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Ofloxacin Produkt Beschreibung

Ofloxacin Struktur
82419-36-1
CAS-Nr.
82419-36-1
Englisch Name:
Ofloxacin
Synonyma:
oflx;pt01;Oflox;floxin;hoe280;Exocin;Floxil;Floxal;Visren;oflocet
CBNumber:
CB7103599
Summenformel:
C18H20FN3O4
Molgewicht:
361.37
MOL-Datei:
82419-36-1.mol

Ofloxacin Eigenschaften

Schmelzpunkt:
270-2750C
Dichte
1.2688 (estimate)
storage temp. 
2-8°C
Löslichkeit
1 M NaOH: soluble50mg/mL
Aggregatzustand
neat
Wasserlöslichkeit
Soluble in acetic acid or water. Slightly soluble in methanol
maximale Wellenlänge (λmax)
326nm(H2O)(lit.)
Merck 
14,6771
CAS Datenbank
82419-36-1(CAS DataBase Reference)
EPA chemische Informationen
7H-Pyrido[1,2,3- de]-1,4-benzoxazine-6-carboxylic acid, 9-fluoro-2,3-dihydro-3-methyl- 10-(4-methyl-1-piperazinyl)- 7-oxo-(82419-36-1)
Sicherheit
  • Risiko- und Sicherheitserklärung
  • Gefahreninformationscode (GHS)
Kennzeichnung gefährlicher Xn,Xi
R-Sätze: 22-42/43-68-36/37/38
S-Sätze: 26-36/37/39-24/25-22-37/39-60
WGK Germany  3
RTECS-Nr. UU8815550
HS Code  29349990
Toxizität LD50 in male, female mice, male, female rats (mg/kg): 5450, 5290, 3590, 3750 orally; 208, 233, 273, 276 i.v.; >10000, >10000, 7070, 9000 s.c. (Ohno)
Bildanzeige (GHS)
Alarmwort
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H303 May be harmfulif swallowed Acute toxicity,oral Category 5 P312
Sicherheit

Ofloxacin Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:

R22:Gesundheitsschädlich beim Verschlucken.
R42/43:Sensibilisierung durch Einatmen und Hautkontakt möglich.
R68:Irreversibler Schaden möglich.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.

S-Sätze Betriebsanweisung:

S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
S22:Staub nicht einatmen.
S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.

Beschreibung

Ofloxacin is an antibacterial agent with increased potency in comparison to the prototype third generation quinolone, norfloxacin. It has a broad spectrum of activity against gram-positive and gram-negative bacteria and is useful in the treatment of kidney, genitourinary, and upper respiratory tract infections.

Chemische Eigenschaften

Off-White Solid

Originator

Daiichi Seiyaku (Japan)

Verwenden

Fluorinated quinolone antibacterial

Definition

ChEBI: An oxazinoquinolone carrying carboxy, fluoro, methyl and 4-methylpiperazino substituents. A synthetic fluoroquinolone antibacterial agent, it inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.

Trademarks

Floxin (Ortho-McNeil); Floxin (Daiichi Pharmaceutical); Ocuflox (Allergan);TARIVID.

Antimicrobial activity

It exhibits good activity against a wide range of enterobacteria, including strains resistant to nalidixic acid, as well as against Aeromonas, Campylobacter, Vibrio and Moraxella spp. Activity against methicillin-sensitive Staph. aureus is good, but streptococci, including Str. pneumoniae and enterococci, are less susceptible. Most anaerobes are moderately or completely resistant. It is active against L. pneumophila, Ch. pneumoniae, C. trachomatis, mycoplasmas, ureaplasmas and M. tuberculosis. Other mycobacteria such as M. fortuitum, M. kansasii, M. chelonei and the M. avium complex are moderately susceptible.

Pharmazeutische Anwendungen

A tricyclic 6-fluoro, 7-piperazinyl quinoline with a methyl substituted oxazine ring substituted. It is a racemic mixture of l- (levofloxacin, see p. 319) and d-isomers.

Biotechnological Applications

Ofloxacin is a fluoroquinolone antibiotic present as a racemic mixture. Levofloxacin, S-isomer of ofloxacin, shows a broad spectrum of antibacterial activity against both gram-positive and gram-negative bacteria. The antibacterial activity of levofloxacin is 8–128 times greater than that of the corresponding R-isomer. A novel esterase of type B1 carboxylesterase/lipase family from a marine isolate Y. lipolytica CL180 was used to resolve a racemic mixture of ofloxacin ester. This esterase showed an enantioselectivity toward R, S-ofloxacin ester, and levofloxacin was produced with an enantiomeric excess of 52 % (Kim et al. 2007).

Pharmakokinetik

Oral absorption: c. 95%
Cmax400 mg oral: 3–5 mg/L after 1–1.5 h
200 mg intravenous (30-min infusion): 1.8 mg/L 1 h after end infusion
Plasma half-life: 5–7 h
Volume of distribution: 1–2.5 L/kg
Plasma protein binding: c. 25%
absorption and distribution
There is no significant interference with absorption by magnesium–aluminum hydroxide or calcium carbonate compounds,providing administration is separated by at least 2 h. In patients receiving repeated 200 mg doses, the mean peak plasma concentration rose from 2.7 mg/L after the first dose to 3.4 mg/L after the seventh.
It is widely distributed, achieving levels ≥50% of simultaneous plasma concentrations in many tissues, including lung and bronchial secretions. In cantharides and suction blisters, peak concentrations exceed those in plasma, while the elimination half-life is similar. In patients with non-inflamed meninges, 200 mg administered orally or by intravenous infusion over 30 min produced CSF concentrations of around 0.4–1 mg/L at 2–4 h while the plasma concentration was 1.7–4 mg/L: a 400 mg intravenous infusion yielded a CSF concentration of 2 mg/L, which is adequate for some Gram-negative bacteria, but not for Gram-positive bacteria or Ps. aeruginosa.
Metabolism and excretion
It is poorly metabolized into desmethyl and N-oxide derivatives (<5% of the administered dose), only about 20% of a dose being eliminated by non-renal routes. There is a very slight effect on cytochrome P450-related isoenzymes and no significant effect on the metabolism of theophylline in dosages of up to 800 mg.
About 60% of a dose appears in the urine over 12 h and 80–90% over 48 h. The apparent elimination half-life is prolonged in renal failure, reaching 30–50 h in anuria, necessitating a dosage reduction. The desmethyl metabolite accumulates in all patients and the N-oxide in 50%. Absorption and distribution are not affected by renal failure. Significant amounts of the drug appear in the feces, producing very variable concentrations up to 100 mg/kg.

Clinical Use

9-Fluoro-2,3-dihydro-3-methyl-10(4-methyl-1-piperazin-yl)-7-oxo-7H-pyrido[1,2,3-de]-1,4,-benzoxazine-6-carboxylicacid (Floxin, Floxin IV) is a member of the quinolone class of antibacterial drugs wherein the 1- and 8-positions are joined in the form of a 1,4-oxazine ring.
Ofloxacin has been approved for the treatment of infectionsof the lower respiratory tract, including chronic bronchitisand pneumonia, caused by Gram-negative bacilli. It isalso used for the treatment of pelvic inflammatory diseaseand is highly active against both gonococci and chlamydia.In common with other fluoroquinolones, ofloxacin is not effectivein the treatment of syphilis. A single 400-mg oraldose of ofloxacin in combination with the tetracycline antibioticdoxycycline is recommended by the Centers forDisease Control and Prevention (CDC) for the outpatienttreatment of acute gonococcal urethritis. Ofloxacin is alsoused for the treatment of urinary tract infections caused byGram-negative bacilli and for prostatitis caused by E. coli.Infections of the skin and soft tissues caused by staphylococci,streptococci, and Gram-negative bacilli may also betreated with ofloxacin.

Clinical Use

Complicated and uncomplicated infections of the urinary tract, chronic prostatitis
Uncomplicated urogenital and anorectal gonorrhea (single-dose), chancroid (3-day course), genital chlamydial infections (7-day course) Lower respiratory tract infections, including bronchopneumonia, community-acquired pneumonia (except pneumococcal pneumonia), acute bacterial exacerbations of chronic bronchitis (unless pneumococci are involved) and bronchiectasis
Enteric fever, including the chronic carrier state; gastroenteritis caused by enterotoxigenic Escherichia coli, Salmonella, Shigella and Campylobacter spp. Ocular infections (ophthalmic preparation)

Nebenwirkungen

Untoward reactions havebeen described in 2.5–7.5% of patients, and are those common to the group: gastrointestinal tract disturbances, rashes, tendon rupture and insomnia. CNS effects rarely occur.

Ofloxacin Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Ofloxacin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 322)Lieferanten
Firmenname Telefon Fax E-Mail Land Produktkatalog Edge Rate
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21696 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20672 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32447 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2543 55
Hubei XinRunde Chemical Co., Ltd.
+8615102730682; +8618874586545
02783214688 bruce@xrdchem.cn CHINA 535 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30001 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 sales@jushengtech.com CHINA 28236 58
QUALITY CONTROL CHEMICALS INC.
(323) 306-3136
(626) 453-0409 orders@qcchemical.com United States 8407 58
Xiamen AmoyChem Co., Ltd
+86 592-605 1114
sales@amoychem.com CHINA 6372 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20115 58

82419-36-1()Verwandte Suche:


  • (+-)-ethyl-10-(4-methyl-1-piperazinyl)-7-oxo
  • dl-8280
  • hoe280
  • oflocet
  • ofloxacine
  • orf18489
  • oxaldin
  • pt01
  • (+/-)-9-fluoro-2, 3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
  • AKOS NCG1-0050
  • floxin
  • oflx
  • OFLOXACIN
  • (-)-(s)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazin-yl)-7-oxo-7h-pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid
  • TARIVID
  • (+/-)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid
  • 9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
  • OFLOXACIN HCL
  • OFLOXACIN USP 24
  • OFLOXACINE USP 23
  • Ofloxaxacin
  • OFLOXACIN USP
  • Ofloxacin, Vetranal
  • OFLOXACIN EP USP
  • OfloxacinUsp26
  • Exocin
  • Flobacin
  • Floxil
  • Monoflocet
  • Ocuflox
  • OFLOXACIN(SUBJECTTOPATENTFREE)
  • 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo- (9CI)
  • 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-, (+-)-
  • 9-Fluoro-2,3-dihydro-3-methyl-10-(N-methylpiperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
  • Floxal
  • Oflocin
  • Oflox
  • Visiren
  • Visren
  • Tariferid
  • (+/-)-Ofloxacin
  • Floxin Exocin
  • Oflocet:Oflocin
  • Tarivid:Visiren
  • 7H-Pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid, 2,3-dihydro-9-fluoro-3-methyl-10- (4-methyl-1-piperazinyl)-7-oxo-, (+-)
  • 9-Fluoro-2,3-dihydro-3-methyl-10-(4-methylpiperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
  • HOF-280
  • 3-Methyl-7-oxo-9-fluoro-10-(4-methyl-1-piperazinyl)-2,3-dihydro-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
  • Ofloxacin (200 mg)
  • Ooxacin (200 mg)
  • Ofloxacin (COS)
  • (2S)-7-fluoro-2-Methyl-6-(4-Methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.0^{5,13}]trideca-5,7,9(13),11-tetraene-11-carboxylic acid
  • Ofloxacin API
  • Levofloxacin , Cravit Tablets
  • Ofloxacin (DL8280)
  • Levofloxacin Mesglate
  • 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid
  • 9-Fluoro-3,7-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic Acid
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