更新于：2024-11-15
Zaleplon
扎来普隆
更新于：2024-11-15
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 + [16] |
作用机制 GABAA receptor调节剂(γ-氨基丁酸 A 受体调节剂) |
治疗领域 |
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
分子式C17H15N5O |
InChIKeyHUNXMJYCHXQEGX-UHFFFAOYSA-N |
CAS号151319-34-5 |
关联
20
项与 扎来普隆 相关的临床试验Study on effect of zaleplon capsules on subjective sleep quality and daytime function in patients with insomnia
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
Impact of a Digital Solution (CardiCare™) on Cardiorespiratory Fitness Improvement in Patients Discharged From a Phase 2 Cardiac Rehabilitation Following an Acute Coronary Syndrome
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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681
项与 扎来普隆 相关的文献（医药）2024-10-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Synthesis and characterization of cellulose fibers modified zinc phosphate/hydroxyapatite core-shell as enhanced carrier of cisplatin: Loading, release, and cytotoxicity
Article
作者: Bin Jumah, May N ; Al Othman, Sarah I ; Allam, Ahmed A ; Abukhadra, Mostafa R ; Alomari, Awatif Abdulaziz
The uncontrolled administration of the cisplatin drug (CPTN) resulted in numerous drawbacks. Therefore, effective, affordable, and biocompatible delivery systems were suggested to regulate the loading, release, and therapeutic effect of CPTN. Zinc phosphate/hydroxyapatite hybrid form (ZP/HP) and core-shell nano-rod morphology, as well as its functionalized derivative with cellulose (CF@ZP/HP), were synthesized by the facile dissolution precipitation method followed by mixing with cellulose fibers, respectively. The developed CF@ZP/HP displayed remarkable enhanced CPTN loading properties (418.2 mg/g) as compared to ZP/HP (259.8 mg/g). The CPTN loading behaviors into CF@ZP/HP follow the Langmuir isotherm properties (R2 > 0.98) in addition to the kinetic activities of the pseudo-first-order model (R2 > 0.96). The steric assessment validates the notable increase in the existing loading receptors after the functionalization of ZP/HP with CF from 57.7 mg/g (ZP/HP) to 90.5 mg/g. The functionalization also impacted the capacity of each existing receptor to be able to ensure 5 CPTN molecules. This, in addition to the loading energies (<40 kJ/mol), donates the loading of CPTN by physical multi-molecular processes and in vertical orientation. The CPTN releasing patterns of CF@ZP/HP exhibit slow and controlled properties (95.7 % after 200 h at pH 7.4 and 100 % after 120 h at pH 5.5), but faster than the properties of ZP/HP. The kinetic modeling of the release activities together with the diffusion exponent (>0.45) reflected the release of CPTN according to both erosion and diffusion mechanisms. The loading of CPTN into both ZP/HP and CF@ZP/HP also resulted in a marked enhancement in the anticancer activity of CPTN against human cervical epithelial malignancies (HeLa) (cell viability = 5.6 % (CPTN), 3.2 % (CPTN loaded ZP/HP), and 1.12 % (CPTN loaded CF@ZP/HP)).
2024-07-01Journal of addiction medicine
Z-Drug Use and Benzodiazepine Use and Misuse Among LGB Populations: The Role of Psychological Distress
Article
作者: Fidalgo, Thiago M ; Martins, Silvia S ; Tardelli, Vitor S
Background:
Z-drugs (hypnotics such as zolpidem, zopiclone, and zaleplon) and benzodiazepines (BZDs) are sedative medications with misuse liability. The goals of this study are to report the (1) prevalence of past-year any Z-drug use, any BZD use, and any BZD misuse by sexual identity category and psychological distress; (2) associations among these 3 categories between sexual identity and past-year psychological distress; (3) associations among these 3 categories with sexual identity by past-year psychological distress status.
Methods:
Data were collected from the National Survey on Drug Use and Health (years 2015–2019 [n = 210,392]), a yearly representative national household survey of the American population. We report prevalences of any Z-drug use, any BZD use, and any BZD misuse by sexual identity and past-year psychological distress status. We ran logistic regressions with complex survey design with the 3 dichotomous variables described above as the dependent variables, stratified and not-stratified by psychological distress.
Results:
Prevalence of any Z-drug an BZD use and any BZD misuse were higher among LGB (lesbian/gay/bisexual) populations, especially gay men and bisexual women. Psychological distress was positively associated with any Z-drug and BZD use and any BZD misuse. Women were at higher risk of Z-drug (odds ratio [OR], 1.27; 95% confidence interval [CI], 1.18–1.37) and BZD use (OR, 1.64; 95% CI, 1.55–1.73), but lower risk of BZD misuse (OR, 0.82; 95% CI, 0.76–0.88). When stratifying by psychological distress, differences between LGB and heterosexuals were more pronounced among those without past-year psychological distress, especially gay men and bisexual women.
Conclusions:
The presence of psychological distress attenuates the disparities between LGB and heterosexual individuals in Z-drug use and BZD use and misuse.
2024-04-01Epilepsia
Pharmacokinetics of Staccato® alprazolam in healthy adult participants in two phase 1 studies: An open‐label smoker study and a randomized, placebo‐controlled ethnobridging study
Article
作者: Chanteux, Hugues ; King, Aliceson ; Roebling, Robert ; Rospo, Chiara ; Bartmann, Ana Paula ; Hayakawa, Yoshinobu
Abstract:
Objective:
Staccato® alprazolam is a single‐use, drug–device combination delivering alprazolam to the deep lung that is being evaluated as treatment for rapid and early seizure termination. This article reports pharmacokinetic (PK) data from two phase 1 studies of Staccato alprazolam in healthy adult participants.
Methods:
The smoker study (EPK‐002/NCT03516305) was an open‐label, nonrandomized, single‐dose, PK study in smokers and nonsmokers aged 21–50 years, administered a single inhaled dose of 1 mg Staccato alprazolam. The ethnobridging study (UP0101/NCT04782388) was a double‐blind, placebo‐controlled study in Japanese, Chinese, and Caucasian participants aged 18–55 years randomized 4:1 to a single inhaled dose of Staccato alprazolam 2 mg or Staccato placebo.
Results:
In the smoker study, 36 participants (18 smokers, 18 nonsmokers) were enrolled and received Staccato alprazolam. Following Staccato administration, alprazolam was rapidly absorbed, with a median time to peak drug plasma concentration (Tmax) of 2 min in both smokers (range = 2–30 min) and nonsmokers (range = 2–60 min). Staccato alprazolam was rapidly absorbed to a similar extent in both smokers and nonsmokers. The most commonly reported treatment‐emergent adverse events (TEAEs) were somnolence and dizziness. In the ethnobridging study, 10 participants each of Japanese, Chinese, and Caucasian ethnicities were randomized 4:1 to Staccato alprazolam or Staccato placebo. Following Staccato administration, alprazolam was rapidly absorbed and distributed, with a median Tmax of 1.5–2 min in Japanese (range = 1–2 min), Chinese (range = 1–34 min), and Caucasian (range = 1–120 min) participants. Somnolence and sedation were the most commonly reported TEAEs. In both studies, there were no deaths, and no participants reported serious or severe TEAEs, or discontinued due to TEAEs.
Significance:
Alprazolam was rapidly absorbed, and therapeutic drug levels were achieved within 2 min postdose when administered to the lung with the Staccato device. Staccato alprazolam was generally well tolerated and displayed a safety profile consistent with that known from other alprazolam applications. No new safety signals were identified.
100 项与 扎来普隆 相关的药物交易
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研发状态
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临床结果
适应症
分期
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N/A | 10 | 壓壓鹹窪淵構壓網窪範(遞廠艱鏇繭窪觸繭壓範) = 5 製積夢齋蓋餘積範觸窪 (壓膚餘夢鏇壓簾鑰鹽鬱 ) 更多 | 积极 | 2019-05-26 | |||
临床2期 | 20 | 淵繭醖鏇衊壓齋衊範鹹(蓋餘艱製窪齋窪鹽艱鬱) = 廠醖鑰鑰壓醖範觸製鏇 窪鏇淵齋鏇鹽鏇觸襯廠 (衊鏇夢遞簾淵選餘願鏇, 繭鬱選齋齋糧窪鑰選醖 ~ 廠淵簾遞艱顧夢鏇願鹹) 更多 | - | 2018-09-18 | |||
临床2期 | 400 | Inhaled Placebo (Inhaled Placebo) | 鑰選獵遞襯壓鹹衊壓築(壓淵繭蓋簾蓋範構築簾) = 顧願鹽膚範齋夢簾糧鬱 積壓壓醖襯鹽網廠糧簾 (遞鏇廠蓋鹹遞繭夢廠襯, 蓋糧構壓憲網窪顧壓鏇 ~ 繭獵鏇鏇遞壓淵鏇鹽齋) 更多 | - | 2018-01-25 | ||
(Inhaled PCZ 5 mg) | 鑰選獵遞襯壓鹹衊壓築(壓淵繭蓋簾蓋範構築簾) = 鏇蓋壓憲壓願選築窪醖 積壓壓醖襯鹽網廠糧簾 (遞鏇廠蓋鹹遞繭夢廠襯, 蓋衊廠蓋願醖築鹽觸壓 ~ 衊憲鹽網繭廠鑰範醖鬱) 更多 | ||||||
临床2期 | 75 | Staccato Placebo (Inhaled Placebo) | 網製淵積廠蓋遞鹽夢獵(餘範壓醖鏇鏇願鏇積衊) = 糧膚網選醖願壓窪窪醖 遞夢糧製衊窪夢繭獵壓 (獵齋衊衊積獵積範廠齋, 膚鏇觸壓餘鑰製願鏇簾 ~ 廠簾齋膚糧構繭範鏇憲) 更多 | - | 2018-01-25 | ||
(Inhaled PCZ 5 mg) | 網製淵積廠蓋遞鹽夢獵(餘範壓醖鏇鏇願鏇積衊) = 淵廠顧衊衊鬱艱鏇網積 遞夢糧製衊窪夢繭獵壓 (獵齋衊衊積獵積範廠齋, 鏇願膚壓築鏇構餘構襯 ~ 願選願製鏇淵鹹鹽壓範) 更多 | ||||||
临床4期 | 20 | Hydroquinone Cream+Salicylic Acid | 鑰願積繭鑰鏇繭遞蓋廠(築鬱壓範製襯餘壓觸艱) = 鹹憲廠築選鹹鑰製願網 醖鏇觸鹽構醖選觸蓋簾 (鏇艱遞醖繭鑰夢觸築製, 糧製構鹹艱鑰膚鬱觸簾 ~ 選遞夢繭顧製壓範淵構) 更多 | - | 2013-12-30 | ||
临床1期 | - | 42 | (Zaleplon) | 鏇蓋遞構膚廠選壓選餘(製鏇鏇築製顧糧製遞淵) = 顧夢繭網構壓鬱鹽築構 遞遞憲範範齋積觸糧繭 (夢憲選築廠膚糧範積選, 鹹膚觸糧蓋積膚構鏇網 ~ 簾鬱構遞糧壓簾壓觸選) 更多 | - | 2009-08-18 | |
(Sonata®) | 鏇蓋遞構膚廠選壓選餘(製鏇鏇築製顧糧製遞淵) = 簾範顧蓋積選壓廠獵憲 遞遞憲範範齋積觸糧繭 (夢憲選築廠膚糧範積選, 選鏇築鏇構鬱繭夢構遞 ~ 鹹衊襯簾繭壓憲壓憲觸) 更多 | ||||||
临床1期 | - | 40 | (Zaleplon) | 積網鬱壓範夢艱艱膚鏇(遞淵遞網網觸餘憲願鏇) = 蓋襯鏇觸範鬱築構願選 繭選積憲窪網餘網壓鹹 (蓋夢獵鑰襯糧鹽觸鑰鏇, 壓鹹願餘製觸網積簾鹽 ~ 艱簾夢願鹽醖鑰醖製淵) 更多 | - | 2009-08-18 | |
(Sonata®) | 積網鬱壓範夢艱艱膚鏇(遞淵遞網網觸餘憲願鏇) = 淵選願餘製淵願齋鹹夢 繭選積憲窪網餘網壓鹹 (蓋夢獵鑰襯糧鹽觸鑰鏇, 築醖網築鏇選窪積願鹹 ~ 醖繭壓鏇觸簾繭觸觸獵) 更多 |
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