| Item |
Information |
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Drug Groups
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approved |
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Description
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A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers. [PubChem] |
| Indication |
For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, active benign gastric ulcer, and active duodenal ulcer. |
| Pharmacology |
Nizatidine is a competitive, reversible inhibitor of histamine at the histamine H2-receptors, particularly those in the gastric parietal cells. By inhibiting the action of histamine on stomach cells, nizatidine reduces stomach acid production. Nizatidine had no demonstrable antiandrogenic action. Full-dose therapy for the problems treated by nizatidine lasts no longer than 8 weeks. It has been demonstrated that treatment with a reduced dose of nizatidine is effective as maintenance therapy following healing of active duodenal ulcers. |
| Toxicity |
Oral, rat LD50: 301 mg/kg. Symptoms of overdose include cholinergic-type effects including lacrimation, salivation, emesis, miosis, and diarrhea. |
| Affected Organisms |
| • |
Humans and other mammals |
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| Biotransformation |
Hepatic. Less than 7% of an oral dose is metabolized as N2-monodes-methylnizatidine, an H2-receptor antagonist, which is the principal metabolite excreted in the urine. Other likely metabolites are the N2-oxide (less than 5% of the dose) and the S-oxide (less than 6% of the dose). |
| Absorption |
Rapid (bioavailability of nizatidine exceeds 70%) |
| Half Life |
1-2 hours |
| Protein Binding |
35% |
| Distribution |
* 0.8 to 1.5 L/kg |
| Clearance |
* 40-60 L/h
* 7 – 14 L/h [functionally anephric patients] |
| External Links |
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