HEARTBURN AND ANTACIDS

The state of dyspepsia - from discomfort in the epigastric region and the severity of pain after eating and vomiting up to almost familiar to everyone. The prevalence of these phenomena in developed countries are 30-40% and associated with the peculiarities of modern life. Filled with a lack of time, stress, the abundance of allergens and pollutants in the environment and food, as well as numerous other unpleasant things that can cause indigestion, even without specific gastrointestinal disease. Heartburn is one of the most sensitive manifestations of dyspeptic symptoms. Of great importance in its development have bad habits (alcohol consumption, smoking) as well as receiving medications. It has long been used to relieve heartburn, antacids. However, taking the safe (non-specialist as it seems!) of medications in many cases may be not only harmful and even fatal effect ...

Dyspepsia of various etiologies define an important sector of the modern pharmacist. According to the literature on a daily basis in industrialized countries, symptoms of heartburn and related health problems point to 10% of the population every week - 30%, and monthly - 50%. Selective studies of individual regions of Russia exhibit periodic heartburn in 48.5% of men and 51.4% of women. But in general, people are constantly in need of taking antacids, according to various estimates, is the world's 12 to 280 million, of which 60 million people in the U.S. [1-3].

Heartburn (latin pyrosis) - a burning sensation behind the breastbone or in the epigastrium, often extending up to the throat due to throwing of gastric contents into the esophagus. Most often this condition in the medical practice associated with Gastaut-Esophageal Reflux Disease (GERD), in which it is permanent, but it may occur in otherwise healthy people. Factors contributing to heartburn in this case are: increased intra-abdominal pressure (obesity, pregnancy), lifestyle characteristics (physical inactivity, excess fat intake, eating "on the fly", overeating, poor nutrition, etc.), some bad habits (abuse spices, smoking, eating foods with excess caffeine, sweets, soft drinks, etc.), wearing tight clothes, taking some medications (expectorant reflex action, antibiotics, NSAIDs, calcium channel blockers, estrogens, antispasmodics, β-blockers, nitrates, anticholinergics, theophylline, etc.). Plays a role, and individual sensitivity to certain foods (citrus fruits, onions, garlic, tomato products - juices, pastas, sauces) [4-6].

Heartburn is often experienced by people with a particular pathology of the gastrointestinal tract. It is frequently observed in GERD, the occurrence of which the population reaches 40% in chronic gastritis type B and gastric or duodenal ulcer, chronic cholecystitis, hiatal hernia, gastrointestinal tract dyskinesia various functional and organic nature. From 40 to 90% of patients with these diagnoses have to take a different frequency - periodically or continuously - antacids.

A direct consequence of the constant heartburn is the development of specific diseases, the so-called "Barrett's esophagus" or Barrett’s syndrome. It is characterized by the inclusion of areas of abnormal columnar epithelium in the lining of the esophagus and is found in approximately 10% of patients with GERD, and in the general population comprises about 1% of the population. This complication is considered as a precancerous condition and is associated with an increased incidence of gastric cancer and adenocarcinoma of the lower third of the esophagus [2, 5, 6].

Of particular importance is heartburn, which is observed during pregnancy, where the safety of the medications have a special meaning. In the different age and ethnic groups, and depending on the time it is celebrated with a frequency of 30-50% to 80% of pregnant women. In the first half of pregnancy heartburn is caused by hormonal changes the body - increase in the blood concentration of progesterone, which has a direct relaxing effect on smooth muscle tone and increases the acidity of gastric juice. In the second half of pregnancy, in addition to this, affects a significant increase in intra-abdominal pressure due to the growth of the pregnant uterus. The special importance of antacids during pregnancy emphasizes the fact that they can not replace with H₂-blockers and proton pump inhibitors, which are contraindicated to the fetus [7, 8].

In this context, the safety profile of the most common antacids, especially used during pregnancy, given the nature of the OTC in many countries and advertising is of particular interest to the consumer. What we tried to analyze in this paper.

Traditionally used in antacids made by subdividing the main mechanism of action for two major groups - absorbed (Rennie, Gaviscon) and nonabsorbable (Almagel, Phosphalugel, Stomalox, Gastal) (Table 1). Acceptance of the medications of the first group contributes to fluid retention and disturbance of acid-base balance, which can fatally affect people with cardiovascular disease and pregnancy. Particular negative effect in this case have pregnant third trimester of pregnancy. The mechanism of fluid retention caused by absorption from the stomach of salts, resulting from inactivation of hydrochloric acid. This happens fairly quickly, dramatically increasing the content of the intravascular fluid. In many cases, it causes congestive heart failure, which can develop even in the absence of pathology of the heart (pulmonary edema in patients with acute glomerulonephritis, increased blood pressure in hypertension, etc.), including pregnant women. Particularly at risk are elderly patients with symptoms of heart failure [9, 10].

Table 1.

Classification of antacids

      Referring in greater detail defects of absorbed antacids should be noted the most important of them, which greatly reduces the safety of these medications, particularly in pregnant women. They are:

1. They are characterized by the phenomenon of rebound. The phenomenon of rebound ("acid rebound") - an increase in acid production in stomach at the end of medication action, which reduces the acidity. Is a physiological response to alkalization of the medium, which activates the secretion of HCl. Implemented by the stimulation of production of gastrin and the direct effect of calcium on the parietal cells of the stomach mucosa. Many medications in this group contribute to the mechanical distension of the stomach wall, which in itself is a potent stimulus of acid. Does not recommend this type of antacids in the nighttime, when the rebound phenomenon can not be neutralized by ingestion.

2. Suction antacids have a immediate and short-lived effect. On the one hand, the first support their widespread use and popularity, and, on the other hand, it compels to receive relatively large doses. That significantly increases the frequency of various side effects.

3. Alter the acid-alkaline balance in favor of metabolic and systemic alkalosis. Metabolic alkalosis - a condition caused by an increase of blood pH. Accompanied by a pressing headache, depression, gastrointestinal dyskinesias, heart disorders, nausea, impaired vision. Dangerous condition in patients with heart disease, and respiratory failure, nephrotic syndrome, cirrhosis of the liver and other metabolic alkalosis the transition into the systemic risk of the patient increases substantially. The first type is real alkalosis in healthy people. However, with increasing doses of antacids and increased risk of a second.

4. Slow down the evacuation of the contents of the stomach and intestines, which can cause a number of complications in elderly patients and pregnant women with a tendency to constipation.

From a clinical point of view of the possible side effects of absorbed antacids in various stages of pregnancy is realized through:

A. Worsening of symptoms "pyelonephritis pregnant" and effects of kidney failure.

B. Increased risk of miscarriage.

C. Effect on fetal calcium metabolism.

D. Interaction with the enzyme systems of the body.

E. The possibility of systemic alkalosis.

In connection with the listed side effects and possible complications associated with the mechanism of action of this group antacids they have long been positioned as undesirable or contraindicated for use in pregnant women, and older, and all patients with cardiac and respiratory failure and a host of other concomitant diseases and states [8, 11]. At present time, for reasons of safety of nonabsorbable antacids are preferred, which have a much smaller number of possible side effects. At the same time use in the medications of the group H₂-blockers and proton pump inhibitors (Gastromax, Nolpaza) or salts of aluminum (Maalox, Altacid, Alma-Gal) is also a limitation for certain categories of patients (primarily the elderly and pregnant women) . However, these effects are generally likely to occur at a sufficiently prolonged admission (weeks).

Regarding the group of nonabsorbable antacids should be noted that significant and severe adverse reactions when they are used much less developed. At the same time and they are not without some shortcomings that reduce the safety of a whole series of patients. They are:

1. The accumulation of Ca²⁺, Mg²⁺ and Al²⁺ at long-term use is dangerous for patients with renal insufficiency. Acceptance of aluminum-containing products is contraindicated in renal insufficiency of any origin. Aluminium and its salts are generally extremely dangerous for oral use, in connection with which almost all of the instructions inscribed medications recommended taking "no more than 4 days" (in the USA - 2 weeks). However, the acceptable level of safety is only available in single dose.

2. The possibility of encephalopathy and arthropathy with chronic administration of antacids, containing bismuth (Vikair, Vikalin).

3. Stone formation in the kidney as a result of silicon, a component of magnesium trisilicate (Gestid, Gelusil-lac).

4. Calcium carbonate is incompatible with dairy products, causing hypercalcemia and milk-alkali syndrome. Clinically it is manifested by nausea, vomiting, polyuria, and transient azotemia, which is very important for pregnancy, as well as for the elderly and children. It is worth mentioning that this does not prevent some manufacturers position their products as a drug of choice for treatment of GERD in infants (Gaviscon mint suspension).

5. Phosphate deficiency syndrome by reducing their absorption in the intestine and associated metabolic bone calcium (Alfogel, Phosphalugel).

Along with the above, an important role in individual patients can play:

A. Systemic toxicity of aluminum, mentioned above and is capable of producing irreversible changes in all parenchymal organs. The probability of this pathology is dramatically increased with chronic administration of aluminum-containing antacids (more than recommended 4-day period).

B. Increased motility of gastrointestinal tract magnesium salts that pregnant women can induce miscarriage and a number of other undesirable effects.

C. H₂-blockers classified FDA in category B at the risk of adverse effects on the fetus, indicating that not enough proof of their safety for use in pregnant women.

D. During pregnancy and a number of other states under the influence of proton pump inhibitors may develop hypochlorhydria and chronic pancreatitis. Under these conditions, is rapidly developing and dysbiosis can develop lesions of secondary infection [12, 13].

All of this should be remembered for a rational pharmaceutical care and early recognition of side effects of antacids. Characteristics of the main active ingredients nonabsorbable antacids given in table. 2. And in the Table. 3 summarizes the pharmacological effects of medications and compatibility with certain medications in this group.

Table 2.

Characteristics of some active ingredients nonabsorbable antacids

Table 3.

The pharmacological effects of certain nonabsorbable antacids

      In recent years, appeared on the market products outside the above classification, which have a high safety profile. For example, quite a successful combination of sufficient efficiency and almost complete absence of these mechanisms of adverse effects is an antacid drug Pepsan, Production Lab. Rosa-Phytopharma. It contains two active ingredients: gvayazulen, which has a regenerative, antibacterial and anti-inflammatory effect on mucous membranes and gastrointestinal tract dimethicone, which is docked through flatulence. In the latter case, it turns off the main path of stimulation of acid the stomach - a mechanical stretching of its walls, preventing the phenomenon of rebound. Go to the relative disadvantage of the drug include the relatively slow onset of effect. And by positive, besides those already mentioned above, the issue - including - in the form of a gel, which increases its koplaetnost and simplicity, as well as the more important advantages: does not contain undesirable for many patients of sugar does not affect the transit of intestinal contents, does not violate the suction other medications and does not interact with them, has no effect on calcium and phosphorus metabolism, which is important for pregnant women [7, 14].
      In the pharmaceutical care pharmacist antacids should always remember, "the warning signs" that are grounds for mandatory doctor's advice. These include: heartburn, which lasts more than 3 days., Its combination with abdominal pain, heartburn due to the ongoing weight loss or accompanied by shortness of breath, difficulty swallowing, sweating, caused by taking some specific LP, heartburn in the presence of black (tarry) stools.
      If you are using antacids should also be aware of possible side effects of this group of medications that, in most cases, are inseparable from their mechanism of action.
      Also, you should not forget that antacids are the occasional drug taking. Their use, especially absorbed, as a rule, is contraindicated in pregnancy, diseases of the cardiovascular system (heart failure, hypertension, etc.), as well as children.

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