更新于：2024-11-15
Levornidazole
左奥硝唑
更新于：2024-11-15
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2009-08-14), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C7H10ClN3O3 |
InChIKeyIPWKIXLWTCNBKN-ZCFIWIBFSA-N |
CAS号166734-83-4 |
关联
8
项与 左奥硝唑 相关的临床试验A multi-center, randomized, double-blind and positive parallel control clinical study of the efficacy and safety of Levornidazole Disodium Phosphate for Injection in the treatment of pelvic anaerobic infections
A pharmacokinetics study of levornidazole sodium chloride injection and ornidazole sodium chloride injection in healthy volunteers
中国健康受试者单/多次口服左奥硝唑片的安全性、耐受性和药动学研究及口服左奥硝唑片500mg绝对生物利用度研究
100 项与 左奥硝唑 相关的临床结果
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100 项与 左奥硝唑 相关的转化医学
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100 项与 左奥硝唑 相关的专利（医药）
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16
项与 左奥硝唑 相关的文献（医药）2023-12-01International journal of clinical pharmacology and therapeutics
Pharmacokinetics and safety of injected ornidazole compared to its enantiomer levornidazole in healthy Chinese subjects
Article
作者: Wang, Tingting ; Wang, Juan ; Wang, Xin ; Xue, Wei ; Bai, Wenjing ; Liu, Yue ; Qin, Jie ; Li, Kexin ; Tang, Kaitian ; Liu, Yao ; Zhang, Ying
OBJECTIVE:
To compare the pharmacokinetics of levornidazole and ornidazole in healthy Chinese subjects after a single intravenous injection, and to determine whether the chiral inversion of levornidazole occurs in vivo.
MATERIALS AND METHODS:
The study was a randomized, open-label, two-period crossover, single-dose design. A total of 12 subjects were enrolled in this study. Subjects received an intravenous injection of either levornidazole sodium chloride injection (200 mL: 0.5 g) or ornidazole sodium chloride injection (200 mL: 0.5 g) once per period. The plasma concentrations of levornidazole, ornidazole, and their metabolites were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. Phenix WinNolin software (version 6.4) was used to calculate the pharmacokinetic parameters of levornidazole, ornidazole, and their metabolites.
RESULTS:
Dexornidazole was not detected in the plasma or urine. After a single intravenous injection of levornidazole or ornidazole, there was no significant difference in Cmax between the two drugs (p < 0.05). The AUC0-∞ and AUC0-t of levornidazole were slightly lower than those of ornidazole. Metabolites M1 and M4 were detected in the plasma of both drugs, and their pharmacokinetic parameters were similar. Metabolites M1, M2, and M4 were present in urine. The average cumulative urinary excretion rates of levornidazole and its metabolites M1 and M4 were: during 0 - 24 hours (8.14 ± 0.80%, 0.560 ± 0.072%, and 1.42 ± 0.19%) and 0 - 60 hours (10.5 ± 1.0%, 0.960 ± 0.084%, and 2.52 ± 0.20%), the average cumulative urinary excretion rates of ornidazole and its metabolites M1 and M4 were: 0 - 24 hours (8.64 ± 0.98%, 0.486 ± 0.074%, and 1.46 ± 0.21%), 0 - 60 hours (11.8 ± 1.0%, 0.888 ± 0.070%, and 2.76 ± 0.20%). The incidence of adverse reactions was similar between the two drugs.
CONCLUSION:
No chiral inversion of levornidazole occurred in vivo after intravenous administration of levornidazole. The pharmacokinetic parameters and cumulative excretion rates of levornidazole and ornidazole were similar. The safety results were basically consistent between the two drugs.
2023-04-01International journal of antimicrobial agents
Population pharmacokinetics of levornidazole in healthy subjects and patients, and sequential dosing regimen proposal using pharmacokinetic/pharmacodynamic analysis
Article
作者: Cao, Guoying ; Li, Yi ; Guo, Beining ; Fan, Yaxin ; Cao, Yuran ; Wu, Xiaojie ; Wu, Hailan ; Zhang, Jing ; Yu, Jicheng
Although sequential treatment with levornidazole has been used for anaerobic infection in clinical practice, there is no evidence-based dosing regimen. This study aimed to evaluate the pharmacokinetics (PK) of levornidazole in healthy subjects and patients, and to propose an evidence-based sequential dosing regimen by pharmacokinetic/pharmacodynamic (PK/PD) analysis. A population PK model was built using the data of 116 Chinese subjects, including 88 healthy young subjects, 12 healthy elderly subjects, and 16 patients with intra-abdominal anaerobic infection. PK/PD analysis was performed combining the minimum inhibitory concentration (MIC) values of levornidazole against 375 anaerobic strains. Four sequential dosing regimens (500 mg q12h, 1000 mg loading dose followed by 500 mg q12h, 750 mg q24h, and 1000 mg q24h) were evaluated in terms of cumulative fraction of response (CFR) and probability of target attainment (PTA) by Monte Carlo simulation. The concentration data of levornidazole and its active metabolites were described adequately by two- and one-compartment models, respectively. Body weight was identified as a significant covariate of levornidazole clearance. Simulations showed that satisfactory PTA (>90%) was achieved for the four dosing regimens when MIC ≤1 mg/L. Considering the simulation results, patients' safety and compliance, levornidazole 750 mg intravenous infusion q24h for 2 days followed by 750 mg oral dose q24h for 5 days was optimal for Bacteroides spp. with an identified MIC ≤1 mg/L.
2021-08-01Current medical science4区 · 医学
The Potential Immunomodulatory Properties of Levornidazole Contribute to Improvement in Experimental Ulcerative Colitis
4区 · 医学
Article
作者: Gao, Yu-Zhi ; Huang, Yan-Xiu ; Gou, Ling-Shan ; Huang, Yu-Qing ; Li, Yu ; Zhang, Rui-Juan ; Xie, Jun ; Chen, Hao ; Wang, Xing-Qi ; Yao, Rui-Qin
The use of an antibiotic with immunomodulatory properties could be fascinating in treating multifactorial inflammatory conditions such as ulcerative colitis (UC). We report our investigations into the immunomodulatory properties of levornidazole, the S-enantiomer of ornidazole, which displayed a tremendous therapeutic potential in UC induced by dextran sodium sulfate (DSS). Levornidazole administration to DSS-colitic mice attenuated the intestinal inflammatory process, with an efficacy better than that shown by 5-amino salicylic acid. This was evidenced by decreased disease activity index, ameliorated macroscopic and microscopic colon damages, and reduced expression of inflammatory cytokines. Additionally, levornidazole displayed anti-inflammatory activity through Caveolin-1-dependent reducing IL-1β and IL-18 secretion by macrophages contributing to its improvement of the intestinal inflammation, as confirmed in vitro and in vivo. In conclusion, these results pointed out that the immunomodulatory effects of levornidazole played a vital role in ameliorating the intestinal inflammatory process, which would be crucial for the translation of its use into clinical settings.
100 项与 左奥硝唑 相关的药物交易
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 细菌感染 | 中国 | 2009-08-14 |
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