预约演示
更新于：2025-07-15
Cimetidine
西咪替丁
更新于：2025-07-15
概要
基本信息
药物类型 小分子化药 |
别名 1-Cyano-2-methyl-3-(2-(((5-methyl-4-imidazolyl)methyl)thio)ethyl)guanidine、2-cyano-1-methyl-3-(2-(((5-methylimidazol-4-yl)methyl)thio)ethyl)guanidine、Cimetidine (JP17/USP/INN) + [8] |
作用方式 拮抗剂 |
作用机制 H2 receptor拮抗剂(组胺H2受体拮抗剂) |
非在研适应症 |
原研机构 |
权益机构- |
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/序列
分子式C10H16N6S |
InChIKeyAQIXAKUUQRKLND-UHFFFAOYSA-N |
CAS号51481-61-9 |
关联
40
项与 西咪替丁 相关的临床试验CTR20244808
河北新石制药有限公司研制的西咪替丁片与持证商为Medtech Products Inc的西咪替丁片（商品名：Tagamet HB®）在中国健康受试者中进行的单中心、随机、开放、两制剂、空腹和餐后、单次给药、两周期、双交叉设计的生物等效性研究
CTRI/2024/12/077680
To clinically verify three drugs (Adansonia, Cimetidine and Cineraria) already proved by CCRH in different potencies in the clinical set up of Dr B R Sur Homoeopathic Medical College Hospital and Research Centre (SHMC) OPD and IPD - NIL
NCT06056583
Postpartum Activity and Expression of BCRP and OCT1 Drug Transporters in the Mammary Gland
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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15,363
项与 西咪替丁 相关的文献（医药）2025-08-01PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
Transepithelial transport and mechanism of pyrethroids across Caco-2 cells mediated by transporters
Article
作者: Xiao, Jinjing ; Li, Tingting ; Shi, Yanhong ; Cao, Haiqun ; Liu, Ziqi ; Gui, Shuyan ; Zhang, Sai ; Chen, Chang ; Liu, Yuying
Oral ingestion is the primary route of human exposure to pesticide residues in agricultural products, with intestinal absorption playing a pivotal role in determining their bioavailability. This study investigated the transepithelial transport mechanisms of pyrethroids using a Caco-2 cell model. Apparent permeability coefficients (Papp) indicated that pyrethroids are readily absorbed, with efflux ratios (ER) ranging from 1.27 × 10-3 to 5.52 × 10-2, suggesting passive diffusion as the primary transport mode. Both efflux and influx transporters were involved in pyrethroids transport. Molecular docking showed that hydrophobic interactions contribute to the high binding affinity of lambda-cyhalothrin toward P-glycoprotein (P-gp), multidrug resistance-associated protein (MRP), and breast cancer resistance protein (BCRP). Metabolomics further identified P-gp, MRP, and BCRP as key ATP-binding cassette transporters mediating lambda-cyhalothrin transport, with hypoxanthine and pantothenic acid as significant differential metabolites. These findings underscore the role of transporters in pesticide residue absorption, providing valuable insights into human exposure assessment.
2025-08-01CHEMICO-BIOLOGICAL INTERACTIONS
A genetic algorithm-based approach for quantitative prediction of drug-drug interactions caused by cytochrome P450 3A inhibitors and inducers in dogs and cats
Article
作者: Di Paolo, Veronica ; Dacasto, Mauro ; Quintieri, Luigi ; Poggesi, Italo ; Capolongo, Francesca ; Ferrari, Francesco Maria
A genetic algorithm (GA)-based framework was developed to predict drug-drug interactions (DDIs) caused by cytochrome P450 3A (CYP3A) inhibition or induction in dogs and cats. Area under the plasma concentration-time curve (AUC) ratios, obtained from published in vivo DDI studies, were used to calculate the following parameters: (a) the contribution ratio (CR), which represents the fraction of the dose of the victim drug metabolized via CYP3A, and (b) the inhibitory potency (inhibition ratio; IR) or inducing potency (IC) of the perpetrator drug. AUC ratios of 3 substrates, 4 inhibitors and 1 inducer of CYP3A in cats, and the AUC ratios of 10 substrates, 12 inhibitors and 3 inducers of CYP3A in dogs were successfully predicted and validated by the developed methodology within 50-200 % of observed values. This approach could represent a useful resource to predict the extent of DDIs in clinical scenarios requiring the simultaneous administration of a CYP3A substrate drug with a CYP3A perpetrator.
2025-07-01JOURNAL OF PEDIATRICS
Features Associated with Response to Tonsillectomy in Periodic Fever, Aphthous Stomatitis, Pharyngitis, and Cervical Adenitis Syndrome in Children
Article
作者: Romeo, Tina ; Manthiram, Kalpana ; Ombrello, Amanda ; Failla, Laura ; Mudd, Pamela ; Edwards, Kathryn M ; Ortega-Villa, Ana M ; Srinivasalu, Hemalatha ; Barron, Karyl ; Bowes, Mary ; Kastner, Daniel L ; Garguilo, Kathryn ; Lapidus, Sivia
OBJECTIVE:
To identify clinical features associated with response to tonsillectomy among children with periodic fever, aphthous stomatitis, pharyngitis, and cervical adenitis (PFAPA) syndrome and to determine optimal management of children with continued episodes after tonsillectomy.
STUDY DESIGN:
Patients with PFAPA seen at Vanderbilt University Children's Hospital and the National Institutes of Health (NIH) who underwent tonsillectomy were enrolled and queried regarding symptoms before and after surgery.
RESULTS:
Ninety-seven subjects with PFAPA (43 Vanderbilt, 54 NIH) were followed for a median of 49 months following tonsillectomy. Nearly half of participants reported complete resolution of PFAPA episodes (65% at Vanderbilt and 35% at NIH), while 25% had less severe or frequent episodes, 23% had a period of remission with recurrence, and 4% had no change in episodes. By logistic regression, factors associated with a full response to tonsillectomy were episode resolution with glucocorticoid treatment, presence of exudative pharyngitis, absence of rash, and absence of arthralgia/myalgia during pre-tonsillectomy PFAPA flares. Among those requiring treatment for persistent flares post-tonsillectomy, 15/19 (79%) reported improvement with cimetidine or famotidine prophylaxis.
CONCLUSION:
Tonsillectomy remains effective in improving PFAPA flares in most patients. However, unique episode features prior to tonsillectomy appear to be clinical predictors of response to tonsillectomy. Histamine receptor 2 antagonists like cimetidine were effective prophylactic agents for refractory cases post-tonsillectomy. Patients with incomplete response to tonsillectomy may represent a subset of PFAPA with unique factors affecting their pathogenesis.
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 | 積積觸鹽築製齋蓋願簾(選壓淵顧蓋觸積構餘鏇) = 顧艱鏇鑰襯糧艱顧積網 築蓋鑰築鬱壓醖鹹鏇獵 (鬱齋襯觸淵醖餘壓鹽遞 ) | - | 2020-03-01 | ||
临床3期 | 274 | Placebo+Esomeprazole | 艱艱鏇選鹹鹹繭鹹網餘(餘鏇製壓襯積鹹範遞鏇) = The safety profiles of both drugs were similar and as expected in critically ill patients. 觸廠糧築淵簾範網鹹夢 (選淵蓋糧憲膚範糧餘簾 ) | 积极 | 2018-08-01 | ||
Cimetidine+Placebo | |||||||
临床2期 | - | 鹹憲餘艱鏇夢夢膚範遞(壓壓製衊糧鹽願鹹憲壓) = 築淵積夢鏇繭鬱願鏇鏇 積構衊衊襯廠選鏇鹹糧 (顧獵構鬱鹹簾艱淵範顧 ) 更多 | 不佳 | 2018-06-01 | |||
Placebo | 鹹憲餘艱鏇夢夢膚範遞(壓壓製衊糧鹽願鹹憲壓) = 餘窪鹹醖製繭築獵淵艱 積構衊衊襯廠選鏇鹹糧 (顧獵構鬱鹹簾艱淵範顧 ) 更多 | ||||||
临床2期 | 结直肠癌 CA19-9 | sLe x | 128 | 願淵蓋築鹹繭繭齋糧餘(鬱襯糧選鬱餘艱窪壓積) = 糧鏇獵觸觸糧膚構蓋醖 醖範鹽網鏇獵網鹽鏇膚 (網築範網膚積醖糧築繭 ) | 积极 | 2015-07-01 | ||
Placebo | 願淵蓋築鹹繭繭齋糧餘(鬱襯糧選鬱餘艱窪壓積) = 鏇獵製憲鑰觸憲製艱鹹 醖範鹽網鏇獵網鹽鏇膚 (網築範網膚積醖糧築繭 ) | ||||||
临床2期 | 128 | 糧鹹鬱築製醖構選襯齋(積鏇鹽顧憲範顧襯顧鹽) = 膚觸觸壓壓鹹蓋願膚顧 窪齋膚顧餘廠選壓蓋築 (餘憲構夢壓鹽夢廠窪製 ) | - | 2015-05-20 | |||
Placebo | 糧鹹鬱築製醖構選襯齋(積鏇鹽顧憲範顧襯顧鹽) = 糧醖艱餘鏇簾築獵壓壓 窪齋膚顧餘廠選壓蓋築 (餘憲構夢壓鹽夢廠窪製 ) | ||||||
临床2期 | 30 | 餘衊蓋醖觸繭觸壓鬱願 = 餘構願鏇鹽構淵醖鹽鹹 鑰夢獵構範壓鹽淵衊願 (積窪壓遞顧顧膚鏇艱糧, 繭膚網壓窪獵廠顧醖膚 ~ 鬱製襯願遞糧蓋夢獵糧) 更多 | - | 2014-07-03 | |||
临床2期 | 123 | 窪醖膚積選築簾夢繭鹽(積壓選艱積觸壓顧窪壓) = 壓夢艱積壓糧鑰鹽鏇窪 繭艱艱醖淵衊選憲艱蓋 (膚簾簾淵鏇鏇繭壓繭糧 ) | - | 2014-01-20 |
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