What are the potential interactions between antacids and antibiotics. How do antacids affect antibiotic absorption. What precautions should be taken when using antacids and antibiotics together. What are the side effects of combining antacids and antibiotics.

Understanding Antacid and Antibiotic Interactions

The use of antacids and antibiotics together can lead to significant drug interactions that may impact the effectiveness of antibiotic treatment. These interactions primarily occur at the absorption stage in the gastrointestinal tract.

How do antacids interfere with antibiotic absorption. Antacids can form chelates or complexes with certain antibiotics in the gastrointestinal tract, delaying and reducing their absorption. This interaction is particularly notable with tetracyclines and clindamycin.

Why is the timing of antacid and antibiotic administration important. Taking antacids and antibiotics at different times can help minimize interactions. Generally, it’s recommended to separate the administration of these medications by at least 2 hours.

Specific Antibiotic Classes Affected by Antacids

Which antibiotic classes are most susceptible to antacid interactions. The following antibiotic classes are known to interact with antacids:

• Tetracyclines (e.g., doxycycline, minocycline)
• Fluoroquinolones (e.g., ciprofloxacin, levofloxacin)
• Macrolides (e.g., azithromycin, clarithromycin)

How do antacids affect tetracycline absorption. Antacids containing calcium, magnesium, or aluminum can bind to tetracyclines, forming insoluble complexes that are poorly absorbed. This can reduce the antibiotic’s effectiveness by up to 50%.

What impact do antacids have on fluoroquinolone absorption. Antacids can significantly reduce the absorption of fluoroquinolones, potentially leading to treatment failure. The interaction is particularly pronounced with aluminum- and magnesium-containing antacids.

Mechanisms of Antacid-Antibiotic Interactions

What are the primary mechanisms behind antacid-antibiotic interactions. The main mechanisms include:

1. Chelation: Formation of insoluble complexes between antibiotics and metal ions in antacids
2. pH alteration: Changes in stomach acidity affecting antibiotic solubility and absorption
3. Gastric emptying: Antacids may influence the rate at which antibiotics pass through the stomach

How does chelation affect antibiotic absorption. Chelation occurs when metal ions in antacids (such as aluminum, calcium, or magnesium) bind to certain antibiotics, forming complexes that are poorly absorbed by the body. This can significantly reduce the antibiotic’s bioavailability and effectiveness.

In what way does gastric pH influence antibiotic absorption. Some antibiotics require an acidic environment for optimal absorption. Antacids, by increasing stomach pH, can interfere with this process, leading to reduced antibiotic absorption and efficacy.

Precautions and Recommendations for Concurrent Use

What precautions should be taken when using antacids and antibiotics together. To minimize interactions and ensure optimal antibiotic efficacy:

• Separate the administration of antacids and antibiotics by at least 2 hours
• Consider alternative acid-reducing medications if necessary
• Consult with a healthcare provider or pharmacist for specific guidance
• Be aware of potential interactions and monitor for reduced antibiotic effectiveness

Are there any alternatives to antacids that may be safer to use with antibiotics. H2 receptor antagonists (e.g., ranitidine) or proton pump inhibitors (e.g., omeprazole) may have fewer interactions with antibiotics compared to traditional antacids. However, these medications should still be used with caution and under medical supervision.

Potential Side Effects and Risks

What are the potential risks of combining antacids and antibiotics. The primary risks include:

• Reduced antibiotic efficacy leading to treatment failure
• Increased risk of antibiotic resistance due to suboptimal drug levels
• Prolonged illness or infection due to inadequate treatment
• Potential for adverse effects from higher antibiotic doses if adjustment is needed

Can antacid-antibiotic interactions lead to antibiotic resistance. While not directly causing resistance, these interactions can result in subtherapeutic antibiotic levels in the body. This may create an environment where resistant bacteria are more likely to survive and proliferate, potentially contributing to the development of antibiotic resistance.

Impact on Specific Medical Conditions

How do antacid-antibiotic interactions affect patients with certain medical conditions. Patients with the following conditions may be particularly vulnerable to these interactions:

• Gastrointestinal disorders (e.g., GERD, peptic ulcers)
• Chronic kidney disease
• Compromised immune systems
• Elderly patients with multiple medications

Why are patients with gastrointestinal disorders at higher risk. These patients often require both antacids and antibiotics, increasing the likelihood of interactions. Additionally, altered GI function may further complicate drug absorption and efficacy.

How does chronic kidney disease influence antacid-antibiotic interactions. Patients with impaired renal function may have altered drug metabolism and excretion, potentially exacerbating the effects of antacid-antibiotic interactions. Close monitoring and dose adjustments may be necessary in these cases.

Other Drug Interactions with Antibiotics

Are there other common drug interactions with antibiotics besides antacids. Yes, antibiotics can interact with various medications, including:

• Oral contraceptives
• Anticoagulants (e.g., warfarin)
• Anticonvulsants (e.g., phenytoin, phenobarbital)
• Oral antidiabetic drugs (e.g., tolbutamide)

How do antibiotics interact with oral contraceptives. Some antibiotics, particularly broad-spectrum ones, can reduce the effectiveness of oral contraceptives by altering gut bacteria or increasing hormone metabolism. This may lead to unintended pregnancies if additional contraceptive measures are not used.

What is the mechanism behind antibiotic-anticoagulant interactions. Certain antibiotics can affect the metabolism of anticoagulants like warfarin, either enhancing or inhibiting their effects. This can result in an increased risk of bleeding or reduced anticoagulant efficacy, respectively.

Antibiotic Classes and Their Specific Interactions

Do different classes of antibiotics have unique interaction profiles. Yes, various antibiotic classes can have distinct interaction patterns:

• Aminoglycosides: Potential for increased nephrotoxicity when combined with certain diuretics
• Macrolides: Can inhibit liver enzymes, affecting the metabolism of drugs like statins
• Fluoroquinolones: May enhance the effects of oral anticoagulants and interact with antacids
• Sulfonamides: Can potentiate the effects of oral hypoglycemic agents and anticoagulants

How do macrolide antibiotics affect drug metabolism. Macrolides like erythromycin and clarithromycin inhibit cytochrome P450 enzymes in the liver, which are responsible for metabolizing many drugs. This can lead to increased blood levels and potential toxicity of affected medications.

Pharmacokinetic Considerations in Antibiotic Interactions

What pharmacokinetic factors influence antibiotic interactions. Several pharmacokinetic parameters play a role in antibiotic interactions:

1. Absorption: Interactions affecting drug uptake from the gastrointestinal tract
2. Distribution: Changes in protein binding or tissue penetration
3. Metabolism: Alterations in liver enzyme activity affecting drug breakdown
4. Excretion: Interactions impacting renal clearance or biliary excretion

How does protein binding affect antibiotic interactions. Highly protein-bound antibiotics may compete with other drugs for binding sites on plasma proteins. This can lead to increased free drug concentrations and potential toxicity or enhanced effects of the displaced medication.

What role does the cytochrome P450 system play in antibiotic interactions. Many antibiotics are either metabolized by or inhibit/induce cytochrome P450 enzymes. This can significantly affect the metabolism of other drugs, leading to interactions. For example, rifampicin is a potent inducer of CYP3A4, which can reduce the effectiveness of many medications metabolized by this enzyme.

Monitoring and Managing Antibiotic Interactions

How can healthcare providers effectively monitor and manage antibiotic interactions. To minimize risks and ensure optimal treatment outcomes, providers should:

• Conduct thorough medication reviews before prescribing antibiotics
• Utilize electronic prescribing systems with drug interaction alerts
• Educate patients about potential interactions and proper medication timing
• Monitor patients for signs of reduced antibiotic efficacy or increased side effects
• Consider therapeutic drug monitoring when appropriate
• Adjust dosages or switch medications if necessary

What role does therapeutic drug monitoring play in managing antibiotic interactions. Therapeutic drug monitoring involves measuring drug concentrations in the blood to ensure they remain within the therapeutic range. This can be particularly useful for antibiotics with narrow therapeutic windows or those prone to significant interactions, allowing for precise dose adjustments.

Future Directions in Antibiotic Interaction Research

What are some emerging areas of research in antibiotic interactions. Ongoing and future research in this field focuses on:

• Developing new antibiotic formulations less prone to interactions
• Investigating the impact of the gut microbiome on drug interactions
• Exploring personalized medicine approaches to predict and prevent interactions
• Studying the long-term consequences of chronic antibiotic use and interactions
• Improving electronic health record systems for better interaction detection and management

How might personalized medicine impact the management of antibiotic interactions. Advances in pharmacogenomics may allow healthcare providers to tailor antibiotic prescriptions based on an individual’s genetic profile, potentially reducing the risk of interactions and improving treatment outcomes. This could involve identifying genetic variants that affect drug metabolism or susceptibility to certain interactions.

What role could artificial intelligence play in predicting and preventing antibiotic interactions. AI and machine learning algorithms could analyze vast amounts of patient data, including medication histories, genetic information, and clinical outcomes, to predict potential interactions more accurately. This could lead to the development of sophisticated clinical decision support tools that help healthcare providers choose the safest and most effective antibiotic regimens for individual patients.

Patient Education and Adherence

How can patient education improve outcomes related to antibiotic interactions. Effective patient education can significantly reduce the risk of adverse interactions and improve treatment adherence. Key elements of patient education include:

• Explaining the importance of taking antibiotics as prescribed
• Providing clear instructions on medication timing, especially in relation to antacids or other interacting drugs
• Discussing potential side effects and warning signs to watch for
• Emphasizing the need to complete the full course of antibiotics
• Encouraging patients to maintain an up-to-date medication list and share it with all healthcare providers

What strategies can improve patient adherence to antibiotic regimens. To enhance adherence and minimize the risk of interactions:

1. Use simplified dosing schedules when possible
2. Provide written instructions and medication calendars
3. Utilize medication reminder apps or text message systems
4. Address potential barriers to adherence, such as cost or side effects
5. Involve patients in shared decision-making regarding their treatment plan

How does patient adherence impact the development of antibiotic resistance. Poor adherence to antibiotic regimens, often exacerbated by drug interactions, can contribute to the development of antibiotic resistance. When patients do not complete their prescribed course or take suboptimal doses due to interactions, it creates an environment where resistant bacteria are more likely to survive and multiply.

Adverse antibiotic drug interactions – PubMed

Review

. 1980 Jul;20(1):57-68.

doi: 10.2165/00003495-198020010-00004.

A J Bint, I Burtt

• PMID:

  6995091

• DOI:

  10.2165/00003495-198020010-00004

Review

A J Bint et al.

Drugs.

1980 Jul.

. 1980 Jul;20(1):57-68.

doi: 10.2165/00003495-198020010-00004.

Authors

A J Bint, I Burtt

• PMID:

  6995091

• DOI:

  10. 2165/00003495-198020010-00004

Abstract

There is enormous potential for drug interactions in patients who, today, often receive many drugs. Antibiotics are prominent amongst the groups of drugs commonly prescribed. Many interactions take place at the absorption stage. Antacids and antidiarrhoeal preparations, in particular, can delay and reduce the absorption of antibiotics such as tetracyclines and clindamycin, by combining with them in the gastrointestinal tract to form chelates or complexes. Other drugs can affect gastric motility, which in turn often controls the rate at which antibiotics are absorbed. Some broad spectrum antibiotics can alter the bacterial flora of the gut which may be related to malabsorption states. The potentiation of toxic side effects of one drug by another is a common type of interaction. Antibiotics which are implicated in this type of interaction are those which themselves possess some toxicity such as aminoglycosides, some cephalosporins, tetracyclines and colistin. Some of the most important adverse interactions with antibiotics are those which involve other drugs which have a low toxicity/efficacy ratio. These include anticoagulants such as warfarin, anticonvulsants such as phenytoin and phenobarbitone and oral antidiabetic drugs like tolbutamide. Risk of interaction arises when the metabolism of these drugs is inhibited by liver microsomal enzyme inhibitors such as some sulphonamides and chloramphenicol, or is enhanced by enzyme inducers such as rifampicin.

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Antacid-Simethicone Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

This medication is used to treat the symptoms of too much stomach acid such as stomach upset, heartburn, and acid indigestion. It is also used to relieve symptoms of extra gas such as belching, bloating, and feelings of pressure/discomfort in the stomach/gut. Simethicone helps break up gas bubbles in the gut. Aluminum and magnesium antacids work quickly to lower the acid in the stomach. Liquid antacids usually work faster/better than tablets or capsules.This medication works only on existing acid in the stomach. It does not prevent acid production. It may be used alone or with other medications that lower acid production (including h3 blockers such as cimetidine/ranitidine and proton pump inhibitors such as omeprazole).If you are self-treating with this medication, carefully read the package instructions before you start using this product to be sure it is right for you. Some products have similar brand names but different active ingredients with different uses. Taking the wrong product could harm you. Ask your pharmacist if you have any questions about your product or its use.

How to use ANTACID WITH SIMETHICONE Suspension, (Final Dose Form)

Take this medication by mouth, usually after meals and at bedtime as needed. Follow all the directions on the product package or use as directed by your doctor. If you have any questions, ask your doctor or pharmacist.

If you are taking the chewable tablets, chew thoroughly before swallowing, then drink a full glass of water (8 ounces or 240 milliliters).

If you are using the liquid form of this medication, shake the bottle well before pouring each dose. Measure the dose out carefully using a medication spoon/cup. Do not use a household spoon because you may not get the right dose. Refrigerating the suspension may improve the flavor. Do not freeze. The liquid form works best if taken without other fluids. You can mix your dose with a little water if needed.

This product may react with other medications (including digoxin, iron, pazopanib, tetracycline antibiotics, quinolone antibiotics such as ciprofloxacin), preventing them from being fully absorbed by your body. Talk with your doctor or pharmacist about how to schedule your medications to prevent this problem.

If your acid problems last or get worse after you have used this product for 1 week, or if you think you have a serious medical problem, get medical help right away. If you are using this medication regularly on a daily basis for more than 2 weeks, you may have a medical problem that needs different treatment. Ask your doctor whether this is the right medication for you.

Side Effects

Nausea, constipation, diarrhea, or headache may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

The magnesium in this product can cause diarrhea. Using an antacid that contains only aluminum along with this product can help control diarrhea. The aluminum in this product can cause constipation. To minimize constipation, drink plenty of fluids and exercise. Diarrhea is more common with this product than constipation.

If your doctor has directed you to use this medication, remember that your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Aluminum-containing antacids bind to phosphate, an important body chemical, in the gut. This can cause low phosphate levels, especially if you use this medication in large doses and for a long time. Tell your doctor right away if you have any of the following symptoms of low phosphate: loss of appetite, unusual tiredness, muscle weakness.

Tell your doctor right away if you have any serious side effects, including: dizziness, fainting.

Get medical help right away if you have any very serious side effects, including: slow/shallow breathing, slow/irregular heartbeat, mental/mood changes (such as confusion), deep sleep, pain with urination.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before taking this product, tell your doctor or pharmacist if you are allergic to aluminum hydroxide; or to magnesium; or to simethicone; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

If you have any of the following health problems, consult your doctor or pharmacist before using this product: frequent alcohol use, dehydration/fluid restriction, kidney problems (including kidney stones).

This medicine may contain aspartame. If you have phenylketonuria (PKU) or any other condition that requires you to restrict your intake of aspartame (or phenylalanine), consult your doctor or pharmacist about using this drug safely.

This medicine may contain sugar. If you have diabetes, consult your doctor or pharmacist about using this drug safely.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

This medication may pass into breast milk. Consult your doctor before breast-feeding.

Interactions

See also How to Use section.

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Some products that may interact with this drug are: phosphate supplements (such as potassium phosphate), sodium polystyrene sulfonate.

Antacids can interfere with the absorption of many other drugs. Be sure to check with your pharmacist before taking antacids with any other medication.

Does ANTACID WITH SIMETHICONE Suspension, (Final Dose Form) interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

Keep all medical and lab appointments.

Lifestyle changes such as stress reduction programs, stopping smoking, limiting alcohol, and diet changes (such as avoiding caffeine, fatty foods, certain spices) may increase the effectiveness of this medication. Talk to your doctor or pharmacist about lifestyle changes that might benefit you.

If you are taking this product on a regular schedule and miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Store at room temperature away from light and moisture. The liquid product may be stored in the refrigerator to improve taste. Do not freeze. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Clinical use of the antacid magaldrate in the treatment of acid-related diseases

It is known from the history of medicine that antacids have been used for therapeutic purposes for more than one century. It can be assumed that they were used to relieve heartburn, pain behind the sternum and in the upper abdomen, which corresponds to the clinical manifestations of acid-dependent diseases (ADD). Now the concept of SCZ unites a whole group of diseases of the upper gastrointestinal tract (GIT), in the development of which the peptic factor is necessarily present, in a number of diseases it can play a leading role in their development. Among these diseases should be called gastric ulcer (GU), duodenal ulcer (DU), gastroesophageal disease (GERD), gastritis (reflux gastritis), Zollinger-Ellison syndrome and other endocrine tumors. Diseases such as pancreatitis, non-steroidal anti-inflammatory drug (NSAID)-induced gastropathy, and certain symptomatic gastrointestinal disorders can also be considered as SCZ. Already one list of these diseases indicates a very high prevalence of CVD and their clinical manifestations. For example, manifestations of GERD occur in almost ½ of the adult population of the globe [1].

Antacids as alkalizing agents were widely used in gastroenterology throughout the 20th century. But only the creation of drugs H ₂ -blockers of histamine receptors and proton pump inhibitors (PPIs) radically changed the situation with the treatment of SCZ, led to a revision of the tactics and schemes for their treatment. Antacids for some time dropped out of the arsenal of doctors who gave a fair preference to drugs – PPIs. Omeprazole and its analogues have become widely used in the treatment of peptic ulcer (PU), especially in cases of PU associated with Helicobacter pylori [2]. Against the backdrop of the obvious successes of anti-Helicobacter pylori therapy, data on the increasing resistance of Helicobacter pylori to a number of PPIs, as well as side effects associated with taking antibiotics, gradually accumulated [3, 4]. These data contributed to a new surge of interest of a number of gastroenterologists in the possibility of using antacids in the treatment of PU and other CVDs [5, 6]. It should be noted that Helicobacter pylori , according to modern views, is the main triggering factor in the development of PU, however, in a number of cases, it is not possible to establish the role of this pathogen in the development of erosive and ulcerative lesions of the mucous membrane. In this regard, the role of Helicobacter pylori in the development of PU is the subject of scientific discussions. Here it is appropriate to recall the existence of symptomatic ulcers (stress, medicinal, endocrine), in the origin of which completely different mechanisms of ulcer formation are involved. Separately, ulcers, erosions and gastropathy induced by NSAIDs can be considered. In the treatment of these diseases, antacids find their place, usually playing an auxiliary role in complex therapy.

The therapeutic effect of antacids is based on the chemical neutralization of hydrochloric acid and the binding of pepsin in the gastric lumen. In addition, modern antacids have important additional properties, such as preventing the back diffusion of hydrogen ions, cytoprotection, adsorption of pepsin, bile acids and lysolecithin, and normalization of the gastric evacuation function. The listed properties inherent in modern antacids make them pharmacologically active against many CCs [7].

Antacids are usually divided into two groups: absorbable and non-absorbable. Absorbable antacids, easily soluble in gastric juice, include sodium bicarbonate, magnesium oxide, magnesium carbonate, calcium carbonate. Non-absorbable antacids are presented as monocomponent preparations (aluminum phosphate, aluminum hydroxide, magnesium hydroxide, magnesium trisilicate), and combined agents (aluminum-magnesium compounds, they are also with additives in the form of alginate, simethicone, etc.). Currently, due to the large number of various side effects, absorbable antacids are practically not used. An exception is a mixture or tablets of rennie (calcium carbonate and magnesium carbonate), which can be used once for heartburn on the principle of self-treatment [1].

We can say that almost all modern antacids are based on various combinations of aluminum and magnesium. The mechanism of their action is associated with the adsorption of hydrochloric acid, so the effect occurs more slowly than that of absorbed antacids, but lasts longer (up to 3 hours). Other additional positive properties of modern antacids were discussed above. It is thanks to the complex of these qualities that it became possible not only to use antacids in the treatment of CVD as additional means, but also to successfully use them as monotherapy for Ya. B. One of these antacids is the drug Maalox, which has long been used in our country. Maalox refers to combined agents, its components are magnesium hydroxide and aluminum hydroxide hydrate (algeldrate). Due to a number of positive qualities (antisecretory, cytoprotective, etc.), Maalox has been widely used in clinical practice in recent decades in the treatment of SCZ and Ya.B. It has been shown that in the treatment of PU, Maalox can be successfully used both as an additional agent to the complex of antiulcer drugs, and as a monotherapy [8].

This article discusses the pharmacological and clinical aspects of the use of another aluminum-magnesium compound, which is increasingly used in the practice of gastroenterologists in the US and Europe, Russian doctors are also familiar with it. This is a non-absorbable antacid magaldrate. This compound (aluminum magnesium hydroxide sulfate 5:10:31:2) has all the qualities of a modern antacid [9-11]. Magaldrate effectively neutralizes free hydrochloric acid (HCl) of the stomach without causing secondary hypersecretion of gastric juice (the “acid rebound” phenomenon), has an enveloping and adsorbing effect on pepsin, binds bile acids and lysolecithin. The latter are adsorbed quickly and for a long time (2 hours), due to which the gastric mucosa is additionally protected. The possibility of a “fast” and “delayed” (long-term) effect in the implementation of the drug’s action is being considered [10]. In the first variant, the speed of action is explained by the antacid properties and the structure of the drug. Additional long-term effects are made up of auxiliary reactions, they occur during the course use of the drug (adsorption of bile acids and lysolecithin, blockade of H ₂ histamine receptors, etc.). The most important link in the action of magaldrate is its cytoprotective properties [12]. Magaldrate stimulates the synthesis of prostaglandins (primarily prostaglandin E ₂ ) in the gastric mucosa, has a moderate antioxidant effect, and is able to reduce the level of lipid peroxidation. A number of authors [13, 14] proved that magaldrate to a certain extent has the properties of a blocker of H ₂ -histamine receptors, and it is comparable in terms of the effectiveness of duodenal ulcer healing with cimetidine. So, in the work of S. Zaterka et al. [13] proved almost equivalent efficacy of cimetidine (800 mg) and magaldrate in the form of a gel (40 ml/day). Patients with duodenal ulcers were treated for 8 weeks. During this period, ulcers healed in 88% of patients treated with cimetidine, and in 81% of patients treated with magaldrate.

The cytoprotective properties of magaldrate were confirmed in studies on various models of the development of gastric ulcers in rats. Magaldrat protected the stomach of rats from ulcers caused by ethanol, cold stress, indomethacin, acetylsalicylic acid, and cysteamine. During these experiments, a protective increase in the secretion of gastric mucus was recorded [15]. Experiments on dogs have shown that magaldrate inhibits the absorption of the ulcerogenic indomethacin and a number of NSAIDs in the blood of animals. The protective properties of magaldrate include its adsorption of bile acids and lysolecithin, active substances that promote erosive processes in the gastroduodenal mucosa. In addition, this antacid has antioxidant, antihistamine and anti-inflammatory effects, it also stimulates the processes of regeneration, cell proliferation and angiogenesis in the area of ​​ulcers. To what has been said, it must be added that in the middle of 9In the 0s of the last century, it was suggested that antacids such as magaldrate contribute to the eradication of the bacterium Helicobacter pylori , which largely determines the occurrence and development of PU [11]. Thus, it becomes obvious that magaldrate has multidirectional, multitarget properties, which are implemented in therapeutic use in the pathology of a number of diseases of the upper gastrointestinal tract, primarily PU and other SCs [10, 16].

The above data on the multilateral effects of magaldrate can be explained by the use of an original layered (network) structure in the development and creation of the drug [11, 12, 16]. Since magalrate is composed of mixed crystals of aluminum and magnesium hydrochlorides in the form of lattice layers, it reacts with the acid in stages. The crystal lattice dissolves gradually, which contributes to the slow release of aluminum and magnesium ions, which settle on the surface of the mucosa. Magalrate acts as an acid buffer and maintains a stable pH level within the ideal therapeutic range, namely between 3 and 5. Thus, the pharmacological activity of magalrate is determined precisely by the layered structure, and not by the chemical properties of the components. This magaldrat differs from all other antacid drugs.

Due to its numerous pharmacological properties, magaldrate has long drawn the attention of gastroenterologists to the possibility of its use in the therapy of SCZ. In the countries of Western Europe, back in the mid-80s of the last century, studies were conducted that confirmed the therapeutic activity of antacid in the treatment of DU. In a comparative randomized study by S. Miederer et al. [17] studied the effectiveness of 5 known antacids (maaloxan, talcid, gelusil, compensan, and magaldrate) with similar acid-neutralizing effects in the treatment of 50 patients with DU in the acute stage. Control of scarring of ulcerative processes was carried out using esophagogastroduodenoscopy (EGDS). The highest frequency of scarring of ulcers was recorded in patients treated with magaldrate (91.6% after 2 weeks, 98.5% after 4 weeks). When used in the treatment of other antacids, lower rates of scarring were recorded. Several double-blind studies confirmed the high antiulcer activity of magaldrate in the treatment of patients with GU, which was practically not inferior to the effectiveness of H ₂ -histamine receptor blockers [18].

In our country, the use of drugs containing magaldrate began in the mid-90s of the last century, when the antacid Magalfil 800 (Germany) was submitted for clinical trials, the active ingredient of which was magaldrate. In the study of O.N. Minushkin and S.A. Bulgakov [9, 16] used an antacid at a dose of 4800 mg/day (2 tablets 3 times a day 1 hour after meals) in the treatment of 30 patients with exacerbation of DU and 1 patient with an ulcer in the pylorus. The control was carried out using EGDS, carried out after 2 and 4 weeks from the start of treatment. 2 weeks after the start of treatment, complete scarring of ulcers was observed in 19 (62%) patients, after 4 weeks – in 28 (91%). Most of the patients received Magalfil 800 as monotherapy, some patients received traditional antiulcer drugs based on the results of the first EGDS. Taking the drug led to the rapid disappearance of pain (in 25 people on average within 4.0 ± 0.3 days) and other manifestations of dyspepsia in most patients. Side effects were minimal: in 4 patients loosening of the stool was recorded, in 1 case there was a slight skin itch, stopped by antihistamines. In the course of the study, acid products were studied. Basal acid production during treatment with a new antacid decreased from 6.1±0.9up to 4.5±0.2 meq/h. The authors made conclusions about the effectiveness of Magalfil 800 in the treatment of exacerbation of DU (not associated with Helicobacter pylori ) and made recommendations for its clinical use. It is proposed to consider the drug as a basic agent for the treatment of DU in the acute stage in patients with a newly diagnosed ulcer up to 1 cm in size, rare recurrence and uncomplicated course. With a complicated course of DU and large ulcers, the drug is recommended as an additional agent for complex therapy [16, 19].

A number of other studies have also shown the possibility of using the drug Magalfil 800 as an antiulcer agent. In the work of V.D. Pasechnikova et al. [20] not only confirmed the ability of the drug Magalfil 800 to actively heal duodenal ulcers (monotherapy), but also proved the cytoprotective properties of magaldrate. The concentration of prostaglandins E ₂ and F ₂ α was studied in duodenal biopsies before and after treatment with antacid. Initially, the examined patients showed a decrease in both types of prostaglandins. During treatment with magaldrate, scarring of ulcers was observed, while the level of prostaglandins increased markedly. Prostaglandin E 9 level0009 2 increased by 86%, and F ₂ α increased by 220%.

The possibility of using magaldrate as a prophylactic and anti-relapse drug has been proven. In the work of V.V. Balykina et al. [21] Magalfil 800 containing magaldrate was prescribed to 50 patients with DU of frequently relapsing type in remission (after discharge from the hospital). Antacid treatment was carried out on an outpatient basis for a long time, for 1 year, under the control of endoscopy. Exacerbation of DU was recorded in 24% of patients, while the morphological substrate of the exacerbation was erosion of the duodenal mucosa, the clinical symptoms of the exacerbation were mild. In the remaining 76% of patients, no relapses were observed during the control period, while patients for therapeutic purposes took only Magalfil 800. The effective dose was 1600 mg / day (taking 2 tablets per day, 1 tablet in the morning and evening). Side effects from treatment occurred in 22% of patients (mostly loosening of the stool), drug withdrawal was not required. Based on the data obtained, the authors concluded that antacids based on magaldrate can be used to prevent erosive and ulcerative lesions of the gastrointestinal tract. At the same time, the positive result of long-term use of magaldrate in this case is more determined by the cytoprotective properties of the drug than by its antisecretory effect.

Foreign authors recommend preparations containing magaldrate for the prevention of stress gastric ulcers. In the study by R. Estruch et al. [22] assessed the severity of bleeding from the upper gastrointestinal tract in 100 patients with stress-induced ulcers while taking magaldrate (800 mg every 4 hours). The studies were conducted using placebo control in a hospital setting. Upper GI bleeding occurred in 11 of 48 placebo patients compared to 1 of 52 patients treated with magaldrate ( p \u003d 0.01). When endoscopy performed in patients of the placebo group, an acute ulcer was recorded in 2 patients and erosive and ulcerative lesions of the mucous membrane in 9. Of the 52 patients who took magaldrate, only 2 had moderately severe diarrhea. Based on the results of the work, the authors concluded that drugs with the active substance magaldrat contribute to the prevention of bleeding caused by stress-induced ulcers.

In the work of A.E. Karateeva and E.L. Nasonova [23] reported a positive experience in the treatment of manifestations of dyspepsia and gastropathy associated with the use of NSAIDs with antacid magaldrat in 30 patients with rheumatic diseases who were in a hospital. The intake of magaldrate contributed to the elimination of the manifestations of gastropathy – heartburn, nausea, pain in the epigastric region. There were no serious side effects as a result of taking the study antacid. GERD remains one of the common CVDs. The use of PPIs is recognized as a basic element of its treatment, however, when assessing satisfaction with the treatment of GERD, patients preferred complex therapy consisting of PPIs, prokinetics, and antacids/alginates. The possibility of using antacids containing magaldrate in the treatment of “refractory” GERD was reported by A.S. Trukhmanov and O.A. Gromov [14]. Own observations allow us to say that the use of magaldrate is quite fast (on the 3-4th day) and effectively relieves heartburn in PU combined with reflux esophagitis. In the treatment of non-severe GERD (without severe esophagitis), magaldrate can be considered as a symptomatic therapy. It may be useful in patients using a single application of an antacid for heartburn and epigastric discomfort (on-demand principle).

Assessing the frequency of side effects and their severity when taking magaldrate, we can conclude that loose stools and diarrhea are most often recorded. However, for a certain category of patients (elderly patients), this effect can even be regarded as positive, since antacids often cause constipation, and constipation is very typical for many elderly people [19]. Among other undesirable reactions, we point out manifestations of dyspepsia, discomfort and spasms in the epigastrium, allergies, and a taste of chalk in the mouth. The toxicity of magalrate for the human body is very low, even when taking 6 daily doses, the critical level of aluminum in the serum (100 ng / ml) in patients without impaired renal function was not recorded.

Despite the abundance of antisecretory pharmacological agents used in the treatment of CVD, antacids remain in the arsenal of gastroenterologists, a number of them are technologically improved, which gives them new medicinal qualities. This trend was also reflected in the magaldrata. Recently, the combined drug Antareit (JSC Valenta Pharma, Russia) has been developed and put into practice, in which magaldrate is combined with the siloxane polymer simethicone [10, 14]. The drug is produced in the form of chewable tablets containing 800 mg of magaldrate and 40 mg of simethicone. Simethicone has an anti-foaming effect, which is provided by its components: at least 91-99% polydimethylsiloxane and 4-7% silica. Simethicone is not absorbed when taken orally, is not metabolized, and is removed by the intestines unchanged. When moving through the alimentary canal, the substance exerts an antifoaming effect by draining liquid from the foam bubbles and by changing the surface tension of the bubbles. Foam from the intestine is removed mechanically during its peristaltic contractions.

Simethicone is widely used to remove gases during endoscopy, in preparation for colonoscopy and ultrasound examination of the abdominal cavity, which improves the quality of manipulations. Fermentative dyspepsia, intestinal dysbiosis, irritable bowel syndrome – all these diseases are accompanied by increased gas formation in the gastrointestinal tract, a feeling of fullness and discomfort. The same phenomena can also disturb practically healthy people with overeating, malnutrition, consumption of juices and carbonated drinks. Simethicone is characterized by another interesting feature. It is capable of exhibiting antibiotic properties against Helicobacter pylori , comparable to those of Gabeksat mesylate (a protease inhibitor) and the antifungal compound ketoconazole [10].

Thus, Antareit, while retaining numerous positive effects of magaldrate, has new additional therapeutic possibilities, which expands the list of diseases in which it is advisable to use drugs containing magaldrate. Antareit can be recommended for the treatment of almost all CVDs that occur with dyspeptic disorders, flatulence – bloating due to increased gas formation. A.S. Trukhmanov and O.A. Gromova [14] reported on the use of Antareit in a hospital setting in the treatment of a patient with refractory GERD. After examination (24-hour pH-impedancemetry), the diagnosis was clarified: non-erosive reflux disease, transient relaxation of the lower esophageal sphincter, duodenogastric reflux. Conducted antisecretory therapy, which included taking drugs rabeprazole 20 mg/day (4 weeks) and Antareyt 1-2 tablets after meals and heartburn. The authors positively assessed the inclusion of Antareit in complex therapy together with PPIs for the relief of GERD symptoms. Further testing of the effectiveness of this drug is required to develop optimal treatment regimens for major CVDs. It should be noted that in Russia, as well as in a number of European countries and the USA, antacids with the active ingredient magaldrate (for example, Riopan) are in free pharmacy sales.

It can be stated that researchers and doctors remain interested in the group of antacids, new innovative technologies for improving medicines are proposed, which leads to an increase in the effectiveness of the treatment of many gastroenterological diseases.

The author declares no conflict of interest.

The author declares no conflict of interest.

Credits

Bulgakov S.A. – Doctor of Medical Sciences, Prof.; https://orcid.org/0000-0002-9004-9400; e-mail: [email protected]

Bulgakov S.A. Clinical use of antacid magaldrate in the treatment of acid-related diseases. Evidence Based Gastroenterology . 2019;8(3):38-43. https://doi.org/10.17116/dokgastro20198031

Drug Compatibility | “Panacea”

Classification of antibacterial agents (according to Manten – Wisse)

Table 4. Incompatible drug combinations