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midazolam

✓ Approved

Rafa Laboratories Ltd · GABRA1 · Small Molecule

What is midazolam?

midazolam is a small molecule developed by Rafa Laboratories Ltd. It is approved for therapeutic indications via injectable (others) or intramuscular (im) injection.

Drug Profile

CompanyRafa Laboratories Ltd
Drug ClassSmall Molecule
Molecular TargetGABRA1, GABRA2, GABRA3, GABRA4, GABRA5
RouteInjectable (Others), Intramuscular (IM) Injection
StatusApproved
Sources: ClinicalTrials.gov, Rafa Laboratories Ltd

Mechanism of Action

Molecular Targets

midazolam acts on 5 molecular targets:

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)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

midazolam is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Nervous system disordersStatus epilepticus✓ Approved

Related Research Articles

PubMedMedicine2026-11-11

Research trends and hotspots in publications jointly addressing remimazolam and midazolam: A bibliometric analysis, 2016-2025.

Liu Yu Y, Cong Liang L, Luo Shengzhen S, Ma Yuying Y et al.

This bibliometric study characterized the research landscape of literature jointly addressing remimazolam and midazolam from January 2016 through September 2025, with emphasis on publication trends, collaboration patterns, intellectual structure, and emerging research topics. Records published from January 1, 2016 through September 30, 2025 were retrieved from the Web of Science Core Collection on October 30, 2025 using a predefined topic search designed to identify publications in which remimazolam and midazolam were jointly represented. After eligibility screening, 349 publications were analyzed using CiteSpace, VOSviewer, and Bibliometrix to evaluate publication trends, collaboration networks, co-citation patterns, and keyword evolution. Publication output increased markedly over the study period. China contributed the largest number of publications, followed by Japan, South Korea, and the United States. Major research themes included pharmacokinetics, safety, efficacy, and procedural sedation. Recent keyword signals included flumazenil, risk, and upper gastrointestinal endoscopy. Research productivity was concentrated within a limited number of journals and institutions, whereas international co-authorship was limited in this dataset. Research jointly addressing remimazolam and midazolam expanded markedly during the study period and was geographically concentrated, with prominent attention to pharmacokinetics, safety, efficacy, and procedural sedation. These findings provide a structured overview of how the field has evolved and highlight priorities for multinational collaboration, direct comparative studies, and patient-specific dosing research.

PMID 43012783
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PubMedNursing in critical care2026-11-09

Complications of Midazolam-Containing Versus Midazolam-Free Analgosedation in Mechanically Ventilated Adult ICU Patients: A Systematic Review.

Takhdat Kamal K, Belcaid Abdessamad A, Zialy Marwa M, Maysour Asma A

Intensive care unit (ICU) patients requiring mechanical ventilation (MV) frequently need analgosedation strategies that combine analgesia and sedation. Analgosedation, often administered with midazolam, is widely employed in middle and low-income countries, but it carries a substantial risk of complications, particularly in older or comorbid patients. Acknowledging these complications is critical for patient safety and quality of care. To examine complications associated with midazolam-containing versus midazolam-free analgosedation in mechanically ventilated adult intensive care unit patients. This systematic review was conducted according to the PRISMA guidelines. A comprehensive search of Scopus, MEDLINE (PubMed), and Web of Science identified randomized controlled trials (RCTs) published between 2015 and 2025. Studies meeting predefined eligibility criteria underwent risk-of-bias assessment using the Cochrane RoB2 tool. Nine RCTs were included. Midazolam-containing analgosedation regimens were generally associated with prolonged mechanical ventilation, increased respiratory depression and higher incidence of neurological complications, particularly delirium. In contrast, midazolam-free analgosedation regimens, especially those using short-acting opioids, were associated with shorter mechanical ventilation duration and fewer haemodynamic incidents. ICU length of stay and healthcare costs favoured opioid-only analgosedation protocols, although mortality findings were inconsistent across studies. Compared with midazolam-free analgosedation, midazolam-containing analgosedation regimens in mechanically ventilated adult ICU patients are associated with a higher incidence of respiratory and neurological complications. Opioid-only protocols appear to offer a more favourable complication profile and may facilitate earlier weaning and shorter ICU stays. These findings support cautious use of midazolam and emphasize the importance of individualized, goal-directed analgosedation strategies. Enhancing critical care nursing staff's awareness of complications associated with different analgosedation regimens is essential to promote vigilant clinical monitoring, thereby reducing adverse events and supporting safer patient management.

PMID 43001426
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PubMedAntimicrobial agents and chemotherapy2026-11-09

SCY-247, a second-generation triterpenoid antifungal, shows low risk for clinically meaningful interactions with CYP3A4 substrates: results from a phase 1 midazolam drug-drug interaction study.

Wring Stephen S, Argent Christopher C, Murphy Gail G, Angulo David D et al.

SCY-247, an oral and intravenous second-generation triterpenoid antifungal, is being developed for treatment and prevention of invasive fungal infections caused by Candida, Aspergillus, and Pneumocystis species. In vitro studies indicated that SCY-247 is metabolized by cytochrome P450 (CYP) 3A4 and 3A5 and that SCY-247 has a lowered potential for CYP450-mediated drug-drug interactions compared with azoles. This phase 1 study in 12 healthy adult participants evaluated the effect of supra-therapeutic repeated doses of SCY-247 on the pharmacokinetics of midazolam, a sensitive substrate of CYP3A4. Participants received midazolam 2 mg oral solution once daily on Day 1 and Day 8. A loading dose of oral SCY-247 300 mg twice daily was administered on Day 3, followed by maintenance dosing of oral SCY-247 300 mg once daily on Days 4 to 9 (for a total of 7 days of SCY-247 dosing). When co-administered with midazolam, SCY-247 was well tolerated in healthy participants, and there were no serious or severe treatment-emergent adverse events. Geometric mean ratios (with and without SCY-247) for the maximum plasma concentration (Cmax) and area under the plasma concentration-time curve from 0 to infinity (AUC0-inf) were 1.26 and 1.44, respectively, classifying SCY-247 as a weak CYP3A4 inhibitor using regulatory criteria. Therefore, SCY-247 displayed weak inhibition of CYP3A4 at supra-therapeutic doses of 300 mg daily, in contrast to posaconazole and voriconazole, which are strong CYP3A4 inhibitors, and isavuconazole, a moderate CYP3A4 inhibitor. These data are supportive of improved clinical management for CYP3A4 drug-drug interactions with SCY-247 when compared to azoles, particularly relevant in the prophylaxis setting.

PMID 43002077
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PubMedJournal of cardiovascular electrophysiology2026-11-09

Deep Sedation in Single-Shot Pulmonary Vein Isolation: A Head-to-Head Look at Two Pulsed Field Versus Cryoballoon Ablation Approaches.

Kheir Joseph A JA, Schaack David D, Urbani Andrea A, Urbanek Lukas L et al.

Deep sedation (DS) is routinely used during single-shot pulmonary vein isolation (PVI) to optimize patient comfort and procedural stability. However, data on sedative requirements and procedural tolerance of pulsed field ablation (PFA) under DS compared with thermal technologies remain limited. In this single-center study, consecutive patients underwent PVI with cryoballoon (CB), PFA using a pentaspline catheter (PC) or the balloon-in-basket catheter (BC). All procedures were performed under DS with midazolam, fentanyl, and propofol, administered by electrophysiology staff without anaesthesiologist supervision. Propensity score matching (1:1:1) was applied for age, sex, body mass index, and hypertension. Procedural characteristics, sedative/analgesic requirements, and complications were analyzed. Acute PVI without major complications was achieved in all 156 enrolled patients. PC procedures were associated with higher body-weight- and time-adjusted requirements for propofol (CB: 0.10 ± 0.04 mg/kg/min; PC: 0.15 ± 0.04 mg/kg/min; BC: 0.11 ± 0.03 mg/kg/min; p < 0.001) despite the lowest total dose of propofol used (CB: 440 ± 144 mg; PC: 348± 80 mg; BC: 433 ± 160 mg; p = 0.00). Procedural times (CB: 47.5 [40-60] min, PC: 29 [25-35] min, BC: 47.5 [40-56] min, p < 0.001) and fluoroscopy times (CB: 9.5 [6.3-13.6] min; PC: 6.2 [4.4-9] min; BC: 7.2 [6.1-11.2] min, p = 0.001) were shortest in the PC group. Sedation-related hemodynamic stability was comparable across all cohorts. The novel BC demonstrated excellent feasibility under DS, with reduced normalized sedative requirements compared with the PC and a safety profile comparable to CB ablation. These findings suggest that optimized waveform design and field homogeneity may enable safe and comfortable PVI under DS without the need for general anesthesia.

PMID 43002580
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PubMedCase reports in anesthesiology2026-11-08

Cerebral Air Embolism Following Endoscopic Retrograde Cholangiopancreatography Stent Removal: A Rare and Fatal Complication.

Senthuran Bavani B, Arulmurali A A, Kajendran Anuratha A, Vijayacumar Thishanthini T et al.

Endoscopic retrograde cholangiopancreatography (ERCP) is a generally performed procedure for biliary pathology. Although usually safe, air embolism is an exceptionally rare but potentially fatal complication. We report the case of a 79-year-old female (ASA II) with a history of dyslipidemia and obesity, who presented for elective ERCP and biliary stent removal. She had previously undergone ERCP and open cholecystectomy for choledocholithiasis. During this time, sedation was administered by using fentanyl, midazolam, and propofol via target-controlled infusion. The procedure was initially uneventful; however, at its conclusion, the patient developed sudden desaturation, bradycardia, and a reduced level of consciousness. Computed tomography (CT) imaging revealed multiple cerebral air emboli. Despite intensive care management and ventilatory support, the patient deteriorated and died 2 days later. This case highlights the importance of maintaining vigilance for air embolism, even in seemingly straightforward ERCP procedures, especially in elderly patients. Early recognition and immediate management are vital to improving outcomes.

PMID 42999672
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PubMedDrug design, development and therapy2026-11-08

In vitro Evaluation of the Physicochemical Stability of Multi-Drug Y-Site Admixtures Using Dynamic Monitoring and Chemometrics.

Zhang Liting L, Gao Jin J, Zhao Xiaofei X, Yu Siqi S et al.

Concurrent continuous infusions of propofol, midazolam, insulin, dexmedetomidine, and morphine are commonly used in ICU for sedation, analgesia, and glycemic control. However, physicochemical compatibility data for Y-site administration are lacking, leading to risky empirical practice. This study evaluated their physicochemical stability to guide safe infusion. Twenty-six admixtures were prepared at clinical concentrations and stored at room temperature. Samples were analyzed at 0, 2, 4, 8, 12, and 24 h for appearance, pH, osmolality, subvisible particles, mean droplet diameter (MDD), polydispersity index (PDI), zeta potential, microscopic aggregation, and drug content by high-performance liquid chromatography (HPLC). Principal component analysis (PCA), hierarchical cluster analysis (HCA), Spearman correlation, and orthogonal partial least squares-discriminant analysis (OPLS-DA) were performed to explore stability patterns and key discriminating variables. No obvious alterations in appearance, pH, or osmolality were observed over 24 h. In propofol-free admixtures, subvisible particles met pharmacopeial limits. In propofol-containing admixtures, MDD (95.6-124.3 nm) and PDI (0.338-0.469) remained acceptable, whereas zeta potential ranged from -12.50 to 6.14 mV. Microscopic aggregation was observed in seven propofol-containing admixtures. HPLC showed that all drugs retained >90% of their initial concentrations. OPLS-DA identified four independent variables with VIP values greater than 1 (R2 Y=0.71, Q2=0.689), and permutation tests confirmed no overfitting. Under the conditions studied, seven propofol-containing admixtures showed aggregation, while the other 19 remained stable for 24 h. Chemometric analysis supported the stability classification and indicated that drug composition, pH and zeta potential were key contributors to emulsion aggregation.

PMID 42997588
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