Sitafloxacin

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H302：삼키면 유해함

  H315：피부에 자극을 일으킴

  H319：눈에 심한 자극을 일으킴

  H335：호흡 자극성을 일으킬 수 있음

• 예방조치문구

  P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P270：이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.

  P271：옥외 또는 환기가 잘 되는 곳에서만 취급하시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P301+P312：삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

  P302+P352：피부에 묻으면 다량의 물로 씻으시오.

  P304+P340：흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.

  P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

  P330：입을 씻어내시오.

  P332+P313：피부 자극이 생기면 의학적인 조치· 조언을 구하시오.

  P337+P313：눈에 대한 자극이 지속되면 의학적인 조치· 조언를 구하시오.

  P362：오염된 의복을 벗고 세척 후에 재사용하기

  P403+P233：용기는 환기가 잘 되는 곳에 단단히 밀폐하여 저장하시오.

  P405：밀봉하여 저장하시오.

  P501：...에 내용물 / 용기를 폐기 하시오.

Sitafloxacin 화학적 특성, 용도, 생산

• 개요

  Sitafloxacin hydrate is the newest member (fourth generation) of the fluoroquinolone family of antibiotics that exhibits broad spectrum activity against many Gram-positive, Gramnegative, and anaerobic clinical isolates, including strains resistant to other fluoroquinolones. Since the launch of the first fluoroquinolone norfloxacin (patented in 1978), 20 other versions have made it to market with ciprofloxacin and levofloxacin experiencing the most prevalent usage. The mechanism of action involves inhibition of bacterial type II topoisomerases, both DNA gyrase and topoisomerase IV. By inhibiting these enzymes and preventing DNA supercoiling, cell division is disrupted leading to cell death. In Gram-negative bacteria, the primary target appears to be gyrase, whereas topoisomerase IV is involved in Gram-positive bacteria. Dual inhibition is attractive for widespread activity and avoidance of resistance as both encoding genes would have to acquire mutations.

• 용도

  Antibacterial (DNA-gyrase inhibitor).

• Pharmaceutical Applications

  A group 4 quinolone formulated for oral or intravenous use. In-vitro activity is similar to or better than that of moxifloxacin. The antibacterial spectrum covers Gram-positive and Gram-negative bacteria including anaerobes. It has a chlorine atom at the C-8 position, and therefore has potential for phototoxicity. Early interest in this compound has not been maintained, but it is available in Japan.

• 부작용

  As a class, the major adverse events for fluoroquinolones are cardiac arrhythmia (due to QT interval 622 Shridhar Hegde and Michelle Schmidt prolongation), major phototoxicity, CNS disturbances (seizures, dizziness, and headaches), and tendonitis. The GI side effects, common to most antimicrobials, include Clostridium difficile-associated diarrhea (CDAD) and alterations in glucose homeostasis. From the clinical safety profile of sitafloxacin (1,059 patients receiving either 50 mg b.i.d. or 100 mg b.i.d.), about a third of patients experienced an adverse event with the most common being diarrhea, liver enzyme elevations, and headaches; however, the risk of QT prolongation, hypoglycemia, and hepatotoxicity were all considered to be low. Phototoxicity appears to be the limiting toxicity, particularly in non-Asian patients.

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