北京若生智能科技有限公司
Drug Database
DI

diazepam (Stesolid / diazepam, Alpharma)

✓ Approved

Pfizer, Inc. · GABRA1 · 小分子

什么是 diazepam？

diazepam 是一种小分子，由Pfizer, Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Rectal。

药物档案

商品名Stesolid, diazepam, Alpharma
公司Pfizer, Inc.
药物类别小分子
分子靶点GABRA1, GABRA2, GABRA3, GABRA5
给药途径Rectal
状态Approved
来源： ClinicalTrials.gov, Pfizer, Inc.

作用机制

分子靶点

diazepam 作用于 4 个分子靶点：

GABRA1gamma-aminobutyric acid type A receptor alpha1 subunit (DEE19, ECA4)
GABRA2gamma-aminobutyric acid type A receptor alpha2 subunit (DEE78, EIEE78)
GABRA3gamma-aminobutyric acid type A receptor alpha3 subunit (EPILX2)
GABRA5gamma-aminobutyric acid type A receptor alpha5 subunit (EIEE79, DEE79)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

diazepam 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersAnxiety✓ Approved
Nervous system disordersEpilepsy✓ Approved

相关研究文献

PubMedFrontiers in human neuroscience2026-09-11

Reduced intra-frontal functional connectivity during a verbal fluency task in depressed individuals with autistic traits: an fNIRS study.

Koeda Michihiko M, Hosokawa En E, Kumagai Akihiro A, Ishikawa Yuki Y et al.

Depressive symptoms accompanied by autistic traits represent an important source of clinical heterogeneity. While aberrant functional connectivity (FC) within prefrontal networks has been implicated as a shared neural feature of both autism spectrum disorder (ASD) and depression, task-evoked FC abnormalities in individuals experiencing both remain poorly understood. This study employed functional near-infrared spectroscopy (fNIRS) to evaluate task-evoked FC during a verbal fluency task (VFT), with a focus on prefrontal network organization. Fifty neurotypical controls and 43 individuals experiencing depressive symptoms were enrolled. The depressive-state cohort was further subdivided into high autistic traits (DP_AQ-high) and low autistic traits (DP_AQ-low) subgroups based on Autism-Spectrum Quotient (AQ) scores. FC among channels in frontal, temporal, and inferior parietal regions was calculated using zero-lag Pearson correlation analysis of oxyhemoglobin (HbO₂) and deoxyhemoglobin (HbR) signals during the VFT. Between-group FC differences were evaluated using ANOVA for the Control versus depressive-state comparison, and medication-adjusted ANCOVA for the DP_AQ-high versus DP_AQ-low comparison, with diazepam-equivalent anxiolytic dosage and imipramine-equivalent antidepressant dosage as covariates. Relative to neurotypical controls, the depressive-state group exhibited decreased interhemispheric frontal FC across both chromophores, alongside network-specific FC increases and decreases. Within the depressive-state group, the DP_AQ-high subgroup consistently demonstrated increased interhemispheric frontoparietal FC across both chromophores, accompanied by localized intra-frontal FC reductions, compared with the DP_AQ-low subgroup. These findings suggest that autistic traits modulate task-evoked large-scale network organization within a clinically relevant depressive-state cohort and support the utility of fNIRS-based network analysis for characterizing neurobiological heterogeneity associated with depressive symptoms.

PMID 42724125
阅读全文 →
PubMedJournal of clinical sleep medicine : JCSM : official publication of the American Academy of Sleep Medicine2026-09-10

Dual orexin receptor antagonist-assisted dose reduction of benzodiazepines and benzodiazepine receptor agonists: a mirror-image analysis of insurance claims data.

Matsui Kentaro K, Sugiura Ko K, Shimura Akiyoshi A, Takagi Shunsuke S et al.

Discontinuing benzodiazepines and benzodiazepine receptor agonists (BZ/BZRAs) remains challenging for patients with chronic insomnia despite safety concerns. This study evaluated whether continuous treatment with dual orexin receptor antagonists (DORAs) facilitates a reduction in BZ/BZRA doses among long-term users. This self-controlled (mirror-image) study, in which each patient served as their own control, used Japanese health insurance claims data (Dokenpo database, 2019-2024). Eligible patients had continuous BZ/BZRA use for ≥ 6 months and initiated suvorexant or lemborexant for ≥ 6 months. Changes in bedtime BZ/BZRA dose (diazepam equivalents) were compared between pre- and post-DORA periods. Logistic regression analyses identified factors associated with ≥ 50% dose reduction and BZ/BZRA discontinuation. Prior to DORA initiation, 605 patients were taking a mean of 1.9 ± 1.0 types of BZ/BZRAs at a pretreatment total daily dose of 8.2 ± 7.4 mg diazepam equivalent. Of these, 42.1% achieved ≥ 50% bedtime BZ/BZRA dose reduction and 21.3% achieved discontinuation. Mean bedtime doses decreased in both the suvorexant group (7.2 to 5.2 mg) and the lemborexant group (8.3 to 5.2 mg). In adjusted analyses, age ≥ 65 years was independently associated with both ≥ 50% reduction (odds ratio [OR] 2.485; 95% confidence interval [CI] 1.190-5.192; p = 0.015) and discontinuation (OR 2.636; 95% CI 1.158-6.000; p = 0.021). Lower pretreatment BZ/BZRA dose and lemborexant use were also associated with dose reduction and discontinuation. DORA treatment for at least six months may support BZ/BZRA dose reduction among long-term users, particularly in older patients. Discontinuing benzodiazepine and benzodiazepine receptor agonists (BZ/BZRAs) in patients with long-term use remains clinically challenging despite well-documented safety concerns. Whether sustained treatment with dual orexin receptor antagonists (DORAs) facilitates BZ/BZRA dose reduction in real-world practice has not been adequately examined in patients already exposed for six months or longer. Sustained DORA treatment for at least six months was associated with substantial bedtime BZ/BZRA dose reduction and discontinuation among long-term users, with older adults (aged 65 years or older) showing the highest odds of success. These findings support DORA co-administration as a practical pharmacological switching strategy to enable safer insomnia management, particularly in populations vulnerable to BZ/BZRA-related adverse events.

PMID 42717137
阅读全文 →
PubMedCureus2026-09-10

Ileal Perforation Caused by the Accidental Ingestion of a Press-Through Package in an Elderly Patient With Dementia: A Case Report.

Inoue Takahiro T, Kobayashi Hiroaki H

A woman in her 90s who lived alone and had a history of unspecified dementia and pulmonary tuberculosis presented with a four-day history of lower abdominal pain. Her only regular medication was diazepam, which she dispensed from a press-through package (PTP) and had been cutting individual tablets from the sheet using scissors. Upon admission, she was hypothermic (body temperature 34°C), with otherwise preserved vital signs (blood pressure 131/65 mmHg, heart rate 79 beats/min, SpO₂ 98% on room air). She had no recollection of having swallowed a PTP. Laboratory findings showed a markedly elevated C-reactive protein level of 32.58 mg/dL, severe hypoalbuminemia (albumin 2.4 g/dL), and mild metabolic acidosis (pH 7.300, HCO₃⁻ 17.6 mmol/L) on arterial blood gas analysis. Abdominal computed tomography (CT) revealed a high-density object surrounded by a low-density halo in the ileum approximately 10 cm proximal to the ileocecal valve, along with localized free air and abscess formation in the right lower abdomen, consistent with a PTP-induced ileal perforation. Emergency laparotomy revealed a spindle-shaped ileal perforation, with an intact PTP sheet partially extruding through the defect. An abscess had formed between the abdominal wall and the bowel at the perforation site. Primary repair, omental reinforcement, and peritoneal lavage with drainage were performed without bowel resection or stoma creation. The patient recovered without complications and was discharged on postoperative day 15. This case illustrates two key points: the characteristic CT appearance of a retained PTP can confirm the diagnosis even without an ingestion history, and occult PTP ingestion should be considered in elderly patients with dementia who present with acute abdomen, irrespective of whether an ingestion history can be elicited.

PMID 42719370
阅读全文 →
PubMedFood science & nutrition2026-09-10

Mechanistic Study of Schisandrin B in Alleviating Anxiety-Like Behaviors in Rats via Enhancement of Hippocampal Synaptic Plasticity and Restoration of the Intestinal Barrier.

Tian Jia-Yu JY, Wang Rui-Ze RZ, Wang Hong-Kun HK, Ye Xiao-Nan XN et al.

This study focused on examining the anxiolytic effects of Schisandrin B (SchB) in rats exhibiting anxiety-like behaviors and investigating the mechanisms involved. Behavioral assessments were conducted using the elevated plus-maze test and the open field test. The results showed that Schisandrin B at a dose of 10 mg/kg significantly alleviated anxiety-like behaviors in rats, with an efficacy comparable to that of the positive control drug diazepam. Mechanistic studies indicate that, at the central level, Schisandrin B effectively maintains the homeostasis of the glutamatergic system in the hippocampus and the HPA axis. Specifically, Schisandrin B downregulates the stress-induced overexpression of ionotropic glutamate receptor subunits at both the mRNA and protein levels, including NMDAR subtypes (GluN1A, GluN2A, and GluN2B) and AMPAR subtypes (GluA1 and GluA2), thereby restoring the glutamate/γ-aminobutyric acid (Glu/GABA) ratio to physiological levels. In addition, Schisandrin B suppresses the hyperactivation of the HPA axis by reducing the secretion of corticotropin-releasing hormone (CRH), adrenocorticotropic hormone (ACTH), and corticosterone (CORT). Meanwhile, it ameliorates neuronal and synaptic ultrastructural damage in the hippocampus and upregulates the expression of synaptic plasticity-related proteins, SYP and PSD-95, thereby improving synaptic transmission and function. At the peripheral intestinal level, Schisandrin B alleviated colon shortening in anxiety-model rats and reduced fecal pH, thereby improving intestinal environmental homeostasis. Schisandrin B also promoted the upregulation of tight junction proteins (ZO-1, Occludin, and Claudin-1) in the colonic tissues, contributing to the restoration of colonic mucosal integrity, attenuation of inflammatory infiltration, and reinforcement of intestinal barrier function. Collectively, Schisandrin B exerts systemic anxiolytic effects by centrally regulating hippocampal glutamatergic neurotransmission, HPA axis activity, and synaptic plasticity, while simultaneously repairing peripheral intestinal barrier dysfunction. These results indicate the potential of Schisandrin B as a therapeutic candidate for anxiety disorders.

PMID 42718869
阅读全文 →
PubMedEmergency medicine Australasia : EMA2026-09-09

Toxicological and Clinical Characteristics of Fatal Cases in the Emerging Drugs Network of Australia-Victoria (EDNAV) Clinical Registry 2020-2025.

White James J, Hampton Sarah J SJ, Greene Shaun S

The objective of this study is to characterise the analytical toxicology findings and clinical features of fatal cases recorded in the Emerging Drugs Network of Australia-Victoria (EDNAV) clinical registry. EDNAV is a state-wide toxicosurveillance system capturing de-identified demographic, clinical and analytical data from ED presentations with illicit drug-related toxicity. Venous blood samples are screened for illicit, pharmaceutical and novel psychoactive substances (NPS) using liquid chromatography-quadrupole time-of-flight mass spectrometry. We conducted a retrospective observational case series of fatal registry cases recorded between September 2020 and December 2025. Forty-six fatal cases were identified (0.9% of 5026 EDNAV cases). Most patients were male (89%) with a median age of 33 years. Out-of-hospital cardiac arrest occurred in 67% of cases. Polysubstance exposure predominated (91%), with a median of three substances detected per case. Mixed stimulant-sedative patterns were most common (64%), followed by opioid-benzodiazepine (19%) and stimulant-only (7%). The most frequent individual detections were methamphetamine (54%), heroin (52%), diazepam (37%), cocaine (20%) and MDMA (17%). NPS accounted for 7.8% of detections, were never identified in isolation and were predominantly novel benzodiazepines (80%). Hypoxic brain injury was the most common terminal complication (72%). Fatal cases were characterised by near-universal polysubstance detections, with methamphetamine and heroin the most frequent individual detections. Most deaths occurred out of hospital, with many patients presenting with irreversible hypoxic brain injury. NPS were rare and co-occurred with traditional illicit substances. Community-based interventions including bystander resuscitation, early emergency service activation and take-home-naloxone represent the highest-yield strategies to reduce mortality from illicit substance use in Victoria.

PMID 42716535
阅读全文 →
PubMedJournal of pain & palliative care pharmacotherapy2026-09-08

Tizanidine Withdrawal Syndrome: Clinical Manifestations and Management Strategies. Case Series.

AlAttar Emad E, AlRawi Farook F, Rafique Samaira S

Tizanidine, an imidazole derived α2 adrenergic agonist, is widely prescribed for spasticity and chronic musculoskeletal pain. Abrupt discontinuation can precipitate withdrawal syndromes characterized by sympathetic overactivity. Although pharmacologically plausible, this phenomenon is potentially underreported in clinical practice. We describe four patients with diverse comorbidities who developed acute tizanidine withdrawal. All cases were directly observed at a single tertiary care center and identified during routine inpatient clinical practice over a defined timeline. Case 1 was a 24 year old female admitted with empagliflozin induced diabetic ketoacidosis who experienced hypertensive crisis and tachycardia following abrupt cessation of chronic high dose tizanidine. Case 2 was a 29 year old female with Crohn's disease who developed tremors, anxiety, and autonomic instability after reducing her regimen from 40 mg nightly to 16 mg daily. She had self-discontinued her last dose prior to presentation. Case 3 was a 29 year old female with recurrent pancreatitis, resistant hypertension, and an adrenal incidentaloma who presented with severe hypertension and tremors after discontinuing both tizanidine and diazepam. Symptoms began within approximately 24 h of abrupt cessation. Case 4 was a 42 year old male with asthma, hypertension, anxiety disorder, bariatric surgery, methamphetamine use, and more than ten prior admissions specifically for tizanidine withdrawal, who presented with palpitations, tremors, vomiting, and hypertensive crisis after abrupt dose reduction. In all cases, reintroduction of tizanidine followed by a structured tapering regimen resulted in clinical stabilization. These cases highlight the clinical significance of tizanidine withdrawal, its diverse presentations, and the importance of cautious tapering. Patient education on avoiding abrupt discontinuation is essential, particularly for individuals with psychiatric comorbidities or prior withdrawal episodes. Awareness of this underrecognized syndrome is critical to prevent misdiagnosis and ensure safe prescribing practices.

PMID 42709596
阅读全文 →

注册免费账户还可查看另外 9996 篇文献

免费注册查看全部文献 →

了解更多diazepam