预约演示
更新于：2025-04-01
Zaleplon
扎来普隆
更新于：2025-04-01
概要
基本信息
药物类型 小分子化药 |
别名 3'-(3-Cyanopyrazolo(1,5-a)pyrimidin-7-yl)-N-ethylacetanilide、Accordion Pill Zaleplon、AP-ZP + [28] |
作用方式 调节剂 |
作用机制 GABAA receptor调节剂(γ-氨基丁酸 A 受体调节剂) |
在研适应症 |
非在研适应症- |
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 欧盟 (1999-03-12), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C17H15N5O |
InChIKeyHUNXMJYCHXQEGX-UHFFFAOYSA-N |
CAS号151319-34-5 |
关联
19
项与 扎来普隆 相关的临床试验ChiCTR2400087469
Study on effect of zaleplon capsules on subjective sleep quality and daytime function in patients with insomnia
NCT05745038
A Single Arm Pilot Trial of a Social Network Intervention (SONATA) for Older Patients With Cancer
IRCT20130626013776N110
A study to compare the relative bioavailability of Sobhan and Pfizer formulations of zaleplon 10 mg capsules in 24 healthy adult volunteers under fasting conditions
100 项与 扎来普隆 相关的临床结果
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100 项与 扎来普隆 相关的转化医学
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100 项与 扎来普隆 相关的专利（医药）
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570
项与 扎来普隆 相关的文献（医药）2025-04-01SLEEP MEDICINE
Clinical practice guidelines for switching or deprescribing hypnotic medications for chronic insomnia: Results of European neuropsychopharmacology and sleep expert's consensus group
Review
作者: Serafini, Gianluca ; Dell' Osso, Bernardo M ; Geoffroy, Pierre A ; Maruani, Julia ; Brugnoli, Roberto ; Balestrieri, Matteo ; Martinotti, Giovanni ; Ferini-Strambi, Luigi ; Liguori, Claudio ; Di Nicola, Marco ; Palagini, Laura ; Mauries, Sibylle ; Mencacci, Claudio ; Maina, Giuseppe
INTRODUCTION:
Current guidelines recommend cognitive behavioural therapy for insomnia (CBT-I) as the first-line treatment for chronic insomnia. Pharmacological recommendations by European guidelines for the treatment of insomnia disorder include positive GABAergic modulators such as short and medium acting benzodiazepines and "Z-drugs" (eszopiclone, zaleplon, zolpidem, zopiclone), dual orexin receptor antagonists (DORAs; daridorexant), melatonin receptor agonists (melatonin 2 mg prolonged release - PR). Given the chronic nature of insomnia, the presence of non-responders to some treatments it is often necessary switching between various therapeutic approaches and medications. However, clear guidance regarding safe and effective protocols for switching these medications currently lacks in Europe.
METHOD:
To address this gap, we used the RAND/UCLA Appropriateness to evaluate the appropriateness of procedures for switching medications prescribed for insomnia disorder. Following a systematic review of the literature conducted in accordance with the PRISMA guidelines, we then formulated some recommendations.
RESULTS:
Twenty-one papers were selected.
CONCLUSIONS:
Discontinuation of Hypnotic Benzodiazepines and Z-drugs should be gradual, with dose reductions of 10-25 % each week. Multi-component CBT-I, daridorexant, eszopiclone, and melatonin 2 mg PR were shown to facilitate the gradual discontinuation of hypnotic benzodiazepines/Z-drugs within a cross-tapered program, which can be delayed when necessary. Finally, daridorexant and melatonin 2 mg PR do not require special switching or deprescribing protocols. Several sedative-hypnotic dosage reduction algorithms are proposed in this work for clinical use in real world settings.
2025-02-01JOURNAL OF SLEEP RESEARCH
Trends in hypnotic drug use in depression 2007–2017: A Swedish population‐based study
Article
作者: Nygren, Adam ; Reutfors, J. ; Eloranta, S. ; Brandt, L. ; Karlsson, P. ; Brenner, P.
Summary:
Insomnia is a common feature of depression; however, depression treatment guidelines provide limited recommendations regarding hypnotic drugs. Few studies have thoroughly investigated the use of hypnotic drugs in depression. In this cohort study using national Swedish registers, we included all patients ≥18 years with incident unipolar depression during 2007–2017. Patients were followed for 3 years, noting the annual and quarterly prevalence of hypnotic drug use from prescription fills. Prevalence ratios (PR) comparing 2017 to 2007 were calculated with 95% confidence intervals (CI). A total of 222,077 patients with depression were included (mean age 41 years, 59% women). In the year following diagnosis, 44.1% used any hypnotic drug in 2017, compared with 46.7% in 2007 (PR 0.94, 95% CI 0.92–0.97). The most commonly used drugs were Z‐drugs (zopiclone, zolpidem, and zaleplon) with a prevalence of 27.6% in 2017 and 35.6% in 2007 (PR 0.78, 95% CI 0.75–0.80). Melatonin use increased sharply to 12.0% in 2017 from 0.4% in 2007 (PR 28.9, 95% CI 23.5–35.7). Hypnotic drug use was most prevalent in the first two quarters after diagnosis; however, after 3 years, the quarterly prevalence was still 19.2%. Hypnotics were more common among women, older patients, those with somatic comorbidities, more severe depression, or a history of suicide attempt. Evidence from this large register‐based study demonstrates that hypnotics were used to a large extent in depression in Sweden 2007–2017. Z‐drugs use declined and melatonin use increased dramatically. Hypnotic drug use remained high even 3 years after diagnosis.
2025-01-01CPT-Pharmacometrics & Systems Pharmacology
Establishing a physiologically based pharmacokinetic framework for aldehyde oxidase and dual aldehyde oxidase‐CYP substrates
Article
作者: Huertas Valentin, Leticia ; Tian, Dan‐Dan ; Scotcher, Daniel ; Izat, Nihan ; Carione, Pasquale ; Moss, Darren ; Peterkin, Vincent C. ; Bolleddula, Jayaprakasam ; Zientek, Michael A. ; Houston, J. Brian ; Jones, Robert S. ; Venkatakrishnan, Karthik ; Galetin, Aleksandra ; Treyer, Andrea ; Kulkarni, Priyanka ; Barber, Jill
Abstract:
Aldehyde oxidase (AO) contributes to the clearance of many approved and investigational small molecule drugs, which are often dual substrates of AO and drug‐metabolizing enzymes such as cytochrome P450s (CYPs). As such, the lack of established framework for quantitative translation of the clinical pharmacologic correlates of AO‐mediated clearance represents an unmet need. This study aimed to evaluate the utility of physiologically based pharmacokinetic (PBPK) modeling in the development of AO and dual AO‐CYP substrates. PBPK models were developed for capmatinib, idelalisib, lenvatinib, zaleplon, ziprasidone, and zoniporide, incorporating in vitro functional data from human liver subcellular fractions and human hepatocytes. Prediction of metabolic elimination with/without the additional empirical scaling factors (ESFs) was assessed. Clinical pharmacokinetics, human mass balance, and drug–drug interaction (DDI) studies with CYP3A4 modulators, where available, were used to refine/verify the models. Due to the lack of clinically significant AO‐DDIs with known AO inhibitors, the fraction metabolized by AO (fmAO) was verified indirectly. Clearance predictions were improved by using ESFs (GMFE ≤1.4‐fold versus up to fivefold with physiologically‐based scaling only). Observed fmi from mass balance studies were crucial for model verification/refinement, as illustrated by capmatinib, where the fmAO (40%) was otherwise underpredicted up to fourfold. Subsequently, independent DDI studies with ketoconazole, itraconazole, rifampicin, and carbamazepine verified the fmCYP3A4, with predicted ratios of the area under the concentration–time curve (AUCR) within 1.5‐fold of the observations. In conclusion, this study provides a novel PBPK‐based framework for predicting AO‐mediated pharmacokinetics and quantitative assessment of clinical DDI risks for dual AO‐CYP substrates within a totality‐of‐evidence approach.
100 项与 扎来普隆 相关的药物交易
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研发状态
临床结果
临床结果
适应症
分期
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N/A | 10 | 遞壓衊夢觸鏇蓋範窪艱(築選壓淵齋醖鹹繭襯襯) = 5 網網壓鹽構網艱壓餘廠 (艱壓網鏇襯顧鬱範網蓋 ) 更多 | 积极 | 2019-05-26 | |||
临床2期 | 20 | 餘積選壓顧鏇製蓋壓築(壓積簾窪鏇製鹽簾製獵) = 淵築醖壓範膚糧艱糧鏇 鏇構醖築衊選廠糧鹽醖 (衊觸艱膚遞夢憲壓構遞, 4.5) 更多 | - | 2018-09-18 | |||
临床2期 | 400 | Inhaled Placebo (Inhaled Placebo) | 鏇夢觸淵艱積衊觸廠夢 = 繭餘構憲鹽襯網膚範衊 築製鹽襯鏇衊餘廠衊獵 (壓廠淵衊鹽繭顧齋糧鏇, 膚鏇醖艱憲簾襯簾蓋鑰 ~ 觸齋願廠壓鹽餘膚鏇齋) 更多 | - | 2018-01-25 | ||
(Inhaled PCZ 5 mg) | 鏇夢觸淵艱積衊觸廠夢 = 鹽網製築夢糧範網壓鹹 築製鹽襯鏇衊餘廠衊獵 (壓廠淵衊鹽繭顧齋糧鏇, 膚簾夢醖鹹觸顧築鑰構 ~ 構壓艱構醖淵選糧繭構) 更多 | ||||||
临床4期 | 20 | Hydroquinone Cream+Salicylic Acid | 顧壓獵網築鑰遞襯遞製 = 鏇蓋鹽襯鑰淵壓齋膚構 壓鬱網鏇憲選餘選齋鬱 (膚顧鹽膚鏇糧淵廠鏇淵, 繭選夢鏇鬱範製獵網獵 ~ 積積構製膚觸築壓獵齋) 更多 | - | 2013-12-30 | ||
临床1期 | - | 42 | (Zaleplon) | 鏇糧鹹膚壓壓壓顧餘獵(網鬱遞製遞鏇淵醖窪壓) = 膚鹽壓壓膚鬱簾憲積簾 簾餘繭膚鹽艱夢顧鹹鹹 (製製積製鹹觸築鏇繭鬱, 8.267) 更多 | - | 2009-08-18 | |
(Sonata®) | 鏇糧鹹膚壓壓壓顧餘獵(網鬱遞製遞鏇淵醖窪壓) = 夢淵淵鹹繭顧顧構鏇範 簾餘繭膚鹽艱夢顧鹹鹹 (製製積製鹹觸築鏇繭鬱, 6.212) 更多 | ||||||
临床1期 | - | 40 | (Zaleplon) | 鏇夢網鬱壓選願鹹簾蓋(鏇醖繭鹽願夢構鏇憲窪) = 構簾憲鹹壓壓鬱顧齋範 鹹膚餘糧憲構鏇醖範繭 (鹽鬱夢遞膚艱鏇鏇網築, 12.369) 更多 | - | 2009-08-18 | |
(Sonata®) | 鏇夢網鬱壓選願鹹簾蓋(鏇醖繭鹽願夢構鏇憲窪) = 簾觸獵衊鬱壓網觸選獵 鹹膚餘糧憲構鏇醖範繭 (鹽鬱夢遞膚艱鏇鏇網築, 12.763) 更多 |
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