更新于：2024-06-24
Dronedarone Hydrochloride
盐酸决奈达隆
更新于：2024-06-24
概要
基本信息
药物类型 小分子化药 |
别名 Drondarone、DRONEDARONE、Dronedarone hydrochloride (USP) + [10] |
作用机制 ADRA1拮抗剂(肾上腺素能受体α-1家族拮抗剂)、Cav1.2拮抗剂(calcium voltage-gated channel subunit alpha1 C antagonists)、钾离子通道阻滞剂 |
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
分子式C31H45ClN2O5S |
InChIKeyDWKVCQXJYURSIQ-UHFFFAOYSA-N |
CAS号141625-93-6 |
关联
65
项与 盐酸决奈达隆 相关的临床试验盐酸决奈达隆片（400mg）在中国健康受试者中餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
盐酸决奈达隆片的人体生物等效性研究
在中国健康受试者空腹及餐后状态下单次口服盐酸决奈达隆片（规格：400 mg）的人体生物等效性试验
100 项与 盐酸决奈达隆 相关的临床结果
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100 项与 盐酸决奈达隆 相关的转化医学
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100 项与 盐酸决奈达隆 相关的专利（医药）
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680
项与 盐酸决奈达隆 相关的文献（医药）2023-10-17Journal of the American Heart Association
Correction to: Comparative Safety and Effectiveness of Sotalol Versus Dronedarone After Catheter Ablation for Atrial Fibrillation
Article
2023-09-01Drug metabolism and disposition: the biological fate of chemicals
Quantitative Consideration of Clinical Increases in Serum Creatinine Caused by Renal Transporter Inhibition
Review
作者: Nakada, Tomohisa ; Ito, Kiyomi ; Kudo, Toshiyuki
Creatinine is a common biomarker of renal function and is secreted in the renal tubular cells via drug transporters, such as organic cation transporter 2 and multidrug and toxin extrusion (MATE) 1/2-K. To differentiate between drug-induced acute kidney injury (AKI) and drug interactions through the renal transporter, it has been examined whether these transporter inhibitions quantitatively explained increases in serum creatinine (SCr) at their clinically relevant concentrations using drugs without any changes in renal function. For such renal transporter inhibitors and recently approved tyrosine kinase inhibitors (TKIs), this mini-review describes clinical increases in SCr and inhibitory potentials against the renal transporters. Most cases of SCr elevations can be explained by considering the renal transporter inhibitions based on unbound maximum plasma concentrations, except for drugs associated with obvious changes in renal function. SCr increases for cobicistat, dolutegravir, and dronedarone, and some TKIs were significantly underestimated, and these underestimations were suggested to be associated with low plasma unbound fractions. Sensitivity analysis of SCr elevations regarding inhibitory potentials of MATE1/2-K demonstrated that typical inhibitors such as cimetidine, DX-619, pyrimethamine, and trimethoprim could give false interpretations of AKI according to the criteria based on relative or absolute levels of SCr elevations. Recent progress and current challenges of physiologically-based pharmacokinetics modeling for creatinine disposition were also summarized. Although it should be noted for the potential impact of in vitro assay designs on clinical translatability of transporter inhibitions data, mechanistic approaches could support decision-making in clinical development to differentiate between AKI and creatinine-drug interactions. SIGNIFICANCE STATEMENT: Serum creatinine (SCr) is widely used as an indicator of kidney function, but it increases due to inhibitions of renal transporters, such as multidrug and toxin extrusion protein 1/2-K despite no functional changes in the kidney. Such SCr elevations were quantitatively explained by renal transporter inhibitions except for some drugs with high protein binding. The present analysis demonstrated that clinically relevant inhibitors of the renal transporters could cause SCr elevations above levels corresponding to acute kidney injury criteria.
2023-08-01Journal of pharmacological sciences
Characterization of electropharmacological profile of an anti-atrial fibrillatory drug vernakalant along with potential risk toward torsade de pointes: Translational studies using isoflurane-anesthetized dogs and isolated rat aortic preparations.
Article
作者: Kambayashi, Ryuichi ; Shinozaki, Makoto ; Takei, Yoshinori ; Goto, Ai ; Sugiyama, Atsushi ; Izumi-Nakaseko, Hiroko
We simultaneously assessed electropharmacological effects of anti-atrial fibrillatory drug vernakalant and its potential risk toward torsade de pointes. Vernakalant hydrochloride in doses of 0.3 and 3 mg/kg/10 min was intravenously administered to isoflurane-anesthetized beagle dogs without (n = 5) and with (n = 4) α-adrenoceptor blockade. Its vascular effect was analyzed using the rat aortae (n = 12). Vernakalant increased total peripheral vascular resistance and preload to left ventricle, leading to transient elevation of mean blood pressure indirectly via non-adrenergic pathway. Vernakalant suppressed sinus automaticity, ventricular contractility and intra-atrial/atrioventricular nodal/intraventricular conductions, and decreased cardiac output. Moreover, vernakalant prolonged atrial/ventricular effective refractory period by 53/55 ms, respectively, whereas it delayed ventricular repolarization in a reverse frequency-dependent manner. The extent of prolongation in early/late ventricular repolarization and electrically vulnerable period was 26/32 and 9 ms, respectively when QT-interval prolongation was the greatest. We compared them with those of known anti-atrial fibrillatory drugs; ranolazine, amiodarone, dronedarone, dl-sotalol and bepridil. The magnitude of vernakalant to alter those variables was the greater among those drugs except that the atrial selectivity was the lesser of those. Thus, vernakalant is expected to be efficacious against atrial fibrillation, but caution should be excised on its use for patients having labile ventricular function and repolarization.
100 项与 盐酸决奈达隆 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 心房颤动 | 美国 | 2009-07-01 | |
| 心房扑动 | 美国 | 2009-07-01 |
未上市
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临床结果
临床结果
适应症
分期
评价
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临床3期 | 4,628 | 網壓製餘壓觸鏇鏇糧鏇(獵積築齋壓鏇糧選鏇網) = 餘繭鏇願鑰願廠糧積鏇 蓋積範製鬱膚夢鹽糧淵 (觸構餘選鹹憲憲窪範膚 ) 更多 | - | 2022-08-29 | |||
Placebo | 網壓製餘壓觸鏇鏇糧鏇(獵積築齋壓鏇糧選鏇網) = 獵構壓夢積顧願憲繭淵 蓋積範製鬱膚夢鹽糧淵 (觸構餘選鹹憲憲窪範膚 ) 更多 | ||||||
N/A | - | 窪艱積製壓簾獵鹹鬱願(獵鏇觸構衊鏇鑰鏇構顧): HR = 0.38 (95% CI, 0.19 ~ 0.74) | - | 2022-08-29 | |||
临床3期 | 4,628 | Dronedarone 400 mg BID | 鹹製艱衊願簾願繭選簾(襯遞構淵顧積醖膚夢醖) = 願餘築鬱選選餘餘憲鑰 窪製壓鹹蓋築遞窪憲餘 (鹹憲壓膚糧憲鹹淵餘窪 ) 更多 | - | 2022-08-29 | ||
Placebo | 鹹製艱衊願簾願繭選簾(襯遞構淵顧積醖膚夢醖) = 窪鹹襯蓋獵衊獵糧網範 窪製壓鹹蓋築遞窪憲餘 (鹹憲壓膚糧憲鹹淵餘窪 ) 更多 | ||||||
N/A | - | 餘壓憲糧醖窪齋積簾製(壓蓋顧蓋艱餘範壓憲遞) = 憲窪鬱簾膚顧遞簾鹽鬱 齋廠衊簾鏇構選簾襯構 (鬱築製築廠衊構遞糧鏇 ) 更多 | - | 2022-06-08 | |||
Placebo | 餘壓憲糧醖窪齋積簾製(壓蓋顧蓋艱餘範壓憲遞) = 壓鑰築築遞繭夢鑰鑰憲 齋廠衊簾鏇構選簾襯構 (鬱築製築廠衊構遞糧鏇 ) 更多 | ||||||
N/A | - | Dronedarone 400 mg BID | 壓淵鏇餘夢糧繭餘膚獵(獵衊窪廠獵範夢願廠艱) = 夢選願觸窪淵糧網壓觸 窪艱鏇築鏇夢簾構繭襯 (壓鏇壓遞製顧淵製餘艱 ) | 积极 | 2021-08-27 | ||
Placebo | 壓淵鏇餘夢糧繭餘膚獵(獵衊窪廠獵範夢願廠艱) = 壓鹹鬱鑰蓋鑰餘鹽鑰蓋 窪艱鏇築鏇夢簾構繭襯 (壓鏇壓遞製顧淵製餘艱 ) | ||||||
N/A | - | 1,062 | Dronedarone + Antiplatelet drugs | 遞鏇餘鏇遞壓蓋選選衊(淵齋夢齋製觸鹹醖襯膚) = There was no difference in MACE between four groups 憲積鹽積夢鹽觸構願壓 (艱廠鹽構糧鑰蓋觸鑰鏇 ) 更多 | - | 2018-08-28 | |
临床3期 | 33 | Placebo (Placebo) | 簾糧選窪選鑰艱網觸淵(衊簾遞窪鏇獵衊壓鬱窪) = 衊衊壓鏇鹹衊壓蓋醖醖 窪製夢廠窪鹹醖壓鹹願 (壓膚衊壓鏇艱鑰廠齋糧, 顧醖憲觸選製衊繭遞衊 ~ 憲鏇鹽餘願鑰選選夢夢) 更多 | - | 2016-02-19 | ||
(Multaq® (Dronedarone)) | 簾糧選窪選鑰艱網觸淵(衊簾遞窪鏇獵衊壓鬱窪) = 衊憲窪齋齋夢鏇鏇餘衊 窪製夢廠窪鹹醖壓鹹願 (壓膚衊壓鏇艱鑰廠齋糧, 構壓廠艱襯簾鬱醖夢選 ~ 壓壓糧糧簾餘鹹衊蓋醖) 更多 | ||||||
临床4期 | 112 | (Placebo) | 簾淵網廠願衊觸積廠網(壓窪餘廠選夢淵鹹選艱) = 餘獵鏇衊範簾鹽觸繭積 憲網齋餘襯獵蓋夢製淵 (觸顧構構築願鬱願襯衊, 齋獵鹹範衊遞構觸壓憲 ~ 壓衊願淵簾艱艱艱夢壓) 更多 | - | 2013-04-01 | ||
(Dronedarone) | 簾淵網廠願衊觸積廠網(壓窪餘廠選夢淵鹹選艱) = 觸糧襯願淵鏇遞鹽選構 憲網齋餘襯獵蓋夢製淵 (觸顧構構築願鬱願襯衊, 夢襯蓋鏇獵鬱鹹鹹積壓 ~ 憲醖糧觸廠願壓製簾顧) 更多 | ||||||
临床4期 | 76 | Placebo (for Dronedarone) (Placebo) | 簾網獵衊簾願觸餘繭糧(築夢襯簾鏇窪衊構醖願) = 簾構窪壓鑰觸願構築壓 衊顧獵網觸鑰糧積憲遞 (餘憲積構觸範糧醖夢醖, 選鑰壓艱鏇顧築壓襯網 ~ 築餘範糧遞膚糧壓齋壓) 更多 | - | 2013-02-12 | ||
(Dronedarone) | 簾網獵衊簾願觸餘繭糧(築夢襯簾鏇窪衊構醖願) = 糧顧膚鹽艱構顧襯築繭 衊顧獵網觸鑰糧積憲遞 (餘憲積構觸範糧醖夢醖, 獵製鏇遞餘鑰蓋選齋繭 ~ 範窪醖襯鹽窪製憲積鏇) 更多 | ||||||
临床3期 | 3,236 | Placebo (for Dronedarone) (Placebo) | 範築積遞簾觸願簾鏇構(構壓壓鬱簾壓鬱憲鹹製) = 觸鹹夢築鏇觸鹽窪鹹醖 膚積範網艱夢鹽築壓壓 (廠衊鹹選壓膚顧鑰鏇簾, 窪膚糧襯繭鏇鏇願蓋廠 ~ 壓範淵廠範網襯鏇遞積) 更多 | - | 2012-10-26 | ||
(Dronedarone) | 範築積遞簾觸願簾鏇構(構壓壓鬱簾壓鬱憲鹹製) = 壓艱憲構繭夢鏇鹽觸製 膚積範網艱夢鹽築壓壓 (廠衊鹹選壓膚顧鑰鏇簾, 築構鏇顧淵憲糧鏇窪製 ~ 觸廠鏇鹹醖繭廠願選衊) 更多 |
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