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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

PubMedExperimental gerontology2026-06-13

Chronic co-prescription of opioids and benzodiazepines is associated with higher frailty prevalence in older US adults: A nationally representative cross-sectional analysis of NHANES 2005-2018.

Luo Zi Z, Ye Qin Q, Xiao Weibo W, Zhang Rijing R et al.

Opioid-benzodiazepine co-prescription carries a US Food and Drug Administration black-box warning for respiratory depression, yet its association with frailty in community-dwelling older adults has not been quantified at population scale. We analysed 18,434 adults aged ≥50 years from seven cycles of the National Health and Nutrition Examination Survey (NHANES 2005-2018). Current opioid and benzodiazepine use was ascertained from prescription-medication interview data, and participants were classified as neither, opioid-only, benzodiazepine-only, or co-prescription under two exposure definitions (any use in the past 30 days; chronic use ≥90 days). A 36-item questionnaire-based frailty index (FI) was constructed following Rockwood's standard procedure (≥30 items meets the canonical threshold), and frailty was defined as FI ≥0.25. Survey-weighted logistic regression with three progressively adjusted models estimated odds ratios, complemented by sub-group stratification across seven effect modifiers, multiple imputation by chained equations, cycle-stratified sensitivity analysis, polypharmacy adjustment, triple-therapy gradient modelling (including gabapentinoids), and E-value computation. Chronic co-prescription prevalence was 1.4% (n = 259). In the fully adjusted model, chronic co-prescription was associated with an odds ratio for frailty of 2.88 (95% CI 2.47-3.35, P = 3.1 × 10-21) relative to neither drug, with a monotonic gradient (benzodiazepine-only 1.60; opioid-only 2.07; co-prescription 2.88; P-trend = 5.1 × 10-29). Adding a gabapentinoid (triple therapy, n = 67) raised the odds ratio to 3.71 (3.07-4.48). The association remained in all 22 pre-specified sub-groups (all P < 0.01), after multiple imputation (OR 2.68), after adjustment for the number of non-study drugs (OR 1.40), and across NHANES cycle halves (OR 2.72 in 2005-2010; 2.96 in 2011-2018). The E-value of 5.20 indicated robustness to moderate unmeasured confounding. Chronic opioid-benzodiazepine co-prescription was consistently associated with a near three-fold higher burden of frailty in older US adults. These findings support prospective evaluation of this high-risk combination in deprescribing and frailty-screening studies.

PMID 42285234
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PubMedScientific reports2026-06-13

Diastereoselective and green synthesis of novel Hexahydro Imidazo [1,2-a] pyrimidine, from Azlactones, Brimonidine and Clonidine.

Rahmati Keikavoos K, Mohammadi Ali A AA, Amani Vahid V, Halvgar Mohammad Reza MR

An efficient direct domino approach has been developed for the diastereoselective synthesis of novel hexahydroimidazo[1,2-a]pyrimidine-6-yl acetamides. This synthesis involves a domino Michael addition/cyclization reaction of azlactones with brimonidine (used as eye drops for treating open-angle glaucoma) and clonidine (used to treat high blood pressure and attention deficit hyperactivity disorder). The reaction is catalyzed by glacial acetic acid (GAA), which acts as a mild organocatalyst in a metal-free environment, adhering to green chemistry principles by utilizing green solvent (EtOH). Additionally, the transformation proceeds with an atom economy of 100%. The imidazo[1,2-a]pyrimidine moiety plays a crucial role as a benzodiazepine receptor agonist, antiviral, antibacterial, antifungal agent, and calcium channel blocker. This reaction has been performed for the first time, and all synthesized compounds are novel. Their structures were confirmed by single-crystal X-ray crystallography, as well as IR, 1H NMR, 13C NMR spectroscopy, and LCMS analysis. Surprisingly, this reaction was diastereoselective, yielding cis-imidazo[1,2-a]pyrimidines 4b-g and trans-imidazo[1,2-a]pyrimidines 6a-g in cyclocondensation reaction of brimonidine 1 or clonidine 2 with azlactones 3a-g, respectively.

PMID 42286094
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PubMedJournal of sleep research2026-06-12

Risks Associated With Benzodiazepine Long-Term Use in Chronic Insomnia: A Systematic Review and (Network) Meta-Analysis.

Riemann Dieter D, Baglioni Chiara C, Nissen Christoph C, Nevière Agathe A et al.

This systematic literature review evaluated the risks of using benzodiazepine medications for more than 3 months in adults with chronic insomnia. Chronic insomnia is defined as ongoing dissatisfaction with sleep quantity or quality, causing significant distress and impaired functioning during the day. Although benzodiazepine medications are often prescribed to treat insomnia, using them longer than 4 weeks raises concerns about dependence, negative side effects, and long-term health risks for patients. This review included 27 studies published between 1987 and 2023, focusing on adults with insomnia symptoms lasting at least 3 months. The main outcomes examined were sleep quality, safety issues such as risk of falls, mental health concerns including depression and anxiety, and overall quality of life. Five outcomes were deemed suitable for meta-analysis: severity of insomnia, sleep quality, incidence of falls, depression, and anxiety. The results showed that people taking benzodiazepine medications had more severe insomnia than healthy sleepers, but less severe than those who were not taking any medication. The risk of falls was similar between those using benzodiazepine medications and those who were not. However, people using these medications experienced significantly higher levels of depression and anxiety compared to healthy sleepers. This review highlights a lack of studies on the long-term use of benzodiazepine medications, but suggests that extended use may worsen sleep quality, mental health, and quality of life. The findings support guidelines recommending limited use and prioritizing behavioural therapy and alternative safer pharmacotherapies for insomnia.

PMID 42277568
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PubMedPilot and feasibility studies2026-06-12

Phenobarbital as an Adjuvant to benzodiazepines when compared to Single-agent benzodiazepine Treatment (usual care) for Alcohol withdrawal syndrome in the intensive care unit (PASTA): a study protocol.

Panganiban Haustine Patt HP, Ricciardone Samuel G SG, Evans Tess T, Ankravs Melissa J MJ et al.

Abrupt cessation of alcohol consumption following hospital admission can induce alcohol withdrawal syndrome. This syndrome is challenging to manage and is associated with considerable morbidity and mortality. Current management of alcohol withdrawal syndrome in Australia is generally titrated benzodiazepine administration. In some regions, phenobarbital is preferred but evidence to support its superiority is weak. We will conduct a single-center, three-arm, open-label, parallel-group, randomized clinical trial. Our primary objective is to determine the feasibility of embedding a randomized clinical trial within an electronic medical record to compare phenobarbital to single-agent benzodiazepine for patients with alcohol withdrawal. We will screen and randomize 45 patients using the Epic electronic medical record system. Patients will receive either low- or standard-dose intravenous phenobarbital (4 or 8 mg per kilogram), or usual care (benzodiazepine regimen). The primary outcomes to assess feasibility are usability, screening rates, enrollment rates, and compliance. Secondary outcomes are exploratory and include alcohol withdrawal scale scores, dose of benzodiazepine administered, health utilization, adjuvant drug treatments, and patient outcomes. There are limited high quality data evaluating the use of phenobarbital administration for alcohol withdrawal syndrome. Additionally, there is limited data evaluating the embedding of screening, randomization, and administration of a sedative drug within the electronic medical record. Our feasibility trial will establish whether this is possible within our health care system. In this protocol paper we detail how we will embed this trial within the electronic medical record Epic. The study (RMH2024.320 v2 06/01/2025) is registered with Australian New Zealand Clinical Trials Registry (ANZCTR) ACTRN12625000320459. Registered on 17 April 2025. Trial Sponsor: The Royal Melbourne Hospital.

PMID 42277965
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PubMedJournal of clinical medicine2026-06-12

Remimazolam-Induced Anaphylaxis After Spinal Anesthesia: A Case Report and Literature Review.

Jo Yumin Y, Kim Juhyun J, Lee Sanghun S, Lim Chaeseong C

Perioperative anaphylaxis, though rare, is a potentially life-threatening complication. While antibiotics and neuromuscular blocking agents are common triggers, benzodiazepine-induced reactions have been considered uncommon. Remimazolam, a novel benzodiazepine sedative, has gained widespread use in Korea due to its rapid onset, short recovery, hemodynamic stability, and availability of flumazenil. However, increasing utilization has coincided with rising reports of hypersensitivity. We report the case of a 62-year-old female undergoing contralateral total knee replacement under spinal anesthesia. Continuous remimazolam infusion was initiated, but within ten minutes the patient developed chest discomfort followed by abrupt hypotension and oxygen desaturation, requiring urgent conversion to general anesthesia. Following a remimazolam bolus and rocuronium administration, sudden cardiac arrest occurred. Return of spontaneous circulation (ROSC) was achieved after approximately 28 min of cardiopulmonary resuscitation with a cumulative intravenous epinephrine dose of approximately 17 mg, and veno-arterial extracorporeal membrane oxygenation (ECMO) was required. Post-ROSC transesophageal echocardiography demonstrated a transient anteroseptal regional wall motion abnormality; subsequent coronary angiography demonstrated no significant coronary disease, and computed tomography pulmonary angiography was negative for embolism, leaving acute hypersensitivity as the most plausible mechanism. Acute serum tryptase was elevated at 11.6 µg/L and normalized to 3.4 µg/L (the patient's individual baseline) prior to discharge, satisfying the World Allergy Organization (WAO) criterion. A skin prick test performed four weeks later was positive for remimazolam and negative for rocuronium and the other coadministered agents. An expanded multi-database literature review identified 16 prior cases of remimazolam-induced anaphylaxis. Most described cardiovascular collapse as the predominant manifestation. To our knowledge, based on available literature, this is among the first reports of remimazolam-induced anaphylaxis occurring in the setting of high spinal anesthesia with sympathetic blockade. Vigilance and adherence to established anaphylaxis management guidelines are essential.

PMID 42278971
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PubMedTrials2026-06-12

Remimazolam besylate reduces hypoxemia during painless gastrointestinal endoscopy in elderly patients: study protocol for a multicenter, randomized, controlled trial.

Zhang Fang-Yu FY, Ma Zhe Z, Zhang Wei W, Gao Zhi-Feng ZF et al.

Hypoxemia and circulatory depression are common complications in elderly patients undergoing procedure sedation anesthesia (PSA) for gastrointestinal (GI) endoscopy. Remimazolam besylate, a novel ultra-short-acting benzodiazepine, is postulated to offer a superior safety profile with reduced respiratory depressant effects compared to propofol. This study aims to compare the incidence of hypoxemia of remimazolam besylate versus propofol for painless GI endoscopy in elderly patients through a multicenter randomized controlled trial. This study is a multicenter, double-blind, parallel, randomized, controlled trial. Six hundred seventy elderly patients scheduled for GI endoscopy under PSA are enrolled at three medical institutions in China from 2025 to 2027. Patients will be randomized 1:1 to receive remimazolam besylate (0.15 mg/kg) plus sufentanil vs propofol (1.5 mg/kg) plus sufentanil, stratified by age (65-70 vs.70-75 years old) and 3 research institution. The primary outcome is the incidence of intraoperative hypoxemia, defined as any event where peripheral oxygen saturation (SpO₂) is ≥ 75% and < 90%, lasting for less than 60 s. Secondary outcomes include hypoxemia degree, emergency airway management, propofol consumption, hemodynamic stability, involuntary body movements, procedure/recovery times, and clinician satisfaction. This trial evaluates whether remimazolam besylate reduces respiratory depression and improves safety profiles in elderly patients during painless GI endoscopy. It may provide evidence for optimizing sedation strategies in high-risk elderly populations. Chinese Clinical Trial Registry ChiCTR2500110081, registrated on September 30, 2025.

PMID 42277954
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