Tacrolimus Monohydrate ointment is indicated for short-term and intermittent long-term treatment of moderate to severe atopic dermatitis in patients for whom conventional therapies are considered unsuitable due to potential risks, or in those who are unresponsive to or intolerant of standard treatments. Tacrolimus ointment is also used in various dermatological conditions, including chronic cutaneous graft-versus-host disease, hand and foot eczema, allergic contact dermatitis, vitiligo, psoriasis, lichen planus, facial lichen, vulvar lichen sclerosus, pyoderma gangrenosum, rheumatoid arthritis–associated leg ulcers, steroid-induced rosacea, alopecia areata, annular erythema, chronic actinic dermatitis, and resistant facial erythema.

Tacrolimus is a macrolide immunomodulatory agent produced by the fungus Streptomyces tsukubaensis. It inhibits T-lymphocyte activation by binding to the intracellular protein FKBP-12. A complex is then formed between Tacrolimus–FKBP-12, calcium, calmodulin, and calcineurin, which leads to inhibition of calcineurin phosphatase activity. This results in suppression of T-cell activation and a reduction in the overall inflammatory cascade.

Use in adults: Apply a thin layer of Tacrolimus ointment onto the affected skin areas twice daily and rub in gently and completely. Treatment should be continued for one week after clearing of signs and symptoms of atopic dermatitis. The safety of Tacrolimus ointment under occlusion which may promote systemic exposure has not been evaluated. Tacrolimus ointment should not be used with occlusive dressings.

Use in Children:

• Tacrolimus 0.03% ointment can be used in pediatric patients 2 years of age and older.
• Tacrolimus 0.1% ointment can be used in children 16 years of age and older.

Use in Elderly Patients: Patients >65 years old received Tacrolimus ointment in phase 3 studies. The adverse event profile for these patients was consistent with that for other adult patients.

Formal topical interaction studies with tacrolimus ointment have not been conducted. However, caution is advised when using concomitant CYP3A4 inhibitors in patients with extensive and/or erythrodermic disease. Examples include erythromycin, itraconazole, ketoconazole, fluconazole, calcium channel blockers, and cimetidine.

Tacrolimus ointment is contraindicated in patients with known hypersensitivity to tacrolimus or any component of the formulation.

Topical tacrolimus ointment is generally well tolerated. Rare side effects may include skin burning, pruritus, flu-like symptoms, allergic reactions, erythema, skin infections, headache, and similar mild local or systemic effects.

Pregnancy Category C. Adequate and well-controlled studies in pregnant women are not available. Although systemic absorption after topical use is minimal compared to systemic administration, tacrolimus is known to be excreted in human milk. Because of potential risk to the nursing infant, a decision should be made to either discontinue breastfeeding or discontinue the drug, considering the importance of therapy to the mother.

Caution is required when using tacrolimus ointment in patients with atopic dermatitis who are prone to superficial skin infections. Safety has not been established in patients with generalized erythroderma.

Tacrolimus ointment is intended for external use only. Accidental oral ingestion may lead to systemic tacrolimus-related adverse effects. In case of ingestion, medical attention should be sought immediately.

Drugs affecting the immune response

Do not store above 30°C. Protect from light and keep out of reach of children.