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Drug Database
BE

benzodiazepine

✓ Approved

Valenta Pharm · 小分子 · 小分子

什么是 benzodiazepine？

benzodiazepine 是一种小分子，由Valenta Pharm研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

公司Valenta Pharm
药物类别小分子
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Valenta Pharm

治疗适应症

benzodiazepine 针对 1 个适应症，涉及 1 个治疗领域。

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

相关研究文献

PubMedBiomolecules2026-10-27

Mechanism-Dependent Effects of the α5 GABAA Receptor Negative Allosteric Modulator Basmisanil on Spatial Memory.

Moraru Miruna Valeria MV, Zugravu Aurelian A, Barbu Aurelia Cristiana AC, Stoleru Smaranda S et al.

Cognitive impairment may arise through multiple pathophysiological mechanisms, including altered GABAergic neurotransmission, cholinergic dysfunction, and neuroinflammation. This study investigated whether basmisanil, a selective negative allosteric modulator of α5-containing GABAA receptors, attenuates spatial memory impairment induced by diazepam, trihexyphenidyl (THP), or lipopolysaccharide (LPS). Adult male Wistar rats were assigned to three experimental models of memory impairment, each comprising four treatment groups (control, inducing agent, basmisanil, and inducing agent plus basmisanil; n = 7/group). Spatial memory was assessed using the two-trial Y-maze paradigm. The primary outcome (Time Index U) was analyzed using two-way factorial general linear models with sensitivity analyses. Significant interactions between the inducing agent and basmisanil were observed in the diazepam and LPS models, indicating attenuation of memory impairment following basmisanil coadministration, whereas no significant interaction was detected in the THP model. The largest estimated recovery effect was observed in the diazepam model, followed by the LPS model and the THP model, although cross-model comparisons were not statistically significant. Basmisanil alone did not enhance baseline memory performance. These findings indicate that the behavioral effects of α5-containing GABAA receptor modulation are mechanism-dependent and support further investigation of selective α5 negative allosteric modulators for benzodiazepine-associated memory impairment.

PMID 42939683
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PubMedJournal of clinical medicine2026-10-27

Zolpidem Intoxication Associated with Probable Reverse Stress-Induced Cardiomyopathy and QT Prolongation: A Case Report.

Byeon Hyeonbeom H, Choi Sehun S, Lee Jisook J, Yang Heewon H et al.

Zolpidem is a widely prescribed non-benzodiazepine hypnotic. A 49-year-old woman presented to the emergency department with altered mental status after intentional ingestion of approximately 300 mg of zolpidem; the blood zolpidem concentration was 674 µg/L approximately 8 h after ingestion. The initial ECG already showed QTc prolongation (499 ms). She developed chest discomfort and modest high-sensitivity troponin T elevation, and echocardiography showed transient left ventricular dysfunction (ejection fraction 42%) with basal-to-mid regional wall motion abnormalities and relative apical sparing, suggestive of probable reverse stress-induced cardiomyopathy. Coronary computed tomography angiography showed no coronary plaque or significant stenosis. On hospital day 2, telemetry captured a brief monomorphic ventricular run and QTc later peaked at 681 ms. Follow-up echocardiography on hospital day 5 showed recovery of left ventricular systolic function (LVEF 60%) and resolution of the regional wall motion abnormalities. These findings cannot be attributed solely to zolpidem. Stress may have contributed to the cardiomyopathy. Mild hypokalemia and left ventricular dysfunction may have reduced repolarization reserve. The peak QTc occurred after blood zolpidem concentrations had substantially decreased and may have reflected evolving stress-induced cardiomyopathy or concurrent exposure to cardiovascular medications. Cardiac evaluation and continuous monitoring should be considered when zolpidem intoxication is accompanied by cardiac symptoms, biomarker elevation, or ECG abnormalities.

PMID 42941460
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PubMedJournal of bronchology & interventional pulmonology2026-10-27

Comparison of the Safety and Efficacy of Remimazolam for Sedation in Adults Undergoing Fiberoptic Bronchoscopy: A Meta-Analysis of Randomized Controlled Trials.

Lee Soowon S, Na Hyo-Seok HS, Koo Bon-Wook BW, Joo Dong-Hyun DH et al.

Fiberoptic bronchoscopy requires effective sedation to ensure patient comfort while preserving gas exchange, hemodynamic stability, and predictable recovery. Remimazolam, a novel ultra-short-acting benzodiazepine, has emerged as a potential alternative to traditional sedatives. However, its safety and efficacy compared with those of other sedatives remain under investigation. This meta-analysis evaluated the safety and efficacy of remimazolam versus dexmedetomidine, midazolam, and propofol in adults undergoing fiberoptic bronchoscopy. A systematic review of randomized controlled trials (RCTs) was conducted using 5 databases through January 2026. Outcomes included respiratory depression, hypotension, bradycardia, time to target sedation depth, procedure success rate, emergence time, and postanesthesia care unit (PACU) stay. Relative risks (RR) or mean differences (MD) with 95% CI were calculated using a random-effects model. Sixteen RCTs (2325 patients) were included. Remimazolam significantly reduced respiratory depression (RR: 0.51, 95% CI: 0.36-0.73, P<0.001), hypotension (RR: 0.50, 95% CI: 0.34-0.73, P<0.001), and bradycardia (RR: 0.37, 95% CI: 0.22-0.65, P=0.001) versus controls. Sedation onset was faster than dexmedetomidine (MD: -2.19 min), but slower than propofol (MD: 0.49 min). Success rates were comparable across groups (RR: 1.12, 95% CI: 0.98-1.28, P=0.097). Compared with dexmedetomidine and midazolam, remimazolam shortened emergence (MD: -1.79 and -4.37 min, respectively) and PACU stay (MD: -3.58 and -6.70 min). Remimazolam provides effective sedation for fiberoptic bronchoscopy with advantages in terms of respiratory and hemodynamic safety, rapid recovery, and procedural efficiency.

PMID 42935012
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PubMedPharmaceuticals (Basel, Switzerland)2026-10-27

A Novel Lorazepam Orodispersible Film: Bioequivalence, Pharmacokinetic, and Tolerability Evaluation Compared with Film-Coated and Orodispersible Tablets in Two Randomized Crossover Studies in Healthy Subjects.

Frangione Valeria V, Sensi Cristina C, Radicioni Milko Massimiliano MM, Marra Fabio F et al.

Introduction: Lorazepam is a widely prescribed benzodiazepine available in multiple pharmaceutical formulations. A novel lorazepam orodispersible film (ODF) has been developed as an alternative dosage form designed to address administration challenges and enhance treatment adherence. Its pharmacokinetic profile, including the rate and extent of absorption, and its tolerability were evaluated in comparison with commercially available oral formulations in two bioequivalence studies. Methods: Two single-center, single-dose, open-label, randomized studies were conducted in healthy adults under fasting conditions. Study A was a three-way crossover pilot study comparing lorazepam 2.5 mg ODF (test, T) with film-coated tablets (Tavor®, reference 1, R1) and orodispersible tablets (Tavor® ORO, reference 2, R2). Study B was a two-way crossover pivotal study comparing T with R1. Treatments were separated by washout periods of ≥7 days. Pharmacokinetic parameters and point estimates (PEs), expressed as the ratios of least-squares geometric means (T/R1 and T/R2), were assessed. Results: In both studies, lorazepam pharmacokinetic profile was comparable across formulations, with similar Cmax and area under the curve (AUC) values. Peak concentrations were reached within 1-1.5 h for all treatments, and the elimination half-life was approximately 15-16 h. The 90% CIs for Cmax, AUC0-t, and AUC0-∞ for T versus R1 and R2 were within the 80-125% bioequivalence range. All treatments were well tolerated, with somnolence being the most frequent adverse event. Conclusions: Lorazepam 2.5 mg ODF demonstrated bioequivalence to both film-coated and orodispersible tablet formulations, with a comparable tolerability profile, supporting its potential as a convenient alternative formulation for lorazepam.

PMID 42943224
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PubMedPharmaceuticals (Basel, Switzerland)2026-10-27

Interventional Effects and Neurometabolic Regulation of a Panax quinquefolius-Containing Herbal Extract (JYF) in Diazepam Withdrawal Syndrome in Mice.

Jiao Yue Y, Gao Chang C, Li Peng P, Liu Yanjiao Y et al.

Background: Long-term benzodiazepine use can lead to dependence and clinically significant withdrawal following discontinuation, highlighting the need to identify effective interventions for withdrawal-associated abnormalities. Methods: High-resolution mass spectrometry was used to characterize the constituents of a Panax quinquefolius-containing herbal extract (JYF) and evaluate their in vivo exposure in rats. Sixty-five C57BL/6 mice were randomly assigned to control, model, and low-, medium-, and high-dose JYF groups. Diazepam withdrawal was induced after 28 days of subcutaneous diazepam administration (12 mg/kg), and JYF was administered orally during the peri-withdrawal period for 7 days, beginning 4 days before diazepam discontinuation. Behavioral assessments, electroencephalographic/electromyographic (EEG/EMG) recordings, histopathological analysis, and neurochemical measurements were performed. Network proximity analysis, widely targeted metabolomics, targeted neurotransmitter quantification, and integrated pathway analysis were subsequently performed. Results: A total of 61 constituents were identified in JYF, of which 44 were detected in serum and 34 in brain tissue. Network proximity analysis highlighted genistein, columbamine, jatrorrhizine, and berberine as candidate constituents associated with withdrawal, anxiety/depression and sleep-related modules. JYF attenuated diazepam withdrawal-associated weight loss, anxiety-like behavior, sleep fragmentation, abnormal EEG activity, and elevations in corticosterone and orexin A. Metabolomic analyses revealed disturbances in lipid, energy, and amino acid metabolism, with tryptophan and phenylalanine metabolism emerging as prominent pathways associated with JYF intervention. Diazepam withdrawal also disrupted cerebral monoamine homeostasis, as reflected by increased serotonin and norepinephrine and decreased dopamine levels; these alterations generally shifted toward control levels after JYF intervention. Conclusions: JYF alleviates behavioral and sleep-related abnormalities associated with diazepam withdrawal. Its effects may be associated with alterations in brain metabolic homeostasis, including tryptophan- and phenylalanine-related metabolism and monoaminergic neurotransmission. Genistein and berberine were identified as candidate active constituents that warrant further experimental validation.

PMID 42943314
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PubMedMedicina (Kaunas, Lithuania)2026-10-27

Age-Stratified Median Effective Dose of a Continuous Remimazolam Maintenance Infusion for Moderate Sedation During Spinal Anesthesia: A Prospective Up-and-Down Dose-Finding Study.

Park Se-Ung SU, Kim Yeon Ju YJ, Yang Min Chul MC, Park Chan-Hye CH et al.

Background and Objectives: Remimazolam is an ultra-short-acting benzodiazepine suitable for continuous infusion; however, evidence regarding its maintenance infusion rate for moderate sedation during spinal anesthesia across age strata is limited. We aimed to estimate and compare the continuous maintenance median effective dose (ED50) of remimazolam across three prospectively defined age groups. Materials and Methods: In this prospective, single-center dose-finding study (ClinicalTrials.gov NCT05379777), 60 patients undergoing lower-extremity orthopedic surgery under spinal anesthesia were stratified into Group A (<60 years), Group B (60-74 years), and Group C (≥75 years) (n = 20 each). After a loading infusion (1.0 mg/kg/h) to achieve moderate sedation (Modified Observer's Assessment of Alertness/Sedation [mOAA/S] score ≤ 3), maintenance rates were assigned using Dixon's up-and-down method; success was defined as maintaining mOAA/S ≤ 3 until the end of surgery without dose titration. The maintenance ED50 was estimated using centered isotonic regression with 90% confidence intervals (CIs). Safety outcomes were evaluated in all patients. Results: Sedation was maintained at the assigned rate in 13, 13, and 14 patients in Groups A, B, and C, respectively, and all failures were managed by upward titration. The maintenance ED50 was 0.238 (90% CI, 0.152-0.336), 0.233 (90% CI, 0.170-0.301), and 0.178 (90% CI, 0.092-0.245) mg/kg/h in Groups A, B, and C, respectively; the CIs overlapped, and no statistically significant difference was observed. Hypotension requiring vasopressors occurred in 25.0% and respiratory depression requiring airway management in 23.3% of patients, without significant intergroup differences; no patient had peripheral oxygen saturation < 90% or required flumazenil. Conclusions: The maintenance ED50 of remimazolam for moderate sedation during spinal anesthesia was numerically lower in patients aged ≥75 years, without a statistically significant difference among age groups. A conservative initial maintenance rate may be considered in this age group; this hypothesis-generating suggestion requires confirmation in adequately powered studies.

PMID 42942468
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