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药品详细

Nystatin(制霉菌素)

化学结构式图
中文名
制霉菌素
英文名
Nystatin
分子式
C47H75NO17
化学名
(21E,23E,25E,27E,31E,33E)-20-{[(3S,4S,5S,6R)-4-amino-3,5-dihydroxy-6-methyloxan-2-yl]oxy}-4,6,8,11,12,16,18,36-octahydroxy-35,37,38-trimethyl-2,14-dioxo-1-oxacyclooctatriaconta-21,23,25,27,31,33-hexaene-17-carboxylic acid
分子量
Average: 926.0949
Monoisotopic: 925.503499979
CAS号
1400-61-9
ATC分类
A07A 未知;D01A 未知;G01A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Nystatin is a polyene antifungal drug to which many molds and yeasts are sensitive, including Candida spp. Nystatin has some toxicity associated with it when given intravenously, but it is not absorbed across intact skin or mucous membranes. It is considered a relatively safe drug for treating oral or gastrointestinal fungal infections.

生产厂家
  • Actavis mid atlantic llc
  • Alpharma us pharmaceuticals division
  • Altana inc
  • Apothecon inc div bristol myers squibb
  • Barlan pharmacal co inc
  • Bausch and lomb pharmaceuticals inc
  • Bayer pharmaceuticals corp
  • Bristol myers squibb
  • Bristol myers squibb co
  • Coastal pharmaceuticals inc
  • Dava pharmaceuticals inc
  • E fougera div altana inc
  • Glenmark generics inc usa
  • Holland rantos co inc
  • Kv pharmaceutical co
  • Lederle laboratories div american cyanamid co
  • Morton grove pharmaceuticals inc
  • Mutual pharmaceutical co inc
  • Odyssey pharmaceuticals inc
  • Paddock laboratories inc
  • Par pharmaceutical inc
  • Perrigo new york inc
  • Pharmaderm div altana inc
  • Pharmafair inc
  • Quantum pharmics ltd
  • Roxane laboratories inc
  • Sandoz inc
  • Savage laboratories inc div altana inc
  • Taro pharmaceuticals usa inc
  • Teva pharmaceuticals usa inc
  • Upsher smith laboratories inc
  • Usl pharma inc
  • Vintage pharmaceuticals inc
  • Vintage pharmaceuticals llc
  • Vistapharm inc
  • Warner chilcott co llc
  • Watson laboratories inc
  • Westwood squibb pharmaceuticals inc
  • Wockhardt eu operations (swiss) ag
  • X gen pharmaceuticals inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Akaike N, Harata N: Nystatin perforated patch recording and its applications to analyses of intracellular mechanisms. Jpn J Physiol. 1994;44(5):433-73. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Aminoglycosides
Substructures
  • Carboxylic Acids and Derivatives
  • Aminoglycosides
  • Hydroxy Compounds
  • Alkanes and Alkenes
  • Pyrans
  • Acetates
  • Acetals and Derivatives
  • Lactones
  • Aliphatic and Aryl Amines
  • Ethers
  • Amino Alcohols
  • Alcohols and Polyols
  • Heterocyclic compounds
  • Ketones
适应症
药理
Indication For treatment of cutaneous or mucocutaneous mycotic infections caused by Candida species
Pharmacodynamics Nystatin is an antibiotic which is both fungistatic and fungicidal in vitro against a wide variety of yeasts and yeast-like fungi, including Candida albicans, C. parapsilosis, C. tropicalis, C. guilliermondi, C. pseudotropicalis, C. krusei, Torulopsis glabrata, Tricophyton rubrum, T. mentagrophytes. Nystatin acts by binding to sterols in the cell membrane of susceptible species resulting in a change in membrane permeability and the subsequent leakage of intracellular components. On repeated subculturing with increasing levels of nystatin, Candida albicans does not develop resistance to nystatin. Generally, resistance to nystatin does not develop during therapy. However, other species of Candida (C. tropicalis, C. guilliermondi, C. krusei, and C. stellatoides) become quite resistant on treatment with nystatin and simultaneously become cross resistant to amphotericin as well. This resistance is lost when the antibiotic is removed. Nystatin exhibits no appreciable activity against bacteria, protozoa, or viruses.
Mechanism of action Nystatin exerts its antifungal activity by binding to ergosterol found in fungal cell membranes. Binding to ergosterol causes the formation of pores in the membrane. Potassium and other cellular constituents leak from the pores causing cell death.
Absorption Nystatin is not absorbed from intact skin or mucous membrane.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Fungi
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 160 °C Not Available
water solubility 360 mg/L (at 24 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP 0.5 Not Available
Predicted Properties
Property Value Source
water solubility 6.60e-02 g/l ALOGPS
logP -2.8 ALOGPS
logP -2.7 ChemAxon
logS -4.2 ALOGPS
pKa (strongest acidic) 3.62 ChemAxon
pKa (strongest basic) 9.11 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 17 ChemAxon
hydrogen donor count 12 ChemAxon
polar surface area 327.45 ChemAxon
rotatable bond count 3 ChemAxon
refractivity 245.18 ChemAxon
polarizability 102.11 ChemAxon
药物相互作用
食物相互作用
  • Take without regard to meals.

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