Aciphex (rabeprazole sodium)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Rabeprazole, commonly referred to as an acid or proton-pump inhibitor, is a gastric antisecretory agent.
Rabeprazole sodium, a substituted benzimidazole proton-pump inhibitor (PPI), is a gastric antisecretory agent. This class of antisecretory compounds does not exhibit anticholinergic or histamine H2-receptor antagonist properties, but inhibits the gastric H+/K+ ATPase at the secretory surface of the gastric parietal cell and thus suppresses gastric acid secretion. Rabeprazole blocks the last step of gastric acid secretion.
After oral administration of rabeprazole 20 mg, peak plasma concentrations are attained in 2-5 hours. Peak plasma concentrations and AUC of rabeprazole are linear over an oral dosage of 10-40 mg; the pharmacokinetics of rabeprazole are not altered by multiple dosing. The absolute bioavailability of a rabeprazole 20 mg oral tablet, when compared to IV administration, is about 52%.
Following oral administration of rabeprazole 20 mg, inhibition of gastric acid is apparent within 1 hour, and the median inhibitory effect of rabeprazole on 24-hour gastric acidity is 88% of maximal after the first dose. When rabeprazole is administered with food, absorption may be delayed by up to 4 hours or longer; when taken with a high-fat meal, the time to peak plasma concentration of rabeprazole is variable. However, peak plasma concentration and AUC of rabeprazole are not substantially altered with food intake.
Rabeprazole is 96.3% plasma protein bound. Rabeprazole undergoes extensive metabolism; a significant portion is metabolized via systemic nonenzymatic reduction. Rabeprazole is also metabolized in the liver via cytochrome P-450 (CYP) enzymes, primarily by CYP3A and CYP2C19.
Following a single radiolabeled oral dose of rabeprazole 20 mg, about 90% of the drug was eliminated in the urine as various metabolites; the remainder of the dose was excreted in the feces. The elimination half-life of rabeprazole is about 1-2 hours. In patients with the poor CYP2C19 metabolizer phenotype, metabolism of rabeprazole is slower than in those with extensive (or rapid) metabolizer phenotype.
Increased serum gastrin levels due to antisecretory agents stimulate the proliferation of gastric enterochromaffin-like (ECL) cells, which may result in ECL cell hyperplasia over time, based on animal studies. Gastric carcinoids have also been observed in rats. In more than 400 patients treated with rabeprazole (10 or 20 mg) once daily for up to 1 year, ECL cell hyperplasia incidence increased with time and dose.
In the gastric mucosa, no patient developed the adenomatoid, dysplastic, or neoplastic changes of ECL cells; no patient developed carcinoid tumors.
USES: Rabeprazole is used to treat certain stomach and esophagus problems (such as acid reflux, ulcers). It works by decreasing the amount of acid your stomach makes. It relieves symptoms such as heartburn, difficulty swallowing, and cough.
This medication helps heal acid damage to the stomach and esophagus, helps prevent ulcers, and may help prevent cancer of the esophagus. Rabeprazole belongs to a class of drugs known as proton pump inhibitors (PPIs).
Generic name: rabeprazole sodium
Pronunciation: (ra-BEP-ra-zole)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Aciphex
Indications
The following indications are listed for Aciphex:
- Duodenal Ulcer
- Duodenal Ulcer Due To H. Pylori
- Gastric Hypersecretion With Systemic Mastocytosis
- Gastroesophageal Reflux Disease
- Heartburn
- Helicobacter Pylori Gastritis
- Multiple Endocrine Neoplasia
- Pathological Gastric Acid Hypersecretory Condition
- Zollinger-Ellison Syndrome
Also known as: Adenomatosis Partial Multiple Endocrine, Brash, Campylobacter Gastritis, Du Due To H. Pylori, Duodenal Ulcer Due To Campylobacter Pylori, Duodenal Ulcer Due To Helicobacter Pylori, Gastric Acid Hypersecretory Conditions Due To Disease, Gastro-Esophageal Reflux, Ge Reflux Disease, H. Pylori Gastritis, Multiple Endocrine Adenoma, Pancreatic Ulcerogenic Tumor Syndrome, Pathological Gastric Acid Hypersecretory States, Pathological Hypersecretion State, Pathological Hypersecretory Condition, Pyrosis, Systemic Mast Cell Disease With Gastric Hypersecretion, Z-E Syndrome.
Dosing
Rabeprazole is available as rabeprazole sodium; dosage is expressed in terms of the salt.
Rabeprazole sodium is administered orally, generally once daily. Rabeprazole sodium tablets should not be chewed, crushed, or split. Food may delay the rate but does not affect the extent of GI absorption; therefore, rabeprazole generally may be given without regard to meals.
When rabeprazole is used for the healing of duodenal ulcers, the manufacturer recommends dosing rabeprazole after the morning meal.
When rabeprazole is used in combination with clarithromycin and amoxicillin (triple therapy) for the treatment of Helicobacter pylori (H. pylori ) eradication, all 3 medications should be taken twice daily with the morning and evening meals. Although concomitant administration of rabeprazole with clarithromycin and amoxicillin may result in increased peak plasma concentrations and AUCs of rabeprazole and 14-hydroxyclarithromycin (the active metabolite of clarithromycin), the increased exposure is not expected to be clinically important.
Store rabeprazole delayed-release tablets protected from moisture at 25degreesC; excursions are permitted to 15-30degreesC.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Rabeprazole is extensively metabolized, mainly via systemic nonenzymatic reduction and hepatic cytochrome P-450 (CYP) 3A and 2C19 isoenzymes.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to rabeprazole, other substituted benzimidazoles (e.g., esomeprazole, lansoprazole, omeprazole, pantoprazole), or any ingredient in the formulation.
*Concomitant use of rilpivirine-containing products.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in >2% of adult patients receiving rabeprazole include pain, pharyngitis, flatulence, infection, and constipation.
Adverse effects occurring in >=2% of adolescents receiving rabeprazole include headache, diarrhea, nausea, vomiting, and abdominal pain.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Efficacy and safety of rabeprazole for symptomatic GERD in adolescents 12-16 years of age are supported by controlled clinical trials in adults and a multicenter, randomized, open-label study in adolescents 12-16 years of age. The adverse reaction profiles of rabeprazole in adolescents with symptomatic or endoscopically diagnosed GERD were similar to those in adults. Safety and efficacy of rabeprazole have not been established in pediatric patients for the healing of erosive or ulcerative GERD, maintenance of healing of erosive or ulcerative GERD, healing of duodenal ulcers, Helicobacter pylori eradication to reduce the risk of duodenal ulcer recurrence, or treatment of pathological hypersecretory conditions (e.g., Zollinger-Ellison Syndrome).
Rabeprazole delayed-release 20 mg tablets are not recommended for pediatric patients <12 years of age as the tablet strength exceeds the dosage recommended for these patients. The safety and efficacy of a different dosage form and dosage strength of rabeprazole had been established in pediatric patients 1-12 years of age for the treatment of GERD; however, this formulation is no longer available in the US.
In a multicenter pharmacokinetic study in adolescents 12-16 years of age, those who received rabeprazole 20 mg once daily for 5-7 days had about a 40% increase in rabeprazole exposure compared with the exposure after 1 day of dosing. In adolescents 12-16 years of age with GERD, pharmacokinetic parameters were within the range observed in healthy adults.
There are no human data available on the use of rabeprazole in pregnant females.
In animal reproductive studies in rats and rabbits administered IV rabeprazole during organogenesis at 13 and 8 times the human AUC at the recommended dose for gastroesophageal reflux disease (GERD), respectively, there was no evidence of fetal harm. In late gestation and during lactation, administration of rabeprazole to rats at an oral dosage of 400 mg/kg per day (about 195 times the human oral dosage based on mg/m2) resulted in decreases in body weight gain of the pups.
In a pre- and postnatal developmental toxicity study in rats, additional outcomes for bone development were evaluated using a different PPI. At doses >=3.4 times an oral human dose based on body surface area (BSA), decreased femur length, width, and thickness of cortical bone, decreased thickness of the tibial growth plate, and minimal to mild bone marrow hypocellularity were observed. At PPI doses >=33.6 times an oral human dose based on BSA, physeal dysplasia in the femur was also observed in offspring after in utero and lactational exposure. At PPI doses of 3.4-57 times an oral human dose based on BSA, effects on maternal bone were observed in pregnant and lactating rats in a pre- and postnatal toxicity study. When dosed from gestational day 7 through weaning on postnatal day 21, a substantial decrease in maternal femur weight of up to 14% was observed when compared to placebo at PPI doses of >=33.6 times an oral human dose based on BSA.
In a follow-up developmental toxicity study in rats, pup bone development was evaluated from postnatal day 2 to adulthood using a different PPI at oral doses of 280 mg/kg per day (approximately 68 times an oral human dose based on BSA), where drug administration was from either gestational day 7 or gestational day 16 until parturition. When maternal administration of the PPI was confined to gestation only, there were no effects on bone physeal morphology in the offspring at any age.
Studies have not been conducted to assess the presence of rabeprazole in human milk, the effects of the drug on the breastfed infant, or the effects on milk production. Rabeprazole is present in rat milk.
Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for rabeprazole and any potential adverse effects on the breastfed infant from the medication or from the underlying maternal condition.
The manufacturer makes no specific dosage recommendations for geriatric patients.
No substantial differences in safety and efficacy have been observed in geriatric patients relative to younger adults, but increased sensitivity cannot be ruled out. In a pharmacokinetic study in geriatric patients administered rabeprazole 20 mg once daily for 7 days, AUC values were approximately doubled, and peak plasma concentrations increased by 60% compared to younger patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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