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Pinazepam
Systematic (IUPAC) name
7-chloro-5-phenyl-1-prop-2-yn-1-yl-1,3-dihydro-2 H-1,4-benzodiazepin-2-one
Identifiers
CAS number 52463-83-9
ATC code N05BA14
PubChem 40391
DrugBank ?
Chemical data
Formula C 18H13ClN2O 
Mol. mass 308.8
Synonyms 9-chloro-6-phenyl-2-prop-2-ynyl-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-3-one
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life  ?
Excretion Renal
Therapeutic considerations
Pregnancy cat.  ?
Legal status Schedule IV(US)
Routes Oral

Pinazepam (marketed under the brand name Domar and Duna) is a drug which is a benzodiazepine derivative.[1] It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.

Pinazepam and its metabolite N-desmethyldiazepam pass over to the developing baby in utero, although the blood plasma level in the mother is not the same as in the baby in utero.[2]

Pinazepam differs from other benzodiazepines in that it has a propargyl group at the n1 position of the benzodiazepine sketal molecule. It is less toxic than diazepam and in animal studies it appears to produce anxiolytic and anti-agitation properties with limited hypnotic and motor coordination impairing properties. Pinazepam is rapidly absorbed after oral administration. The main active metabolite of pinazepam is depropargylpinazepam (N-desmethyldiazepam) and oxazepam. In humans it acts as a pure anxiolytic agent in that it does not possess to any significant degree the other pharmacological characteristics of benzodiazepines. Its lack of intellectual, motor and hypnotic impairing effects makes it more appropriate than other benzodiazepines for day time use.[3][4][5] The elimination half life is longer in the elderly.[6]

See also

References

  1. ^ Schütz, H; Holland; Kazemian-Erdmann; Schölermann (Sep 1988). "Screening of the new benzodiazepine derivative, pinazepan, and its major metabolites". Arzneimittel-Forschung 38 (9): 1372–5. ISSN 0004-4172. PMID 3146986.  
  2. ^ Pacifici, GM; Cuoci; Guarneri; Fornaro; Arcidiacono; Cappelli; Moggi; Placidi (1984). "Placental transfer of pinazepam and its metabolite N-desmethyldiazepam in women at term". European journal of clinical pharmacology 27 (3): 307–10. ISSN 0031-6970. PMID 6150857.  
  3. ^ Janbroers, JM (1984). "Pinazepam: review of pharmacological properties and therapeutic efficacy". Clinical therapeutics 6 (4): 434–50. ISSN 0149-2918. PMID 6147192.  
  4. ^ Pacifici, GM; Placidi; Fornaro; Gomeni (1983). "Pharmacokinetics of pinazepam in healthy volunteers". International journal of clinical pharmacology research 3 (5): 331–7. ISSN 0251-1649. PMID 6147314.  
  5. ^ Pacifici, GM; Placidi; Fornaro; Gomeni (1982). "Pinazepam: a precursor of N-desmethyldiazepam". European journal of clinical pharmacology 22 (3): 225–8. ISSN 0031-6970. PMID 6809477.  
  6. ^ Pacifici, GM; Cuoci; Placidi; Fornaro; Gomeni (Jan 1982). "Elimination kinetics of desmethyldiazepam in two young and two elderly subjects". European journal of drug metabolism and pharmacokinetics 7 (1): 69–72. ISSN 0398-7639. PMID 6802645.  

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