Drug Database
DI

diazepam (Stesolid / diazepam, Alpharma)

✓ Approved

Pfizer, Inc. · GABRA1 · 小分子

什么是 diazepam?

diazepam 是一种小分子,由Pfizer, Inc.研发。该药已获批,用于治疗相关适应症,给药途径:Rectal。

药物档案

商品名Stesolid, diazepam, Alpharma
公司Pfizer, Inc.
药物类别小分子
分子靶点GABRA1, GABRA2, GABRA3, GABRA5
给药途径Rectal
状态Approved

作用机制

分子靶点

diazepam 作用于 4 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)
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

diazepam 针对 2 个适应症,涉及 2 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersAnxiety✓ Approved
Nervous system disordersEpilepsy✓ Approved

相关研究文献

PubMedOrvosi hetilap2026-08-02

[Comparison of the side effect profiles of compounds with central muscle-relaxing effect].

Kopitkó Csaba C, Pettendi Éva É

In addition to other conditions involving increased muscle spasms, centrally acting muscle relaxants (guaifenesin, tolperisone, methocarbamol, chlorzoxazone, diazepam, baclofen and tizanidin) provide relief for a significant proportion of patients suffering from low back pain. Of these, tolperisone has recently been restricted by official decision due to the high incidence of anaphylactic reactions associated with its use. The aim of our work is to analyze the frequency of side effects of this group of drugs in order to help clinicians choose the appropriate medication. According to data from the World Health Organization, tolperisone is considered a safe drug, except for the aforementioned serious allergic side effect. Mortality (including suicide) associated with the administration of these medicines is the highest among the reported side effects for diazepam, followed by tizanidine and methocarbamol. Ineffectiveness was most commonly reported for guaifenesin, followed by baclofen and tizanidine. Tolperisone was the most favorable drug in terms of both mortality and ineffectiveness. We present in detail the gastrointestinal, major neurological, and psychiatric side effects that make it difficult, and in some cases impossible, to take the drugs, and we also mention the disturbing skin and eye symptoms. Orv Hetil. 2026; 167(31): 1224-1230.

PMID 42543011
阅读全文 →
PubMedEpilepsia2026-08-02

Acute effects of anti-seizure medications on network level dynamics: A systematic comparison using multielectrode arrays.

Marku Griselda G, Gschossmann Lena L, Hallmann Kerstin K, Beck Heinz H et al.

A multi-electrode array (MEA) is a powerful extracellular recording technique for long-term monitoring of neuronal network activity. In recent years, MEA-based assays have been applied increasingly to evaluate drug efficacy and neurotoxicity, including the assessment of anti-seizure medications (ASMs). However, systematic comparisons of ASMs with different mechanisms of action under identical experimental conditions remain limited. In this study, we evaluated the effects of 18 ASMs on neuronal network activity using MEA recordings under standardized conditions. Network activity was characterized using four components-spike, burst, network burst, and synchrony-and a total of 44 MEA-derived parameters were analyzed. Dimensionality reduction by t-distributed stochastic neighbor embedding (t-SNE) followed by hierarchical clustering classified the 18 ASMs into four distinct clusters. Cluster 1, including S-licarbazepine, oxcarbazepine, and lamotrigine, exhibited pronounced effects across all four network components. Cluster 2, comprising carbamazepine, eslicarbazepine acetate, phenytoin, phenobarbital, and stiripentol, significantly affected spike and burst duration but showed only limited effects on burst frequency, network burst frequency, or synchrony. Cluster 3 was solely diazepam, for which minimal effects were detected. The remaining ASMs were assigned to Cluster 4 and produced only minimal measurable effects in network activity. Several limitations should be considered, including the use of primary neuron cultures, incomplete maturation of certain drug targets, evaluation of only acute drug effects, and the limited spatial resolution of low-density MEA systems. Nevertheless, our results demonstrate that this MEA-based platform enables systematic evaluation of ASM effects on neuronal networks under identical experimental conditions. Furthermore, multivariate and unsupervised clustering analysis of 44 MEA parameters facilitated classification independent of drug mechanism of action. These findings suggest that MEA, combined with multidimensional data analysis, may provide a useful platform for the direct comparison of ASMs and could contribute to future pharmacological screening and drug discovery efforts.

PMID 42541378
阅读全文 →
PubMedSalud publica de Mexico2026-07-31

López-Brambila Miguel Ángel MÁ, Fleiz-Bautista Clara C, Cruz-Martín Del Campo Silvia Lorenia SL, Cruz-López Miguel Bencomo MB et al.

Identificar los medicamentos con potencial psicoactivo y uso indebido en la población mexicana. Material y métodos. Se utilizaron datos de la Encuesta Nacional de Consumo de Drogas, Alcohol y Tabaco 2025, la muestra incluyó a 555 personas que reportaron uso indebido de medicamentos psicoactivos alguna vez en la vida, y representan a 2.4 millones de personas. El medicamento más reportado fue el tramadol (86.8%), sustancia clasificada como opioide. Le siguieron el clonazepam (76.5%) y el diazepam (15.1%), ambos tranquilizantes. En tercer lugar, se encontró el metilfenidato (37.8%), considerado un estimulante de uso médico. Otros medicamentos fueron mencionados con muy baja frecuencia, entre ellos morfina, fentanilo, alprazolam, flunitrazepam, clobenzorex, fentermina, anfetamina, fenobarbital y pregabalina. Conclusión. La regulación del uso indebido de medicamentos psicoactivos en México requiere fortalecer los mecanismos de coordinación, supervisión y vigilancia, así como promover estrategias de prevención e impulsar la educación en salud.

PMID 42536901
阅读全文 →
PubMedCureus2026-07-31

Intentional Large-Volume Diazinon Ingestion Complicated by Seizure and Acute Respiratory Failure: A Case Report.

Alnuaimi Khuloud H KH, Alharmoodi Salama S, Almerri Reem R, Alneyadi Mouza M et al.

Organophosphate poisoning is a major cause of acute cholinergic toxicity and can progress rapidly to respiratory failure and death. In the emergency setting, diagnosis is often clinical, and treatment should not be delayed while awaiting confirmation of the specific compound. We report a case of a 30-year-old male patient who presented after intentional ingestion of a large reported volume of diazinon-containing pesticide. Within approximately 30 minutes of ingestion, he developed acute cholinergic manifestations, including bradypnea, bradycardia, hypotension, hypersalivation, vomiting, diarrhea, and depressed level of consciousness, complicated by a generalized tonic-clonic seizure. The seizure was treated with diazepam, and atropine was initiated before transfer to the emergency department. On arrival, the patient was in severe respiratory distress with profuse secretions and required urgent endotracheal intubation and mechanical ventilation. Empiric treatment for suspected organophosphate poisoning was continued with atropine and pralidoxime, alongside supportive care. Collateral history later identified the ingested product as Diacidol 600 Emulsifiable Concentrate, containing diazinon 600 g/L, equivalent to 60% weight/volume. Plasma butyrylcholinesterase, red blood cell acetylcholinesterase, and toxicological confirmation testing were not available at our institution at the time of evaluation, which represents a limitation of this report. The patient was admitted to the intensive care unit and managed with atropine and pralidoxime infusions, ventilatory support, and close monitoring for delayed neuromuscular complications. His cholinergic features resolved, and he was successfully extubated within 24 hours. Antidotal therapy was discontinued after sustained clinical improvement, and he remained stable during subsequent ward observation. This case emphasizes that severe organophosphate poisoning remains a clinical diagnosis during initial resuscitation. Early airway protection, titrated atropinization, pralidoxime therapy, benzodiazepines for seizures, and observation for delayed complications are central to favorable outcomes.

PMID 42535217
阅读全文 →
PubMedPediatric neurology2026-07-30

Neurodevelopmental Risk Factors and Comparative Efficacy of Ketogenic Diet in Children With Spike-Wave Activation in Sleep: A Cohort Study.

Ma Jiannan J, Wang Juan J, Song Xiaojie X, Xie Lingling L et al.

Children with spike-wave activation in sleep (SWAS) face significant neurodevelopmental impairments, including cognitive deficits, oropharyngeal dysfunction and attention-deficit/hyperactivity disorder (ADHD). While SWAS is a known contributor, the impact of specific clinical factors and the comparative efficacy of treatments like ketogenic diet (KD), steroids, and benzodiazepines (BZDs) on outcomes remain unclear. This retrospective cohort study analyzed 134 children with SWAS treated at Children's Hospital of Chongqing Medical University (2015-2024). Clinical data, electroencephalograph, neurodevelopmental assessment, and treatment response were collected. Treatment included KD (n = 11), steroids (n = 72), BZDs (n = 105, including a high-dose diazepam subgroup n = 5), and antiseizure medication (ASM) adjustments (n = 275). Higher seizure frequency correlated significantly with increased cognitive impairment (P < 0.05), oropharyngeal dysfunction (P < 0.05), ADHD (P < 0.05), and relapse rate (P < 0.05). Earlier seizure onset and SWAS onset predicted higher relapse. Structural abnormalities were associated with earlier seizure onset (P < 0.05) and greater cognitive impairment (P < 0.05). Relapse correlated with earlier onset and higher oropharyngeal dysfunction/ADHD (P < 0.05). Treatment response rates were: KD 81.8% (9/11), steroids 65.3% (47/72), BZDs 47.6% (50/105), ASM adjustments 18.9% (52/275). High-dose diazepam (0.5-1.0 mg/kg/day) achieved 80% (4/5) response. KD, steroids, and BZDs were significantly more effective than ASM adjustments (P < 0.05). Seizure frequency is a critical modifiable predictor of neurodevelopmental impairment and relapse in SWAS, independent of SWAS burden. Structural etiology increases cognitive impairment risk. KD demonstrates efficacy for Spike-Wave Index reduction, comparable to steroids and BZDs, with no statistically significant intergroup differences. High-dose diazepam shows promise for refractory cases. ASM adjustments, while less effective for Spike-Wave Index, offer practical seizure control.

PMID 42526162
阅读全文 →
PubMedEnvironmental geochemistry and health2026-07-30

Pharmaceutical cocktails in aquatic ecosystems: unveiling the hidden ecotoxicological threats to Microcystis aeruginosa.

Souaf Bouthaina B, Methneni Nosra N, Hassani Rym R, Bosly Hanan Abo Alkasem HAA et al.

Pharmaceutical compounds (PhACs), continuously released into the environment, represent a growing ecotoxicological threat to aquatic ecosystems. While the toxicity of individual pharmaceuticals has been extensively investigated, the effects of complex mixtures, the so-called "cocktail effect", remain poorly understood, particularly for primary producers such as cyanobacteria. This study evaluates the individual and combined effects of four commonly detected pharmaceuticals in aquatic environments: acetaminophen (APAP), atenolol (ATN), carbamazepine (CBZ), and diazepam (DZP), using the model cyanobacterium Microcystis aeruginosa over a 25-day exposure period at environmentally relevant concentrations (0.01-545 µg/L). The results demonstrate a clear dose-dependent toxicity of the individual compounds (biomass reduced by 85-91%; chlorophyll reduced by 54-70%). Exposure to lower concentrations exhibited moderate reductions in chlorophyll (0.23-0.81 mg/L to 4.90-5.96 mg/L). The most remarkable results are the amplification of toxicity at combined low concentration (low-mix group caused 52% growth inhibition compared to only 14-24% of single pharmaceuticals at the same low doses). The high-dose mixture had the greatest effect on M. aeruginosa by 58.7% growth inhibition. Multi-biomarker analyses indicated significant changes in 1) esterase activity (60.7% decrease), 2) microcystin-LC production (fivefold increase from 0.55 to 2.90 µg/L), and 3) genotoxic effects (IF > 1.5), as evidenced by the SOS chromotest particularly in treatments containing CBZ. Overall, the multi-biomarker responses indicate that pharmaceutical mixtures overwhelm cellular defenses, inducing amplified stress responses even at environmentally realistic concentrations. These findings highlight the urgent need to incorporate mixture toxicity into risk assessment frameworks.

PMID 42530741
阅读全文 →

注册免费账户还可查看另外 9996 篇文献

免费注册查看全部文献 →

了解更多diazepam