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口服给药后人体血浆、尿液和前列腺组织中的西诺沙星浓度。

Cinoxacin concentrations in plasma, urine and prostatic tissue after oral administration to man.

作者信息

Burt R A, Morgan T, Payne J P, Bonner R M

出版信息

Br J Urol. 1977 Apr;49(2):147-52. doi: 10.1111/j.1464-410x.1977.tb04089.x.

DOI:10.1111/j.1464-410x.1977.tb04089.x
PMID:858034
Abstract

Cinoxacin, a synthetic antibacterial compound, was given orally in a dose of 500 mg to 8 patients undergoing transurethral prostatectomy. The drug was well absorbed and the peak plasma level (mean 13.9 mcg/ml) occurred 1 or 2 hours after administration. Concentrations of cinoxacin in the urine reached a peak (mean 236.5 mcg/ml) 4 to 6 hours after dosing, and remained higher than the mean MIC for most common urinary pathogens for 12 hours after administration. The concentration of cinoxacin in prostatic tissue 2.5-4 hours after administration varied between 0.6 and 6.3 mcg/g. The individual variations were unrelated to the concurrent plasma level and appeared to be influenced more by inter-subject variation than by the physicochemical properties of the drug. In 1 patient the cinoxacin level was estimated in renal tissue (70.1 mcg/g), in muscle (12.6 mcg/g), and in perirenal fat (4.7 mcg/g).

摘要

西诺沙星是一种合成抗菌化合物,以500毫克的剂量口服给予8名接受经尿道前列腺切除术的患者。该药物吸收良好,给药后1至2小时达到血浆峰值水平(平均13.9微克/毫升)。给药后4至6小时,尿液中西诺沙星浓度达到峰值(平均236.5微克/毫升),给药后12小时内,其浓度一直高于大多数常见尿路病原体的平均最低抑菌浓度。给药后2.5至4小时,前列腺组织中西诺沙星浓度在0.6至6.3微克/克之间变化。个体差异与同时期的血浆水平无关,似乎更多地受到个体间差异的影响,而非药物的物理化学性质。在1名患者中,测定了肾组织(70.1微克/克)、肌肉(12.6微克/克)和肾周脂肪(4.7微克/克)中的西诺沙星水平。

相似文献

1
Cinoxacin concentrations in plasma, urine and prostatic tissue after oral administration to man.口服给药后人体血浆、尿液和前列腺组织中的西诺沙星浓度。
Br J Urol. 1977 Apr;49(2):147-52. doi: 10.1111/j.1464-410x.1977.tb04089.x.
2
Rosoxacin and cinoxacin distribution in prostate, vagina, and female urethra. An experimental study in dogs.罗索沙星和西诺沙星在前列腺、阴道及女性尿道中的分布:一项犬类实验研究
Invest Urol. 1979 Sep;17(2):149-52.
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Influence of probenecid on serum levels and urinary excretion of cinoxacin.丙磺舒对西诺沙星血清水平及尿排泄的影响。
Antimicrob Agents Chemother. 1979 Mar;15(3):465-9. doi: 10.1128/AAC.15.3.465.
4
Pharmacology of cinoxacin in humans.西诺沙星在人体中的药理学。
Antimicrob Agents Chemother. 1979 Feb;15(2):165-70. doi: 10.1128/AAC.15.2.165.
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Cinoxacin: pharmacokinetics and the effect of probenecid.西诺沙星:药代动力学及丙磺舒的影响
J Clin Pharmacol. 1978 Oct;18(10):491-9. doi: 10.1002/j.1552-4604.1978.tb01577.x.
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[Tissue diffusion of flumequine into human renal and prostatic tissues. Assay of flumequine by high performance liquid chromatography after administration of 800 mg/day over 48 hours, the sampling being done 12 hours after the last ingestion].氟甲喹在人体肾脏和前列腺组织中的组织扩散。在48小时内每日服用800毫克后,通过高效液相色谱法测定氟甲喹,在最后一次摄入后12小时进行取样。
J Urol (Paris). 1985;91(3):159-62.
7
Cinoxacin in urinary tract infections. Theoretical and practical considerations.西诺沙星用于尿路感染:理论与实践考量
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8
Influence of urinary pH on the pharmacokinetics of cinoxacin in humans and on antibacterial activity in vitro.尿液pH值对西诺沙星在人体内药代动力学及体外抗菌活性的影响。
Antimicrob Agents Chemother. 1982 Mar;21(3):472-80. doi: 10.1128/AAC.21.3.472.
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Efficacy of cinoxacin in urinary tract infections.西诺沙星在尿路感染中的疗效。
Antimicrob Agents Chemother. 1976 Mar;9(3):502-5. doi: 10.1128/AAC.9.3.502.
10
Cinoxacin: pharmacokinetics and tolerance in patients with normal and impaired renal function.西诺沙星:肾功能正常和受损患者的药代动力学及耐受性
Antimicrob Agents Chemother. 1979 Sep;16(3):411-6. doi: 10.1128/AAC.16.3.411.

引用本文的文献

1
Comparative pharmacokinetic profiles of cinoxacin and pipemidic acid in humans.西诺沙星和吡哌酸在人体中的比较药代动力学概况。
Eur J Drug Metab Pharmacokinet. 1983 Jul-Sep;8(3):251-9. doi: 10.1007/BF03188755.
2
Cinoxacin. A review of its pharmacological properties and therapeutic efficacy in the treatment of urinary tract infections.西诺沙星。其药理学特性及治疗尿路感染疗效的综述。
Drugs. 1983 Jun;25(6):544-69. doi: 10.2165/00003495-198325060-00002.
3
Cinoxacin: pharmacokinetics and tolerance in patients with normal and impaired renal function.
西诺沙星:肾功能正常和受损患者的药代动力学及耐受性
Antimicrob Agents Chemother. 1979 Sep;16(3):411-6. doi: 10.1128/AAC.16.3.411.
4
Pharmacology of cinoxacin in humans.西诺沙星在人体中的药理学。
Antimicrob Agents Chemother. 1979 Feb;15(2):165-70. doi: 10.1128/AAC.15.2.165.