LUCEN ® Esomeprazole

LUCEN ® 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 LUCEN ® Esomeprazole

LUCEN ® is useful both as a pharmacological support for the prevention and healing of gastric and duodenal ulcers associated with prolonged therapy with non-steroidal anti-inflammatory drugs, and as a therapeutic approach to the treatment of all those morbid states associated with gastric hyperacidity such as gastroesophageal reflux disease, esophagitis erosive, duodenal ulcers, gastric and peptic ulcers, and Zollinger-Ellison syndrome.

In association with antibiotics, LUCEN ® can also be used in the eradicating treatment of Helicobacter Pylori

Mechanism of action LUCEN ® Esomeprazole

As with the other active ingredients belonging to the category of proton pump inhibitors, also esomeprazole, isomer of the more common omeprazole, is able to act selectively on the acid proton pump expressed by the parietal cells of the stomach, reducing the proton secretion towards the gastric lumen.

The activation of the active principle is observed following protonation, exclusively in the intracellular canaliculi, where the pH reaches low values, while following oral administration, it succeeds in passing the acid barrier of the stomach unscathed, thanks to the Gastroresistant formulation, thus being absorbed subsequently from the duodenal mucosa.

The maximum plasma peak is observed after about 2 hours with a maximum bioavailability of around 64% of the total dose taken, given the presence of a mild pre-hepatic metabolism.

All the active ingredient, instead, is completely metabolized at the hepatic level, by the cytochrome p450, isoform CYP2C19 and subsequently excreted mainly through the renal route.

Studies carried out and clinical efficacy

1. ESOMEPRAZOLE AND NSAIDs

As is known, one of the therapeutic indications of esomeprazole is represented by the prevention of gastric and duodenal ulcers associated with prolonged therapy with non-steroidal anti-inflammatory drugs. In this study, the concomitant administration of fixed doses of naproxen and esomeprazole was particularly useful in reducing the incidence of gastric and duodenal complications.

2. EXOMEPRAZOLE AND MAINTENANCE THERAPY

The oral administration of esomeprazole, after endoscopic therapy for the treatment of a bleeding ulcer, has proved to be very well tolerated and effective in preventing the possible bleeding and failure to heal the ulcer.

3. EXOMEPRAZOLE AND DISPLEASIA

In some patients the digestive difficulties seem to be determined by an alteration of the normal gastro-intestinal microenvironment. In this study, in fact, 68% of patients with dyspepsia have been shown to benefit from significant reductions in heartburn, abdominal pain, nausea and vomiting, with esomeprazole intake.

Method of use and dosage

LUCEN ® gastro-resistant coated tablets of 20 - 40 mg of esomeprazole:

the posology used varies according to the therapeutic purposes and the clinical picture of the patient.

In principle, the daily dose of 80 mg is used in the treatment of Zollinger-Ellison syndrome, while in most cases the doses of 40 and 20 mg / day of esomeprazole are sufficient for the treatment of erosive reflux oesophagitis, of gastro-oesophageal reflux disease, duodenal and peptic ulcer from H. Pylori in combination with antibiotics, and in the prevention of gastric ulcers from prolonged treatment with non-steroidal anti-inflammatory drugs.

The correct dosage should in any case be established by the doctor, after a careful evaluation of the patient's physiopathological conditions and his therapeutic goals.

Warnings LUCEN ® Esomeprazole

The hepatic and renal metabolism of esomeprazole requires careful medical supervision, when LUCEN ® is taken in patients with reduced liver and kidney function.

As with other proton pump inhibitors, the administration of esomeprazole should be preceded by an evaluation of the patient's clinical picture, which is able to exclude the malignant origin of gastro-intestinal disorders, reducing the risk of delaying the diagnosis following taking LUCEN ® due to its ability to mask the symptoms.

The use of prolonged this medicine has been associated with an increase in blood concentrations of gastrin, probably associated with the appearance of gastric and intestinal neoformations, fortunately not of malignant origin.

The reduction in acidity of the gastric environment could promote infection with Salmonella and Campylobacter, especially for patients who continuously use these 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

The safety profile of LUCEN ® when taken during pregnancy, is still in the debate phase given the presence of experimental studies and clinical trials with conflicting results.

For this reason, therefore, the intake of esomeprazole is contraindicated both during pregnancy and in the subsequent period of breastfeeding.

Interactions

The interactions described for LUCEN ® are essentially due to:

CYP2C19-induced metabolism, a highly polymorphous enzyme, involved in the metabolism of numerous other active ingredients, and inhibited by the metabolites of esomeprazole itself. It is therefore evident that the concomitant administration of esomeprazole and substrates of the aforementioned enzyme, or modulators thereof and esomeprazole can be associated respectively with a variation in the pharmacokinetic properties of the various compounds and of esomeprazole.
Reduction of intragastric acidity, which can reduce the absorption of drugs such as some antifungals, whose absorption is regulated by gastric pH.

To avoid, therefore, the appearance of unpleasant side effects, it would be useful to avoid the concomitant administration of these drugs or adjust the relative dosages.

Contraindications LUCEN ® Esomeprazole

LUCEN ® is contraindicated during pregnancy and lactation and in patients with known hypersensitivity to the active ingredient and its excipients, or to other benzimidazole derivative drugs, given the possibility of cross-reactivity.

Undesirable effects - Side effects

The main side effects described following the administration of LUCEN ® were found to be clinically insignificant, and essentially characterized by abdominal pain, constipation, diarrhea, nausea, vomiting, flatulence, dizziness and insomnia.

More serious and clinically more relevant disorders have been observed rarely and especially in particular categories of patients at risk.

In any case, all the aforementioned side effects tend to be promptly regressed once the therapy has been suspended.