Lirequinil Explained

Lirequinil (Ro41-3696) is a nonbenzodiazepine hypnotic drug which binds to benzodiazepine sites on the GABAA receptor. In human clinical trials, lirequinil was found to have similar efficacy to zolpidem, with less side effects such as clumsiness and memory impairment. However it was also much slower acting than zolpidem, with peak plasma concentrations not reached until 2.5 hours after oral administration, and its O-desethyl metabolite Ro41-3290 is also active with a half-life of 8 hours.[1] [2] [3] [4] This meant that while effective as a hypnotic, lirequinil failed to prove superior to zolpidem due to producing more next-day sedation, and it has not been adopted for clinical use. It was developed by a team at Hoffmann-La Roche in the 1990s.[5]

Notes and References

  1. Dingemanse J, Bury M, Roncari G, Zell M, Gieschke R, Gaillard AW, Odink J, van Brummelen P . Pharmacokinetics and pharmacodynamics of Ro 41-3696, a novel nonbenzodiazepine hypnotic . Journal of Clinical Pharmacology . 35 . 8 . 821–9 . August 1995 . 8522640 . 10.1002/j.1552-4604.1995.tb04126.x. 20456430 .
  2. Dingemanse J, Bury M, Bock J, Joubert P . Comparative pharmacodynamics of Ro 41-3696, a new hypnotic, and zolpidem after night-time administration to healthy subjects . Psychopharmacology . 122 . 2 . 169–74 . November 1995 . 8848532 . 10.1007/BF02246091. 11960902 .
  3. Dingemanse J, Bury M, Hussain Y, van Giersbergen P . Comparative tolerability, pharmacodynamics, and pharmacokinetics of a metabolite of a quinolizinone hypnotic and zolpidem in healthy subjects . Drug Metabolism and Disposition . 28 . 12 . 1411–6 . December 2000 . 11095577 .
  4. Dingemanse J, Pedrazzetti E, van Giersbergen PL . Multiple-dose tolerability, pharmacodynamics, and pharmacokinetics of the quinolizinone hypnotic Ro 41-3696 in elderly subjects . Clinical Neuropharmacology . 24 . 2 . 82–90 . 2001 . 11307042 . 10.1097/00002826-200103000-00003. 21588500 .
  5. US Patent 5561233 Process for the preparation of an intermediate of a benzo[a]quinolizinone derivative

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