药品详细
Nizatidine(尼扎替丁)
化学结构式图
中文名
尼扎替丁
英文名
Nizatidine
分子式
C12H21N5O2S2
化学名
dimethyl[(4-{[(2-{[(E)-1-(methylamino)-2-nitroethenyl]amino}ethyl)sulfanyl]methyl}-1,3-thiazol-2-yl)methyl]amine
分子量
Average: 331.457
Monoisotopic: 331.113666321
Monoisotopic: 331.113666321
CAS号
76963-41-2
ATC分类
A02B 未知
药物类型
small molecule
阶段
approved
商品名
Acinon;Antizid;Axid;Axid Ar;Calmaxid;Cronizat;Distaxid;Galitidin;Gastrax;Naxidine;Niatidine;Nizatidina [Spanish];Nizatidine [Usan:Ban:Inn:Jan];Nizatidinum [Latin];Nizax;Nizaxid;Panaxid;Splendil Er;Tazac;Ulcosol;Ulxid;Zanizal;Zinga;
同义名
基本介绍
A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers. [PubChem]
生产厂家
- Amneal pharmaceuticals
- Apotex inc
- Braintree laboratories inc
- Dr reddys laboratories ltd
- Genpharm inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Mylan pharmaceuticals inc
- Sandoz inc
- Smithkline beecham corp dba glaxosmithkline
- Teva pharmaceuticals usa inc
- Watson laboratories inc
- Wyeth consumer healthcare
封装厂家
- Affordable Pharmaceuticals LLC
- Amneal Pharmaceuticals
- Apotex Inc.
- Braintree Laboratories Inc.
- Cardinal Health
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Doctor Reddys Laboratories Ltd.
- Eon Labs
- H.J. Harkins Co. Inc.
- Lyne Laboratories Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Novopharm Ltd.
- Par Pharmaceuticals
- Patheon Inc.
- PD-Rx Pharmaceuticals Inc.
- Pharmedix
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prescript Pharmaceuticals
- Promex Medical Inc.
- Rebel Distributors Corp.
- Reliant Pharmaceuticals
- Sandhills Packaging Inc.
- Southwood Pharmaceuticals
- Stat Rx Usa
- Teva Pharmaceutical Industries Ltd.
- Torpharm Inc.
- UDL Laboratories
- Vangard Labs Inc.
- Watson Pharmaceuticals
- Wyeth Pharmaceuticals
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
gastric acid RELATED DISORDERS 中和胃酸;
药理
| Indication | For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, active benign gastric ulcer, and active duodenal ulcer. | ||||||||
| 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. | ||||||||
| 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%) | ||||||||
| Volume of distribution |
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| Protein binding | 35% | ||||||||
| 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).
Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.
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| Route of elimination | Not Available | ||||||||
| Half life | 1-2 hours | ||||||||
| Clearance |
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| Toxicity | Oral, rat LD50: 301 mg/kg. Symptoms of overdose include cholinergic-type effects including lacrimation, salivation, emesis, miosis, and diarrhea. | ||||||||
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理化性质
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| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Atazanavir | This gastric pH modifier decreases the levels/effects of atazanavir |
| 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. |
| Enoxacin | Nizatidine may decrease the absorption of enoxacin. |
| Itraconazole | The H2-receptor antagonist, nizatidine, may decrease the absorption of itraconazole. |
| Ketoconazole | The H2-receptor antagonist, nizatidine, may decrease the absorption of ketoconazole. |
食物相互作用
- Avoid alcohol.
- Avoid excessive quantities of coffee or tea (Caffeine).
- Do not take Aluminum or magnesium antacids or supplements while on this medication.
- May take Vitamin D.
- No iron, zinc or fluoride within 2 hours of taking this medication.
- Take without regard to meals.
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