药品详细
Nedocromil(奈多罗米)
化学结构式图
中文名
奈多罗米
英文名
Nedocromil
分子式
C19H17NO7
化学名
9-ethyl-4,6-dioxo-10-propyl-4H,6H,9H-chromeno[7,6-b]pyridine-2,8-dicarboxylic acid
分子量
Average: 371.3408
Monoisotopic: 371.100501903
Monoisotopic: 371.100501903
CAS号
69049-73-6
ATC分类
R01A 未知;R03B 未知;S01G 解充血药及抗过敏药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. [PubChem]
生产厂家
- Allergan inc
- King pharmaceuticals inc
- Sanofi aventis us llc
封装厂家
- Allergan Inc.
- Fisons PLC
- King Pharmaceuticals Inc.
- Rhone Poulenc Rorer Respiratory
- Sanofi-Aventis Inc.
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
药理
Indication | For the treatment of mild to moderate asthma |
Pharmacodynamics | Nedocromil is a anti-inflammatory agent and can be administered directly to the bronchial mucosa. It has significant inhibitory effect on allergen-induced early and late asthmatic reactions and on bronchial hyperresponsiveness. |
Mechanism of action | Nedocromil has been shown to inhibit the in vitro activation of, and mediator release from, a variety of inflammatory cell types associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. Nedocromil inhibits activation and release of inflammatory mediators such as histamine, prostaglandin D2 and leukotrienes c4 from different types of cells in the lumen and mucosa of the bronchial tree. These mediators are derived from arachidonic acid metabolism through the lipoxygenase and cyclo-oxygenase pathways. The mechanism of action of nedocromil may be due partly to inhibition of axon reflexes and release of sensory neuropeptides, such as substance P, neurokinin A, and calcitonin-geneñrelated peptides. The result is inhibition of bradykinin-induced bronchoconstriction. Nedocromil does not posess any bronchodilator, antihistamine, or corticosteroid activity. |
Absorption | Low |
Volume of distribution | Not Available |
Protein binding | approximately 89% protein bound in human plasma over a concentration range of 0.5 to 50 µg/mL |
Metabolism |
Nedocromil is not metabolized after IV administration and is excreted unchanged.
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Route of elimination | It is not metabolized and is eliminated primarily unchanged in urine (70%) and feces (30%). |
Half life | ~3.3 hours |
Clearance | Not Available |
Toxicity | Side effects include headache, nasal congestion, ocular burning, irritation and stinging, unpleasant taste, cough, difficulty breathing, noisy breathing, shortness of breath, tightness in chest, wheezing, conjunctivitis, blurred vision, change in color vision, difficulty seeing at night, increased sensitivity of eyes to sunlight. |
Affected organisms |
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Pathways | Not Available |
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
食物相互作用
Not Available