What are the specific dosing examples for topical immunomodulators, such as Protopic (tacrolimus), and other calcineurin inhibitors used around the eye?

From the Guidelines

Topical calcineurin inhibitors like tacrolimus (Protopic) can be used for dermatologic conditions around the eyes, with a recommended dosing of 0.03% or 0.1% ointment applied thinly twice daily for 2-4 weeks, then tapered to once daily or intermittent use as maintenance, as supported by the most recent evidence from 2024 1.

Key Considerations

• For children, the 0.03% strength is preferred, while adults may use either strength, with a consensus that tacrolimus 0.1% ointment can be applied once daily to the external eyelids and including the lid margins for 2–4 weeks 1.
• Pimecrolimus 1% cream can be used similarly, applied twice daily until improvement, then reduced to once daily.
• When applying these medications around the eyes, use a small amount (pea-sized) and avoid getting the medication directly in the eyes.
• If accidental eye contact occurs, rinse thoroughly with water.

Mechanism and Safety

• These medications work by inhibiting T-cell activation and inflammatory cytokine production without causing skin atrophy, making them safer than topical steroids for delicate periocular skin.
• Patients may experience temporary burning or stinging upon application, which typically diminishes with continued use.
• These medications should be used for short courses when possible, and patients should be advised to use sun protection as they may increase photosensitivity.

Special Populations

• For patients aged 2–17 years, tacrolimus ointment can be considered, but only following advice from ophthalmology, with a recommended starting dose of tacrolimus 0.03% ointment 1.
• In cases with a history of ocular-surface herpes simplex virus or varicella zoster virus, the use of tacrolimus ointment is not recommended.

From the FDA Drug Label

To apply tacrolimus ointment: Advise patients: Wash their hands before applying tacrolimus ointment Apply a thin layer of tacrolimus ointment twice daily to the areas of skin affected by eczema. Use the smallest amount of tacrolimus ointment needed to control the signs and symptoms of eczema.

The dosing for tacrolimus ointment is twice daily, with a thin layer applied to the affected areas. The amount used should be the smallest amount needed to control symptoms.

• Key considerations:
  • Wash hands before applying
  • Apply to affected areas only
  • Use smallest amount needed
  • Avoid getting in eyes or mouth
  • Do not swallow
  • Do not use with ultraviolet light therapy, sun lamps, or tanning beds
  • Limit sun exposure 2

From the Research

Medication Dosing Examples

• Protopic (tacrolimus) 0.03% ointment applied to the eyelid skin twice daily 3
• Protopic (tacrolimus) 0.1% ointment applied twice daily for 8 weeks 4
• Topical cyclosporine 0.1% four times a day, combined with topical tacrolimus 0.03% twice a day 5
• Topical 0.1% tacrolimus, used in combination with steroids, for the treatment of chronic ocular surface inflammatory diseases 6

Important Considerations

• The use of topical calcineurin inhibitors, such as tacrolimus, may be associated with a theoretical risk of malignancy, although evidence suggests that this risk is low 7
• Long-term use of topical immunosuppressants and steroids may increase the risk of developing cytomegalovirus corneal endotheliitis 6
• Patients using these medications should be closely monitored for potential side effects and complications 3, 4, 7, 6