Nexium lyophilisate for preparation of intravenous solution 40 mg vial N10
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Active ingredients
Esomeprazole
Composition
1 fl. esomeprazole sodium 42.5 mg, which corresponds to the content of esomeprazole 40 mg. Excipients: sodium chloride - 8.6 mg, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / and.
Pharmacological effect
Inhibitor of H + -K + -ATP-ase. Esomeprazole is the S-isomer of omeprazole and reduces the secretion of hydrochloric acid in the stomach by specifically inhibiting the proton pump in parietal cells. S- and R-isomer of omeprazole have similar pharmacodynamic activity. Mechanism of action: Esomeprazole is a weak base, which passes into the active form in the highly acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, where it inhibits the proton pump - the enzyme H + -K + -ATF-ase. When this occurs, inhibition of both basal and stimulated secretion of hydrochloric acid. Effect on gastric acid secretion: After ingestion of esomeprazole at a dose of 20 mg or 40 mg for 5 days, patients with gastroesophageal reflux disease (GERD) with symptoms showed a decrease in the secretion of hydrochloric acid in the stomach for most of the day. The effect was the same with the on / in the introduction and when taken orally. Analysis of the pharmacokinetic data revealed the relationship between inhibition of acid secretion and plasma drug concentration after oral administration (the AUC parameter was used to estimate the concentration). Amid iv administration to healthy volunteers, 80 mg of esomeprazole for 30 min followed by prolonged iv infusion of esomeprazole at a dose of 8 mg / h for 23.5 h, the gastric pH was higher than 4 for an average of 21 h and higher 6 - within 11-13 hours. The therapeutic effect achieved as a result of inhibition of acid secretion. Healing of reflux esophagitis with the use of esomeprazole in a dose of 40 mg occurs in approximately 78% of patients after 4 weeks of therapy and in 93% of patients after 8 weeks of therapy (with ingestion). The effectiveness of the drug Nexium in bleeding from peptic ulcers was shown in a study of patients with bleeding from peptic ulcers, confirmed endoscopically. Other effects associated with inhibition of acid secretion: During treatment with drugs that lower the secretion of the gastric glands,the concentration of gastrin in plasma increases as a result of a decrease in the secretion of hydrochloric acid. Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA) increases. Increasing the CgA concentration may influence the results of examinations for the detection of neuroendocrine tumors. To prevent this effect, it is necessary to temporarily stop taking esomeprazole 5 days before the CgA concentration study. If during this time the concentration of CgA did not return to normal, the study should be repeated. In children and adult patients who received esomeprazole by mouth for a long time, there was an increase in the number of enterochromaffin-like cells, which is probably due to an increase in gastrin content in plasma. This phenomenon has no clinical significance. In patients who took orally for a long time, drugs that lower the secretion of the gastric glands, more often noted the formation of glandular cysts in the stomach. These phenomena are due to physiological changes as a result of inhibition of the secretion of hydrochloric acid. The cysts are benign and undergo a reverse development. The use of drugs that suppress the secretion of hydrochloric acid, including proton pump inhibitors, accompanied by an increase in the content of the microbial flora in the stomach, normally present in the gastrointestinal tract. The use of proton pump inhibitors may lead to a slight increase in the risk of gastrointestinal infections caused by Salmonella spp., Campylobacter spp. and probably Clostridium difficile in hospitalized patients. Children aged less than 1 month and 1-11 months of age with esomeprazole administered orally at a dose of 0.5 mg / kg and 1 mg / kg, respectively, showed a decrease in the average time percentage with an intragastric pH of less than 4. Safety profile of esomeprazole in children similar to that in adults.
Indications
Adults As an alternative to oral therapy when it is impossible to carry out: - with gastroesophageal reflux disease in patients with esophagitis and / or severe symptoms of reflux disease. - for the healing of peptic ulcers associated with the intake of NSAIDs. - for the prevention of peptic ulcers associated with taking NSAIDs in patients at risk. For the prevention of recurrence of bleeding from peptic ulcers after endoscopic hemostasis.Children and adolescents (aged from 1 year to 18 years) As an alternative to oral therapy when it is impossible to carry out: - for gastroesophageal reflux disease in patients with erosive reflux esophagitis and / or severe symptoms of reflux disease.
Contraindications
- children up to 1 year old - children and adolescents up to 18 years old for other indications, except gastroesophageal reflux disease - simultaneous use with atazanavir and nelfinavir - hypersensitivity to esomeprazole, substituted benzimidazoles or other ingredients of the drug. Precautions should be prescribed to patients with severe renal insufficiency.
Use during pregnancy and lactation
Currently, data on the use of esomeprazole during pregnancy is limited. Prescribe the drug during pregnancy should be only if the expected benefit to the mother outweighs the possible risk to the fetus. In experimental animal studies, no direct or indirect negative effect of Nexium on the development of the embryo or fetus was detected. The introduction of the racemic mixture of the drug also did not have any negative effects on animals during pregnancy, childbirth, as well as during postnatal development. No data on the use of the drug in women during lactation. It is not known whether esomeprazole is excreted in breast milk; therefore, Nexium should not be administered during breastfeeding. If necessary, therapy with Nexium during lactation should consider the possibility of stopping breastfeeding.
Dosage and administration
Adults As an alternative to oral therapy when it is impossible, it can be recommended in / in the introduction of esomeprazole in a dose of 20-40 mg 1 time / day. When GERD in patients with esophagitis, the recommended dose of Nexium is 40 mg 1 time / day. For the treatment of symptoms of GERD, the drug is prescribed at a dose of 20 mg 1 time / day. For the healing of peptic ulcers associated with the intake of NSAIDs, in patients at risk, esomeprazole in a dose of 20 mg is recommended 1 time / day. For the prevention of peptic ulcers associated with taking NSAIDs, the recommended dose of the drug Nexium 20 mg 1 time / day.As a rule, the period of parenteral use of the drug Nexium is short, the patient should be transferred as soon as possible to receive the drug inside. In order to prevent recurrence of bleeding from peptic ulcers, after endoscopic hemostasis, esomeprazole is recommended at a dose of 80 mg as an intravenous infusion for 30 minutes, followed by prolonged intravenous infusion of esomeprazole at a dose of 8 mg / h for 3 days (72 hours). After the end of parenteral therapy, antisecretory therapy is recommended to suppress acid secretion (for example, esomeprazole 40 mg 1 time / day for 4 weeks). Duration of injections and infusions In / in injections Dose 40 mg: a prepared solution of esomeprazole (5 ml, 8 mg / ml) is injected intravenously for at least 3 minutes. Dose 20 mg: half of the prepared solution of esomeprazole (2.5 ml, 8 mg / ml) is injected intravenously for at least 3 minutes. unused solution residues must be disposed of. In / in the infusion Dose 40 mg: the prepared solution of esomeprazole is administered in the form of / in infusion for 10-30 minutes. A dose of 20 mg: half of the prepared solution of esomeprazole is administered as an intravenous infusion for 10-30 minutes. Unused solution residues must be disposed of. Dose 80 mg: the prepared solution of esomeprazole is administered as an intravenous infusion over 30 minutes. Dose of 8 mg / h: the prepared solution of esomeprazole is administered as an extended intravenous infusion over 71.5 hours (8 mg / h). Children and adolescents (aged 1 to 18 years) As an alternative to oral therapy when it is impossible to carry out with gastroesophageal reflux disease in patients with erosive reflux esophagitis and / or severe symptoms of reflux disease, esomeprazole is administered parenterally 1 time per day as part of course of treatment of GERD (recommendations for dosing are presented in the table). As a rule, the period of parenteral use of the patient's Nexium drug should be switched to ingestion of the drug as soon as possible. Recommendations for dosing of esomeprazole for children and adolescents Age Treatment of erosive reflux esophagitis Symptomatic treatment of GERD 1-11 years old body weight less than 20 kg: 10 mg 1 time / day body weight & # 8805 .20 kg: 10 mg or 20 mg 1 time / day 10 mg 1 time / day 12-18 years 40 mg 1 time / day 20 mg 1 time / day B / in injection Dose 40 mg: a prepared solution of esomeprazole (5 ml, 8 mg / ml) is injected intravenously for not less than 3 minDose 20 mg: half of the prepared solution of esomeprazole (2.5 ml, 8 mg / ml) is injected intravenously for at least 3 minutes. Unused solution residues should be disposed of. Dose 10 mg: 1.25 ml of the prepared solution of esomeprazole (8 mg / ml) is injected intravenously for at least 3 minutes. Unused solution residues should be disposed of. In / in the infusion Dose 40 mg: the prepared solution of esomeprazole is administered in the form of / in infusion for 10-30 minutes. A dose of 20 mg: half of the prepared solution of esomeprazole is administered as an intravenous infusion for 10-30 minutes. Unused solution residues should be disposed of. A dose of 10 mg: a quarter of the prepared solution of esomeprazole is administered as an intravenous infusion over a period of 10-30 minutes. Unused solution residues should be disposed of. Special patient groups No dose adjustment of Nexium is required in patients with impaired renal function. Due to the limited experience of using the drug Nexium in patients with severe renal insufficiency, caution should be exercised in treating these patients. When GERD is not required dose adjustment of the drug in patients with impaired liver function of mild and moderate severity. In patients with severely impaired liver function, the maximum daily dose is 20 mg. When bleeding from peptic ulcers, dose adjustment of the drug Nexium in patients with mild or moderately impaired liver function is not required. In patients with severely impaired liver function, the following Nexium administration is recommended: 80 mg as an intravenous infusion for 30 minutes, followed by a prolonged intravenous infusion at a maximum dose of 4 mg / h for 71.5 hours. In elderly patients dosage adjustment required. Rules for the preparation and use of solutions for IV injection The degradation of the prepared solution mainly depends on the pH value, therefore, only 0.9% sodium chloride solution for IV injection should be used to dissolve the drug. The prepared solution should not be mixed or administered in conjunction with other drugs. Before use, the solution should be evaluated visually for the absence of visible mechanical impurities and discoloration. Only a clear solution can be used. The prepared solution is recommended to be injected immediately after preparation (from a microbiological point of view).The prepared solution should be used within 12 hours. Store at a temperature not exceeding 30 ° C. Unused solution residues should be disposed of in accordance with local requirements. The solution for IV injection (8 mg / ml) is prepared by adding 5 ml of a 0.9% sodium chloride solution for intravenous administration in a vial with 40 mg of esomeprazole. The diluted esomeprazole solution is a clear liquid from colorless to pale yellow color. A 40 mg solution for IV infusion is prepared by dissolving the contents of one vial with 40 mg of esomeprazole in 100 ml of a 0.9% sodium chloride solution for IV administration. A solution for intravenous infusion of 80 mg is prepared by dissolving the contents of 2 vials of esomeprazole 40 mg in 100 ml of a 0.9% sodium chloride solution for intravenous administration. The diluted esomeprazole solution for infusion is a clear liquid from colorless to pale yellow color.
Side effects
Below are the side effects noted in the IV and oral use of the drug Nexium during clinical trials and in post-marketing study of the drug Nexium for oral administration. The frequency of side effects is given in the form of the following gradation: very often (& # 8805 .1 / 10), often (& # 8805 .1 / 100, less than 1/10), infrequently (& # 8805 .1 / 1000, less than 1 / 100), rarely (& # 8805 .1 / 10 000, less than 1/1000), very rare (less than 1/10 000). On the part of the skin and subcutaneous tissues: often - reactions at the injection site *. Infrequently - dermatitis, itching, rash, urticaria. rarely - alopecia, photosensitivity. very rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. From the musculoskeletal system: rarely - arthralgia, myalgia. very rarely - muscle weakness. On the part of the nervous system: often - a headache. infrequently - dizziness, paresthesia, drowsiness. rarely - a violation of taste. Mental disorders: infrequently - insomnia. rarely - depression, agitation, confusion. very rarely - hallucinations, aggressive behavior. On the part of the digestive tract: often - abdominal pain, constipation, diarrhea, flatulence, nausea / vomiting. infrequently - dry mouth. rarely - stomatitis, gastrointestinal candidiasis. very rarely - microscopic colitis (confirmed histologically). On the part of the liver and biliary tract: infrequently - increased activity of liver enzymes. rarely, hepatitis (with and without jaundice). very rarely - liver failure, encephalopathy in patients with liver diseases. On the part of the reproductive system and the mammary gland: very rarely - gynecomastia. From the hemopoietic system: rarely - leukopenia, thrombocytopenia. very rarely - agranulocytosis, pancytopenia.Allergic reactions: rarely hypersensitivity reactions (for example, fever, angioedema, anaphylactic reaction / anaphylactic shock). On the part of the respiratory system: rarely - bronchospasm. On the part of the urinary system: very rarely - interstitial nephritis. On the part of the organ of vision: rarely - blurred vision. Metabolism: rarely - hyponatremia. very rarely - hypomagnesemia, hypocalcemia due to severe hypomagnesemia, hypokalemia due to hypomagnesemia. Other: Infrequent - peripheral edema. rarely - indisposition, sweating. * Reactions at the injection site were mainly observed in a clinical trial when prescribing a high dose of esomeprazole for 3 days (72 hours). In the preclinical study of esomeprazole for intravenous irritation was not detected, however, a weak inflammatory reaction was observed at SC injection of the drug, depending on the concentration of esomeprazole. It was reported on individual cases of irreversible visual impairment with the on / in the introduction of omeprazole to patients in critical condition, especially when administered in high doses, a causal relationship with taking the drug has not been established. Data on the safety of esomeprazole in children and adolescents are consistent with the safety profile in adults.
special instructions
Below are the side effects noted in the IV and oral use of the drug Nexium during clinical trials and in post-marketing study of the drug Nexium for oral administration. The frequency of side effects is given in the form of the following gradation: very often (& # 8805 .1 / 10), often (& # 8805 .1 / 100, less than 1/10), infrequently (& # 8805 .1 / 1000, less than 1 / 100), rarely (& # 8805 .1 / 10 000, less than 1/1000), very rare (less than 1/10 000). On the part of the skin and subcutaneous tissues: often - reactions at the injection site *. Infrequently - dermatitis, itching, rash, urticaria. rarely - alopecia, photosensitivity. very rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. From the musculoskeletal system: rarely - arthralgia, myalgia. very rarely - muscle weakness. On the part of the nervous system: often - a headache. infrequently - dizziness, paresthesia, drowsiness. rarely - a violation of taste. Mental disorders: infrequently - insomnia. rarely - depression, agitation, confusion. very rarely - hallucinations, aggressive behavior.On the part of the digestive tract: often - abdominal pain, constipation, diarrhea, flatulence, nausea / vomiting. infrequently - dry mouth. rarely - stomatitis, gastrointestinal candidiasis. very rarely - microscopic colitis (confirmed histologically). On the part of the liver and biliary tract: infrequently - increased activity of liver enzymes. rarely, hepatitis (with and without jaundice). very rarely - liver failure, encephalopathy in patients with liver diseases. On the part of the reproductive system and the mammary gland: very rarely - gynecomastia. From the hemopoietic system: rarely - leukopenia, thrombocytopenia. very rarely - agranulocytosis, pancytopenia. Allergic reactions: rarely hypersensitivity reactions (for example, fever, angioedema, anaphylactic reaction / anaphylactic shock). On the part of the respiratory system: rarely - bronchospasm. On the part of the urinary system: very rarely - interstitial nephritis. On the part of the organ of vision: rarely - blurred vision. Metabolism: rarely - hyponatremia. very rarely - hypomagnesemia, hypocalcemia due to severe hypomagnesemia, hypokalemia due to hypomagnesemia. Other: Infrequent - peripheral edema. rarely - indisposition, sweating. * Reactions at the injection site were mainly observed in a clinical trial when prescribing a high dose of esomeprazole for 3 days (72 hours). In the preclinical study of esomeprazole for intravenous irritation was not detected, however, a weak inflammatory reaction was observed at SC injection of the drug, depending on the concentration of esomeprazole. It was reported on individual cases of irreversible visual impairment with the on / in the introduction of omeprazole to patients in critical condition, especially when administered in high doses, a causal relationship with taking the drug has not been established. Data on the safety of esomeprazole in children and adolescents are consistent with the safety profile in adults.