苯佐那酯(Benzonatate) - 药物靶点：SCNA_在研适应症：咳嗽_专利_临床

概要

基本信息

简介TESSALON® (苯佐那酯) 是辉瑞公司生产的FDA批准的非麻醉性口服抗咳药。它于1958年首次在美国获得批准，用于缓解咳嗽的症状。苯佐那酯作为钠通道阻滞剂，能够麻醉呼吸道、肺和胸膜中的牵伸受体，减弱它们的活动并降低咳嗽反射。它的效果在15-20分钟内开始，并可持续3-8小时。苯佐那敏在推荐使用时不会对呼吸中枢产生抑制作用。其活性成分为2，5，8，11，14，17，20，23，26-九氧二十八烷基-p-（丁基氨基）苯酸酯，分子量为603.7。苯佐那酯仅适用于缓解咳嗽，与麻醉性抗咳药物不同，它没有滥用或成瘾的风险。

药物类型

小分子化药

别名

2,5,8,11,14,17,20,23,26-nonaoxaoctacosan-28-yl p-(butylamino)benzoate、2-[2-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl 4-butylaminobenzoate、3,6,9,12,15,18,21,24,27-nonaoxaoctacosyl 4-butylaminobenzoate

+ [7]

靶点

SCNA

作用机制

SCNA阻滞剂(钠通道α亚基家族阻滞剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

非在研机构

最高研发阶段批准上市

首次获批日期

美国 (1958-02-10),

咳嗽

最高研发阶段(中国)临床3期

特殊审评-

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结构

分子式C30H53NO11

InChIKeyMAFMQEKGGFWBAB-UHFFFAOYSA-N

CAS号104-31-4

关联

6

项与苯佐那酯相关的临床试验

CTR20180960 / Recruiting临床3期

苯佐那酯软胶囊用于改善成人咳嗽症状的有效性和安全性多中心、随机、双盲、安慰剂对照研究

主要目的：以安慰剂为对照，评价苯佐那酯软胶囊用于改善成人咳嗽症状的有效性次要目的：以安慰剂为对照，评价苯佐那酯软胶囊用于改善成人咳嗽症状的安全性

开始日期2018-05-11

申办/合作机构

石药集团恩必普药业有限公司

NCT03722914 / Unknown status临床3期

A Multicentric Randomized Double-blind Placebo-controlled Study on the Efficacy and Safety of Benzonatate Soft Capsules for Improving Adult Cough Symptoms

The purpose of this study is evaluate the efficay and safety of benzonatate soft capsules for improving adult cough symtoms.

开始日期2018-03-01

申办/合作机构

石药集团中奇制药技术（天津）有限公司

NCT02207699 / Completed临床1期

Evaluation of the Effect of Benzonatate on QT Intervals Following Single Dose Administration of Benzonatate to Healthy Volunteers

The primary objective of this study is to determine the effects of benzonatate (200 mg and 800 mg) on the QT interval following single dose oral administration at each time point post-dose.

开始日期2014-05-01

申办/合作机构

Pfizer Inc.

100 项与苯佐那酯相关的临床结果

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100 项与苯佐那酯相关的转化医学

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100 项与苯佐那酯相关的专利（医药）

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86

项与苯佐那酯相关的文献（医药）

2024-01-09·ACS Nano

Design and Synthesis of a Water-Based Nanodelivery Pesticide System for Improved Efficacy and Safety

Article

作者: Huang, Bingna ; An, Changcheng ; Wu, Qingjun ; Li, Ningjun ; Shen, Yue ; Gao, Jin-Ming ; Lynch, Iseult ; Sun, Changjiao ; Cui, Haixin ; Zhan, Shenshan ; Liu, Huihui ; Jiang, Jiajun ; Li, Xingye ; Wang, Xinyue ; Zeng, Zhanghua ; Wang, Yan ; Zhang, Youjun ; Zhang, Peng ; Guo, Zhiling ; Wang, Chong

Developing an environmentally friendly and safe nanodelivery system is crucial to improve the efficacy of pesticides and minimize environmental and health risks. However, preparing a completely water-based nanopesticide without using harmful solvents is a technical challenge. In this study, a water-based nanodelivery pesticide system was constructed to improve the efficacy and safety of Emamectin Benzoate (EB). A specific surfactant, 29-(4-(5-hydroxynonan-5-yl)phenoxy)-3,6,9,12,15,18,21,24,27-nonaoxanonacosan-1-ol (SurEB) was designed and synthesized to form a water-based nanodelivery system (EBWNS) with EB. Molecular dynamics simulations revealed the self-assembly and interaction forces between SurEB and EB in water, providing insights into the formation mechanism of EBWNS nanoparticles. The nanodelivery system showed the prolonged effectivity of EB with reduced degradation and demonstrated a good control efficacy for multiple target pests, such as red spider mite, beet armyworm larvae (Lepidoptera: Noctuidae), and rice stem borers (Chilo suppressalis). Toxicology tests on various objects demonstrated that the EBWNS has low toxicity for seeds, HaCaT cells, zebrafish, earthworm, and E. coli. This study provides a distinctive perspective for developing environmentally friendly nanopesticide formulations, which clarified a water-based treatment method for specific lipid-soluble pesticides. The water-based nanodelivery pesticide system has the potential to improve the efficacy and safety of pesticides in the process of field applications.

2023-09-29·Journal of clinical medicine

Patterns of Cough Medication Prescribing among Patients with Chronic Cough in Florida: 2012-2021.

Article

作者: Schelfhout, Jonathan ; Wilson, Debbie L ; Huang, Shu ; Lo-Ciganic, Wei-Hsuan ; Sher, Mandel R ; Ke, Xuehua ; Ding, Helen ; Yang, Seonkyeong ; Jones, Bobby ; Hincapie-Castillo, Juan M

Among patients with chronic cough (CC) in the 2012-2021 statewide OneFlorida Clinical Research Consortium database, we examined trends in cough medication (CM) prescribing prevalence over time in repeated cross-sectional analyses and identified distinct CM utilization trajectories using group-based trajectory modeling (GBTM) in a retrospective cohort study. Among eligible adults (≥18 years) without cancer/benign respiratory tumor diagnoses, we identified CC patients and non-CC patients with any cough-related diagnosis. In the GBTM analysis, we calculated the number of monthly prescriptions for any CMs (excluding gabapentinoids) during the 12 months from the first qualifying cough event to identify distinct utilization trajectories. From 2012 to 2021, benzonatate (9.6% to 26.1%), dextromethorphan (5.2% to 8.6%), and gabapentinoid (5.3% to 14.4%) use increased among CC patients, while opioid antitussive use increased from 2012 to 2015 and decreased thereafter (8.4% in 2012, 14.7% in 2015, 6.7% in 2021; all p < 0.001). Of 15,566 CC patients and 655,250 non-CC patients identified in the GBTM analysis, CC patients had substantial burdens of respiratory/non-respiratory comorbidities and healthcare service and concomitant medication use compared to non-CC patients. Among CC patients, GBTM identified three distinct CM utilization trajectories: (1) no CM use (n = 11,222; 72.1%); (2) declining CM use (n = 4105; 26.4%); and (3) chronic CM use (n = 239; 1.5%). CC patients in Florida had limited CM use with increasing trends in use of benzonatate, dextromethorphan, and gabapentinoids and a decreasing trend in opioid antitussive use. CC patients, particularly with chronic prescription CM use, experienced substantial disease burden.

2023-01-01·PloS one

Benzonatate as a local anesthetic.

Article

作者: McGuire, Anna ; Aizik, Gil ; Li, Yang ; Ostertag-Hill, Claire A ; Kohane, Daniel S

INTRODUCTIONBenzonatate is an FDA-approved antitussive agent that resembles tetracaine, procaine, and cocaine in its chemical structure. Based on structural similarities to known local anesthetics and recent findings of benzonatate exerting local anesthetic-like effects on voltage-gated sodium channels in vitro, we hypothesized that benzonatate will act as a local anesthetic to yield peripheral nerve blockade.METHODSBenzonatate was injected at the sciatic nerve of Sprague-Dawley rats. Sensory and motor blockade were assessed using a modified hot plate test and a weight-bearing test, respectively. Additionally, the effect of co-injection with tetrodotoxin and Tween 80 (a chemical permeation enhancer) was examined. Myotoxicity of benzonatate was assessed in vivo by histological analysis.RESULTSBenzonatate produced a concentration-dependent sensory and motor nerve blockade with no appreciable systemic effects. Co-injection with tetrodotoxin or Tween 80 produced prolongation of sensory nerve blockade. Histologic assessment showed significant inflammation and myotoxicity from benzonatate injection, even at low concentrations.CONCLUSIONThis study demonstrates that benzonatate does act as a local anesthetic at the peripheral nerve, with sensory and motor nerve blockade. Benzonatate interacts with tetrodotoxin and Tween 80 to prolong nerve blockade. However, benzonatate causes significant myotoxicity, even at subtherapeutic concentrations.

100 项与苯佐那酯相关的药物交易

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