Heerdin

Heerdine is a proton pump inhibitor drug.

Indications of the geerdine

Rabeprazole in the form of lyophilizate for injection solutions is used in case of inability to use this substance in oral form:

• exacerbated ulcer in the area of the duodenum gut or stomach, accompanied by erosions in severe degree and bleeding;
• short-term therapy with GERD with peptic ulcers and erosions;
• for the prevention of aspiration with acidic gastric juice;
• with gastrinoma.

Release form

Release in the form of lyophilizate for injection solutions, in a vial of 10 ml (inside 20 mg of rabeprazole). In a separate pack contains 1 bottle.

Pharmacodynamics

Drug-inhibitor element of H ⁺ -K ⁺ -ATPase. Inhibition of the activity of this enzyme inside the gastric lining facilitates the blocking of the final stage of the formation of hydrochloric acid. This effect depends on the size of the dosage and is able to cause suppression of stimulated and basal hydrochloric acid release (the type of stimulus does not matter at the same time).

Synthesis of rabeprazole is carried out with the participation of covalent binding to the proton pump of the covering cells. Against the backdrop of this process, an irreversible decrease in the amount of the released acid occurs. Its secretion can be carried out only with the participation of a newly formed proton pump. This allows us to conclude that the plasma pharmacokinetics of rabeprazole does not have a decisive influence on the antisecretory effect. The bioactive time of the active ingredient is significantly longer than its half-life. More important is the half-life of the proton pump (20-24 hours), and not half-life of rabeprazole.

The peak of the decrease in secretion can develop when rabeprazole reaches the lining cell at the exact moment when its activation takes place. To receive such effect it is possible at infusion of a medicine v / in a method. As a result, the proton pump, activated by the action of circadian rhythms (acetylcholine substance) or after ingestion of food (gastrin substance with histamine), is immediately synthesized with the molecule of the active component of the drug, thus stopping the production of hydrochloric acid.

The active component of the drug rapidly accumulates inside the acidic environment of the gastric lining cells, transforming there into an active form - by attaching the category of sulfamides to it. Has an interaction with cysteine proton pump.

The use of drugs in a daily dosage of 20 mg in the period of 2 weeks has no effect on the thyroid function, carbohydrate metabolism, and in addition, blood levels of substances such as cortisol, parathyroid hormone, LH and FSH, testosterone with estrogens, as well as cholecystokinin, prolactin , renin with glucagon and STH with aldosterone and secretin.

Pharmacokinetics

The medicine begins to act 1 hour after the injection, reaching its maximum after 2-4 hours. The level of average clearance after IV injection in the amount of 20 ml is 283 +/- 98 ml / minute. The half-life of this dosage is approximately 1.02 +/- 0.63 hours. Excretory activity of the stomach is restored 2-3 days after drug withdrawal.

The absolute bioavailability index after intravenous injection of 20 mg is approximately 100% (all molecules of the substance enter the lining cells). This indicator does not change after a multiple introduction. Synthesis with plasma protein - 97%. With multiple injection of drugs, pharmacokinetic characteristics remain linear (level of distribution volume, clearance and half-life do not depend on dose).

It is exposed to hepatic metabolism - it occurs with the subsequent formation of the main decay products - carbonic acid with thioether. Other decay products - such as dimethyl ether with a sulfone, as well as a mercapturic acid conjugate - have a low concentration.

The half-life of the serum is approximately 1 hour. About 90% of the dose is excreted in the urine, mainly in the form of 2 decay products: carboxylic acid with a mercaptopuric acid conjugate. A small part of the decay products is excreted with feces.

Dosing and administration

Injections of Geberdin IV in the method should be performed only in situations where it is not possible to take the drug orally. When receiving the possibility of taking the medicine inside, you must immediately cancel it in / in the introduction.

The recommended size of a daily dose is a single application of 20 mg. The solution is introduced exclusively in / in the method.

Before the injection, it is necessary to dissolve the lyophilizate in a special solvent (5 ml). To do this, you can use injection water or a solution of sodium chloride (0.9%). The procedure of administration is slow - about 5-15 minutes.

When using drugs in the form of infusion, the lyophilizate is also dissolved, first in injectable water (5 ml), and then transfer the resulting solution to a container with sodium chloride (0.9% solution, 100 ml) or glucose solution (5%; 100 ml). Before starting the infusion, a visual assessment of the dissolution of the powder is required to exclude the presence of sediment and a change in the color shade of the liquid, as well as its transparency. The medicine (in the amount of 100 ml) is introduced in the period of 15-30 minutes and is used for 4 hours.

Do not store the unused solution during the procedure.

Use of the geerdine during pregnancy

There have been no studies on the safety of the use of Gerdin by pregnant women, as a result of which it is forbidden to apply it in this period.

There is no information on the penetration of the active ingredient into the mother's milk. No corresponding tests have been performed, therefore, the drug is not prescribed for lactation.

Contraindications

Among the contraindications:

• intolerance to rabeprazole, as well as substituted benzimidazoles or other elements of the drug;
• it is forbidden to combine with atazanavir;
• since there is insufficient experience of using drugs in children, it is contraindicated in this age category.

Side effects of the geerdine

The drug often causes mild and weak side effects, which quickly disappear:

• invasive and infectious diseases: the emergence of infectious processes or the development of interstitial type pneumonia;
• lymphatic and systemic blood flow reactions: development of neutron, pancito-, thrombocyto-, leuko-, lymphopenia and erythrocytopenia, as well as leukocytosis, anemia (this includes the hemolytic form), and agranulocytosis;
• immune disorders: dry mouth mucous membranes, rashes, manifestations of hypersensitivity (including shock), anaphylactoid signs, facial swelling, urticaria, dyspnea and lowering blood pressure. Also common manifestations of allergy in acute form are noted, which usually pass after withdrawal of drugs;
• disorders of metabolic processes: the development of hyponatremia or hypomagnesemia, as well as anorexia;
• reactions of the psyche: sensation of excitement, drowsiness, confusion and nervousness, and in addition insomnia, delirium, depression and the state of coma;
• manifestations from the NA: dizziness, asthenia, a sense of disorientation, headaches, a feeling of weakness in the limbs and numbness, as well as hypodesis, speech disorder and weakening of the compression force;
• disorders on the part of the visual organs: problems with vision and an increase in IOP;
• disorders of vascular function: increased pressure, the appearance of peripheral edemas and palpitation;
• respiratory system reactions: bronchitis and pharyngitis with glossitis and sinusitis, and in addition a runny nose with cough, bronchial spasms and Quincke edema;
• disorders in the gastrointestinal tract: the appearance of nausea, constipation, abdominal pain, bloating, vomiting, diarrhea, eructations and dyspepsia. In addition, dry mouth mucosal and rash in the mouth, stomatitis, candidiasis, gastritis, esophagitis with enteritis, heartburn and cheilosis develop. There is a feeling of heaviness and overcrowding of the stomach, a disorder of taste buds and hemorrhoids;
• problems with the liver, as well as the system of ZHVP: the development of hepatitis (also its fulminant form), jaundice and hepatic encephalopathy (occasionally it occurred in people with hepatic cirrhosis), in addition, functional hepatic disorder;
• manifestations of the subcutaneous layer and skin: the appearance of erythema (also polyform type), rashes, pruritus, TEN and Stevens-Johnson syndrome, as well as hyperhidrosis, acute common manifestations of allergy and bullous reactions;
• musculature and bone structure: development of rhabdomyolysis, arthralgia or myalgia, as well as leg cramps, back pain or nonspecific pain;
• disorders of the function of the organs of urination and kidneys: tubulointerstitial nephritis, infectious diseases of the urinary ducts and kidney failure in acute form;
• violations in the work of reproductive organs: there is an increase in erection and gynecomastia;
• local manifestations and systemic disorders: the appearance of pain in the sternum and back, a feeling of weakness, malaise, fever, thirst and heat, and with it asthenia, hyperhidrosis, chills, alopecia and influenza-like syndrome, and reactions at the injection site;
• laboratory test data: an increase in the parameters of AST and ALT (liver enzymes), GGT, total cholesterol and bilirubin, and in addition, alkaline phosphatides, triglycerides, CK, TSH and urea nitrogen with uric acid. In addition, there is hyperammonemia, proteinuria, and with it weight gain and glucose level in the urine.

Interactions with other drugs

Rabeprazole is metabolized by the CYP-450 liver enzyme system - elements such as CYP2C19, and CYP3A4. The substance does not have drug-relevant or pharmacokinetic interactions with phenytoin, diazepam, warfarin, or theophylline (all of which are metabolized with the CYP-450 system).

Interactions provoked by oppression of the processes of gastric acid secretion.

Rabeprazole sodium contributes to a prolonged and powerful decrease in the production of hydrochloric acid. Because of this, the substance can interact with drugs, the absorption of which depends on the level of gastric pH. When a combination of Geerdin with itraconazole or ketoconazole, the plasma values of the latter may decrease, and when combined with digoxin, an increase in the latter is observed. Therefore, those who combine the above drugs with rabeprazole require constant monitoring during treatment - in order to adjust the dosage in time.

The combination of atazanavir (300 mg) / ritonavir (100 mg) with omeprazole (single 40 mg per day) or atazanavir (400 mg dose) with lansoprazole (a single 60 mg dose per day) significantly reduces the level of AUC atazanavir. The absorption of this component depends on the pH value. Similar results can be expected with other proton pump inhibitor drugs. Therefore, they (including rabeprazole) are not allowed to be used together with atazanavir.

When combined with food that contains a small amount of fat, the absorption of rabeprazole does not change. In the case of use with fatty dishes, absorption can be slowed down for 4+ hours, but its degree, as well as the peak concentration of the substance, do not change.

In vitro studies revealed that rabeprazole slows the metabolism of the substance cyclosporin. The inhibition rate in this case is similar to the level of inhibition by omeprazole.

Medicines that are forbidden to combine with the component rabeprazole: sulphate atazanavir - because its medicinal effect may be weakened. The antisecretory properties of rabeprazole increase the gastric acidity index and decrease the solubility of atazanavir sulfate, as a result of which its plasma level also decreases.

Medications prescribed with caution:

• digoxin and methyldigoxin - their indices inside the blood can increase. The anti-secretory effect of Geerdin helps to increase the value of gastric pH, which is why the absorption of the above substances is accelerated;
• gefitinib and itraconazole - it is possible to reduce the indices of these components inside the blood. An increased level of pH in the stomach results in the fact that the absorption of these elements slows down;
• Aluminum- and magnesium-containing antacid drugs - with the combination of rabeprazole and antacid agents, a decrease in the values of this substance is observed.

[1], [2]

Storage conditions

Heerdine is required to be kept out of reach of small children. The temperature level is a maximum of 25 ° C.

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Shelf life

Heyerdin can be used in the period of 2 years from the date of release of the drug.