1-hydroxy-midazolam

1-hydroxy-midazolam (also known as alpha-hydroxymidazolam) is the primary active metabolite of midazolam, formed in humans through hepatic CYP3A-mediated oxidation. It possesses pharmacological activity at the benzodiazepine binding site on the GABA-A receptor, with in vitro receptor affinity approximately 20% that of midazolam. Clinical data suggest it is at least as potent as the parent compound in humans and contributes to the net CNS depressant, anxiolytic, sedative, amnestic, anticonvulsant, and muscle relaxant effects observed after midazolam administration. The metabolite is primarily excreted as its glucuronide conjugate in urine[1][5].

Other names

alpha-hydroxymidazolam1-hydroxymidazolam1-hydroxy midazolamα-hydroxymidazolam