Aciphex

Name: Aciphex

US Brand Name

  1. Aciphex
  2. Aciphex Sprinkle

How should this medicine be used?

Rabeprazole comes as a delayed-release (releases the medication in the intestine to prevent break-down of the medication by stomach acids) tablet to take by mouth. When rabeprazole is used to treat most conditions, it is usually taken once a day. When used to treat ulcers, rabeprazole is taken after the morning meal. When used in combination with other medications to eliminate H. pylori, rabeprazole is taken twice a day, with the morning and evening meals, for 7 days. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take rabeprazole exactly as directed. Do not take more or less of it or take it more often or for a longer period of time than prescribed by your doctor.

Swallow the tablets whole with water; do not split, chew, or crush them.

Continue to take rabeprazole even if you feel well. Do not stop taking rabeprazole without talking to your doctor. If your condition does not improve or gets worse, call your doctor.

Is rabeprazole available as a generic drug?

GENERIC AVAILABLE: Yes

What is the dosage for rabeprazole?

Tablets should be swallowed whole and should not be crushed, split or chewed. Rabeprazole can be taken with or without meals since food has little effect on its absorption.

  • For healing ulcerating GERD, the recommended dose for adults is 20 mg daily for 4-8 weeks. If healing does not occur after 8 weeks, another 8 week course may be considered. The recommended maintenance dose is 20 mg daily.
  • Heartburn due to GERD is treated with 20 mg daily for 4 weeks and an additional 4 weeks if symptoms do not resolve.
  • Ulcers are treated with 20 mg daily for 4 weeks.
  • For the management of Zollinger-Ellison Syndrome, the starting dose for adults is 60 mg daily, and the dose is adjusted based on improvement in symptoms, healing of ulcers, or the effectiveness of acid suppression. Doses of 100 mg per day and 60 mg twice daily have been used in some patients with Zollinger-Ellison Syndrome.
  • The regimen for eradication of Helicobacter pylori is rabeprazole 20 mg, clarithromycin 500 mg, amoxicillin 1000 mg all given twice daily (morning and evening) for 7 days.

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Reviewed on 7/12/2016 References Reference: FDA Prescribing Information

Overdose

If overdose is suspected, contact a poison control center or emergency room immediately. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

What is rabeprazole?

Rabeprazole is a proton pump inhibitor that decreases the amount of acid produced in the stomach.

Rabeprazole is used short-term to treat symptoms of gastroesophageal reflux disease (GERD) in adults and children who are at least 1 year old.

Rabeprazole is used only in adults to treat conditions involving excessive stomach acid, such as Zollinger-Ellison syndrome. Rabeprazole is also used in adults to promote healing of duodenal ulcers or erosive esophagitis (damage to your esophagus caused by stomach acid).

Rabeprazole may also be given with an antibiotic to prevent duodenal ulcer caused by infection with Helicobacter pylori (H. pylori).

Rabeprazole is not for immediate relief of heartburn symptoms.

Rabeprazole may also be used for purposes not listed in this medication guide.

How should I take rabeprazole?

Rabeprazole is usually taken once per day. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Do not give this medicine to a child without medical advice. Certain forms and strengths of rabeprazole should not be given to a child younger than 12 years old.

AcipHex Sprinkle should not be given to a child younger than 1 year old.

Rabeprazole is for short-term use only, usually 4 to 8 weeks. Your doctor may recommend a second course of treatment if you need additional healing time.

When treating H. pylori infection, rabeprazole may be needed for only 7 days. Follow your doctor's dosing instructions very carefully.

Take this medicine with a full glass of water.

If you take rabeprazole to treat duodenal ulcers, take the medicine after a meal. If you take rabeprazole to prevent ulcers caused by Helicobacter pylori, take the medicine with food. If you take rabeprazole for any other condition, you may take the medicine with or without food.

The rabeprazole delayed-release capsule (AcipHex Sprinkle) should be taken 30 minutes before a meal.

Do not crush, break, or chew a rabeprazole tablet. Swallow it whole.

To take delayed-release rabeprazole (AcipHex Sprinkle), open the capsule and sprinkle the medicine into a spoonful of soft food such as applesauce, yogurt, or baby food made from fruit or vegetable. You may also mix the medicine with apple juice, Pedialyte, or infant formula. Swallow right away without chewing. Do not save the mixture for later use; it will go bad after 15 minutes.

Some conditions are treated with a combination of rabeprazole and antibiotics. Use all medications as directed by your doctor. Read all patient information, medication guides, and instruction sheets provided to you. Ask your doctor or pharmacist if you have any questions.

Do not change your doses or medication schedule without your doctor's advice.

Take your medicine for the full prescribed length of time. Your symptoms may improve before your condition is completely cleared.

Call your doctor if your symptoms do not improve, or if they get worse while using rabeprazole.

If you use rabeprazole for longer than 3 years, you could develop a vitamin B-12 deficiency. Talk to your doctor about how to manage this condition if you develop it.

Store at room temperature away from moisture and heat.

AcipHex Dosage and Administration

Administration

Oral Administration

Administer orally; may give without regard to meals, but manufacturer recommends administration after morning meal in patients with duodenal ulcer.1

When used in combination with clarithromycin and amoxicillin for treatment of H. pylori infection and duodenal ulcer disease, take all 3 drugs twice daily with morning and evening meals.1

Swallow tablets intact; do not chew, crush, or split.1

Antacids may be used concomitantly as needed for pain relief.1 19

Dosage

Available as rabeprazole sodium; dosage expressed in terms of the salt.1

Pediatric Patients

GERD Symptomatic GERD Oral

Adolescents ≥12 years of age: 20 mg once daily for up to 8 weeks.1

Adults

GERD GERD without Erosive Esophagitis Oral

20 mg once daily for 4 weeks; may give additional 4 weeks if symptoms are not completely resolved.1

Treatment of Erosive Esophagitis Oral

20 mg once daily1 2 15 18 for 4–8 weeks.1 15 If not healed after 8 weeks, consider additional 8 weeks of therapy (up to 16 weeks for a single course).1

Maintenance of Healing of Erosive Esophagitis Oral

20 mg once daily.1 2 15 18 Chronic, lifelong therapy may be appropriate.26

Duodenal Ulcer Treatment of Active Duodenal Ulcer Oral

20 mg once daily for up to 4 weeks;1 2 17 18 some patients may require additional therapy.1

Helicobacter pylori Infection and Duodenal Ulcer Disease Oral

Triple therapy: 20 mg twice daily for 7 days in conjunction with amoxicillin and clarithromycin.1

Pathologic GI Hypersecretory Conditions (e.g., Zollinger-Ellison Syndrome) Oral

60 mg once daily.1 Dosages up to 100 mg once daily or 60 mg twice daily have been used.1 Divided doses may be required.1 Adjust dosage as needed, continue treatment as long as necessary.1 Has been used continuously for up to 1 year.1

Cautions for AcipHex

Contraindications

  • Known hypersensitivity to rabeprazole, any ingredient in the formulation, or other substituted benzimidazoles (e.g., esomeprazole, lansoprazole, pantoprazole, omeprazole).1

Warnings/Precautions

Gastric Malignancy

Response to rabeprazole does not preclude presence of occult gastric neoplasm.1

Clostridium difficile Infection

Proton-pump inhibitors associated with possible increased (1.4–2.75 times) risk of Clostridium difficile infection, including C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis).335 336 339 340 Many patients also had other risk factors for CDAD.335 May be severe; colectomy and, rarely, death reported.335

Use the lowest effective dosage and shortest duration of therapy appropriate for the patient's clinical condition.335

Consider CDAD if persistent diarrhea develops and manage accordingly; initiate supportive therapy (e.g., fluid and electrolyte management), anti-infective therapy directed against C. difficile (e.g., metronidazole, vancomycin), and surgical evaluation as clinically indicated.335 336

Respiratory Effects

Administration of proton-pump inhibitors has been associated with an increased risk for developing certain infections (e.g., community-acquired pneumonia).35 36

Bone Fracture

Several observational studies suggest that use of proton-pump inhibitors, particularly in high dosages (i.e., multiple daily doses) and/or for prolonged periods of time (i.e., ≥1 year), may be associated with increased risk of osteoporosis-related fractures of the hip, wrist, or spine.1 39 300 301 302 303 304 305 Magnitude of risk is unclear;39 300 301 302 303 304 305 310 causality not established.305 FDA is continuing to evaluate this safety concern.305

Use the lowest effective dosage and shortest duration of therapy appropriate for the patient’s clinical condition.1 39 301 303 305 307

Individuals at risk for osteoporosis-related fractures should receive an adequate intake of calcium and vitamin D; assess and manage these patients’ bone health according to current standards of care.1 39 303 305 307

Hypomagnesemia

Hypomagnesemia, symptomatic and asymptomatic, reported rarely in patients receiving long-term therapy (≥3 months or, in most cases, >1 year) with proton-pump inhibitors, including rabeprazole.1 317 318 319 320 321 322 323 324 325 326 327 328 329 330 Serious adverse effects include tetany, seizures, tremors, carpopedal spasm, arrhythmias (e.g., atrial fibrillation, supraventricular tachycardia), and abnormal QT interval.1 318 319 321 322 323 325 327 328 329 Paresthesia, muscle weakness, muscle cramps, lethargy, fatigue, and unsteadiness may occur.319 320 321 325 330 Most patients required magnesium replacement and discontinuance of the proton-pump inhibitor.1 317 319 321 322 323 324 325 326 327 330 Hypomagnesemia resolved within 1 week (median) following discontinuance and recurred within 2 weeks (median) of rechallenge.327

In patients expected to receive long-term proton-pump inhibitor therapy or in patients currently receiving digoxin or drugs that may cause hypomagnesemia (e.g., diuretics), consider measuring serum magnesium concentrations prior to initiation of prescription proton-pump inhibitor therapy and periodically thereafter.1 319 326 327 328 330

Specific Populations

Pregnancy

Category B.1

Lactation

Not known whether rabeprazole is distributed into milk; discontinue nursing or the drug.1

Pediatric Use

Safety and efficacy for short-term treatment of symptomatic GERD established in adolescents 12–16 years of age.1 Pharmacokinetic and adverse effect profiles similar to those in adults.1

Safety and efficacy not established in children <12 years of age.1

Geriatric Use

No substantial differences in safety or efficacy relative to younger adults, but increased sensitivity cannot be ruled out.1

Hepatic Impairment

Use with caution in patients with severe impairment.1 21

Common Adverse Effects

Pain,1 pharyngitis,1 flatulence,1 infection,1 constipation.1

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).1 Protect from moisture.1

Actions

  • Inhibits basal and stimulated gastric acid secretion.1

  • Concentrates in acid conditions of parietal cell secretory canaliculi; forms active sulfenamide metabolite that binds to and inactivates hydrogen-potassium ATPase (proton- or acid-pump), blocking final step in secretion of hydrochloric acid.1 2 3 4 5 6 Sustained inactivation of hydrogen-potassium ATPase results in prolonged duration of action.1 3

  • Suppresses gastric H. pylori in patients with duodenal ulcer and/or reflux esophagitis infected with the organism.2 3 10 11 Combined therapy with rabeprazole and one or more appropriate anti-infectives (e.g., amoxicillin, clarithromycin) can effectively eradicate H. pylori gastric infection.2 3 10 11

Commonly used brand name(s)

In the U.S.

  • Aciphex
  • Aciphex Sprinkle

Available Dosage Forms:

  • Capsule, Delayed Release
  • Tablet, Enteric Coated

Therapeutic Class: Gastrointestinal Agent

Pharmacologic Class: Proton Pump Inhibitor

Drug interactions

Table 2 includes drugs with clinically important drug interactions when administered concomitantly with Aciphex delayed-release tablets and instructions for preventing or managing them.

Consult the labeling of concomitantly used drugs to obtain further information about interactions with PPIs.

Table 2: Clinically Relevant Interactions Affecting Drugs Co-Administered with Aciphex Delayed-Release Tablets 
Antiretrovirals
Clinical Impact: 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.
Intervention: Rilpivirine-containing products:  Concomitant use with Aciphex delayed-release tablets is contraindicated [see Contraindications (4)].  See prescribing information.
     
Atazanavir:  See prescribing information for atazanavir for dosing information.
    
Nelfinavir: Avoid concomitant use with Aciphex delayed-release tablets. See prescribing information for nelfinavir.
    
Saquinavir:  See the prescribing information for saquinavir and monitor for potential saquinavir toxicities.
     
Other antiretrovirals:  See prescribing information.
Warfarin
Clinical Impact: 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 [see Warnings and Precautions (5.2)].
Intervention: Monitor INR and prothrombin time. Dose adjustment of warfarin may be needed to maintain target INR range.  See prescribing information for warfarin.
Methotrexate
Clinical Impact: 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 [see Warnings and Precautions (5.9)].
Intervention: A temporary withdrawal of Aciphex delayed-release tablets may be considered in some patients receiving high dose methotrexate administration.
Digoxin
Clinical Impact: Potential for increased exposure of digoxin [see Clinical Pharmacology (12.3)].
Intervention: Monitor digoxin concentrations. Dose adjustment of digoxin may be needed to maintain therapeutic drug concentrations. See prescribing information for digoxin.
Drugs Dependent on Gastric pH for Absorption (e.g., iron salts, erlotinib, dasatinib, nilotinib, mycophenolate mofetil, ketoconazole, itraconazole)
Clinical Impact: Rabeprazole can reduce the absorption of drugs due to its effect on reducing intragastric acidity. 
Intervention: Mycophenolate mofetil (MMF): Co-administration of PPIs in healthy subjects and in transplant patients receiving MMF has been reported to reduce the exposure to the active metabolite, mycophenolic acid (MPA), possibly due to a decrease in MMF solubility at an increased gastric pH.  The clinical relevance of reduced MPA exposure on organ rejection has not been established in transplant patients receiving PPIs and MMF.  Use Aciphex delayed-release tablets with caution in transplant patients receiving MMF.
See the prescribing information for other drugs dependent on gastric pH for absorption.
Combination Therapy with Clarithromycin and Amoxicillin
Clinical Impact: 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.
Intervention: See Contraindications and Warnings and Precautions in prescribing information for clarithromycin.
      
See Drug Interactions in prescribing information for amoxicillin.
    

Nonclinical toxicology

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

In a 88/104-week carcinogenicity study in CD-1 mice, rabeprazole at oral doses up to 100 mg/kg/day did not produce any increased tumor occurrence.  The highest tested dose produced a systemic exposure to rabeprazole (AUC) of 1.40 µg•hr/mL which is 1.6 times the human exposure (plasma AUC0-∞ = 0.88 µg•hr/mL) at the recommended dose for GERD (20 mg/day).  In a 28-week carcinogenicity study in p53+/- transgenic mice, rabeprazole at oral doses of 20, 60, and 200 mg/kg/day did not cause an increase in the incidence rates of tumors but produced gastric mucosal hyperplasia at all doses.  The systemic exposure to rabeprazole at 200 mg/kg/day is about 17 to 24 times the human exposure at the recommended dose for GERD.  In a 104-week carcinogenicity study in Sprague-Dawley rats, males were treated with oral doses of 5, 15, 30 and 60 mg/kg/day and females with 5, 15, 30, 60, and 120 mg/kg/day.  Rabeprazole produced gastric enterochromaffin-like (ECL) cell hyperplasia in male and female rats and ECL cell carcinoid tumors in female rats at all doses including the lowest tested dose.  The lowest dose (5 mg/kg/day) produced a systemic exposure to rabeprazole (AUC) of about 0.1 µg•hr/mL which is about 0.1 times the human exposure at the recommended dose for GERD.  In male rats, no treatment related tumors were observed at doses up to 60 mg/kg/day producing a rabeprazole plasma exposure (AUC) of about 0.2 µg•hr/mL (0.2 times the human exposure at the recommended dose for GERD).

Rabeprazole was positive in the Ames test, the Chinese hamster ovary cell (CHO/HGPRT) forward gene mutation test, and the mouse lymphoma cell (L5178Y/TK+/–) forward gene mutation test.  Its demethylated-metabolite was also positive in the Ames test.  Rabeprazole was negative in the in vitro Chinese hamster lung cell chromosome aberration test, the in vivo mouse micronucleus test, and the in vivo and ex vivo rat hepatocyte unscheduled DNA synthesis (UDS) tests.

Rabeprazole at intravenous doses up to 30 mg/kg/day (plasma AUC of 8.8 µg•hr/mL, about 10 times the human exposure at the recommended dose for GERD) was found to have no effect on fertility and reproductive performance of male and female rats.

How supplied/storage and handling

Aciphex 20 mg is supplied as delayed-release light yellow enteric-coated tablets.  The name and strength, in mg, (Aciphex 20) is imprinted on one side.

      Bottles of 30 (NDC 62856-243-30)

      Bottles of 90 (NDC 62856-243-90)

      Unit Dose Blisters Package of 100 (10 x 10) (NDC 62856-243-41)

Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [see USP Controlled Room Temperature].  Protect from moisture.

Aciphex Drug Class

Aciphex is part of the drug class:

  • Proton pump inhibitors

Aciphex Food Interactions

Medicines can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of Aciphex there are no specific foods that you must exclude from your diet when receiving this medication.

Administration

Oral Administration

Delayed-release tablet

  • Administer with or without meals
  • Swallow tablet whole; do not chew or crush

Delayed-release capsule

  • Take 30 minutes before a meal
  • Contains enteric coated granules (acid labile); do not chew or crush
  • Do not swallow capsule whole
  • Open capsule and sprinkle entire contents on small amount of soft food (eg, applesauce, fruit- or vegetable-based baby food, or yogurt) or empty contents into a small amount of liquid (eg, infant formula, apple juice, or pediatric electrolyte solution)
  • Take entire dose within 15 minutes of preparation
  • Food or liquid should be at or below room temperature; do not store mixture for future use

Missed dose

  • Administer a missed dose as soon as possible
  • If administration time is close to the following dose, skip missed dose and take current dose
  • Do not take 2 doses at the same time

Storage

Delayed release tablet and capsule: Store at room temperature at 77°F (25°C); excursions permitted to 59-86°F (15-30°C)

Breastfeeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

In Summary

Common side effects of Aciphex include: atrophic gastritis. See below for a comprehensive list of adverse effects.

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