Product Name

Nizatidine

CAS Number

76963-41-2

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Product Name:
Nizatidine
CAS Number:
76963-41-2
Indication:
For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, active benign gastric ulcer, and active duodenal ulcer.
Mode of Action:

Nizatidine competes with histamine for binding at the H_-receptors on the gastric basolateral membrane of parietal cells. Competitive inhibition results in reduction of basal and nocturnal gastric acid secretions. The drug also decreases the gastric acid response to stimuli such as food, caffeine, insulin, betazole, or pentagastrin.

Pharmacodynamics:

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.

Metabolism:

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).

Toxicity:

Oral, rat LD50: 301 mg/kg. Symptoms of overdose include cholinergic-type effects including lacrimation, salivation, emesis, miosis, and diarrhea.

IUPAC:
dimethyl[(4-{[(2-{[(E)-1-(methylamino)-2-nitroethenyl]amino}ethyl)sulfanyl]methyl}-1, 3-thiazol-2-yl)methyl]amine
ATC:
A02BA04
PubChem:
3033637
DrugBank:
DB00585 (APRD00706)
Formula:
C49H66N10O10S2
Molecular Mass:
331.457
SMILES:
CNC(NCCSCC1=CSC(CN(C)C)=N1)=C/[N+]([O-])=O
AHFS Code:
56:28.1
InChi:
SGXXNSQHWDMGGP-IZZDOVSWSA-N

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