ネオマイシン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H361：生殖能または胎児への悪影響のおそれの疑い

  H373：長期にわたる、または反復暴露により臓器の障 害のおそれ

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ と。

  P260：粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ と。

  P281：指定された個人用保護具を使用すること。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

  P314：気分が悪い時は、医師の診断/手当てを受けること。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

ネオマイシン 化学特性,用途語,生産方法

• 解説

  フラジオマイシンともいう．ネオマイシンA：C12H26N4O6(322.36)，BおよびC：C23H46N6O13(614.65)の3種類が知られている．アミノ配糖体抗生物質．放線菌Streptomyces fradiae，S.albogriseolusなどの培養液から，イオン交換樹脂または活性炭で吸着して分離される．塩基性の無色の結晶または粉末状物質．ネオマイシンBの分解生成物であるAの分解点250～256 ℃．"112.8°(水)．B，Cは非結晶体であるが，ライネッケ塩などとして結晶化する．"A：＋123°(水)，B：＋83°(0.2 mol L－1 塩酸)，C：＋121°(0.1 mol L－1 硫酸)．紫外部吸収極大は末端吸収以外ない．カナマイシン類と同様に，主としてグラム陽性菌に有効である．LD50 A：1250 mg/kg(マウス，皮下)，B：220 mg/kg(マウス，皮下)，C：290 mg/kg(マウス，皮下)．"
  森北出版「化学辞典（第2版）

• 用途

  ネオマイシン（neomycin）は1948年にウクライナ出身のセルマン?ワクスマンにより発見されたアミノグリコシド系抗生物質である。 ネオマイシンの作用機序はカナマイシンのそれと類似し、30Sリボソームに結合することにより細菌のタンパク質合成を阻害する。 比較的広範な抗菌スペクトルを有し、グラム陰性菌、グラム陽性菌ともに強く阻害する。 分子生物学の研究においてネオマイシン耐性遺伝子は、選択マーカーとして形質細胞の分離に利用される。

• 効能

  抗生物質, タンパク質合成阻害薬

• 説明

  Neomycin is an antibiotic from the aminoglycoside group, and has two isomers - neomycin Band neomycin C. Occupational contact dermatitis mainly occurs in workers at animal-feed mills, in veterinaries and in health workers.

• 使用

  Neomycin, like streptomycin, has a broad spectrum of antibacterial activity. It is effective with respect to the majority of Gram-negative and a few Gram-positive bacteria; staphylococci, pneumococci, gonococci, meningococci, and stimulants of dysentery. It is not very active with respect to streptococci. The antibiotic effect of neomycin with respect to many types of bacteria is higher than that of streptomycin. At the same time, microorganisms sensitive to neomycin become resistant to a lesser degree than streptomycin.
  It is used for various gastrointestinal diseases caused by microorganisms sensitive to it, including enteritis, which is caused by microbes that are resistant to antibiotics. However, because of its high oto- and nephrotoxicity, its local use is preferred for infected skin diseases, infected wounds, conjunctivitis, keratitis, and others. Synonyms of this drug are framycetin, soframycin, tautomycin, and others.

• 定義

  An antibiotic complex obtained from Streptomyces fradiae; it is soluble in water and methanol but insoluble in most organic solvents. It consists of three component substances, all of which function as antiinfective agents; some derivatives have fungicidal properties. The three types are A (also called neamine): C12H26N4O6; B: C 23H46N6O13 (also available as hydrochloride and sulfate); and C: C23H46O13

• 抗菌性

  Among other organisms susceptible in vitro (MIC 4–8 mg/L) are Pasteurella, Vibrio, Borrelia and Leptospira spp. It is active against M. tuberculosis, including streptomycin-resistant strains. Synergy has been reported with polymyxin B. The bactericidal effect is enhanced at alkaline pH.

• 獲得抵抗性

  Resistance is acquired in a stepwise fashion and staphylococci may become resistant as a result of prolonged topical use. The use of neomycin–bacitracin–polymyxin mixtures may contribute to this, as many strains resistant to neomycin are also resistant to bacitracin. Resistant enterobacteria may appear in the feces of patients treated orally and in those treated for prolonged periods; most have been found to possess multiple transferable antibiotic resistance. Cross-resistance with kanamycin is often due to the synthesis of APH(3′), although AAC(6′) some forms of AAC(3) and ANT(4′) also modify both neomycin and kanamycin. Resistant strains of Staph. aureus are usually more resistant to kanamycin than to neomycin. The rare enzyme AAC(1) confers resistance to neomycin and paromomycin, but not to other aminoglycosides.

• 接触アレルゲン

  Neomycin is an antibiotic complex of the aminoglycosides group, extracted from Streptomyces fradiae. It is composed of neomycin A (neamin) and an isomer neobiosamin, either neomycin B (framycetin or Soframycin?) or neomycin C. Its use has been progressively forbidden in cosmetics and as an additive for animal feed. Occupational contact dermatitis occurs in workers at animal feed mills, in veterinaries, or in health workers. Nonoccupational dermatitis mainly concerns patients with chronic dermatitis, leg ulcers, or chronic otitis. Cross-sensitivity is usual with other aminoglycosides (amikacin, arbekacin, butirosin, dibekacin, gentamicin, isepamicin, kanamycin, paromomycin, ribostamycin, sisomycin, tobramycin), is rare with netilmicin and streptomycin, but nonexistent with spectinomycin.

• 作用機序

  Neomycin has a wide spectrum of antibacterial action. It is effective against both a number of Gram-positive as well as Gram-negative microorganisms. However, it is able to bind with cholesterol and bile salts. In combination with other bile salt-reducing drugs or nicotinic acid, neomycin is able to block cholesterol and bile salt absorption, which significantly increases the level of cholesterol in the plasma.

• 薬物動態学

  C_{max 0.5 g intramuscular: 20 mg/L after 1 h
  Plasma half-life: 2–3 h
  Volume of distribution: 0.25–0.35 L/kg
  Plasma protein binding: Low
  Very little is absorbed after oral administration and more than 95% is eliminated unchanged in the feces. Peak plasma concentrations of less than 4 mg/L have been found after an oral dose of 3 g. Distribution and excretion resemble that of streptomycin, but the toxicity of neomycin precludes systemic administration except in the most extreme cases.}

• 臨床応用

  Superficial infections with staphylococci and Gram-negative bacilli (topical; alone or in combination with bacitracin, chlorhexidine or polymyxin)
  Treatment of staphylococcal nasal carriers (topical, in combination with chlorhexidine or bacitracin)
  Eye infections (topical; alone or in combination)
  Otitis externa (alone or with a corticosteroid)
  Gut decontamination before abdominal surgery (oral)
  Prophylaxis after urinary tract instrumentation (instillation)
  Use is discouraged because of the possibility of promoting the appearance of aminoglycoside-resistant strains, and because of the risk of absorption with the consequent danger of systemic toxicity or neuromuscular blockade.

• 副作用

  Neomycin is the most likely of all the aminoglycosides to damage the kidneys and the auditory branch of the eighth nerve. This has almost entirely restricted it to topical and oral use.
  Irreversible deafness may develop even if the drug is stopped at the first sign of damage. Loss of hearing may occur as a result of topical applications to wounds or other denuded areas, particularly if renal excretion is impaired. Instillation of ear drops containing neomycin can result in deafness. This generally develops in the second week of treatment and is usually reversible.
  Rashes have been described in 6–8% of patients treated topically and these patients may be rendered allergic to other aminoglycosides. Nausea and protracted diarrhea may follow oral administration. Sufficient drug may be absorbed from the gut on prolonged oral administration to produce deafness but not renal damage. Intestinal malabsorption and superinfection have been seen in patients receiving 4–9 g per day and may develop in patients receiving as little as 3 g of the drug per day. Precipitation of bile salts by the drug may impair the hydrolysis of long-chain triglycerides. Large doses instilled into the peritoneal cavity at operation may be absorbed, with resultant systemic toxicity, and patients concurrently exposed to anesthetics and muscle relaxants are liable to suffer neuromuscular blockade, which is reversible by neostigmine.

• 安全性プロファイル

  Poison by intraperitoneal, intravenous, and subcutaneous routes. Moderately toxic by ingestion. Human systemic effects: changes in hearing acuity, liver tubule changes, and decreased urine volume or anuria. Mutation data reported. When heated to decomposition it emits acrid smoke and irritating fumes.

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1404-04-2, ネオマイシン キーワード