Products
Topical calcineurin inhibitors are commercially available in many countries as ointments and creams (Protopic, Elidel). They have been approved in many countries since 2001 and 2003, respectively.
Effects
The active ingredients (ATC D11AH) have anti-inflammatory and immunomodulatory properties. The effects are based on inhibition of the calcium-dependent phosphatase calcineurin. This reduces T-cell activation and proliferation and the synthesis and release of proinflammatory cytokines.
Indications
For short-term and intermittent long-term treatment of atopic dermatitis as a second-line agent. The drugs are also used for other skin conditions but are not officially approved by regulatory authorities for this purpose (e.g., vitiligo, contact dermatitis).
Dosage
According to the professional information. The agents are applied thinly once or twice daily.
- Uninterrupted long-term treatment should be avoided.
- The skin should be well protected from the sun.
- Do not apply under occlusion.
- Do not apply to mucous membranes.
Active ingredients
- Tacrolimus (Protopic)
- Pimecrolimus (Elidel)
Contraindications
- Hypersensitivity
- Children under 2 years
- Pregnancy and lactation: see SmPC
For full precautions, see the drug label.
Interactions
Systemic interactions are unlikely but must be considered. Pimecrolimus and tacrolimus are metabolized via CYP3A4. Tacrolimus is a potent inhibitor of CYP1A and CYP3A4.
Adverse effects
The most common potential adverse effects include local skin reactions such as infection, a burning sensation, itching, and redness. In rare cases, malignancies such as skin cancer have been reported. However, the connection has not been proven with certainty. For this reason, the drugs should be used only in the short term and as a 2nd-line agent.
