纳呋拉啡(Remitch)适应症,功效作用,用法用量,副作用,疗效？

Author: Medicalhalo

Release time: 2025-10-19 11:44:20

Nalfuraphine (Remitch) Indications

It is suitable for improving pruritus in dialysis patients and patients with chronic liver disease (limited to cases where the existing treatment effect is insufficient).

China listing information

Nafuraphine hydrochloride orally disintegrating tablets will be launched in China on September 13, 2023, but are not included in medical insurance. In addition, nalfuraphine (Remitch) is also launched in Japan and South Korea.

Efficacy

Nafurapine (Remitch) is an opioid receptor agonist that selectively accepts opioid κ based on the results of in vitro receptor binding tests and receptor motility tests using human opioid receptor-expressing cells. In clinical application, nalfuraphine (Remitch) can significantly improve patients' sleep quality and refractory skin itching, and it still has a significant effect on hemodialysis pruritus that is resistant to existing treatments.

Usage and Dosage

Patients taking nalfuraphine (Remitch) should take it orally once a day, usually after dinner or before going to bed, 2.5 μg each time, calculated as nalfuraphine hydrochloride. In addition, the dose can be increased according to symptoms, but the maximum dose once a day is 5 μg.

1. Improvement of pruritus in hemodialysis patients

A sufficient interval should be left between the administration of this agent and the start of hemodialysis. Since this agent is removed by hemodialysis, the blood concentration of this agent may decrease if the time from taking nalfurorphine (Remitch) to hemodialysis is short.

2. Improvement of pruritus in peritoneal dialysis patients

There should be sufficient interval between administration of this agent and replacement of dialysate. If the time between taking Remitch and changing the dialysate is short, the plasma concentration of Remitch may decrease.

3. Improvement of pruritus in patients with chronic liver disease

The starting dose of nalfurorapine (Remitch) is 2.5 μg, once a day. If the effect is not good, the dose can be increased to once a day, 5 μg each time.

Side Effects

Nafurapine (Remitch) can cause skin, digestive system, nervous system, etc. Side effects include liver dysfunction, jaundice, insomnia, constipation, dizziness, frequent urination, elevated prolactin, headache, etc.

Methods for dealing with side effects

1. Nausea and vomiting: Patients are advised to adjust their diet, avoid greasy, spicy, and irritating foods, and choose foods that are easy to digest and nutritious. This can help reduce the burden on the gastrointestinal tract and relieve symptoms such as vomiting and diarrhea.

2. Dizziness and headache: Under the guidance of a doctor, patients can use some anti-dizziness drugs, analgesics, etc., such as ibuprofen, promethazine, etc., to relieve dizziness and headache caused by nalfurapine.

3. Constipation: Proper exercise can promote intestinal peristalsis and help relieve constipation symptoms. Regular defecation can help relieve constipation symptoms by avoiding bad habits such as holding in stool. Patients with constipation can also use some laxatives or probiotics, such as lactulose, bifidobacteria, etc., to relieve constipation symptoms.

4. Skin rash: If patients with rash are caused by drug allergy, they should stop taking the medication immediately and use antihistamines such as diphenhydramine, cetirizine, and loratadine as directed by the doctor to relieve symptoms.

5. Liver dysfunction: If the side effects are severe and liver dysfunction occurs, the patient can adjust the dosage of nalfuraphine (Remitch) under the guidance of a doctor, or suspend the medication for a period of time, and then continue treatment after the symptoms are relieved.

Clinical efficacy analysis

Uremic pruritus has a significant negative impact on the quality of life of hemodialysis (HD) patients and, more importantly, on the risk of death. Recently, the opioid kappa-selective agonist nalfuraphine (Remitch) was officially approved for the treatment of refractory pruritus in HD patients on the basis of a well-documented clinical trial in Japan.

Based on clinical observations, it has been shown that the upper nervous system plays a role in its pathogenesis. Based on previous experimental results using opioid-injected mice, dynorphin suppresses itch by binding to kappa-opioid receptors, suggesting kappa-opioid receptor agonists as potential treatments for itch in HD patients.

In Japan, a large-scale placebo-controlled study was conducted to examine the efficacy and safety of oral nalfuraphine (Remitch) in the treatment of refractory pruritus in 337 HD patients. 2.5 or 5 μg of nalfurapine (Remitch) or placebo was administered orally twice daily for 2 weeks, and clinical response was analyzed. The results showed that compared with baseline, the visual analogue score of pruritus decreased by an average of 22 mm in the 5 μg nalfuraphine (Remitch) group (n=114) and the 2.5 μg nalfuraphine (Remitch) group (n=112).

These reductions were statistically significant compared with the mean visual analog scale reduction of 13 mm in the placebo group (n=111), indicating that nalfuraphine (Remitch) is an effective and safe drug for the treatment of uremic pruritus in HD patients.

In addition, another open-label trial (n=145) examining the long-term effects of 5 μg oral nalfuraphine (Remitch) showed that the antipruritic effect of nalfuraphine (Remitch) was maintained for 52 weeks.

Based on recent data showing kappa-opioid receptor expression in the epidermis of atopic dermatitis and psoriasis, nalfurapine (Remitch) may also potentially be used in these two skin diseases.

Notes

1. Strictly follow the doctor's instructions when taking medication: During treatment, patients should take medication on time and in accordance with the dose. Do not overdose on medication to avoid causing hallucinations, restlessness, insomnia, severe drowsiness, etc.

2. Liver damage: When using this product in patients with severe (Child-Pugh classification C) liver damage, risk preference should be considered, and the patient's status should be fully observed during medication.

3. Avoid driving and operating: Since nalfurapine (Remitch) can cause adverse reactions in the nervous system, patients with symptoms such as drowsiness and dizziness should be careful not to drive cars and other dangerous machine operations.

4. Increased prolactin: Nafuraphine (Remitch) may cause endocrine dysfunction such as increased prolactin, and it is recommended that patients undergo regular examinations.

5. Use by pregnant women: It is best not to give medicine to pregnant women or women who may be pregnant. In animal experiments (rats), there have been reports of placental passage, reduced birth rates, reduced number of viable fetuses, and reduced birth weight.

6. Drug interactions: Nafurafine (Remitch) should be avoided in combination with sleeping pills, antidepressants, azole antifungals, grape juice, anti-anxiety drugs, opioids, anti-epileptic drugs, antipsychotic drugs, etc., so as not to affect the therapeutic effect of the drug.

Price

1. Nalfurafine Hydrochloride, an anti-itch drug for hemodialysis patients, the reference price of Nalfurafine Hydrochloride 140 capsules is about $4250 per box.

2. The reference price of 14 capsules of nalfuraphine hydrochloride, an anti-itch drug for hemodialysis patients, is about $470 per box.

Due to the influence of factors such as foreign exchange rates on drug prices, drug prices are not static. Patients who need to purchase drugs can consult the medical companion travel service for specific prices and drug purchase procedures.