Saturday, March 2, 2013

RABEPRAZOLE




Rabeprazole  is an antiulcer drug in the class of proton pump inhibitors. It was developed by Eisai Co. and is marketed by Janssen-Cilag as rabeprazole sodium under the brand names AcipHex  in the US, Pariet in Europe, Brazil, Canada, Japan, Russia and Australia, and Razo and Parit in India.


(RS)-2-([4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methylsulfinyl)-1H-benzo[d]imidazole

Indications and usage
Short-term treatment in healing and symptomatic relief of duodenal ulcers and erosive or ulcerative gastroesophageal reflux disease (GERD); maintaining healing and reducing relapse rates of heartburn symptoms in patients with GERD; treatment of daytime and nighttime heartburn and other symptoms associated with GERD; long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome and in combination with amoxicillin and clarithromycin to eradicate Helicobacter pylori.

Gastric ulcer (GU)
Peptic ulcer disease (PUD)
Maintenance of healing of erosive or ulcerative GERD
Healing of erosive and ulcerative GERD
Healing of duodenal ulcers.
Treatment of symptomatic GERD
Treatment of pathological hypersecretory conditions (Zollinger-Ellison syndrome)
Helicobacter pylori eradication to reduce risk of duodenal ulcer recurrence


Contraindications   -   hypersensitivity to rabeprazole, substituted benzimidazoles or any of components of its pharmaceutical forms.
pregnancy: FDA Pregnancy Ratings: B
lactation: Thomson Lactation Ratings: Infant risk cannot be ruled out.

Restriction of usage   -    acute hepatic failure
pediatric use in patients under 18 years of age (there are insufficient data about safety and efficiency of rabeprazole in this group of patients)



Rabeprazole adverse reactions/side effects include
In clinical trials the most common side effect assessed as possibly or probably related to AcipHex was headache in 2.4% of patients vs 1.6% taking placebo.
abdominal pains
anxiety    , arthralgia    ,    asthenia     ,    constipation  ,    diarrhea  ,     dry mouth  ,      erythema   ,     Granulocytopenia ,    headache   ,   increased or decreased appetite    ,     insomnia    ,     leukocytopenia  ,    meteorism   ,       muscle or bone pain      ,    myalgia   ,   nausea   ,    skin eruption  ,    thrombocytopenia   , vertigo   ,   vomiting
Antacid preparations such as rabeprazole by suppressing acid mediated break down of proteins, leads to an elevated risk of developing food or drug allergies. This happens due to undigested proteins then passing into the gastrointestinal tract where sensitisation occurs. It is unclear whether this risk occurs with only long-term use or with short-term use as well.


DRUG INTERACTION -   Rabeprazole decreases the concentration of ketoconazole in the plasma (in 33%), increases the concentration of digoxin (in 22%), and does not interact with liquid antacids. Rabeprazole is compatible with any medicine metabolized by the CYP450 (theophylline, warfarin, diazepam, phenytoin).

OVER DOSAGE   -   Studies in mice and rats indicated the symptoms of acute toxicity due to overdose included: hypoactivity, labored respiration, convulsion, diarrhea, tremor, and coma. A study in dogs indicated that a dose of 2000mg/kg was not lethal.


BRANDS  -  Rabeprazole as "CYRA" (Systopic Labs Pvt Ltd),"Elpizole" (Orchid Chemicals & Pharmaceuticals), "Elpizole -20" (Orchid Chemicals & Pharmaceuticals) Rablet (Lupin),Acigard (3D), AcipHex, Rabeloc, Pariet is supplied in:
Tablet, enteric-coated; 10 mg
Tablet, enteric-coated; 20 mg
Rabeprazole is sold under the brand names Acigard,Cyra, Rabium, Esoon, Rabemac, Rabiloz, Razo, Rabifast and Rablet in India, and Zechin in Pakistan.


Rabeprazole is in a group of drugs called proton pump inhibitors. Rabeprazole decreases the amount of acid produced in the stomach.

Rabeprazole is used to treat symptoms of gastroesophageal reflux disease (GERD) and other conditions involving excessive stomach acid such as Zollinger-Ellison syndrome. Rabeprazole is also used to promote healing of erosive esophagitis (damage to your esophagus caused by stomach acid).

Rabeprazole may also be given with an antibiotic to prevent gastric 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.


What is the most important information I should know about rabeprazole?
Heartburn is often confused with the first symptoms of a heart attack. Seek emergency medical attention if you have chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, and a general ill feeling.

You should not use this medication if you are allergic to rabeprazole or to similar medicines such as lansoprazole (Prevacid), esomeprazole (Nexium), omeprazole (Prilosec, Zegerid), or pantoprazole (Protonix).

Rabeprazole is not for immediate relief of heartburn symptoms.

Some conditions are treated with a combination of rabeprazole and antibiotics. Use all medications as directed by your doctor. Read the medication guide or patient instructions provided with each medication. Do not change your doses or medication schedule without your doctor's advice.

Take this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared.

What should I discuss with my healthcare provider before taking rabeprazole?

Heartburn is often confused with the first symptoms of a heart attack. Seek emergency medical attention if you have chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, and a general ill feeling.

You should not use this medication if you are allergic to rabeprazole or to similar medicines such as lansoprazole (Prevacid), esomeprazole (Nexium), omeprazole (Prilosec, Zegerid), or pantoprazole (Protonix).

To make sure you can safely take rabeprazole, tell your doctor if you have severe liver disease or low magnesium levels in your blood.

Some conditions are treated with a combination of rabeprazole and antibiotics. Use all medications as directed by your doctor. Read the medication guide or patient instructions provided with each medication. Do not change your doses or medication schedule without your doctor's advice.

Taking a proton pump inhibitor such as rabeprazole may increase your risk of bone fracture in the hip, wrist, or spine. This effect has occurred mostly in people who have taken the medication long term or at high doses, and in those who are age 50 and older. It is not clear whether rabeprazole is the actual cause of an increased risk of fracture. Before you take this medication, tell your doctor if you have osteoporosis or osteopenia (low bone mineral density).

FDA pregnancy category B. This medication is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

It is not known whether rabeprazole passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.




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