シタフロキサシン
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/12/20 23:37:36」(JST)
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Sitafloxacin
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Systematic (IUPAC) name |
7-[(4S)-4-Amino-6-azaspiro[2.4]heptan-6-yl]-8-chloro-6-fluoro-1-[(2S)-2-fluorocyclopropyl]-4-oxoquinoline-3-carboxylic acid |
Clinical data |
Pregnancy cat. |
? |
Legal status |
℞ Prescription only |
Routes |
Oral |
Identifiers |
CAS number |
127254-12-0 N |
ATC code |
J01MA21 |
PubChem |
CID 461399 |
ChemSpider |
405945 Y |
UNII |
3GJC60U4Q8 N |
ChEMBL |
CHEMBL108821 Y |
Chemical data |
Formula |
C19H18ClF2N3O3 |
Mol. mass |
409.81 |
SMILES
- F[C@H]5C[C@H]5N2/C=C(/C(=O)O)C(=O)c1cc(F)c(c(Cl)c12)N4C[C@@H](N)C3(CC3)C4
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InChI
-
InChI=1S/C19H18ClF2N3O3/c20-14-15-8(17(26)9(18(27)28)5-25(15)12-4-10(12)21)3-11(22)16(14)24-6-13(23)19(7-24)1-2-19/h3,5,10,12-13H,1-2,4,6-7,23H2,(H,27,28)/t10-,12+,13+/m0/s1 Y
Key:PNUZDKCDAWUEGK-CYZMBNFOSA-N Y
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N (what is this?) (verify) |
Sitafloxacin (INN; also called DU-6859a) is a fluoroquinolone antibiotic[1] that shows promise in the treatment of Buruli ulcer. The molecule was identified by Daiichi Sankyo Co., which brought ofloxacin and levofloxacin to the market. Sitafloxacin is currently marketed in Japan by Daiichi Sankyo under the tradename Gracevit.
Contents
- 1 See also
- 2 References
- 3 Further reading
- 4 External links
See also[edit]
- Adverse effects of fluoroquinolones
References[edit]
- ^ Anderson, DL. (Jul 2008). "Sitafloxacin hydrate for bacterial infections.". Drugs Today (Barc) 44 (7): 489–501. doi:10.1358/dot.2008.44.7.1219561. PMID 18806900.
Further reading[edit]
- Keating GM (April 2011). "Sitafloxacin: in bacterial infections". Drugs 71 (6): 731–44. doi:10.2165/11207380-000000000-00000. PMID 21504249.
External links[edit]
- (Japanese) Gracevit グレースビット (PDF) Daiichi Sankyo Co. January 2008.
Antibacterials: nucleic acid inhibitors (J01E, J01M)
|
|
Antifolates
(inhibits
purine metabolism,
thereby inhibiting
DNA and RNA synthesis) |
DHFR inhibitor |
- 2,4-Diaminopyrimidine
- Trimethoprim#
- Brodimoprim
- Tetroxoprim
- Iclaprim†
|
|
Sulfonamides
(DHPS inhibitor) |
Short-
acting |
- Sulfaisodimidine
- Sulfamethizole
- Sulfadimidine
- Sulfapyridine
- Sulfafurazole
- Sulfanilamide
- Sulfathiazole
- Sulfathiourea
|
|
Intermediate-
acting |
- Sulfamethoxazole
- Sulfadiazine#
- Sulfamoxole
|
|
Long-
acting |
- Sulfadimethoxine
- Sulfadoxine
- Sulfalene
- Sulfametomidine
- Sulfametoxydiazine
- Sulfamethoxypyridazine
- Sulfaperin
- Sulfamerazine
- Sulfaphenazole
- Sulfamazone
|
|
Other/ungrouped |
- Sulfacetamide
- Sulfadicramide
- Sulfametrole
|
|
|
Combinations |
- Trimethoprim/sulfamethoxazole#
|
|
|
Topoisomerase
inhibitors/
quinolones/
(inhibits
DNA replication) |
1st g. |
- Cinoxacin‡
- Flumequine
- Nalidixic acid
- Oxolinic acid
- Pipemidic acid
- Piromidic acid
- Rosoxacin
|
|
Fluoro-
quinolones |
2nd g. |
- Ciprofloxacin#
- Enoxacin‡
- Fleroxacin‡
- Lomefloxacin
- Nadifloxacin
- Ofloxacin
- Norfloxacin
- Pefloxacin
- Rufloxacin
|
|
3rd g. |
- Balofloxacin
- Grepafloxacin‡
- Levofloxacin
- Pazufloxacin
- Sparfloxacin‡
- Temafloxacin‡
- Tosufloxacin
|
|
4th g. |
- Besifloxacin
- Clinafloxacin†
- Garenoxacin
- Gemifloxacin
- Moxifloxacin
- Gatifloxacin‡
- Sitafloxacin
- Trovafloxacin‡/Alatrofloxacin‡
- Prulifloxacin
|
|
Vet. |
- Danofloxacin
- Difloxacin
- Enrofloxacin
- Ibafloxacin
- Marbofloxacin
- Orbifloxacin
- Pradofloxacin
- Sarafloxacin
|
|
Related (DG) |
- Aminocoumarins: Novobiocin
|
|
|
|
Anaerobic DNA
inhibitors |
Nitro- imidazole derivatives |
- Metronidazole#
- Tinidazole
- Ornidazole
|
|
Nitrofuran derivatives |
- Nitrofurantoin#
- Furazolidone‡
- Nifurtoinol
|
|
|
RNA synthesis |
Rifamycins/
RNA polymerase |
- Rifampicin#
- Rifabutin
- Rifapentine
- Rifaximin
|
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
gr+f/gr+a (t)/gr-p (c)/gr-o
|
drug (J1p, w, n, m, vacc)
|
|
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English Journal
- Nationwide surveillance of the antimicrobial susceptibility of Chlamydia trachomatis from male urethritis in Japan.
- Takahashi S1, Hamasuna R2, Yasuda M3, Ishikawa K4, Hayami H5, Uehara S6, Yamamoto S7, Minamitani S8, Kadota J9, Iwata S9, Kaku M9, Watanabe A9, Sato J9, Hanaki H10, Masumori N11, Kiyota H12, Egawa S13, Tanaka K14, Arakawa S14, Fujisawa M14, Kumon H15, Wada K15, Kobayashi K16, Matsubara A16, Matsumoto T17, Eto M18, Tatsugami K18, Kuroiwa K18, Ito K19, Hosobe T20, Hirayama H21, Narita H22, Yamaguchi T23, Ito S24, Sumii T25, Kawai S26, Kanokogi M27, Kawano H28, Chokyu H29, Uno S30, Monden K31, Kaji S32, Kawahara M33, Takayama K34, Ito M35, Yoshioka M36, Kano M37, Konishi T37, Kadena H38, Nishi S39, Nishimura H40, Yamauchi T41, Maeda S42, Horie M43, Ihara H44, Matsumura M45, Shirane T46, Takeyama K47, Akiyama K48, Takahashi K49, Ikuyama T50, Inatomi H51, Yoh M52.
- Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy.J Infect Chemother.2016 Sep;22(9):581-6. doi: 10.1016/j.jiac.2016.06.010. Epub 2016 Jul 21.
- Genital chlamydial infection is a principal sexually transmitted infection worldwide. Chlamydia trachomatis can cause male urethritis, acute epididymitis, cervicitis, and pelvic inflammatory disease as sexually transmitted infections. Fortunately, homotypic resistant C. trachomatis strains have not
- PMID 27452428
- Efficacy of 10-day Sitafloxacin-Containing Third-Line Rescue Therapies for Helicobacter pylori Strains Containing the gyrA Mutation.
- Mori H1, Suzuki H2, Matsuzaki J1, Tsugawa H3, Fukuhara S1, Miyoshi S1, Hirata K1, Seino T1, Matsushita M1, Masaoka T1, Kanai T1.
- Helicobacter.Helicobacter.2016 Aug;21(4):286-94. doi: 10.1111/hel.12286. Epub 2015 Nov 27.
- BACKGROUND AND AIM: Sitafloxacin-containing Helicobacter pylori eradication therapy is a promising third-line therapeutic approach, but there is no previous studies between gyrA mutation status of H. pylori strains and the efficacy of 10-day sitafloxacin-containing regimens. Here, we assessed the ef
- PMID 26612407
- Four-times-daily Dosing of Rabeprazole with Sitafloxacin, High-Dose Amoxicillin, or Both for Metronidazole-Resistant Infection with Helicobacter pylori in Japan.
- Sugimoto M1,2, Sahara S2, Ichikawa H2, Kagami T2, Ban H1, Otsuka T3, Andoh A3, Furuta T4.
- Helicobacter.Helicobacter.2016 May 23. doi: 10.1111/hel.12319. [Epub ahead of print]
- BACKGROUND: The bacterial resistance of Helicobacter pylori to antimicrobial agents such as clarithromycin and metronidazole has been increasing worldwide, leading to the failure of eradication treatment. Here, we present an eradication regimen consisting of four-times-daily dosing (q.i.d.) of rabep
- PMID 27213463
Japanese Journal
- DC-159a Shows Inhibitory Activity against DNA Gyrases of Mycobacterium leprae
- Preliminary Evaluation of a Sitafloxacin-Containing Regimen for Relapsed or Refractory PulmonaryMycobacterium aviumComplex Disease
- Sitafloxacinに対する非定型菌(2009年~2014年分離株)の感受性調査結果および2009年,2012年に分離された一般細菌の感受性推移の検討
Related Links
- 特長. 呼吸器感染症、耳鼻咽喉科領域感染症、尿路感染症、性感染症、歯科・口腔外科領域感染症の主要原因菌に適した抗菌スペクトルと優れた抗菌活性を示した(in vitro)。. ヒト血清中濃度シミュレーションモデルで優れた殺菌力を示した(in vitro)。. 標的酵素であるDNA ジャイレース、トポイソメラーゼⅣの両方に優れた阻害活性を示した(in vitro)。. 肺炎球菌 ...
- YJコード. 薬価. 規制区分. シタフロキサシン錠50mg「サワイ」 (後発品) SITAFLOXACIN. 沢井製薬. 6241018F1035. 75.3円/錠. 処方箋医薬品.
- 洋名:Sitafloxacin Hydrate 製造販売承認年月日 薬価基準収載 ・発売年月日 製造販売承認年月日: 2017年8月15日 薬価基準収載年月日: 2017年12月8日 発 売 年 月 日: 2018年1月10日 開発・製造
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★リンクテーブル★
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- 英
- sitafloxacin
- 化
- シタフロキサシン水和物 sitafloxacin hydrate
- 商
- グレースビット
- 関
- [合成抗菌剤]]。抗菌薬