Tacrolimus
Tacrolimus is a topical calcineurin inhibitor.
Group
Topical calcineurin inhibitor
Mechanism of Action
Blocks calcineurin-dependent T-cell activation through an intracellular immunophilin complex.
Dose Rates
Dogs
| Use / stage | Dose | Route | Schedule | Instructions |
|---|---|---|---|---|
| Localized immune-mediated skin disease | Reference only | TOPICAL | Apply 0.1% ointment to affected localized lesions; amount per application is not specified. Canine application has been twice daily. | |
| Perianal fistula | Reference only | TOPICAL | Apply 0.1% ointment twice daily; may be used with systemic prednisolone in an individualized plan. |
Cats
| Use / stage | Dose | Route | Schedule | Instructions |
|---|---|---|---|---|
| Localized immune-mediated skin disease | Reference only | TOPICAL | Apply 0.1% ointment to affected localized lesions; amount per application is not specified. Canine application has been twice daily. |
Indications
- Localized immune-mediated skin lesions
- Canine perianal fistula
Contraindications
- Infection susceptibility requires caution; systemic safety is unestablished.
Interactions
- No topical interactions are identified in the clinical guidance.
Adverse effects
- Transient local burning or itch; systemic administration can cause severe GI injury.
Preparations
| Preparation | Form | Strength | Route |
|---|---|---|---|
| Tacrolimus ointment 0.1% | Other | 1 mg / g | TOPICAL |
| Tacrolimus ointment 0.03% | Other | 0.3 mg / g | TOPICAL |
| Compounded sterile tacrolimus ophthalmic solution 0.01% For ocular use only; validated sterile compounding and formulation required. Not interchangeable with skin ointment. | Other | 0.1 mg / mL | TOPICAL |
| Compounded sterile tacrolimus ophthalmic solution 0.03% For ocular use only; not prepared from Protopic skin ointment. | Other | 0.3 mg / mL | TOPICAL |
Monitoring and Administration
Limit application to affected skin and prevent handler skin contact. Use the original formulation; do not extrapolate skin ointments to sterile ophthalmic use.
Compounded sterile tacrolimus 0.01-0.03% ophthalmic solutions/ointments have been described for keratoconjunctivitis sicca, including cyclosporine-resistant cases. Commercial Protopic skin ointment contains ocular-irritant excipients and must not be used in, or compounded into preparations for, the eye. Exact drop amount/frequency is not specified in the tacrolimus subsection.
Skin treatment is usually twice daily until controlled, then reduced to the minimum effective frequency. Additional localized indications include discoid lupus, pemphigus, pinnal vascular lesions and alopecia areata. Wear gloves or use an applicator; long-term cutaneous safety is incompletely characterized.