Tacrolimus, cutaneous

Generic name
Tacrolimus, cutaneous
Brand name
ATC Code
D11AH01
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Tacrolimus, cutaneous

Dosages
Side effects in children
Warnings & precautions in children
Contra-indications in children

Interactions
PK
Renal impairment
References

Pharmacokinetics in children

The pharmacokinetics of tacrolimus after topical application are similar to those reported in adults, with minimal systemic exposure and no evidence of accumulation.

Absorption:

Data from healthy human subjects indicate that there is little or no systemic exposure to tacrolimus following single or repeated topical application of tacrolimus ointment.Most atopic dermatitis patients (adults and children) treated with single or repeated application of tacrolimus ointment (0.03-0.1%), and infants from age of 5 months treated with tacrolimus ointment (0.03%) had blood concentrations <1.0 ng/ml.

When observed, blood concentrations exceeding 1.0 ng/ml were transient. Systemic exposure increases with increasing treatment areas. However, both the extent and the rate of topical absorption of tacrolimus decrease as the skin heals. In both adults and children with an average of 50% body surface area treated, systemic exposure (i.e. AUC) of tacrolimus from Protopic is approximately 30-fold less than that seen with oral immunosuppressive doses in kidney and liver transplant patients. The lowest tacrolimus blood concentration at which systemic effects can be observed is not known.

There was no evidence of systemic accumulation of tacrolimus in patients (adults and children) treated for prolonged periods (up to one year) with tacrolimus ointment.

T1/2: 65 Stunden.

(SmPC Protopic 0.03% ointment)

dose recommendation of formulary compared to licensed use (on-label versus off-label)

No information is present at this moment.

Available formulations

No information is present at this moment.

Dosages

Atopic dermatitis
  • Cutaneous
    • 2 years up to 16 years

      • Initial dose:   0.03% ointment: apply twice daily to the affected skin for a maximum of 3 weeks. Then reduce the frequency to once daily until the wound is fully healed.
        Maintenance dose: 0.03% ointment: apply the ointment twice a week (at an interval of 2-3 days) to areas that were previously affected.
        If there are signs of a relapse, twice daily treatment with the ointment should be resumed.

    • 16 years up to 18 years

      • Initial dose: 0.1% ointment: apply twice daily and continue the treatment until the lesion has disappeared. Then reduce the frequency or use lower-strength Protopic ointment (0.03%).
        Maintenance dose: 0.1% ointment: apply the ointment twice a week (at an interval of 2-3 days) to areas that were previously affected.

        If there are signs of a relapse, twice daily treatment with the ointment should be resumed.
Therapy-resistant psoriasis in the face and intertriginous psoriasis
  • Cutaneous
    • 2 years up to 18 years

      • 0.03% or 0.1% ointment: apply twice daily.

      • The long-term safety has not been described in studies.

Renal impaiment in children > 3 months

GFR ≥10 ml/min/1.73m2: Dose adjustment not required.

GFR <10 ml/min/1.73m2: A general recommendation on dose adjustment cannot be provided.

The complete list of all undesirable drug reactions can be found in the national Summary of Product Characteristics (SmPC) – click here

Side effects in children

The frequency, nature and intensity of the adverse reactions observed in children are comparable to those reported in adults. Impetigo at the application site (7.7% in children) and infections at the application site (6.4% in children) have ocurred (SmPC).

The complete list of all contra-indications can be found in the national Summary of Product Characteristics (SmPC) – click here

Contra-indications

No information available on specific contra indications in children.

The complete list of all warnings and precautions can be found in the national Summary of Product Characteristics (SmPC) – click here

Warnings & precautions in children

Caution is needed when used for a lengthy period on a large affected skin area

Interactions

The complete list of all interactions can be found in the national Summary of Product Characteristics (SmPC) – click here

OTHER DERMATOLOGICAL PREPARATIONS

This pages provides a list of drugs from the same ATC class for comparison. This does not necessarily mean that these drugs are interchangeable.

Other dermatologicals
D11AX
Agents for dermatitis, excluding corticosteroids
D11AH08
D11AH05
D11AH02
D11AH07
OTHER DERMATOLOGICALS
D11AX

References

  1. Astellas Pharma, SPC Protopic (EU/1/02/201/001, EU/1/02/201/002, EU/1/02/201/005) , www.ema.europa.eu, Geraadpleegd 1 april 2011
  2. CBO, Richtlijn Constitutioneel Eczeem, www.cbo.nl, Maart 2015
  3. NVDV, Multidisciplinaire evidencebased richlijn Psoriasis, 2017
  4. Uptodate: UpToDate®, Pediatric Drug information: Tacrolimus topical Lexicomp® Topic 16050 Version 132.0, accessed 01/19
  5. LEO Pharma A/S, SmPC, Protopic® 0,1 % Salbe (EU/1/02/201/003), 06/18
  6. LEO Pharma A/S, SmPC, Protopic® 0,03 % Salbe (EU/1/02/201/001), 06/18
  7. Astellas Pharma, SPC Protopic (EU/1/02/201/001, EU/1/02/201/002, EU/1/02/201/005), www.ema.europa.eu, Geraadpleegd 1 april 2011

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