カプレオマイシン

カプレオマイシン 化学特性,用途語,生産方法

• 効能

  抗結核薬, タンパク質合成阻害薬

• 説明

  Capreomycin is a semisynthetic antibiotic (34.1.21) that is isolated from the cultural fluid of Streptomyces capreolus, and it is a complex of a minimum of four microbiologically active ingredients that have only partially been characterized.
  Capreomycin has a pronounced suppressive effect against Mycobacterium tuberculosis and Mycobacterium bovis. Most strains of Mycobacterium kansasii are also sensitive to kanamycin, while other, nontuberculous strains are not sensitive to it. It is often used upon necessity of using parenternal therapy through deep intramuscular injections. Capreomycin is less toxic than kanamycin and has somewhat more of a bacteriostatic effect. Synonyms of this drug are capromycin, capastat, ogostal, and others.

• 使用

  Capreomycin is a complex of cyclic pentopeptides isolated from Streptomyces capreolus, first reported in 1962. The complex has two major components, IA and IB, with an exocyclic lysine residue and two minor delysinyl components, IIA and IIB. Capreomycin is a potent antibiotic with activity against mycobateria, Gram positive and Gram negative organisms. Capreomycin acts by binding to the 23S ribosomal subunit, disrupting protein synthesis.

• 適応症

  Capreomycin (Capastat) is a polypeptide antibiotic derived from Streptomyces capreolus. It is bacteriostatic against most strains of M. tuberculosis, including the MDR strain. In addition, it is active against M. kansasii, M. avium, and in high concentrations, some grampositive and gram-negative bacteria. Like other antitubercular drugs, resistance to capreomycin occurs rapidly if the drug is used alone.There is no cross-resistance between streptomycin and capreomycin, but some isolates resistant to capreomycin are resistant to viomycin.

• 薬理学

  Capreomycin is poorly absorbed from GI tract and so must be given parenterally. It is excreted mainly unchanged in the urine following glomerular filtration. Capreomycin is a used as a second-line agent in combination with other drugs. It appears to be particularly useful in multidrug regimens for the treatment of drugresistant tuberculosis, especially with streptomycin resistance. Capreomycin is associated with ototoxicity and nephrotoxicity, and these adverse effects can be severe in patients with preexisting renal insufficiency.

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