Pimecrolimus

What it is and how it works

Mechanism of Action The mechanism of action of pimecrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that 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.

Mechanism class: Calcineurin Inhibitors

Indications

Pimecrolimus cream, 1% is indicated as second-line therapy for the short-term and non-continuous chronic treatment of mild to moderate atopic dermatitis in non-immunocompromised adults and children 2 years of age and older, who have failed to respond adequately to other topical prescription treatments, or when those treatments are not advisable. Pimecrolimus c ream, 1% is not indicated for use in children less than 2 years of age . Pimecrolimus cream, 1% is a calcineurin inhibitor immunosuppressant indicated as s e c o n d -l i n e th e r a p y for the short-term and non-continuous chronic treatment of mild to moderate atopic dermatitis in non-immunocompromised adults and children 2 years of age and older, who have failed to respond adequately to other topical prescription treatments, or when those treatments are not advisable.

Dosage and administration (summary)

Apply a thin layer of pimecrolimus cream, 1% to the affected skin twice daily. The patient should stop using pimecrolimus cream, 1% when signs and symptoms (e.g., itch, rash and redness) resolve and should be instructed on what actions to take if symptoms recur. If signs and symptoms persist beyond 6 weeks, patients should be re-examined by their health care provider to confirm the diagnosis of atopic dermatitis. Continuous long-term use of pimecrolimus cream, 1% should be avoided, and application should be limited to areas of involvement with atopic dermatitis . The safety of pimecrolimus cream, 1% under occlusion, which may promote systemic exposure, has not been evaluated.

Contraindications

Pimecrolimus cream, 1% is contraindicated in individuals with a history of hypersensitivity to pimecrolimus or any of the components of the cream. Pimecrolimus cream 1% is contraindicated in individuals with a history of hypersensitivity to pimecrolimus or any of the components of the cream. ( 4 , 6.2 )

Warnings and precautions

Should not be used in immunocompromised adults and children, including patients on systemic immunosuppressive medications. Avoid treatment on malignant or pre-malignant skin conditions, as these can present as dermatitis. Should not be used in patients with Netherton’s Syndrome or skin diseases with a potential for increased systemic absorption. 5.

Pregnancy

8. 1 Pregnancy Pregnancy Category C There are no adequate and well-controlled studies with pimecrolimus cream, 1% in pregnant women. Therefore, pimecrolimus cream, 1% should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Storage and supply

Pimecrolimus cream, 1% is a whitish cream available in tubes of 30 grams, 60 grams, and 100 grams. 30 gram tube………………………………………………………………NDC 0591-2944-30 60 gram tube………………………………………………………………NDC 0591-2944-60 100 gram tube……………………………………………………………..NDC 0591-2944-87 Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) . Do not freeze.

Source: Pimecrolimus (Pimecrolimus) — US FDA prescribing information, 2018-05-07, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.