罗氟司特乳膏的作用与功效？

Roflumilast cream is a white to off-white topical cream. The active ingredient roflumilast is a phosphodiesterase 4 (PDE4) inhibitor with anti-allergic, anti-inflammatory, immunomodulatory and other effects. It is widely used to treat a variety of skin diseases, such as psoriasis, atopic dermatitis, etc.

Roflumilast cream benefits

Roflumilast can inhibit the activity of PDE4, thereby reducing the degradation of intracellular cAMP and increasing the level of intracellular cAMP. cAMP is an important intracellular signaling molecule that can participate in the regulation of a variety of cell functions, including anti-inflammation, anti-proliferation, immune regulation, etc.

It exerts therapeutic effects through multiple mechanisms. It can inhibit the release of various cytokines and inflammatory mediators in the inflammatory response, reduce inflammatory symptoms, and the specific mechanism of its therapeutic effect on psoriasis is not yet clear. It may be related to inhibiting the activity of phosphodiesterase 4 (PDE4), affecting the metabolism of intracellular cyclic adenosine monophosphate (cAMP), and ultimately exerting anti-inflammatory and anti-proliferative effects.

Roflumilast cream

A total of 881 subjects with mild to severe plaque psoriasis and BSA involvement of 2%-20% were enrolled in two multicenter, randomized, double-blind, vehicle-controlled trials. 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 (20%) subjects had a baseline intertrigo IGA (I-IGA) score of 2 or higher (mild), and 678 (77%) subjects had a baseline worst itching numeric rating scale (WI-NRS) score of 4 or higher.

Subjects were randomized in a 2:1 ratio to receive roflumilast cream or vehicle once daily for 8 weeks. The primary endpoint was the proportion of subjects who achieved IGA treatment success at week 8, defined as a score of "clear" (0) or "almost clear" (1) and a 2-grade improvement from baseline.

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 cream group than in the vehicle group.

In Study 1, IGA success at week 8 was 41.5% in the roflumilast cream group and 5.8% in the vehicle group, and in Study 2, IGA success at week 8 was 36.7% in the roflumilast cream group and 7.1% in the vehicle group.

Medication for special populations

1. Pregnant women: There are no randomized clinical trials of oral or topical roflumilast for pregnant women. In animal reproduction studies, oral administration of roflumilast during the organogenesis period in pregnant rats and rabbits can induce stillbirth and reduced fetal viability in mice. The background risk of major birth defects and miscarriage in the indicated population is currently unknown. In the U.S. general population, the estimated background risks of major birth defects and miscarriage in clinically confirmed pregnancies are 2%-4% and 15%-20%, respectively.

2. Lactating women: Roflumilast or its metabolites can be secreted into the milk of lactating rats. When the drug is present in animal milk, it is likely to be present in human milk. The development and health benefits of breastfeeding should be considered.

To minimize potential exposure of breastfed infants through breast milk, use roflumilast cream to the smallest skin area and for the shortest duration possible during breastfeeding. Nursing women are advised not to apply roflumilast cream directly to the nipple and areola to avoid direct exposure to the infant.

3. Pediatric patients: The safety and effectiveness of roflumilast cream for the treatment of plaque psoriasis has been established in pediatric patients 12 years of age and older. The safety and effectiveness of roflumilast cream has not yet been established in pediatric patients under 12 years of age.

4. Patients with liver damage: Roflumilast cream is contraindicated in patients with moderate to severe liver damage (Child-Pugh B or C).

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