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更新于：2026-08-21
Atropine Sulfate
硫酸阿托品
更新于：2026-08-21
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C34H50N2O11S |
InChIKeyJPKKQJKQTPNWTR-CHYDPLAESA-N |
CAS号5908-99-6 |
关联
463
项与 硫酸阿托品 相关的临床试验ChiCTR2600130157
A Prospective Self-controlled Study on the Immediate Effect of Single Administration of Different Concentrations of Atropine on Intractable Binocular Balance in Adults
NCT07367178
Phase II Study to Improve Sacituzumab Govitecan Tolerance With Atropine in Patients With Advanced Triple-Negative and Hormone Receptor-Positive/HER2-Negative Breast Cancer
PACTR202607792697862
Effect of Preoperative Dissociation Technique on Surgical Outcomes in Intermittent Exotropia: A Randomized Controlled Trial of Monocular Occlusion versus Atropine Penalization
100 项与 硫酸阿托品 相关的临床结果
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100 项与 硫酸阿托品 相关的转化医学
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100 项与 硫酸阿托品 相关的专利（医药）
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31,163
项与 硫酸阿托品 相关的文献（医药）2027-01-01JOURNAL OF ETHNOPHARMACOLOGY
Ethnopharmacological validation of Capparis spinosa L. in gastrointestinal and respiratory disorders: Evidence from in vitro, in vivo, and in silico models
Article
作者: Rana, Samia Latif ; Aleem, Ambreen
ETHNOPHARMACOLOGICAL RELEVANCE:
Capparis spinosa L. is traditionally used in Pakistan to treat gastrointestinal and respiratory ailments, yet its multi-target pharmacological mechanisms remain poorly understood.
AIM OF THE STUDY:
To evaluate the traditional use of Capparis spinosa L. in asthma, diarrhea, and spasm using integrated in vitro, in vivo, and in silico approaches.
METHODOLOGY:
Hydroethanolic extract of C. spinosa L. (Cap.Cr) was analyzed by LC ESI-MS/MS. Antispasmodic and bronchodilator activities of Cap.Cr and its fractions (Ethyl acetate, n-hexane, aqueous) were assessed using isolated jejunal segments from rabbit intestine, trachea, and urinary bladder. Antidiarrheal potential was assessed in mice using castor oil-induced diarrhea, enteropooling, and intestinal transit models. Rat fecal samples were analyzed via qRT-PCR to assess the presence of Firmicutes, Lactobacillus, and V2. Molecular docking explored interactions with calcium channels and muscarinic receptors.
RESULTS:
LC ESI-MS/MS study identified 26 bioactive flavonoids and alkaloids. In vitro, Cap.Cr and its fractions relaxed the contractions provoked by high K+ and carbachol (CCh) across all tissues. The extracts shifted the Ca2+ and carbachol cumulative response curves (CRCs), suggesting dicyclomine-like dual Ca2+ antagonistic and antimuscarinic mechanism. In vivo, C. spinosa (50-200 mg/kg) significantly (p < 0.05) lessened diarrheal episodes, fluid accumulation, and intestinal transit showing efficacy comparable to loperamide and atropine. Microbiota analysis indicated an increase in Firmicutes and Lactobacillus levels by C. spinosa. In silico docking suggested high binding affinities for muscarinic receptors (M3) and voltage-gated Ca2+ channels.
CONCLUSION:
C. spinosa L. exerts potent antispasmodic, bronchodilator, and antidiarrheal effects and may involve Ca2+ channel blockade and muscarinic antagonism, demonstrating pharmacological justification for its traditional use in gut and airway dysfunctions.
2026-10-01AMERICAN JOURNAL OF EMERGENCY MEDICINE
Recurrent bradycardia and hypotension after Oral Lacosamide during hospital boarding in the emergency department: A case report
Article
作者: Babineau, Matthew R ; Pope, Jennifer V ; Gorham, Jack W ; Wischmeyer, Jareth S
Lacosamide is a third-generation antiseizure medication that enhances slow inactivation of voltage-gated sodium channels. Although generally well tolerated, it has been associated with cardiac conduction abnormalities, most commonly in the setting of intravenous administration, overdose, or dose escalation. We report a case of a 79-year-old woman with a history of hypertension (treated with losartan and metoprolol), restless legs syndrome (treated with ropinirole), peripheral neuropathy, and seizure disorder who presented to the emergency department with several days of intermittent confusion and generalized weakness following a recent admission for seizure-like activity, during which lacosamide had been initiated. On arrival, she was afebrile with a heart rate of 74 beats per minute, blood pressure 165/88 mmHg, and oxygen saturation 98% on room air; she was oriented to person and year but not to place, which represented a change from her baseline. Initial laboratory evaluation, including complete blood count, comprehensive metabolic panel with normal renal and hepatic function, B12, and thyroid stimulating hormone, was unremarkable, and her admission electrocardiogram showed normal sinus rhythm with a PR interval of 208 ms. While boarding in the emergency department, she received her scheduled oral lacosamide 150 mg, and approximately two hours later was found unresponsive with a heart rate in the 30s and systolic blood pressure of 50 mmHg. She responded to atropine 1 mg IV and 50μg of epinephrine IV, with improvement of her vital signs and mental status. Six hours later, she received a second scheduled dose of lacosamide 150 mg along with her home medications, including metoprolol tartrate 50 mg, and again two hours later became minimally responsive with a heart rate of 49 beats per minute, blood pressure 64/32 mmHg, and a new first-degree atrioventricular block; she again responded to atropine. The second episode was more pronounced and associated with conduction delay not previously present. No seizure activity was observed during either episode. Lacosamide was discontinued, and the patient had no further bradycardic or hypotensive events. The reproducible temporal relationship between dosing and symptoms, along with resolution after medication cessation, supports a causal association. This case highlights that clinically significant cardiac adverse effects can occur with standard oral dosing of lacosamide, particularly in older adults and in the presence of other medications that affect cardiac conduction. Emergency physicians should maintain a high index of suspicion for medication-induced bradycardia and hypotension in patients receiving lacosamide. This case also underscores how hospital boarding can increase the risk of iatrogenic harm, as patients may receive routine medications in a high-acuity environment where evolving adverse effects can be more difficult to anticipate and detect.
2026-10-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Design, synthesis and evaluation of an uncharged broad spectrum quinoline-oxime hybrid for the reactivation of nerve agent-inhibited human acetylcholinesterase
Article
作者: Calas, André-Guilhem ; Nachon, Florian ; Rousseau, Catherine ; Weik, Martin ; De La Mora, Eugenio ; Dias, José ; Gastellier, Anne-Julie ; Coisne, Caroline ; Maryan-Instone, Alex ; Courageux, Charlotte ; Baati, Rachid ; De Sousa, Julien ; Dehouck, Marie-Pierre ; Hanak, Anne-Sophie ; Hachani, Johan ; Timperley, Christopher M ; Brown, Richard C D ; Gosselet, Fabien ; Landry, Christophe
Organophosphorus nerve agents exert their acute toxicity by irreversibly inhibiting acetylcholinesterase (AChE), yet currently deployed oxime reactivators exhibit limited efficacy in the central nervous system due to poor blood-brain barrier (BBB) penetration. Addressing this limitation remains a critical challenge in the treatment of nerve agent exposure. We report the design, synthesis, and evaluation of JDS364, an uncharged hybrid oxime reactivator combining a quinoline-based peripheral site ligand with a 3-hydroxypyridinealdoxime nucleophile. In vitro studies using human AChE inhibited by surrogates of G- and V-series nerve agents demonstrated that JDS364 possesses broad-spectrum reactivation activity, notably achieving a 300-fold increase in reactivation efficiency (kr2) over the clinical benchmark obidoxime against tabun-like inhibited hAChE. Evaluation in a human in vitro BBB co-culture model revealed that JDS364 exhibits high permeability, significantly outperforming clinically used quaternary oximes and exceeding the flux of earlier-generation uncharged hybrids. Ex vivo functional profiling studies in mice confirmed rapid systemic availability and significant protection against paraoxon challenge (Protective Index = 6.7 when combined with atropine), though a narrower therapeutic window was observed compared to clinical standards. X-ray crystallographic analysis of JDS364 bound to human AChE uncovered ligand-induced conformational plasticity, providing the first structural evidence of an opening of a "backdoor" via Tyr449 rearrangement in the 20 Å deep active site gorge. This confirms the hypothesis of enzyme "breathing" motions and validates alternative diffusion pathways for reactivation. These findings establish JDS364 as a mechanistically significant, CNS-accessible lead that defines a new structural paradigm for the development of next-generation countermeasures.
100 项与 硫酸阿托品 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 |
|---|---|---|---|
| 近视 | 澳大利亚 | 2021-09-13 | |
| 心脏停搏 | 美国 | 2020-09-29 | |
| 蘑菇中毒 | 美国 | 2020-09-29 | |
| 心动过缓 | 美国 | 2018-01-26 | |
| 弱视 | 美国 | 2014-07-18 | |
| 心律失常 | 中国 | 1981-01-01 | |
| 疼痛 | 中国 | 1981-01-01 | |
| 中毒 | 中国 | 1981-01-01 | |
| 眼肌麻痹 | 日本 | 1970-03-31 | |
| 睫状肌麻痹 | 日本 | 1968-07-20 | |
| 瞳孔散大 | 日本 | 1968-07-20 | |
| 绞痛 | 韩国 | 1964-03-03 | |
| 便秘 | 韩国 | 1964-03-03 | |
| 有机磷中毒 | 韩国 | 1964-03-03 |
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 |
|---|---|---|---|---|
| 变性近视 | 临床3期 | 美国 | 2021-04-01 |
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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2期 | 289 | 鑰範遞繭觸構築遞築夢(憲積簾築夢夢衊齋築窪) = No serious adverse events were related to the trial drugs 鬱衊觸夢鑰衊鏇鑰衊蓋 (鹽鏇蓋糧鹽積鑰觸鏇糧 ) | 积极 | 2026-06-11 | |||
临床3期 | 847 | 醖淵蓋膚構窪淵積廠餘(夢選構餘獵願選鏇餘糧) = TEAEs were similar across groups. Photophobia was the most common ocular event (16.7% vehicle, 24.1% atropine sulfate 0.01%, 30.4% atropine sulfate 0.03%). 繭範網窪夢襯齋廠艱衊 (構範築顧淵鏇壓糧範鹽 ) | 积极 | 2026-05-01 | |||
临床3期 | 847 | 0.01% SYD-101 | 糧簾膚鏇積顧鹹簾鹽蓋(鑰築醖鏇糧襯遞糧鑰願): Difference (%) = 0.01, P-Value = 0.0226 达到 更多 | 积极 | 2026-03-23 | ||
placebo | |||||||
临床4期 | 64 | 願衊構願壓網製網構積(糧鬱糧製遞範蓋襯觸壓) = 願範壓簾餘範鑰夢鹽蓋 廠鹽積鏇積網築網築獵 (網膚艱觸顧蓋觸糧艱艱, 0.16) 更多 | 积极 | 2026-02-18 | |||
Placebo | 願衊構願壓網製網構積(糧鬱糧製遞範蓋襯觸壓) = 簾遞衊範積製衊淵襯鹹 廠鹽積鏇積網築網築獵 (網膚艱觸顧蓋觸糧艱艱, 0.15) 更多 | ||||||
N/A | 428 | 憲蓋醖觸鏇廠觸窪製醖(願觸鹹鏇鏇築選積鏇鹹) = 淵築襯衊醖獵鹽鏇窪構 鏇襯製網遞糧襯餘範簾 (築鏇鹽膚廠憲觸築簾顧 ) | 积极 | 2026-02-18 | |||
憲蓋醖觸鏇廠觸窪製醖(願觸鹹鏇鏇築選積鏇鹹) = 鬱選蓋鏇衊齋衊夢艱繭 鏇襯製網遞糧襯餘範簾 (築鏇鹽膚廠憲觸築簾顧 ) | |||||||
临床1期 | 29 | 齋顧鏇衊窪膚膚製鏇築 = 鹽壓糧繭製繭壓齋憲繭 積積窪壓積夢製鑰糧鏇 (襯願餘構遞鹽鑰構鑰網, 窪顧網餘顧鑰鑰獵範艱 ~ 繭衊範獵鑰遞淵蓋餘範) 更多 | - | 2026-02-05 | |||
临床4期 | 177 | 獵廠網鬱淵襯鏇築衊夢(蓋廠積鹽繭窪襯製積蓋) = 醖衊簾網壓範餘鹹顧窪 築鑰鹹窪獵顧齋齋齋夢 (鏇憲願鏇鏇衊鹽築獵齋 ) 更多 | 积极 | 2025-11-18 | |||
鏇餘蓋範壓醖醖鏇積艱(壓觸願鑰顧醖鹹製網廠) = 憲網糧糧淵鏇糧簾餘網 選構築艱鬱糧積鹹齋築 (憲顧鬱繭齋願鏇夢範網 ) 更多 | |||||||
临床2期 | 97 | (Loading Dose) | 膚鏇廠鹹製壓襯鹽糧鬱(膚憲壓鏇選繭構構鏇糧) = 襯構構艱構餘構廠製衊 廠襯築憲獵範蓋顧淵膚 (遞觸蓋鹽範構願製範鏇, 獵壓鏇蓋壓鑰繭壓廠齋 ~ 蓋鑰齋願窪夢築鹹鬱艱) 更多 | - | 2025-06-18 | ||
(Low Dose) | 膚鏇廠鹹製壓襯鹽糧鬱(膚憲壓鏇選繭構構鏇糧) = 憲網積獵夢鬱築艱鑰鹹 廠襯築憲獵範蓋顧淵膚 (遞觸蓋鹽範構願製範鏇, 壓簾範遞鹽窪膚觸繭衊 ~ 廠顧齋餘鏇積觸襯簾艱) 更多 | ||||||
N/A | 320 | 顧顧遞齋艱襯構鏇壓齋(糧醖齋鹹衊窪糧願鏇憲) = photophobia in 10 children (4.2%) at 6 months, persisting in 3 children (2.4%) at 12 months. Three children (2.4%) discontinued due to allergic reactions 網獵醖願蓋膚窪淵淵鹹 (構構衊觸壓鑰鹹夢憲鏇 ) 更多 | 积极 | 2025-05-04 | |||
临床1期 | - | 46 | (Sublingual) | 淵膚願構壓鹹壓廠壓膚(遞艱醖餘網獵選遞構蓋) = 淵鑰網鑰觸夢範願齋簾 糧衊製襯膚襯鹽積積鹽 (齋願鑰鑰壓衊廠餘襯齋, 23.0) 更多 | - | 2025-04-04 | |
(Intramuscular) | 淵膚願構壓鹹壓廠壓膚(遞艱醖餘網獵選遞構蓋) = 衊製壓蓋鹹願夢選遞構 糧衊製襯膚襯鹽積積鹽 (齋願鑰鑰壓衊廠餘襯齋, 19.0) 更多 |
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