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midazolam

✓ Approved

Rafa Laboratories Ltd · GABRA1 · 小分子

什么是 midazolam？

midazolam 是一种小分子，由Rafa Laboratories Ltd研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intramuscular (IM) Injection。

药物档案

公司Rafa Laboratories Ltd
药物类别小分子
分子靶点GABRA1, GABRA2, GABRA3, GABRA4, GABRA5
给药途径Injectable (Others), Intramuscular (IM) Injection
状态Approved
来源： ClinicalTrials.gov, Rafa Laboratories Ltd

作用机制

分子靶点

midazolam 作用于 5 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)
GABRA4gamma-aminobutyric acid type A receptor alpha4 subunit ()
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

midazolam 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
Nervous system disordersStatus epilepticus✓ Approved

相关研究文献

PubMedJournal of personalized medicine2026-07-27

Use of Sedation During Non-Invasive Ventilation in Intensive Care Unit: A Systematic Review and Meta-Analysis.

Iacovazzo Carmine C, de Siena Andrea Uriel AU, Kotfis Katarzyna K, Buonanno Pasquale P et al.

Background: Non-invasive ventilation (NIV) is a well-established approach for preventing endotracheal intubation (ETI) in critically ill patients with acute respiratory failure (ARF). Sedation is frequently used to improve comfort. This study aimed to analyze the impact of sedation during NIV on ETI rates and NIV success in critically ill patients. Methods: We systematically searched in PubMed, EMBASE, MEDLINE, Web of Science, and CENTRAL up to September 2023, including prospective observational studies, retrospective cohort studies (nRCTs), and randomized controlled trials (RCTs). Primary outcomes were NIV success and ETI rates; secondary outcomes were hypotension, bradycardia, 28-day mortality, delirium, and oversedation. Proportions were used for observational studies, odds ratios (OR) for retrospective studies, and risk ratios (RR) for RCTs. Retrospective studies compared intermittent and continuous analgosedation, while RCTs evaluated dexmedetomidine versus other sedatives, including direct comparisons. Results: Four observational studies, 2 retrospective studies, and 7 RCTs (738 patients) were selected. Dexmedetomidine showed increased NIV success (RR = 1.167, 95%C.I. 1.014-1.343, p = 0.032) and reduced ETI rate (RR = 0.553, 95%C.I. 0.405-0.755, p < 0.001), but higher rate of bradycardia (RR = 2.172, 95%C.I. 1.819-4.042, p < 0.001) and hypotension (RR = 2.441, 95%C.I. 1.608-3.706, p < 0.001). nRCTs revealed higher NIV success (Proportion = 0.694, 95%C.I. 0.528-0.912, p = 0.009), moderate ETI rates (Proportion = 0.379, 95%C.I. 0.282-0.511, p < 0.001), and low bradycardia and hypotension rates. Conclusions: Our findings suggest that sedation, particularly dexmedetomidine-based strategies, may enhance NIV success and lower ETI rates. However, dexmedetomidine was also associated with higher rates of bradycardia and hypotension, especially compared with midazolam. To establish the correct sedation strategy, it is important to tailor the drug to the patient, considering its hemodynamic instability, delirium risk, and mortality risk.

PMID 42506109
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PubMedJournal of pain and symptom management2026-07-25

Subcutaneous Drug Administration in Pediatric Palliative Home Care: A Multicenter Prospective Study.

Riva de la Hoz Belén B, de Miguel Marta Echávarri ME, Gorbe Cristina Latre CL, Tristancho-Pérez Ángela Á et al.

Pediatric palliative care patients frequently present with complex, life-limiting conditions and a high symptom burden requiring effective therapeutic strategies. The subcutaneous route is an important alternative for symptom control care when enteral or intravenous administration is not feasible. However, evidence supporting its use in children remains limited. To describe real-world use, safety, and administration characteristics of subcutaneous drug administration for symptom control in children receiving palliative home care. A multicenter, prospective observational study was conducted between April 2023 and June 2024 across Pediatric palliative care Units from nine Spanish hospitals. Pediatric patients receiving home-based palliative care and requiring subcutaneous drug administration were included. Data were collected at patient, catheter, and treatment levels. Descriptive statistics and mixed-effects logistic regression models were used to evaluate factors associated with catheter-related complications. Forty patients, 140 subcutaneous catheters, and 214 treatment episodes were analyzed. The main indication for subcutaneous use was inadequate symptom control with other routes (75%). Median catheter dwell time was 6 days (IQR, 2.7-12.2). Catheter-related complications occurred in 40% and were predominantly mild local reactions, mainly induration. Most treatments consisted of single-drug regimens administered by continuous infusion. Midazolam (58.9%) and morphine (33.6%) were the most commonly administered drugs. Scopolamine was associated with increased complication risk (OR, 6.94; 95% CI, 1.14-42.18; P=.035). Subcutaneous drug administration was a feasible and generally safe strategy for symptom control in pediatric palliative home care. These findings support collaborative research to standardize pediatric subcutaneous therapy.

PMID 42498184
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PubMedFrontiers in immunology2026-07-25

Immunological mechanisms and prevention strategies for febrile seizures in children.

Chen Binbin B, Tao Enfu E

Febrile seizures (FS) affect 2-5% of children globally, causing significant caregiver anxiety and healthcare utilization. Emerging evidence implicates neuroinflammation and T-cell-mediated immunity in FS pathogenesis, suggesting potential targets for future investigation. This Review synthesizes current evidence on FS prevention, emphasizing a paradigm shift from universal pharmacological approaches toward risk-stratified, personalized strategies. The COVID-19 pandemic provided unique insights: non-pharmaceutical interventions reduced FS incidence by 54-70%, while the Omicron variant emerged as a novel trigger associated with complex FS features. Prevention is conceptualized within a three-level framework: primary prevention targets all children through vaccination (MMR, PCV13, COVID-19 vaccines) and infection control; secondary prevention focuses on high-risk children with prior FS, where risk stratification integrates clinical predictors (complex features, young age, low fever), biomarkers (hyponatremia, zinc/vitamin D deficiency, inflammatory indices), and pathogen-specific risks (influenza A, Omicron); tertiary prevention addresses complications and epileptogenesis in children with complex FS or genetic predisposition (SCN1A, PCDH19). Key immunological mechanisms include HMGB1-NLRP3 inflammasome activation, TRPV1-mediated Th17 differentiation, and IL-1β/IL-10 dysregulation. Antipyretics do not prevent FS recurrence during distant febrile episodes, while intermittent benzodiazepines (diazepam, intranasal midazolam) effectively reduce early recurrence in high-risk children (NNT = 6.8), albeit with adverse effects in up to 36%. Emerging frontiers include novel therapeutic targets (HMGB1 inhibitors, TRP channel modulators, TSP-1 pathway inhibitors) and non-pharmacological innovations (wearable sensors, chronotherapy). Crucially, caregiver education underpins all prevention levels, addressing high rates of parental anxiety (58.2%). This integrated framework guides clinical practice toward more individualized, risk-based management.

PMID 42500652
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PubMedCNS neuroscience & therapeutics2026-07-24

Midazolam Exerts Sedative Effects by Differentially Modulating Cortical Pyramidal Neurons and PV Interneurons.

Sun Yao Y, Wang Dijia D, Wu Kaibin K, Yin Mengyu M et al.

Midazolam is a sedative that acts on γ-aminobutyric acid type A receptors, but whether its effects are region-specific, especially in the neocortex, and the mechanisms underlying these effects remain unclear. Using microendoscopic Ca2+ imaging and whole-cell recording in brain slices, we systematically investigated the effects of midazolam on excitatory pyramidal neurons and inhibitory parvalbumin-positive interneurons (PV+) in the mouse auditory cortex (AC) and anterior cingulate cortex (ACC). Midazolam dose-dependently suppressed pyramidal neurons more potently in the AC than in the ACC (Evoked: pyramidal neurons: 0.65 ± 0.30 vs. 1.36 ± 0.34, p < 0.0001; Spontaneous: pyramidal neurons: 1.49 ± 0.48 vs. 2.25 ± 0.42, p = 0.0006). In slices, midazolam reduced the action potential firing of pyramidal neurons in a concentration-dependent manner, with greater sensitivity in the AC. In contrast, PV+ neurons showed little change in intrinsic excitability in either region. Functional assays suggested that midazolam responsiveness was associated with GABRA1 expression, which was higher in AC pyramidal neurons than in those of the ACC (1.77 ± 0.55 vs. 1.01 ± 0.36, p = 0.002), while PV+ neurons showed no significant regional difference in GABRA1 expression. Midazolam suppresses cortical excitatory neurons in a region- and cell-type-dependent manner that is associated with differential expression of GABRA1.

PMID 42496092
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PubMedBritish journal of anaesthesia2026-07-24

Economic impact of switching to licensed ready-to-administer injectable anaesthetic and critical care medicines in the National Health Service: a model-based evaluation of prefilled syringes.

Al-Rawi Suzanne S, Mehta Jaidev J, Taylor Karl K, Glover David D et al.

Licensed, ready-to-administer injectable medicines can reduce medication errors, minimise waste, and streamline perioperative workflows, but higher acquisition costs have limited uptake in England. This study evaluated the economic impact of switching selected anaesthetic and critical care medicines from conventional ampoules and vials to licensed prefilled syringes within NHS practice. An economic model compared current mixed-use practice with a hypothetical switch to 100% licensed ready-to-administer products for eight medicines: epinephrine 1 mg in 10 ml, ephedrine 30 mg, atropine 3 mg, rocuronium 100 mg in 10 ml, lidocaine (1% and 2%), and midazolam (5 mg in 5 ml and 50 mg in 50 ml). Modelled cost components included medicine acquisition, wastage, nursing preparation time, consumables and preventable adverse drug events. Preparation time reductions were interpreted as capacity release rather than workflow substitution. Deterministic sensitivity analyses explored variation in key assumptions and procurement thresholds. Under the modelling assumptions, epinephrine, ephedrine, atropine and lidocaine 2% were associated with reduced overall system costs of more than £5.3 million annually, largely driven by reduced wastage, preparation workload and modelled adverse drug events. Rocuronium and midazolam were associated with increased costs because of higher acquisition prices despite operational advantages. Sensitivity analyses did not alter the direction of findings. Substantial price reductions would be required for certain medicines to achieve cost neutrality. Licensed ready-to-administer injectable medicines can provide safety and workflow advantages and be associated with economic benefit. Acquisition cost remains a barrier, but broader adoption and market development could improve affordability.

PMID 42493387
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PubMedReports (MDPI)2026-07-24

Posterior Single-Window Ultrasound-Guided Cryoneurolysis for Severe Pediatric Spastic Equinovarus: Technical Feasibility and Same-Patient Comparison.

Di Lorenzo Luigi L, Zmerly Hassan H, Agliaroro Emiliano E, Forte Alfonso Maria AM et al.

Background and Clinical Significance: Severe pediatric spastic equinovarus may significantly impair positioning, orthotic tolerance, hygiene management, caregiver-assisted mobilization, and assisted standing activities. In children with severe cerebral palsy, clinically meaningful outcomes frequently include reduction in caregiver burden and facilitation of daily care rather than restoration of autonomous gait. Ultrasound-guided cryoneurolysis has recently emerged as a minimally invasive option for focal spasticity management, although procedural workflow and tolerability remain challenging in severe deforming patterns. Case Presentation: We report a CARE-compliant same-patient bilateral technical comparison in a 9-year-old child with severe spastic cerebral palsy and bilateral dynamic equinovarus refractory to intensive rehabilitation and repeated botulinum toxin treatment. Baseline severity was consistent with GMFCS level IV. One lower limb was treated using the proposed posterior single-window ultrasound-guided cryoneurolysis approach through a single posterior proximal-calf window, whereas the contralateral limb underwent a conventional multi-point supine strategy. The posterior single-window approach enabled sequential targeting of multiple motor branches through a single posterior access corridor under continuous ultrasound guidance. The procedure required approximately 1 mL of 2% lidocaine without additional sedation and was completed in approximately 4 min, whereas the conventional supine strategy required multiple access points, repeated probe repositioning, minimal conscious sedation with midazolam, and approximately 20 min. At follow-up, lower-limb spasticity improved from approximately MAS 3 toward MAS 2, passive ankle angle, measured as the tibia-foot angle with 90° corresponding to the neutral ankle position, improved from approximately 80° to 95°, and semitendinosus-related hypertonia was reduced. Clinically meaningful improvement in positioning, hygiene management, assisted standing, and rehabilitation handling was observed. Caregiver-reported satisfaction and procedural tolerability were qualitatively perceived as better with the posterior single-window approach. Conclusions: The proposed posterior single-window cryoneurolysis strategy may represent a technically simplifying and clinically relevant minimally invasive approach for severe pediatric spastic equinovarus. Further prospective studies are required to confirm reproducibility, safety, and long-term outcomes.

PMID 42496521
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