Roxatidine

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	C19H28N2O4
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.^{[citation needed]}

Roxatidine acetate has no antiandrogenic effects and does not influence drug-metabolizing enzymes in the liver.^{[citation needed]}

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

Structure of roxatidine, the metabolite and active pharmaceutical ingredient.

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