更新于：2024-12-15
Perospirone Hydrochloride Hydrate
盐酸哌罗匹隆
更新于：2024-12-15
概要
基本信息
药物类型 小分子化药 |
别名 cis-N-(4-(4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl)butyl)-1,2-cyclohexanedicarboximide、Perospirone、Perospirone Hydrochloride + [6] |
作用机制 5-HT2A receptor拮抗剂(5-羟色胺2A受体拮抗剂)、D2 receptor拮抗剂(多巴胺D2受体拮抗剂) |
治疗领域 |
在研适应症 |
非在研适应症- |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2000-12-22), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C23H35ClN4O4S |
InChIKeyLZQKLGXZZSMREH-SMMZMSQNSA-N |
CAS号192052-81-6 |
关联
9
项与 盐酸哌罗匹隆 相关的临床试验盐酸哌罗匹隆片在健康人体空腹/餐后状态下的生物等效性试验
盐酸哌罗匹隆片在中国健康受试者中进行的单中心随机开放单次（空腹/餐后）口服给药两制剂两序列四周期完全重复交叉的人体生物等效性试验
盐酸哌罗匹隆片在健康受试者中单中心、随机、开放、两制剂、单次给药、四周期、两序列、完全重复交叉餐后生物等效性试验
100 项与 盐酸哌罗匹隆 相关的临床结果
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100 项与 盐酸哌罗匹隆 相关的转化医学
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100 项与 盐酸哌罗匹隆 相关的专利（医药）
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183
项与 盐酸哌罗匹隆 相关的文献（医药）2024-09-01Neuropsychopharmacology reports
Continuous alcohol withdrawal delirium and physical illness‐associated delirium in a man brought to the emergency department after a disaster: A case report
Article
作者: Sasaki, Taro ; Sato, Yoshiteru ; Sugawara, Norio ; Owada, Tamaki ; Hasegawa, Chie ; Yasui‐Furukori, Norio ; Shindo, Yunosuke ; Kawamata, Yasushi ; Kikuchi, Kota
Abstract:
Background:
Risk factors for alcohol withdrawal delirium include heavy drinking, prior alcohol withdrawal delirium or convulsions, nondrug sedative use, and a history of tachycardia, withdrawal, and infections.
Case Presentation:
A 76‐year‐old man with a history of heavy drinking and type 2 diabetes was hospitalized for hypothermia, rhabdomyolysis, and acute renal failure after a typhoon. He developed alcohol withdrawal symptoms 24 h after his last drink, leading to severe withdrawal delirium characterized by restlessness, delusions, and altered consciousness. Treatment included lorazepam, in addition to comprehensive care for his physical condition. His condition fluctuated, especially at night, with his psychiatric symptoms exacerbated by his physical illnesses, suggesting delirium due to the coexistence of severe and multiple physical illnesses. After 44 days, following substantial improvements in both mental and physical health with perospirone, the patient was discharged.
Conclusion:
This case emphasizes the need for multidisciplinary collaboration in the treatment of such patients, especially during disasters, and the importance of long‐term monitoring for elderly patients with alcohol dependence syndrome after a disaster.
2024-06-01Neuropsychopharmacology reports
The effective perospirone augmentation with clonazepam for treatment‐resistant burning mouth syndrome: A case report
Article
作者: Takao, Chihiro ; Maeda, Chizuko ; Tu, Trang Thi Huyen ; Toyofuku, Akira ; Tominaga, Risa ; Nayanar, Gayatri ; Kimura, Yasuyuki ; Watanabe, Motoko ; Nagamine, Takahiko
Abstract:
Burning mouth syndrome (BMS) is characterized by burning sensations in the oral region without corresponding abnormalities and is often accompanied by uncomfortable sensations. Herein, we present cases of BMS in which the remaining uncomfortable sensations improved with perospirone augmentation with clonazepam. Case 1: A 61‐year‐old man complained of a burning pain in his tongue, a sensation of dryness and discomfort as if his tongue was sticking to a palatal plate. With the diagnosis of BMS, psychopharmacotherapy was initiated with amitriptyline. At the dose of amitriptyline 50 mg, the pain lessened but uncomfortable sensations persisted. Further attempts to alleviate symptoms by combining aripiprazole with amitriptyline, aripiprazole with mirtazapine, or aripiprazole with clonazepam were limited; however, nearly all symptoms were relieved by a combination of perospirone 8.0 mg with clonazepam 1.5 mg. Case 2: A 51‐year‐old woman complained of a burning sensation along with oral dryness and crumb‐like feeling on her tongue. She was diagnosed with BMS and began treatment with amitriptyline. Her burning sensation improved at the dose of 25 mg, but uncomfortable sensations persisted. Augmentation of amitriptyline with aripiprazole, aripiprazole either with valproate, mirtazapine, or clonazepam failed to produce a significant improvement. However, a regimen of perospirone 6.0 mg and clonazepam 1.5 mg relieved the crumb‐like sensation and pain and culminated in a stabilized condition. The reported cases suggested that multiple approaches targeting the dopaminergic circuit in basal ganglia involving the serotoninergic and GABA systems, through the administration of perospirone with clonazepam is an effective adjunctive treatment for the remaining uncomfortable sensations in patients with BMS.
2024-06-01Molecular diversity
Exploration of interaction interface of TRKβ/BDNF through fingerprint analysis to disinter potential agonists
Article
作者: Murthy, T P Krishna ; Burri, Raghunadha R ; Hemasree, G N S ; Satish, Kshreeraja S ; Rajalekshmi, Saraswathy Ganesan
Tyrosine Kinase beta (TRKβ), is a type I membrane receptor which plays a major role in various signalling pathways. TRKβ was found to be upregulated in various cancers and contrastingly downregulated in various neurodegenerative disorders. Hitherto, contemporary drug research is oriented towards discovery of TRKβ inhibitors, thus neglecting the development of TRKβ agonists. This research is aimed at identifying FDA approved drugs exhibiting repurposable potential as TRKβ agonists by mapping them with fingerprints of the BDNF/TRKβ interaction interface. Initially, crucial interacting residues were retrieved and a receptor grid was generated around it. TRKβ agonists were retrieved from literature search and a drug library was created for each agonist based on its structural and side effect similarities. Subsequently, molecular docking and dynamics were performed for each library to identify the drugs possessing affinity towards the binding pocket of TRKβ. The study revealed molecular interactions of Perospirone, Droperidol, Urapidil, and Clobenzorex with the crucial amino acids lining the active binding pocket of TRKβ. Subsequent network pharmacological analysis of the above drugs revealed their interactions with key proteins involved in neurotransmitter signalling pathways. Clobenzorex displayed high stability in dynamics simulation and therefore this drug is recommended for further experimental evaluations to attain better mechanistic insights and predict its implications in correcting neuropathological aberrations. This study's focus on the interaction interface between TRKβ and BDNF, combined with the utilization of fingerprint analysis for drug repurposing, contributes to our understanding of neurotrophic signalling and holds potential for identifying new therapeutic options for neurological disorders.
100 项与 盐酸哌罗匹隆 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 精神分裂症 | 日本 | 2000-12-22 |
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