Roxatidine acetate

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]

Roxatidine acetate
Clinical data
Routes of
administration		Oral
ATC code
Pharmacokinetic data
Bioavailability80–90%
Protein binding5–7%
MetabolismHepatic deacetylation
Minor involvement of CYP2D6 and CYP2A6
Elimination half-life5–7 hours
ExcretionRenal
Identifiers
IUPAC name
  • 2-oxo-2-(3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino)ethyl acetate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H28N2O4
Molar mass348.443 g·mol−1
3D model (JSmol)
SMILES
  • O=C(C)OCC(=O)NCCCOc1cccc(c1)CN2CCCCC2
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
 NY (what is this?)  (verify)

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 was patented in 1979 and approved for medical use in 1986.[3] 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. S2CID 46973503.
  2. BioSpectrum Bureau 1 November 2012 Sinhuan's generic heart drug gets production approval
  3. Fischer, János; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 444. ISBN 9783527607495.


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