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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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