Rosoxacin
(Synonyms: 罗索沙星,Acrosoxacin) 目录号 : GC38843Rosoxacin (Acrosoxacin)是一种有效且口服有效的喹诺酮类抗生素。Rosoxacin (Acrosoxacin) 具有广谱的抗菌活性,抑制革兰氏阴性菌,包括淋病奈瑟氏球菌(MIC90=0.03 mg/ml)。Rosoxacin (Acrosoxacin) 具有治疗尿路感染的潜力。
Cas No.:40034-42-2
Sample solution is provided at 25 µL, 10mM.
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Rosoxacin (Acrosoxacin) is a potent and orally active quinolone antibiotic. Rosoxacin (Acrosoxacin) has antibacterial activities against a broad spectrum of Gram negative bacteria including Neisseria gonorrhoeae (MIC90=0.03mg/ml). Rosoxacin has the potential for urinary tract infections treatment[1].
[1]. Lim KB, et al. Treatment of uncomplicated gonorrhoea with rosoxacin (acrosoxacin).Br J Vener Dis. 1984 Jun;60(3):157-60.
Cas No. | 40034-42-2 | SDF | |
别名 | 罗索沙星,Acrosoxacin | ||
Canonical SMILES | O=C(C1=CN(CC)C2=C(C=CC(C3=CC=NC=C3)=C2)C1=O)O | ||
分子式 | C17H14N2O3 | 分子量 | 294.3 |
溶解度 | DMSO: 20.83 mg/mL (70.78 mM) | 储存条件 | Store at -20°C |
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10 mM | 0.3398 mL | 1.6989 mL | 3.3979 mL |
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Rosoxacin in the treatment of uncomplicated acute gonococcal urethritis
J Postgrad Med 1990 Oct;36(4):191-3.PMID:1966732doi
A total of 112 male patients presenting with acute gonococcal urethritis were admitted to the hospital. The diagnosis was confirmed by smear, culture, oxidase reaction and sugar fermentation tests. The patients were treated with a single 300 mg capsule of Rosoxacin. All patients except one showed adequate response to Rosoxacin.
Rosoxacin in the therapy of uncomplicated gonorrhea
Antimicrob Agents Chemother 1984 Apr;25(4):455-7.PMID:6428307DOI:10.1128/AAC.25.4.455.
In this randomized, multicentered study, 157 males and 130 females with laboratory-confirmed, uncomplicated anogenital Neisseria gonorrhoeae infections were evaluated to determine the efficacy and safety of a single 300-mg oral dose of Rosoxacin versus 3.5 g of ampicillin plus 1 g of probenecid. A total of 130 males and 101 females were evaluated. Rosoxacin cured 90.3% (P = 0.053) and 94.1% (P = 0.62), respectively, whereas ampicillin was effective in 98.5 and 98% of males and females, respectively. All 39 patients with anorectal infections were cured. One penicillinase-producing N. gonorrhoeae strain was isolated and was eradicated with Rosoxacin. Of 212 pretreatment isolates tested, 201 were inhibited by 0.06 micrograms or less of Rosoxacin per ml. The MICs of Rosoxacin for the remaining 11 isolates ranged up to 0.5 micrograms/ml. The incidence of adverse effects was relatively high (29% for the Rosoxacin group versus 18% for the ampicillin group), but none of the reactions required medical intervention nor did they result in serious sequelae.
Clinical evaluation of Rosoxacin for the treatment of chancroid
Antimicrob Agents Chemother 1986 Jul;30(1):39-41.PMID:3489439DOI:10.1128/AAC.30.1.39.
One hundred seven men with Haemophilus ducreyi-positive chancroid were assigned to receive 300 mg of Rosoxacin as a single dose or 150 mg twice daily for 3 days. Ulcers and buboes were followed clinically and bacteriologically for 1 month. Of 40 evaluable males on the 3-day regimen, 38 (95%) were cured, while only 14 of 23 (61%) males on the single-dose regimen were cured; this regimen was discontinued. There was one ulcer relapse at day 21 in both groups; the one relapse in the single-dose group had a persistent culture-positive bubo. Eight of nine (89%) buboes followed to the endpoint on the 3-day Rosoxacin regimen were cured, versus three of six (50%) on the single-dose regimen. Adverse effects were mainly related to the central nervous system but were minor and did not require intervention. None of the treatment failures was due to organisms resistant to Rosoxacin, and failure of the single-dose regimen presumably was related to duration of tissue levels rather than to drug resistance. Administration of 150 mg of Rosoxacin twice daily for 3 days is an effective regimen for the therapy of chancroid and is a reasonable alternative to other short-course regimens.
Treatment of uncomplicated gonorrhea with Rosoxacin
Antimicrob Agents Chemother 1981 Nov;20(5):625-9.PMID:6798924DOI:10.1128/AAC.20.5.625.
In a randomized, double-blind, dose-ranging study, single oral doses of Rosoxacin were used to treat 126 patients with uncomplicated genital or anorectal gonorrhea. Neisseria gonorrhoeae was eradicated from 5 (28%) of 18 men treated with 100 mg, compared with 101 (94%) of 108 men and women treated with 200 mg, 300 mg, or 400 mg (P less than 0.001). Susceptibility to Rosoxacin was determined for 6 pretreatment gonococcal isolates from these patients and for 194 stored clinical isolates; 296 (98.7%) of these 300 isolates, including 10 strains of penicillinase-producing N. gonorrhaeae, required a minimal inhibitory concentration of less than or equal to 0.062 microgram/ml. Urethral or cervical infection with Chlamydia trachomatis coexisted with gonococcal infection in 14 (22%) of 63 patients and persisted in 7 of 10 patients treated with Rosoxacin. Postgonococcal urethritis developed in 11 (34%) of 32 men who were monitored for 12 to 30 days. Sixty-four subjects (51%) developed transient dizziness, drowsiness, altered visual perceptions, or other symptoms suggestive of central nervous system dysfunction after treatment with Rosoxacin, but these symptoms were not clearly dose related. Rosoxacin in doses of greater than or equal to 200 mg appears to be effective for single-dose treatment of uncomplicated gonorrhea, but further studies of its possible central nervous system toxicity are indicated.
Rosoxacin in the treatment of uncomplicated gonorrhoea in men
Br J Vener Dis 1984 Aug;60(4):231-4.PMID:6234966DOI:10.1136/sti.60.4.231.
Between 3 January and 4 March 1983 we treated 200 male patients diagnosed as having uncomplicated gonococcal urethritis with one of two regimens. They were divided into two groups and randomly assigned to treatment with either 2 g spectinomycin administered intramuscularly (group A) or 300 mg Rosoxacin by mouth (group B). Of 187 isolates tested for the production of beta-lactamase, 101 (54%) were penicillinase producing Neisseria gonorrhoeae (PPNG) strains. All 81 cases followed in group A (spectinomycin) were cured, compared with 88.5% (77 out of 87) of the patients followed in group B (Rosoxacin). We concluded that Rosoxacin at a dosage of 300 mg administered orally was fairly effective in the treatment of gonococcal urethritis in men caused by both PPNG and non-PPNG strains.