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diazepam (Stesolid / diazepam, Alpharma)

✓ Approved

Pfizer, Inc. · GABRA1 · Small Molecule

What is diazepam?

diazepam is a small molecule developed by Pfizer, Inc.. It is approved for therapeutic indications via rectal.

Drug Profile

Brand NamesStesolid, diazepam, Alpharma
CompanyPfizer, Inc.
Drug ClassSmall Molecule
Molecular TargetGABRA1, GABRA2, GABRA3, GABRA5
RouteRectal
StatusApproved

Mechanism of Action

Molecular Targets

diazepam acts on 4 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)
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

diazepam is developed for 2 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
Psychiatric disordersAnxiety✓ Approved
Nervous system disordersEpilepsy✓ Approved

Related Research Articles

PubMedJournal of veterinary pharmacology and therapeutics2026-07-17

Residue Kinetics and Dietary Risk Assessment of Diazepam and Its Metabolites in Grass Carp (Ctenopharyngodon idella): Implications for Aquaculture Safety.

Shan Qi Q, Xu Feng F, Wu Mingyuan M, Zhou Hao H et al.

Diazepam (DZP), a benzodiazepine sedative, has been increasingly detected in various aquatic products including fish, shrimp, and crab in recent surveillance studies, raising public health concerns. This study systematically investigates the residue behavior, metabolite profile, and dietary risk of DZP in grass carp (Ctenopharyngodon idella) following oral administration at a dose of 500 μg/kg body weight. Concentrations of DZP and its metabolites in plasma and tissues were determined using ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS), and the drug concentration-time data were fitted using a non-compartmental model embedded in WinNonLin 6.1 pharmacokinetic software. The results indicate that DZP exhibits prolonged elimination kinetics, with tissue elimination half-lives (T1/2λz) ranging from 309.44 to 509.75 h, and residues in skin-on muscle did not fall below the limit of quantification until 98 days. Metabolite analysis identified nordiazepam as the primary metabolite, with its concentration surpassing that of the parent compound by Day 21 post-administration, establishing it as a reliable residue marker for DZP in grass carp. The peak human health risk index (HRI) value was 0.392 on Day 4, remaining above the alert threshold (HRI ≥ 0.1) for 21 days, though all values remained below the safety limit (HRI < 1). These findings provide critical data to support the regulation of aquaculture practices and the assessment of dietary exposure risks associated with DZP-contaminated aquatic products.

PubMedEpilepsy & behavior : E&B2026-07-17

Caregiver preferences and training needs in the administration of rescue medication for prolonged convulsive seizures in children and adolescents with epilepsy: Results from a multinational survey.

Vigevano Federico F, Arzimanoglou Alexis A, Auvin Stéphane S, Kaindl Angela M AM et al.

This multinational survey explored caregivers' preferences and training needs regarding the administration of rescue medication for prolonged convulsive seizures in children and adolescents with epilepsy across 7 European countries. A total of 68 caregivers of children with epilepsy (aged 6 months to 18 years) who had experienced a prolonged convulsive seizure in the past 12 months completed an anonymous survey in 2024. The survey assessed caregiver preferences and satisfaction with buccal, nasal, or rectal rescue medication, quality of life (QoL), valued medication attributes, and training experience. Intranasal formulations were not consistently available across countries during the study period. Most caregivers (80.9%) preferred buccal over rectal or nasal administration, and satisfaction was higher among users of buccal midazolam compared with rectal diazepam. This preference aligned with a positive impact on patients' and caregivers' QoL. Caregivers rated ease of administration as the most important attribute of rescue medication (mean: 4.8/5), followed by effectiveness in stopping seizures (mean: 4.1/5). Despite their critical role, 44.1% had received no specific training; among those trained, 62.2% preferred face-to-face sessions. Training satisfaction was higher among caregivers who administered buccal midazolam (mean: 8.3/10; standard deviation [SD]: 2.4) compared with those using rectal diazepam (mean: 5.3/10; SD: 3.3). This survey underscores a strong caregiver preference for buccal midazolam in pediatric out-of-hospital settings. However, caregiver training remains a substantial unmet need, and standardized programs could improve preparedness for managing prolonged seizures. These findings reinforce the importance of integrating caregiver perspectives to optimize emergency pediatric epilepsy care.

PubMedJournal of paediatrics and child health2026-07-17

Epidemiology of Children and Young People Presenting to Australian Emergency Departments for the Management of Acute Severe Behavioural Disturbance: Secondary Analysis of a Randomised Controlled Trial.

Bourke Elyssia M EM, Klein Kate K, Selman Chris J CJ, Lee Katherine J KJ et al.

To describe the epidemiological characteristics of children and young people presenting to the emergency department (ED) with acute severe behavioural disturbance (ASBD) who were deemed to require oral sedative medication. Secondary analysis of a randomised controlled open-label multi-centre trial of oral olanzapine versus oral diazepam for the management of ASBD in children and young people aged nine to 17 years for whom epidemiological data were recorded. There were 348 participants enrolled in the randomised controlled trial (RCT). The majority were female (215/348, 62%) with a mean age of 14.6 years (standard deviation 2.2). The most common pre-existing medical or mental health condition was anxiety (122/299, 35%) followed by attention deficit hyperactivity disorder and autism spectrum disorder (33% and 32%, respectively). Two-thirds of the study population (216/348, 62%) had previously attended the ED for ASBD management and 61% (212/348) reported previous intentional self-harm. Nearly three-quarters (247/348, 71%) were accessing psychiatric care in the community prior to their ED presentation. Half of the study population (178/348, 52%) presented to the ED with emergency services (e.g., ambulance, police). The median length of stay in the ED was 5.7 h (interquartile range 3.9-10.2 h) and 28% (98/348) of study participants required admission to hospital. For children and young people presenting to the ED with ASBD who were deemed to require oral sedative medication to assist with behavioural containment, pre-existing mental health disorders were common. There is a need for focussed management procedures for more targeted, trauma-focussed care for children and young people presenting to the ED with ASBD and for support and education in the pre-hospital setting. The primary study (PEAChY-O) was registered with the Australian and New Zealand Clinical Trials Registry (ANZCTR) (ACTRN12621001236886) prior to commencement.

PubMedDusunen adam : Bakirkoy Ruh ve Sinir Hastaliklari Hastanesi yayin organi2026-07-16

Successful initiation of catatonia treatment with oral diazepam in bipolar disorder: A case report.

Sungur Ibrahim I, Eker Mehmet Cagdas MC

PubMedJournal of forensic sciences2026-07-16

Response surface methodology-based optimization of high-performance liquid chromatography for simultaneous detection of nimetazepam and diazepam in spiked beverages.

Fauzi Nur Adriana Zulaikha NAZ, Kunalan Vanitha V, Limbut Warakorn W, Abdullah Ahmad Fahmi Lim AFL et al.

Misuse of benzodiazepines in drug-facilitated crimes requires sensitive and selective analytical methods, yet their detection in beverages remains challenging due to matrix interferences and restriction by one-variable-at-time (OVAT) optimization approach. This study was aimed at applying response surface methodology (RSM) to optimize a high-performance liquid chromatography (HPLC) method for simultaneous detection of nimetazepam and diazepam in beverage samples. From the study, an 80% acetonitrile and wavelength of 210 nm for the detector were determined to be optimum through OVAT. On the other hand, the central composite design, an RSM approach, suggested that flow rate at 0.50 mL/min, ammonium formate buffer concentration at 0.04 M with a pH of 4.24 had produced a chromatogram with good separation and high sensitivity. The method showed good linearity (R2 > 0.99) with limit of detection (LOD) and limit of quantification (LOQ) were 0.45 μg/mL and 1.50 μg/mL for nimetazepam, as well as 0.07 and 0.23 μg/mL for diazepam, respectively. Precision was determined in a range between 1.59% and 4.11% while accuracy was reported from 99.62% to 101.24% of percent recoveries with satisfactory selectivity. Recovery studies by spiking both analytes into beverages, resulting in recovery percentages ranged between 70.18% and 110.97%. Our study successfully demonstrated the enhanced performance of the HPLC method through the application of the RSM approach, particularly in recovering the target analytes from beverage samples and suitable for forensic analysis, providing a reliable and efficient simultaneous detection method.

PubMedClinical practice and cases in emergency medicine2026-07-16

A Case Report of Delayed, Severe, Paroxysmal Muscle Cramping After Chilean Rose Tarantula (Grammostola rosea) Envenomation.

Gooley Brian B, Hughes Kirk K, Gooley Mark M, Keyler Daniel D et al.

Grammostola rosea (Chilean rose tarantula) is a common exotic pet belonging to the Theraphosidae (tarantula) family. Case reports of theraphosid bites in adults commonly describe local tissue damage and local pain. Muscle spasms have also been described as a result of the bites but are rarer. We present a case of severe and persistent muscle spasms after a G rosea bite, which is uncommonly reported in the literature. A 42-year-old woman was holding a G rosea tarantula when she was bit on the forearm. Within hours, severe local muscle cramping occurred. Due to worsening cramping, she initially presented to the emergency department the day after the bite, and again on the following day. She was admitted on her second visit and treated with diazepam, cephalexin, diphenhydramine, baclofen, cefpodoxime, doxycycline, prednisone, and topical hydrocortisone. Her laboratory testing was unremarkable, and while medical management may have mildly improved her symptoms, painful cramping persisted. After discharge, her paroxysmal muscle cramping continued for four weeks before completely resolving. While local tissue damage and pain are common, G rosea bites may lead to severe muscle cramping that persists for weeks. Standard laboratory testing may be completely normal in these cases. Muscle cramps may be persistent and are difficult to manage.

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