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modified on 29 April 2009 at 13:08 ••• 2,431 views

Quazepam

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Quazepam induces impairment of motor function and has hypnotic properties. Quazepam is used to treat insomnia.

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Quazepam
Systematic (IUPAC) name
7-chloro- 5-(2-fluorophenyl)- 1-(2,2,2-trifluoroethyl)- 1,3-dihydro- 2H -1,4-benzodiazepin- 2-thione
Identifiers
CAS number 36735-22-5
ATC code N05CD10
PubChem 4999
DrugBank DB01589
Chemical data
Formula C17H11ClF4N2S 
Mol. mass 386.795 g/mol
Pharmacokinetic data
Bioavailability 29–35%
Metabolism Hepatic
Half life 39 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

X(AU) X(US)

Legal status

Schedule IV(US)

Routes Oral


Contents

Quazepam Indication

Used to treat insomnia.


Quazepam Pharmacology

Quazepam is a benzodiazepine derivative. The main pharmacological action of quazepam is the enhancement of the neurotransmitter, GABA at the GABAA receptor.


Quazepam Mechanism of Action

Benzodiazepines bind nonspecifically to benzodiazepine receptors, which affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

Quazepam Absorption

Bioavailability is 29-35% following oral administration.


Quazepam Half Life

39 hours


Additional Information

More likely than short-acting benzodiazepine to cause daytime sedation and fatigue; is classified as a long-acting benzodiazepine hypnotic (eg, flurazepam), this long duration of action may prevent withdrawal symptoms when therapy is discontinued. Abrupt discontinuation after sustained use (generally >10 days) may cause withdrawal symptoms.


Anesthesia and Critical Care Concerns

Quazepam is more likely than short-acting benzodiazepine to cause daytime sedation and fatigue. It is classified as a long-acting benzodiazepine hypnotic (like flurazepam - Dalmane®); this long duration of action may prevent withdrawal symptoms when therapy is discontinued. Abrupt discontinuation after sustained use (generally >10 days) may cause withdrawal symptoms.

Quazepam brand names

  • Doral® (US, CA)
  • Dormé® (ZA)
  • Quazium® (IT)
  • Quiedorm® (ES)
  • Cetrane
  • Dormalin
  • Oniria
  • Prosedar
  • Selepam