纳地美定治疗阿片类药物引起便秘的效果？

Natimide

Is an opioid antagonist with binding affinity for μ-, 8-, and K-opioid receptors. (Naldimedine acts as a peripherally acting opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby reducing the constitutive effects of opioids.

Naldimedine is a derivative of naltrexone whose side chains increase the molecular weight and polar surface area, thereby reducing its ability to cross the blood-brain barrier and thereby limiting the potential to interfere with centrally mediated opioid analgesia.

Naldimedine is indicated for the treatment of chronic non-cancer pain in adult patients with opioid-induced constipation, including chronic pain associated with prior cancer or its treatment.

Nadimedine treats opioid-induced constipation

For patients with opioid-induced constipation suffering from cancer pain or chronic non-cancer pain, naldimedine is an effective and generally well-tolerated treatment option with the convenience of once-daily oral administration.

Opioid-induced bowel dysfunction (OIBD) is a common complication in long-term opioid users and abusers. OIBD affects up to 60% of patients with chronic non-cancer pain and more than 80% of patients with cancer pain, and is one of the most common symptoms associated with opioid maintenance.

Overall, the available data suggest that naldimedine is an effective treatment option for OIBD because it is a well-tolerated medication that relieves constipation without affecting analgesia or causing opioid withdrawal symptoms.

Nadimetin was approved by the U.S. FDA in 2017 for the treatment of opioid-induced constipation in adults with chronic non-cancer pain-related syndromes.

In the Phase III trial, patients receiving naldimedine were more likely to achieve the primary endpoint of ≥3 spontaneous bowel movements/week and to increase ≥1 spontaneous bowel movement/week from baseline in at least 9/12 weeks compared with placebo (p < 0.0001). The most common adverse events were abdominal pain (8%) and diarrhea (7%), and severe ones were gastrointestinal perforation and opiate withdrawal reactions.

Based on available data, naldimedine appears to be an effective and safe first-line therapy for the treatment of opioid-induced constipation in adults with chronic noncancer pain.

The recommended dose of naldimedine is 0.2 mg, taken once daily, with or without food. It is contraindicated in patients with suspected or confirmed gastrointestinal obstruction.

References:

Liu JJ, Quinton SE, Brenner DM. Naldemedine for the treatment of opioid-induced constipation in adults with chronic noncancer pain. Pain Manag. 2020 Sep;10(5):301-306. doi: 10.2217/pmt-2020-0019. Epub 2020 Jun 19. PMID: 32552565.

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