纳地美定的药效如何？

(Naldemedine) has good efficacy, has significant and sustained improvement in defecation frequency and constipation-related symptoms, and is generally well tolerated.

Nadimedine drug introduction

Opioid-induced constipation (OIC) is the most common side effect of opioid therapy and can lead to decreased quality of life. Naldemedine is a peripherally acting μ-opioid receptor antagonist developed by Shionogi Co., Ltd. and has been approved in the United States and Japan for the treatment of opioid-induced constipation. The drug inhibits peripheral mu-opioid receptors, such as those found in the gastrointestinal tract, and has little or no effect on central opiate activity.

Natimide

Opioids are widely used for pain management of moderate to severe pain. However, opioids are associated with adverse events such as constipation and vomiting. In order to reduce these adverse effects, structure-activity relationship studies of morphine derivatives were conducted, and a promising lead compound with inhibitory effects on opioid receptors was obtained. With further improvements in the pharmacodynamic and pharmacokinetic characteristics of the lead compound, naldemedine was discovered. Naldimedine has anti-constipation and antiemetic effects on the adverse reactions caused by morphine, but does not affect the analgesic effect of morphine.

One endpoint included 5 randomized clinical trials (total 1751 participants), 3 trials looking at the effect of naldimedine in the treatment of OIC in non-cancer patients, and 2 trials looking at the effect in cancer patients. A random effects model was used for all comparisons, and subgroup analyzes were performed on the following subgroups: naldimedine 0.1 mg, 0.2 mg, 0.4 mg, patients with cancer, patients without cancer.

Final conclusion: Naldemedine increased the proportion of responders and the frequency of spontaneous defecation, and Naldemedine 0.2 mg daily improved the quality of life of patients. Patients taking naldimedine experienced mild to moderate symptoms during treatment and were well tolerated.

Medication for special populations

1. Pregnancy: Naldemedine can pass through the placenta. Due to the immaturity of the fetal blood-brain barrier, it may promote fetal opioid withdrawal. Therefore, when naldimedine is used in pregnant women, the fetus may undergo opioid withdrawal, and naldimedine should be used during pregnancy only if the potential benefits outweigh the potential risks.

2. Breastfeeding: Due to the possibility of serious adverse reactions, including discontinuation of opioids in breastfed infants, the importance of the drug to the mother should be considered when deciding to discontinue breastfeeding or discontinue the drug.

If drug is discontinued to minimize drug exposure to the breastfed infant, it is recommended that women resume breastfeeding 3 days after the last dose of naldimedine.

3. Liver damage: Avoid use in patients with severe liver damage.

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