阿法沙龙(Alfaxalone) - 药物靶点：GABAA receptor_在研适应症：麻醉，镇静_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Alfaxalone (INN)、Phaxan

+ [3]

靶点

GABAA receptor

作用机制

GABAA receptor正向变构调节剂(γ-氨基丁酸 A 受体正向别构调节剂)

治疗领域

其他疾病

在研适应症

麻醉镇静

非在研适应症-

原研机构

Drawbridge Pharmaceuticals

在研机构

加立生物科技有限公司

非在研机构

Drawbridge Pharmaceuticals

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)临床前

特殊审评-

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结构

分子式C21H32O3

InChIKeyDUHUCHOQIDJXAT-OLVMNOGESA-N

CAS号23930-19-0

关联

2

项与阿法沙龙相关的临床试验

ACTRN12618000064202 / Suspended临床3期IIT

A Pivotal Phase III trial of Phaxan™, a new formulation of alphaxalone dissolved in sulfobutyl ether beta cyclodextrin, for anaesthesia in patients undergoing hip joint replacement; stage 1, the pilot study

开始日期2018-04-12

申办/合作机构-

ACTRN12611000343909 / Completed临床1期

Induction of anaesthesia with an intravenous injection of PHAX001, a new water soluble anaesthetic compared with propofol for speed of onset and recovery from anaesthesia.

开始日期2013-11-14

申办/合作机构

Southern Health Partners, Inc.

[+1]

100 项与阿法沙龙相关的临床结果

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100 项与阿法沙龙相关的转化医学

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100 项与阿法沙龙相关的专利（医药）

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473

项与阿法沙龙相关的文献（医药）

2024-11-01·Veterinary Anaesthesia and Analgesia

A survey on the use of total intravenous anaesthesia in small animals by veterinary anaesthesiologists

Article

作者: Bustamante, Rocío ; Gómez de Segura, Ignacio A. ; Aguado, Delia ; Gómez de Segura, Ignacio A ; Ortiz-Díez, Gustavo ; Canfrán, Susana

OBJECTIVETo describe the use of total intravenous anaesthesia (TIVA) in dogs and cats by veterinary anaesthesiologists.STUDY DESIGNA cross-sectional online, voluntary, anonymous survey.POPULATIONData from 153 answered questionnaires.METHODSAn anonymous questionnaire was sent via e-mail to diplomates, residents and residency-trained individuals from the American and European Colleges of Veterinary An(a)esthesia and Analgesia, to gather information on the use, perceived advantages, reasons for the use or not of TIVA and attitudes towards this technique in dogs and cats. Descriptive statistics and logistic regression analysis to detect significant associations were performed. The effect size was estimated using the odds ratio (OR) and 95% confidence interval (CI). A significance level of p < 0.05 was used.RESULTSWe obtained 153/703 responses (66% diplomates, 34% residents; overall response rate of 21.7%). Although 99% and 94% of respondents used TIVA in dogs and cats, respectively, only 14% used it frequently (several times a week) in dogs, and < 1% in cats. Most respondents used propofol (97%, dogs) and alfaxalone (85%, cats), mostly combined with opioids. Reasons for not using TIVA more frequently included prolonged recovery (49%, dogs; 61%, cats), higher cost (46%, dogs) and concerns about drug accumulation (44%, cats). Frequent TIVA use was driven by clinical indications (100%) and greater haemodynamic stability (87%). A higher proportion of respondents using TIVA frequently reported the high stability of the anaesthetic plane (20%; OR = 5.0; 95% CI: 1.4-17.8; p = 0.013) and disagreed with using TIVA only when a specific clinical indication existed (OR = 3.3; 95% CI: 1.4-10.0; p = 0.013).CONCLUSIONS AND CLINICAL RELEVANCEAlthough occasional, TIVA use is reported among veterinary anaesthesiologists. Clinical indications for TIVA are the most likely reason for its use, whereas factors such as a prolonged recovery or higher cost might limit its use.

2024-09-01·Journal of the American Association for Laboratory Animal Science

Sedation Efficacy of Midazolam in Conjunction with Ketamine and Alfaxalone in Female Laboratory Guinea Pigs (Cavia porcellus)

Article

作者: Walsh, Courtney A ; Haulter, Marlena ; Ekanayake-Alper, Dil ; Wharton, Keely Nicole ; Ekanayake, Dinesh

AbstractGuinea pigs have been integral as models used in biomedical research, making significant contributions to nutritional, auditory, immunologic, and hypersensitivity studies, and necessitating the routine need for sedation in laboratory settings. The ketamine-xylazine (KX) combination has been the standard sedation protocol for decades. However, due to the adverse effects and abuse potential of xylazine, this study explores the possibility of substituting xylazine with midazolam and examines the combined use of midazolam with ketamine and alfaxalone in female laboratory guinea pigs. Our findings indicate that KX facilitates the fastest induction and longest duration of sedation compared with other sedatives, including ketamine-midazolam (KM), which, despite its rapid induction, results in significantly shorter sedation durations. KX also ensures a deeper anesthetic depth and greater odds of loss of withdrawal and inguinal reflexes, in contrast to KM and alfaxalone-midazolam (AM), under which only 15% of the animals lost these reflexes. In terms of cardiopulmonary function, KM led to an increased heart rate attributed to elevated sympathetic activity. All 4 sedative protocols lead to respiratory depression, except KM, which causes minimal reduction. Adverse events varied, with 75% of animals experiencing injection site reactions after KX administration and 67% exhibiting regurgitation post-KM administration. No adverse events were reported for the AM combination, suggesting its safer profile. In conclusion, while KX remains the superior protocol for sedation due to its efficiency, reliability, and minimal impact on physiologic parameters, midazolam is not a preferable alternative to replace xylazine. Its increased sympathetic tone, hyperesthesia, and shorter action duration, coupled with a higher potential for adverse events, limit its suitability to combine with ketamine in guinea pig sedation. However, when midazolam is used in conjunction with safer alternatives like alfaxalone, it presents a viable sedation strategy, emphasizing the need for further research into optimizing sedative combinations for laboratory guinea pigs.

2024-09-01·Journal of Feline Medicine and Surgery

Use of a quadratus lumborum block in queens undergoing ovariectomy: a randomised controlled trial

Article

作者: Ristori, Claudia ; Bucci, Roberta ; Vignoli, Massimo ; Collivignarelli, Francesco ; Santoro, Francesco ; Carluccio, Augusto ; Bianchi, Amanda ; Costanzini, Giulia ; Parrillo, Salvatore ; Tamburro, Roberto ; Robbe, Domenico ; Di Giosia, Alessandro ; Paolini, Andrea

Objectives The aim of the study was to evaluate the perioperative analgesic effect of a quadratus lumborum (QL) block in queens undergoing ovariectomy. Methods A total of 37 healthy queens admitted for elective ovariectomy were randomised into two groups: control (CTRL, n = 19) and QL block (QL, n = 18). All cats were premedicated with dexmedetomidine 0.005 mg/kg, alfaxalone 1 mg/kg and methadone 0.1 mg/kg IM. Under general anaesthesia, cats allocated to the QL group received a bilateral ultrasound-guided QL block with 0.4 ml/kg of ropivacaine 0.4% (3.2 mg/kg). No treatment was administered to cats in the CTRL group. Intraoperative rescue fentanyl boluses were administered if haemodynamic and/or respiratory parameters exceeded 30% of the pre-incisional values. Postoperative methadone boluses were administered based on Feline Grimace Scale scores. Demographics, baseline vital parameter values, requirement for rescue analgesia, incidence of hypotension, sialorrhoea, vomiting and dysphoria, and number of cats accepting food at 6 h after extubation were compared between groups. Results A higher number of queens required intraoperative fentanyl in the CTRL group (14/18, 77.8%) compared with the QL group (1/19, 5.3%) ( P <0.001). The median total fentanyl dose was 4 µg/kg (range 0–4) in the CTRL group and 0 µg/kg (range 0–4) in the QL group ( P <0.001). No statistically significant difference was found between groups when comparing the number of animals requiring postoperative methadone, total methadone dose, episodes of hypotension, sialorrhoea, vomiting and dysphoria, and number of queens accepting food at 6 h postoperatively. No adverse effect or complication potentially related to the block was recorded. Conclusions and relevance The QL block resulted in a lower intraoperative fentanyl requirement in queens undergoing ovariectomy. Further studies are needed to clarify the postoperative analgesic effect of this technique in cats.

100 项与阿法沙龙相关的药物交易

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