Tacrolimus (Topical)

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Tacrolimus.jpg

[edit] MECHANISM OF ACTION

Tacrolimus is a macrolide immunosuppressant produced by Streptomyces tsukubaensis. It reduces interleukin-2 (IL-2) production by T-cells

[edit] INDICATIONS

Approved Indications
Flare treatment:

  • Adults and adolescents (16 years of age and above): Treatment of moderate to severe atopic dermatitis in adults who are not adequately responsive to or are intolerant of conventional therapies such as topical corticosteroids.
  • Children (2 years of age and above): Treatment of moderate to severe atopic dermatitis in children who failed to respond adequately to conventional therapies such as topical corticosteroids.

Maintenance treatment: Treatment of moderate to severe atopic dermatitis for the prevention of flares and the prolongation of flare-free intervals in patients experiencing a high frequency of disease exacerbations (i.e. occurring 4 or more times per year) who have had an initial response to a maximum of 6 weeks treatment of twice daily tacrolimus ointment (lesions cleared, almost cleared or mildly affected).


Off-label

  • Treatment of geographic tongue: Geographic tongue is an inflammatory condition of the dorsal surface and lateral border of the tongue, which may be asymptomatic. Successful management was achieved with topical application of 0.1% tacrolimus on a 6-year-old child Ref and on two adult patients. After two weeks of treatment with 0.1% tacrolimus ointment twice daily, their troublesome condition (lesions and discomfort) was improved without any side effects and no exacerbation was found after the follow-up period of 2 months.Ref
  • Psoriasis: tacrolimus 0.1% ointment may be a safe and effective treatment option for patients with psoriasis on the face, genital, and intertriginous areas.RefRef
  • Vitiligo: Topical tacrolimus can be used for the treatment of patients (adult and children) with vitiligo.Ref Repigmentation of lesions on the head and neck is superior to repigmentation of the body and extremities.Ref

[edit] DOSAGE

Topical Tacrolimus is available in two strengths, 0.03% and 0.1% ointment.


Flare treatment
Tacrolimus (Topical) can be used for short-term and intermittent long-term treatment. Treatment should not be continuous on a long-term basis. Tacrolimus (Topical) treatment should begin at the first appearance of signs and symptoms. Each affected region of the skin should be treated with Tacrolimus (Topical) until lesions are cleared, almost cleared or mildly affected. Thereafter, patients are considered suitable for maintenance treatment (see below). At the first signs of recurrence (flares) of the disease symptoms, treatment should be re-initiated.

  • Adults and adolescents (16 years of age and above)

Treatment should be started with Tacrolimus (Topical) 0.1% twice a day and treatment should be continued until clearance of the lesion. If symptoms recur, twice daily treatment with Tacrolimus (Topical) 0.1% should be restarted. An attempt should be made to reduce the frequency of application or to use the lower strength Tacrolimus (Topical) 0.03% ointment if the clinical condition allows. Generally, improvement is seen within one week of starting treatment. If no signs of improvement are seen after two weeks of treatment, further treatment options should be considered.

  • Older people

Specific studies have not been conducted in older people. However, the clinical experience available in this patient population has not shown the necessity for any dosage adjustment.

  • Pediatric population

Children (2 years of age and above) should use the lower strength Tacrolimus (Topical) 0.03% ointment.
Treatment should be started twice a day for up to three weeks. Afterwards the frequency of application should be reduced to once a day until clearance of the lesion.

Tacrolimus (Topical) ointment should not be used in children aged below 2 years until further data are available.


Maintenance treatment
Patients who are responding to up to 6 weeks treatment using tacrolimus ointment twice daily (lesions cleared, almost cleared or mildly affected) are suitable for maintenance treatment.

  • Adults and adolescents (16 years of age and above)

Adult patients should use Tacrolimus (Topical) 0.1% ointment.
Tacrolimus (Topical) ointment should be applied once a day twice weekly (e.g. Monday and Thursday) to areas commonly affected by atopic dermatitis to prevent progression to flares. Between applications there should be 2–3 days without Tacrolimus (Topical) treatment.
After 12 months treatment, a review of the patient`s condition should be conducted by the physician and a decision taken whether to continue maintenance treatment in the absence of safety data for maintenance treatment beyond 12 months.
If signs of a flare reoccur, twice daily treatment should be re-initiated (see flare treatment section above).

  • Older people

Specific studies have not been conducted in older people (see flare treatment section above).

  • Pediatric population

Children (2 years of age and above) should use the lower strength Tacrolimus (Topical) 0.03% ointment.
Tacrolimus (Topical) ointment should be applied once a day twice weekly (e.g. Monday and Thursday) to areas commonly affected by atopic dermatitis to prevent progression to flares. Between applications there should be 2–3 days without Tacrolimus (Topical) treatment.
The review of the child`s condition after 12 months treatment should include suspension of treatment to assess the need to continue this regimen and to evaluate the course of the disease.

Tacrolimus (Topical) ointment should not be used in children aged below 2 years until further data are available.


Method of administration
Tacrolimus (Topical) ointment should be applied as a thin layer to affected or commonly affected areas of the skin.
Tacrolimus (Topical) ointment may be used on any part of the body, including face, neck and flexure areas, except on mucous membranes. Tacrolimus (Topical) ointment should not be applied under occlusion because this method of administration has not been studied in patients.

[edit] CONTRAINDICATIONS

  • Hypersensitivity to the active substance, macrolides in general, or to any of the excipients
  • Children less than 2 years of age

[edit] WARNINGS AND PRECAUTIONS

  • Malignancy: Although a causal relationship has not been established, rare cases of malignancy (e.g., skin and lymphoma) have been reported in patients treated with topical calcineurin inhibitors, including topical Tacrolimus. Therefore: Continuous long-term use of topical Tacrolimus, in any age group should be avoided, and application limited to areas of involvement with atopic dermatitis. The use of topical Tacrolimus should be avoided on pre-malignant and malignant skin conditions.
  • Sun Exposure: During the course of treatment, patients should minimize or avoid natural or artificial sunlight exposure, even while Tacrolimus is not on the skin.
  • Renal Insufficiency: Rare post-marketing cases of acute renal failure have been reported in patients treated with topical Tacrolimus

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Topical Tacrolimus should be used during pregnancy only if the potential benefit to the mother justifies a potential risk to the fetus.
  • Nursing Mothers: It is known that tacrolimus is excreted in human milk. Because of the potential for serious adverse reactions in nursing infants from tacrolimus, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

[edit] SIDE EFFECTS

Topical Tacrolimus may cause local symptoms such as skin burning (burning sensation, stinging, soreness) or pruritus. Localized symptoms are most common during the first few days of treatment and typically improve as the lesions of atopic dermatitis resolve.

Other side effects include acne, swollen or infected hair follicles, headache, increased sensitivity of the skin to hot or cold temperatures, or flu-like symptoms such as the common cold and stuffy nose, skin tingling, upset stomach, muscle pain, swollen glands (enlarged lymph nodes), or skin infections including cold sores, chicken pox or shingles.

[edit] RELATED LINKS

Eczema (Atopic Dermatitis) Treatment

[edit] BIBLIOGRAPHY

[edit] REFERENCES