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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

PubMedBritish journal of clinical pharmacology2026-09-18

Benzodiazepines use in primary care England: Prescribing patterns and adverse consequences.

Chaudhry Alvina A, Khan Muhammad Umair MU, Conway Barbara B, Hasan Syed Shahzad SS

Benzodiazepines (BZDs) are commonly prescribed for anxiety and insomnia but carry risks such as dependence, adverse drug reactions (ADRs) and mortality. Despite deprescribing efforts, the influence of recent prescribing trends, COVID-19 and adverse outcomes on prescribing patterns in England remains uncertain. This study evaluates trends in BZD prescribing, costs, and safety outcomes and explores their socioeconomic associations. This population-level observational study analysed prescribing, cost and ADR data for 14 BZDs using national datasets. Prescribing rates were standardized per 100 000 population, fatality ratios were calculated, and regression models assessed yearly changes by drug, region, and pandemic phase. Socioeconomic influences on prescribing were analysed using a generalized additive model. Total BZD prescribing decreased from 15562.34 items per 100 000 population in 2020 to 12284.01 in 2025, a mean annual change of -4.3% (95% CI: -4.5% to -4.03%), largely because of reduced prescribing of diazepam, temazepam and chlordiazepoxide. Conversely, specialist-use agents increased, including clobazam (6.36% per year, 95% CI: 0.34% to 12.39%) and midazolam (1.03% per year, 95% CI: -1.30% to 3.37%). Ethnicity influenced deprivation-related prescribing patterns, indicating disparities beyond socioeconomic status. The average lifetime fatality ratio across all BZDs was 4.5 deaths per 100 reported cases, with oxazepam the highest (17.9), followed by lorazepam (9.1) and alprazolam (8.6). Benzodiazepine prescribing in England continues to decline, reflecting successful deprescribing policies. However, increasing specialist use, persistent inequities, and drug-specific safety and cost concerns highlight the need for cautious prescribing, enhanced pharmacovigilance and equitable access.

PMID 42758106
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PubMedFrontiers in pediatrics2026-09-18

Clinical utility and tolerability of ketamine as adjunctive rescue therapy for refractory neonatal status epilepticus: a case report of a late preterm infant with multifocal hemorrhagic brain injury.

Gulisano Chiara C, Pepe Alessia A, Amadori Elisabetta E, Caruggi Samuele S et al.

Neonatal status epilepticus (NSE) is a life-threatening neurological emergency associated with high mortality and long-term neurodevelopmental morbidity. Although phenobarbital remains the recommended first-line antiseizure medication (ASM), followed by agents such as phenytoin or levetiracetam, seizure control is not always achieved. Ketamine, a non-competitive N methyl-D-aspartate (NMDA) receptor antagonist, has emerged as a potential rescue therapy for refractory status epilepticus because of its unique mechanism of action and favorable hemodynamic profile. However, evidence supporting its use in neonates remains scarce. Despite increasing recognition of refractory neonatal status epilepticus (RNSE), no universally accepted definition exists. Current recommendations suggest considering RNSE when electroclinical or electrographic seizures persist despite appropriate first- and second-line treatment, highlighting the importance of continuous EEG monitoring. We report a late preterm male infant with multifocal hemorrhagic brain injury who developed RNSE on the second day of life despite sequential treatment with phenobarbital, levetiracetam and midazolam. Ketamine was associated with disappearance of clinical seizures and persistence of shorter electrographic-only seizures. Complete electrographic seizure cessation occurred after continued ketamine and the subsequent addition of phenytoin. No acute hemodynamic or respiratory adverse events attributable to ketamine were observed. This case highlights both the potential and the limitations of ketamine in RNSE. Although seizure control cannot be attributed solely to ketamine because of concomitant multimodal therapy, its distinct pharmacological mechanism, favorable cardiovascular profile, and ease of administration make it a feasible and well-tolerated adjunctive treatment option. Continuous EEG monitoring remains essential for evaluating treatment response. Prospective neonatal studies are needed to define the optimal timing, dosing strategies, efficacy, and long-term safety of ketamine in RNSE.

PMID 42756223
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PubMedFrontiers in veterinary science2026-09-16

Correction: Electrocardiographic and echocardiographic profiles of white-lipped peccaries (Tayassu pecari) under ketamine-dexmedetomidine or ketamine-midazolam anesthesia.

Gorczak Rochelle R, Valandro Marilia Avila MA, Barbosa Helena Bulhoes HB, Niella Raquel Vieira RV et al.

[This corrects the article DOI: 10.3389/fvets.2026.1803243.].

PMID 42746220
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PubMedProceedings (Baylor University. Medical Center)2026-09-16

Periprocedural rescue antiemetic administration during radiologic procedures performed under conscious sedation.

Weingarten Toby N TN, Ubl Courtney E CE, Reisenauer Chris J CJ, Sprung Juraj J et al.

This study aimed to determine the incidence and clinical predictors of periprocedural rescue antiemetic administration during radiologic procedures performed under conscious sedation. We performed a retrospective review of adult patients who underwent radiologic procedures under conscious sedation with midazolam and/or fentanyl between May 6, 2018, and December 31, 2024. Rescue antiemetics was defined as the use of an antiemetic during the procedure or recovery period. A modified Apfel score (excluding need for postprocedural opioids) was calculated. Logistic regression was used to assess the association of clinical characteristics with the need for rescue antiemetics. Among 21,343 unique patients, 990 (4.64%; 95% confidence interval [CI] 4.34-4.93) were administered a rescue antiemetic. Clinical factors associated with the need for rescue antiemetics included female sex (adjusted odds ratio [OR], 2.31; 95% CI, 1.99-2.67), history of postprocedural nausea and vomiting (OR, 1.99; 95% CI, 1.59-2.48), younger age (OR, 0.84 per decade of life; 95% CI, 0.81-0.88), procedural duration (OR, 1.78 per hour; 95% CI, 1.60-1.99), and fentanyl dose (OR, 1.12 per 25 mcg; 95% CI, 1.07-1.16). Risk increased with higher modified Apfel scores. Duration of recovery was longer among patients who were administered vs not administered a rescue antiemetic (median duration 116 [73, 165] vs 47 [27, 100] minutes, P < 0.001). Rescue antiemetic administration during radiologic procedures with conscious sedation complicates <5% of cases. Risk factors for rescue antiemetics are similar to those for postprocedural nausea and vomiting following general anesthesia.

PMID 42747022
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PubMedEuropean journal of pediatrics2026-09-15

Electro-clinical efficacy and safety of midazolam in neonatal seizures: a systematic review with individual level exploratory analysis of gestational age-related treatment response.

Falsaperla Raffaele R, Sortino Vincenzo V, Cimino Carla C, Saporito Marco Andrea Nicola MAN et al.

Neonatal seizures are the most common neurological emergency during the neonatal period and are associated with increased mortality and adverse neurodevelopmental outcomes. Despite current recommendations supporting phenobarbital as first-line therapy, seizure control remains suboptimal in a large proportion of neonates, prompting the use of second-line antiseizure medications. Midazolam is increasingly administered in refractory neonatal seizures but evidence regarding its electro-clinical efficacy and safety remains limited and heterogeneous. To systematically review the available evidence on the electro-clinical efficacy and safety of midazolam in neonatal seizures and to perform an exploratory individual-level analysis investigating the association between gestational age and treatment response. A systematic review was conducted according to PRISMA 2020 guidelines. Studies including neonates with EEG- or aEEG-confirmed seizures treated with midazolam were included. Binary logistic regression was performed to assess the individual-level association between gestational age and treatment response. Eleven studies involving 146 neonates treated with midazolam were included. Electro-clinical response was observed in 101/146 neonates (69.2%), while seizure cessation was achieved in 61/146 neonates (41.8%). In an exploratory complete-case logistic regression analysis, higher gestational age appeared to be associated with a greater probability of electro-clinical response. The predicted probability curve crossed the 50% response probability at approximately 36.5 weeks of gestation. Hypotension was the most frequently reported adverse event, while respiratory depression, sedation-related effects, and transient EEG/aEEG suppression were reported less frequently. Midazolam may have a role as an add-on antiseizure medication in neonatal seizures, particularly in refractory cases. However, the evidence remains limited by heterogeneity in study design, EEG monitoring strategies, outcome definitions, and incomplete individual-level data. The observed association between gestational age and response is hypothesis-generating and requires prospective validation. • Phenobarbital often provides incomplete seizure control in neonates, making second-line antiseizure therapies necessary in refractory cases. • Evidence supporting midazolam for neonatal seizures remains limited and heterogeneous. • This systematic review summarizes the electro-clinical efficacy and safety of midazolam and includes an exploratory patient-level analysis suggesting that higher gestational age may be associated with improved treatment response. • These findings support further prospective studies on developmental determinants of response to GABAergic therapy.

PMID 42736513
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PubMedThe Journal of antimicrobial chemotherapy2026-09-15

BV100 (rifabutin IV) drug interaction studies in healthy subjects with index CYP450 3A probes midazolam and itraconazole.

Delique Pierre P, Kemmer Christian C, Husband Lisa L, Lakner Géza G et al.

BV100 is a novel intravenous (IV) formulation of rifabutin under development for the treatment of serious Acinetobacter baumannii infections. The primary objectives of these studies were to assess potential pharmacokinetic interactions between BV100 and two index cytochrome P450 3A enzymes (CYP3A) probes, midazolam (substrate) and itraconazole (inhibitor), and to evaluate BV100's safety profile. Two open-label Phase 1 studies were conducted in healthy participants. Study 1 evaluated the impact of multiple IV doses of BV100 (300 mg) on the pharmacokinetics of a single oral dose of midazolam (5 mg). Study 2 assessed the impact of repeated oral doses of itraconazole (200 mg) on the pharmacokinetics of a single IV dose of BV100 (300 mg). Pharmacokinetic parameters [maximum plasma concentration (Cmax), area under the plasma concentration-time curve from zero to 24 hours (AUC0-24), area under the plasma concentration-time curve from zero to infinity (AUC0-∞)] were analysed using geometric means and 90% confidence intervals (CI). Drug-drug interactions (DDIs) were defined as a 90% CI outside the equivalence range of 80%-125%. Both studies demonstrated DDIs. BV100 increased midazolam metabolism, with Cmax and AUC test/reference ratios of 77% and 53%, respectively. The decreased midazolam AUC (47%) indicated BV100 is a mild/weak CYP3A inducer by EMA/FDA criteria. Itraconazole decreased BV100 metabolism, resulting in increased BV100 exposure (Cmax 1.1-fold; AUC 1.3-1.7-fold), consistent with mild inhibition. BV100 was considered generally safe and well tolerated in both studies, with no serious adverse events reported. BV100 is a mild/weak CYP3A enzyme inducer and a mild substrate for CYP3A inhibitors. However, co-administration with strong CYP3A inhibitors resulted in a disproportionate increase in exposure to the active metabolite 25-O-desacetyl rifabutin, leading to an ∼2-fold increase in total active-moiety exposure. Clinical monitoring is advised when BV100 is co-administered with a strong CYP3A inhibitor. BV100 was safe and well tolerated.

PMID 42736170
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