フロキサシリン

フロキサシリン 化学特性,用途語,生産方法

• 効能

  抗生物質, 細胞壁合成阻害薬

• 説明

  Chemically this is 3(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolyl penicillin; this differs from dicloxacillin only by the substitution of a fluorine for a chlorine atom (Sutherland et al., 1970). It comes as oral capsules of 250 and 500 mg, as a suspension of 25 and 50 mg/ml, and in an injectable formulation of 500 mg and 1 g.

• 使用

  Antibacterial.

• 定義

  ChEBI: A penicillin compound having a 6beta-[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazole-4-carboxamido] side-chain.

• 抗菌性

  There is complete cross-resistance with other penicillinase-stable penicillins.

• 一般的な説明

  Flucloxacillin was synthesized by Beecham Research Laboratories in 1962 as a penicillinase-stable and orally active semisynthetic penicillin. It shows almost the same activity as dicloxacillin, and it has slightly higher serum and tissue concentrations than dicloxacillin. This drug has been used to treat pyoderma, sepsis, and postoperative infections as well as ear and nose, respiratory tract, and other infections caused by Staphylococcus and Streptococcus, including benzylpenicillin-resistant strains.

• 薬物動態学

  Oral absorption: c. 80%
  C_max 250 mg (oral): 11 mg/L after 0.5–1 h
  Plasma half-life: 2 h
  Plasma protein binding: 95%
  Absorption and distribution
  It is well absorbed after oral administration and penetrates rapidly into extravascular exudates. Its high protein binding limits its diffusion, notably into the normal CSF.
  Metabolism and excretion
  Flucloxacillin is partly metabolized in the liver and about 10% of the plasma concentration is made up of metabolites. It is more slowly eliminated than cloxacillin. Some appears in the bile but about 50–80% of an oral dose is recovered from the urine, about 20% as metabolites.

• 臨床応用

  Uses are those of group 3 penicillins.

• 副作用

  In patients treated by intravenous infusion, about 5% developed phlebitis by the first and 15% by the second day, after which the proportion rose dramatically. Side effects are otherwise those common to penicillins.

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