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药品详细

Spectinomycin(大观霉素)

化学结构式图
中文名
大观霉素
英文名
Spectinomycin
分子式
C14H24N2O7
化学名
(1R,3S,5R,8R,10R,11S,12S,13R,14S)-8,12,14-trihydroxy-5-methyl-11,13-bis(methylamino)-2,4,9-trioxatricyclo[8.4.0.0^{3,8}]tetradecan-7-one
分子量
Average: 332.3496
Monoisotopic: 332.158351132
CAS号
1695-77-8
ATC分类
J01X Other Antibacterials
药物类型
small molecule
阶段
approved
商品名
Actinospectacin;Spectam;Togamycin;Trobicin;
同义名
Actinospectacina [Italian];Antibiotic 2233wp;Espectinomicina [INN-Spanish];SCM;Spectinomicina [Italian];Spectinomycin Di HCl;Spectinomycin HCl/ Sulphate;Spectinomycine [INN-French];Spectinomycinum [INN-Latin];
基本介绍

An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of gonorrhea.

生产厂家
  • Pharmacia and upjohn co
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
  • Amynoglycosides
Substructures
  • Glycerol and Derivatives
  • Hydroxy Compounds
  • Pyrans
  • Acetals and Derivatives
  • Aliphatic and Aryl Amines
  • Ethers
  • Dioxanes
  • Amynoglycosides
  • Amino Alcohols
  • Heterocyclic compounds
  • Alcohols and Polyols
  • Ketones
适应症
antibacterials 抗细菌;
药理
Indication For use in the treatment of acute gonorrheal urethritis and proctitis in the male and acute gonorrheal cervicitis and proctitis in the female when due to susceptible strains of Neisseria gonorrhoeae.
Pharmacodynamics Spectinomycin is an aminocyclitol antibiotic produced by a species of soil microorganism designated as Streptomyces spectabilis. In vitro studies have shown spectinomycin to be active against most strains of Neisseria gonorrhoeae (minimum inhibitory concentration <7.5 to 20 mcg/mL). Footprint studies indicate that spectinomycin exerts regional effects on ribosomal structure.
Mechanism of action Spectinomycin is an inhibitor of protein synthesis in the bacterial cell; the site of action is the 30S ribosomal subunit. It is bactericidal in its action.
Absorption Rapidly and almost completely absorbed after intramuscular injection.
Volume of distribution Not Available
Protein binding Not significant
Metabolism
Not Available
Route of elimination Not Available
Half life 1 to 3 hours in patients with normal renal function and 10 to 30 hours in patients with impaired renal function with a creatinine clearance < 20 mL per minute.
Clearance Not Available
Toxicity Acute oral toxicity (LD50): >5000 mg/kg [Rat]. Information on overdosage in humans is not available.
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways
Pathway Name SMPDB ID
Smp00258 Spectinomycin Pathway SMP00258
理化性质
Properties
State solid
Experimental Properties
Property Value Source
water solubility Easily soluble in cold water Not Available
logP -2.3 Not Available
pKa 6.95 MERCK INDEX (1996); pKa1
Predicted Properties
Property Value Source
water solubility 1.50e+02 g/l ALOGPS
logP -1.4 ALOGPS
logP -2.4 ChemAxon
logS -0.35 ALOGPS
pKa (strongest acidic) 8.58 ChemAxon
pKa (strongest basic) 9.4 ChemAxon
physiological charge 2 ChemAxon
hydrogen acceptor count 9 ChemAxon
hydrogen donor count 5 ChemAxon
polar surface area 129.51 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 75.44 ChemAxon
polarizability 33.39 ChemAxon
药物相互作用
食物相互作用
Not Available

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