QuickView for Nizatidine (compound)

Summary
General Info

PubChem

PubChem Compound 3033637

Name:	Nizatidine
PubChem Compound ID:	3033637
Description:	A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers.
Molecular formula:	C₁₂H₂₁N₅O₂S₂
Molecular weight:	331.46 g/mol
Synonyms:	LY-139037; Gastrax; Acinon; Nizax; Acinon (TN); Cronizat; ZL-101; C07270; Distaxid; Naxidine. show more » LY-139037; Gastrax; Acinon; Nizax; Acinon (TN); Cronizat; ZL-101; C07270; Distaxid; Naxidine; Nizatidine; Zanizal; Nizatidine (JAN/USP); HSDB 3574; N-(2-(((2-((Dimethylamino)methyl)-4-thiazolyl)methyl)thio)ethyl)-N'-methyl-2-nitro-1,1-ethenediamine; Splendil ER; 1,1-Ethenediamine, N-(2-(((2-((dimethylamino)methyl)-4-thiazoly)methyl)thio)ethyl)-N'-methyl-2-nitro-; Ulxid; Nizatidine [USAN:BAN:INN:JAN]; Tazac; Axid (TN); Nizatidinum [Latin]; ZE-101; D00440; Nizaxid; Ulcosol; BRN 4846056; N-(4-(6-Methylamino-7-nitro-2-thia-5-aza-6-hepten-1-yl)-2-thiazolylmethyl)-N,N-dimethylamin; Axid; Antizid; CAS-76963-41-2; Galitidin; NCGC00016934-01; Calmaxid; LY 139037; Nizatidina [Spanish]; 76963-41-2; Panaxid; Zinga; 1,1-Ethenediamine, N-(2-(((2-((dimethylamino)methyl)-4-thiazolyl)methyl)thio)ethyl)-N'-methyl-2-nitro- show less «

DrugBank

Identification

Name:	Nizatidine
Name (isomeric):	DB00585
Drug Type:	small molecule
Description:	A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers.
Brand:	Panaxid, Nizatidina [Spanish], Zinga, Ulcosol, Tazac, Nizatidinum [Latin], Nizaxid, Cronizat, Calmaxid, Zanizal, Splendil Er, Axid, Acinon, Antizid, Axid Ar, Naxidine, Distaxid, Ulxid, Nizax, Niatidine, Galitidin, Gastrax, Nizatidine [Usan:Ban:Inn:Jan]
Category:	Anti-Ulcer Agents, Histamine H2 Antagonists
CAS number:	76963-41-2

Pharmacology

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 nizati... show more » 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. show less «
Mechanism of Action:	Nizatidine competes with histamine for binding at the H₂-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.
Absorption:	Rapid (bioavailability of nizatidine exceeds 70%)
Protein binding:	35%
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).
Half Life:	1-2 hours
Clearance:	40-60 L/h 7 – 14 L/h [functionally anephric patients]
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

Interactions

Food interaction:

Avoid alcohol.

No iron, zinc or fluoride within 2 hours of taking this medication.

May take Vitamin D.

Take without regard to meals.

Avoid excessive quantities of coffee or tea (Caffeine).

Drug interaction:

Itraconazole	The H2-receptor antagonist, nizatidine, may decrease the absorption of itraconazole.
Atazanavir	This gastric pH modifier decreases the levels/effects of atazanavir
Enoxacin	Nizatidine may decrease the absorption of enoxacin.
Cefditoren	H2-Antagonists such as nizatidine may decrease the serum concentration of cefditoren. Cefditoren prescribing information recommends to avoid concomitant use with H2-antagonists (eg, famotidine, ranitidine) and antacids as well. Consider alternative methods to minimize/control acid reflux (eg, diet modification) or alternative antimicrobial therapy if use of H2-antagonists can not be avoided.
Ketoconazole	The H2-receptor antagonist, nizatidine, may decrease the absorption of ketoconazole.

Targets

Histamine H2 receptor

Transporters

Multidrug resistance protein 1