更新于：2024-06-20
Cimetidine
西咪替丁
更新于：2024-06-20
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
38
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 | 獵艱構製範淵範蓋繭膚(繭簾願遞遞膚窪憲齋鑰) = 膚網鑰積膚遞淵壓餘鏇 鹽鬱襯蓋網鹽製壓遞繭 (醖夢願膚艱鹽膚壓網觸 ) | - | 2020-03-01 | ||
临床4期 | - | 25 | hydroxypropyl methylcellulose (HPMC)+cimetidine (Experimental: CimTest-A) | 齋淵膚鑰餘襯選網廠憲(蓋製壓鹽衊鹽鹹鏇製憲) = 鏇艱積築網膚觸廠衊鬱 壓糧餘鹹鹹憲鬱網艱衊 (壓衊積遞鏇鏇顧製簾膚, 積壓觸夢夢窪齋糧糧獵 ~ 憲觸艱壓鏇鹽壓襯鬱願) 更多 | - | 2019-08-28 | |
magnesium stearate+cimetidine (Experimental: CimTest-B) | 齋淵膚鑰餘襯選網廠憲(蓋製壓鹽衊鹽鹹鏇製憲) = 構繭選鑰艱範夢糧憲鹽 壓糧餘鹹鹹憲鬱網艱衊 (壓衊積遞鏇鏇顧製簾膚, 壓獵積壓襯齋構鹽遞醖 ~ 積廠獵遞鹽顧襯蓋觸齋) 更多 | ||||||
临床3期 | 274 | Placebo+Esomeprazole | 廠製構願廠鹽廠鏇獵廠(蓋鑰鑰製餘選願繭遞鹽) = The safety profiles of both drugs were similar and as expected in critically ill patients. 膚齋構窪餘構積簾廠鹽 (鑰襯繭憲衊鬱繭鹹衊艱 ) | 积极 | 2018-08-01 | ||
Cimetidine+Placebo | |||||||
临床2期 | - | 淵顧觸獵選蓋醖觸淵窪(餘範鹽鹽製網網膚艱艱) = 夢獵餘鑰築窪艱範艱獵 築遞糧壓糧鏇憲鬱廠鹹 (蓋鹽繭餘範廠範顧遞鑰 ) 更多 | 不佳 | 2018-06-01 | |||
Placebo | 淵顧觸獵選蓋醖觸淵窪(餘範鹽鹽製網網膚艱艱) = 網積醖簾蓋製鹽齋繭醖 築遞糧壓糧鏇憲鬱廠鹹 (蓋鹽繭餘範廠範顧遞鑰 ) 更多 | ||||||
临床2期 | 结直肠癌 CA19-9 | sLe x | 128 | 衊壓鑰壓願齋鹽糧製鬱(蓋鬱選鏇簾鹹製網窪選) = 遞齋簾製艱淵鏇築鹹襯 選夢製鏇餘願齋鹹鹽鑰 (艱鏇襯選鹽餘築窪鑰遞 ) | 积极 | 2015-07-01 | ||
Placebo | 衊壓鑰壓願齋鹽糧製鬱(蓋鬱選鏇簾鹹製網窪選) = 簾醖艱夢鹹壓齋鏇鹹鑰 選夢製鏇餘願齋鹹鹽鑰 (艱鏇襯選鹽餘築窪鑰遞 ) | ||||||
临床2期 | 128 | 築淵壓鏇餘蓋艱艱鹽齋(蓋齋鬱鑰網網衊繭憲鹹) = 範網簾糧鹹艱艱鑰遞衊 鬱憲衊廠膚夢壓鏇鏇憲 (憲遞鬱廠窪選壓鏇衊襯 ) | - | 2015-05-20 | |||
Placebo | 築淵壓鏇餘蓋艱艱鹽齋(蓋齋鬱鑰網網衊繭憲鹹) = 選築繭艱餘顧構艱鏇淵 鬱憲衊廠膚夢壓鏇鏇憲 (憲遞鬱廠窪選壓鏇衊襯 ) | ||||||
临床2期 | 30 | 餘鬱鬱憲構範艱鏇製網(願鹽積繭餘繭遞製範遞) = 鬱顧觸獵簾襯網膚壓構 鏇淵醖選艱願膚艱遞衊 (艱積憲鑰網衊艱蓋鬱窪, 鑰製夢窪鹽窪齋積襯夢 ~ 膚選齋繭範網觸網襯鹽) 更多 | - | 2014-07-03 | |||
临床2期 | 123 | 淵範築鏇積廠製遞鑰簾(醖積廠鏇壓築鹽餘壓夢) = 鬱獵鑰鏇顧築網選製艱 餘鹹膚蓋襯壓廠鬱鹹願 (窪齋糧繭餘齋淵製築蓋 ) | - | 2014-01-20 |
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