Nalbuphine: some aspects of the research and applications

Abstract

Nalbuphine hydrochloride is a synthetic, non-scheduled opioid agonist/antagonist analgesic, widely used across different branches of medicine. Despite the fact that nalbuphine has been used in the clinical setting for more than 40 years, there is still a lot of controversy regarding its mechanism of action and side-effects, including the development of the addiction to the drug. Recent data demonstrated the increase of non-medical use of nalbuphine. Moreover, in some countries it was placed in list of psychotropic and addictive substances. The increasing popularity of nalbuphine led us to review and analyse the data regarding both clinical and non-clinical applications of the drug. Furthermore, we performed an extensive analysis regarding available experimental models and approaches used in the research of opioid substances. Despite a set of problems in clinical settings due to the opioid nature of nalbuphine, it belongs to an indispensable group of analgesics for pain control. StreszczenieChlorowodorek nalbufiny jest syntetycznym, opioidowym agonistycznym i antagonistycznym lekiem przeciwbólowym, szeroko wykorzystywanych w różnych gałęziach medycyny. Mimo że nalbufina jest stosowana w postępowaniu klinicznym od ponad 40 lat nadal istnieje wiele kontrowersji dotyczących mechanizmu jej działania i skutków ubocznych, w tym uzależnienia od narkotyków. Ostatnie dane dowodzą zwiększonego niemedycznego wykorzystania nalbufiny. W niektórych krajach nalbufina została umieszczona w wykazie substancji psychotropowych i uzależniających. Wzrastające zastosowanie tego leku skłania do przeglądu i analizy danych dotyczących klinicznych i nieklinicznych jego aplikacji. Ponadto przeprowadzono analizę dotyczącą dostępnych modeli eksperymentalnych i podejść stosowanych w badaniach substancji opioidowych. Pomimo licznych problemów w praktyce klinicznej ze względu na opioidowy charakter nalbufina należy do grupy analgetyków niezbędnych w kontroli bólu.

EPD1504: a novel μ-opioid receptor partial agonist attenuates obsessive–compulsive disorder (OCD)-like behaviors

“…Compared to other partial agonists (with comparable or lower intrinsic MOR efficacy), EPD1504 (like buprenorphine) is somewhat unique in that it exhibits limited off-target agonist activity; examples of other partial MOR agonists with off-target agonist activity include nalbuphine and butorphanol that are both potent MOR and kappa opioid receptor agonists, the latter has been shown to induce hallucinations and dysphoric effects ( 66 , 67 ). Other examples include the prodrug tramadol and tapentadol, which are both partial MOR agonists and potent amine modulators, importantly the metabolites of tramadol are high-efficacy MOR agonists ( 68 , 69 ).…”

Morphometric study of angioarchitectonic under the effect of opioid (experimental study)

“…Nalbuphine is an agonist of -opioid receptors and a partial antagonist of μ-opioid receptors, which can stimulate -receptors and antagonize the acute rewarding effects of morphine, has a short duration of action and rapid clearance compared with other opioids and is less likely to cause side effects [15]. It is widely used either as an analgesic or as an adjuvant with morphine [4,12,19]. For this reason, the number of requests for opioids in Pubmed has traditionally remained the same.…”

Construction of novel potentiometric sensors modified with biogenically synthesized metal oxide nanoparticles for sensitive detection of the opioid agonist-antagonist nalbuphine hydrochloride in its injection

“…Nalbuphine, which is derived chemically from oxymorphone, is a powerful analgesic with narcotic antagonist effect. Due to the scarcity of methamphetamine, the misuse of nalbuphine as a substitute for methamphetamine has increased [ 65 ]. Accordingly, analytical approaches for NBP detection may be of interest, particularly in settings when traditional techniques are ineffective, as is the case in many on-site tests and fast screening applications.…”