Rabeprazole, Uses, Dosage, Side Effects, Interactions, Pregnancy

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Rabeprazole is an alpha-pyridyl methyl sulfinyl benzimidazole and a selective and irreversible proton pump inhibitor with the antisecretory property. Rabeprazole enters the parietal cell and accumulates in the acidic secretory canaliculi where the agent is activated by a proton-catalyzed process that results in the formation of a thiophilic sulfonamide or sulfenic acid. The activated rabeprazole forms covalent bonds with the sulfhydryl amino acids cysteine on the extracellular domain of the proton pump (H+/K+ ATPase) at the secretory surface, thereby inhibiting the transport of hydrogen ions, via exchange with potassium ions, into the gastric lumen. Binding to cysteine 813, in particular, is essential for the inhibition of gastric acid production.
Rabeprazole is a proton pump inhibitor (PPI) and a potent inhibitor of gastric acidity used in the therapy of gastroesophageal reflux and peptic ulcer disease. Rabeprazole therapy is associated with a low rate of transient and asymptomatic serum aminotransferase elevations and is a rare cause of clinically apparent liver injury.

Mechanism of Action of Rabeprazole

Rabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine H2-receptor antagonist properties but suppress gastric acid secretion by inhibiting the gastric H+/K+ATPase (hydrogen-potassium adenosine triphosphatase) at the secretory surface of the gastric parietal cell. Because this enzyme is regarded as the acid (proton) pump within the parietal cell, rabeprazole has been characterized as a gastric proton-pump inhibitor. Rabeprazole blocks the final step of gastric acid secretion. In gastric parietal cells, rabeprazole is protonated, accumulates, and is transformed to an active sulfenamide. When studied in vitro, rabeprazole is chemically activated at pH 1.2 with a half-life of 78 seconds.
Or
Rabeprazole is a selective and irreversible proton pump inhibitor. Rabeprazole suppresses gastric acid secretion by specific inhibition of the hydrogen-potassium adenosine triphosphatase (H+, K+-ATPase) enzyme system found at the secretory surface of parietal cells. It inhibits the final transport of hydrogen ions (via exchange with potassium ions) into the gastric lumen. Since the H+, K+-ATPase enzyme system is regarded as the acid (proton) pump of the gastric mucosa, rabeprazole is known as a gastric acid pump inhibitor. Rabeprazole does not have anticholinergic or histamine H2-receptor antagonist properties.

Indications of Rabeprazole

Therapeutic Indications of Rabeprazole

Contra-Indications of Rabeprazole

Dosage of Rabeprazole

Strengths:  5 mg ,20 mg,10 mg

Gastroesophageal Reflux Disease

  • 20 mg orally once a day
  • Duration of therapy: Up to 4 weeks

Duodenal Ulcer

  • 20 mg orally once a day
  • Duration of therapy: 4 weeks

Erosive Esophagitis

  • 20 mg orally once a day
  • Duration of therapy: 4 to 8 weeks

Helicobacter pylori Infection

  • 20 mg orally 2 times a day, taken concomitantly with amoxicillin and clarithromycin
  • Duration of therapy: 7 days

Gastric Ulcer

  • 20 mg orally once a day
  • Duration of therapy: 4 to 8 weeks

Zollinger-Ellison Syndrome

  • Initial dose: 60 mg orally once a day
  • Maintenance dose: 60 mg orally 2 times a day or 100 mg orally once a day
  • Duration of therapy: Up to 1 year.

Pediatric Gastroesophageal Reflux Disease

1 to 11 years

  • Less than 15 kg: 5 mg orally once a day, with the option to increase to 10 mg if inadequate response
  • 15 kg or more: 10 mg orally once a day
  • Duration of therapy: Up to 12 weeks
  • 12 years or older: 20 mg orally once a day
  • Duration of therapy: Up to 8 weeks

Side Effects of Rabeprazole

The most common

Common

Rare

Drug Interactions of Rabeprazole

Rabeprazole may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy Category

FDA Pregnancy Category B

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. Rabeprazole may pass into breast milk and may cause side effects in a child who is breastfed. Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

It is not known if rabeprazole passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children and adolescents less than 18 years of age.

References

 

dexlansoprazole

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