NEXIUM ® Esomeprazole

NEXIUM ® is a drug based on esomeprazole.

THERAPEUTIC GROUP: Antireflux - Antiulcer-Proton pump inhibitors

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications NEXIUM ® Esomeprazole

NEXIUM ® is used in clinical practice in the treatment of all those pathological manifestations of the gastro-intestinal tract, associated with gastric hyperacidity, such as duodenal ulcers, peptic ulcers, gastric ulcers, gastro-esophageal reflux diseases and esophagitis.

In combination with antibiotics, NEXIUM ® can also be used in the eradication of Helicobacter Pylori, while in conjunction with non-steroidal anti-inflammatory drugs to reduce the development of gastric and duodenal ulcers associated with prolonged use of these medicines.

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 + ATPasi pump.

Taken orally, thanks to the gastro-resistant formulation, the gastric barrier passes unaltered, to be absorbed at the duodenal level, reaching the maximum plasma concentration within 2 hours of oral administration.

Linked to plasma proteins, it is distributed in the circulatory stream, where it is transformed into the active form, following protonation induced by the acidic 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 of intragastric acid concentrations of about 80%, with a therapeutic effect that maximizes within 2-3 days of first hiring.

Once its action is over, the parietal cell re-synthesizes new functioning proteins, while esomeprazole undergoes an important hepatic metabolism by cytochrome p450 enzymes and a subsequent renal excretion.

Studies carried out and clinical efficacy

ESOMEPRAZOLO ETI 'PEDIATRICA

The gastro esophageal reflux, and the associated symptomatology, is one of the most frequent pathological conditions in pediatric patients. In this study the efficacy of esomeprazole treatment was evaluated for 8 weeks in small patients aged 12 to 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

Esomeprazole is one of the few proton pump inhibitors also available in intravenous infusion vials. This study shows how the use of this method of administration can prove to be particularly safe and effective, for patients hospitalized and suffering from bleeding peptic ulcer, both reducing the symptoms and the costs of managing the patient himself.

3. COMPARISON OF THE PROTONIC PUMP INHIBITORS

This study conducted about 5, 000 patients with erosive esophagitis, showed that the daily administration of 40 mg of esomeprazole may be more effective than lansoprazole, in the resolution of erosive esophagitis and heartburn.

Method of use and dosage

NEXIUM ® 20- 40 mg gastro-resistant coated tablets of esomeprazole or NEXIUM ® injectable 40 mg bottles:

despite the correct formulation of the dosage, it should be elaborated by your doctor, after a careful evaluation of the patient's physiopathological conditions and his therapeutic goals, it is possible to describe in general some dosages widely used in the common clinical practice.

More precisely, the daily dose of 20 - 40 mg seems sufficient for the treatment of erosive reflux oesophagitis, gastro-oesophageal reflux disease, duodenal and peptic ulcer from 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 is instead exclusively of interest to the hospital.

Warnings NEXIUM ® Esomeprazole

The use of NEXIUM ® should be preceded by a careful evaluation of the patient's clinical picture in order to exclude the malignant origin of pathologies of the gastro-intestinal 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 should also be carried out with particular care in patients with reduced liver and kidney function, for whom a significant increase in exposure to the active ingredient has been described.

The antacid action induced by NEXIUM ® could both determine an increased risk of Salmonella and Campylobacter infections, and an alteration in the absorption of other drugs.

The appearance of episodes of drowsiness, mental confusion and dizziness following the use of esomeprazole, could make the use of machinery and driving vehicles dangerous.

PREGNANCY AND BREASTFEEDING

NEXIUM ® as well as other preparations based on esomeprazole, are contraindicated during 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 the infant .

Interactions

Esomeprazole is known to be metabolised by cytochrome p450 and more precisely by isoforms CYP2C19 and CYP3A4, and how its metabolites can reduce the activity of these enzymes.

In light of these data, therefore, it is clear that the concomitant administration of active ingredients metabolized by the same enzyme system can result in a significant variability of the pharmacokinetic characteristics of the same.

Therefore, in these cases, it would be necessary to avoid such interaction or adjust the dose so as to be able to maintain the therapeutic effect while minimizing the risk of side effects.

Furthermore, the reduction of the intragastric acidity induced by NEXIUM ® could reduce the absorption of drugs that require particularly acid pH to be absorbed as some antifungal agents.

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 experimentation and post-marketing monitoring have highlighted a series of side effects, fortunately easily tolerable and clinically unimportant such as headache, abdominal pain, nausea, vomiting, diarrhea, constipation, flatulence, dizziness and insomnia.

Clinically more important adverse events, such as changes in liver and kidney function, changes in the hematological and immune status, have been observed more rarely and exclusively in particular categories of patients at risk.