Opioid-induced gastrointestinal side effects, the role of naldemedine in their therapy

Abstract

Although opioid analgesics are highly effective in the treatment of pain, one of the main disadvantages of their use is their negative effect on the functioning of the gastrointestinal tract. Opioid-induced side effects include a variety of symptoms known as opioid gastrointestinal disorders (OIBD). One of the effective drugs used in OIBD is naldemedine, which, due to its pharmacokinetic and pharmacodynamic profile and safety profile, is currently the optimal therapeutic option.

The use of opioid receptor agonists and antagonists in the treatment of patients with advanced chronic kidney disease and undergoing renal replacement therapy

“…Opioid-induced constipation, the most common side effect of opioids, affects patients with chronic non-cancer pain (60%) and cancer patients (85%) [9,21,22]. Opioid analgesics inhibit propulsive peristalsis and secretory functions of the gastrointestinal tract by acting on μ-, κand δ-opioid receptors in the myenteric and submucosal plexuses of the small and large intestine, modulating opioid receptor function at the level of the spinal cord [23,24].…”

“…Naldemedine is a naltrexone derivative, an antagonist of μ-, κ-, δ-opioid receptors [22,23,27,37]. Its penetration into the CNS is negligible [26,27].…”