Razol 20

Razol 20 is a medicinal product intended for use as an antiulcer agent. The action of its main pharmacologically active substance rabeprazole is that it inhibits the proton pump due to the fact that under its influence in the gastric parietal cells the enzyme H+-K+-ATPase is suppressed. As a result, the final stage of the processes in which hydrochloric acid is produced is blocked. This effect is dependent on the dose of the drug and as a result of its use, basal as well as stimulated secretion of hydrochloric acid is suppressed, regardless of the nature of the irritant.

This medicine has such qualities as the ability to be almost completely absorbed in the gastrointestinal tract within a very short time after oral administration. The antisecretory effect of the drug is actualized in the first 60 minutes, and after 2-4 hours from the moment the initial dose was taken, a maximum decrease in the acid-base pH in the stomach is noted. The optimization of the level of gastric acid secretion achieved in this way is stabilized and fixed after 3 days from the beginning of the treatment course.

And finally, another advantage of Razol 20 is that its absorption is not affected by food or the time of day at which food is consumed.

Indications Razol 20

Indications for use of Razol 20 suggest the use of this drug mainly for short-term treatment of diseases, which include in particular: gastroesophageal reflux disease, which is accompanied by ulcers and erosions; the presence of Zollinger-Ellison syndrome in the patient. In addition, this drug is also used as one of the preventive measures aimed at preventing aspiration of acidic gastric contents.

In addition, Razol 20 is included in the list of medical prescriptions for peptic ulcer disease of the duodenum or stomach at the acute stage and with the occurrence of bleeding and the development of severe erosions. In such cases, the use of the drug in its oral dosage form is impossible, it is advisable to use it in the form of a solution for injection.

Thus, indications for the use of Razol 20 are mainly caused by the existence of one or another of the diseases in the patient that are characterized by an increased level of gastric acid production with the possibility of its release into the gastrointestinal tract. The drug causes a positive tendency to restore and stabilize the acid-base balance in these internal organs.

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Release form

Release form Razol 20 is presented in the form of a powder, from which a solution for injections is prepared. The powder is a lyophilized mass of completely white color or having an almost white shade. A 20-milligram amount of powder is contained in a glass bottle. In a cardboard box, depending on the packaging, there is either 1 such bottle (No. 1), or 10 of them - No. 10.

On the market of medicinal products, the drug is often also found as lyophilized powder in bulk in 20 ml vials for the preparation of injection solution in packages No. 50 and No. 100, respectively. The in bulk form implies finished pharmaceutical products that are manufactured in compliance with all necessary technological processes by one manufacturer, the packaging, final packaging and labeling of which can be carried out by another company.

The main active ingredient of Razol 20 is rabeprazole. Each bottle contains rabeprazole sodium 20 mg. In addition, this form of release of this drug has a number of auxiliary components such as: sodium hydroxide, mannitol E 421.

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Pharmacodynamics

Pharmacodynamics Razol 20 has a number of features, the key one of which is the effect of the drug on the enzyme H+–K+–ATPase in parietal gastric cells. It consists in the fact that the drug acts as an inhibitor at the final stage of hydrochloric acid production. The consequence of this is that both basal and stimulated secretion of hydrochloric acid is inhibited.

Binding of rabeprazole in parietal cells by covalent bonds with the proton pump causes a decrease in the level of acid secretion, which is irreversible. Acid secretion becomes possible only with the participation of the newly formed proton pump. The effect of rabeprazole on the parietal cell at the time when it is activated causes the maximum degree of decrease in secretory function.

This effect is achieved by intravenous infusion of the drug. As a result, rabeprazole molecules bind to the proton pump, which in turn causes the cessation of hydrochloric acid production. In an acidic environment in the parietal cells of the stomach, an accumulation of the active substance is formed within a short time, which is activated as a result of the fact that a sulfonamide group is attached to it. The interactions involve the cysteines of the proton pump.

When administered intravenously, the action of Razol 20 is revealed within 1 hour and reaches its maximum degree of expression after 2 to 4 hours. The value of the average clearance with intravenous infusion at a dose of 20 ml is 283 ± 98 ml / min. The half-life of a 20-milliliter dose intravenously is characterized by an indicator of 1.02 ± 0.63 h. After stopping the use of the drug, the restoration of secretory activity occurs in a period of 2 to 3 days.

Pharmacodynamics of Razol 20 is such that its use in the designated daily dose of 20 mg during the treatment course of 14 days does not cause changes in the functioning of the thyroid gland, does not affect carbohydrate metabolism. Also, the drug does not change the concentration in which the hormones aldosterone, glucagon, cortisol, parathyroid hormone, prolactin, renin, secretin, testosterone, cholecystokinin, estrogen are present in the blood.

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Pharmacokinetics

Pharmacokinetics Razol 20 is characterized by absolute bioavailability. This means that the molecules of the main active substance of the drug - rabeprazole in their full 100 percent quantity are able to reach the parietal cells. It should be noted that the degree of bioavailability does not depend on whether this medication was administered once or repeatedly.

One of the key features is that the pharmacokinetic properties of Razol 20 are linear. That is, depending on the dosage, both the half-life and the clearance and distribution volume do not tend to change.

Metabolism of rabeprazole sodium in the human body occurs in the liver, where it undergoes biotransformation, during which the main metabolites are formed: carbonic acid and thioether. In extremely small quantities, the presence of other metabolites can also be observed: dimethylthioether, mercapturic acid conjugate, sylphon.

The half-life requires a period of approximately 60 minutes. The dose is 90% excreted in urine, primarily as two metabolites: a mercaptopuric acid conjugate and a carboxylic acid. A small amount of metabolites are excreted in the feces.

Pharmacokinetics of Razol 20 in elderly patients is characterized by a longer elimination. Cumulative effect of the drug was not observed.

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Dosing and administration

When prescribing Razol 20, the following method of administration and dosage of this medication is used.

First of all, it is necessary to take into account that intravenous injections and infusions are indicated only if it is impossible to use it in a medicinal form intended for oral administration. When it becomes possible to prescribe oral administration of the drug, its intravenous administration should be discontinued.

The solution prepared for infusion and injection should be administered only intravenously at the recommended daily dose of 20 milligrams.

The injection solution is prepared by dissolving the contents of the ampoule in sterile water in an amount of 5 ml. The injection should be carried out gradually over a period of time from 5 minutes to a quarter of an hour.

The infusion requires the following preparatory process: the contents of the ampoule must first be dissolved in 5 milliliters of sterile water, and then added to 100 ml of 0.9% sodium chloride infusion solution. The time interval during which the drug is administered must be 15-30 minutes.

There are certain conditions for using the ready-made solution: it must be used within a time period not exceeding 4 hours from the moment it was prepared. Another important point is that only a solution that has been previously checked for the absence of sediment, whether its color has changed, and whether there are any other changes may be introduced. A properly prepared solution is transparent, colorless, and should not contain any foreign inclusions. A solution that has not been used within the specified period is subject to disposal.

The method of administration and dosage of Razol 20, subject to all prescribed rules and necessary conditions, ensure the effectiveness of treatment using this drug.

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Use Razol 20 during pregnancy

The use of Razol 20 during pregnancy and also during the period when the baby is breastfed is one of the existing contraindications for this medication.

As the results of specially conducted experimental studies show, the drug is not completely retained by the placental barrier and can penetrate it in some quantities. It should be noted, however, that any disturbances of the fertile function or occurrence of deviations from the norm in the processes of intrauterine development of the fetus were not observed.

The presence of Razol 20 or any of its components may occur in the breast milk of a nursing mother.

Thus, the decision on whether it is advisable to use Razol 20 during pregnancy, lactation and breastfeeding should be taken with full responsibility and caution, having thoroughly considered and carefully weighed all the pros and cons. The fundamental factor in this matter is the expected greater positive result of its use for the mother, rather than the possibility of its harmful effect on the child.

Contraindications

Contraindications for the use of Razol 20 imply, first of all, that it is not allowed to be prescribed to those patients who have hypersensitivity to rabeprazole or other active substances from the benzimidazole group.

The drug is considered unacceptable for use if the patient has any kind of respiratory, renal or hepatic insufficiency.

Due to the lack of clinical experience in treating children with drugs containing rabeprazole, Razol 20 is contraindicated for children and adolescents under 18 years of age.

During pregnancy, the use of this drug may be justified only if the achievement of a positive effect for the mother is not associated with the risk of negative consequences for the development of the fetus.

When a woman is prescribed this medication during lactation and breastfeeding, breastfeeding of the infant should be discontinued during the course of such treatment.

Considering contraindications to the use of Razol 20, it is impossible not to mention a number of cases in which it is necessary to focus on the possibility of its use with some existing factors. Thus, the prescription of the drug, diagnosed and detected in the patient's stomach cancerous neoplasm, excludes. Severe renal and hepatic dysfunctions also call for special caution in therapy with the use of this remedy in its early stages.

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Side effects Razol 20

Side effects of Razol 20 may include the appearance of various types of symptoms occurring in different organs and systems of the human body.

The gastrointestinal tract produces the following adverse reactions to the drug: dry mouth, belching, nausea, vomiting, abdominal pain, constipation and flatulence. Liver transaminase activity increases. Dyspeptic symptoms are possible, very rarely – stomatitis, gastritis, anorexia.

The central nervous system may experience such disturbances as headaches and dizziness, agitation, insomnia or, on the contrary, drowsiness. It is possible that the patient may become depressed, and his vision and sense of taste may be impaired.

The response of the respiratory system under the influence of Razol 20 can be the appearance of a cough, the development of bronchitis, rhinitis, sinusitis and pharyngitis.

There is a possibility of allergic reactions to the use of this drug, appearing in the form of rashes on the skin, in rare cases accompanied by itching.

Other adverse effects may include back pain, flu-like syndrome, myalgia, arthralgia and fever. Medical statistics have recorded isolated cases where, as a result of using the drug, patients gained weight, developed a predisposition to increased sweating, and developed neutropenia, thrombocytopenia, leukopenia and leukocytosis.

If any side effects of Razol 20 are observed, its use should be discontinued.

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Overdose

There is currently no specific information regarding what characterizes an overdose of Razol 20. It is assumed that in case of exceeding the maximum permissible doses of the drug, one should expect an increase in the severity of side effects that may occur under the influence of this medication.

To treat the negative consequences of an excessively high dosage of Razol 20, symptomatic therapeutic measures are used.

Due to the high degree of binding of rabeprazole to proteins in blood plasma, dialysis to remove the drug from the patient's body appears ineffective.

A specific antidote that may be useful when overdose of this drug occurs is currently unknown.

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Interactions with other drugs

The interactions of Razol 20 with other drugs are largely determined by the pharmacological properties of rabeprazole as the main active ingredient of this drug.

Like all other sodium proton pump inhibitors, rabeprazole is metabolized by hepatic cytochrome P450 enzymes. Rabeprazole sodium is not involved in clinically significant interactions involving amoxicillin, warfarin, diazepam, theophylline, and phenytoin, drugs that are metabolized by P450 enzymes.

Since sodium rabeprazole has an effect that leads to an active and prolonged decrease in the level of produced hydrochloric acid, it is possible that it can interact with those medications whose absorption properties are determined by the acid-base balance indicator pH in the stomach. Thus, in a combination formed with ketoconazole, the concentration of the latter in the blood plasma decreases by 33%, and in relation to digoxin, its minimum concentration increases by 22%. Based on this, it is necessary to monitor the combined use of Razol 20 and the above drugs in order to identify the possible need to adjust the dosage.

The active metabolite of clarithromycin in combination with rabeprazole in the blood plasma forms a concentration that is 50% higher for the former, and 24% higher for the latter. This effect is seen as a positive result of interaction in the eradication of H.pylori.

In a clinical study, no interactions were found when used in combination with antacids in liquid dosage form. The clinical significance of interactions with food intake has also not been established.

The effect on the metabolism of cyclosporine is similar to that of other proton pump inhibitors.

In vitro studies on human liver microsomes have shown that sodium rabeprazole is metabolized by the P450 system isoenzymes – CYP 2C9, CYP 3A. Based on this, it can be stated that the interaction potential of Razol 20 with other drugs is low.

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Storage conditions

Storage conditions for Razol 20 stipulate that the drug should be kept in a place inaccessible to children, where a constant ambient temperature of 25 degrees Celsius is maintained.

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Shelf life

The shelf life of Razol 20 is 2 years from the date of manufacture indicated by the manufacturer on the packaging. The drug should not be used after this period.

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