Fentanyl and the 4-Anilinopiperidine Group of Analgesics

  • Alan F. Casy
  • Robert T. Parfitt
Chapter

Abstract

Paul Janssen’s exploitation of 4-piperidone chemistry during the early 1960s proved remarkably successful in that it led to the clinical use of both a major tranquillizer (haloperidol)(1) and a potent narcotic analgesic, fentanyl.(2) Fentanyl (1, Sublimaze, Leptanol) is related to pethidine and also to basic anilides with analgesic properties such as diampromide 2 (p. 311) and is characterized by high potency and short duration of action. Thus, in mice (tail-clip method) fentanyl is almost 200 times as active as morphine by the sc route and has a faster onset and shorter duration of action than the standard
drug. It shows the usual morphinelike effects, namely, Straub tails, mydriasis, and constipation in mice; in dogs and cats it causes respiratory depression but is devoid of emetic action.(3) A clinical study in postsurgical patients and healthy volunteers showed 0.2 mg fentanyl to be equianalgesic with 10 mg morphine (im route) and the two drugs had similar side effects.(4) The respiratory action of fentanyl in healthy males was judged to be somewhat greater than that of pethidine at equianalgesic dose levels.(5) The rapid onset and short duration of action of fentanyl make it particularly well suited for use in neuroleptanalgesia and it has now achieved widespread use in surgical analgesia,(6) especially when given in combination with a major tranquilizer such as droperidol (3) (Thalamontal contains fentanyl, 50 μg, and droperidol, 2.5 mg/ml).(7)

Keywords

Schiff Base Trans Isomer Potency Ranking Piperidine Ring Propionic Anhydride 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Springer Science+Business Media New York 1986

Authors and Affiliations

  • Alan F. Casy
    • 1
  • Robert T. Parfitt
    • 1
    • 2
  1. 1.University of BathBathUK
  2. 2.Canberra College of Advanced EducationBelconnenAustralia

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