{"title":"Preliminary evaluation of the efficacy and safety of brimonidine for deep sedation","authors":"Xiaohui Wang, Rui Zhang, Bin Chen, Ting Zhang, Xinghua Jin, Ping Gao","doi":"10.1111/fcp.12944","DOIUrl":null,"url":null,"abstract":"<div>\n \n \n <section>\n \n <h3> Background</h3>\n \n <p>Although brimonidine is currently used in the clinical treatment of glaucoma and rosacea, research of the deep sedative effect on animals after systemic administration is reported firstly and has shown promising results.</p>\n </section>\n \n <section>\n \n <h3> Methods</h3>\n \n <p>The median effective dose (ED<sub>50</sub>), the median lethal dose (LD<sub>50</sub>), and the therapeutic index of brimonidine for deep sedation and formalin stimulation assay were determined by various animal experiments. The effect of synergistic anesthesia in rabbits with brimonidine and chloral hydrate was preliminarily evaluated.</p>\n </section>\n \n <section>\n \n <h3> Results</h3>\n \n <p>The ED<sub>50</sub> of brimonidine for highly effective sedation by intraperitoneal injection in rats was calculated to be 2.05 mg kg<sup>−1</sup> with a 95% confidence interval (CI) of 1.87 to 2.25 mg kg<sup>−1</sup>. The ED<sub>50</sub> of brimonidine for deep sedation by intravenous and intrarectal injection in rabbits was calculated to be 0.087 mg kg<sup>−1</sup> with a 95% CI of 0.084 to 0.091 mg kg<sup>−1</sup> and 1.65 mg kg<sup>−1</sup> with a 95% CI of 1.43 to 1.91 mg kg<sup>−1</sup>, respectively. The LD<sub>50</sub> of intraperitoneal brimonidine injection in rats was calculated to be 468 mg kg<sup>−1</sup> with a 95% CI of 441 to 497 mg kg<sup>−1</sup> and a therapeutic index of 228. Brimonidine has a certain analgesic and heart rate lowering effects.</p>\n </section>\n \n <section>\n \n <h3> Conclusion</h3>\n \n <p>The results confirmed that brimonidine has deep sedation and analgesic effects after systemic administration and has high safety. It can be used in combination with other types of sedative drugs to achieve better effects.</p>\n </section>\n </div>","PeriodicalId":12657,"journal":{"name":"Fundamental & Clinical Pharmacology","volume":null,"pages":null},"PeriodicalIF":2.1000,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Fundamental & Clinical Pharmacology","FirstCategoryId":"3","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1111/fcp.12944","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
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Abstract
Background
Although brimonidine is currently used in the clinical treatment of glaucoma and rosacea, research of the deep sedative effect on animals after systemic administration is reported firstly and has shown promising results.
Methods
The median effective dose (ED50), the median lethal dose (LD50), and the therapeutic index of brimonidine for deep sedation and formalin stimulation assay were determined by various animal experiments. The effect of synergistic anesthesia in rabbits with brimonidine and chloral hydrate was preliminarily evaluated.
Results
The ED50 of brimonidine for highly effective sedation by intraperitoneal injection in rats was calculated to be 2.05 mg kg−1 with a 95% confidence interval (CI) of 1.87 to 2.25 mg kg−1. The ED50 of brimonidine for deep sedation by intravenous and intrarectal injection in rabbits was calculated to be 0.087 mg kg−1 with a 95% CI of 0.084 to 0.091 mg kg−1 and 1.65 mg kg−1 with a 95% CI of 1.43 to 1.91 mg kg−1, respectively. The LD50 of intraperitoneal brimonidine injection in rats was calculated to be 468 mg kg−1 with a 95% CI of 441 to 497 mg kg−1 and a therapeutic index of 228. Brimonidine has a certain analgesic and heart rate lowering effects.
Conclusion
The results confirmed that brimonidine has deep sedation and analgesic effects after systemic administration and has high safety. It can be used in combination with other types of sedative drugs to achieve better effects.
期刊介绍：
Fundamental & Clinical Pharmacology publishes reports describing important and novel developments in fundamental as well as clinical research relevant to drug therapy. Original articles, short communications and reviews are published on all aspects of experimental and clinical pharmacology including:
Antimicrobial, Antiviral Agents
Autonomic Pharmacology
Cardiovascular Pharmacology
Cellular Pharmacology
Clinical Trials
Endocrinopharmacology
Gene Therapy
Inflammation, Immunopharmacology
Lipids, Atherosclerosis
Liver and G-I Tract Pharmacology
Metabolism, Pharmacokinetics
Neuropharmacology
Neuropsychopharmacology
Oncopharmacology
Pediatric Pharmacology Development
Pharmacoeconomics
Pharmacoepidemiology
Pharmacogenetics, Pharmacogenomics
Pharmacovigilance
Pulmonary Pharmacology
Receptors, Signal Transduction
Renal Pharmacology
Thrombosis and Hemostasis
Toxicopharmacology
Clinical research, including clinical studies and clinical trials, may cover disciplines such as pharmacokinetics, pharmacodynamics, pharmacovigilance, pharmacoepidemiology, pharmacogenomics and pharmacoeconomics. Basic research articles from fields such as physiology and molecular biology which contribute to an understanding of drug therapy are also welcomed.
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