盐酸纳呋拉啡(Remitch)改善瘙痒的疗效如何？

Nalfuraphine hydrochloride (Remitch) has a good effect on improving itching, and can significantly reduce the severity and frequency of itching attacks.

Nalfurapine hydrochloride

It is a kappa opioid receptor agonist that was approved in January 2009 and launched in Japan in March 2009. It is used to improve itching in hemodialysis patients. In addition to its antipruritic effects, nalfurapine hydrochloride has been shown to improve pain, neuropathic pain, drug dependence, schizophrenia, and movement disorders in nonclinical studies.

Mechanism of action

Research shows that itching may be caused by an imbalance in the activity of the μ- and κ-opioid receptor systems in the skin or central nervous system. Stimulation of kappa-opioid receptors by kappa-opioid receptor agonists inhibits itch in animals and humans. It is currently believed that the antipruritic effect of nalfuraphine hydrochloride is related to their binding to κ-opioid receptors on keratinocytes and skin and/or central pruritus nerves.

The efficacy of nalfuraphine hydrochloride (Remitch) in improving itching

A clinical study showed that within the first 12 weeks, 82.5% of patients were effective in taking nalfuraphine hydrochloride (Remitch). Within 1 year after starting treatment, 84.95% of patients were effective, and nalfuraphine hydrochloride (Remitch) had a significant anti-itching effect.

Thirty-seven peritoneal dialysis patients with pruritus who were resistant to existing treatments were used as subjects. Using the pruritus index VAS, the effectiveness of repeated oral administration of 2.5 μg nalfurapine hydrochloride for 2 weeks and then repeated oral administration of 5 μg for 2 weeks was studied through an unblinded and uncontrolled trial.

The results showed that the average VAS change before and after administration in the second week of 2.5 μg administration was 24.93 mm, and the lower limit of the 90% confidence interval was the preset VAS change threshold.

Special groups

1. Pregnant women: In animal experiments (rats), it has been reported that nalfurapine hydrochloride causes placental passage, a reduction in the number of viable fetuses, a reduction in birth rate, and a reduction in birth weight. Therefore, it is best not to give the drug to pregnant women or women who may be pregnant.

2. Breastfeeding women: Nafurafine hydrochloride may be transferred into breast milk. Considering the therapeutic benefits and the nutritional benefits of breast milk, consider continuing or stopping breastfeeding.

3. Children: No clinical trials have been conducted on children, so children should use it with caution or not.

Drug interactions

1. CYP3A4 inhibitors: such as itraconazole, cyclosporine, nifedipine, cimetidine, grapefruit juice, etc. Since the plasma concentration of nalfuraphine hydrochloride may increase, the patient's condition must be fully observed when merging, changing the dosage, or discontinuing the drug.

2. Opioids: The combined use of the two can lead to the enhancement or weakening of the efficacy of nalfuraphine hydrochloride.

3. Other drugs: such as sleeping pills, anti-anxiety drugs, antidepressants, antipsychotics, and anti-epileptic drugs. When combined with nalfuraphine hydrochloride, symptoms such as insomnia, hallucinations, drowsiness, floating dizziness, tremor, and delirium may occur. Pay attention to adverse reactions during medication.

Summary

Nalfuraphine hydrochloride has a certain effect on improving itching symptoms, but the specific clinical efficacy varies with individual differences and needs to be evaluated based on individual circumstances and disease severity.

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