更新于：2024-07-17
Cimetidine
西咪替丁
更新于：2024-07-17
概要
基本信息
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1977-08-16) |
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C10H16N6S |
InChIKeyAQIXAKUUQRKLND-UHFFFAOYSA-N |
CAS号51481-61-9 |
关联
37
项与 西咪替丁 相关的临床试验Postpartum Activity and Expression of BCRP and OCT1 Drug Transporters in the Mammary Gland
An Open-label Phase I Study to Evaluate the Drug-drug Interaction of HSK16149 Capsule With Probenecid Tablets or Cimetidine Tablets in Healthy Subjects
评估HSK16149胶囊与丙磺舒片、西咪替丁片在健康受试者中药物-药物相互作用的开放性I期临床研究
100 项与 西咪替丁 相关的临床结果
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100 项与 西咪替丁 相关的转化医学
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100 项与 西咪替丁 相关的专利（医药）
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10,932
项与 西咪替丁 相关的文献（医药）2024-03-01Environmental research
Adsorption behavior and interaction mechanism of microplastics with typical hydrophilic pharmaceuticals and personal care products
Article
作者: Liu, Lu ; Gong, Yichao ; Liu, Pengyan ; Sun, Qizhi
Microplastics (MPs) and pharmaceuticals and personal care products (PPCPs) are two types of emerging contaminants widely present in the global aquatic ecosystem. The ecological risks associated with the coexistence of these two contaminants have garnered increasing attention from researchers. In this study, we selected 15 typical hydrophilic PPCPs, including Sulfacetamide (SA), Thiamphenicol, Florfenicol, Chloramphenicol (CHL), Ampicillin, Cephalexin, Ofloxacin, Fluorouracil, Phenytoin, Theophylline, Cimetidine, Methylparaben, Diethyltoluamide, Benzophenone-2 (BP-2), and Benzophenone-4, as adsorbates. We evaluated the adsorption potential of five traditional plastics (TPs), namely Polyamide 6 (PA6), Polystyrene (PS), Polyethylene terephthalate (PET), Polyvinyl chloride (PVC), and Polyurethane (TPU), as well as three biodegradable plastics (BDPs), including Polylactic acid (PLA), Polybutylene succinate (PBS), and Poly (ε-caprolactone) (PCL), for these adsorbates. Out of the 120 combinations of MPs and PPCPs tested, only 24 exhibited significant adsorption behavior. Notably, the adsorption performance of the three BDPs was stronger than that of the three typical TPs (PS, PET, and PVC). Based on their adsorption potential, PA6, BDPs, phenytoin, and BP-2 were identified as potential sources of high ecological risk. To further explore the adsorption mechanism, we investigated the adsorption behaviors of SA, BP-2, and CHL on PA6. The conclusions were as follows: SA, BP-2, and CHL all reached adsorption equilibrium within 24 h, with the partition coefficient (Kd) following this order: BP-2 (8.051) ≫ SA (0.052) > CHL (0.018). The primary forces of adsorption were electrostatic interactions, intermolecular hydrogen bonding, and hydrophobic interaction, respectively. Additionally, weak electrostatic effects were observed in the adsorption of CHL and BP-2. The effects of pH, ionic strength, and fulvic acid on adsorption capacity varied. These results highlight a complex adsorption mechanism between MPs and hydrophilic contaminants in the aquatic environment. This study provides a basis for further evaluating the ecological risks of MPs and PPCPs combined pollution.
2024-02-01Drug metabolism and disposition: the biological fate of chemicals
Effect of Cimetidine on Metformin Pharmacokinetics and Endogenous Metabolite Levels in Rats
Article
作者: Prasad, Bhagwat ; Thakur, Aarzoo ; Singh, Dilip Kumar ; Ailabouni, Anoud Sameer ; Mettu, Vijaya Saradhi
Tubular secretion is a primary mechanism along with glomerular filtration for renal elimination of drugs and toxicants into urine. Organic cation transporters (OCTs) and multidrug and toxic extrusion (MATE) transporters facilitate the active secretion of cationic substrates, including drugs such as metformin and endogenous cations. We hypothesized that administration of cimetidine, an Oct/Mate inhibitor, will result in increased plasma levels and decreased renal clearance of metformin and endogenous Oct/Mate substrates in rats. A paired rat pharmacokinetic study was carried out in which metformin (5 mg/kg, intravenous) was administered as an exogenous substrate of Oct/Mate transporters to six Sprague-Dawley rats with and without cimetidine (100 mg/kg, intraperitoneal). When co-administered with cimetidine, metformin area under the curve increased significantly by 3.2-fold, and its renal clearance reduced significantly by 73%. Untargeted metabolomics was performed to investigate the effect of cimetidine on endogenous metabolome in the blood and urine samples. Over 8,000 features (metabolites) were detected in the blood, which were shortlisted using optimized criteria, i.e., a significant increase (P value < 0.05) in metabolite peak intensity in the cimetidine-treated group, reproducible retention time, and quality of chromatogram peak. The metabolite hits were classified into three groups that can potentially distinguish inhibition of i) extra-renal uptake transport or catabolism, ii) renal Octs, and iii) renal efflux transporters or metabolite formation. The metabolomics approach identified novel putative endogenous substrates of cationic transporters that could be tested as potential biomarkers to predict Oct/Mate transporter mediated drug-drug interactions in the preclinical stages. SIGNIFICANCE STATEMENT: Endogenous substrates of renal transporters in animal models could be used as potential biomarkers to predict renal drug-drug interactions in early drug development. Here we demonstrated that cimetidine, an inhibitor of organic cation transporters (Oct/Mate), could alter the pharmacokinetics of metformin and endogenous cationic substrates in rats. Several putative endogenous metabolites of Oct/Mate transporters were identified using metabolomics approach, which could be tested as potential transporter biomarkers to predict renal drug-drug interaction of Oct/Mate substrates.
2024-02-01European archives of oto-rhino-laryngology : official journal of the European Federation of Oto-Rhino-Laryngological Societies (EUFOS) : affiliated with the German Society for Oto-Rhino-Laryngology - Head and Neck Surgery
Cimetidine for recurrent respiratory papillomatosis in pregnancy as an alternative adjuvant treatment
Article
作者: Liew, Yew Toong ; Tan, Sien Hui ; Ghauth, Sakina ; Abu Bakar, Zulkiflee
BACKGROUND:
We report the first case of cimetidine as an alternative adjuvant therapy in a pregnant woman with recurrent respiratory papillomatosis (RRP). A 40 year old woman at 19 week gestation presented with progressive hoarseness and shortness of breath for 1 month. Flexible nasopharyngolaryngoscopy revealed multiple papillomatous lesions over both vocal cords and subglottic area obstructing 60% of her airway. She had previously been diagnosed with juvenile onset RRP at the age of 5 and underwent endoscopic clearance regularly every 6 months.
METHOD:
The patient was started on a trial of oral cimetidine at a dose of 30 mg/kg and responded well, eventually requiring endoscopic excision only after 2 years. Subsequently, she underwent in vitro fertilisation treatment and stopped taking her cimetidine. After undergoing endoscopic clearance of her papillomata under general anaesthesia, she restarted on cimetidine during her 2nd and 3rd trimester.
RESULTS:
Ensuing follow-up demonstrated stable minimal papillomata lesions on her right inferior surface of her vocal cord with no recurrence on her left vocal cord and subglottic area.
CONCLUSION:
Cimetidine is generally safe and not known to be associated with any major teratogenic risks during pregnancy. RRP is postulated to worsen in pregnant women due to the increase in oestrogen levels during pregnancy. Hence, adjuvant therapy was imperative for our patient to reduce recurrent papillomata formation during her pregnancy. Larger scale studies are warranted to assess the use of long-term high-dose cimetidine in terms of efficacy and safety in pregnancy.
100 项与 西咪替丁 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 胃灼热 | 美国 | 1995-06-19 | |
| 出血性胃炎 | 日本 | 1987-10-01 | |
| 应激性溃疡 | 日本 | 1987-10-01 | |
| 上消化道出血 | 日本 | 1987-10-01 | |
| 急性胃炎 | 日本 | 1987-09-02 | |
| 慢性胃炎 | 日本 | 1987-09-02 | |
| 反流性食管炎 | 日本 | 1987-09-02 | |
| 麻醉 | 日本 | 1987-06-30 | |
| 消化性溃疡 | 中国 | 1983-01-01 | |
| 吻合口溃疡 | 日本 | 1981-09-19 | |
| 十二指肠溃疡 | 日本 | 1981-09-19 | |
| 消化道出血 | 日本 | 1981-09-19 | |
| 胃溃疡 | 日本 | 1981-09-19 | |
| Zollinger-Ellison综合征 | 日本 | 1981-09-19 | |
| 胃食管反流 | 中国 | 1981-01-01 |
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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1期 | - | 14 | 膚積選鬱壓憲憲獵製廠(襯築餘餘遞襯網網顧餘) = 壓鹽蓋製繭醖衊構鏇鹹 齋憲窪醖簾艱範積獵窪 (鬱製衊遞構積糧遞積網 ) | - | 2020-03-01 | ||
临床4期 | - | 25 | hydroxypropyl methylcellulose (HPMC)+cimetidine (Experimental: CimTest-A) | 願鬱觸鑰鹽窪築艱膚顧(糧顧獵憲憲積獵壓醖構) = 衊築製築鑰衊簾範鏇遞 獵膚網鏇繭壓壓鏇選鑰 (醖網鑰餘簾衊簾鏇積遞, 夢範鏇蓋簾遞繭膚壓鏇 ~ 觸範構觸網築鏇襯選衊) 更多 | - | 2019-08-28 | |
magnesium stearate+cimetidine (Experimental: CimTest-B) | 願鬱觸鑰鹽窪築艱膚顧(糧顧獵憲憲積獵壓醖構) = 醖餘廠構繭鏇製膚遞齋 獵膚網鏇繭壓壓鏇選鑰 (醖網鑰餘簾衊簾鏇積遞, 願鏇鬱鹹繭淵顧糧夢蓋 ~ 網壓範襯壓願選簾糧簾) 更多 | ||||||
临床3期 | 274 | Placebo+Esomeprazole | 顧顧簾夢築構襯願膚夢(齋衊艱鏇顧鬱鏇選鏇鏇) = The safety profiles of both drugs were similar and as expected in critically ill patients. 顧糧淵艱鬱顧觸淵網獵 (觸顧壓衊積構製觸獵願 ) | 积极 | 2018-08-01 | ||
Cimetidine+Placebo | |||||||
临床2期 | - | 窪製膚積鏇壓鹹簾遞憲(壓鏇鏇選鏇醖鑰壓窪蓋) = 簾製蓋製夢糧遞積選鬱 築醖糧簾顧網蓋製鏇膚 (壓遞壓築廠壓鏇鹹願衊 ) 更多 | 不佳 | 2018-06-01 | |||
Placebo | 窪製膚積鏇壓鹹簾遞憲(壓鏇鏇選鏇醖鑰壓窪蓋) = 壓遞衊繭鑰鹽觸膚鏇齋 築醖糧簾顧網蓋製鏇膚 (壓遞壓築廠壓鏇鹹願衊 ) 更多 | ||||||
临床2期 | 结直肠癌 CA19-9 | sLe x | 128 | 願餘鹹遞餘製遞鬱糧蓋(鹽艱夢鑰壓鹹積製獵糧) = 觸憲築鹹範襯糧餘膚壓 淵觸願鏇繭築製蓋網齋 (憲糧築願獵餘齋憲築鹽 ) | 积极 | 2015-07-01 | ||
Placebo | 願餘鹹遞餘製遞鬱糧蓋(鹽艱夢鑰壓鹹積製獵糧) = 糧憲衊遞繭壓構鑰願蓋 淵觸願鏇繭築製蓋網齋 (憲糧築願獵餘齋憲築鹽 ) | ||||||
临床2期 | 128 | 遞壓製網觸鬱襯範製齋(衊艱願網範積膚鹽網鑰) = 願窪襯餘窪範蓋顧網鹹 糧餘鑰築廠鹹壓襯鑰窪 (築夢壓繭範積範夢糧積 ) | - | 2015-05-20 | |||
Placebo | 遞壓製網觸鬱襯範製齋(衊艱願網範積膚鹽網鑰) = 艱憲餘鬱製餘遞觸遞簾 糧餘鑰築廠鹹壓襯鑰窪 (築夢壓繭範積範夢糧積 ) | ||||||
临床2期 | 30 | 餘廠鏇鏇構淵選鬱選夢(憲蓋鬱膚範觸艱觸選糧) = 製蓋構觸構艱獵築積鹽 蓋鏇繭鹽願獵夢網衊願 (鏇淵膚夢積醖範鬱鹹顧, 艱壓衊窪鑰獵願鹹膚襯 ~ 鬱繭願鹹鏇齋積選範餘) 更多 | - | 2014-07-03 | |||
临床2期 | 123 | 顧遞鏇艱襯鬱繭鹹積廠(憲衊選憲廠繭鹽夢艱選) = 壓選窪衊鹽鏇窪願製襯 觸膚鏇網夢鹹艱艱獵窪 (廠壓襯繭顧繭醖網蓋遞 ) | - | 2014-01-20 |
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