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Esomeprazole is the S-isomer of omeprazole and reduces the secretion of hydrochloric acid in the stomach by specifically inhibiting the proton pump in the parietal cells of the stomach. S- and R-isomers of omeprazole have similar pharmacodynamic activity.
Mechanism of action
Esomeprazole is a weak base that becomes active in the highly acidic environment of the secretory tubules of the parietal cells of the gastric mucosa and inhibits the proton pump, the enzyme H + / K + - ATPase, and inhibition of both basal and stimulated secretion of hydrochloric acid occurs.
Effect on the secretion of hydrochloric acid in the stomach
After oral administration of 20 mg or 40 mg, the effect of esomeprazole develops within 1 hour. With daily intake of the drug for 5 days at a dose of 20 mg once a day, the average maximum concentration of hydrochloric acid after stimulation with pentagastrin is reduced by 90% (when measuring the concentration of acid 6-7 hours after taking the drug on the 5th day of therapy).
In patients with gastroesophageal reflux disease (GERD) and the presence of clinical symptoms after 5 days of daily oral administration of esomeprazole at a dose of 20 mg or 40 mg, the intragastric pH above 4.0 was maintained for an average of 13 and 17 hours from 24 hours. While receiving esomeprazole at a dose of 20 mg per day, the intragastric pH value above 4.0 was maintained for at least 8, 12, and 16 hours in 76%, 54%, and 24% of patients, respectively.
A correlation was found between the concentration of the drug in plasma and the inhibition of the secretion of hydrochloric acid (the AUC parameter, the area under the concentration-time curve, was used to estimate the concentration.
The therapeutic effect achieved by inhibiting the secretion of hydrochloric acid
When taking the drug in a dose of 40 mg, reflux esophagitis heals in approximately 78% of patients after 4 weeks of therapy and in 93% of patients after B weeks of therapy.
Treatment with esomeprazole at a dose of 20 mg 2 times a day in combination with appropriate antibiotics for one week leads to successful eradicationHelicobacter pylori approximately 90% of patients. Patients with uncomplicated peptic ulcer disease after a week-long eradication course do not require subsequent monotherapy with drugs that lower the secretion of the gastric glands to treat the ulcer and eliminate the symptoms.
The effectiveness of esomeprazole in bleeding from a peptic ulcer, confirmed endoscopically, has been shown.
Other effects associated with inhibition of the secretion of hydrochloric acid
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 can influence the results of examinations to identify neuroendocrine tumors. To prevent this effect, it is necessary to temporarily stop taking esomeprazole 5 days before the CgA concentration study.
In patients who received esomeprazole for a long time, there was an increase in the number of enterochromaffin-like cells, probably due to an increase in plasma gastrin concentration.
In patients taking drugs that lower the secretion of the gastric glands, over a long period of time, the formation of glandular cysts in the stomach is more often noted. These phenomena are due to physiological changes as a result of marked inhibition of the secretion of hydrochloric acid. The cysts are benign and reverse developed.
The use of drugs that suppress the secretion of hydrochloric acid in the stomach, including proton pump inhibitors, is 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 can lead to a slight increase in the risk of infectious diseases of the gastrointestinal tract caused by bacteria of the genus Salmonella spp. and Campylibacter spp and probablyClostridium difficile in hospitalized patients.
In the course of two comparative studies with ranitidine, esomeprazole showed the best efficacy in treating gastric ulcers in patients who received non-steroidal anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase-2 inhibitors (COX-2).
Gastroesophageal Reflux Disease (GERD)
Long-term supportive treatment after healing of erosive reflux esophagitis, prevention of relapse;
Symptomatic treatment of GERD.
Peptic ulcer and duodenal ulcer
in combination therapy:
Treatment of duodenal ulcers associated with Helicobacter pylori;
Prevention of recurrence of peptic ulcers associated with Helicobacter pylori.
Prolonged acid suppression therapy in patients who have undergone bleeding from peptic ulcers (after intravenous administration of drugs that lower the secretion of the gastric glands, to prevent relapse).
Patients for a long time taking NSAIDs
Treatment of gastric ulcers caused by taking NSAIDs;
Prevention of gastric and duodenal ulcers, due to the use of NSAIDs in patients at risk.
Zollinger-Ellison syndrome or other conditions characterized by pathological hypersecretion of the gastric glands, including idiopathic hypersecretion.
Dosage 20 mg
1 enteric film-coated tablet contains:
active ingredient: esomeprazole magnesium dihydrate 21.8 mg, calculated as esomeprazole 20 mg;
excipients: low substituted hyprolose (hydroxypropylcellulose) 14 mg, pregelatinized corn starch 37.2 mg, colloidal silicon dioxide 2 mg, mannitol 23 mg, sodium fumarate 2 mg, microcrystalline cellulose 140 mg;
film coating composition: Opadry clear 8 mg, including: [hypromellose (hydroxypropylmethylcellulose) 6.4 mg, macrogol (polyethylene glycol) 1.6 mg]. Acryl-From green 22 mg, including: [methacrylic acid and ethyl acrylate copolymer [1: 1] 14.52 mg, colloidal silicon dioxide 0.22 mg, sodium bicarbonate 0.22 mg, sodium lauryl sulfate 0.11 mg, iron yellow oxide 0.154 mg, indigocarmine dye 0.176 mg, brilliant blue dye 0.066 mg, talc 3.63 mg, titanium dioxide 2.904 mg]. Triethyl citrate 2 mg.
Esomeprazole is marketed under different brands and generic names, and comes in different dosage forms:
|Brand name||Manufacturer||Country||Dosage form|
|Emanera||Krka dd Novo mesto AO||Slovenia||capsules|
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Dosage and Administration
Inside The tablet should be swallowed whole, without chewing, with a sufficient amount of water.
Classification of the incidence of side effects of the World Health Organization (WHO):
very often - 1/10 of appointments (> 10%)
often from 1/100 to <1/10 of appointments (> 1% and
infrequently - from 1/1000 to 0.1% and
rarely from 1/10000 to 0.01% and
very rarely — astrota is unknown — cannot be estimated based on available data.
In each group, unwanted effects are presented in order of decreasing severity.
Nervous system disorders
Infrequently: drowsiness, sleeplessness, dizziness, paresthesias.
Seldom: excitement, confusion, depression.
Very rarely: aggressive behavior, hallucinations.
Disorders of the digestive system
Often: abdominal pain, diarrhea, flatulence, nausea, vomiting, constipation.
Infrequently: dry mouth, increased activity of "liver" enzymes.
Rarely: stomatitis, gastrointestinal candidiasis (GIT), hepatitis (with or without jaundice).
Very rare: liver failure, hepatic encephalopathy in patients with a history of liver disease, microscopic colitis.
Kidney and urinary tract disorders
Very rare: interstitial nephritis.
Frequency unknown: renal failure.
Reproductive system disorders
Very rare: gynecomastia.
Violations of the musculoskeletal system
Rarely: arthralgia, myalgia.
Very rare: muscle weakness.
Frequency unknown: fractures of the femoral neck, wrist bones, vertebrae.
Violations of the skin
Infrequently: itch, rash, urticaria, dermatitis, peripheral edema.
Rarely: alopecia, photosensitivity, malaise, excessive sweating.
Very rarely: Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme.
Disorders of the blood-forming organs
Rarely: leukopenia, thrombocytopenia.
Very rare: agranulocytosis, pancytopenia.
Violations of the sense organ
Infrequently: blurred vision.
Rarely: a violation of taste.
Rarely: hypersensitivity reactions (eg, fever, angioedema, anaphylactic reaction / anaphylactic shock).
Laboratory and instrumental data
Very rarely: hypomagnesemia, hypocalcemia due to severe hypomagnesemia, hypokalemia due to severe hypomagnesemia.
- Hypersensitivity to esomeprazole, substituted benzimidazoles or other components of the drug;
- Children's age up to 12 years (due to the lack of data on the efficacy and safety of the drug in this group of patients);
- Children's age from 12 to 18 years old by all indications, except GERD;
- Simultaneous reception with atazanavir and nelfinavir.
Severe renal failure (experience of use is limited).
Pregnancy and Lactation
There are currently insufficient data on the use of esomeprazole during pregnancy. The results of epidemiological studies of esomeprazole, which is a racemic mixture, showed no fetotoxic effect or impaired fetal development. In animal studies, no direct or indirect adverse effect on the development of the embryo or fetus was found, both with the administration of esomeprazole and with the administration of the racemic mixture. Pregnant women should be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus. It is not known whether esomeprazole is excreted in breast milk, so the drug should not be used during breastfeeding
Currently, cases of overdose of the drug esomeprazole are described extremely rarely.Oral administration of esomeprazole at a dose of 280 mg was accompanied by general weakness and symptoms of the gastrointestinal tract. Single dose of 80 mg of esomeprazole did not cause any negative effects.
Treatment: The specific antidote is unknown. Hemodialysis is ineffective. In case of overdose, symptomatic and general maintenance therapy is recommended.
- Brand name: Esomeprazole
- Active ingredient: Esomeprazole
- Manufacturer: Canonpharma
- Country of Origin: Russia
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- Mechanism of the Asymmetric Sulfoxidation in the Esomeprazole Process: Effects of the Imidazole Backbone for the Enantioselection
- ChemInform Abstract: An Efficient Procedure for the Synthesis of Esomeprazole (II) Using a Titanium Complex with Two Chiral Ligands.
- Racemization of the gastrointestinal antisecretory chiral drug esomeprazole magnesium via the pyramidal inversion mechanism: A theoretical study
- Preparation of esomeprazole zinc solid dispersion and study on its pharmacokinetics
- Population pharmacokinetics of esomeprazole in adult patients with gastroesophageal reflux disease
- Esomeprazole-induced healing of gastroesophageal reflux disease is unrelated to the genotype of CYP2C19: Evidence from clinical and pharmacokinetic data
- Determination of esomeprazole and its two main metabolites in human, rat and dog plasma by liquid chromatography with tandem mass spectrometry
- Effect of the H, K–ATPase inhibitor, esomeprazole magnesium, on gut total antioxidant capacity in mice
- Asymmetric synthesis of esomeprazole
- Esomeprazole in the treatment of Helicobacter pylori
- Review article: esomeprazole − the first proton pump inhibitor to be developed as an isomer
- Review article: pharmacology of esomeprazole and comparisons with omeprazole
- Review article: gastric acidity − comparison of esomeprazole with other proton pump inhibitors
- Review article: initial therapy of reflux disease with esomeprazole
- Review article: esomeprazole, 40 mg once daily, compared with lansoprazole, 30 mg once daily, in healing and symptom resolution of erosive oesophagitis
- Esomeprazole 20 mg and lansoprazole 15 mg in maintaining healed reflux oesophagitis: Metropole study results
- Esomeprazole provides improved acid control vs. omeprazole in patients with symptoms of gastro-oesophageal reflux disease
- Esomeprazole improves healing and symptom resolution as compared with omeprazole in reflux oesophagitis patients: a randomized controlled trial
- One-week triple therapy with esomeprazole provides effective eradication of Helicobacter pylori in duodenal ulcer disease
- Esomeprazole 20 mg maintains symptom control in endoscopy-negative gastro-oesophageal reflux disease: a controlled trial of ‘on-demand’ therapy for 6 months