Roxatidine
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Roxatidine
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| Systematic (IUPAC) name | |
| 3-[3-(1-piperidylmethyl)phenoxy]propylcarbamoylmethyl acetate | |
| Identifiers | |
| CAS number | |
| ATC code | A02 |
| PubChem | |
| 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. |
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| 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.
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