Pimecrolimus

Products

Pimecrolimus is commercially available as a cream (Elidel). It has been approved in many countries since 2003.

Structure and properties

Pimecrolimus (C43H68ClNO11, Mr = 810.5 g/mol) is a lipophilic macrolactam derivative of ascomycin, an ethyl analog of tacrolimus. It exists as a white crystalline powder that is insoluble in water.

Effects

Pimecrolimus (ATC D11AX15) has immunosuppressive and anti-inflammatory properties. It inhibits the calcium-dependent phosphatase calcineurin and thus T-cell activation and proliferation, as well as the synthesis of proinflammatory cytokines.

Indications

As a 2nd-line agent for the treatment of mild to moderate atopic dermatitis. The drug may be used in children 2 years of age and older. Other indications are described in the literature, but the cream has not yet been approved for these indications.

Dosage

According to the expert information. The cream is applied thinly to the affected areas twice daily and rubbed in gently.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Pimecrolimus is metabolized by CYP3A4. Drug-drug interactions with systemically applied agents are unlikely. Vaccination during treatment-free intervals is recommended. Concurrent treatment with glucocorticoids or other immunosuppressive therapies should be refrained from. Alcohol intolerance has rarely been observed, so alcohol should be consumed with caution.

Adverse effects

The most common potential adverse effects include local reactions at the application site such as burning, irritation, itching, redness, and skin infections. Very rarely, the development of skin cancer and lymphoma has been reported. However, whether a link actually exists is controversial.