Delving into the Latest Updates on Benzonatate with Synapse

Overview

Basic Info

SummaryTESSALON® (Benzonatate) is an FDA-approved non-narcotic oral antitussive medication manufactured by Pfizer Inc. It was first approved in the United States in 1958 for the symptomatic relief of cough. TESSALON acts as a sodium channel blocker, anesthetizing the stretch receptors in the respiratory passages, lungs, and pleura to dampen their activity and reduce the cough reflex. Its effect starts within 15-20 minutes and can last between 3-8 hours. TESSALON has no inhibitory effect on the respiratory center when used as recommended. The active ingredient, 2, 5, 8, 11, 14, 17, 20, 23, 26-nonaoxaoctacosan-28-yl p-(butylamino) benzoate, has a molecular weight of 603.7. TESSALON is solely indicated for the relief of cough, but it has no known potential for abuse or addiction, unlike narcotic antitussives.

Drug Type

Small molecule drug

Synonyms

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

+ [8]

Target

SCNA

Mechanism

SCNA blockers(Sodium channel alpha subunit blockers)

Therapeutic Areas

Respiratory Diseases

Active Indication

Cough

Inactive Indication

Dry cough

Originator Organization

Pfizer Inc.

Active Organization

CSPC NBP Pharmaceutical Co., Ltd.

Pfizer Inc.

Inactive Organization

Biocon Ltd.

Drug Highest PhaseApproved

First Approval Date

US (10 Feb 1958),

Cough

Regulation-

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Structure

Molecular FormulaC30H53NO11

InChIKeyMAFMQEKGGFWBAB-UHFFFAOYSA-N

CAS Registry104-31-4

Author: 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.

29 Sep 2023·Journal of clinical medicine

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

Article

Author: 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.

01 Jan 2023·PloS one

Benzonatate as a local anesthetic.

Article

Author: 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 Deals associated with Benzonatate

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