Мидазолам

Описание

Midazolam is the most commonly used parenteral sedative in anaesthetic practice. The structure of midazolam is altered by local changes in pH (tautomerism), and the two different forms confer either water or lipid solubility to the drug . At pH<4 the benzodiazepine nucleus opens because of an ionisable amine group in the molecule's structure, and this increases water solubility. At plasma pH the amine group is incorporated back into the unionised ring form of the molecule, which is highly lipid soluble and diffuses rapidly into the brain. A concentrated preparation (5mgml ?1 ) is available for i.m. injection and absorption is rapid compared with diazepam.

Химические свойства

White Crystaline Solid

Использование

In many countries this product is controlled. An import permit may be required. Anesthetic; anticonvulsant; sedative; hypnotic

Общее описание

Midazolam is a benzodiazepine, sold as Dormicum, Hypnovel^?, and Versed as a sedative and treatment for insomnia and seizures. This Snap-N-Spike^? Reference Solution is suitable for many GC/MS or LC/MS applications from clinical toxicology and urine drug testing to pain prescription monitoring or forensic analysis.

Фармакокине?тика

Midazolam undergoes hepatic oxidative metabolism and has an elimination half-life of 2–4h. The major metabolite is 1-hydroxymidazolam, which is biologically active. Midazolam has been used as a sole hypnotic for TI VA and produces superior procedural amnesia compared with propofol, but CSHT increases significantly when used by continuous infusion, and this delays recovery. Clinical studies demonstrate the inferiority of midazolam in terms of time to onset of desired sedation score, slower recovery, less clear-headedness, and significantly longer period of postoperative amnesia compared with propofol.