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Roxatidine
Systematic (IUPAC) name
2-oxo-2-(3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino)ethyl acetate
Identifiers
CAS number 78628-28-1
ATC code A02BA06
PubChem 5105
Chemical data
Formula C 19H28N2O4  
Mol. mass 348.437 g/mol
Pharmacokinetic data
Bioavailability 80–90%
Protein binding 5–7%
Metabolism Hepatic deacetylation
Minor involvement of CYP2D6 and CYP2A6
Half life 5–7 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral

Roxatidine acetate is a specific and competitive H2 receptor antagonist. The antisecretory effect of roxatidine acetate is mediated by its main metabolite, roxatidine. Pharmacodynamic studies revealed 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.

Roxatidine acetate has no antiandrogenic effects and does not influence drug-metabolizing enzymes in the liver.

It is currently sold in South Africa under the tradename Roxit.

Structure of roxatidine, the metabolite and active pharmaceutical ingredient.







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