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zolpidem tartrate (Intermezzo / zolpidem, TransOral)

✓ Approved

Transcept Pharmaceuticals · GABRA1 · Small Molecule

What is zolpidem tartrate?

zolpidem tartrate is a small molecule developed by Transcept Pharmaceuticals. It is approved for therapeutic indications via oral (po) or sublingual (sl)/oral transmucosal.

Drug Profile

Brand NamesIntermezzo, zolpidem, TransOral
CompanyTranscept Pharmaceuticals
Drug ClassSmall Molecule
Molecular TargetGABRA1
RouteOral (PO), Sublingual (SL)/Oral Transmucosal
StatusApproved

Mechanism of Action

Molecular Targets

zolpidem tartrate acts on 1 molecular target:

GABRA1gamma-aminobutyric acid type A receptor alpha1 subunit (DEE19, ECA4)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

zolpidem tartrate is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Psychiatric disordersInsomnia✓ Approved

Related Research Articles

PubMedFrontiers in pharmacology2026-09-18

Cross national pharmacovigilance analysis of drug-induced delirium: a comparative study using the US FAERS, Japanese JADER, and canadian CVAR datasets.

Jiao Jinghua J, Liu Shunming S, Fang Ying Y, Song Xin X et al.

Drug-induced delirium is a clinically important and potentially preventable adverse event, especially in older adults, yet large-scale cross-national pharmacovigilance evidence remains limited. We conducted a retrospective analysis using three major spontaneous reporting systems: the FDA Adverse Event Reporting System (FAERS, 2004-Q3 2025), the Japanese Adverse Drug Event Report (JADER, 2004-Q2 2025), and the Canada Vigilance Adverse Reaction database (CVAR, 2004-Q3 2025). Delirium cases were identified using five pre-specified Preferred Terms (PTs) selected from the narrow scope of the Standardised MedDRA Query (SMQ) Noninfectious encephalopathy/delirium. Disproportionality analyses were performed using reporting odds ratio, proportional reporting ratio, and empirical Bayes geometric mean, with signal strength defined by lower confidence bounds. Time-to-onset (TTO) was summarized using medians, IQRs, and early-onset proportions. A total of 263,327 reports were identified (FAERS: 243,572; JADER: 7,512; CVAR: 12,243). Delirium was more frequently reported in females (49%-57%) and individuals aged ≥60 years (55%-70%). Strong and consistent signals were observed for nervous system drugs, particularly psycholeptics, analgesics, and psychoanaleptics. Duloxetine, lamotrigine, pregabalin, quetiapine fumarate, and zolpidem demonstrated consistent signals across databases. Additional signals involved antipsychotics, benzodiazepines, opioids, and selected anti-infective agents. Time-to-onset analysis demonstrated early-onset clustering, suggesting an acute temporal pattern. Cross-database consistency in drug class signals and early-onset temporal patterns highlights the need for medication review and risk mitigation in high-risk populations.

PubMedJournal of bone metabolism2026-09-18

Differential Effects of Psychogenic Stress on Bone Morphology and Metabolism in Wistar Rats.

Lee Sangun S, Tatehana Haruka H, Saito Takumi T, Sugimoto Issei I et al.

Psychogenic stress (PS) significantly contributes to the development of various pathological conditions, including psychiatric, cardiovascular, and metabolic disorders. Furthermore, PS has been shown to influence bone health. In this study, we aimed to elucidate PS effects on bone morphology and metabolism during distinct developmental periods in male Wistar rats. PS was induced by combined restraint and water immersion stress for 3 hr per day over 4 weeks. In the end of the experiment, femora and tibiae were analyzed to determine bone length, cross-sectional area, and bone mass. Internal organ weights were also recorded. Bone-specific alkaline phosphatase and tartrate-resistant acid phosphatase activities were measured as markers of bone formation and resorption, respectively. Data were analyzed using the Student's ttest and Scheffé's multiple comparison test. PS significantly reduced body and organ weights at all developmental stages, indicating systemic growth suppression. The degree of stress-induced alterations in bone metabolism differed depending on the developmental stage: PS during growth impaired bone formation and enhanced resorption. Our findings demonstrate that PS exerts stage-specific effects on skeletal development and maintenance. The results highlight the importance of considering developmental stage in evaluating the impact of PS on bone health and suggest potential mechanisms linking chronic stress exposure to altered bone metabolism and increased risk of osteoporosis.

PubMedInternational journal of molecular sciences2026-09-15

Role of the Amygdala in the Complex Relationship Between Sleep and Anxiety.

Grzybowski Filip F, Kaczmarski Piotr P, Strzelecki Dominik D, Wysokiński Adam A et al.

This review explores the multifaceted roles of the amygdala, focusing on its structural components, projections, physiological aspects, and key functions in emotional processing and fear conditioning. Beyond traditional roles, it examines the amygdala's involvement in sleep architecture during the NREM and REM phases. In NREM sleep, the amygdala is involved in memory replay and encoding. During REM sleep, it is highly active, contributing to the emotional content of dreams. This state is characterized by increased cerebral blood flow to the amygdaloid complexes and the generation of Ponto-Geniculo-Occipital (PGO) waves, which are linked to vivid visual imagery and emotional experiences. The review establishes a critical link between the amygdala and the cycle of anxiety disorders and sleep disturbances. It explores anxiety disorders' specific impact on the amygdala and their influence on sleep patterns. Additionally, the review discusses how medications for anxiety disorders and sleep disturbances act on the amygdala. Selective serotonin reuptake inhibitors (SSRIs) regulate amygdala function, affecting emotional responses and connectivity patterns, improving anxiety, and potentially enhancing sleep quality over time. Trazodone, a serotonin antagonist and reuptake inhibitor (SARI), improves sleep by blocking serotonin receptors and is effective in treating post-traumatic stress disorder (PTSD) related sleep disturbances. Benzodiazepines and zolpidem affect sleep architecture and anxiety by selectively enhancing the actions of both endogenous and exogenous GABA through GABA-A receptors. At the same time, agomelatine, an antidepressant with anxiolytic properties, improves sleep quality without disrupting REM sleep and treats insomnia associated with various conditions, including alcohol dependence. The aim of this review is to summarize amygdala functions, with a focus on their role in regulating sleep and affective responses. Moreover, it discusses possible therapeutic targets in the amygdala for anxiety and sleep disorders.

PubMedInternational journal of molecular sciences2026-09-15

Microbial-Derived Daidzin (Eco-3) Suppresses RANKL-Induced Osteoclastogenesis by Targeting the TBK1-NFATc1 Signaling Axis.

Perumal Nivethasri Lakshmana NL, Koo Kyung-Bon KB, Park Gi-Young GY, Jang Byeong-Churl BC

Eco-3, a microbial-derived daidzin, has been reported to possess diverse biological activities; however, its effects on osteoclast differentiation and the underlying molecular mechanisms remain unclear. In the present study, we investigated the effects of Eco-3 on receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and explored the signaling pathways involved using RAW264.7 macrophages. Eco-3 suppressed RANKL-induced osteoclast formation at the concentrations tested without significantly affecting cell viability. Eco-3 also altered F-actin organization and reduced the expression of key osteoclastogenic markers, including tartrate-resistant acid phosphatase (TRAP), nuclear factor of activated T cells c1 (NFATc1), c-Fos, and cathepsin K (CTSK). In particular, Eco-3 attenuated NFATc1 expression during the early stage of osteoclast differentiation, suggesting interference with the transcriptional program associated with osteoclastogenesis. Furthermore, RANKL stimulation progressively increased TANK-binding kinase 1 (TBK1) phosphorylation during osteoclast differentiation, whereas Eco-3 attenuated this activation. Genetic silencing of TBK1 suppressed osteoclast formation, while pharmacological inhibition of TBK1 reduced TBK1 phosphorylation, osteoclastogenic gene expression, and osteoclast formation. Collectively, these findings suggest that Eco-3 suppresses RANKL-induced osteoclastogenesis, at least in part, through modulation of the TBK1-NFATc1 signaling axis in RAW264.7 macrophages. Our findings identify TBK1 as a potential regulatory component of osteoclast differentiation and suggest that Eco-3 warrants further investigation as a potential bioactive candidate for osteoclast-related bone disorders.

PubMedBiology2026-09-15

CD226 Deficiency Attenuates Periodontal Bone Destruction in a Murine Ligature-Induced Periodontitis Model.

Li Yi Y, Zhou Wenjing W, Chen Xutao X, Dan Wenli W et al.

Periodontal disease is widely recognised as a chronic infectious-inflammatory disorder, leading to the destruction of alveolar bone. Osteoclasts and their progenitors have been demonstrated to play pivotal roles in the process of periodontitis-induced bone damage. The mechanisms that govern the differentiation of osteoclasts in the context of periodontitis remain to be elucidated. In this study, we assessed the expression of CD226 on osteoclasts and their progenitors, as well as the function of CD226 in experimental periodontitis mice. Periodontitis was induced in C57BL/6 wild-type and CD226 knockout (CD226-KO) mice. Micro-CT was used to analyse bone loss. Haematoxylin-eosin (HE) or tartrate-resistant acid phosphatase (TRAP) staining was conducted to examine osteoclast differentiation. Flow cytometric analysis and quantitative real-time PCR (qRT-PCR) were used to identify the expression of CD226 and related molecules. The expression of CD226 on osteoclasts was found to decrease gradually during the process of osteoclastogenesis. In addition, the study revealed that the knockout of CD226 inhibited osteoclast differentiation in vitro. Furthermore, the knockout of CD226 has been demonstrated to attenuate inflammatory responses and alleviate bone damage in a murine periodontitis model. The present study suggests that CD226 plays an important role in regulating the function and differentiation of osteoclasts and their progenitors. The targeting of CD226 has the potential to be developed as a potent therapy for bone loss caused by periodontitis.

PubMedPoultry science2026-09-15

Phosphorus alleviates age-associated osteoporosis in laying hens by reshaping bone metabolism and modulating cecal microbial communities.

Guan Kai K, Xiao Yu Y, Xu Changchun C, Zhang Haijun H et al.

Osteoporosis in aged laying hens poses a major constraint on long-term egg production system. This study investigated the efficacy and underlying mechanisms of dietary phosphorus (P) in alleviating age-associated osteoporosis. A completely randomized design was employed, with 300 Hy-Line Brown laying hens (58 weeks of age) randomly assigned to one of three dietary treatments: a low-phosphorus diet (LP, 0.12% non-phytate phosphorus [NPP]), a regular-phosphorus diet (RP, 0.32% NPP), or the LP diet supplemented with 10,000 FTU/kg phytase (PHY, 0.12% NPP). Each treatment comprised 10 replicates of 10 hens. Following a 2-week adaptation period, the experiment lasted for 12 weeks. The results showed that dietary P reduction or phytase supplementation had no significant effect (P > 0.05) on egg production performance or egg quality throughout the experimental phase. However, at the end of the trial, hens fed the LP diet exhibited significantly lower serum P concentration and alkaline phosphatase (ALP) activity, along with reduced tibial P and magnesium (Mg) contents (P < 0.05), compared with the RP group. Conversely, serum calcium (Ca) level and tartrate-resistant acid phosphatase (TRACP) activity were significantly elevated in the LP group (P < 0.05). In contrast, phytase supplementation in the PHY group significantly increased serum ALP activity and tibial P and Mg contents relative to the LP group (P < 0.05). Notably, the PHY group also showed higher serum Ca concentration than the RP group (P < 0.05). Histomorphological examination revealed progressive cortical bone thinning accompanied by irregular erosion and increased demineralized areas in the tibiae of LP-fed hens, whereas only mild pathological changes were observed in the PHY group. Analysis of cecal microbiota indicated that dietary P modulation significantly altered microbial community structure: principal coordinate analysis (PCoA) showed distinct clustering for the LP and PHY group at week 8 and week 12, respectively (P < 0.05). Linear discriminant analysis effect size (LEfSe) further revealed that the LP group was enriched with pro-inflammatory taxa and microbes associated with nutrient metabolism stress. The RP group harbored a more complex and diverse microbial community, while the PHY group was characterized by an enrichment of beneficial bacteria involved in short-chain fatty acid (SCFA) production. Spearman correlation analysis demonstrated significant associations between specific bacterial genera and tibial health parameters. Genera such as Phascolarctobacterium, Rikenellaceae_RC9_gut_group, and Bacteroides were positively correlated with tibial mineral content and structural integrity, whereas Lactobacillus, Olsenella, and Prevotellaceae_Ga6A1_group showed negative correlations with these bone traits (P < 0.05). Collectively, these findings indicate that chronic P deficiency induces severe skeletal deterioration and gut microbiota dysbiosis in aged laying hens. Phytase supplementation partially counteracts the adverse effects of low-P diet by improving P utilization and reshaping the cecal microbiota toward a more beneficial composition. Nevertheless, long-term feeding of P-deficient diet even with phytase remains insufficient to fully preserve skeletal health. Therefore, ensuring adequate dietary P supply is essential for alleviating age-associated osteoporosis in aged laying hens, likely through integrated regulation of bone metabolic homeostasis and gut microbial ecology.

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