Analgesic effect of intramuscular and oral nalbuphine in postoperative pain.

In a double-blind study using patients' subjective reports as indices of analgesia, the relative analgesic potency of intramuscular and oral nalbuphine was determined in 104 postoperative patients. Effects of single doses of 3 and 9 mg of intramuscular nalbuphine were compared with those of 15- and 45-mg oral doses of nalbuphine by means of a parallel study design (26 patients per treatment group). When both intensity and duration of analgesia are considered (i.e., total analgesic effect), oral nalbuphine is 1/4 to 1/5 as potent as intramuscular nalbuphine. In terms of peak effect, however, oral nalbuphine is only 1/10 as potent. The oral/parenteral potency ratio for total effect is close to those obtained by Houde et al. in studies of morphine (1/6), metopon (1/5), hydromorphone (1/5), and oxymorphone (1/6) and suggests that oral nalbuphine undergoes substantial biotransformation on first pass through gut mucosa and liver. Since intramuscular nalbuphine is approximately equipotent to morphine, it should be feasible to equal the analgesia induced by the usual intramuscular doses of morphine with reasonable oral doses of nalbuphine. Although nalbuphine is a mixed agonist/antagonist analgesic, no psychotomimetic reactions were observed.