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 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.

Drug Label Information | Brands:

Brands of Rabeprazole in Kenya:

Barole® , Mega Lifesciences (Australia) PVT Ltd
Bepra®, Global Navi
Pariet®, Janssen Pharmaceutica pty Ltd
Prompto®, Getz
Rabekind® ,Mankind Pharma Ltd
Rabeloc® , Cadila Pharmaceuticals (EA) Ltd
Rabemac®, Macleods Pharmaceuticals Limited
Rabosec® , Innocia Lifesciences Pvt. Ltd.
Rabtas®, Intas Pharmaceuticals Ltd
Rapeed®, Alkem Laboratories Limited
Raz-tab | Raz-IV, Brawn Laboratories Limited
Razid®, Global
Robort®, Dolopharma Healthcare Ltd
Rzole®, Ravian Life Sciences Pvt Ltd
Strirab® ,Gufic Stridden Biopharma Private Ltd.
Veloz®, Torrent

INDICATIONS

1.Healing of Erosive or Ulcerative GERD in Adults
Rabeprazole is indicated for short-term (4 to 8 weeks) treatment in the healing and symptomatic relief of erosive or ulcerative gastroesophageal reflux disease (GERD). For those patients who have not healed after 8 weeks of treatment, an additional 8-week course of rabeprazole sodium may be considered.
Rabeprazole 20 mg once daily 4 to 8 weeks.

2.Maintenance of Healing of Erosive or Ulcerative GERD in Adults
Rabeprazole is indicated for maintaining healing and reduction in relapse rates of heartburn symptoms in patients with erosive or ulcerative gastroesophageal reflux disease (GERD Maintenance). Controlled studies do not extend beyond 12 months.
Rabeprazole 20 mg once daily Controlled studies do not extend beyond 12 months

3.Treatment of Symptomatic GERD in Adults
Rabeprazole is indicated for the treatment of daytime and nighttime heartburn and other symptoms associated with GERD in adults for up to 4 weeks.
Rabeprazole 20 mg once daily Up to 4 weeks

4. Healing of Duodenal Ulcers in Adults
Rabeprazole is indicated for short-term (up to four weeks) treatment in the healing and symptomatic relief of duodenal ulcers. Most patients heal within four weeks.
Rabeprazole 20 mg once daily after the morning meal Up to 4 weeks

5.Helicobacter pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence in Adults
Rabeprazole , in combination with amoxicillin and clarithromycin as a three drug regimen, are indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or history within the past 5 years) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Rabeprazole 20 mg Amoxicillin 1,000 mg Clarithromycin 500 mg Take all three medications twice daily with morning and evening meals; it is important that patients comply with the full 7-day regimen

6.Treatment of Pathological Hypersecretory Conditions, Including Zollinger-Ellison Syndrome in Adults
Rabeprazole is indicated for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome.
Starting dose 60 mg once daily then adjust to patient needs; some patients require divided doses
Dosages of 100 mg once daily and 60 mg twice daily have been administered

7.Treatment of Symptomatic GERD in Adolescent Patients 12 Years of Age and Older
Rabeprazole is indicated for the treatment of symptomatic GERD in adolescents 12 years of age and above for up to 8 weeks.
Rabeprazole 20 mg once daily Up to 8 weeks

CONTRAINDICATIONS

Rabeprazole sodium is contraindicated in patients with known hypersensitivity to rabeprazole, substituted benzimidazoles, or to any component of the formulation. Hypersensitivity reactions may include anaphylaxis, anaphylactic shock, angioedema, bronchospasm, acute interstitial nephritis, and urticaria
PPIs, including rabeprazole sodium, are contraindicated with rilpivirine-containing products

ADVERSE DRUG REACTIONS

The following serious adverse reactions are listed below :

  • Acute Interstitial Nephritis
  • Clostridium difficile-Associated Diarrhea
  • Bone Fracture
  • Cutaneous and Systemic Lupus Erythematosus
  • Cyanocobalamin (Vitamin B-12) Deficiency
  • Hypomagnesemia
  • Fundic Gland Polyps

DRUG INTERACTIONS:

Antiretrovirals:
The effect of PPI on antiretroviral drugs is variable. The clinical importance and the mechanisms behind these interactions are not always known.

  • Decreased exposure of some antiretroviral drugs (e.g., rilpivirine, atazanavir, and nelfinavir) when used concomitantly with rabeprazole may reduce antiviral effect and promote the development of drug resistance.
  • Increased exposure of other antiretroviral drugs (e.g., saquinavir) when used concomitantly with rabeprazole may increase toxicity.
  • There are other antiretroviral drugs which do not result in clinically relevant interactions with rabeprazole.

Warfarin:
Increased INR and prothrombin time in patients receiving PPIs, including rabeprazole, and warfarin concomitantly. Increases in INR and prothrombin time may lead to abnormal bleeding and even death

Methotrexate:
Concomitant use of rabeprazole with methotrexate (primarily at high dose) may elevate and prolong serum levels of methotrexate and/or its metabolite hydroxymethotrexate, possibly leading to methotrexate toxicities. No formal drug interaction studies of methotrexate with PPIs have been conducted

Digoxin
Potential for increased exposure of digoxin

Drugs Dependent on Gastric pH for Absorption (e.g., iron salts, erlotinib, dasatinib, nilotinib, mycophenolate mofetil, ketoconazole, itraconazole):
Rabeprazole can reduce the absorption of drugs due to its effect on reducing intragastric acidity.

Combination Therapy with Clarithromycin and Amoxicillin:
Concomitant administration of clarithromycin with other drugs can lead to serious adverse reactions, including potentially fatal arrhythmias, and are contraindicated.

Amoxicillin also has drug interactions.

Tacrolimus:
Potentially increased exposure of tacrolimus, especially in transplant patients who are intermediate or poor metabolizers of CYP2C19.

Interactions with Investigations of Neuroendocrine Tumors:
Serum chromogranin A (CgA) levels increase secondary to PPI-induced decreases in gastric acidity. The increased CgA level may cause false positive results in diagnostic investigations for neuroendocrine tumors.

Interaction with Secretin Stimulation Test:
Hyper-response in gastrin secretion in response to secretin stimulation test, falsely suggesting gastrinoma.

False Positive Urine Tests for THC:
There have been reports of false positive urine screening tests for tetrahydrocannabinol (THC) in patients receiving PPIs.

PHARMACOKINETICS

Absorption
Absolute bioavailability for a 20 mg oral tablet of rabeprazole (compared to intravenous administration) is approximately 52%.

Distribution
Rabeprazole is 96.3% bound to human plasma proteins.

Elimination
Metabolism: Rabeprazole is extensively metabolized. A significant portion of rabeprazole is metabolized via systemic nonenzymatic reduction to a thioether compound. Rabeprazole is also metabolized to sulphone and desmethyl compounds via cytochrome P450 in the liver. The thioether and sulphone are the primary metabolites measured in human plasma.

Excretion: Following a single 20 mg oral dose of 14C-labeled rabeprazole, approximately 90% of the drug was eliminated in the urine, primarily as thioether carboxylic acid; its glucuronide, and mercapturic acid metabolites.

Excretion: Following a single 20 mg oral dose of 14C-labeled rabeprazole, approximately 90% of the drug was eliminated in the urine, primarily as thioether carboxylic acid; its glucuronide, and mercapturic acid metabolites.