tacrolimus

Common name: tacrolimus

Trade name: Protopic

All names: Tacrolimus ointment, Protopic, tacrolimus, Protopic

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Indications:

This product is suitable for use as short-term or intermittent long-term treatment in patients with moderate to severe atopic dermatitis who are not suitable for using traditional therapies due to potential risks, or who have insufficient response to traditional therapies, or who are unable to tolerate traditional therapies. Both 0.03% and 0.1% concentrations of this product can be used in adults, but only the 0.03% concentration of this product can be used in children 2 years and older.

Usage and dosage:

Adults

0.03% and 0.1% tacrolimus ointment

Apply a thin layer of this product to the affected skin, rub it evenly and cover it completely, twice a day.

Children

0.03% Tacrolimus Ointment

Apply a thin layer of this product to the affected skin, rub it evenly and cover it completely, twice a day.

This product should be used in the smallest amount that can control the symptoms and signs of atopic dermatitis. Use should be discontinued when the symptoms and signs of atopic dermatitis disappear. This product should not be used externally in a sealed dressing.

Specification:

0.1% (10g: 10mg)

0.03% (10g: 3mg)

Adverse reactions:

Generally speaking, topical use of this product may cause local symptoms, such as skin burning (burning, stinging, pain) or itching.

Exceptionally, patients with infectious atopic dermatitis should not use this drug. Because people with infectious atopic dermatitis are susceptible to superficial skin infections, including eczema herpeticum (Kaposi's varicella-like eruption). Treatment with this product may increase the risk of herpes zoster virus infection (chickenpox or herpes zoster), herpes simplex virus infection, or eczema herpeticum, so it is not recommended for the treatment of infectious atopic dermatitis.

A very few people have developed cancer (such as skin cancer or lymphoma) after using Protopic Ointment, but there is no evidence that it is related to Protopic Ointment.

Contraindications:

This product is contraindicated in patients with a history of allergy to tacrolimus or any other ingredient in the preparation.

Notes:

General precautions

Protopic ointment should be avoided for use in skin diseases that may worsen and malignant skin diseases. Some malignant skin diseases, such as cutaneous T-cell lymphoma, may resemble atopic dermatitis.

Protopic ointment is not recommended for the treatment of patients with Netherton syndrome or other dermatoses as it may increase the systemic absorption of tacrolimus. The safety of Protopic Ointment in the treatment of patients with diffuse erythroderma has not been established.

Topical Protopic ointment may cause local symptoms, such as skin burning (burning, stinging, pain) or cancer itching. Local symptoms are most common during the first few days of using Protopic Ointment and usually disappear as the affected skin improves. When applying 0.1% Protopic ointment for treatment. 90% of skin burning sensations last between 2 minutes and 3 hours (median 15 minutes). 90% of cancer itch symptoms lasted between 3 minutes and 10 hours (median 20 minutes). (See Adverse Reactions).

Bacterial and Viral Skin Infections

The safety and effectiveness of Protopic Ointment for infectious atopic dermatitis have not been clinically evaluated. Before starting treatment with Protopic Ointment, the infection in the treatment area should be eliminated first.

Patients with atopic dermatitis are susceptible to superficial skin infections, including herpetic eczema (Kaposi varicella-like eruption). Treatment with Protopic Ointment may increase the risk of herpes zoster virus infection (chickenpox or shingles), herpes simplex virus infection, or eczema herpeticum.

Patients with lymphadenopathy

In clinical studies, 112 out of 13,494 patients reported lymphadenopathy (0.8%), which was usually related to infection (especially skin infection). It was relieved after corresponding antibiotic treatment. Most of these 112 patients had a clear cause or eventually resolved. Organ transplant patients receiving immunosuppressive therapy (eg, systemic tacrolimus) are at increased risk for developing lymphoma; therefore, patients receiving Protopic ointment who develop lymphadenopathy should be investigated for the cause of their lymphadenopathy. If no clear cause of lymphadenopathy is found, or if the patient also suffers from acute infectious mononucleosis, discontinuation of Protopic ointment should be considered. Patients who develop lymphadenopathy should be further monitored to ensure resolution of lymphadenopathy.

Sunlight Exposure

During treatment, patients should minimize or avoid exposure to natural or artificial sunlight, even when there is no sun exposure on the skin. It is not known whether Protopic ointment interferes with the skin's response to UV damage.

Immunocompromised patients

The efficacy and safety of Protopic Ointment in immunocompromised patients have not been studied.

Renal Insufficiency

Rare cases of acute renal failure have been reported in patients treated with Protopic Ointment post-marketing. Systemic absorption is more likely to occur in patients with compromised epidermal barriers, especially those who apply Protopic ointment to large areas of the body. Patients prone to renal insufficiency should be alerted.

Storage:

Store at room temperature 25℃; the allowed temperature range is 15-30℃.

Mechanism of action:

The mechanism of action of tacrolimus in atopic dermatitis is not fully understood. Although the following has been observed, the clinical significance of these observations in atopic dermatitis is unclear.

By binding to a specific cytoplasmic immunophilin (FKBP12), tacrolimus inhibits calcium-dependent signal transduction pathways in T cells, thereby preventing the transcription and synthesis of IL-2, IL-3, IL-4, IL-5 and other cytokines, such as GM-CSF, TNF-α and IFN-γ.

In vitro, tacrolimus reduced the stimulatory activity of T cells in Langerhans cells isolated from normal human skin. Tacrolimus has also been shown to inhibit the release of inflammatory mediators from cutaneous mast cells, basophils, and eosinophils.

In animals, tacrolimus ointment suppresses inflammatory responses in experimental and spontaneous dermatitis models similar to human atopic dermatitis. Tacrolimus ointment does not reduce skin thickness and does not cause skin atrophy in animals.

In patients with atopic dermatitis, improvement in skin lesions during tacrolimus ointment treatment was associated with a reduction in Fc receptor expression on Langerhans cells and a reduction in their hyperstimulatory activity on T cells. Tacrolimus ointment does not affect the body's collagen synthesis.

Safety and efficacy:

Purpose: To evaluate the clinical effectiveness of 0.1% and 0.03% tacrolimus ointment in the treatment of atopic dermatitis. Methods: 171 clinical adult patients with atopic dermatitis were selected and randomly divided into 3 groups in a ratio of 1:1:1. They were treated with 0.1%, 0.03% tacrolimus ointment and 0.05% desonide cream (control group) respectively. The medication rate was the same, and the course of treatment was 3 weeks. Results: The overall treatment rate, clinical evaluation and patient evaluation of 0.1% tacrolimus ointment were higher than those of the control group. Results: Statistically significant difference, no serious side effects. Conclusion: Using 0.1% tacrolimus ointment to treat atopic dermatitis can achieve better therapeutic effects.