Tacrolimus ointment

The mechanism of action of tacrolimus in the treatment of atopic dermatitis is still unclear. Although the mechanism of action of tacrolimus is somewhat understood, the clinical relevance of these findings to atopic dermatitis is unclear. Tacrolimus has been shown to inhibit T lymphocyte activation by first binding to the intracellular protein FKBP-12 to form a complex composed of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin, thereby inhibiting the phosphatase activity of calcineurin and preventing the dephosphorylation and translocation of nuclear factor of activated T cells (NF-AT), a nuclear component that initiates gene transcription to form lymphokines (e.g., IL-2, interferon-γ). Tacrolimus also inhibits the transcription of genes encoding IL-3, IL-4, IL-5, GM-CSF, and TNF-α, all of which are involved in the early stages of T cell activation. In addition, tacrolimus can inhibit the release of synthesized mediators in skin mast cells and basophils and downregulate the expression of FCΣRI on the surface of Langerhans cells.

The main ingredient of this product and its chemical name are: tacrolimus.

This product is a white to light yellow ointment.

This product is suitable for patients with moderate to severe atopic dermatitis who are not suitable for traditional treatments due to potential risks, or who have responded inadequately to traditional treatments, or who cannot tolerate traditional treatments, as a short-term or intermittent long-term treatment. Both 0.03% and 0.1% concentrations of this product can be used in adults, but only 0.03% concentration of this product can be used in children aged 2 years and above.

Adults 0.1% Tacrolimus Ointment: Apply a thin layer of this product to the affected skin, rub it in gently and cover it completely, twice a day. This product should be used in the minimum amount that can control the symptoms and signs of atopic dermatitis, and should be discontinued when the symptoms and signs of atopic dermatitis disappear. This product should not be used externally with an occlusive dressing.

Phototoxicity and photosensitivity were not reported in clinical studies with 12 and 216 healthy volunteers, respectively. In a contact sensitization study with 198 healthy volunteers, one case showed signs of contact sensitization. In three randomized vehicle-controlled studies and two long-term safety studies, 655 and 571 patients were treated with this drug, respectively. The following table lists the adjusted adverse event rates for vehicle, 0.03% and 0.1% of this drug in three identically designed 12-week studies, as well as the unadjusted adverse event rates in two one-year safety studies, regardless of whether these adverse events were related to the study drug. Possibly related to the use of this drug. A total of 4 cases of varicella occurred in the 12-week study in children; 1 case of herpes zoster on the labialis in the 12-week study in adults; 7 cases of varicella and 1 case of herpes zoster occurred in the open-label study in children; 2 cases of herpes zoster occurred in the open-label study in adults. Usually warts. Other adverse events with an incidence greater than or equal to 1% in various clinical trials include alopecia, increased ALT or AST, allergic reactions, angina pectoris, angioedema, anorexia, anxiety, arrhythmia, arthralgia, arthritis, hyperbilirubinemia, breast pain, cellulitis, cerebrovascular accident, cheilitis, chills, constipation, increased creatinine, dehydration, depression, dizziness, dyspnea, ear pain, skin ecchymosis, edema, epistaxis, worsening of untreated sites, eye discomfort, eye pain, furunculosis, gastritis, hernia, hyperglycemia, hypertension, hypoglycemia, hypoxia, laryngitis, leukocytosis, leukopenia, abnormal liver function tests, lung disease, general discomfort, migraine, neck pain, neuritis, palpitations, paresthesia, peripheral vascular abnormalities, photosensitivity reactions, complications of the treatment process, skin depigmentation, sweating, abnormal taste, dental disease, unintended pregnancy, vaginal candidiasis, vasodilation and dizziness. (See instructions for details)

This product is contraindicated in patients with a history of hypersensitivity to tacrolimus or any other component of the formulation.

Precautions for children: This product at a concentration of 0.03% can be used in children aged 2 years and above. Two Phase III pediatric clinical studies have been conducted with a total of 606 patients aged 2-15 years: one is a 12-week randomized vehicle-controlled study, and the other is a one-year open-label long-term safety study, in which 330 patients are aged between 2 and 6 years. The most common adverse reactions of this product in children are burning sensation and itching of the skin (see adverse reactions). In addition, compared with the vehicle, patients treated with 0.03% concentration of this product have a higher frequency of less common adverse events (incidence less than 5%) such as herpes zoster (mainly chickenpox) and vesicular herpes. In a one-year long-term safety study, a total of 255 children were treated with this product, and the incidence of adverse events (including infection) did not increase with the extension of medication time or the increase of medication dosage. Among the 491 children treated with this product, 3 cases (accounting for 0.6%) developed herpetic eczema. Since the safety and efficacy of this product in children under 2 years old have not been established, it is not recommended for use in this age group. Pregnancy and lactation precautions: Teratogenic effect: Pregnancy medication classification C1. There has been no adequate and appropriately controlled study on the topical application of this product to pregnant women. The experience of using this product in pregnant women is also very limited and is not enough to evaluate its safety during pregnancy. 2. Reproductive toxicity studies of systemic tacrolimus have been conducted on rats and rabbits. When the mother was given an oral toxic dose of the drug, the fetus had adverse reactions. Oral doses of 0.32 and 1.0 mg/kg of tacrolimus (equivalent to 0.04 and 0.12 times the maximum recommended dose for humans, respectively, were given to rabbits during the embryonic organ formation stage, which produced toxic reactions to the mother rabbits and increased the abortion rate. Only in the higher dose group was the proportion of fetal malformations and developmental abnormalities increased. Oral administration of 3.2 mg/kg of tacrolimus to rats during the period of embryonic organogenesis produced toxic reactions in the mother rats, and led to increased resorption in the later period, decreased number of live fetuses, and decreased weight and developmental capacity of the pups. After the period of embryonic organogenesis and during lactation, oral administration of 1.0 and 3.2 mg/kg (equivalent to 0.04 and 0.12 times the maximum recommended dose for humans, based on body surface area) of tacrolimus to pregnant rats resulted in decreased weight of the pups. 3. No reduction in reproductive capacity was observed in male or female animals. 4. No appropriately controlled studies have been conducted on the systemic administration of tacrolimus to pregnant women. Tacrolimus can cross the placenta, and systemic administration of tacrolimus during pregnancy can cause neonatal hyperkalemia and renal dysfunction. This product can only be used during pregnancy when the benefits of treatment to the mother outweigh the potential harm to the fetus. 5. Although the systemic absorption of tacrolimus after topical application of this product is very small compared to systemic medication, it is known that tacrolimus can be secreted into breast milk. Because of the potential for serious adverse reactions in breastfeeding infants, the decision to stop breastfeeding or medication should be made based on the importance of the drug treatment to the mother. Elderly precautions: In Phase III clinical trials, 25 patients aged 65 and over were treated with this product. The adverse events in these patients were consistent with those in other adult patients.

The drug interaction of this product for topical application has not been studied. Due to the extremely small amount of absorption, this product is unlikely to interact with systemically administered drugs, but it cannot be completely ruled out. Patients with more extensive dermatitis and/or erythroderma should be cautious when taking known CYP3A4 inhibitors. Examples of these drugs include erythromycin, itraconazole, ketoconazole, fluconazole, calcium channel blockers and cimetidine.

Room temperature, 15-30℃

0.1% (10g: 10mg)

24 months

Sichuan MED-SHINE Pharmaceutical Co., Ltd.

• Founded in:

  1998-09-15

• Address:

  No. 1069, Tsingtao Beer Avenue, Chengdu Cross-Strait Science and Technology Industrial Development Park, Wenjiang District, Chengdu

• Tax NO.:

  9151011570915754XK

• Registered Funds:

  50 million yuan

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