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Information @ a Glance

General

  • Diazepam is a "classical" benzodiazepine derivative drug.
  • Other classical benzodiazepines include clonazepam, lorazepam, oxazepam, alprazolam, nitrazepam, flurazepam, bromazepam and clorazepate.
  • Diazepam, first marketed as Valium by Hoffmann-La Roche.
  • Diazepam possesses anxiolytic, anticonvulsant, sedative, skeletal muscle relaxant and amnestic properties.
  • Diazepam occurs as solid white or yellow crystals.
  • Diazepam can absorb into plastic, and therefore diazepam solution is not stored in plastic bottles or syringes etc.

Synthesis & Process

  • Diazepam works by acting on receptors in the brain called GABA receptors. This causes the release of a neurotransmitter called GABA in the brain.
  • Electron-capture gas chromatography or reversed-phase “high-performance” liquid chromatography is used for concurrent analysis for diazepam and nordiazepam in serum.
  • The psychomotor recovery of patients sedated with either midazolam or Diazepam has been compared using the digit symbol substitution test and the Trieger test.
  • Open-heart operations with cardiopulmonary bypass, anaesthetized by using primarily the combination of diazepam with pentazocine.

Application

  • Diazepam is mainly used to treat anxiety, insomnia, and symptoms of acute alcohol or opiate withdrawal.
  • Diazepam is rarely used for the long-term treatment of epilepsy.
  • Diazepam is used as a short term sedative and anxiolytic for cats and dogs.
  • Diazepam is also used as a muscle relaxant for horses.
  • Diazepam increases the central depressive effects of alcohol, other hypnotics/sedatives (e.g. barbiturates), narcotics, and other muscle relaxants.
  • Diazepam-binding inhibitor(DBI) mediates the postprandial rise in plasma cholecystokinin-releasing peptide(CCK) levels.

Technology

  • The heat effect associated with the binding of diazepam to human serum albumin has been measured using flow microcalorimetry technique.
  • The effect of diazepam on respiration has been investigated by the modification of the rebreathing CO2-challenge technique.
  • The drug diazepam is measured by gas-liquid chromatography technique, with use of an electron capture detector.
  • HPLC method is developed for identification and simultaneous determination of diazepam and preservatives (benzyl alcohol and benzoic acid/sodium benzoate).

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