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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
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
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Chromones
  • (Iso)quinolines and Derivatives
  • Fluoroquinolones and Quinolones
Substructures
  • Hydroxy Compounds
  • Acetates
  • Pyridines and Derivatives
  • Benzene and Derivatives
  • Chromones
  • Carboxylic Acids and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • (Iso)quinolines and Derivatives
  • Imines
  • Fluoroquinolones and Quinolones
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.
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
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 299 dec °C PhysProp
water solubility 145 mg/L Not Available
logP 2.22 SANGSTER (1994)
Predicted Properties
Property Value Source
water solubility 4.59e-02 g/l ALOGPS
logP 2.18 ALOGPS
logP 2.5 ChemAxon
logS -3.9 ALOGPS
pKa (strongest acidic) 2.28 ChemAxon
pKa (strongest basic) -4.2 ChemAxon
physiological charge -2 ChemAxon
hydrogen acceptor count 8 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 121.21 ChemAxon
rotatable bond count 5 ChemAxon
refractivity 98.09 ChemAxon
polarizability 36.95 ChemAxon
药物相互作用
食物相互作用
Not Available

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