Sufentanil (fig. 1) is an opioid analgesic, the thienyl analogue of the 4-anilinopiperidine, fentanyl.

Like fentanyl, it is a centrally acting analgesic which is used in the induction and maintenance of
anaesthesia during cardiac surgery and as a supplement to balanced anaesthesia in general surgery.
As yet, unlike other opioids, it is not used in non-anaesthetic clinical practice. 1.1 Effect on the
Opiate Receptor The multiplicity of the opiate receptor was first recognised by Martin et al. (1976),
and the endogenous opioid system is now considered to involve many receptor subtypes. The
functional significance of the 2 major subtypes /L and 0 has not yet been elucidated fully, but it
appears that the wsubtype may mediate analgesia, and the o-subtype catatonia and other
behavioural phenomena (Kostelitz et al. 1980). In vitro ligand studies have shown that sufentanil is
highly selective for /L-receptors (James & Goldstein 1984; Leysen & Gommeren 1982), being more
selective than fentanyl, methadone, pethidine (meperidine) and morphine (Hermans et al. 1983).
The binding affinity of sufentanil for the w receptor site was 100 times greater than its affinity for
the o-binding .site (Leysen et al. 1983). In vivo studies comparing receptor occupancy and
pharmacological effects in rats have also shown that sufentanil is highly selective for the /L-receptor
si

inistered by other routes. When given by intraventricular injection, sufentanil was more potent than
fentanyl (7 times) and morphine (410 times) with regard to discriminative stimulus (cueing) activity
and analgesic activity in rats (Colpaert et al. 1978). Intrathecal administration of 4-anilinopiperidine
analogues produced analgesia in rats (hot plate and tail flick tests) and cats (skin twitch). Sufentanil
was more potent than morphine, alfentanil and fentanyl but less potent than lofentanil (Noueihed et
al. 1984; Yaksh et al. I 986b). The analgesia produced in decerebrate cats by sufentanil 2.5/Lg was
similar to that produced by fentanyl 25/Lg (Aoki et al. 1986). Although high doses of int~athecal
morphine produced hyperaesthesia in cats and rats, no hyperaesthesia was produced by comparable
doses of sufentanil or alfentanil (Yaksh et al. I 986a). In dogs, the analgesic potency of sufentanil was
625 times that of morphine and 5 times that of fentanyl, the minimal effective doses being 0.00025,
0.0012 and 0.15 mg/kg intravenously, respectively. The safety margin for deep surgical analgesia in
dogs (ratio between the intravenous dose producing severe cardiovascular side effects and that
producing deep surgical analgesia), relative to morphine, was 5 for fentanyl and 24 fo