Roxatidine acetate

Chemical compound
  • A02BA06 (WHO)
Pharmacokinetic dataBioavailability80–90%Protein binding5–7%MetabolismHepatic deacetylation
Minor involvement of CYP2D6 and CYP2A6Elimination half-life5–7 hoursExcretionRenalIdentifiers
  • 2-oxo-2-(3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino)ethyl acetate
CAS Number
  • 78628-28-1 checkY
  • roxatidine: 78273-80-0 checkY
PubChem CID
  • 5105
DrugBank
  • DB08806 checkY
ChemSpider
  • 4926 checkY
UNII
  • ZUP3LSD0DO
  • roxatidine: IV9VHT3YUM checkY
KEGG
  • D08495 checkY
ChEMBL
  • ChEMBL46102 checkY
CompTox Dashboard (EPA)
  • DTXSID2048325 Edit this at Wikidata
Chemical and physical dataFormulaC19H28N2O4Molar mass348.443 g·mol−13D model (JSmol)
  • Interactive image
  • O=C(C)OCC(=O)NCCCOc1cccc(c1)CN2CCCCC2
  • 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) checkY
  • Key:SMTZFNFIKUPEJC-UHFFFAOYSA-N checkY
 ☒NcheckY (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.[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

  1. ^ a b Murdoch D, McTavish D (August 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. ^ a b BioSpectrum Bureau 1 November 2012 Sinhuan's generic heart drug gets production approval
  3. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 444. ISBN 9783527607495.
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H1
Agonists
Antagonists
  • Unknown/unsorted: Azanator
  • Belarizine
  • Elbanizine
  • Flotrenizine
  • GSK1004723
  • Napactadine
  • Tagorizine
  • Trelnarizine
  • Trenizine
H2
Agonists
Antagonists
H3
Agonists
Antagonists
H4
Agonists
Antagonists
See also
Receptor/signaling modulators
Monoamine metabolism modulators
Monoamine reuptake inhibitors
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Drugs for peptic ulcer and GERD/GORD (A02B)
H2 antagonists ("-tidine")
Prostaglandins (E)/
analogues ("-prost-")
Proton-pump inhibitors
("-prazole")
Potassium-competitive
acid blockers ("-prazan")
Others
Combinations
  • See also: Helicobacter pylori eradication protocols
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