Pinazepam Explained

Pinazepam (marketed under the brand name Domar and Duna) is a benzodiazepine drug.[1] It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.[2]

Pinazepam and its metabolite N-desmethyldiazepam are transferred to the developing fetus in utero, but the plasma drug level in the mother is usually significantly higher than in the fetus.[3]

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.[4] Pinazepam is rapidly absorbed after oral administration. The main active metabolites of pinazepam are depropargylpinazepam (N-desmethyldiazepam, nordazepam) and oxazepam.[5] 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.[6] [7] [8] The elimination half-life is longer in the elderly.[9]

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Notes and References

  1. Schütz H, Holland EM, Kazemian-Erdmann F, Schölermann K . [Screening of the new benzodiazepine derivative, pinazepan, and its major metabolites] . Arzneimittel-Forschung . 38 . 9 . 1372–5 . September 1988 . 3146986 .
  2. Janbroers. J. M.. 1984. Pinazepam: review of pharmacological properties and therapeutic efficacy. Clinical Therapeutics. 6. 4. 434–450. 0149-2918. 6147192.
  3. Pacifici GM, Cuoci L, Guarneri M, Fornaro P, Arcidiacono G, Cappelli N, Moggi G, Placidi GF . 6 . Placental transfer of pinazepam and its metabolite N-desmethyldiazepam in women at term . European Journal of Clinical Pharmacology . 27 . 3 . 307–10 . 1984 . 6150857 . 10.1007/BF00542165 . 1389302 .
  4. Web site: Diazepam Injection BP - Summary of Product Characteristics (SmPC) - (emc). 2021-08-23. www.medicines.org.uk.
  5. Dinis-Oliveira. Ricardo Jorge. Sep 14, 2017. Metabolic profile of oxazepam and related benzodiazepines: clinical and forensic aspects. Drug Metabolism Reviews. 49. 4. 451–463. 10.1080/03602532.2017.1377223. 1097-9883. 28903606. 4528255.
  6. Janbroers JM . Pinazepam: review of pharmacological properties and therapeutic efficacy . Clinical Therapeutics . 6 . 4 . 434–50 . 1984 . 6147192 .
  7. Pacifici GM, Placidi GF, Fornaro P, Gomeni R . Pharmacokinetics of pinazepam in healthy volunteers . International Journal of Clinical Pharmacology Research . 3 . 5 . 331–7 . 1983 . 6147314 .
  8. Pacifici GM, Placidi GF, Fornaro P, Gomeni R . Pinazepam: a precursor of N-desmethyldiazepam . European Journal of Clinical Pharmacology . 22 . 3 . 225–8 . 1982 . 6809477 . 10.1007/BF00545219 . 1977572 .
  9. Pacifici GM, Cuoci L, Placidi GF, Fornaro P, Gomeni R . Elimination kinetics of desmethyldiazepam in two young and two elderly subjects . European Journal of Drug Metabolism and Pharmacokinetics . 7 . 1 . 69–72 . Jan 1982 . 6802645 . 10.1007/bf03189546 . 21836038 .

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