Pharm

Tacrolimus Ointment

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Tacrolimus Ointment, Protopic, Elidel, Pimecrolimus

Indications

Severe refractory Atopic Dermatitis

Pharmacokinetics

Normal topical use causes <5 ng/ml serum concentration
1. Greater absorption in severely damaged skin
Factors increasing serum concentrations
1. Higher doses or greater surface area of application
2. Inflamed skin

Mechanism

Macrolide with similar activity to Cyclosporine
Specifically binds T Cell receptors
1. Inhibits Cytokine production
2. Inhibits IgE sensitivity

Precautions

Increased risk of Skin Malignancy and Lymphoma
1. FDA black box warning has been added
Do not use for extended periods of time
Use only in refractory Eczema

Preparations

Pimecrolimus (Elidel)
Tacrolimus (Protopic)

Dosing
Tracolimus

Children over age 2 years: Apply 0.03% ointment bid
Adults: Apply 0.03% or 0.1% ointment bid

Adverse Effects

Local irritation (transient <1 week)
1. Burning
2. Erythema
3. Pruritus
Less common adverse effects
1. Skin Tingling
2. Acne
3. Hyperesthesia
4. Alcohol intolerance
Immunosuppression related adverse effects
1. Varicella zoster increased Incidence
2. Eczema herpeticum
Increased malignancy risk in mice (see precautions)
1. Skin Cancer
2. Lymphoma

Precautions

Protect treated areas from direct sunlight
Systemic Tacrolimus associated with Skin Cancer
1. Non-melanoma Skin Cancer

Advantages

Very effective in refractory atopic cases
Unlike Corticosteroids, does not cause skin atrophy
1. May be useful on face and neck

Disadvantages

Expensive (costs per Red Book)
1. Tacrolimus Ointment (0.03 or 0.1%): $60 per 30 grams
Risk of malignancy (see prcautions)
1. Skin Cancer
2. Lymphoma

References