Pantoprazole (Dosage)

Pantoprazole is a proton pump inhibitor used for the treatment of stomach ulcers or gastroesophageal reflux disease, among others. Up to 40% of patients show an ineffective response and do not find relief of symptoms. Genetic polymorphisms in the enzymes that metabolize these drugs, such as CYP2C19, are responsible for a significant percentage of this drug resistance.

Pantoprazole is an antiulcer drug, proton pump inhibitor (PPI). The drug inhibits the enzyme adenosine triphosphatase H+/K+, which is the final common pathway of acid production by gastric parietal cells. It binds to the proton pump in the gastric parietal cell, inhibiting the transport of H+ to the gastric lumen.

These group of drugs are the most potent inhibitors of acid secretion.

CONTRAINDICATIONS

Hypersensitivity to the active substance or to substituted benzimidazoles. Pantoprazole is contraindicated for the eradication of H. pylori in patients with hepatic insufficiency or moderate-severe renal insufficiency.

CAUTIONS

Precautions should be taken in patients with severe hepatic insufficiency, in which it is necessary to adjust doses, monitor liver enzymes and stop treatment if these enzymes increase.

Cautions should also be taken in patients with renal insufficiency. It is advisable to take precautions if pantoprazole is prescribed to elderly patients.

Pantoprazole is not indicated to treat nervous dyspepsia.

Pantoprazole can reduce the absorption of vitamin B12, monitor symptoms of deficit in Zollinger-Ellison syndrome, in long-term treatment and in individuals with vitamin B12 deficiency or in those who have risk factors for reduced absorption.

The use of pantoprazole is associated with a possible increased risk of gastrointestinal infection caused by bacteria (eg Salmonella, Campylobacter, C. difficile). An increase in the risk of contracting gastroenteritis or pneumonia acquired in the community has been described with the use of this drug.

A regular monitorization should be done if treatment with pantoprazole is prolonged (more than one year). There is a risk of hypomagnesemia in prolonged treatment and in concomitance with digoxin or other drugs that may reduce the plasma level of Mg (for example, diuretics); consider the plasma control of Mg at the beginning and periodically during the treatment.

At high doses and in prolonged treatment, pantoprazole increases the risk of fracture of the hip, wrist and spine, especially in the elderly or in the presence of other risk factors, so it must be ensured the intake of Ca and D vitamin if there is risk of osteoporosis .

Treatment with pantoprazole is associated with a possible risk of developing subacute cutaneous erythematosus lupus (SCEL) (if lesions occur, especially in areas of the skin exposed to the sun, accompanied by arthralgia, consider stopping treatment).

The withdrawal of pantoprazole should be slow (within a month) to avoid rebound acid secretion that would lead to recurrence of symptoms.

SIDE EFFECTS

Headache, abdominal pain, nausea, dizziness, insomnia and diarrhea

PHARMACOLOGIC INTERACTIONS

Pantoprazole reduces the absorption of: ketoconazole, itraconazole, posaconazole and erlotinib.

Monitor INR (International Normalized Ratio)/prothrombin time if pantoprazole is taken in concomitance with coumarin anticoagulants.

At high doses, pantoprazole may increase methotrexate levels.

The intake of pantoprazole together with atazanavir is not recommended because of the risk of decreasing bioavailability (if necessary, monitor clinically and increase the dose of atazanavir to 400 mg + 100 mg ritonavir and not exceed 20 mg pantoprazole / day).

BRAND NAMES

  • Alpanzol ®
  • Anagastra ®
  • Citrel ®
  • Nolpaza ®
  • Panpronton ®
  • Pantecta ®
  • Pantoloc ®
  • Ulcotenal ®

Genes analyzed

CYP2C19

Bibliography

Chiba K, Shimizu K, Kato M, et al.Prediction of inter-individual variability in the pharmacokinetics of CYP2C19 substrates in humans. Drug Metab Pharmacokinet. 2014;29(5):379-86.

Eken E, Estores DS, Cicali EJ, et al. A Pharmacogenetics-Based Approach to Managing Gastroesophageal Reflux Disease: Current Perspectives and Future Steps. Pharmgenomics Pers Med. 2023 Jun 23;16:645-664.

El Rouby N, Lima JJ, Johnson JA.Proton pump inhibitors: from CYP2C19 pharmacogenetics to precision medicine. Expert Opin Drug Metab Toxicol. 2018 Apr;14(4):447-460.

Lima JJ, Thomas CD, Barbarino J, et al.Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2C19 and Proton Pump Inhibitor Dosing. Clin Pharmacol Ther. 2021 Jun;109(6):1417-1423.

Zhao F, Wang J, Yang Y, et al.Effect of CYP2C19 genetic polymorphisms on the efficacy of proton pump inhibitor-based triple therapy for Helicobacter pylori eradication: a meta-analysis. Helicobacter. 2008 Dec;13(6):532-41.

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