ミノサイクリン

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

  H319：強い眼刺激

  H361：生殖能または胎児への悪影響のおそれの疑い

  H362：授乳中の子に害を及ぼすおそれ

• 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。

  P263：妊娠中/授乳期中は接触を避けること。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P281：指定された個人用保護具を使用すること。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  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。

  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。

ミノサイクリン 価格

MSDS Information

• Minocycline

ミノサイクリン 化学特性,用途語,生産方法

• 性質

  ミノサイクリンの作用機序は、細菌のリボソームサブユニットへ結合しタンパク質合成を阻害することです。動物のリボソームサブユニットへは結合しないため、細菌に静菌的かつ特異的に作用します。

  そのほか、リパーゼ活性抑制作用や白血球遊走抑制作用、活性酸素抑制作用があることから、尋常性ざ瘡 (ニキビ) に効果が期待できます。ミノサイクリンの発現頻度が高い副作用は、めまいと吐き気です。

  服用後の車の運転など、危険な動作は避けてください。他の重大な副作用として、血液障害、急性腎障害、ショック・アナフィラキシー、肝機能障害などがあります。特に肝機能障害は、大量投与で引き起こされる可能性が高いです。

  ただし、ミノサイクリンは肝臓で代謝される薬物です。そのため、腎機能に応じて投与量を減量する必要はありません。

• 解説

  ミノサイクリンとは、で示されるテトラサイクリン系抗生物質です。

  細菌内に入った後に、リボソームのサブユニット (30S) に結合し、 タンパク質合成を阻害します。

  黄色の結晶性粉末で、N,N-ジメチルホルムアミドやに溶けやすいですが、水やには溶けにくいです。

• 用法用量

  錠剤、注射剤共に、初回にミノサイクリンを100〜200mg投与したのち、12時間ごとあるいは24時間ごとに100mgを投与します。

  優先的に使用するのは錠剤です。経口摂取が不可能な場合や緊急の場合は、注射剤から開始して、経口摂取可能になった時点で錠剤に移行することが推奨されています。

• 効能

  抗生物質, タンパク質合成阻害薬

• 使用上の注意

  錠剤を服用する際は、多めの水で服用してください。錠剤が食道に停留し崩壊すると食道潰瘍を起こす恐れがあります。特に就寝直前の服用や、服用後すぐ横になる行為は避けてください。

  また、錠剤、注射剤に共通して、投与により尿が黄褐〜茶褐色、緑、青に変色した報告や甲状腺が黒色になった報告があります。

• 説明

  An important antibiotic produced by semisynthesis from demeclocycline is minocycline. It is much more lipophilic than its precursors, gives excellent blood levels following oral administration (90–100% available),and can be given once a day. Its absorption is lowered by approximately 20% when taken with food or milk. It is less dependent on active uptake mechanisms and has a somewhat broader antimicrobial spectrum. It also, apparently, is less painful on IM or IV injection, but it has vestibular toxicities (e.g., vertigo, ataxia, and nausea) not generally shared by other tetracyclines.

• 使用

  Minocycline is a semi-synthetic tetracycline prepared by sequential hydrogenolysis, nitration and reductive methylation. Minocycline, together with doxycycline, is regarded as a ‘third generation’ tetracycline largely replacing the natural products and pro-drugs produced in the early 1950s for mainstream antibiotic applications. Like all tetracyclines, minocycline shows broad spectrum antibacterial and antiprotozoan activity and acts by binding to the 30S and 50S ribosomal sub-units, blocking protein synthesis. Minocycline has been extensively cited in the literature with over 5,000 references.

• 定義

  ChEBI: A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5.

• 適応症

  The tetracycline antibiotic minocycline (Minocin) is modestly effective in the treatment of rheumatoid arthritis and is generally well tolerated. Radiographic evidence of its efficacy as a DMARD is lacking, although clinical symptoms do abate. It can be useful in the treatment of early, mild disease.

• 世界保健機関（WHO）

  Minocycline, a semi-synthetic tetracycline derivative was introduced in 1967. It is used today in the treatment of bacterial, rickettsial and amoebic infections. Symptoms described as dizziness or vertigo have been recognized in association with minocycline administration, however, these symptoms are usually not severe. Minocycline is registered in many countries and the World Health Organization is not aware that registration has been refused elsewhere.

• 抗菌性

  It exhibits the broad-spectrum activity typical of the group, but retains activity against some strains of Staph. aureus resistant to older tetracyclines. It is active against β-hemolytic streptococci and some tetracycline- resistant pneumococci. It is also active against some enterobacteria resistant to other tetracyclines, probably because some Gram-negative efflux pumps remove minocycline less effectively than other tetracyclines. Some strains of H. influenzae resistant to other tetracyclines are susceptible. Sten. maltophilia is susceptible, as are most strains of Acinetobacter spp. and L. pneumophila.
  It is notable for its activity against Bacteroides and Fusobacterium spp., and is more active than other tetracyclines against C. trachomatis, brucellae and nocardiae. It inhibits Mycobacterium tuberculosis, M. bovis, M. kansasii and M. intracellulare at 5–6 mg/L. Candida albicans and C. tropicalis are also slightly susceptible.

• 併用する際の注意点

  錠剤を服用する際、カルシウム、マグネシウム、アルミニウム、ランタン、鉄などの金属を含む食物との併用には注意が必要です。ミノサイクリンと上記の金属がキレートを形成し、ミノサイクリンの吸収が低下する恐れがあります。併用する場合は2〜4時間間隔をあけてください。

  錠剤と注射剤共通して挙げられる併用注意薬は、ワルファリンカリウムなどの抗凝血剤、SU系血糖降下剤、メトトレキサート、ポリフィマーナトリウム、ジゴキシン、経口避妊剤、ビタミンA製剤 (経口剤) です。

• 使用用途

  ミノサイクリンは、テトラサイクリン系抗生物質として幅広く医療の現場で使用されています。効果を示すのは、ブドウ球菌属、溶血性レンサ球菌、肺炎球菌などのグラム陽性細菌や、大腸菌、クレブシエラ属、エンテロバクター属などのグラム陰性細菌です。

  また、作用する部位が細胞壁ではないため、細胞壁を持たないリケッチア、クラミジアに対しても、抗菌作用を期待できます。ミノサイクリンの適応症は多岐にわたりますが、代表的なものは前立腺炎、肺炎、膀胱炎、外耳・中耳炎、尋常性ざ瘡などです。

  特に尋常性ざ瘡 (ニキビ) に関しては、日本皮膚科学会の「尋常性ざ瘡治療ガイドライン」にて推奨度Aの薬剤に分類されています。

• 応用例（製薬）

  A semisynthetic tetracycline derivative supplied as the hydrochloride for oral administration.

• 薬物動態学

  Oral absorption： 95–100%
  Cmax 150 mg oral： 4 mg/L after 2h
  300 mg oral： 2 mg/L after 2 h
  Plasma half-life： 12–24 h
  Volume of distribution： 80–115 L
  Plasma protein binding： 76%
  Absorption
  Food does not significantly affect absorption, which is depressed by co-administration with milk. It is chelated by metals and suffers the effects of antacids and ferrous sulfate common to tetracyclines. On a regimen of 100 mg every 12 h, steady-state concentrations ranged between 2.3 and 3.5 mg/L.
  Distribution
  The high lipophilicity of minocycline provides wide distribution and tissue concentrations that often exceed those of the plasma. The tissue:plasma ratio in maxillary sinus and tonsillar tissue is 1.6： that in lung is 3–4. Sputum concentrations may reach 37–60% of simultaneous plasma levels. In bile, liver and gallbladder the ratios are 38, 12 and 6.5, respectively.
  Prostatic and seminal fluid concentrations range from 40% to 100% of those of serum. CSF penetration is poor, especially in the non-inflamed state. Concentrations in tears and saliva are high, and may explain its beneficial effect in the treatment of meningococcal carriage.
  Metabolism
  Biotransformation to three microbiologically inactive metabolites occurs in the liver： the most abundant is 9-hydroxyminocycline.
  Excretion
  Only 4–9% of administered drug is excreted in the urine, and in renal failure elimination is little affected. Neither hemodialysis nor peritoneal dialysis affects drug elimination. Fecal excretion is relatively low and evidence for enterohepatic recirculation remains uncertain. Despite high hepatic excretion, dose accumulation does not occur in liver disease, such as cirrhosis. Type IIa and type IV hyperlipidemic patients show a decreased minocycline clearance of 50%, suggesting that dose modification may be necessary.

• 臨床応用

  There appear to be few situations in which it has a unique therapeutic advantage over other tetracyclines. Its use has been tempered by the high incidence of vestibular side effects.
  Although used in the long-term management of acne, the potential for skin pigmentation must be considered. Because of its high tissue concentrations, it may occasionally provide a useful alternative to other agents for the treatment of chronic prostatitis. It has a role in the treatment of sexually transmitted chlamydial infections.

• 副作用

  Minocycline shares the untoward reactions common to the group with gastrointestinal side effects being most common, and more prevalent in women. Diarrhea is relatively uncommon, presumably as a result of its lower fecal concentrations. Hypersensitivity reactions, including rashes, interstitial nephritis and pulmonary eosinophilia, are occasionally seen.
  Staining of the permanent dentition occurs with all tetracyclines; a side effect that appears to be unique to minocycline is that of tissue discoloration and skin pigmentation. Tissues that may become pigmented include the skin, skull and other bones and the thyroid gland, which at autopsy appears blackened. The pigmentation tends to resolve slowly with discontinuation of the drug and is related to the length of therapy.
  Three types of pigmentation have been identified:
  ? A brown macular discoloration (‘muddy skin syndrome’), which occurs in sun-exposed parts and is histologically associated with melanin deposition.
  ? Blue–black macular pigmentation occurring within inflamed areas and scars associated with hemosiderin deposition.
  ? Circumscribed macular blue–gray pigmented areas occurring in sun-exposed and unexposed skin, which appears to be linked to a breakdown product of minocycline.
  CNS toxicity has been prominent, notably benign intracranial hypertension, which resolves on discontinuation of the drug, and, more commonly, dizziness, ataxia, vertigo, tinnitus, nausea and vomiting, which appear to be more frequent in women. These primarily vestibular side effects have ranged in frequency from 4.5% to 86%. They partly coincide with plasma concentration peaks, but their exact pathogenesis has yet to be determined.

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