Esomeprazole (Efficacy)

Esomeprazole is an S-isomer of omeprazole with a profile similar to this one and is used to reduce the secretion of gastric acid. It is a selective inhibitor of the proton pump (PPI) in the parietal cell. It acts on the acid medium where it inhibits the proton pump and inhibits basal and stimulated acid secretion.

The data available suggest that esomeprazole does not provide relevant advantages over omeprazole (in trials on the eradication of H. pylori in triple therapy it has shown a somewhat lower efficacy than that usually obtained with other PPI.) In essays on healing of reflux esophagitis, a slightly superior but not clinically relevant efficacy has been demonstrated.

Esomeprazole can be dissolved in water, which facilitates its administration by nasogastric tube in patients with dysphagia.

CONTRAINDICATIONS

Esomeprazole is contraindicated in patients with hypersensitivity to esomeprazole, to substituted benzimidazoles or to any excipient in the formulation. Do not administer with nelfinavir.

CAUTIONS

The main metabolic pathway of esomeprazole is the CYP2C19 cytochrome. The polymorphisms of this enzyme will cause interindividual differences in the elimination of esomeprazole. In slow metabolizing patients the plasma concentrations of the drug are increased. .

In patients with severe hepatic impairment there is an increase in the bioavailability of the drug, since it is metabolized primarily in the liver. In patients with severe hepatic impairment, the maximum dose will be 10 mg in children under 12 years of age and 20 mg in children over 12 years of age.

Hyperplasia of parietal cells, fundic glandular polyps and hyperplasia of enterochromaffin-like cells has been observed as a consequence of acid suppression and hypergastrinemia.

An increase in the risk of developing gastroenteritis or pneumonia acquired in the community as a consequence of hypochlorhydria has been described.

The withdrawal of the PPI should be slow (in the course of a month) to avoid the rebound of acid secretion that would lead to the recurrence of symptoms.

In treatments lasting more than a year, there is a risk of fracture of the hip, wrist and spine, especially in the elderly or in patients with risk factors. In patients at risk of osteoporosis ensure the intake of vitamin D and calcium.

There exists risk of subacute cutaneous lupus erythematosus (SCLE) if injuries occur, especially in areas of the skin exposed to the sun, accompanied by arthralgia. In these cases consider stopping treatment with esomeprazole.

SIDE EFFECTS

Headache, drowsiness, dizziness. Abdominal pain, diarrhea, flatulence, nausea/vomiting, constipation. Pruritus.

PHARMACOLOGIC INTERACTIONS

By competitive inhibition of cytochrome P450 (CYP2C19 isoenzyme), it can cause an elevation in the plasma levels of other drugs metabolized by the CYP system, the most important being benzodiazepines, acenocoumarol, warfarin, phenytoin, carbamazepine, citalopram, methotrexate, methylphenidate.

The co-administration of esomeprazole with clopidogrel and dabigatran is not recommended, as it reduces biotransformation to their respective active metabolites.

Esomeprazole may increase tacrolimus levels, so the association should be avoided, changing it to rabeplazole or pantoprazole, which appear to have less interaction or to selective H2 inhibitors (famotidine, ranitidine).

Esomeprazole is not recommended together with atazanavir, if it is necessary, adjust the dose of atazanavir to 400 mg + ritonavir 100 mg + a maximum ofr. esomeprazole 20 mg and perform a close monitorization.

Due to an increase in gastric pH, esomeprazole reduces the absorption of atazanavir and nelfinavir (the concomitant use is contraindicated), cefditoreno, iron salts, tyrosine kinase inhibitors, ketoconazole, itraconazole and posaconazole.

By increasing gastric pH, esomeprazole increases the absorption of digoxin, furosemide and acetylsalicylic acid.

Rifampin may decrease serum levels of esomeprazole.

St. John's wort may decrease the effects of esomeprazole. The association should be avoided.

BRAND NAMES

  • Axiago ®
  • Nexium ®

Genes analyzed

CYP2C19

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