格帕沙星

维基百科中的醫學内容仅供参考，並不能視作專業意見。如需獲取醫療幫助或意見，请咨询专业人士。詳見醫學聲明。
格帕沙星
臨床資料
AHFS/Drugs.comMultum消费者信息
ATC碼
藥物動力學數據
血漿蛋白結合率50%
识别信息
  • (RS)-1-Cyclopropyl-6-fluoro-5-methyl-7-(3-methylpiperazin-1-yl)-4-oxo-quinoline-3-carboxylic acid
CAS号119914-60-2  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.159.692 編輯維基數據鏈接
化学信息
化学式C19H22FN3O3
摩尔质量359.40 g·mol−1
3D模型（JSmol（英语：JSmol））
手性外消旋混合物
  • O=C(O)\C2=C\N(c1cc(c(F)c(c1C2=O)C)N3CC(NCC3)C)C4CC4
  • InChI=1S/C19H22FN3O3/c1-10-8-22(6-5-21-10)15-7-14-16(11(2)17(15)20)18(24)13(19(25)26)9-23(14)12-3-4-12/h7,9-10,12,21H,3-6,8H2,1-2H3,(H,25,26) checkY
  • Key:AIJTTZAVMXIJGM-UHFFFAOYSA-N checkY

格帕沙星（Grepafloxacin）是一种喹诺酮类抗生素，用于治疗多种细菌感染[1][2]。包括流感嗜血杆菌、肺炎链球菌或卡他莫拉菌敏感菌株引起的轻度至中度感染[1]。

格帕沙星的常见的副作用包括过敏反应、心律不齐、昏厥、癫痫发作、幻觉、肝损伤、肌肉或关节疼痛[2]。

格列帕沙星于1999年在全球范围内撤出市场，因它延长心电图上的QT间期，导致心脏事件和猝死[1]。

临床用途

格帕沙星用于治疗敏感菌（如流感嗜血杆菌、肺炎链球菌、卡他莫拉菌）引起的慢性支气管炎加重[3]、社区获得性肺炎（除上述细菌外，还包括由肺炎支原体）[4]、淋病和非淋菌性尿道炎和宫颈炎（如沙眼衣原体或解脲脲原体引起）的急性加重[5]。

抗菌谱

格帕沙星具有高组织渗透率和广谱抗菌活性，对革兰氏阳性菌尤其是肺炎链球菌具有更高的活性[6]。格帕沙星对肺炎链球菌的活性似乎始终比环丙沙星高出至少4倍。 同样，格帕沙星对肺炎支原体的活性是环丙沙星的8倍[6]。

有代表性的研究表明，格帕沙星对潜在的呼吸道病原体具有与环丙沙星（Ciprofloxacin）相似或更高的体外活性[6]格帕沙星对肠杆菌科细菌的体外活性与环丙沙星相似或略低，但对大多数革兰氏阳性菌的体外活性优于环丙沙星。[6]。格帕沙星对眼生殖病原体沙眼衣原体的体外活性似乎大于环丙沙星[6]，对淋病奈瑟菌的活性似乎与环丙沙星相似[6]，而在体外对厌氧微生物的活性似乎略高于环丙沙星[6]。

一项调查肠杆菌科和葡萄球菌临床分离株交叉耐药性的研究表明，与环丙沙星相比，随着对环丙沙星耐药性的增加，格列帕沙星的相对效力增加[6]。研究表明，某些葡萄球菌耐药机制对格帕沙星的影响可能比环丙沙星更大[6]。

相互作用

在动物研究中，当以高剂量与非甾体抗炎药（NSAIDs）联合使用时，格帕沙星不会引起惊厥。[6]

作用机制

格帕沙星通过抑制细菌拓扑异构酶II（DNA旋转酶）和拓扑异构酶IV发挥其抗菌活性，这些酶是细菌DNA复制、转录和修复的必需酶。[1]

药代动力学

动物研究表明，格帕沙星几乎分布于除中枢神经系统以外的所有组织，口服 10 至 40 mg/kg 后对肺组织的渗透率特别高。[6]

参见

参考文献

  1. ^ 1.0 1.1 1.2 1.3 Grepafloxacin: Uses, Interactions, Mechanism of Action. DrugBank Online. [2022-06-20]. （原始内容存档于2017-07-11） （加拿大英语）. 
  2. ^ 2.0 2.1 Grepafloxacin Uses, Side Effects & Warnings. Drugs.com. [2022-06-20]. （原始内容存档于2022-06-30） （美国英语）. 
  3. ^ Chodosh, S.; Lakshminarayan, S.; Swarz, H.; Breisch, S. Efficacy and safety of a 10-day course of 400 or 600 milligrams of grepafloxacin once daily for treatment of acute bacterial exacerbations of chronic bronchitis: comparison with a 10-day course of 500 milligrams of ciprofloxacin twice daily. Antimicrobial Agents and Chemotherapy. 1998-01, 42 (1) [2022-06-20]. ISSN 0066-4804. PMID 9449270. doi:10.1128/AAC.42.1.114. （原始内容存档于2022-06-23）. 
  4. ^ O'Doherty, B.; Dutchman, D. A.; Pettit, R.; Maroli, A. Randomized, double-blind, comparative study of grepafloxacin and amoxycillin in the treatment of patients with community-acquired pneumonia. The Journal of Antimicrobial Chemotherapy. 1997-12,. 40 Suppl A [2022-06-20]. ISSN 0305-7453. PMID 9484876. doi:10.1093/jac/40.suppl_1.73. （原始内容存档于2022-06-20）. 
  5. ^ Ridgway, G. L.; Salman, H.; Robbins, M. J.; Dencer, C.; Felmingham, D. The in-vitro activity of grepafloxacin against Chlamydia spp., Mycoplasma spp., Ureaplasma urealyticum and Legionella spp. The Journal of Antimicrobial Chemotherapy. 1997-12,. 40 Suppl A [2022-06-20]. ISSN 0305-7453. PMID 9484871. doi:10.1093/jac/40.suppl_1.31. （原始内容存档于2022-06-20）. 
  6. ^ 6.00 6.01 6.02 6.03 6.04 6.05 6.06 6.07 6.08 6.09 6.10 Wagstaff, A. J.; Balfour, J. A. Grepafloxacin. Drugs. 1997-05, 53 (5) [2022-06-22]. ISSN 0012-6667. PMID 9129868. doi:10.2165/00003495-199753050-00007. （原始内容存档于2022-06-22）. 

Read other articles:

Limelight (grup musik)

LimeLightLimeLight pada Februari 2023 Dari kiri ke kanan: Gaeun, Suhye, dan MiUInformasi latar belakangAsalSeoul, Korea SelatanGenreK-poppop bubblegumpop dansapop remajaTahun aktif2022 (2022)–presentLabel143 EntertainmentAnggota MiU Suhye Gaeun Limelight (grup musik) Nama Jepang Hiragana: らいむらいと Katakana: ライムライト Alih aksara - Revisi: Raimuraito - Kunrei-shiki: Raimuraito Nama Korea Hangul: 라임라잇 Alih aksara - Romanisasi: Raimrait - McCune-Reischauer: Raim...

 

Calvert Watkins

American linguist and philologist Calvert WatkinsBorn(1933-03-13)March 13, 1933Pittsburgh, Pennsylvania, United StatesDiedMarch 20, 2013(2013-03-20) (aged 80)Los Angeles, California, United StatesTitleVictor S. Thomas Professor of Linguistics and ClassicsSpouses Jane Williams Cushman (married 1961) Stephanie Jamison (married 1980) ChildrenCynthia Watkins, David Cushman, Catherine Cushman, and Nicholas WatkinsAwards Guggenheim Fellowship Goodwin Award Academic backgroundEducationHarvard U...

 

2018 North Carolina's 9th congressional district election

Uncertified election 2018 North Carolina's 9th congressional district election ← 2016 November 6, 2018 2019 (special) →   Candidate Mark Harris Dan McCready Party Republican Democratic Popular vote 139,246 138,341 Percentage 49.25% 48.93% U.S. Representative before election Robert Pittenger Republican Elected U.S. Representative Election results annulled Elections in North Carolina Federal government U.S. President 1792 1796 1800 1804 1808 1812 1816 1820 1824 1...

Newton Commonwealth Golf Course

Massachusetts public golf course This article relies excessively on references to primary sources. Please improve this article by adding secondary or tertiary sources. Find sources: Newton Commonwealth Golf Course – news · newspapers · books · scholar · JSTOR (March 2014) (Learn how and when to remove this template message) Golf course with view towards Boston Pond on the course The Newton Commonwealth Golf Course is an 18-hole public golf course locat...

 

أمينتايو

أمينتايو   تقسيم إداري البلد اليونان  [1] خصائص جغرافية إحداثيات 40°41′23″N 21°40′47″E / 40.689722222222°N 21.679722222222°E / 40.689722222222; 21.679722222222   الارتفاع 589 متر  السكان التعداد السكاني 3779 (resident population of Greece) (2021)3856 (resident population of Greece) (2001)3205 (resident population of Greece) (1991)3671 (resident popu...

 

Vtáčkovce

Košice-okolie District in the Kosice Region Vtáčkovce (Slovak pronunciation: [ˈftaːtʂkɔwtse]; Hungarian: Patacskő) is a village and municipality in Košice-okolie District in the Kosice Region of eastern Slovakia. History In historical records the village was first mentioned in 1427. Geography The village lies at an altitude of 400 metres and covers an area of 3.25 km². It has a population of over 800 people with almost 100 new inhabitants since December 2004. External l...

XIX век

2-е тысячелетие XVII век XVIII век XIX век XX век XXI век 1790-е 1790 1791 1792 1793 1794 1795 1796 1797 1798 1799 1800-е 1800 1801 1802 1803 1804 1805 1806 1807 1808 1809 1810-е 1810 1811 1812 1813 1814 1815 1816 1817 1818 1819 1820-е 1820 1821 1822 1823 1824 1825 1826 1827 1828 1829 1830-е 1830 1831 1832 1833 1834 1835 1836 1837 1838 1839 1840-е 1840 1841 1842 1843 1844 1845 1846 1847 1848 1849 1850-е 1850 1851 1852 1853 1854 ...

 

Pierre Tendean

Ini adalah nama Minahasa, marganya adalah Tendean. Untuk halte busway, lihat Halte Transjakarta Tendean Kapten Czi. (Anumerta)Pierre TendeanTendean, c. 1963 Informasi pribadiLahir(1939-02-21)21 Februari 1939Batavia, Hindia BelandaMeninggal1 Oktober 1965(1965-10-01) (umur 26)Jakarta, Lubang BuayaSebab kematianDisiksa lalu dibunuh di Lubang Buaya, Jakarta, IndonesiaHubunganMitzi Tendean (kakak)Rooswidiati Tendean (adik) Rukmini Chamim (kekasih)Orang tuaAurelius Lammert Tendean (ayah)M...

 

Послание к Титу

Послание к Титудр.-греч. Ἐπιστολή πρὸς Τίτον Раздел Новый завет Название на других языках: лат. Epistula ad Titum; Язык оригинала древнегреческий (койне) Автор (церковное предание) апостол Павел Предыдущая (православие) Второе послание к Тимофею Следующая Послание к Филимону �...

Zwinger (Dresda)

ZwingerLocalizzazioneStato Germania LandSassonia LocalitàDresda IndirizzoSophienstraße, 01067 Dresden Coordinate51°03′11″N 13°44′02″E / 51.053056°N 13.733889°E51.053056; 13.733889Coordinate: 51°03′11″N 13°44′02″E / 51.053056°N 13.733889°E51.053056; 13.733889 Informazioni generaliCondizioniIn uso Costruzione1710-1728 StileBarocco, neorinascimentale RealizzazioneArchitettoMatthäus Daniel Pöppelmann ProprietarioAugusto II di Poloni...

 

Edith May (barge)

Historic British sailing vessel Edith May on the River Medway near Chatham History United Kingdom NameEdith May OwnerWilliam Barrett OperatorWilliam Barrett BuilderJohn and Herbert Cann (Harwich)[1] Commissioned1906 Decommissioned1952 StatusPrivate use and private charter ship General characteristics Tonnage125 Length86 ft (26 m) Beam20.75 ft (6.32 m) Height0 ft (0 m) to top of mainmast Draught4 ft (1.2 m) distance between the waterline and the ...

 

2018 in Vietnam

List of events ← 2017 2016 2015 2018 in Vietnam → 2019 2020 2021 Decades: 1990s 2000s 2010s 2020s See also: Other events of 2018 History of Vietnam Timeline of Vietnamese history List of years in Vietnam Events in the year 2018 in Vietnam. Incumbents Party General Secretary: Nguyễn Phú Trọng President: Trần Đại Quang (until 21 September), Nguyễn Phú Trọng (since 23 October) Prime Minister: Nguyễn Xuân Phúc Assembly Chairperson: Nguyễn Thị Kim Ngân Events 23...

DJ Yella

American hip hop musician DJ YellaCarraby in 2015Background informationBirth nameAntoine CarrabyAlso known asYella, YellaboyBorn (1961-12-11) December 11, 1961 (age 62)Compton, California, U.S.GenresHip hop, gangsta rapOccupation(s)DJ, rapper, record producer, film directorInstrument(s)Turntables, keyboards, drums, vocalsYears active1984–1996, 2009, 2016Websitedjyellaofnwa.comMusical artist Antoine Carraby (born December 11, 1961), known professionally as DJ Yella, is an American DJ, r...

 

Jigni State

Jigni Stateजिगनी रियासतPrincely State of British India1730–1950Jigni State in the Imperial Gazetteer of IndiaArea • 190157 km2 (22 sq mi)Population • 1901 3,838 History • Established 1730• Independence of India 1950 Succeeded by India Today part ofHamirpur district, Uttar Pradesh, India Jigni State was a princely state of the Bundelkhand Agency of the British Raj. It was a small Sanad state of about 82.87 ...

 

Mount Cook Airline

Mount Cook Airline IATA ICAO Kode panggil NM NZM MOUNTCOOK Didirikan1969Penghubung Bandar Udara Christchurch Bandar Udara Wellington Kota fokusRotorua, QueenstownProgram penumpang setiaAirpointsLounge bandaraKoru ClubAliansiStar AllianceArmada13Tujuan10Perusahaan indukAir New ZealandKantor pusatChristchurch, Selandia BaruTokoh utama Sarah Williamson GM of Mount Cook Bruce Parton GGM of Shorthaul Airlines Rob Fyfe (CEO) Situs webhttp://www.airnz.co.nz/ Mount Cook Airline adalah maskapai penerb...

X Congresso Olimpico

10° Congresso OlimpicoMichael Morris Killanin, promotore del X Congresso Olimpico TemaSport per un mondo di pace, Il futuro del movimento olimpico Partecipanti307 delegati Apertura30 settembre 1973 Chiusura4 ottobre 1973 Stato Bulgaria LocalitàPalazzo della cultura e dello sport, Varna IX Congresso Olimpico XI Congresso Olimpico Il X Congresso Olimpico venne organizzato dal Comitato Olimpico Internazionale dal 30 settembre al 4 ottobre 1973 a Varna, in Bulgaria. Indice 1 Sviluppo ...

 

Dewan Perwakilan Rakyat Daerah Kabupaten Lumajang

Dewan Perwakilan Rakyat Daerah Kabupaten LumajangDewan Perwakilan RakyatKabupaten Lumajang2019-2024JenisJenisUnikameral Jangka waktu5 tahunSejarahSesi baru dimulai21 Agustus 2019PimpinanKetuaEko Adis Prayoga, S.E. (PKB) sejak 20 Maret 2023 Wakil Ketua IH. Bukasan, S.Pd. M.M. (PDI-P) sejak 20 September 2019 Wakil Ketua IIHj. Oktafiyani, S.H. (Gerindra) sejak 20 September 2019 Wakil Ketua IIIH. Akhmat, S.T. (PPP) sejak 20 September 2019 KomposisiAnggota50Partai & kursi ...

 

Despenser's Crusade

14th-century military campaign Despenser's CrusadePart of the Hundred Years' War and the Western SchismMap of English conquests in France from 1360 to 1453, shown in pink and in yellow in FlandersDateDecember 1382 – September 1383LocationWestern FlandersResult Franco-Flemish victoryBelligerents Kingdom of England Ghent rebels Papal States Kingdom of France County of Flanders Avignon Papacy Commanders and leaders Bishop Henry le Despenser Frans Ackerman Pope Urban VI King Charles VI Count Lo...

Jardim Olinda

Questa voce sull'argomento centri abitati del Paraná è solo un abbozzo. Contribuisci a migliorarla secondo le convenzioni di Wikipedia. Jardim Olindacomune LocalizzazioneStato Brasile Stato federato Paraná MesoregioneNoroeste Paranaense MicroregioneParanavaí AmministrazioneSindacoJuraci Paes da Silva TerritorioCoordinate22°33′06″S 52°02′15″W22°33′06″S, 52°02′15″W (Jardim Olinda) Altitudine331 m s.l.m. Superficie128,51 km² Abitanti1 409...

 

Fångad av en stormvind

Cet article est une ébauche concernant une chanson, le Concours Eurovision de la chanson et la Suède. Vous pouvez partager vos connaissances en l’améliorant (comment ?) selon les recommandations des projets correspondants. Fångad av en stormvind Chanson de Carola auConcours Eurovision de la chanson 1991 Sortie 1991 Durée 3:00 Langue Suédois Auteur-compositeur Stephen Berg Classement 1re (146 points) Chansons représentant la Suède au Concours Eurovision de la chanson Som e...