Prazepam

Source: Wikipedia, the free encyclopedia.
Prazepam
Clinical data
Other names9-chloro-2-(cyclopropylmethyl)-6-phenyl-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen- 3-one
AHFS/Drugs.comMicromedex Detailed Consumer Information
MedlinePlusa601036
Routes of
administration
Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
MetabolismHepatic
Elimination half-life36–200 hours
ExcretionRenal
Identifiers
  • 7-Chloro-1-(cyclopropylmethyl)-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one
JSmol)
  • Clc4cc\1c(N(C(=O)C/N=C/1c2ccccc2)CC3CC3)cc4
  • InChI=1S/C19H17ClN2O/c20-15-8-9-17-16(10-15)19(14-4-2-1-3-5-14)21-11-18(23)22(17)12-13-6-7-13/h1-5,8-10,13H,6-7,11-12H2 checkY
  • Key:MWQCHHACWWAQLJ-UHFFFAOYSA-N checkY
  (verify)

Prazepam is a

desmethyldiazepam which is responsible for the therapeutic effects of prazepam.[4]

Indications

Prazepam is indicated for the short-term treatment of

Desmethyldiazepam, an active metabolite, has a very long half-life of 29 to 224 hours, which contributes to the therapeutic effects of prazepam.[7][8]

Side effects

Side effects of prazepam are less profound than with other

fatigue or "feeling spacey" can also occur but less commonly than with other benzodiazepines. Other side effects include feebleness, clumsiness or lethargy, clouded thinking and mental slowness.[12][13][14]

Tolerance, dependence and withdrawal

protracted withdrawal syndrome.[18]

Benzodiazepines can induce serious problems of addiction, which is one of the main reasons for their use being restricted to short-term use. A survey in Senegal found that the majority of doctors believed that their training in this area was generally poor. It was recommended that national authorities take urgent action regarding the rational use of benzodiazepines. Almost one-fifth of doctors ignored prescription guidelines regarding short-term use of benzodiazepines, and almost three-quarters of doctors regarded their training and knowledge of benzodiazepines to be inadequate. More training regarding benzodiazepines has been recommended for doctors.[19][20]

Contraindications and special caution

Benzodiazepines require special precaution if used in the elderly, during pregnancy, in children, alcohol or drug-dependent individuals and individuals with

psychiatric disorders.[21]

Mechanism of action

Prazepam exerts its therapeutic effects primarily via modulating the

GABA function in the brain.[22] Prazepam like other benzodiazepines has anticonvulsant properties, but its anticonvulsant properties are not as potent as other benzodiazepines when tested in animal studies.[23][24][25][26]

Pharmacokinetics

Prazepam is metabolised into descyclopropylmethylprazepam (also known as

desmethyldiazepam) and 3-hydroxyprazepam which is further metabolised into oxazepam.[27][28][29][30][31] Prazepam is a prodrug for descyclopropylmethylprazepam/desmethyldiazepam (also known as norprazepam or nordazepam) which is responsible for most of the therapeutic activity of prazepam rather than prazepam itself.[15][22][32][33]

Interactions

Prazepam may interact with

Overdose

The symptoms of an

sleepiness, agitation and ataxia. Hypotonia may also occur in severe cases. Overdoses in children typically result in more severe symptoms of overdose.[36]

Abuse potential

Prazepam like other benzodiazepines has abuse potential and can be

habit forming. However, its abuse potential may be lower than other benzodiazepines because it has a slow onset of action.[15][37]

Toxicity

Animal studies have found prazepam taken during pregnancy results in delayed growth and causes reproductive abnormalities.[38][39][40]

Trade names

Common

Macedonia: Demetrin, Prazepam, Netherlands: Reapam, Portugal: Demetrin, South Africa: Demetrin, Switzerland: Demetrin, Thailand: Pozapam; Prasepine.[41]

See also

References

  1. ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  2. ^ US Patent 3192199 – Process for the production of I-CYCLO- ALKYL derivatives of I,X-BENZODIAZEPINE
  3. PMID 45081
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  41. ^ "Benzodiazepine Names". non-benzodiazepines.org.uk. Archived from the original on 2008-12-08. Retrieved 2009-05-31.

External links