When antacids are prescribed, a list of drugs in this group should be given by the doctor depending on the individual characteristics of the patient. Since ancient times, people have used drugs for pain and cramps in the abdomen. These drugs were the first antacids. The function of such drugs, like antacids, was to interact with stomach acid. After all, excess hydrochloric acid leads to problems in the functioning digestive tract. Modern pharmaceuticals is finding more and more ways to get rid of excess acid in the gastrointestinal tract.
For convenience, the entire list of antacid drugs was divided into 2 groups: absorbable and non-absorbable. The absorbable group is used less and less due to side effects. The first group includes funds:
- magnesium oxide (burnt magnesia);
- calcium carbonate;
- sodium carbonate;
- Rennie;
- Bourget mixture;
- Tams.
But these remedies are rarely used, as they contribute to the appearance of bloating and belching due to the carbon dioxide formed. But at the same time, they have a quick effect. Second group of drugs:
- magnesium hydroxide;
- aluminum hydroxide;
- Phosphalugel;
- Maalox;
- Topalkan.
These drugs act more slowly, but the effect lasts for longer time(up to 1.5 hours), side effects are unlikely. Another important advantage of a non-absorbable product is that it has an enveloping property, thereby neutralizing both perchloric acid and bile acids.
Antacid medications are also divided according to the speed of action and its duration. They also make a list of drugs divided by solubility in water: soluble and insoluble.
- Water soluble products. Well-soluble agents in water include: calcium carbonate, soda, sodium sulfate, sodium phosphate, sodium bicarbonate, calcium carbonate, magnesium carbonate. They act quickly, but as a result of this action, the gastric pouch is stretched due to the formation carbon dioxide, which contributes to rebound syndrome. Sodium bicarbonate due to its solubility in aqueous solutions can be absorbed and systematically affect the entire body.
- Insoluble agents. These drugs include all compounds of magnesium and aluminum. Compared to soluble agents, these have a slow effect, but longer. This product partially absorbs toxins and is practically not absorbed into the liquid environment of the body. If the dose is exceeded, aluminum salts have a blocking effect, and magnesium salts have a laxative effect.
The most common drugs in this group are this list from the most common to the average popularity and use of the drug.
Medicines included in the list of insoluble antacids
- Phosphalugel, consisting of aluminum phosphate, is available in gel form. Enveloping, adsorbing agent.
- Maalox - aluminum hydroxide and magnesium hydroxide. Release form: tablets, suspension in a bottle and packaged.
- Talcide consists of hydrotalcite. Chewable tablets. Gastroprotective drug.
- Gelusil-Lak - compounds of aluminum, magnesium, silicon (simaldrate). Pills. The medicine is often used as an adsorbent.
- Rennie, consisting of magnesium carbonate. Chewable tablets.
- Almagel - from magnesium hydroxide and aluminum hydroxide, suspension. It has good antacid, enveloping, and adsorbing properties.
- Almagel A. An additional substance - benzocaine, is available as a bottle of suspension.
- Almagel Neo. An additional substance is simethicone. Release form: suspension bottle.
- Alma-Gal - chewable tablets or a bottle of suspension consisting of aluminum hydroxide and magnesium hydroxide, with the additional substance sorbitol.
- Alumag consists of magnesium hydroxide and algeldrate, available in tablets, antiulcer, antacid.
- Sucralfate is aluminum hydroxide, available in tablets or granules.
- Vikalin consists of magnesium carbonate, sodium bicarbonate, bismuth subnitrate and auxiliary substances - calamus rhizomes, buckthorn bark.
- Gastal is an enveloping tablet containing hydroxides of aluminum, magnesium and carbonate.
- Gastrik are chewable tablets consisting of calcium carbonate and hydroxide.
- Gelusil is a suspension for internal use, consisting of simaldrate, in addition to its antacid effect, it is also a cytoprotective drug.
- Rutacid - chewable hydrotalcite tablets.
- Tisacid consists of hydrotalcite and is available in tablets.
- Entegnin is an adsorbent tablet containing hydrolytic lignin.
This is a small list of antacids that are not absorbed into the blood. All of the above medications are complex means, which means they contain a complex of compounds that affect stomach acid.
The drug Maalox acts the fastest, followed by increasing time:
- Phosphalugel.
- Remagel.
- Megalac.
- Almagel.
Antacids often used in therapy.
Treatment with Phosphalugel does not lead to secondary hypersecretion of gastric acid.
Hydrotalcite (rutacid, talcid) quickly and for a long time binds hydrochloric acid to maintain normal level acidity of the stomach, protects the mucous membrane from the action of the enzyme pepsin.
Almagel and all drugs containing simethicone eliminate discomfort in the gastrointestinal tract, promote the natural release of gases and prevent stool retention.
Almagel is a well-known and widely used drug that eliminates the symptoms of gastritis, duodenitis, stomach ulcers and duodenum, esophagitis. Almagel also eliminates stomach pain and heartburn. Yellow Almagel, in addition, has analgesic properties, therefore it is used to eliminate severe pain syndrome at various diseases digestive system.
The drug Almagel also has a variant spelling "Almagel". This confusion is due to the fact that the title of the original is written with Latin letters"Almagel". The letter "l" in the Latin word is usually read softly, like "l". However, it is impossible to accurately convey phonetics and pronunciation using Cyrillic letters, which is why there are options for spelling the name with both soft “l”, or with only one - at the end of the word, as is typical of the Russian language.
Types and forms of release
Today, the drug Almagel is available in two main dosage forms:1. Suspension.
2. Pills.
The suspension contains various components that give the drug certain additional properties. The following suspension options are available today:
- Almagel suspension (contains only the main components - aluminum and magnesium hydroxide gel);
- Almagel A suspension (together with the main components contains the painkiller benzocaine);
- Almagel Neo suspension (together with the main components contains the substance simethicone, which eliminates gases);
- Almagel T tablets (contain only the main components).
Due to such convenient and unified coloring of the packages, drug variants are often named by the color of the box, for example, Almagel green (basic, regular suspension), Almagel yellow (Almagel A with anesthetic), Almagel red (Almagel Neo). The name “Almagel in bags” refers to the release form of Almagel Neo, which is bottled in small plastic bags of 10 ml.
All Almagel suspensions are available in 170 ml bottles with a 5 ml measuring spoon. Almagel Neo is also available in the form of 10 ml sachets. Tablets are sold in packs of 12 and 24 pieces.
Maalox suspension in everyday speech is often called “Maalox in bags”, “liquid Maalox” or “Maalox gel”. All of these names use some kind of hallmark dosage form for its designation, which allows both doctors and pharmacists to clearly and quickly understand what the patient means. Therefore, these incorrect and unofficial names are often and widely used. However, it must be remembered that no matter which of the listed names a person uses, he means by it the Maalox suspension.
Compound
Both tablets and suspension contain Maalox and Maalox Mini as active ingredients aluminum hydroxide (algeldrat) And magnesium hydroxide. The amount of active substances in each form differs slightly, but this is necessary so that they all have approximately the same severity and duration. therapeutic effect. The dosage of active substances of various varieties and forms of Maalox is shown in the table.It is also important to wear uncomfortable clothes and accessories - for example, tight belts and tight trousers can also lead to this disease. Heartburn can occur during pregnancy or as a result of a hernia hiatus diaphragm.
What to do when heartburn hits you here and now?
In this case you can use effective means Rennie, which will relieve you from heartburn without harm to your health.
Rennie - composition
The main components of the drug - calcium carbonate(680 mg) and magnesium carbonate(80 mg). The medicine also contains excipients.Release form
This popular medicine comes in tablet form.Each tablet form contains the same composition of calcium carbonate and magnesium carbonate. Excipients vary depending on the aroma of the drug (mint, orange and menthol). All tablets are sold in cardboard packages.
Aluminum hydroxide is used somewhat less frequently to eliminate hyperphosphatemia (increased levels of phosphates in the blood) against the background renal failure. The fact is that aluminum hydroxide binds excess phosphates in the intestines, which in case of renal failure are not excreted from the body in a normal volume, thereby helping the kidneys remove these salts.
In addition, in rare cases, aluminum hydroxide is used externally as an astringent for skin diseases.
Aluminum hydroxide is usually taken internally in the form of a suspension, which is a powder thoroughly mixed in water. In rare cases, if it is impossible to prepare a suspension, aluminum hydroxide is taken orally directly in powder form.
Externally, aluminum hydroxide is used only in powder, sprinkling it on the affected areas of the skin.
Medicines containing aluminum hydroxide
In the CIS countries there are only two drugs containing aluminum hydroxide as active substance– these are Rokzhel (Rokgel) and Aluminum hydroxide-Rivopharm. In Europe and the USA there are much more wide range drugs with aluminum hydroxide as the only active substance, such as Alternagel, Amphojel, Aloh-Gel, etc. There are significantly more drugs on the market of CIS countries that contain algeldrate as one of the active components, since they are more effective, safe and modern. To make it easier for you to navigate, here is a list of antacid drugs present on pharmaceutical market CIS countries containing algeldrate as an active substance:
- Ajiflux (algeldrate + magnesium hydroxide) tablets;
- Almagel, Almagel A and Almagel Neo (algeldrate + magnesium hydroxide) – suspension;
- Altacid (algeldrate + magnesium hydroxide) – suspension and chewable tablets;
- Alumag (algeldrate + magnesium hydroxide) tablets;
- Gastracid (algeldrate + magnesium hydroxide) tablets;
- Maalox and Maalox mini (algeldrate + magnesium hydroxide) tablets and suspension;
- Palmagel (algeldrate + magnesium hydroxide) gel for oral administration;
- Simalgel VM (algeldrate + magnesium hydroxide + simethicone) suspension for oral administration.
Therapeutic effect
Aluminum hydroxide has three main pharmacological properties:- Antacid action;
- Adsorbent action;
- Enveloping effect.
In the intestines, aluminum is not absorbed, but forms insoluble salts - phosphates, which cause constipation. Therefore, when using only aluminum hydroxide as an antacid, laxatives should be taken. Constipation can be eliminated by taking aluminum hydroxide in combination with magnesium hydroxide, which is usually done successfully.
Adsorbent property aluminum hydroxide lies in its ability to bind hydrochloric acid molecules and thereby neutralize them, enhancing the antacid effect based on a chemical reaction.
Enveloping property aluminum hydroxide lies in its ability to be evenly distributed over the gastric mucosa, forming a thin protective film on it that protects it from the damaging effects of both hydrochloric acid and certain types of food.
Thus, aluminum hydroxide is used as symptomatic remedy to eliminate various discomfort caused by increased acidity of gastric juice. Since the acidity of gastric juice can be increased not only in severe serious diseases, but also against the background functional disorders, then aluminum hydroxide cannot be considered a drug only for the treatment of pathology, since it can be used exclusively as a symptomatic remedy to eliminate unpleasant sensations.
Separately, it should be said about one more property of aluminum hydroxide, which is also used in medical practice. So, this substance, getting from the stomach into the intestines, binds phosphates, forming insoluble salts with them and removing them from the body along with feces. The ability of aluminum hydroxide to remove phosphates from the body is used in complex therapy renal failure, in which, on the contrary, these salts accumulate and cause various disorders. After all, phosphates are normally excreted mainly by the kidneys, and in case of renal failure, accordingly, these salts are not removed from the body in the required volume and accumulate. The use of aluminum hydroxide allows you to remove excess phosphates from the body and thereby improve the well-being of a person suffering from kidney failure.
Indications for use
Aluminum hydroxide is indicated for use as part of the complex therapy of the following diseases, as well as to eliminate dyspeptic symptoms: - Esophagitis;
- Reflux - esophagitis;
- Acute gastritis;
- Chronic gastritis with increased acidity of gastric juice;
- Acute duodenitis;
- Peptic ulcer of the stomach or duodenum during an exacerbation;
- Symptomatic ulcers or erosions on the mucous membranes of the digestive tract;
(from Greek ἀντἰ- - against, lat. acidus- sour) - medications, the mechanism of action of which is based on the chemical neutralization of gastric acid.
Composition of antacids
Main acid-neutralizing active ingredients modern antacids are compounds of magnesium, aluminum and calcium. Many of the modern antacid medications also contain components that affect gastrointestinal tract, in a way other than neutralizing the acid: laxatives, carminatives, antispasmodics, anesthetics and others.Most modern antacid preparations use a balanced combination of magnesium compounds (magnesium oxide, magnesium hydroxide, magnesium peroxide, magnesium carbonate) and aluminum (aluminum hydroxide, aluminum phosphate and others). Such antacid drugs are characterized by a slower onset of therapeutic effect compared to sodium and calcium compounds, but they have a longer effect time. Such compounds do not dissolve in water, are practically not absorbed into the blood, are characterized by antipeptic properties and partially adsorb toxins. Aluminum compounds help slow intestinal motility and in large quantities can cause constipation, while magnesium compounds accelerate it and have a laxative effect.
Aluminum compounds enhance the synthesis of prostaglandins, promote the formation of a protective film on the surface of damaged tissues, adsorb bile acids and lysolecithin, and increase the tone of the lower esophageal sphincter. Magnesium compounds increase mucus formation and resistance of the gastric mucosa. The table below (Kharchenko N.V., Chernenko V.V.) shows the effects of the main components of modern antacid drugs (– no effect, + low activity, ++ medium activity, +++ high activity).
|
Characteristics of some components modern antacids |
||||
| Action/cations | Mg | Ca | Al | Bi |
| Neutralizing | +++ | + | ++/+++ | – |
| Adsorbent | + | + | +++ | + |
| Enveloping | – | – | + | – |
| Astringent | – | – | + | +++ |
| Cytoprotective | – | – | +++ | + |
Absorbable antacids
Absorbed antacids are those that either themselves or the products of their reaction with gastric acid dissolve in the blood. Positive quality absorbed antacids is a rapid decrease in acidity after taking the medicine. Negative - short duration of action, acid rebound (increased secretion of hydrochloric acid after the end of the drug), the formation of carbon dioxide during their reaction with hydrochloric acid, stretching the stomach and stimulating gastroesophageal reflux (see picture from the article by D.S. Bordin, below and to the right). Absorption of bicarbonates into the blood can lead to the development of systemic alkalosis. Long-term use Absorbable antacids containing calcium can cause constipation and hypercalcemia, and in combination with milk or dairy products - milk-alkali syndrome, manifested by nausea, vomiting, polyuria, transient azotemia. The development of calcium kidney stones and nephrocalcinosis is possible. 
Examples of absorbable antacids:
- sodium bicarbonate (baking soda)
- Bourget mixture (a mixture of sodium bicarbonate, sulfate and sodium phosphate)
- medicines "Rennie", "Tams", "Andrews antacid" (a mixture of calcium carbonate and magnesium carbonate).
Non-absorbable antacids
Active components non-absorbable antacids are aluminum hydroxide, aluminum phosphate, magnesium hydroxide, magnesium trisilicate.
Non-absorbable antacids begin to act later than absorbable ones, but their duration of action is longer and reaches 2.5–3 hours. They are buffered against hydrochloric acid of gastric juice and, due to this, maintain acidity during their period of action within the range of 3–4 pH. Non-absorbable antacids are divided into the following groups: 
Comparison of the effects of various antacids
At the Central Research Institute of Gastroenterology with the help intragastric pH-metry Studies have been conducted on the acid-neutralizing effect of various antacids. Table 2 (see below) presents average data for some drugs: the time of onset of action of the antacid from the moment of taking the drug, the time of action of the antacid drug, the area of alkalization (corresponding to the volume of acid neutralized by the antacid) and the alkalization index, equal to the area alkalization divided by the acidity of gastric juice at the time the drug begins to act.|
Indicators |
A drug | ||||
| Almagel | Remagel | Phosphalugel | Megalac | Maalox | |
| Action onset time, min | 13,5 | – | – | – | 8,9 |
| Action time, min | 28 | 32,5 | 40 | 46 | 56 |
| Alkalinization area |
6,6 | 4,5 | 5,4 | 6,5 | 13,2 |
| Alkalinity index |
9,0 | 11,4 | 6,7 | 13,5 | 18,0 |
The time for the onset of antacid action after administration was the shortest for Maalox (an average of 8.9 minutes), the longest for Almagel (an average of 13.5 minutes). The average duration of the alkalizing effect of antacids also varied widely, from 28 minutes for Almagel to 56 minutes for Maalox. At the same time, Remagel, Phosphalugel and Megalac occupied an intermediate position between them. Analysis of pH grams showed that the maximum acidity values after taking various antacids differed slightly. However, indicators of the severity of the alkalizing effect are the time to reach maximum pH values and the duration of “retention” maximum effect the most optimal were those of Maalox (Ilchenko A.A., Selezneva E.Ya.).
Dosage forms of antacids
The most common forms of release of antacid drugs are: tablets, lozenges, oral suspension in a bottle, oral suspension in sachets containing a single dose of the drug. The release form is important for the neutralizing ability of the antacid, as well as for its convenience for use by patients. Antacids interact with hydrogen ions only in a dissolved state, so solubility is important parameter affecting the effectiveness of antacids. Suspensions are made up of smaller particles than tablets, so they have a larger surface area and dissolve faster in the stomach. Pre-chewed and dissolved tablets have more effective action than swallowed whole. However, taking the suspension is not always convenient for patients who lead an active lifestyle, so some of them take the suspension at home and tablets in public places.
Antacids in the treatment of duodenal ulcers
Modern medical science absolutely rightly believes that the main drugs used in the treatment of acid-related diseases should be drugs that most effectively inhibit gastric acid production, which today are proton pump inhibitors. Taking any antacids and adsorbents during eradication Helicobacter pylori undesirable due to possible decrease in efficiency antibacterial treatment. Antacids, losing the championship in suppression stomach acidity proton pump inhibitors and other antisecretory drugs occupy a significant niche in the treatment of acid-dependent conditions.
For example, a modern non-absorbable antacid based on the aluminum-magnesium combination “aluminum hydroxide + magnesium hydroxide” (for example, “Almagel”, “Altacid”, “Alumag”, “Gastratsid”, “Maalox”, “Maalukol”, “Palmagel” and similar) can be used in the treatment of duodenal ulcers in the following situations (Maev I.V., Samsonov A.A., Minushkin O.N.):
- for pain relief during the screening phase, as well as on the first day of taking proton pump inhibitors before the start of blockade of acid production
- with small ulcer sizes (no more than 1.0 cm) and a short ulcer history, in the absence Helicobacter pylori aluminum-magnesium antacids can be prescribed as the only drug.
- for ulcers larger than 1.0 cm, for long-term non-healing ulcers, such antacids are used in combination with proton pump inhibitors in order to enhance the cytoprotective effect (growth factor fixation phenomenon) - for those not associated with Helicobacter pylori ulcers, as well as for associated ones, in cases with ulcers that are difficult to scar
- in the case of the use of H2-histamine blockers and their withdrawal, to level out the possible “acid rebound”
- after eradication Helicobacter pylori to relieve possible episodic pain and heartburn
- as anti-relapse therapy
The use of antacids in treatment chronic duodenitis
Antacids in the treatment of chronic duodenitis are used in the following situations (Maev I.V., Samsonov A.A.):
- as an additional antisecretory agent to H2 blockers or proton pump inhibitors, as an additional adsorbent agent in the treatment of acute gastroduodenitis or acute duodenitis
- as an additional antisecretory agent during therapy with H2 blockers or proton pump inhibitors during exacerbation of chronic gastroduodenitis or chronic duodenitis, including against the background of celiac disease,
Currently, there is a qualitative revision of many established ideas about acid-related diseases, their treatment and prevention of exacerbations. The authors of review articles devoted to these issues either mention antacids in passing or do not mention them at all, and this is understandable. When the tendency for spontaneous healing of peptic ulcers was not well known, antacids were considered reliable therapeutic agent for ulcers, since practical experience has shown that they relieve pain and promote ulcer healing. With the accumulation of knowledge about the strong tendency of ulcers to heal spontaneously and the insufficient ability of antacid drugs to bind hydrochloric acid, these drugs were transferred to the class of “logical placebos”, and it was then concluded that short-term changes in gastric pH caused by antacids were not able to promote healing ulcers and that the observed healing should be attributed solely to a spontaneous process.
However, the first controlled studies on the effect of antacid drugs on ulcer healing, conducted in the USA (1977), showed that peptic ulcers heal faster with antacids than with placebo (for example, duodenal ulcers after 4 weeks of treatment with antacid drugs healed in 78% of cases, compared with placebo - 45% healing - Peterson W. Letal, 1977; and stomach ulcers in 89% of cases compared with 52% placebo - Littman A. et al., 1977). Thus, evidence was obtained that antacid drugs are in no way just “logical placebos” - they are drugs for the treatment of peptic ulcers with proven effectiveness. In subsequent years, these data were repeatedly reproduced both in relation to duodenal and gastric ulcers. The analgesic effect of antacids and approximately the same effectiveness of antacids and histamine H2 receptor blockers have also been proven. The next question that the researchers decided was what should be the dose of the antacid; should it bind all the hydrochloric acid that is produced by the stomach? It turned out that it should be a tenth of the dose that is necessary to neutralize all the hydrochloric acid (i.e. 90 to 120 mmol per day) in order for the ulcer to heal (Berndt H., 1985). From a series of these works, it became clear that antacid drugs exert their effect not only through the binding of hydrochloric acid (Arend R., Roesch W., 1993).
In subsequent years, it was found that antacid drugs:
adsorb bile acids and lysolecithin (involved in damage to the mucous membrane of the stomach and esophagus);
have a protective effect associated with stimulation of prostaglandin synthesis (and therefore have priority use in cases where the pathogenesis of ulcers or damage to the mucosa is associated with a weakening of the protective properties of the mucosa);
have the ability to bind epithelial growth factor and fix it in the area ulcerative defect, thereby stimulating local reparative and regenerative processes, cell proliferation and angiogenesis. This makes it possible to fully restore the mucous membrane in a functional sense, which should lead to an extension of the period of remission. Thus, only enumeration pharmacological effects antacid drugs show a very wide spectrum of their action, which significantly distinguishes them from other antiulcer drugs.
Currently, acid-dependent diseases include not only those in which hydrochloric acid acts as a implementing factor, but also diseases in which hydrochloric acid supports the course (progression) of the disease and in the treatment of which it is impossible to do without blockers of secretion (or acid binding). All acid-dependent diseases can be divided into three groups:
Group I – classic:
Stomach ulcer;
Duodenal ulcer;
Gastroesophageal reflux disease;
Zollinger-Ellison syndrome;
Ulcer due to hyperthyroidism.
Group II – indirect:
Acute (exacerbation of chronic) pancreatitis;
Reflux gastritis;
NSAID gastropathy.
Group III – reflex:
Intestinal disorders (caused by hyperproduction of hydrochloric acid);
Biliary dysfunction (formed when acidic contents enter the duodenal bulb), etc.
In the treatment of these diseases, the main or noticeable effect is the blockade of hydrochloric acid production. In general, the idea of acid-related diseases began to take shape more than 100 years ago, at which time the main stimulants and structures through which gastric secretion was carried out were discovered. However, the first drugs that effectively block gastric secretion appeared about 50 years ago, and the most effective drugs that block the “proton pump” only appeared in recent years.
More recently, it was also possible to clarify the role Helicobacter pylori in the genesis of peptic ulcer disease. In this regard, the tactics of treating this disease have also changed. It was decided to carrying out eradication treatment – first by the American Gastroenterological Association in 1994, then by the European (Maastricht I, 1996) and Russian (1997). The European Association adjusted the recommendations in 2000 (Maastricht II). Thus, today, in accordance with modern ideas about the pathogenesis of the disease drug treatment is based on two main approaches:
1. Eradication drug therapy if an infection is detected Helicobacter pylori(Hp).
2. Effective suppression of gastric acid production with modern antisecretory drugs. It should be noted that the causal relationship between peptic ulcer disease and HP (more than 90%) at first seemed very close.
The results of recent large-scale studies in different countries worldwide have shown that peptic ulcer disease associated with Hp infection accounts for 70–80% duodenal ulcers and more than 50–60% of stomach ulcers. This again allows us to speak about the multifactorial nature of the pathogenetic mechanisms of damage to the gastrointestinal tract, and to consider complex therapy as the basis for the treatment of these injuries. According to modern ideas about the pathogenesis of ulcerative lesions of the stomach and duodenum, they are the result of an imbalance of aggressive and protective factors, regardless of whether the imbalance is associated with increased secretion or reduced mucosal resistance. It has now been proven that ulcer scarring occurs in all cases when it is possible to maintain intragastric pH>3 for 18 hours throughout the day. The list of drugs currently used for basic (i.e., aimed at suppressing acid-peptic aggression) therapy for peptic ulcer disease is presented in four groups medicines: H2-histamine receptor blockers, proton pump blockers, anticholinergics and antacids.
These drugs differ in the strength and duration of action aimed at increasing intragastric pH, however, since the level of acid production is different in different patients, they require different degrees of suppression of acid production. When choosing a particular drug for the treatment of ulcerative lesions, it is necessary to take into account not only the intensity of acid formation, but also the stage of the ulcer.
Currently there are four stages of ulcer:
first – lasting 48–72 hours, characterized by a breakthrough of the “protective barrier” in a limited area of the mucous membrane and the formation of an ulcerative defect here under the influence of aggressive factors of gastric juice, with the defect spreading in depth and to the sides.;
second stage is called the “rapid regeneration” stage and lasts about two weeks. This stage begins with the restoration of balance between the factors of aggression and defense, which is taken over by the immune system. Morphologically, this stage is characterized by the presence of necrotic masses filling the defect, damaged vessels, pronounced swelling of the mucosa in the periulcer area with lympho- and capillary stasis. Macrophages, lymphocytes, and plasma cells are attracted to the damaged area. The main biologically active factors acting at this stage are growth factors. The ulcer is cleared of decay products, intensive processes of collagen formation and regeneration of the epithelium, endothelium and other cellular structures begin. These processes require significant energy expenditure, as evidenced by intense DNA synthesis, recorded within 12 hours after the formation of the ulcer.
At the third stage (slow regeneration or late healing), lasting 3-4 weeks, the activity of the immune system increases, growth factors, enzyme-hormonal factors continue to act, under the influence of which the epithelization of the ulcer is completed, the reconstruction of microcirculation, cell differentiation and their functional “maturation” begin.
In the fourth stage , the duration of which is difficult to determine, the restoration of the functional activity of the mucous membrane continues, and sometimes ends. The duration and durability of remission (rarely, often, continuously relapsing types of ulcer or recovery) depend on the completeness of these processes. Identification of the stages of an ulcer is an important recent achievement, which has shown that ulcerogenesis is standard for all ulcers, and ulcer healing proceeds according to its own laws, little or not at all dependent on pathogenesis.
If speak about place of antacids in the treatment of ulcers, they can be used:
As basic drug with low aggressiveness of gastric juice;
In the second and third stages of ulcers with insufficient intensity of scarring of the ulcer (as a means of stimulating regeneration processes due to the fixation of growth factor);
In the fourth stage of the ulcer for complete functional restoration of the mucous membrane;
During the period of withdrawal of secretion blockers to prevent the “rebound” phenomenon.
The second group of diseases caused by the aggressive properties of gastric and duodenal contents includes gastroesophageal reflux disease (GERD), the morphological essence of which is degenerative changes in the esophagus associated with the reflux and long-term exposure of gastric and, in the case of a resected stomach, duodenal contents.
Of particular importance are: an increase in the volume of gastric contents due to hypersecretion and delayed gastric emptying, an increase in the concentration of hydrochloric acid in it, bile acids, as well as increased intra-abdominal pressure. Today in treatment of GERD It is proposed to use proton pump inhibitors until clinical and endoscopic remission is achieved, and then switch to maintenance doses, which the patient should receive continuously for a long time. Moreover, depending on economic capabilities, the patient may choose secretion blockers or antacid drugs. Wherein The antacids of choice are those containing alginic acid , which keeps the drug on the surface of the stomach contents and is thrown into the esophagus with each reflux. In addition, modern non-absorbable antacids have the ability to bind bile acids, so in conditions of “alkaline” reflux they are pathogenetically justified.
Traditionally, all antacids are divided into absorbable and non-absorbable. TO absorbable antacids relate:
Sodium bicarbonate (soda - NaHCO 3);
Magnesium oxide (burnt magnesia);
Basic magnesium carbonate – mixture of Mg(OH) 2, 4MgCO 3, H 2 O;
Basic calcium carbonate – CaCO 3;
Bourget's mixture (Na sulfate, Na phosphate, Na bicarbonate);
Rennie's mixture (calcium carbonate + magnesium carbonate);
Tams mixture (calcium carbonate + magnesium carbonate). They neutralize hydrochloric acid, but their effect is very short-lived - when absorbed, they can significantly affect the exchange of electrolytes. Some of them have the “ricochet” phenomenon, i.e. stimulates gastric secretion, so their use should be symptomatic (until relief of the symptom), usually one, two doses or a short period of time (days) when their possible side effects do not develop.
Thus, we, together with obstetricians, studied the effectiveness of Rennie’s mixture in pregnant women to relieve heartburn. The drug turned out to be quite effective, while calcium metabolism turned out to be very stable. Non-absorbable antacids have a greater buffer (neutralizing) capacity. Their duration of action reaches 2.5–3 hours.
They are divided into three groups:
1. Aluminum salt of phosphoric acid.
2. Aluminum-magnesium antacids (Almagel Neo, Almagel) .
3. Aluminum-magnesium preparations with the addition of alginate.
Drugs of the third group are very actively used in various clinical forms of gastroesophageal reflux disease. Based on modern ideas about GERD, they can be successfully and for a long time effective in the negative phase of the disease (both in “on-demand” regimens and in a permanent version). After the discovery of all the clinical and pharmacological effects of antacids, interest in antacid drugs increased again. Works have appeared (O.N. Minushkin et al., 1996, 1998, 2001, 2002, 2003, 2004; A.A. Sheptulin et al., 1996, E.S. Ryss, E.E. Zvartau, 1998 ; V.T. Ivashkin et al., 2002; A.V. Okhlobystin, 2002; Yu.V. Vasiliev 2002, 2003, etc.), in which an attempt is again made to determine the place of antacid drugs in the treatment of acid-related diseases. Back in 1990, Tytgat et al., having analyzed the results of treatment of GERD, proposed the use of antacids in the treatment of stage I–II disease as monotherapy. Other stages of the disease require a different approach, and, as a rule, a complex effect. The review (O.N. Minushkin et al., 1998) analyzed the effectiveness of treatment in 206 patients with GERD of different ages and different degrees of damage. The effectiveness of monotherapy has been confirmed in the early stages of the disease, especially in elderly patients, old age and in children. In these situations, antacids should be preferred. In a number of studies, the effectiveness of antacids was compared with the effectiveness of histamine H2 receptor blockers both in the relief of clinical manifestations and in the dynamics of the morpho-endoscopic substrate, which we associated with the protective effect of the action. If we talk about peptic ulcer disease, then in cases where the disease is associated with Helicobacter pylori, treatment should begin with HP eradication, and then therapy with secretion blockers should be continued until the ulcer scars, and then can be continued with antacids to prevent rebound syndrome, or they can be added to treatment if the scarring process slows down or the ulcer is resistant to treatment.
If the ulcer is not associated with HP, then antacids can be used as monotherapy (when we are talking about small (up to 8 mm) duodenal ulcers, in patients with a short history of ulcers) or as part of combination therapy , when a protective effect is necessary. The introduction of antacids into the treatment complex in patients with long-term non-healing ulcers (using the phenomenon of growth factor fixation) is especially indicated.
In pediatric practice, antacids should be of greater importance, since childhood pathology develops in a growing organism with an “incomplete” hormonal status, unstable secretion and motility, and an imperfect circulatory regulation system. Our two works (1996, 1998) analyzed the results of treatment of 433 children aged 6 to 15 years (pathology: erosive gastritis, duodenitis, reflux esophagitis, peptic ulcer).
It has been shown that non-absorbable aluminum/magnesium-containing antacids in children are effective means treatment and prevention of “acid-dependent” pathology. They should be considered as a means of basic therapy, as they have an acid-neutralizing, protective, growth factor-stimulating effect and absorb bile acids. At the same time, the risk of developing side effects is minimal, since there is no direct connection between the dose of the drug (which is typical for gastric secretion blockers) and the effect. Finally, speaking of ulcers, antacids can and should be used as a means of preventing exacerbation. We carried out preventive treatment in 50 patients (dose of 800 mg and 1600 mg of Magalfil-800) for a year, and the ulcer did not recur in 66% of patients. Relapses in patients who do not receive preventive treatment develop in 80% of cases. The difference is significant. I would like to note that in the treatment of reflux gastritis, where the main damaging factors are bile acids and lysolecithin, antacids are the drugs of choice for both treatment and prevention. The drugs of the remaining groups are of relative importance (auxiliary, symptomatic). If we talk about acid-dependent diseases that occur with impaired intestinal motility (constipation, laxity), then non-absorbable antacids are very effective (for laxity, antacids with a predominance of aluminum; for constipation, with a predominance of magnesium). In the treatment of pancreatitis and NSAID gastropathy, antacids are of little importance, since in these cases the blockade of gastric secretion should be maximum and throughout the day, which is very difficult to provide with antacids without serious side effects. IN Lately An antacid drug appeared on the domestic market "Almagel-Neo" , which contains aluminum and magnesium hydroxide, presented in an optimal ratio. It is known that aluminum hydroxide causes a slow development of the effect and can cause constipation; on the contrary, magnesium hydroxide leads to a rapid effect, but has a laxative effect.
The combination of these components in Almagel-Neo has an optimal therapeutic effect and has the greatest antacid capacity, which ensures a high acid-neutralizing effect. Compared to the previously known Almagel suspension, the new preparation increases the content of magnesium hydroxide by 3.9 times and adds the defoamer simethicone, which has a beneficial effect on belching and flatulence - facilitating the rapid absorption of the resulting gas (Table 1). We studied the effectiveness of Almagel-Neo in 20 patients with exacerbation chronic gastritis and duodenitis. All patients had preserved or increased gastric secretion.
The influence of Almagel-Neo on:
Speed and completeness of pain relief and symptoms of gastric dyspepsia;
Frequency and consistency of stool, flatulence;
The speed and duration of action with a single dose and a course of treatment (alkaline time was assessed by intragastric pH-metry);
Side effects and tolerability of the drug were recorded. Almagel-Neo was prescribed as monotherapy at a dose of 2 sachets 3 times a day for the first 3–5 days, then 1 sachet 3 times a day 1 hour after meals (10–14 days).
A positive effect was obtained in 100% of patients, with good and excellent effects in 70% of patients. The effectiveness of the antacid drug determines the rate of development of the therapeutic effect and the duration of neutralization of hydrochloric acid. What matters is that The clinical effect of treatment with Almagel-Neo was achieved in a short time: pain was relieved in the first 3 days, gastric dyspepsia and flatulence - in the first 3-7 days. Almagel-Neo provided the onset of action in 8–12 minutes, the duration of the effect was 3 hours. The alkaline time after taking 20 ml of Almagel-Neo averaged 40 minutes, while the pH increased to 5–7.2. The phenomenon of a secondary increase in gastric secretion was absent. The drug was well tolerated; a dose of 3 sachets per day had no effect on intestinal motility. In general, we assessed the effectiveness of the drug Almagel-Neo as high: the effect was achieved quickly, in the first 3 days, a sufficient dose is 30 ml of the drug per day, and in cases of severe acidism, the initial dose can be 60 ml. In general, when concluding about the place of antacid drugs in the treatment of gastroenterological pathology (acid-dependent diseases), it should be recognized that antacids continue to maintain the positions they have gained over decades, and with the discovery of new properties (protective effect, influence on growth factor and absorption of bile acids), these positions consolidated and expanded. In addition, these drugs are relatively inexpensive and therefore in demand by patients.
Literature
1. Minushkin O.N. etc. – Maalox in clinical practice. – M., 1996.
2. Minushkin O.N. and etc. - Modern aspects antacid therapy - M., 1998.
3. Minushkin O.N. – The place of modern antacid drugs in the treatment of acid-related diseases. – Medical doctor, 2001, 5–6, 8–10.
4. Minushkin O.N. and others - Almagel-Neo in modern therapy acid-related diseases. – XI Congress “Man and Medicine”, 2004, p.154.
5. Minushkin O.N., Elizavetina G.A. – Antacids in modern therapy of acid-dependent diseases. – Consilium, No. 7, 2003, 8–10.
6. Sheptulin A.A. – Modern principles pharmacotherapy of peptic ulcer. – Klin.med., 1996, 8, 7–8.
7. Ryss E.S., Zvartau E.E. – Pharmacotherapy of peptic ulcer, M., 1998.
8. Ivashkin V.T. et al. – The place of antacids in modern therapy of peptic ulcer – RMZH (supplement), 2002, 4(2), 42–46.
9. Okhlobystin A.V. – Modern features use of antacid drugs – Breast Cancer (supplement), 4(2), 51–54.
10. Vasiliev Yu.V. – Antacid drugs in modern treatment of diseases of the upper gastrointestinal tract. – Cons.med, (appendix), No. 7, 2003, 3–7.
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