Pinazepam

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Pinazepam
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Systematic (IUPAC) name
7-chloro-5-phenyl-1-prop-2-yn-1-yl-1,3-dihydro-2H-1,4-benzodiazepin-2-one
Clinical data
Pregnancy
category
  •  ?
Routes of
administration
Oral
Legal status
Legal status
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Biological half-life ?
Excretion Renal
Identifiers
CAS Number 52463-83-9
ATC code N05BA14 (WHO)
PubChem CID 40391
DrugBank ?
Synonyms 9-chloro-6-phenyl-2-prop-2-ynyl-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-3-one
Chemical data
Formula C18H13ClN2O
Molar mass 308.8[[Script error: No such module "String".]]
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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 (nordiazepam, nordazepam) are transferred to the developing fetus in utero, but the plasma drug level in the mother is usually significantly higher than in the fetus.[2]

Pinazepam differs from other benzodiazepines in that it has a propargyl group at the N-1 position of the benzodiazepine structure. 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 metabolites of pinazepam are depropargylpinazepam (N-desmethyldiazepam, nordazepam) and oxazepam. In humans pinazepam 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

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External links


sv:Pinazepam
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  2. Pacifici, GM; Cuoci, L; Guarneri, M; Fornaro, P; Arcidiacono, G; Cappelli, N; Moggi, G; Placidi, GF (1984). "Placental transfer of pinazepam and its metabolite N-desmethyldiazepam in women at term". European journal of clinical pharmacology. 27 (3): 307–10. doi:10.1007/BF00542165. 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, GF; Fornaro, P; Gomeni, R (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, GF; Fornaro, P; Gomeni, R (1982). "Pinazepam: a precursor of N-desmethyldiazepam". European journal of clinical pharmacology. 22 (3): 225–8. doi:10.1007/BF00545219. ISSN 0031-6970. PMID 6809477. 
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