midazolam   Click here for help

GtoPdb Ligand ID: 3342

Synonyms: Buccolam® | Dormicum® | Nayzilam® | USL261 (nasal spray formulation) [1] | Versed®
Approved drug PDB Ligand
midazolam is an approved drug (FDA (2000), EMA (2011))
Compound class: Synthetic organic
Comment: Midazolam is a benzodiazepine class sedative drug.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 2
Hydrogen bond donors 0
Rotatable bonds 1
Topological polar surface area 29.66
Molecular weight 325.08
XLogP 4.57
No. Lipinski's rules broken 0
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Canonical SMILES Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F
Isomeric SMILES Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F
InChI InChI=1S/C18H13ClFN3/c1-11-21-9-13-10-22-18(14-4-2-3-5-16(14)20)15-8-12(19)6-7-17(15)23(11)13/h2-9H,10H2,1H3
No information available.
Summary of Clinical Use Click here for help
Used as an agent for sedation, anziolysis or amnesia prior to surgical, diagnostic or endoscopic procedures. Also used in the induction of general anaesthesia.
In May 2019, the FDA approved the use of a nasal spray formulation of midazolam (Nayzilam®) as an anti-epileptic therapy, based on results from clinical trial NCT01390220 [2]. Nayzilam® is indicated as a short-term treatment for seizure clusters in patients (≥12 years old) with epilepsy.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Midazolam is a benzodiazepine (BZ) drug binds to the allosteric BZ site on the GABAA channel. This potentiates the inhibitory activity of GABA by increasing the period for which the chloride channel remains open.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01390220 Study to Evaluate the Safety and Efficacy of USL261 (Intranasal Midazolam) in Patients With Seizure Clusters Phase 3 Interventional UCB Pharma
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