Pharmacological properties
Pharmacodynamics. The drug Riopan is an antacid with a layered lattice structure. The active ingredient of the drug Riopan is magaldrate. It contains aluminum and magnesium hydroxide in one molecule.
The drug Riopan reduces the amount of acid in the stomach and, depending on the dose and pH level, binds pepsin, bile acids and lysolecithin. Thus, the aggressive effect of gastric juice is eliminated and a layer is formed that protects its mucous membrane.
Acid binding is due to the binding of protons by sulfate and hydroxide ions in the middle layer of the lattice. During neutralization, the lattice structure is destroyed.
800 mg of anhydrous magaldrate neutralizes approximately 18-25 mg-eq of hydrochloric acid.
A Riopan 800 mg tablet corresponds in vitro to approximately 19 mg-eq of acid-neutralizing activity.
10 ml of Riopan, oral suspension, 800 mg corresponds in vitro to approximately 20 mg-eq of acid-neutralizing activity.
10 ml of Riopan oral suspension, 1600 mg corresponds in vitro to approximately 45.2 mg-eq of acid-neutralizing activity.
Since the pH level for 20-40 minutes is in the range of 3 to 5, which is therapeutically optimal, the use of the drug does not cause acid rebound.
Magaldrate does not affect gastric peristalsis.
Pharmacokinetics. Magaldrate is not absorbed in the gastrointestinal tract. During the neutralization process, a small amount of aluminum and magnesium ions is released, which, when passing through the intestine, are converted into sparingly soluble phosphates and then excreted in the feces. A certain amount of cations is absorbed. A slight increase in aluminum levels has been noted even in patients with normal renal function. Long-term use of antacids containing aluminum may lead to a decrease in phosphate absorption.
Indication
Heartburn, sour belching, feeling of heaviness and fullness in the stomach area.
Application
Riopan, chewable tablets. Adults: The recommended dose is 1 tablet of Riopan.
For minor complaints, the drug should be used 0.5-1 hour after eating or immediately if significant complaints appear.
Chewable tablets must be dissolved or chewed thoroughly.
The maximum daily dose of 8 chewable tablets (6.4 g of magaldrate) should not be exceeded.
Riopan oral suspension. Adults: the recommended dose is 1 sachet of Riopan.
For minor complaints, the drug should be used 0.5-1 hour after eating or immediately if significant complaints appear.
The Riopan sachet should be shaken before use, opened along the marked line. The contents of the sachet should be squeezed directly into the mouth and swallowed.
Do not exceed the maximum daily dose - 8 sachets of 800 mg or 4 sachets of 1600 mg (6.4 g of magaldrate).
If symptoms do not disappear after 2 weeks of treatment, you should consult a doctor for examination.
Elderly patients do not require dose adjustment.
Contraindication
Hypersensitivity to the active substance or other components of the drug. hypophosphatemia. habitual constipation. chronic diarrhea. severe abdominal pain of unspecified genesis. Alzheimer's disease. fructose and sorbitol intolerance (riopan, chewable tablets).
The drug can be used in patients with impaired renal function (creatinine clearance 30 ml/min) only with regular monitoring of magnesium and aluminum levels in the blood plasma. The level of aluminum in the blood plasma should not exceed 40 ng/ml.
Side effects
Side effects are classified by frequency of occurrence into the following categories: very common (≥10%), common (≥1% -10%), uncommon (≥0.1% -1%), rare (≥0.01% -0.1%), very rare (1/10,000, including isolated cases).
Gastrointestinal tract: often - soft stools (especially when using high doses); very rarely - diarrhea, constipation.
In patients with renal insufficiency or with prolonged use of high doses, an increase in the level of aluminum and magnesium in the blood is possible, which can lead to the accumulation of aluminum, mainly in nervous and bone tissues, and to phosphate deficiency.
Taste disturbances (chalky taste), nausea, vomiting, aluminum and/or magnesium intoxication, most often in patients with renal failure.
Dementia, worsening of Alzheimer's disease.
Osteomalacia, osteoporosis.
Hypersensitivity reactions, including itching, urticaria, angioedema and anaphylactic reactions, bronchospasm.
A decrease in phosphorus content in the body is also possible when using the drug in normal doses in patients whose diet is characterized by a low phosphorus content.
Increased resorption processes in bone tissue, hypercalciuria.
In patients with renal failure, prolonged use of aluminum and magnesium salts in high doses may lead to the development of encephalopathy, microcytic anemia, or worsen the course of dialysis-induced osteomalacia. Prolonged use or administration of the drug in high doses may cause phosphorus deficiency syndrome (loss of appetite, muscle weakness, weight loss).
Aluminum hydroxide may be dangerous for patients with porphyria who are on hemodialysis.
Riopan should not be used for more than 2 weeks without consulting a doctor. If the complaints persist for a long time and/or recur frequently, an examination should be performed to rule out the presence of a serious illness, such as a peptic ulcer or malignant tumor. A doctor should be consulted for a diagnosis.
In rare cases, after using the drug in high doses for several years, a decrease in calcium and phosphate absorption was observed, followed by osteomalacia.
The drug can be used in patients with impaired renal function (creatinine clearance 30 ml/min), especially those on dialysis, only with regular monitoring of magnesium and aluminum levels in the blood plasma. The level of aluminum in the blood plasma should not exceed 40 ng/ml. The drug is contraindicated in patients with Alzheimer's disease and should be used with caution in patients with metabolic disorders in bone tissue, patients on a low-phosphate diet to reduce the risk of aluminum intoxication, hypermagnesemia and hypophosphatemia. When using the drug for a long time and in high doses, it is necessary to regularly monitor the level of magnesium and aluminum in the blood serum.
In case of impaired renal function and prolonged use of the drug due to the content of aluminum salts, high levels of aluminum in the blood plasma and / or tissues (deposition of aluminum, primarily in nervous and bone tissues), as well as signs of overdose, may be noted. However, the results of studies indicate that the absorption of aluminum in patients with impaired renal function when using magaldrate is lower than when using aluminum salts. In addition, after short-term use of magaldrate in patients with normal renal function, no aluminum deposits are observed in the brain and bone tissue, in contrast to the use of aluminum salts without the use of antacids.
An increase in the pH of gastric juice increases the risk of reproduction of pathogenic microorganisms, and during artificial respiration may increase the incidence of nosocomial pneumonia in patients.
Since Riopan does not contain sugar and contains a small amount of sodium, it can be used to treat patients with diabetes and hypertension.
Aluminum hydroxide may cause constipation, and magnesium hydroxide may cause intestinal hypokinesia. High doses may cause or worsen intestinal obstruction and ileus, especially in patients at increased risk of such complications, such as patients with renal insufficiency or the elderly.
Patients should consult a doctor if they experience weight loss, difficulty swallowing, persistent abdominal discomfort, digestive disorders, new onset or worsening of existing digestive disorders, or renal failure.
With prolonged use of the drug, it is necessary to ensure the intake of sufficient phosphorus into the body, since aluminum hydroxide binds to phosphates and reduces their absorption from the digestive tract. Urinary excretion of calcium increases, which can lead to disturbances in the calcium-phosphate balance and create conditions for the development of osteomalacia (symptoms - complaints of weakness and pain in the bones).
During the treatment of patients with renal failure, it is necessary to monitor the dynamics of kidney function, ulcer size, diarrhea, and serum aluminum and magnesium levels.
Use during pregnancy and breastfeeding
Controlled studies of the effects of magaldrate in animals, as well as in humans during pregnancy, have not been conducted. Experiments on animals have shown that the use of aluminum salts has a negative effect on the fetus. To prevent aluminum intoxication, the drug is taken for a short time and in the lowest possible dose.
Aluminum compounds also pass into breast milk. Studies have shown that aluminum levels increase significantly after taking aluminum salts, while after taking magaldrate, due to the layered lattice structure, the aluminum level in the blood plasma does not differ from the level without the use of antacids.
It is necessary to take into account the content of aluminum and magnesium ions, which can affect transit in the gastrointestinal tract, namely:
Magnesium hydroxide salts can cause diarrhea; aluminum salts can cause constipation and worsen constipation, which is often observed during pregnancy.
Prolonged use and excessive doses of the drug should be avoided during pregnancy.
Breastfeeding should be discontinued during treatment.
Children: Currently, there are no systematic studies on the use and safety of the drug in children.
The ability to influence the reaction speed when driving vehicles or working with other mechanisms. Does not affect.
Interactions
A significant decrease in the absorption of antibiotics, including tetracycline, quinolone derivatives (ciprofloxacin, ofloxacin, norfloxacin), was observed, therefore it is not recommended to take antacids during treatment with these antibiotics. A slight decrease in the absorption of digoxin, isoniazid, iron preparations, chlorpromazine, benzodiazepines, Heno and ursodeoxycholic acid, indomethacin and cimetidine was also observed when these drugs were used simultaneously with Riopan.
Potential enhancement of the effect of coumarin anticoagulants has been noted.
Antacids containing aluminum should not be used in combination with acidic drinks (fruit juices, wines), effervescent tablets, citric and tartaric acid, as the absorption of aluminum salts in the intestines increases.
When used simultaneously with salicylates, the excretion of salicylates by the kidneys is increased due to alkalization of urine.
Overdose
No cases of overdose with Riopan have been recorded.
Symptoms of an overdose of aluminum hydroxide and magnesium hydroxide are manifested by rapid fatigue, facial flushing, exhaustion, muscle weakness, and inappropriate behavior.
Signs of metabolic alkalosis may also be observed: changes in mood or mental activity, numbness or pain in the muscles, nervousness and fatigue, slowed breathing, unpleasant taste sensations.
Treatment of magnesium overdose: rehydration, forced diuresis. Intravenous administration of calcium gluconate may be prescribed. In case of renal failure, hemodialysis or peritoneal dialysis is necessary.
Storage conditions
At a temperature not exceeding 25 °C. Riopan oral suspension Do not freeze.
UA / (PPIF) / 1018/0045.
