis.

Assign 1 tablet three times a day half an hour before meals and 1 tablet before bedtime. De-nol is contraindicated in severe renal failure.

VENTER (sucrat; in tab. 0.5) is a basic aluminum salt of sucrose octasulfate. The antiulcer effect is based on binding with proteins of dead tissue in complex complexes that form a strong barrier. Locally, gastric juice is neutralized, the action of pepsin is slowed down, the drug also absorbs bile acids. At the site of the ulcer, the drug is fixed for six hours.

Venter and de-nol cause scarring of duodenal ulcers in three weeks.

Sukrat is used 1.0 four times a day before meals and before bedtime.

Side effect: constipation, dry mouth.

Preparations that improve trophism, regeneration and mucus formation.

Among "reparants" there are many herbal preparations, there are biological preparations and artificially synthesized ones.

The following drugs are most often used in the practice of gastroenterology:

1st generation:

Oxyferriscarbon sodium;

Gefornil;

Gastrofarm.

Sodium oxyferriscarbon contains ferrous and ferric iron in a complex with sodium salts of various acids (gulonic and alloxonic).

The drug has a regenerating, anti-inflammatory and analgesic effect. It is effective for stomach ulcers. In case of duodenal ulcer disease, the drug is ineffective.

Oxyferriscarbon sodium is prescribed intramuscularly at 30-60 mg for 10-20 days, the course is repeated 2-3 times.

SOLKOSERIL (Solcoseryl) - protein-free extract from the blood of cattle. Protects tissues from hypoxia and necrosis. It is used for trophic ulcers of any localization.

Apply 2 ml 2-3 times a day, administering intravenously and intramuscularly, until the ulcer heals.

Prostaglandin preparations:

MISOPROSTOL (cytotec), etc. Under the influence of these drugs, the acidity of gastric juice decreases, the motility of the stomach and intestines increases, and there are favorable effects on the ulcer niche in the stomach.

The drugs also have a reparative, hypoacid (by increasing mucus formation), hypotensive effect.

MISOPROSTOL (Misoprostol; in tab. 0.0002) is a preparation of prostaglandin E-2, obtained from plant materials.

Synonym - SITEOTEK.

Prostaglandin preparations are indicated for acute and chronic ulcers of the stomach and duodenum.

Side effects: transient diarrhea, mild nausea, headache, abdominal pain.

Assign one tablet twice a day. The combination of misoprostol with an NSAID (voltaren), the drug ARTROTEK, is used.

DALARGIN (Dаlarginum; in amp. And vials. 0.001 each) is a peptide drug that promotes healing of stomach and duodenal ulcers, reduces gastric acidity, has a hypotensive effect.

The drug is indicated for exacerbation of gastric ulcer and duodenal ulcer.

Contraindications to the use of dalargin are hypotension and pregnancy.

DRUGS WITH SPECIFIC ANTIBACTERIAL EFFECT ON Helicobacter pylory

(De-nol, metronidazole, oxacillin, furazolidone) The drug metronidazole has a broad spectrum of action against protozoa (Trichomonas, amoeba, lamblia), acts on the anaerobic microflora (for diseases of the chest, urinary tract), as well as Helicobacter pylory. The most effective antibacterial effect is observed with a combination of metronidazole and de-nol.

DRUGS AFFECTING THE INTESTINAL MOTOR