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Roxatidine


Roxatidine
Systematic (IUPAC) name
3-[3-(1-piperidylmethyl)phenoxy]propylcarbamoylmethyl 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.

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

v • d • e Drugs for acid related disorders: Drugs for peptic ulcer and GERD/GORD (A02B)
H₂-receptor antagonists	Cimetidine, Famotidine, Nizatidine, Ranitidine, Roxatidine
Prostaglandins/analogues	Misoprostol, Enprostil
Proton pump inhibitors	Esomeprazole, Lansoprazole, Omeprazole, Pantoprazole, Rabeprazole, Tenatoprazole
Other	Carbenoxolone, Sucralfate, Pirenzepine