Igor E. Kuznetsov* and Volodymyr G. Tymko
Opioids are used for the treatment of moderate to severe pain that is not responsive to other analgesics. Powerful opioid analgesics (full mu-agonists), such as morphine and fentanyl, are highly effective but have multiple harmful side effects, including abuse and dependence. The decades-long search for an ‘ideal analgesic’ that provides fast pain relief for various types of pain, has long-lasting effects, is well-tolerated and can be taken orally has led to the development of biased opioid agonists providing potent pain relief with reduced side effects. These promising new medications still need extensive clinical investigation, while the potential for pharmacokinetic improvements of well-studied and long-used opioid medications remains.
Nalbuphine, a mixed partial mu-receptor antagonist and kappa-receptor agonist, is as effective as morphine in relieving moderate to severe pain and has no serious side effects. It could be considered close to an 'ideal analgesic', with one exception of being administered solely through parenteral routes due to extensive pre-systemic metabolism and poor oral bioavailability.
Intranasal nalbuphine delivery represents a safe and non-invasive alternative to parenteral routes of administration. Although nalbuphine has been used clinically for 40 years, the first results of clinical trials on nasal administration of the injectable solution were published in 2019. Certain progress has been made in the pharmaceutical development of nasal forms of nalbuphine, leading to the recent development of a nasal spray. Retrospective analysis of the issue and recently published data from clinical investigations of the newly developed nalbuphine nasal spray, are briefly reviewed.
Published Date: 2024-08-15; Received Date: 2024-06-24
