Further research is therefore needed to compare nalbuphine with other postoperative opioids.Although nalbuphine possesses opioid antagonist activity, there is evidence that in nondependent patients it will not antagonize an opioid analgesic administered just before, concurrently, or just after an injection. Therefore, patients receiving an opioid analgesic, general anesthetics, phenothiazines, or other tranquilizers, sedatives, hypnotics, or other CNS depressants (including alcohol) concomitantly with Nalbuphine may exhibit an additive effect. When such combined therapy is contemplated, the dose of one or both agents should be reduced. In addition to the relief of pain, the drug has been studied as a treatment for morphine induced pruritus (itching). Pruritus is a common side effect of morphine or other pure MOR agonist opioid administration. Kjellberg et al. (2001) published a review of clinical trials relating to the prevalence of morphine induced pruritus and its pharmacologic control. The authors state that nalbuphine is an effective anti-pruritic agent against morphine induced pruritus. The effect may be mediated via central nervous system mechanisms. Pan (1998) summarizes the evidence that activation at the pharmacological level of the KOR antagonizes various MOR-mediated actions in the brain. The author states that the neural mechanism for this potentially very general MOR-antagonizing function by the KOR may have broad applications in the treatment of central nervous system mediated diseases. He does not state, however, that nalbuphines pharmacological mechanism of action for pruritus is the result of this interaction between the two opioid receptors.
Nalbuphine, sold under the brand names Nubain among others, is an opioid analgesic which is used in the treatment of pain. It is given by injection into a vein, muscle, or fat.Side effects of nalbuphine include sedation, sweatiness, clamminess, nausea, vomiting, dizziness, vertigo, dry mouth, and headache. Unlike other opioids, it has little to no capacity for euphoria or respiratory depression. It also has little to no incidence of dysphoria, dissociation, hallucinations, and related side effects at typical therapeutic doses. Nalbuphine is a mixed agonist/antagonist opioid modulator. Specifically, it acts as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor (MOR) and as a high-efficacy partial agonist of the κ-opioid receptor (KOR), whereas it has relatively low affinity for the δ-opioid receptor (DOR) and sigma receptors.Nalbuphine was patented in 1963 and was introduced for medical use in the United States in 1979. It is marketed in many countries throughout the world. Medical uses
Nalbuphine is indicated for the relief of moderate to severe pain. It can also be used as a supplement to balanced anesthesia, for preoperative and postoperative analgesia, and for obstetrical analgesia during labor and delivery. However, a 2014 Cochrane Systematic Review concluded that from the included studies, there was limited evidence to demonstrate that "0.1 to 0.3mg/kg nalbuphine compared to placebo might be an effective postoperative analgesic" for pain treatment in children.