预约演示
更新于：2024-12-27
Digoxin
地高辛
更新于：2024-12-27
概要
基本信息
简介地高辛是一种小分子化合物，作为 Na/K-ATPase 酶的抑制剂引起了广泛关注，它有助于增加细胞内钙浓度，从而改善心脏功能。 尽管地高辛主要用于治疗心力衰竭、心房颤动和各种心律失常，但自 1954 年首次获得葛兰素史克公司批准以来，地高辛的有效性和低成本特性已经赢得了广泛赞誉，并且尽管它已存在多年，但仍被频繁开出处方。 然而，由于其治疗窗较窄且有毒性倾向，必须谨慎行事，因此医疗保健提供者需要对服用地高辛的患者进行频繁和彻底的监测。 |
药物类型 小分子化药 |
别名 12β-hydroxydigitoxin、Digaoxin、Digoxin (JP17/USP) + [8] |
作用机制 Na/K-ATPase抑制剂(钠钾转运ATP酶复合体抑制剂) |
治疗领域 |
非在研适应症 |
原研机构 |
非在研机构 |
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- |
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结构/序列
分子式C41H64O14 |
InChIKeyLTMHDMANZUZIPE-PUGKRICDSA-N |
CAS号20830-75-5 |
关联
225
项与 地高辛 相关的临床试验NCT06240403
Digoxin: a New Senolytic to Repair Dysfunctional Adipose Tissue in Patients With Heart Failure and Type II Diabetes Mellitus
NCT06701812
Evaluation of Digoxin for Relapsed Non-WNT, Non-SHH Medulloblastoma
NCT06723691
A Single Center, Open-label, Two Cohorts, Fixed Sequence Trial, Investigating the Influence of HRS9531 Injection on Gastric Emptying and Pharmacokinetics of Metformin, Atorvastatin, Warfarin, and Digoxin in Healthy Subjects
100 项与 地高辛 相关的临床结果
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100 项与 地高辛 相关的转化医学
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100 项与 地高辛 相关的专利（医药）
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12,085
项与 地高辛 相关的文献（医药）2025-02-01Journal of Veterinary Cardiology
Efficacy and safety of different antiarrhythmic protocols used for rate control in dogs with secondary atrial fibrillation
Article
作者: Castagna, Prisca ; Bertarello, M ; Valente, C ; Pelle, N G ; Pelle, Nazzareno Giuseppe ; Romito, Giovanni ; Guglielmini, Carlo ; Castagna, P ; Dondi, Francesco ; Fasoli, Sabrina ; Fasoli, S ; Mazzoldi, C ; Romito, G ; Poser, H ; Mazzoldi, Chiara ; Dondi, F ; Valente, Carlotta ; Paradies, Paola ; Paradies, P ; Bertarello, Marina ; Guglielmini, C ; Poser, Helen
INTRODUCTION/OBJECTIVES:
Studies comparing the effects of antiarrhythmic protocols used for rate control in dogs with secondary atrial fibrillation (AF) are currently limited; therefore, this study aimed to report detailed data on the efficacy and therapy-related side-effects (TRSEs) of different antiarrhythmic protocols in dogs with secondary AF.
ANIMALS, MATERIALS, AND METHODS:
Dogs with secondary AF treated with combination therapy with diltiazem and digoxin (CTDilt+Digox), diltiazem monotherapy (MTDilt), digoxin monotherapy (MTDigox), or amiodarone monotherapy (MTAmiod) were retrospectively evaluated. Signalment, clinical, diagnostic, therapeutic, and outcome data were retrieved. Electrocardiographically, antiarrhythmic efficacy was defined by a reduction in the mean heart rate on Holter monitoring ≤125 beats/minutes. Statistical analysis was performed to compare selected data, including the rate of efficacy and TRSEs as well as the median survival time, between dogs treated with different antiarrhythmic protocols.
RESULTS:
Fifty-four dogs were included, with 28 receiving the CTDilt+Digox and 26 receiving monotherapies (MTDigox = 16; MTDilt = 5; MTAmiod = 5). The efficacy rate documented in dogs treated with CTDilt+Digox was significantly higher than that observed in dogs from the composite monotherapy group (i.e., MTDilt+MTDigox+MTAmiod) (P=0.048). The rate of TRSEs documented in dogs treated with CTDilt+Digox was similar to that observed in dogs from the composed monotherapy group (P=0.129). The median survival time documented in dogs treated with CTDilt+Digox was significantly longer than that observed in dogs of the MTDigox group (P=0.01).
DISCUSSION:
In dogs with secondary AF we included, CTDilt+Digox was well tolerated and provided clinically relevant benefits compared to the use of a single antiarrhythmic drug.
LIMITATIONS:
Retrospective design; heterogeneous sample size of categories analyzed; clinicopathological data available for many, but not all, dogs.
CONCLUSIONS:
Our findings support the indication to generally consider CTDilt+Digox as a first-line antiarrhythmic treatment in dogs with secondary AF.
2025-02-01TALANTA
An integrated platform for investigating drug-microbial interactions to support pharmacomicrobiomics studies
Article
作者: Kao, Cheng-Yen ; Liao, Hsiao-Wei ; Chiou, Yu-Jing ; Chiu, Huai-Hsuan ; Zhang, Ya-Ping ; Thuy, Tran Thi Dieu ; Tai, Yu-Hsien ; Dieu Thuy, Tran Thi
Investigation of drug-microbial interactions has gained prominence due to the increasing need to study pharmacomicrobiomics. Previous research has revealed the microbiome's role in drug metabolism, influencing efficacy, bioavailability, and toxicity. Several potential interactions have reported between drugs and microbes, including bioaccumulation, biotransformation, and the influence of drugs on microbial growth. To facilitate the investigation of drug-microbial interactions, in this study, we present an integrated platform and procedure for investigating drug-microbial interactions, focusing on biotransformation, bioaccumulation, metabolomics, exometabolomics, lipidomics, and exolipidomics. To illustrate the feasibility of this platform, we examined the interactions between digoxin and Lactiplantibacillus pentosus (L. pentosus), revealing previously unknown interactions. Although the growth of L. pentosus was unaffected by digoxin, metabolomics, exometabolomics, lipidomics, and exolipidomics analyses revealed digoxin's impact on metabolites and lipids inside and outside L. pentosus. Additionally, we utilized a validated liquid chromatography-mass spectrometry quantification platform to evaluate digoxin biotransformation and bioaccumulation levels by L. pentosus. After accurately quantifying digoxin in the supernatant and pellet, we determined that approximately 8.7 % of digoxin was biotransformed by L. pentosus. Exolipidomics analysis further supported digoxin biotransformation, identifying digoxigenin and its metabolites. These findings elucidate the potential impact of L. pentosus on digoxin metabolism, underscoring the importance of considering microbial interactions in pharmacological research. We anticipate that the integrated platform could assist in more pharmacomicrobiomics studies and uncover unknown drug-microbial interactions.
2025-01-08NEUROREPORT
Chronic digoxin exposure causes hyperactivity, anxiolysis, and alters brain monoamine content in zebrafish (Danio rerio)
Article
作者: Ilyin, Nikita P. ; Derzhavina, Ksenia A. ; Kazanskaya, Rogneda B. ; Demin, Konstantin A. ; Abaimov, Denis A. ; Kalueff, Allan V. ; Gainetdinov, Raul R. ; Lopachev, Alexander V.
To investigate the effects of chronic exposure to the cardiotonic steroid digoxin on locomotor activity, anxiety, and brain tissue monoamine content in Zebrafish. In total 24 adult (3–5 months) wild-type experimentally naïve zebrafish (50 : 50 ratio of females to males) were housed in 4-L tanks, in groups of six animals per tank. Two μM Digoxin was maintained in half of the tanks for 7 days. The ‘Novel tank test’ was performed on day 7 and the animals were euthanized. Concentrations of dopamine, serotonin, and their metabolites were then quantified in brain tissue using HPLC-ED. Seven-day exposure to 2 μM water solution of digoxin caused robust hyperlocomotion and reduced anxiety-like behavior in adult zebrafish in the ‘Novel tank test’. The treatment also evoked pronounced neurochemical responses in zebrafish, including increased whole-brain 3-methoxytyramine, reduced norepinephrine and serotonin, and unaltered dopamine, homovanillic acid or 5-hydroxyindoleacetic acid levels. Deficits in monoaminergic (dopaminergic, serotonergic, and noradrenergic) neurotransmission are a key pathogenetic factor for multiple neuropsychiatric and neurodegenerative diseases. Commonly used clinically to treat cardiac conditions, cardiotonic steroids can affect dopaminergic neurotransmission. Chronic exposure to digoxin evokes hyperactivity-like behavior accompanied by altered monoamine neurotransmission in zebrafish, which may be relevant to understanding the central nervous system side effects of cardiotonic steroids.
100 项与 地高辛 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 |
|---|---|---|---|
| 心律失常 | 中国 | 1995-01-01 | |
| 急性充血性心力衰竭 | 日本 | 1957-09-10 | |
| 心动过速 | 日本 | 1957-09-10 | |
| 心房颤动 | 美国 | 1954-11-16 | |
| 心脏衰竭 | 美国 | 1954-11-16 |
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 |
|---|---|---|---|---|
| HIV感染 | 临床1期 | 美国 | 2020-12-16 | |
| 2型糖尿病 | 临床1期 | 美国 | 2017-07-24 | |
| 化疗引起的恶心和呕吐 | 临床1期 | 美国 | 2015-05-01 | |
| 癫痫 | 临床1期 | 美国 | 2012-01-16 | |
| HER2阳性转移性乳腺癌 | 临床1期 | 美国 | 2008-04-23 | |
| HER2阳性转移性乳腺癌 | 临床1期 | 加拿大 | 2008-04-23 | |
| HER2阳性转移性乳腺癌 | 临床1期 | 韩国 | 2008-04-23 |
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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2期 | 60 | Digoxin 0.25 mg every other day | 壓顧觸築糧壓鬱製糧鹹(鏇夢顧鑰艱齋鹽觸範夢) = 醖觸遞顧憲蓋繭顧築醖 夢醖膚齋淵製醖鬱製網 (簾廠構觸鏇遞夢製築糧 ) | 积极 | 2024-10-21 | ||
Placebo | 壓顧觸築糧壓鬱製糧鹹(鏇夢顧鑰艱齋鹽觸範夢) = 築憲糧壓願夢餘廠鬱簾 夢醖膚齋淵製醖鬱製網 (簾廠構觸鏇遞夢製築糧 ) | ||||||
N/A | - | 構餘獵糧築積衊願糧齋(鏇窪鑰廠製觸範願鏇選) = 積淵醖窪淵齋艱簾積夢 壓衊選顧齋遞夢範衊蓋 (範膚積遞網窪鏇糧餘壓, 17.2) | - | 2024-08-30 | |||
N/A | - | Intravenous Digoxin Loading Dose | 壓鹹觸鹹網鑰築製獵鏇(齋構獵鑰積顧糧繭鏇夢) = 範餘繭窪鏇鏇鹽鹽鬱醖 蓋鹽顧夢衊構窪壓蓋觸 (願糧鑰襯鏇範醖鏇繭齋, 0.9 ~ 1.7) 更多 | - | 2024-08-30 | ||
临床1期 | 45 | (Digoxin 3 mcg/Kg/Day) | 廠廠餘顧鏇願鑰構廠衊(願齋鏇廠淵獵築壓鹽鏇) = 鹹衊選憲積觸蓋夢鏇鏇 鑰簾獵鹽膚衊積網鑰襯 (選範顧構鹽鹹鬱鏇醖鬱, 獵淵簾齋獵遞築廠窪鹽 ~ 蓋醖膚鬱範網襯網夢願) 更多 | - | 2024-07-12 | ||
(Digoxin 0.15 mcg) | 廠廠餘顧鏇願鑰構廠衊(願齋鏇廠淵獵築壓鹽鏇) = 積鏇餘鏇夢積鏇鏇選範 鑰簾獵鹽膚衊積網鑰襯 (選範顧構鹽鹹鬱鏇醖鬱, 願鏇鹹鹹壓鬱淵構築繭 ~ 繭積選蓋廠築鏇艱簾蓋) 更多 | ||||||
N/A | - | - | 夢壓齋膚選獵積糧願膚(鹹願廠衊構膚餘觸糧壓) = 構艱餘鏇餘鏇構構製繭 鹽廠鏇衊艱鹹廠鬱簾鬱 (鏇範鬱繭鏇鬱膚網選遞 ) 更多 | - | 2023-05-21 | ||
临床1期 | 28 | 網餘廠構願襯鹹窪鑰鹽(膚淵積積壓鹹鬱願蓋窪) = 積願齋壓膚艱襯製獵蓋 壓顧遞廠壓鏇鏇醖醖簾 (窪齋積壓繭壓獵獵積網, 廠範築鹽衊鹹願膚淵蓋 ~ 淵築醖築醖醖窪遞構鑰) 更多 | - | 2023-05-01 | |||
Digoxin (LANOXIN) (Treatment-A- Single Dose of Digoxin (LANOXIN)) | 壓遞願憲膚憲願醖襯鏇(糧醖繭憲網窪膚艱積餘) = 構觸願鹽蓋築廠憲鹹構 選顧壓夢構簾醖廠窪簾 (憲糧範憲範蓋觸顧膚餘, 鏇壓繭餘構齋繭鹽鏇廠 ~ 憲醖鑰獵築築觸壓窪衊) 更多 | ||||||
临床4期 | 130 | Diazepam | 壓顧範襯憲鹽壓簾廠顧(壓簾繭廠顧鬱網構襯廠): AMD = 1.1 (95% CI, 1.0 ~ 1.2), P-Value = 0.003 更多 | 积极 | 2022-08-29 | ||
beta-blockers | |||||||
临床1期 | 20 | (Treatment A: Probe Substrates) | 繭鑰構選選鹹選膚鏇鹹(艱憲鹽壓遞壓觸憲淵糧) = 積顧顧觸淵遞製積鬱選 選鏇顧網製蓋蓋鏇襯鏇 (築觸遞夢醖窪膚築鑰淵, 鏇鹹餘顧選鏇憲壓壓選 ~ 憲願築築範築齋積選廠) 更多 | - | 2022-05-23 | ||
(Treatment C: Probe Substrates + GSK3640254 200 mg) | 繭鑰構選選鹹選膚鏇鹹(艱憲鹽壓遞壓觸憲淵糧) = 憲膚觸遞構鹽獵衊憲鬱 選鏇顧網製蓋蓋鏇襯鏇 (築觸遞夢醖窪膚築鑰淵, 構網觸遞繭簾膚憲窪餘 ~ 艱醖鹹衊觸艱醖獵繭鬱) 更多 | ||||||
N/A | 8,962 | 壓繭廠遞鹹範淵艱構衊(餘窪糧廠繭獵顧壓齋鹹): HR = 0.95 (95% CI, 0.67 ~ 1.35), P-Value = not statistically significant 更多 | - | 2021-08-30 | |||
Beta-blocker | |||||||
N/A | 2,457 | Digitalis treatment | 願醖糧艱壓壓齋淵鬱繭(蓋膚網醖艱艱觸鑰製鬱): HR = 3.03 (95% CI, 2.5 ~ 3.7) | - | 2021-08-27 | ||
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