Razol 20

Razol 20 is a medicinal preparation intended for use as an antiulcer. The action of its main pharmacologically active substance, rabeprazole, is that it inhibits the proton pump because of the inhibition of the enzyme H + -K + -ATPase in gastric parietal cells. As a result, the final stage of the processes in which hydrochloric acid is produced is blocked. This effect differs depending on the dose of the drug and as a result of its use, basal, as well as stimulated secretion of hydrochloric acid is exposed to oppression, which nature would not be an irritant.

This drug has such qualities as the ability to be almost fully absorbed in the gastrointestinal tract for the shortest time after ingestion. The actualization of the antisecretory action of the drug occurs in the first 60 minutes, and already after 2-4 hours from the moment when the initial dose was taken, there is a maximum in the decrease in the acid-base medium pH in the stomach. 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, as another advantage of Razol 20, it should be mentioned that its absorption is not affected by food, and the time at which food takes place during the day.

Indications Razol 20

Indications for use Razol 20 suggests the use of this medication mainly for short-term treatment of diseases, which include, in particular: gastroesophageal reflux disease, accompanied by the presence of ulcers and erosions; The patient has Zollinger-Ellison syndrome. In addition, this drug is also used as one of the preventive measures aimed at preventing aspiration with 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 stage of exacerbation and with the appearance of bleeding and the development of severe erosion. In such cases, the use of the drug in its oral dosage form is impossible, it is advisable to use it as a solution for injection by injection.

So, the indications for the use of Rasol 20 are mainly caused by the existence of one or another of the diseases in the patient that is characterized by an increased level of production of gastric acid 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.

[1], [2], [3], [4], [5], [6]

Release form

Form release Razol 20 is presented in the form of a powder from which a solution for injections is prepared. Powder is a completely freeze-dried lyophilized mass or almost white in color. A 20-milligram quantity of powder is contained in a glass vial. In a box of cardboard, depending on the packaging, there is 1 such bottle (No. 1) and 10 pieces of them - No. 10.

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

The main active ingredient of Razol 20 is rabeprazole. In the contents of each bottle there is 20 mg rabeprazole sodium. In addition, this form of release of this drug has a number of auxiliary components such as sodium hydroxide, manitol E 421.

[7]

Pharmacodynamics

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

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

This effect is achieved due to intravenous infusion introduction of the drug. As a consequence, binds the molecules of rabeprazole to the proton pump, which in turn causes the production of hydrochloric acid to cease. In an acidic environment in the parietal cells of the stomach, an accumulation of the active substance is formed in a short time, which is activated as a result of the addition of a sulfonamide group to it. Cysteines of the proton pump will be activated in the interaction.

When administered intravenously, the action of Razol 20 is revealed within 1 hour and comes to its maximum extent after 2 to 4 hours. The value of the average clearance for intravenous infusion in a dose of 20 ml is 283 ± 98 ml / min. The half-life of a 20-ml dose is intravenously characterized by an index of 1.02 ± 0.63 hours. After discontinuation of the use of the drug, the recovery of secretory activity occurs in the period from 2 to 3 days.

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

[8], [9], [10], [11], [12], [13]

Pharmacokinetics

Pharmacokinetics Rasol 20 is characterized by absolute bioavailability. This means that the molecules of the main active substance of the drug - rabeprazole in full 100% of them are able to reach the parietal cells. It should be noted that there is no dependence of the degree of bioavailability on whether this medication was administered once or repeatedly.

One of the key features is that the pharmacokinetic properties of Razol 20 are inherent in linearity. That is, depending on the amount of dosage, both the half-life period, and the clearance and volume of distribution, it is not inherent to undergo changes.

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 a very small amount, one can also observe the presence of other metabolites: dimethyl thioester, mercapturic acid conjugate, bellows.

Half-life requires a time period of approximately 60 minutes. A 90% dose is exposed to excretion in the urine, mainly as two metabolites: the mercaptopuric and carboxylic acid conjugate. To a small extent, metabolites leave the patient's body with feces.

Pharmacokinetics Rasol 20 in patients in old age is characterized by a longer excretion. The cumulative effect of the drug was not observed.

[14], [15], [16], [17], [18]

Dosing and administration

In the appointment of Razol 20, the following method of administration and dose of this medication is used.

First of all, it is necessary to take into account that intravenous injections and infusion are shown exclusively if it is impossible to use it in a dosage form intended for oral administration. When it becomes possible to prescribe oral intake of the drug, its administration intravenously should be discontinued.

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

Preparation of the injection solution is made by dissolving the contents of the ampoule in sterile water in an amount of 5 ml. The introduction should be done gradually over a period of 5 minutes to a quarter of an hour.

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

There are certain conditions for using a ready-made solution: it must be applied in a time interval not exceeding 4 hours from the time it was prepared. Another important point is that only a solution is allowed to enter, which has been pre-checked to ensure that there is no sediment in it, whether its color has changed, and whether there are any other changes. The correctly prepared solution is clear, colorless, and no foreign inclusions should be observed in it. A solution that has not been used within the time limit is recyclable.

Dosage and administration 20% of Razol 20, provided all the prescribed rules and the necessary conditions are observed in this regard, ensure the effectiveness of treatment with this drug.

[27], [28], [29]

Use Razol 20 during pregnancy

The use of Razol 20 during pregnancy and, in addition, during the period in which the infant is breastfed, refers to the contraindications to the medicament for this medication.

As shown by the results of specially conducted experimental studies, the drug is not fully retained by the placental barrier and in a certain amount can penetrate through it. It should be noted, however, that no violations of the fertile function or the occurrence of abnormalities in the processes of intrauterine development of the fetus have not been observed.

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

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

Contraindications

Contraindications to the use of Rasol 20 imply, first of all, that it is not permissible for it to be administered by those patients who have a hypersensitivity to rabeprazole or other active substances from the benzimidazole group.

To the category of drugs that are unacceptable for use, the preparation contains a certain type of insufficiency of the respiratory, renal and hepatic function that the patient has.

In view of the lack of clinical experience in treating children with drugs with rabeprazole, Razol is contraindicated in 20 children and adolescents under the age of 18 years.

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

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

Considering the contraindications to the use of Razol 20, we can not fail to mention a number of cases in which it is necessary to focus attention on the possibility of its use under certain existing factors. So excludes the purpose of the drug, diagnosed and identified in the patient's stomach cancer. Special care of therapy with the use of this remedy in its early stages is also called for by severe renal and hepatic dysfunctions.

[19], [20]

Side effects Razol 20

Side effects of Rasol 20 may occur as the appearance of various kinds of symptoms occurring from different organs and systems of the human body.

The gastrointestinal tract gives the following negative reactions to the drug: the appearance of dry mouth, belching, nausea, vomiting, the appearance of abdominal pain, the development of constipation and flatulence. Increases the activity of liver transaminases. Dyspeptic phenomena are possible, very rarely - stomatitis, gastritis, anorexia.

In the central nervous system, such violations of her activity as the occurrence of headache and dizziness, an agitated condition, insomnia, or vice versa - drowsiness may occur. It is not excluded that the patient can become depressed, his vision and taste can be disturbed.

Response of the respiratory system under the influence of Razol 20 is able to become the appearance of cough, the development of bronchitis, rhinitis, sinusitis and pharyngitis.

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

Other adverse manifestations can be noted as back pain, the appearance of an influenza-like syndrome, the development of myalgia, arthralgia and fever. In medical statistics, isolated cases were recorded, when due to the use of the drug in patients the body weight increased, there was a predisposition to increased sweating, neutropenia progressed, thrombocytopenia, leukocytopenia and leukocytosis.

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

[21], [22], [23], [24], [25], [26]

Overdose

With respect to what is characterized by an overdose of Razol 20, at the present time, no information is available. It is assumed that in case of exceeding the maximum admissible doses of the drug, one should expect an increase in the severity of the side effects that may occur under the influence of this medication.

To treat the adverse effects of an overly high dosage, Razol 20 resort to symptomatic therapeutic measures.

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

A specific antidote that may be appropriate when there is an overdose of this drug is not known to date.

[30], [31], [32], [33]

Interactions with other drugs

The interactions of Rasol 20 with other drugs are largely due to the pharmacological properties of rabeprazole as the main active active ingredient of this drug.

Like all other inhibitors of sodium proton pump, rabeprazole undergoes metabolism under the influence of enzymes of the hepatic cytochrome P450 system. There is no involvement of rabeprazole sodium in interactions of clinical significance, in which amoxicillin, warfarin, diazepam, theophylline and phenytoin are involved - that is, those drugs that metabolize the enzymes of the P450 system.

Since sodium rabeprazole has an effect leading to an active and prolonged decrease in the level of hydrochloric acid produced, it is possible to interact with those medicines in which their absorption properties are due to the acid-base balance of pH in the stomach. So in the combination formed with ketoconazole, the concentration of the latter in the blood plasma is reduced by 33%, and with respect to digoxin - by 22% its minimum concentration rises. On this basis, control of the combined use of Rasol 20 and the given preparations is required to determine the possible need to adjust the dosage.

The active metabolite of clarithromycin in combination with rabeprazole in plasma produces a large concentration of 50% for the first, and 24% for the second. This effect is seen as a positive result of the interaction during the eradication of H. Piori.

As part of the clinical study, no interactions were identified with antacids having a medicinal form of fluid. The clinical significance of interactions with the ingested food is also not established.

The influence exerted on metabolic processes of cyclosporine is similar to that of other inhibitors of the proton pump.

As a result of in vitro studies on human liver microsomes, it has been established that metabolism of rabeprazole sodium occurs under the action of the isoenzymes of the P450-CYP2C9, CYP3A system. Based on this, it can be argued that the ability of Razol 20 to interact with other drugs is low.

[34], [35], [36], [37], [38], [39]

Storage conditions

Storage conditions Razol 20 provide that the drug should be in a place inaccessible to children, which maintains a constant temperature of the environment at 25 degrees Celsius.

[40], [41], [42], [43], [44]

Shelf life

Shelf life 20 - 2 years from the date of manufacture specified by the manufacturer on the packaging. Do not use the drug after the end of this period.

[45], [46], [47], [48]