L. Miclea 1, V.A. Negulescu 2
1 Conf. univ. dr., medic primar Farmacologie Clinică, Catedra de Farmacologie Clinică, Toxicologie şi Psihofarmacologie, UMF Carol Davila Bucureşti
2 Asist. Univ., Catedra de Farmacologie Clinică, Toxicologie şi Psihofarmacologie, UMF Carol Davila Bucureşti
Abstract
Opiate analgesics provide the most effective pain relief of any class of agents and are a standard of care for control of mild to severe pain [1]. But even with , the side effects of mu-agonist analgesia are occasionally troublesome. The side effects most commonly encountered are pruritis, nausea/emesis, constipation, urinary retention, respiratory depression and undesirable sedation, and the development of tolerance and dependence. These can remain obstacles to optimally effective employment of opioid analgesia. The use of the opioid mixed agonist—antagonist nalbuphine as an analgesic agent provides a number of advantages. Used as the sole opioid analgesic, it can satisfactorily cover mild to moderate pain with a low incidence of side effects. The ceiling effect of nalbuphine, which prevents it from supplying sufficient analgesia to cover the most severe discomfort, also prevents increasing sedation and respiratory depression as the dose is increased, potentially providing an increased safety margin in comparison to mu-agonists. When nalbuphine is used concurrently with mu-agonists (e.g. morphine, hydromorphone, fen-tanyl), the benefits of both mu- and kappa-analgesia can be obtained, with simultaneously decreased incidence and severity of the common mu-agonist side effects (pruritis, nausea/emesis, constipation, urinary retention, respiratory depression and undesirable sedation). Data from animal studies also suggest that combined nalbuphine and mu-agonist administration may decrease the development of opioid tolerance and dependence. In this article we review an alternative manner of providing opioid analgesia. This is the use, either singly or in combination with other opioid agents, of the mixed opioid agonist—antagonist nalbuphine. Nalbuphine has the potential to maintain or even enhance mu-opioid based analgesia while simultaneously mitigating the common mu-opioid side effects.