Phenoperidine
Encyclopedia
Phenoperidine was discovered by Janssen Pharmacutica 1960. Marketed as its hydrochloride as Operidine or Lealgin, is an opioid
used as a general anesthetic. It is a derivative of isonipecotic acid
, like pethidine
, and is metabolized in part to norpethidine
. It is 20-200 times as potent as pethidine as an analgesic.
In humans 1 milligram is equipotent with 10 mg morphine. It has less effect on the circulatory system
and is less hypnotic
than morphine, but it has about the same emetic effect. The nausea can be prevented by giving droperidol
or haloperidol
. After an intravenous dose the analgesia sets in after 3-5 minutes.
Phenoperidine shares structural similarities with both pethidine
and haloperidol
(and related butyrophenone antipsychotics, e.g. droperidol
). While not commonly used today in clinical practice, it is of historical interest as a precursor in the development of some of the most widely used neuroleptic drugs on the market today.
Opioid
An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...
used as a general anesthetic. It is a derivative of isonipecotic acid
Isonipecotic acid
Isonipecotic acid is a heterocyclic compound which acts as a GABAA receptor partial agonist.It consists of a piperidine ring with a carboxylic acid moiety in the iso position ....
, like pethidine
Pethidine
Pethidine or meperidine Pethidine (INN) or meperidine (USAN) Pethidine (INN) or meperidine (USAN) (commonly referred to as Demerol but also referred to as: isonipecaine; lidol; pethanol; piridosal; Algil; Alodan; Centralgin; Dispadol; Dolantin; Mialgin (in Indonesia); Petidin Dolargan (in Poland);...
, and is metabolized in part to norpethidine
Norpethidine
Norpethidine is a 4-phenylpiperidine derivative that is both a metabolite of and a precursor to pethidine ....
. It is 20-200 times as potent as pethidine as an analgesic.
In humans 1 milligram is equipotent with 10 mg morphine. It has less effect on the circulatory system
Circulatory system
The circulatory system is an organ system that passes nutrients , gases, hormones, blood cells, etc...
and is less hypnotic
Hypnotic
Hypnotic drugs are a class of psychoactives whose primary function is to induce sleep and to be used in the treatment of insomnia and in surgical anesthesia...
than morphine, but it has about the same emetic effect. The nausea can be prevented by giving droperidol
Droperidol
Droperidol is an antidopaminergic drug used as an antiemetic and antipsychotic...
or haloperidol
Haloperidol
Haloperidol is a typical antipsychotic. It is in the butyrophenone class of antipsychotic medications and has pharmacological effects similar to the phenothiazines....
. After an intravenous dose the analgesia sets in after 3-5 minutes.
Phenoperidine shares structural similarities with both pethidine
Pethidine
Pethidine or meperidine Pethidine (INN) or meperidine (USAN) Pethidine (INN) or meperidine (USAN) (commonly referred to as Demerol but also referred to as: isonipecaine; lidol; pethanol; piridosal; Algil; Alodan; Centralgin; Dispadol; Dolantin; Mialgin (in Indonesia); Petidin Dolargan (in Poland);...
and haloperidol
Haloperidol
Haloperidol is a typical antipsychotic. It is in the butyrophenone class of antipsychotic medications and has pharmacological effects similar to the phenothiazines....
(and related butyrophenone antipsychotics, e.g. droperidol
Droperidol
Droperidol is an antidopaminergic drug used as an antiemetic and antipsychotic...
). While not commonly used today in clinical practice, it is of historical interest as a precursor in the development of some of the most widely used neuroleptic drugs on the market today.