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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

PubMedSaudi journal of anaesthesia2026-08-05

A comparative study to assess the efficacy of atomized versus drops administration of intranasal midazolam as premedication in pediatric patients undergoing elective surgery under general anesthesia-A prospective randomized double-blind study.

Mandaknalli Parag P, Sholapur Imran I, Kori Rachana Shivanand RS

Preoperative anxiety is one of the major challenges in perioperative care of pediatric surgical patients. Intranasal midazolam is a preferred route of drug administration owing to its ease of administration, non-invasive delivery, and rapid absorption through the highly vascular nasal mucosa, but the method of administration affects the efficacy. To compare the efficacy of atomized versus drop administration of intranasal midazolam (0.3 mg/kg) as a premedication in pediatric patients aged 2-6 years undergoing elective surgery under general anesthesia. This prospective double-blind study was conducted in 60 pediatric patients randomly allocated into the Atomized Group or the nasal drops group. Drug acceptance by a 4-point Medicine Acceptance Scale, Sedation, anxiolysis at the time of shifting, assessed by the Parental Separation Anxiety Scale (PSAS), and adverse events. Drug acceptance was superior in the atomized group compared to the nasal drops group (56.7% vs 3.3%; P < 0.001). The atomized group demonstrated statistically significantly higher sedation scores (2.53 ± 0.776 vs. 1.93 ± 0.583; P = 0.001) at 5 mins, indicating faster onset of sedation. PSAS scores were better in the atomized group (1.17 ± 0.592 vs. 1.53 ± 0.629; P = 0.024). Incidence of adverse events was comparable between both groups (P = 0.379), and no respiratory depression or hemodynamic instability was noted. Atomized intranasal midazolam via mucosal atomization device is superior to conventional nasal drops in achieving higher drug acceptance, faster sedation, and better parental separation anxiolysis in pediatric patients.

PMID 42553955
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PubMedFrontiers in pediatrics2026-08-05

Opioid and benzodiazepine requirements in neonatal and pediatric patients undergoing venoarterial ECMO: insights from a predominantly cardiac cohort.

Alsuhaibani Somayah A SA, Alghanem Ashjan F AF, Alredaini Ibrahim A IA, Alsulami Shaimaa S et al.

Managing sedation and analgesia in neonates and pediatric patients supported with extracorporeal membrane oxygenation (ECMO) is challenging due to altered pharmacokinetics, prolonged critical illness, and the need for deep sedation to maintain circuit integrity. Limited data describing cumulative opioid and benzodiazepine exposure and factors associated with dose escalation in pediatric ECMO populations. We conducted a retrospective cohort study of neonates and pediatric patients aged ≤14 years who received ≥72 h of venoarterial ECMO support in a pediatric cardiac surgical intensive care unit between 2019 and 2023. Exclusions included early mortality, neurological conditions requiring altered sedation strategies, or sedation primarily used for seizure management. Opioid and benzodiazepine doses administered during ECMO were converted to intravenous morphine and midazolam equivalents. Cumulative (mg/kg) and average daily (mg/kg/day) exposures were calculated. Multivariable regression analyses were performed to identify clinical predictors of sedative and analgesic dose requirements and associations with outcomes. Eighty patients were included, with postoperative cardiac disease accounting for 68.8% of primary diagnoses. All patients received opioids, and 96.3% received benzodiazepines; 66.3% received adjunctive sedative agents. Median cumulative opioid and benzodiazepine exposures were 7.33 mg/kg and 15.75 mg/kg, respectively. Prolonged ICU length of stay and ECMO duration were independently associated with higher cumulative opioid exposure (Coeff = 0.02; 95% CI: 0.01 to 0.03; p = 0.001 and Coeff = 0.02; 95% CI: 0.01 to 0.04; p = 0.001, respectively). Furthermore, multivariable analysis demonstrated that higher in-hospital mortality was significantly associated with prolonged ICU length of stay (Coeff = 0.73; 95% CI: 0.12 to 1.34; p = 0.02), higher average opioid doses (Coeff = 1.75; 95% CI: 0.11 to 3.39; p = 0.04), acute kidney injury (Coeff = 3.34; 95% CI: 0.32 to 6.35; p = 0.03), and longer ECMO duration (Coeff = 0.43; 95% CI: 0.06 to 0.80; p = 0.02). Prolonged ICU stays and ECMO courses in neonatal and pediatric patients significantly increase cumulative opioid burdens. Crucially, higher average opioid doses, acute kidney injury, and extended ICU and ECMO durations serve as key clinical predictors of increased in-hospital mortality. These findings highlight the need for individualized, physiology-informed sedation strategies and structured weaning approaches to optimize outcomes in this high-risk population.

PMID 42553372
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PubMedPain physician2026-08-04

Prolonging Peripheral Nerve Blocks in Adults: A Narrative Review of Adjunct Medications for Single-Injection Techniques.

Jha Sachin Sunny SS

Single-injection peripheral nerve blocks (PNBs) are a cornerstone of multimodal perioperative analgesia. However, the duration of commonly used long-acting local anesthetics is finite; many patients experience abrupt and sometimes severe "rebound pain" as the block resolves. This phenomenon is particularly prominent after painful orthopedic procedures and may increase early opioid consumption and reduce patient satisfaction. To review the effectiveness and safety of pharmacologic adjuncts used to prolong adult single-injection PNBs and to provide practical, clinically oriented recommendations for their use. Narrative review. I conducted a focused narrative review of randomized controlled trials, observational studies, and systematic reviews or meta-analyses evaluating adjunct medications administered with single-injection PNBs in adults. The agents considered were dexamethasone, dexmedetomidine, clonidine, morphine, fentanyl, buprenorphine, magnesium sulfate, midazolam, and ketamine. The outcomes of interest were sensory block duration and analgesia, postoperative opioid consumption, rebound pain, and adverse events. Dexamethasone, given intravenously or perineurally, consistently prolongs analgesia by approximately 6-8 hours and reduces early opioid use. Buprenorphine, administered perineurally, often extends analgesia to 24-48 hours but increases postoperative nausea. Dexmedetomidine modestly prolongs a block's duration and improves a block's quality, but is associated with dose-dependent bradycardia, hypotension, and sedation. Clonidine yields smaller gains in a block's duration with similar hemodynamic and sedative concerns to dexmedetomidine. Magnesium sulfate and midazolam produce modest and more variable benefits. Ketamine has inconsistent effects on a block's duration but may help mitigate hyperalgesia in select patients. Conventional opioids (morphine, fentanyl) provide little incremental benefit as perineural adjuncts; they also increase opioid-typical adverse effects. This is a narrative rather than a systematic review; heterogeneity among studies in block type, local anesthetic formulation, dosing, and outcome definitions precludes pooled quantitative estimates. Dexamethasone and buprenorphine have the strongest and most consistent evidence for clinically meaningful prolongation of single-injection PNBs in adults and may be considered first-line adjuncts in appropriate patients. Dexmedetomidine, clonidine, magnesium, midazolam, and ketamine may be useful in some situations when their specific benefit-risk profiles are acceptable. Conventional opioids offer little advantage as perineural adjuncts and are not recommended for routine use. Evidence-based selection of adjuncts within a multimodal analgesic strategy can improve postoperative analgesia, reduce opioid exposure, and potentially attenuate rebound pain.

PMID 42550518
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PubMedTopics in companion animal medicine2026-08-04

Effect of 24-hour sedation during mechanical ventilation on hematological, biochemical, and coagulation parameters in bitches: a randomized clinical study.

Regalin Doughlas D, Adorno Barbara Ataíde BA, Chimenes Natielly Dias ND, Ribeiro Diego D et al.

The effects of prolonged sedation on hematological, biochemical, and coagulation variables have not been previously investigated in veterinary medicine. Twelve healthy adult mixed-breed female dogs were included. Blood samples (6 mL) were collected at baseline (M0) for complete blood count (CBC), biochemical testing, prothrombin time (PT), activated partial thromboplastin time (PTT) and fibrinogen. After M0, dogs were allocated into two groups: midazolam-fentanyl-propofol group (MFG; n=6), which received a continuous infusion of midazolam (0.5 mg/kg/h), fentanyl (10 µg/kg/h), and propofol (18 mg/kg/h); and ketamine-morphine-propofol group (KMG; n=6), which received a continuous infusion of ketamine (0.6 mg/kg/h), morphine (0.26 mg/kg/h), and propofol (18 mg/kg/h). The infusion was maintained for 24 hours under mechanical ventilation. Laboratory parameters were reassessed from 12 and 24 hours after the beginning of infusion (M12 and M24), and at 12, 24, and 48 hours after the infusion (T12, T24, and T48). Both protocols significantly reduced erythrocyte count, packed cell volume, and haemoglobin concentration. In KMG, TTP decreased significantly at M12, M24, and T24; TSP at M24; and lymphocytes at M12 and M24. No significant changes were observed in ALP, ALT, albumin, globulins, creatinine, urea, glucose and blood coagulation. Triglyceride and cholesterol concentrations increased significantly from M6 to T48, but without biochemical evidence of hepatic, renal, or coagulation impairment. Overall, both protocols induced transient hematological and biochemical changes without clinically meaningful alterations in hepatic or renal function, supporting their use in healthy dogs mechanically ventilated for 24 hours.

PMID 42546968
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PubMedCardiovascular and interventional radiology2026-08-03

Clinical Outcome and Safety of Procedural Sedation and Analgesia Performed by Interventional Radiologists in Patients Undergoing Local Tumor Ablation of the Liver.

Puhr-Westerheide Daniel D, Hannak Camilla C, Fabritius Matthias P MP, Öcal Osman O et al.

To evaluate clinical outcome and safety of procedural conscious sedation and analgesia (PCSA) performed by interventional radiologists (IRs) for patients undergoing percutaneous high-dose-rate brachytherapy (HDR-BT) of the liver. This large-scale, monocentric, retrospective study analyzed the safety-profile of PCSA using fentanyl and midazolam in patients undergoing HDR-BT for liver tumors. Medication was administered by trained IRs exclusively responsible for drug administration and cardiorespiratory monitoring. American Association of Anesthesiologists (ASA) status was recorded for all patients. Peri- and post-interventional complications directly or presumably related to PCSA, were assessed. Between 08/2017 and 12/2023, 1062 minimally invasive tumor ablations were performed in 686 patients with: 29.4% hepatocellular carcinoma, 28.7% metastasized colorectal cancer, 6.4% cholangiocarcinoma, metastases from lung cancer (6.1%), pancreatic cancer (4.1%), neuroendocrine tumors (5.1%) and 15.8% other metastases. PCSA-related complications were low (14/1062 procedures, 1.3%). Peri-interventional arrhythmias occurred during 4 procedures (0.4%). One patient (0.09%) experienced severe hypoxemia requiring brief cardiopulmonary resuscitation with return of spontaneous circulation, intubation and ICU-admission. Multivariable regression showed no significant correlations of PCSA-related complications with age, sex, BMI, ASA, chronic obstructive pulmonary disease (COPD), liver cirrhosis or medication doses but a significant correlation of obstructive sleep apnea syndrome (OSAS). No peri- or post-procedural deaths occurred. PCSA can safely be performed by adequately trained IRs with standardised protocols and support from anesthesiologists for emergencies or high-risk-patients. Careful patient selection, hemodynamic monitoring, structured PCSA documentation and immediate availability of anesthesiological support for severe AEs are essential to minimize risks. PCSA in OSAS should be managed by anesthesiologists.

PMID 42543402
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PubMedEpilepsy & behavior reports2026-08-02

Everolimus initiated in the neonatal period for refractory seizures associated with tuberous sclerosis complex: long-term clinical outcome.

Suh Yoong-A YA, Kim Seong Wan SW, Choi Seohui S, Park Moon Sung MS et al.

Everolimus is an established therapy for tumor manifestations and refractory focal seizures in tuberous sclerosis complex (TSC) in patients aged ≥2 years. Evidence regarding its use during the neonatal period, particularly for seizure control, remains extremely limited. We describe the clinical course, neuroimaging findings, treatment response, and developmental outcome of a neonate with genetically confirmed TSC who received early everolimus therapy for refractory seizures. A term female neonate developed multifocal drug-resistant seizures beginning on day 3 of life. Brain magnetic resonance imaging demonstrated multiple cortical and subcortical tubers, and electroencephalography revealed multifocal epileptiform discharges. Despite treatment with phenobarbital, midazolam, and vigabatrin, seizures remained uncontrolled. Everolimus was initiated on day 30 of life. Seizure activity resolved completely within one week and remained controlled for over one year. The treatment was well tolerated, with no serious adverse events. Early developmental assessment at 12 months showed cognitive, language, and motor scores within the lower range of normal. This case suggests that early initiation of everolimus may represent a feasible adjunctive treatment option for selected neonates with TSC-associated refractory seizures.

PMID 42540542
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