罗氟司特乳膏(roflumilast)适应症,作用功效,用法用量,副作用,疗效？

Author: Medicalhalo

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

Indications for roflumilast cream

It is a selective PDE-4 inhibitor indicated for the treatment of plaque psoriasis, including intertriginous psoriasis in skin fold areas, in patients 12 years of age and older.

Efficacy

Roflumilast and its active metabolite (roflumilast N-oxide) are inhibitors of PDE4 and have anti-allergic, anti-inflammatory and immunomodulatory effects.

1. Anti-inflammatory effect: Roflumilast cream can inhibit the release of inflammatory mediators and the activation of immune cells, thereby reducing the inflammatory response.

2. Immunomodulatory effect: Roflumilast cream can regulate the immune system and enhance the body's immunity by regulating the function of immune cells and inhibiting the activation of immune cells.

3. Anti-allergic effect: Preliminary research found that roflumilast cream can significantly reduce the activity of PDE4 enzyme, reduce the degradation of cAMP, and increase the intracellular cAMP content.

Usage and Dosage

Roflumilast cream (roflumilast) needs to be applied to the affected area, and massage until absorbed. Pay attention to washing hands after application. Roflumilast cream is for topical use only and is not for intravaginal, intraocular or oral use.

Dosage forms and specifications

0.3% roflumilast cream: Each gram of white to off-white cream in a 60g tube contains 3 mg of roflumilast.

Contraindications

Roflumilast cream (roflumilast) should be contraindicated in patients with moderate to severe liver damage.

Side effects

The most common symptoms of roflumilast cream are pain at the application site, headache, insomnia, diarrhea, upper respiratory tract infection and urinary tract infection.

Methods for dealing with side effects

1. Pain at the medication site: If the pain is bearable, you can try to reduce the dosage of roflumilast cream to reduce the pain. If the pain is severe, it is recommended to discontinue use of roflumilast cream.

2. Headache: Patients with headache after taking medication should pay attention to rest and maintain adequate sleep. They can relieve discomfort through local massage and moxibustion. If the headache symptoms are severe, acupuncture or analgesic drugs can be used under the guidance of a doctor.

3. Insomnia: Patients with insomnia should avoid drinking alcohol, coffee and other irritating drinks before going to bed to avoid disturbing sleep. Create a relaxed and comfortable sleeping environment to help relieve insomnia. If necessary, sedative and sleeping drugs can be used under the guidance of a doctor to relieve symptoms.

4. Diarrhea: Patients with diarrhea should pay attention to a light diet, avoid eating foods that aggravate diarrhea, such as cold drinks, ice cream, etc., pay attention to keeping the abdomen warm, and use montmorillonite powder and other drugs to relieve diarrhea symptoms.

5. Upper respiratory tract infection: Patients can follow the doctor's advice and take oral antibiotics, such as cephalosporins, amoxicillin, etc., to help patients control the infection. Symptoms such as fever and cough in early summer are followed by symptomatic treatment.

6. Urinary tract infection: It is recommended that patients drink more water and urinate more during treatment, pay attention to private parts hygiene, and change and wash underwear frequently. Antibiotic treatment can be used under the guidance of a doctor, such as cefuroxime, cefoperazone, amoxicillin, etc.

Clinical efficacy analysis

Two multi-center, randomized, double-blind, vehicle-controlled trials enrolled a total of 881 subjects with mild to severe plaque psoriasis and BSA involvement of 2%-20%. The age range of the study population was 6-88 years, with 4 subjects younger than 12 years old at baseline. At baseline, 16% of subjects had an Investigator's Global Assessment (IGA) score of 2 (mild), 76% had an IGA score of 3 (moderate), and 8% had an IGA score of 4 (severe). 179 subjects (20%) had a baseline scratch IGA score of 2 or above (mild), and 678 subjects had a baseline Most Severe Itch Quantification Scale score of 4 or above.

Experimental subjects used roflumilast cream once a day in a 2:2 ratio for a total of 8 weeks. The primary endpoint was the percentage of patients successfully treated with IGA at 8 weeks (Table 2). The success criteria are "clear" (0) and "almost clear" (1), and an improvement of 2 levels from the baseline.

Secondary endpoints include the proportion of subjects achieving I-IGA success at Week 8 and consecutive WI-NRS success at Weeks 8, 4, and 2. WI-NRS success was defined as a reduction of at least 4 points from baseline in subjects with a baseline WI-NRS score of at least 4.

Results: Among subjects with a baseline I-IGA score of at least 2 (mild), the percentage of subjects who achieved I-IGA success at week 8 was higher in the roflumilast group than in the vehicle group (71.5% vs 13.8%, 67.5% vs 17.4%).

Medication Precautions

Roflumilast cream (roflumilast) should not be used during delivery. There are no human studies investigating the effects of roflumilast cream (roflumilast) on preterm or term delivery. However, animal studies have shown that oral administration of roflumilast disrupts the birthing process in mice.

Drug interactions

Roflumilast cream (roflumilast) should be avoided as much as possible in combination with systemic CYP3A4 inhibitors or dual inhibitors that can inhibit both CYP3A4 and CYP1A2, such as enoxacin, cimetidine, erythromycin, ketoconazole, fluvoxamine, etc. Coadministration may increase the systemic exposure of roflumilast and may result in increased adverse reactions.

Therefore, it is recommended that patients should consult a doctor in advance and use it correctly under the guidance of a doctor if they need to combine it with other drugs while using roflumilast cream.

China listing information

As of December 4, 2203, roflumilast cream (roflumilast) has not yet been launched in mainland China. It has been launched in the United States, Taiwan, Canada, Hong Kong, France, Germany, the United Kingdom, etc.

Drug price

Manufacturer Arcutis Biotherapeutics, Inc., trademark: ZORYVE, common name: roflumilast, Chinese translation: roflumilast cream, the reference price is about $12,420 per box.