Roxatidine acetate

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Roxatidine acetate
Roxatidine acetate.svg
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
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H28N2O4
Molar mass348.437 g/mol g·mol−1
3D model (JSmol)
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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 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[edit]

  1. ^ a b 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. ^ a b 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.