TRICOLIMUS

Indications

• Atopic dermatitis (eczema)
• Psoriasis
• Seborrheic dermatitis

Dosage

Children: For children aged 6-11 years, medical supervision is required. Apply 1-2 times a day as needed. For those aged 12-17 years, the recommended application is once weekly as required, or alternatively, apply daily for the first 3-7 days if the condition is severe.

Adults: Apply 1-2 times a day to affected areas. For the short-term treatment of moderate to severe cases, it may be applied twice daily until symptoms resolve, then frequency can be reduced as needed.

Mechanism of action

Pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium-dependent phosphatase calcineurin. This action blocks T cell activation by preventing the transcription of early cytokines, specifically inhibiting interleukin-2 and interferon gamma (Th1-type) as well as interleukin-4 and interleukin-10 (Th2-type) cytokine synthesis in human T cells. Additionally, pimecrolimus inhibits the release of inflammatory cytokines and mediators from mast cells upon stimulation.

Pharmacodynamics

Pimecrolimus is utilized to manage atopic dermatitis, a condition marked by skin inflammation characterized by itching and redness. Though the precise mechanisms of pimecrolimus remain partially understood, it is known to decrease the activity of T-cells and mast cells involved in immune responses, thereby reducing inflammation and other related symptoms.

Pharmacokinetics

Pimecrolimus is administered topically, leading to minimal systemic absorption. Its pharmacokinetics are characterized by localized action at the site of application, with a rapid onset of therapeutic effects. The drug is metabolized primarily in the liver, and its elimination half-life is not well-defined due to its topical administration, which limits systemic exposure.

Contra-indications

• Hypersensitivity to pimecrolimus or any excipients
• Application to malignant skin lesions

Adverse effects

• Increased risk of infection
• Skin discolouration
• Skin papilloma
• Facial flushing and skin irritation with alcohol consumption

Interactions

• Severe interactions with mifamurtide due to decreased efficacy

Precautions

• Avoid excessive exposure to sunlight and sunlamps
• Avoid other topical treatments except emollients at treatment site

Pregnancy

Manufacturer advises avoidance due to potential toxicity in animal studies following systemic administration.

Breast-feeding

Manufacturer advises caution; ensure infant does not come in contact with treated areas.

Storage

Store below 25°C. Protect from light.

Formulations

• Pimecrolimus cream 1% (Elidel)
• Pimecrolimus ointment

Mechanism of action

Pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium-dependent phosphatase, calcineurin. As a consequence, it inhibits T cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T cells. Also, pimecrolimus prevents the release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/lgE.

Pharmacodynamics

Pimecrolimus is a chemical that is used to treat atopic dermatitis (eczema). Atopic dermatitis is a skin condition characterized by redness, itching, scaling and inflammation of the skin. The cause of atopic dermatitis is not known; however, scientists believe that it may be due to activation of the immune system by various environmental or emotional triggers. Scientists do not know exactly how pimecrolimus reduces the manifestations of atopic dermatitis, but pimecrolimus reduces the action of T-cells and mast cells which are part of the immune system and contribute to responses of the immune system. Pimecrolimus prevents the activation of T-cells by blocking the effects of chemicals (cytokines) released by the body that stimulate T-cells. Pimecrolimus also reduces the ability of mast cells to release chemicals that promote inflammation.