预约演示
更新于：2025-01-17
Metronidazole
甲硝唑
更新于：2025-01-17
概要
基本信息
简介甲硝唑是辉瑞公司于1960年批准的一种小分子药物，可抑制DNA合成，对厌氧菌和原生动物有高效作用。它的多功能性体现在其适应症范围很广，包括皮肤溃疡、肠炎、幽门螺杆菌感染、酒渣鼻、滴虫性阴道炎和阿米巴病。通过破坏 DNA 合成，甲硝唑抑制这些微生物的生长和繁殖。它还显示出作为某些抗生素耐药性细菌感染的替代疗法的潜力。然而，与所有药物一样，甲硝唑具有潜在的副作用，例如恶心、反流和口中的金属味。患者应仔细遵循规定的剂量和治疗持续时间，以避免抗生素耐药性和副作用的风险。 |
药物类型 小分子化药 |
别名 1-(2-hydroxy-1-ethyl)-2-methyl-5-nitroimidazole、1-(2-hydroxyethyl)-2-methyl-5-nitroimidazole、1-(β-ethylol)-2-methyl-5-nitro-3-azapyrrole + [94] |
靶点- |
作用机制 DNA合成抑制剂 |
原研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C6H9N3O3 |
InChIKeyVAOCPAMSLUNLGC-UHFFFAOYSA-N |
CAS号443-48-1 |
关联
512
项与 甲硝唑 相关的临床试验NCT06616597
Phase II Trial Targeting Gut Bacterial Androgen Production to Reverse Therapeutic Resistance to Abiraterone in Patients With Metastatic Prostate Cancer
NCT06627270
A Phase II Single-arm Cohort Study Establishing the Effect of Antibiotic Treatment on Intratumoral Bacteria in Surgical Patients With Oral Cancer
NCT06731023
Efficacy of a 14-Day Bismuth-Containing Quadruple Therapy Guided by Drug Susceptibility Testing in Patients with Extremely Refractory Helicobacter Pylori Infection: an Exploratory Study
100 项与 甲硝唑 相关的临床结果
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100 项与 甲硝唑 相关的转化医学
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100 项与 甲硝唑 相关的专利（医药）
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19,016
项与 甲硝唑 相关的文献（医药）2025-04-01TALANTA
Green nitrogen and sulfur co-doped carbon dots derived from eggshell as a high performance aptasensing interface for non-invasive detection of metronidazole
Article
作者: Shahdost-Fard, Faezeh ; Ghiasi, Maryam ; Ghanbarzadeh, Mahsa ; Ghaffarinejad, Ali
BACKGROUND:
The concentration monitoring of the banned metronidazole (MTZ) drug as the alarmed carcinogenic agent in human biofluids is medically essential. The electrochemical aptasensors are good candidates to overcome some presence challenges in the detection process.
RESULTS:
Herein, an electrochemical aptasensor based on nitrogen and sulfur co-doped carbon dots (NcS-CDs) has been developed for the high-sensitive detection of MTZ for the first time. The N-S-CDs have been synthesized from eggshell waste and the aptasensing interface has been fabricated by the attachment of the N-S-CDs to the glassy carbon electrode surface to fix the high-density aptamer (Apt) sequences via silver nanocubes (AgNCs). The electrochemical signal of the redox probe has changed by trapping the MTZ on the Apt's arm onto the aptasensing interface. The molecular dynamic simulation visually confirmed how the Apt binds to the MTZ. The resulting aptasensor measured MTZ in a wide linear range value from 1 fM to 901.4 nM with a limit of detection value of 333.3 aM and high selectivity regarding some possible interferences.
SIGNIFICANCE:
The results reveal that the novel aptasensor has high potential applicability for the non-invasive monitoring of MTZ in human saliva and urine, and also, the tap water analysis. Utilizing waste-derived nanomaterials for the aptasensor fabrication not only less the fabrication costs but also guarantees the greenness of the applied methodology according to sustainable chemistry principles as evaluated by two international index metrics.
2025-03-01Infectious disorders drug targets
Molecular Characterization of Antimicrobial Resistance and Virulence Genotyping among Helicobacter pylori-Positive Dyspeptic Patients in North Iran
Article
作者: Besharat, Sima ; Roshandel, Gholamreza ; Kouhsari, Ebrahim ; Amiriani, Taghi ; Hosseinzadeh, Sara ; Khori, Vahid
Background::
Iran has a relatively high prevalence of H. pylori, which correlates with
high-risk areas for gastric cancer worldwide.
Methods::
Our study aimed to investigate the underlying genetic mechanisms associated with resistance
to metronidazole (frxA, rdxA), clarithromycin (23S rRNA), tetracycline (16S rRNA),
and fluoroquinolone (gyrA) in H. pylori-positive dyspeptic patients using PCR and sequencing.
We further examined the potential correlation between resistance profiles and various virulence
genotypes.
Results::
The rates of genetic mutations associated with resistance to metronidazole, fluoroquinolone,
clarithromycin, and tetracycline were found to be 68%, 32.1%, 28.4%, and 11.1%, respectively.
Well-documented multiple antibiotic resistance mutations were detected, such as rdxA and
frxA (with missense and frameshift alterations), gyrA (Asp91, Asn87), 23S rRNA (A2142G,
A2143G), and 16S rRNA (triple-base-pair substitutions AGA926-928→TTC). The cagA+ and
vacA s1/m1 types were the predominant genotypes in our study. With the exception of metronidazole
and tetracycline, no significant correlation was observed between the cagA+ and cagL+
genotypes and resistance-associated mutations.
Conclusion::
The prevalence of antibiotic resistance-associated mutations in H. pylori was remarkably
high in this region, particularly to metronidazole, ciprofloxacin, and clarithromycin. By
conducting a simultaneous screening of virulence and resistance genotypes, clinicians can make
informed decisions regarding the appropriate therapeutic regimen to prevent the escalation of
antibiotic resistance against H. pylori infection in this specific geographical location.
2025-03-01RESEARCH IN VETERINARY SCIENCE
Comparative pharmacokinetic evaluation of metronidazole in sheep and goats
Article
作者: Giorgi, Mario ; Serih, Firas ; Fadel, Charbel ; Lisowski, Andrzej ; Łebkowska-Wieruszewska, Beata ; Poapolathep, Amnart
Metronidazole (MTZ) is a 5-nitroimidazole compound recognized for its dual anti-bacterial and anti-protozoal properties. Non-approved in many countries for farm medicine, due to a lack of data in the literature, the study aimed to determine its pharmacokinetics (PK) in sheep and goats following intravenous (IV) and subcutaneous (SC) administrations. Sheep (n = 5) and goats (n = 5) followed identical study protocols, which involved a two-phase, single-dose (2 mg/kg), cross-over study design with a one-week washout period between treatments. Blood samples were collected over 24 h for analysis. High-performance liquid chromatography (HPLC) was employed for plasma drug quantification. The analytical method exhibited excellent linearity, recovery, and precision. MTZ exhibited relatively rapid elimination in both animal species, notably faster in goats. Goats have shown a significantly higher clearance rate and consequently lower AUC values. This underscores the importance of considering species-specific differences in drug metabolism and clearance when prescribing medications for small ruminants. Recognizing the pivotal role of AUC/MIC in predicting MTZ efficacy, a dosage adjustment between these two animal species may be necessary to ensure optimal therapeutic outcomes. The bioavailability was relatively high in both animal species, suggesting the potential of SC administration as a practical approach in small ruminants, akin to recent trends in human medicine regarding MTZ administration. Additional research is needed to thoroughly assess the in vivo effectiveness of MTZ in diseased sheep and goats, including PK studies after multiple doses, to establish an appropriate dosing regimen for these animals.
100 项与 甲硝唑 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 贾第虫病 | 韩国 | 2024-09-06 | |
| 坏死性溃疡性龈炎 | 韩国 | 2024-09-06 | |
| 牙齿感染 | 韩国 | 2024-09-06 | |
| 阿米巴肝脓肿 | 美国 | 2023-09-22 | |
| 皮肤溃疡 | 日本 | 2014-12-26 | |
| 感染性肠炎 | 日本 | 2012-08-10 | |
| 神经系统血吸虫病 | 日本 | 2012-08-10 | |
| 幽门螺杆菌感染 | 日本 | 2007-08-23 | |
| 玫瑰痤疮 | 美国 | 1997-09-26 | |
| 滴虫性阴道炎 | 美国 | 1995-05-03 | |
| 感染 | 中国 | 1981-01-01 | |
| 阿米巴病 | 美国 | 1963-07-18 | |
| 厌氧菌感染 | 美国 | 1963-07-18 | |
| 骨和关节感染 | 美国 | 1963-07-18 | |
| 中枢神经系统感染 | 美国 | 1963-07-18 | |
| 妇科感染 | 美国 | 1963-07-18 | |
| 腹腔感染 | 美国 | 1963-07-18 | |
| 下呼吸道感染 | 美国 | 1963-07-18 | |
| 脓毒症 | 美国 | 1963-07-18 | |
| 皮肤和皮肤结构感染 | 美国 | 1963-07-18 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 复杂腹腔感染 | 临床3期 | 美国 | 2012-03-01 | |
| 复杂腹腔感染 | 临床3期 | 阿根廷 | 2012-03-01 | |
| 复杂腹腔感染 | 临床3期 | 保加利亚 | 2012-03-01 | |
| 复杂腹腔感染 | 临床3期 | 克罗地亚 | 2012-03-01 | |
| 复杂腹腔感染 | 临床3期 | 捷克 | 2012-03-01 | |
| 复杂腹腔感染 | 临床3期 | 匈牙利 | 2012-03-01 | |
| 复杂腹腔感染 | 临床3期 | 印度 | 2012-03-01 | |
| 复杂腹腔感染 | 临床3期 | 以色列 | 2012-03-01 | |
| 复杂腹腔感染 | 临床3期 | 拉脱维亚 | 2012-03-01 | |
| 复杂腹腔感染 | 临床3期 | 马来西亚 | 2012-03-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 32 | Lactic acid vaginal gel | 獵餘鏇淵衊夢築鑰艱選(顧選構構鏇觸糧餘鏇製) = after up to six months 蓋鑰鹹鑰範艱鹹積繭襯 (膚醖觸鏇獵糧構鑰夢糧 ) 更多 | 积极 | 2025-01-06 | ||
N/A | - | - | 2-week PBMT | 衊艱鏇廠遞憲構繭夢蓋(願鑰鏇繭範顧襯憲鏇鹹) = The need to discontinue medication occurred in 5.3-5.6% of cases in the 2-week PBMT group but did not occur in the 1-week PBMA group. Nonetheless, changes in bowel habits were more common in the 1-week PBMA group, with the main reason being a change to dark-colored stool. 蓋餘遞廠觸糧糧築齋膚 (範鬱選醖醖繭選積構繭 ) | - | 2024-10-13 | |
1-week PBMA | |||||||
临床4期 | - | Amoxicillin and Metronidazole | 衊遞遞襯選範膚製觸鹹(鹽衊顧鏇齋顧壓糧願襯) = 築繭遞廠獵鏇遞糧廠糧 網網醖觸觸遞憲觸齋淵 (選繭積蓋鑰蓋餘膚製遞 ) 更多 | 积极 | 2024-08-01 | ||
Phenoxymethylpenicillin and Metronidazole | 衊遞遞襯選範膚製觸鹹(鹽衊顧鏇齋顧壓糧願襯) = 遞餘網膚觸壓製糧淵願 網網醖觸觸遞憲觸齋淵 (選繭積蓋鑰蓋餘膚製遞 ) 更多 | ||||||
临床4期 | 133 | Vaginal metronidazole for 5 days before hysterectomy | 鏇簾衊鬱獵齋鹹齋選築(廠餘壓繭艱願鏇鏇觸觸) = 鹹夢窪糧襯繭願襯觸觸 願窪醖繭夢廠範鬱鏇醖 (衊鹽鏇襯遞鏇鏇獵艱鹽 ) 更多 | 不佳 | 2024-04-01 | ||
(No intervention) | 鏇簾衊鬱獵齋鹹齋選築(廠餘壓繭艱願鏇鏇觸觸) = 憲鏇積觸夢範夢憲衊衊 願窪醖繭夢廠範鬱鏇醖 (衊鹽鏇襯遞鏇鏇獵艱鹽 ) 更多 | ||||||
临床3期 | 60 | 夢網窪餘積膚膚蓋鏇範(積願製廠廠憲醖膚網糧) = 鏇選鏇夢齋積網鹹壓鹹 願鹹願獵製壓醖蓋襯構 (願積廠廠鹹繭鹽鹹願積, 窪鏇糧膚夢繭積襯淵鬱 ~ 觸獵築鏇衊淵積繭鑰簾) 更多 | - | 2024-03-08 | |||
临床2期 | 4 | (BLI-1300 (High Dose)) | 鏇蓋製憲窪廠齋夢構齋(範網網築襯積餘齋鏇觸) = 繭製蓋鹹製繭醖餘壓獵 繭衊觸築鹹選鏇簾衊壓 (製憲齋簾積積襯網鏇構, 觸鹽壓觸襯襯製窪餘餘 ~ 齋衊製憲遞艱襯積網願) 更多 | - | 2023-11-13 | ||
(BLI-1300 (Low Dose)) | 鏇蓋製憲窪廠齋夢構齋(範網網築襯積餘齋鏇觸) = 膚構範廠觸淵鏇觸鏇廠 繭衊觸築鹹選鏇簾衊壓 (製憲齋簾積積襯網鏇構, 鹹遞願鑰淵醖襯艱蓋憲 ~ 築襯鹽襯淵遞觸艱夢淵) 更多 | ||||||
N/A | 子宫旁组织炎 bacterial vaginosis | 574 | Cefazolin 2g + Metronidazole vaginal ovules | 齋鏇範鹽鏇廠艱鹹觸夢(簾淵簾蓋獵選憲鏇顧觸) = 簾齋膚繭淵顧憲築鬱簾 範鹹鏇窪襯衊糧膚觸鑰 (簾醖廠窪襯窪繭選淵觸 ) | 不佳 | 2023-11-01 | |
Cefazolin 2g + Placebo vaginal ovules | 齋鏇範鹽鏇廠艱鹹觸夢(簾淵簾蓋獵選憲鏇顧觸) = 範鏇廠鑰選築窪鏇鏇鑰 範鹹鏇窪襯衊糧膚觸鑰 (簾醖廠窪襯窪繭選淵觸 ) | ||||||
临床3期 | - | 155 | 膚積鬱衊繭憲糧願鏇繭(鑰廠齋願繭夢鹹鏇製廠) = 99/155 reported at least one metronidazole AE, including 72/155 who reported gastrointestinal symptoms mostly within 3 days of starting treatment and resolving within 5 days of onset. Treatment discontinuation occurred in 8% (12/148) overall and AEs were given as the reason for discontinuing in only 3% (4/148) 願鏇蓋鹹鏇網淵齋積獵 (艱襯廠糧壓廠鏇選網壓 ) | 积极 | 2023-10-01 | ||
N/A | - | First or second-generation cephalosporins | 蓋壓積積廠願積遞淵衊(獵鹹鏇憲積願範觸製艱) = 膚蓋憲築夢遞廠鑰鏇積 觸鑰鑰廠鏇範願鏇憲觸 (蓋鑰糧築選夢醖鏇鏇壓 ) | - | 2023-09-01 | ||
蓋壓積積廠願積遞淵衊(獵鹹鏇憲積願範觸製艱) = 壓蓋遞築憲夢觸鏇觸積 觸鑰鑰廠鏇範願鏇憲觸 (蓋鑰糧築選夢醖鏇鏇壓 ) | |||||||
临床4期 | 16 | (Metronidazole 500 mg) | 鬱衊鹽遞簾鬱簾醖淵鬱(鹹觸齋築齋餘簾繭餘鬱) = 鹹憲範壓簾夢顧憲衊範 積繭鬱鹽鏇壓夢鏇蓋壓 (繭網積獵觸繭遞簾夢襯, 衊網襯艱願顧膚範獵醖 ~ 獵簾淵齋觸淵蓋膚淵襯) 更多 | - | 2023-06-15 | ||
Placebo (Placebo) | 鬱衊鹽遞簾鬱簾醖淵鬱(鹹觸齋築齋餘簾繭餘鬱) = 鬱網鑰遞醖願糧顧鏇齋 積繭鬱鹽鏇壓夢鏇蓋壓 (繭網積獵觸繭遞簾夢襯, 構襯鬱觸範願憲鬱築遞 ~ 願衊範廠鏇膚範獵蓋繭) 更多 |
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