Roxatidine acetate is a specific and competitive H2 receptor antagonist. It is currently approved in South Africa under the tradename Roxit.
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|Weight||Average: 348.4366 |
For the treatment of disorders of the upper gastro-intestinal region that are due to an excess of hydrochloric acid in the gastric juice, i.e. duodenal ulcers, benign gastric ulcers. Also for prophylaxis of recurrent gastric and duodenal ulcers
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Roxatidine acetate suppresses the effect of histamine on the parietal cells of the stomach (H2-receptor antagonist). This suppressive action is dose-dependent. As a result, the production and secretion, particularly of gastric acid, are reduced. Roxatidine acetate has no antiandrogenic effects and does not influence drug-metabolizing enzymes in the liver.
|Mechanism of action|
The H2 antagonists are competitive inhibitors of histamine at the parietal cell H2 receptor. They suppress the normal secretion of acid by parietal cells and the meal-stimulated secretion of acid. They accomplish this by two mechanisms: histamine released by ECL cells in the stomach is blocked from binding on parietal cell H2 receptors which stimulate acid secretion, and other substances that promote acid secretion (such as gastrin and acetylcholine) have a reduced effect on parietal cells when the H2 receptors are blocked.
Well absorbed orally (80–90% bioavailability).
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Roxatidine acetate is rapidly metabolised to the primary, active desacetyl metabolite.
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Oral, mouse LD50: 1000 mg/kg
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|ATC Codes||A02BA06 — Roxatidine|
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|MSDS||Download (1.19 MB)|
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|Description||This compound belongs to the class of chemical entities known as n-benzylpiperidines. These are heterocyclic Compounds containing a piperidine ring conjugated to a benzyl group through one nitrogen ring atom.|
|Super Class||Organic compounds|
|Alternative Parents||Benzylamines / Phenol ethers / Phenoxy compounds / Phenylmethylamines / Alkyl aryl ethers / Aralkylamines / Amino acids and derivatives / Carboxylic acid esters / Secondary carboxylic acid amides / Trialkylamines / Monocarboxylic acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds|
|Substituents||N-benzylpiperidine / Phenoxy compound / Benzylamine / Phenol ether / Phenylmethylamine / Alkyl aryl ether / Aralkylamine / Monocyclic benzene moiety / Benzenoid / Amino acid or derivatives/ Carboxamide group / Carboxylic acid ester / Secondary carboxylic acid amide / Tertiary amine / Tertiary aliphatic amine / Monocarboxylic acid or derivatives / Ether / Carboxylic acid derivative / Azacycle / Organonitrogen compound / Organic oxide / Organic nitrogen compound / Amine / Carbonyl group / Organooxygen compound / Hydrocarbon derivative / Organic oxygen compound / Organopnictogen compound / Aromatic heteromonocyclic compound|
|Molecular Framework||Aromatic heteromonocyclic compounds|
|External Descriptors||Not Available|
- Pharmacological action
- General Function:
- Histamine receptor activity
- Specific Function:
- The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and, through a separate G protein-dependent mechanism, the phosphoinositide/protein kinase (PKC) si...
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- Molecular Weight:
- 40097.65 Da
- Agrawal SS, Alvin Jose M: Roxatidine, an H(2) receptor blocker, is an estrogenic compound--experimental evidence. Syst Biol Reprod Med. 2010 Aug;56(4):286-91. doi: 10.3109/19396368.2010.496894. [PubMed:20718616 ]