Rabeprazole

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Rabeprazole
Systematic (IUPAC) name
2-[(4-(3-methoxypropoxy)- 3-methyl-pyridin-2-yl) methylsulfinyl]- 1H-benzoimidazole
Identifiers
CAS number	117976-89-3
ATC code	A02BC04
PubChem	5029
DrugBank	APRD01212
Chemical data
Formula	C18H21N3O3S
Mol. mass	359.444 g/mol
Pharmacokinetic data
Bioavailability	52%
Metabolism	Hepatic
Half life	1 - 1.5 hours
Excretion	Renal
Therapeutic considerations
Licence data	US
Pregnancy cat.	B(US)
Legal status	POM(UK) ℞-only(US)
Routes	Oral

Rabeprazole is an antiulcer drug in the class of proton pump inhibitors. It was developed by Eisai and is marketed by Janssen-Cilag as rabeprazole sodium under the brand names Aciphex and Pariet.

Contents 1 Pharmacology 2 Indications and usage 3 Contraindications 4 Restriction of usage 5 Side effects 6 Drug interactions 7 Overdosage 8 How supplied 9 References 10 External links

[edit] Pharmacology

Rabeprazole is a prodrug (metabolized by the cytochrome P450 (or CYP450)) - in the acid environment of the parietal cells it turn into active sulphenamide form associated with cysteine of H+, K+ATPase (proton pump). Rabeprazole inhibits (partly reversibly) H+, K+ATPase of the coating gastric cells and dose-dependent oppresses basal and stimulated gastric acid secretion. Rabeprazole has anti Helicobacter pylori activity (MIC 4-16 mg/ml) and accelerates the one for some antibiotics. There was showed effectiveness of Rabeprazole at the patients with pathological hypersecretory activity (incl. Zollinger-Ellison Syndrome).

[edit] Indications and usage

• gastric ulcer
• peptic ulcer (PUD)
• duodenal ulcer
• ulcerative gastroesophageal reflux disease (GERD) - erosive (erosive or ulcerative gastroesophageal reflux disease) and non erosive (gastroesophageal reflux disease) manifestations
• pathological hypersecretory activity (incl. Zollinger-Ellison syndrome)
• Helicobacter pylori eradication (combination therapy with antibacterial medicines)

[edit] Contraindications

• hypersensitivity to Rabeprazole, substituted benzimidazoles or any of components of its pharmaceutical forms.
• pregnancy
• lactation

[edit] 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)

[edit] Side effects

Rabeprazole Adverse reactions/Side effects include:

• diarrhea
• vomiting
• nausea
• abdominal pains
• constipation
• meteorism
• dry mouth
• increased or decreased appetite
• asthenia
• headache
• sleeplessness
• vertigo
• thrombocytopenia
• granulocytopenia
• leukocytopenia
• skin eruption
• erythema
• myalgia
• arthralgia
• muscle or bone pain

[edit] Drug interactions

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

[edit] Overdosage

There have been no data symptoms of overdosage of Rabeprazole about.

[edit] How supplied

Rabeprazole as Aciphex and Pariet is supplied in:

• Tablet, Enteric-Coated; 10mg
• Tablet, Enteric-Coated; 20mg

[edit] References

• Morii M, Takata H, Fujisaki H, Takeguchi N., The potency of substituted benzimidazoles such as E3810, omeprazole, Ro 18-5364 to inhibit gastric H+, K(+)-ATPase is correlatedwith the rate of acid-activation of the inhibitor, Biochem Pharmacol. 1990 Feb 15;39(4):661-7.
• Prakash A, Faulds D., Rabeprazole, Drugs. 1998 Feb;55(2):261-7; discussion 268.

[edit] External links

• Official product site