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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
- For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevention of gastrointestinal bleeds with NSAID use.
- To treat symptoms of GORD such as heartburn and acid regurgitation
- Gastroesophageal reflux disease (GERD)
- Erosive esophagitis (acid-related damage to the esophagus, the tube that connects your mouth to your stomach)
- Gastric (stomach) ulcers or duodenal ulcers. Duodenal ulcers occur in your duodenum. This is the first part of your small intestine. It is the part connected to your stomach.
- Conditions where your stomach makes too much acid, such as Zollinger-Ellison Syndrome
- Stomach infections caused by Helicobacter pylori bacteria.
- Ulcers in the upper part of the intestine (duodenal ulcer) or stomach (gastric ulcer).
- Ulcers caused by medicines called NSAIDs (Non-Steroidal Anti-Inflammatory Drugs).
- Too much acid in the stomach caused by a growth in the pancreas (Zollinger-Ellison syndrome).
- Benign gastric ulcers
- Heartburn and other symptoms associated with GERD,
- Erosive esophagitis, and long-term treatment of pathological hypersecretory conditions
- Multiple endocrine adenomas,
- Systemic mastocytosis.
- Maintenance therapy for duodenal ulcer patients at reduced dosage after healing of acute ulcers. No placebo-controlled comparative studies have been carried out for periods of longer than 1 year.
- The treatment of pathological hypersecretory conditions (e.g., Zollinger-Ellison syndrome and systemic mastocytosis).
- Short-term treatment of active, benign gastric ulcer. Most patients heal within 6 weeks and the usefulness of further treatment has not been demonstrated. Studies available to date have not assessed the safety of ranitidine in uncomplicated, benign gastric ulcer for periods of more than 6 weeks.
- Maintenance therapy for gastric ulcer patients at reduced dosage after healing of acute ulcers. Placebo-controlled studies have been carried out for 1 year.
- Symptomatic relief commonly occurs within 24 hours after starting therapy with ranitidine 150 mg twice daily
- Prevention of stress-induced ulcers in critically ill patients
- Recurrent postoperative ulcer
- Treatment of endoscopically diagnosed erosive esophagitis. Symptomatic relief of heartburn commonly occurs within 24 hours of therapy initiation with ranitidine 150 mg4 times daily.
- Maintenance of healing of erosive esophagitis. Placebo-controlled trials have been carried out for 48 weeks.
Therapeutic Indications of Rabeprazole
- Antiulcerative
- Rabeprazole is indicated for the short-term treatment 4-8 weeks for symptomatic relief and healing of erosive or ulcerative gastroesophageal reflux disease.
- Rabeprazole may be indicated for an additional 8 weeks of treatment for patients in whom healing has not occurred. Rabeprazole also is indicated to maintain healing of erosive or ulcerative gastroesophageal reflux disease.
- Rabeprazole is indicted for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome.
- Rabeprazole is indicated for short-term treatment (up to 4 weeks) in the healing and symptomatic relief of patients with active duodenal ulcers
Contra-Indications of Rabeprazole
- People with a known hypersensitivity to PPI, substituted benzimidazoles or any other component of the capsule formulation (e.g. certain dyes)
- Pregnancy
- Breastfeeding women
- People with known hypersensitivity (allergy) to PPI or any of the ingredients in the medication.
- Clostridium difficile infection
- Inadequate Vitamin B12
- Low amount of magnesium in the blood
- Liver problems
- Interstitial Nephritis
- Subacute cutaneous lupus erythematosus
- Systemic Lupus Erythematosus
- Osteoporosis
- Broken Bone
- Allergies to Proton Pump Inhibitors
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
- Disturbances of the gut such as diarrhea, constipation, nausea, vomiting or abdominal pain.
- Drowsiness and lightheadedness
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Loss of memory (amnesia).
- Muscle weakness.
- Dizziness.
- A headache.
- Skin rashes.
- Difficulty in passing urine (urinary retention).
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Unexpected aggression, restlessness or irritability
- Nightmares or hallucinations
Common
- Constipation
- Diarrhea
- Loss of muscle coordination
- Sleepiness or unusual drowsiness
- Clumsiness or unsteadiness
- Dizziness
- Drowsiness
- Dry mouth
- Lightheadedness
- Muscle weakness.
- A headache.
- Skin rashes.
Rare
- seizures
- dizziness
- irregular or fast heartbeat
- tremors (jerking movements or shaking)
- muscle weakness
- spasms of the hands and feet
- cramps or muscle aches
- trouble breathing, coughing, wheezing, hoarse voice, or
- throat tightness
- watery stool
- rash on the skin and nose, raised, red, scaly, red or purple rash on your body
- convulsions (seizures)
- a sore throat
- difficulty with breathing
- unusual tiredness or weakness
Drug Interactions of Rabeprazole
Rabeprazole may interact with following drugs, supplements, & may change the efficacy of drugs
- aripiprazole
- “azole” antifungal medications (e.g., itraconazole, fluconazole, ketoconazole, posaconazole)
- bisphosphonates (e.g., alendronate, risedronate)
- carbamazepine
- certain protein kinase inhibitors (e.g. dasatinib, nilotinib
- clopidogrel
- dexamethasone
- iron salts
- methotrexate
- methylphenidate
- mycophenolate
- phenobarbital
- phenytoin
- pioglitazone
- rosiglitazone
- “statin” cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
- tocilizumab
- warfarin
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
