Pifatidine
Pifatidine Uses, Dosage, Side Effects, Food Interaction and all others data.
Pifatidine is a specific and competitive H2 receptor antagonist. It is currently approved in South Africa under the tradename Roxit.
Pifatidine 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. Pifatidine has no antiandrogenic effects and does not influence drug-metabolizing enzymes in the liver.
| Trade Name | Pifatidine |
| Generic | Roxatidine acetate |
| Roxatidine acetate Other Names | Pifatidine |
| Type | |
| Formula | C19H28N2O4 |
| Weight | Average: 348.4366 Monoisotopic: 348.204907394 |
| Protein binding | 5-7% |
| Groups | Experimental |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
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
How Pifatidine works
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.
Toxicity
Oral, mouse LD50: 1000 mg/kg
Elimination Route
Well absorbed orally (80–90% bioavailability).
Half Life
5-6 hours
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