Roxatidine acetate

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 Number	78628-28-1
ATC code	A02BA06 (WHO)
PubChem	CID 5105
DrugBank	DB08806
ChemSpider	4926
UNII	IV9VHT3YUM
KEGG	D08495
ChEMBL	CHEMBL46102
Chemical data
Formula	C19H28N2O4
Molar 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) Key:SMTZFNFIKUPEJC-UHFFFAOYSA-N
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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.^[1][2]

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.^[1]

It is available in countries including China, Japan, Korea, Germany, Italy, the Netherlands, Greece and South Africa.^[2]

References

1. Murdoch D, McTavish D (1991). "Roxatidine acetate. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic potential in peptic ulcer disease and related disorders". Drugs 42 (2): 240–260. doi:10.2165/00003495-199142020-00006. PMID 1717223.
2. BioSpectrum Bureau 1 November 2012 Sinhuan's generic heart drug gets production approval