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]
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| Routes of administration | Oral |
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| Bioavailability | 80–90% |
| Protein binding | 5–7% |
| Metabolism | Hepatic deacetylation Minor involvement of CYP2D6 and CYP2A6 |
| Elimination half-life | 5–7 hours |
| Excretion | Renal |
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| Formula | C19H28N2O4 |
| Molar mass | 348.437 g/mol g·mol−1 |
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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
- 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.
- BioSpectrum Bureau 1 November 2012 Sinhuan's generic heart drug gets production approval
- Fischer, János; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 444. ISBN 9783527607495.
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