Rabeprazole
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Rabeprazole
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| Systematic (IUPAC) name | |
| 2-[(4-(3-methoxypropoxy)- 3-methyl-pyridin-2-yl) methylsulfinyl]- 1H-benzoimidazole | |
| Identifiers | |
| CAS number | |
| ATC code | A02 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C18H21N3O3S |
| Mol. mass | 359.444 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | 52% |
| Metabolism | Hepatic |
| Half life | 1 - 1.5 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Licence data |
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| Pregnancy cat. |
B(US) |
| Legal status | |
| Routes | Oral |
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 and Pariet.
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[edit] Pharmacology
Rabeprazole is a prodrug (metabolized by the cytochrome P450 (or CYP450)) - in the acid environment of the parietal cells it turns 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 shows synergistic activity with some antibiotics. Rabeprazole has been demonstrated to be effective in patients with pathological hypersecretory activity (incl. Zollinger-Ellison Syndrome).
[edit] Indications and usage
- gastric ulcer
- peptic ulcer (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)
- Helicobactor Pylori Eradication to Reduce Risk of Duodenal Ulcer Recurrence
[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:
- 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.
- 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 is no available data on symptoms of rabeprazole overdose.
[edit] How supplied
Rabeprazole as Aciphex,Rabeloc, Pariet is supplied in:
[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
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