roxatidine

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roxatidine acetate hydrochloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/11/03 15:50:35」(JST)

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Roxatidine acetate

Systematic (IUPAC) name
2-oxo-2-(3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino)ethyl acetate
Clinical data
Routes of administration	Oral
Pharmacokinetic data
Bioavailability	80–90%
Protein binding	5–7%
Metabolism	Hepatic deacetylation Minor involvement of CYP2D6 and CYP2A6
Biological half-life	5–7 hours
Excretion	Renal
Identifiers
CAS Registry Number	78628-28-1 N
ATC code	A02BA06
PubChem	CID: 5105
DrugBank	DB08806 Y
ChemSpider	4926 Y
UNII	IV9VHT3YUM Y
KEGG	D08495 Y
ChEMBL	CHEMBL46102 Y
Chemical data
Formula	C19H28N2O4
Molecular mass	348.437 g/mol
SMILES O=C(OCC(=O)NCCCOc1cc(ccc1)CN2CCCCC2)C
InChI InChI=1S/C19H28N2O4/c1-16(22)25-15-19(23)20-9-6-12-24-18-8-5-7-17(13-18)14-21-10-3-2-4-11-21/h5,7-8,13H,2-4,6,9-12,14-15H2,1H3,(H,20,23) Y Key:SMTZFNFIKUPEJC-UHFFFAOYSA-N Y
N (what is this?)  (verify)

Roxatidine acetate is a specific and competitive histamine H₂ receptor antagonist drug that is used to treat gastric ulcers, Zollinger–Ellison syndrome, erosive esophagitis, gastro-oesophageal reflux disease, and gastritis.

Pharmacodynamic studies showed that 150 mg of roxatidine acetate were optimal in suppressing gastric acid secretion, and that a single bedtime dose of 150 mg was more effective than a dose of 75 mg twice daily in terms of inhibiting nocturnal acid secretion.

It is available in countries including China, Japan, Korea, Germany, Italy, the Netherlands, Greece and South Africa.

References

English Journal

• Comparative validations of non-aqueous capillary electrophoresis and high-performance liquid chromatography methods for the simultaneous determination of histamine H2 receptor antagonists in human urine.

• Berzas Nevado JJ, Castañeda Peñalvo G, Rodríguez Dorado RM, Rodríguez Robledo V.SourceDepartment of Analytical Chemistry and Food Technology, Faculty of Chemistry, University of Castilla-La Mancha, Ciudad Real, Spain.
• Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.J Chromatogr B Analyt Technol Biomed Life Sci.2013 Jan 29;921-922C:56-63. doi: 10.1016/j.jchromb.2013.01.020. [Epub ahead of print]
• This paper reports a previously optimised method based on non-aqueous capillary electrophoresis (NACE) using UV detection for the separation and simultaneous determination of cimetidine (CIM), ranitidine (RAN), roxatidine (ROX), nizatidine (NIZ) and famotidine (FAM) in human urine. Separation is per
• PMID 23485449

• Effects of oral rehydration therapy on gastric volume and pH in patients with preanesthetic H2 antagonist.

• Nakai K, Niwa H, Kitayama M, Satoh Y, Hirota K.SourceDepartment of Anesthesiology, Seihoku Central Hospital, Goshogawara, Japan. kishiko@cc.hirosaki-u.ac.jp
• Journal of anesthesia.J Anesth.2012 Dec;26(6):936-8. doi: 10.1007/s00540-012-1449-8. Epub 2012 Jul 20.
• Recent preanesthetic fasting practice allows patients to take clear fluids up to 2 h before surgery without taking any antacid for the prophylaxis of aspiration pneumonia; this practice is defined as oral rehydration therapy (ORT). It has been reported that with ORT the gastric volume may be signif
• PMID 22814485

• Different effects of two types of H2-receptor antagonists, famotidine and roxatidine, on the mucus barrier of rat gastric mucosa.

• Shikama N, Ichikawa T, Iwai T, Yamamoto H, Kida M, Koizumi W, Ishihara K.SourceDepartment of Internal Medicine, Kitasato University School of Medicine, Sagamihara, Japan.
• Biomedical research (Tokyo, Japan).Biomed Res.2012 Feb;33(1):45-51.
• Compared with the aggressive factors, little attention has been paid to the mucosal defensive factors in ulcer therapy, and the role of the H2-receptor antagonists in gastric mucosal protection has not been well characterized. In the present study, the effects of different types of H2-receptor antag
• PMID 22361886

Japanese Journal

• Different effects of two types of H2-receptor antagonists, famotidine and roxatidine, on the mucus barrier of rat gastric mucosa

• Biomedical Research 33(1), 45-51, 2012
• NAID 130004470801

• Pharmacokinetics of the H2 Blocker Roxatidine Acetate Hydrochloride in Pediatric Patients, in Comparison with Healthy Adult Volunteers

• Drug Metabolism and Pharmacokinetics 27(4), 422-429, 2012
• NAID 130004463267

• Effect of lansoprazole versus roxatidine on prevention of bleeding and promotion of ulcer healing after endoscopic submucosal dissection for superficial gastric neoplasia

• Journal of gastroenterology 46(11), 1267-1272, 2011-11-01
• NAID 10030294788

Related Links

• Roxatidine - Wikipedia, the free encyclopedia

Roxatidine acetate is a specific and competitive H2 receptor antagonist. The antisecretory effect of roxatidine acetate is mediated by its main metabolite, roxatidine. Pharmacodynamic studies revealed that 150 mg of roxatidine acetate were ...

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