纳呋拉菲口崩片的作用机制、副作用及治疗效果？

Nafurafil orally disintegrating tablets are selective kappa-opioid receptor agonists and have anti-itching effects. Patients may experience side effects such as jaundice and liver dysfunction during use. It is recommended that patients take medication correctly under the guidance of a doctor to avoid adverse reactions and worsening discomfort.

Mechanism of action

Nafurafil orally disintegrating tablets can act on three types of opioid receptors, including κ, μ, and δ. In in vitro tests, various receptors, transporters, and ions other than the opioid receptor containing histamine receptors did not bind to the channel, and did not inhibit the degranulation reaction of mast cells. In addition, the inhibitory effect of intradermal administration of picostat on scratching behavior in mice was completely antagonized by intracerebroventricular administration of the opioid kappa receptor antagonist norepinephrine (nor-BNI)25.

Intradermal administration of histamine, which is effective in existing antipruritic drugs such as antihistamines, can inhibit the scratching behavior of mice and the scratching behavior of mice induced by intradermal administration of substance p, which is ineffective with antihistamine drugs. In addition, the scratching behavior of mice induced by administration of morphine in a large tank of a central itch model in which antihistamine drugs are ineffective was also inhibited, thereby exerting an anti-itching effect.

Nafurafil orally disintegrating tablets

A study evaluated the safety of nalfurafil and included 3762 patients. Among them, 402 patients experienced adverse reactions. The most common adverse reactions were insomnia, constipation, drowsiness, dizziness, nausea and discomfort. None of the patients developed nalfuranfine dependence. Serious side effects include liver dysfunction and jaundice (both frequency unknown). Nafurafil may also cause the following other side effects:

1. Psychological nervous system: floating dizziness, headache, irritability, hallucinations, dysarthria, pressure leg syndrome, concussion, numbness, delirium, and irritability.

2. Digestive system: constipation, thirst, nausea, vomiting, loss of appetite, abdominal discomfort, gastritis, stomatitis.

3. Skin: worsening of itching, eczema, rash, urticaria, erythema, papules, and pigmentation.

4. Liver system: Increase in total bile acids, AST, ALT, Al-P, γ-GTP, bilirubin, and LDH.

5. Renal system: Frequent urination at night.

6. Endocrine system: decreased testosterone, decreased thyroid-stimulating hormone, increased thyroid-stimulating hormone, increased antidiuretic hormone, increased prolactin, etc.

Therapeutic effect

Intractable skin itching can significantly reduce the quality of life of maintenance hemodialysis patients and is associated with poor prognosis. Although multiple causes of intractable pruritus have been identified in these patients, no existing treatments have proven to be sufficiently effective. A post-marketing surveillance to follow up and evaluate the safety and efficacy of the selective kappa-opioid receptor agonist nalfurafil for the treatment of refractory cutaneous pruritus in hemodialysis patients.

Hemodialysis patients with refractory cutaneous pruritus receiving oral nalfurafil hydrochloride were enrolled and safety data were collected and analyzed within 1 year after the initiation of nalfurafil treatment, as well as efficacy data (using physician's global assessment of improvement in pruritus, visual analogue scale, and Shiratori severity score) for the first 12 weeks of treatment and subsequently up to 1 year after the initial dose to assess nalfurafil.

Results: The effective rate of nalfurafil was 82.50% in the first 12 weeks of treatment, and the effective rate in 1 year after treatment was 84.95%. There was a statistically significant decrease in visual analog scale and Shiratori severity scores.

Conclusion: Oral nalfurafil hydrochloride at 2.5-5.0 μg/d is effective in treating refractory skin itching in hemodialysis patients.

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