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Mechanism of Action
Nizatidine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
Pharmacology
Nizatidine¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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
Nizatidine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
Protein Binding
Nizatidine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 35%
Half-life
Nizatidine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1-2 hours
Absorption
Nizatidine¿¡ ´ëÇÑ Absorption Á¤º¸ Rapid (bioavailability of nizatidine exceeds 70%)
Biotransformation
Nizatidine¿¡ ´ëÇÑ Biotransformation Á¤º¸ 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
Nizatidine¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, rat LD50 : 301 mg/kg. Symptoms of overdose include cholinergic-type effects including lacrimation, salivation, emesis, miosis, and diarrhea.
Drug Interactions
Nizatidine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Atazanavir This gastric pH modifier decreases the levels/effects of atazanavirEnoxacin The agent decreases the absorption of enoxacinItraconazole The anti-H2 decreases the absorption of the imidazoleKetoconazole The anti-H2 decreases the absorption of the imidazole
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Food Interaction
Nizatidine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Avoid excessive quantities of coffee or tea (Caffeine).No iron, zinc or fluoride within 2 hours of taking this medication.May take Vitamin D.Do not take Aluminum or magnesium antacids or supplements while on this medication.Take without regard to meals.
Drug Target
[Drug Target]
Description
Nizatidine¿¡ ´ëÇÑ Description Á¤º¸ A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers. [PubChem]
Drug Category
Nizatidine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Ulcer AgentsHistamine H2 Antagonists
Smiles String Canonical
Nizatidine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CNC(NCCSCC1=CSC(CN(C)C)=N1)=C[N+]([O-])=O
Smiles String Isomeric
Nizatidine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN\C(NCCSCC1=CSC(CN(C)C)=N1)=C/[N+]([O-])=O
InChI Identifier
Nizatidine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C12H21N5O2S2/c1-13-11(6-17(18)19)14-4-5-20-8-10-9-21-12(15-10)7-16(2)3/h6,9,13-14H,4-5,7-8H2,1-3H3/b11-6+
Chemical IUPAC Name
Nizatidine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (E)-N-[2-[[2-(dimethylaminomethyl)-1,3-thiazol-4-yl]methylsulfanyl]ethyl]-N'-methyl-2-nitroethene-1,1-diamine
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