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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
Sources: ClinicalTrials.gov, Pfizer, Inc.

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

PubMedThe International journal of neuroscience2026-10-14

Myrtenol mitigates seizure activity and oxidative imbalance in a mouse model of PTZ-induced seizure.

Rasouli Fatemeh F, Hojjat Seyed Hesam SH, Shakeri Farzaneh F

Pentylenetetrazole (PTZ)-induced seizures are strongly associated with oxidative imbalance, and the monoterpenoid alcohol myrtenol has been proposed to exert antioxidant and neuroprotective effects. This study investigated whether myrtenol attenuates PTZ-evoked seizure activity and oxidative disturbances in the mouse hippocampus and cerebral cortex. Sixty male mice were assigned to six groups: control, PTZ-only, three myrtenol pretreatment doses (25, 50, 100 mg/kg), and diazepam. Seizure susceptibility was evaluated by measuring latencies to minimal clonic and generalized tonic-clonic seizures following PTZ administration. Oxidative stress markers, including malondialdehyde (MDA), nitric oxide (NO), superoxide dismutase (SOD), catalase (CAT), and total thiol content, were quantified in brain homogenates. PTZ reliably induced seizures and oxidative alterations. Myrtenol pretreatment increased seizure latencies in a dose-dependent manner, although diazepam produced the greatest protection. Myrtenol, particularly at 100 mg/kg, reduced PTZ-induced elevations in MDA and NO, restored SOD and CAT activities, and improved thiol levels, with effects approaching those of diazepam. Lower myrtenol doses produced partial or nonsignificant biochemical improvements. These findings indicate that myrtenol mitigates PTZ-induced seizure expression and oxidative stress, with the highest dose demonstrating the most consistent neuroprotective profile.

PMID 42872728
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PubMedJournal of mass spectrometry : JMS2026-10-13

Assessing the use of ASAP-MS for Screening a UK Pub for Illicit Drug Substances.

Michailidis Andriana A, Mathias Simone S, Edgar-Gibson Eloise E, Douce David D et al.

Illicit drug use in social environments, such as pubs and bars, has become an increasingly significant issue for public health and safety. These venues often provide a setting where individuals may engage in recreational drug use, resulting in their residual presence on high-contact surfaces. This study aims to investigate the presence of illicit drugs in a pub within the United Kingdom, focusing on common touchpoints such as the tables, bar and men's/women's bathrooms. Over 400 surface swabs were collected across 3 weeks, with the objective of identifying traces of illicit substances commonly associated with recreational use. This study additionally explored the potential of atmospheric solids analysis probe mass spectrometry (ASAP-MS) as a screening tool for the on-site detection of cocaine, ketamine, amphetamine, diazepam and tetrahydrocannabinol (THC). Previous research has demonstrated that ASAP-MS is an effective method for detecting illicit drugs with minimal sample preparation. An untargeted screening method was developed for direct swab analysis via glass capillary rod, whereas a combined untargeted and targeted approach was used for solvent-extracted samples. For confirmatory testing, liquid chromatography mass spectrometry (LC-MS) determined the effectiveness of each ASAP-MS analysis. Results indicated that the targeted method with minimal sample preparation detected trace amounts of illicit drugs that were previously undetected using the initial screening method. However, the untargeted method, with direct sample analysis, showed potential for detecting larger quantities, particularly cocaine. Overall, the findings revealed drug residues at all touchpoints within the pub, particularly in the bathrooms which contained traces of cocaine in all samples.

PMID 42864952
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PubMedJAMA internal medicine2026-10-12

Comparative Effectiveness of Phenobarbital vs Diazepam for Alcohol Withdrawal Syndrome.

Bradley Tess T, Feeney Megan M, Law Anica C AC, Peterkin Alyssa F AF et al.

Phenobarbital use for alcohol withdrawal syndrome is increasing, but its effectiveness and safety have largely been compared with lorazepam rather than against more pharmacokinetically similar long-acting, self-tapering benzodiazepines such as diazepam. To emulate a clinical trial comparing patients randomized to phenobarbital vs diazepam for alcohol withdrawal syndrome. This multicenter comparative effectiveness research study analyzed data from the Premier Healthcare Database (October 2022 to August 2024), representing 754 US acute care hospitals. Adult inpatients with a primary diagnosis of alcohol withdrawal syndrome present on admission who initiated phenobarbital or diazepam on the day of hospital admission were included. Initiation of phenobarbital or diazepam on the day of hospital admission. The primary effectiveness outcome was hospital length of stay in days. The primary safety outcome was invasive mechanical ventilation use. Secondary outcomes assessed treatment escalation, complications of severe alcohol withdrawal syndrome, and resource utilization. Targeted maximum likelihood estimation with ensemble machine learning was used to estimate marginal mean differences and risk differences between exposure groups. Among 24 643 patients (median [IQR] age, 45 [35-56] years; 18 511 male [75.1%]), 11 919 (48.4%) received phenobarbital and 12 724 (51.6%) received diazepam on the day of admission. There were no differences in hospital length of stay (marginal mean, 4.1 vs 4.3 days; marginal mean difference, -0.21 [95% CI, -0.42 to 0.00] days) or invasive mechanical ventilation use (marginal risk, 3.1% vs 2.7%; marginal risk difference, 0.4% [95% CI, -0.7% to 1.4%]) between initiation of phenobarbital vs diazepam. Secondary outcomes were also not different between phenobarbital and diazepam, except for self-directed discharge, which was more frequent among those initiated on diazepam (marginal risk, 9.5% vs 12.6%; marginal risk difference, -3.1% [95% CI, -4.9% to -1.3%]). In this multicenter study of patients hospitalized for alcohol withdrawal syndrome, there were no differences in hospital length of stay or the need for invasive mechanical ventilation between initiation of phenobarbital vs diazepam. These results may suggest near therapeutic equivalence between phenobarbital and long-acting benzodiazepines.

PMID 42862568
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PubMedEnvironmental science and pollution research international2026-10-07

Psychotropic drugs in drinking water? A scoping review of evidence on diazepam and fluoxetine.

Teixeira Paula Pinheiro PP, Pereira Beatriz Assunção BA, da Silva Carneiro Roberta R, de Assis Lara Júlia Moraes LJM et al.

The global prevalence of mental disorders has increased considerably in recent decades. This evidence, associated with population growth and the expansion of access to medications, favors the growing global consumption of psychotropic drugs. Consequently, an increasing load of these substances is introduced into the environment, especially into water bodies, characterizing them as emerging contaminants. This scoping review study aimed to integrate data and provide a global overview of the occurrence of widely used psychotropic drugs (diazepam, fluoxetine, and haloperidol) in drinking water. The search for studies was conducted across 7 databases, with no language or publication year restrictions. We included only original studies in this review and synthesized data from the included studies for water sampled, sampling location, year of sampling, analytical method used, psychotropic drug found, and concentration found. Our review identified 13 studies published between 2000 and 2024 on the occurrence of diazepam and fluoxetine in tap water, drinking water, bottled water, and drinking well water from 7 countries, with concentrations ranging from 0.2 to 300 ng/L. No studies on the occurrence of haloperidol in drinking water were found. Our data highlight that the occurrence of psychotropic drugs in drinking water is a growing global reality and also show a significant lack of research dedicated to the topic. Furthermore, the results of this scoping review reinforce the need to expand water quality monitoring, improve analytical techniques, invest in advanced water treatment technologies, and implement public policies on the proper disposal of medication and the control of drug pollution.

PMID 42839167
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PubMedPaediatric anaesthesia2026-10-07

Intrathecal Hydromorphone Dosing for Adolescent Spinal Fusion: A Prospective Dose-Escalation Study.

Handlogten Kathryn S KS, Warner Lindsay L LL, Larson A Noelle AN, Milbrandt Todd A TA et al.

Intrathecal opioids are widely used for postoperative analgesia in pediatric spine surgery, but optimal dosing remains undefined. We evaluated the relationship between intrathecal hydromorphone (ITH) dose, analgesia, and adverse effects in adolescents undergoing posterior spinal fusion (PSF). In this single-center, prospective, blinded dose-escalation study using a biased-coin up-down sequential allocation design, patients aged 10-17 years undergoing PSF received ITH starting at 3.5 mcg kg-1, with dose adjustments based on analgesic response (range 2.0 to 7 mcg kg-1 with a maximum of 400 mcg). The primary outcome was maximum postoperative pain within 18 h. Secondary outcomes included pain burden (area under the curve), 24-h systemic opioid consumption (oral morphine equivalents [OME], excluding ITH), adverse effects, supplemental diazepam use, and rescue opioid use. Associations between dose and outcomes were assessed using Spearman correlation and logistic regression. Twenty-seven patients completed the study. The median ITH dose received was 5.5 mcg kg-1 (IQR, 3.5-7.0), with a median absolute dose of 370 mcg (IQR, 180-400). No significant association was observed between ITH dose and maximum pain (r = 0.16, p = 0.41), pain burden (r = 0.32, p = 0.10), or 24-h OME (r = 0.13, p = 0.52). ITH dose was not significantly associated with the time to rescue opioid (HR = 1.24; 95% CI 0.68-2.25; p = 0.485) or diazepam (HR = 1.10; 95% CI 0.72-1.71; p = 0.655). Adverse respiratory events occurred at doses > 5 mcg kg-1 without improved analgesia. Increasing ITH dose was not associated with improved analgesia or change in supplemental opioid or diazepam use. Doses > 5 mcg kg-1 were associated with adverse respiratory effects. These findings support conservative dosing strategies and underscore the need to define the minimum effective dose in pediatric populations.

PMID 42841453
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PubMedDrug testing and analysis2026-10-07

Population-Stratified Distributions of Post-Mortem Blood Drug Concentrations: An Epidemiological Framework for Contextual Interpretation.

Algahtani Thikra T, Rock Kirsten L KL, Rice-Davies Kathleen K, Lo Rebecca R et al.

Interpretation of post-mortem drug concentrations remains a major challenge in forensic toxicology because factors, including post-mortem redistribution, drug tolerance, polypharmacy and inter-individual variability, limit the utility of fixed therapeutic, toxic or purportedly fatal concentration thresholds. Using data from the National Programme on Substance Use Mortality (NPSUM), we examined post-mortem blood drug concentrations within a population-based epidemiological framework. Quantitative concentration data were available for 93 psychoactive substances reported to NPSUM up to 1 November 2022. Concentrations were stratified by age, sex, ethnicity, prescription status, drug involvement in death and co-detection with other substances. Four exemplar drugs representing distinct pharmacological classes and toxicological profiles were selected for detailed evaluation: methadone, diazepam, 3,4-methylenedioxymethamphetamine (MDMA) and quetiapine. Quantifiable concentrations were available in 4514 methadone, 3482 diazepam, 540 MDMA and 677 quetiapine cases. Across all four drugs, concentration distributions demonstrated substantial variability and extensive overlap between deaths in which the drug was implicated and those in which it was not. Although some substances showed higher median concentrations in implicated cases, no concentration threshold reliably differentiated drug-related from non-drug-related deaths. Demographic stratification altered concentration distributions but did not materially improve discrimination. These findings suggest that extensive overlap in post-mortem drug concentrations is a fundamental characteristic of forensic toxicology data. Population-based concentration distributions provide important contextual information but should be interpreted within a holistic framework that incorporates pathological findings, clinical history, co-administered substances and the circumstances of death.

PMID 42839309
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