Diazepam
Diazepam is a long-acting benzodiazepine that acts as a positive allosteric modulator of the GABA-A receptor, enhancing the brain's dominant inhibitory signaling. That amplified inhibition yields anti-anxiety, sedative, anticonvulsant, and muscle-relaxant effects, and the drug is used for anxiety, alcohol withdrawal, seizures, and sedation before procedures. A small molecule (C16H13ClN2O), it is distinguished by an especially long reach: its half-life spans roughly 20 to 100 hours, extended further by active metabolites, so effects and any accumulation persist well beyond a single dose. This durability suits some indications but also raises the potential for dependence with prolonged use, as the nervous system adapts to continuous GABA enhancement. Diazepam is an approved medicine used across neurology, psychiatry, and acute care.
A long-acting benzodiazepine that enhances GABA-mediated inhibition in the brain, providing anxiolytic, sedative, anticonvulsant, and muscle-relaxant effects; used for anxiety, alcohol withdrawal, seizures, and procedural sedation. It has a risk of dependence with long-term use.
分子量
284.7400 g/mol
LogP
3.00
TPSA
32.70 Ų
Lipinski 五规则
符合
治疗领域
药物分类
作用机制
Positive allosteric modulator of GABA-A receptors.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Positive allosteric modulator of GABA-A receptors.
二维结构
Cite this structure
Embed this structure
SMILES
CN1C(=O)CN=C(c2ccccc2)c2cc(Cl)ccc21
InChI
InChI=1S/C16H13ClN2O/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9H,10H2,1H3
Molecular Formula
C16H13ClN2O
HBD / HBA
- / 2
可旋转键数
1
重原子数
20
Diazepam and morphine together produce additive CNS and respiratory depression, carrying an FDA boxed warning for fatal outcomes.
Diazepam and quetiapine together significantly increase CNS depression and carry risk of severe sedation and cardiorespiratory compromise.
Diazepam and tramadol together produce additive CNS and respiratory depression with an FDA boxed warning for concomitant opioid-benzodiazepine use.
Concurrent use of diazepam and oxycodone dramatically increases the risk of fatal respiratory depression, per FDA boxed warning.
Diazepam and zolpidem together produce compounded GABA-A-mediated CNS depression, with risk of severe sedation and respiratory compromise.
Ranitidine can modestly increase diazepam bioavailability by raising gastric pH and weakly inhibiting hepatic CYP2C19-mediated diazepam metabolism.
Diazepam and diphenhydramine produce additive CNS depression, with risk of profound sedation, cognitive impairment, and falls.
No side effects recorded
Side effect data is not yet available for this drug.
常见问题
A long-acting benzodiazepine that enhances GABA-mediated inhibition in the brain, providing anxiolytic, sedative, anticonvulsant, and muscle-relaxant effects; used for anxiety, alcohol withdrawal, seizures, and procedural sedation. It has a risk of dependence with long-term use.
Positive allosteric modulator of GABA-A receptors.
Key pharmacokinetic parameters for Diazepam: Half-life: 20-100 hours.
Yes, Diazepam is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
Related Drugs
Same Drug Class
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL12. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 3016. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.
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