NEXIUM ® Esomeprazole
NEXIUM ® is an esomeprazole-based drug.
THERAPEUTIC GROUP: Antireflux - Antiulcer-Inhibitors of the proton pump
Indications NEXIUM ® Esomeprazole
NEXIUM ® is used in clinical practice in the treatment of all pathological manifestations of the gastrointestinal tract associated with gastric hyperacidity, such as duodenal ulcers, peptic ulcers, gastric ulcers, gastro-oesophageal reflux diseases and esophagitis.
In combination with antibiotics, NEXIUM ® can also be used in the eradication of Helicobacter Pylori, while concomitantly with non-steroidal anti-inflammatory drugs to reduce the development of gastric and duodenal ulcers associated with the prolonged use of these drugs.
Mechanism of action NEXIUM ® Esomeprazole
NEXIUM ® is a drug based on esomeprazole, an active ingredient belonging to the category of proton pump inhibitors, and active on the H + / K + ATPase pump.
Taken orally, thanks to the gastro-resistant formulation, it passes the gastric barrier unaltered, to be absorbed at the duodenal level, reaching the maximum plasma concentration within 2 hours of oral administration.
Bound to plasma proteins, it is distributed in the bloodstream, where it is transformed into the active form, following protonation induced by the acid environment of the intracellular canaliculi of the parietal cells of the stomach.
Here the active form of esomeprazole can selectively bind a Cys residue of the acid proton pump, irreversibly inhibiting it and guaranteeing a reduction in intragastric acid concentrations of about 80%, with a therapeutic effect that is maximized within 2-3 days from first hiring.
At the end of its action, the parietal cell resynthesizes new functioning proteins, while esomeprazole undergoes an important hepatic metabolism by the cytochrome p450 enzymes and a subsequent renal excretion.
Studies carried out and clinical efficacy
ESOMEPRAZOLE PEDIATRIC AGE
J Pediatr Gastroenterol Nutr. 2010 Nov; 51: 593-8.
Healing of erosive esophagitis and improvement of symptoms of gastroesophageal reflux disease after esomeprazole treatment in children 12 to 36 months old.
Tolia V, Gilger MA, Barker PN, Illueca M.
Gastroesophageal reflux, and associated symptoms, is one of the most frequent pathological conditions in pediatric patients. This study evaluated the efficacy of treatment with esomeprazole for 8 weeks in small patients aged between 12 and 36 months and suffering from erosive esophagitis. As many as 84% of treated patients demonstrated a significant improvement in symptoms, without clinically significant side effects.
2. EXOMEPRAZOLE AND HOSPITAL TREATMENT
Expert Rev Pharmacoecon Outcomes Res. 2010 Aug; 10: 371-4.
Cost-effectiveness of high-dose intravenous esomeprazole in patients with peptic ulcer bleeding in the USA and Europe.
Brown RE, Nandi J.
Esomeprazole is one of the few proton pump inhibitors also available in ampoules for intravenous infusion. This study shows how the use of this method of administration can be particularly safe and effective, for hospitalized patients with bleeding peptic ulcer, both reducing the symptomatology that the patient's own management costs.
3. COMPARISON BETWEEN PROTONIC PUMP INHIBITORS
Am J Gastroenterol. 2002 Mar; 97: 575-83.
Esomeprazole (40 mg) compared with lansoprazole (30 mg) in the treatment of erosive esophagitis.
Castell DO, Kahrilas PJ, Richter JE, Vakil NB, Johnson DA, Zuckerman S, Skammer W, Levine JG.
This study, conducted on about 5000 patients suffering from erosive esophagitis, has shown that the daily administration of 40 mg of esomeprazole can be more effective than lansoprazole, in the resolution of erosive esophagitis and heartburn.
Method of use and dosage
NEXIUM ® gastro-resistant coated tablets of 20 - 40 mg esomeprazole or NEXIUM ® Injectable bottles of 40 mg:
despite the correct formulation of the dosage, it should be elaborated by one's doctor, after a "careful evaluation of the physio-pathological conditions of the patient and of his therapeutic objectives, it is possible to describe in principle, some dosage widely used in common clinical practice.
More precisely, the daily dose of 20 - 40 mg seems sufficient for the treatment of erosive reflux esophagitis, gastroesophageal reflux disease, duodenal and peptic ulcer caused by H. Pylori in association with antibiotics, and in the prevention of gastric ulcers. from prolonged treatment with non-steroidal anti-inflammatory drugs, while for the treatment of Zollinger-Ellison syndrome, the dosage could even be doubled.
The formulation in injectable vials, on the other hand, is exclusively of hospital interest.
NEXIUM ® Esomeprazole warnings
The assumption of NEXIUM ® should be preceded by a careful evaluation of the clinical picture of the patient in order to exclude the malignant origin of the pathologies of the gastrointestinal tract.
This need is particularly relevant, given the ability of esomeprazole to mask some important signs and symptoms, which could delay the time of diagnosis, facilitating disease progression and therapeutic failure.
The administration of esomeprazole, moreover, should be carried out with particular care, in patients with reduced hepatic and renal function, for whom a significant increase in exposure to the active principle has been described.
The antacid action induced by NEXIUM ® could determine both an increased risk of Salmonella and Campylobacter infections, and an alteration in the absorption of other drugs.
The onset of episodes of drowsiness, mental confusion and dizziness following the intake of esomeprazole, could make the use of machinery and driving of vehicles dangerous.
PREGNANCY AND BREASTFEEDING
NEXIUM ® as well as other esomeprazole-based preparations, are contraindicated in pregnancy and lactation, given the absence of studies and experimental models that show the total safety of the active ingredient when taken in these moments, on the health of the fetus and infant. .
It is known that esomeprazole is metabolised by cytochrome p450 and more precisely by the isoforms CYP2C19 and CYP3A4, and how its metabolites can reduce the activity of these enzymes.
In the light of these data, therefore, it appears evident that the concomitant administration of active principles metabolized by the same enzymatic system can result in a significant variability of the pharmacokinetic characteristics of the same.
Therefore, in these cases, it would be necessary to avoid this interaction or to adjust the dose in such a way as to be able to maintain the therapeutic effect while minimizing the risk of side effects.
Furthermore, the reduction of intragastric acidity induced by NEXIUM ® could reduce the absorption of drugs that require particularly acid pH to be absorbed, such as some antifungals.
Contraindications NEXIUM ® Esomeprazole
Given a documented cross-reactivity between the various proton pump inhibitors, NEXIUM ® is contraindicated in case of known hypersensitivity to the active ingredient or to other benzimidazole derivatives.
Undesirable Effects - Side Effects
Clinical trials and post-marketing monitoring have highlighted a series of side effects, fortunately easily tolerated and clinically not very relevant, such as headache, abdominal pain, nausea, vomiting, diarrhea, constipation, flatulence, dizziness and insomnia.
Clinically more important adverse events, such as impaired liver and kidney function, changes in the haematological and immune picture, were observed more rarely and exclusively in particular categories of patients at risk.
NEXIUM ® can only be sold under medical prescription
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