Tacrolimus topical
- Drugs List
- Therapeutic Indications
- Dosage
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Topical formulations of tacrolimus.
Drugs List
Therapeutic Indications
Uses
Moderate/severe atopic dermatitis when other therapy unsuitable/ineffective
Treatment of moderate to severe atopic dermatitis in patients over 2 years of age who are not adequately responsive to or intolerant of conventional therapies, and, prevention of flares or prolongation of flare-free intervals in patients, who have had an initial response to treatment, experiencing a high frequency of disease exacerbations (four or more times a year).
Dosage
Adults
Treatment of flares
Apply tacrolimus 0.1% ointment as a thin layer twice a day to affected areas and continue until clearance of the lesions.
It may be applied on any part of the body, including face, neck and flexure areas, except on mucous membranes.
An attempt should be made to reduce the frequency of application or to use the lower strength tacrolimus 0.03% ointment if the clinical condition allows.
If signs of a flare occur, twice daily treatment with tacrolimus 0.1% ointment should be restarted.
Patients who are responding to up to six weeks treatment using tacrolimus ointment twice daily (lesions cleared, almost cleared or mildly affected) are considered suitable for maintenance treatment.
Maintenance Treatment
Apply tacrolimus 0.1% ointment once a day as a thin layer twice weekly to commonly affected areas to prevent progression of flares.
Between applications there should be two or three days without treatment.
If signs of a flare occur, twice daily treatment should be re-initiated.
After twelve months a review of a patient's condition should be conducted by the physician to consider whether to continue maintenance treatment in the absence of safety data for maintenance treatment beyond twelve months.
Elderly
(See Dosage; Adult)
Children
Treatment of flares
Children over 16 years of age
(See Dosage; Adult)
Children aged 2 to 16 years
Apply tacrolimus 0.03% ointment as a thin layer twice a day to affected areas for up to three weeks.
It may be applied on any part of the body, including face, neck and flexure areas, except on mucous membranes.
The frequency of application should be reduced to once a day until clearance of the lesion has occurred.
Treatment should be restarted at the first signs of recurrence of flare symptoms.
Patients who are responding to treatment using tacrolimus ointment twice daily (lesions cleared, almost cleared or mildly affected) are considered suitable for maintenance treatment.
Maintenance Treatment
Children over 16 years of age
(See Dosage; Adult)
Children aged 2 to 16 years
Tacrolimus 0.03% ointment should be applied once a day as a thin layer twice weekly to commonly affected areas to prevent progression of flares.
Between applications there should be two or three days without treatment.
If signs of a flare occur, twice daily treatment should be re-initiated.
After twelve months a review of a patient's condition should be conducted by the physician to consider whether to continue maintenance treatment in the absence of safety data for maintenance treatment beyond twelve months.
Contraindications
Children under 2 years
Immunosuppression
Suspected malignant melanoma
Pre-malignant skin lesions
Skin infection
Precautions and Warnings
Children aged 2 to 16 years
Acute erythroderma
Breastfeeding
Netherton syndrome
Pregnancy
Severe hepatic impairment
Administration of live vaccines is not recommended
Safety of maintenance treatment beyond 12 months has not been established
Clinical infections at treatment sites should be cleared before treatment
Not all available brands are licensed for all age groups
Treatment to be initiated by specialist
Contains butylated hydroxytoluene - May irritate skin/eyes/mucous membranes
Avoid contact with eyes
Avoid contact with mucous membranes
Avoid occlusive dressings
Breastfeeding: Do not treat the breast area if patient breastfeeding
Emollients should not be applied to the same area within 2 hours
Increased risk of eczema herpeticum
Increased risk of skin herpes
Possible systemic effects if applied to broken or ulcerated skin
Discontinue if lymphadenopathy of unknown origin occurs during therapy
Discontinue in acute infectious mononucleosis
Advise patient alcohol intake may cause flushing/irritation of treated skin
Advise patient on appropriate sun protection methods
Advise patient residue on clothing/bedding may cause fire hazard
Advise pt. to minimise exposure to sunlight & avoid sunlamps during therapy
Fire hazard: Keep away from naked flames and potential sources of ignition
If symptoms persist or worsen for more than 2 weeks, consult a doctor
Pregnancy and Lactation
Pregnancy
Tacrolimus ointment should be used with caution in pregnancy.
There are insufficient data from the use of tacrolimus ointment in pregnant women.
Human data show that the drug is able to cross the placenta. Data from systemic treatments indicate no evidence of increased risk of adverse effects on the course and outcome of pregnancy compared with other immunosuppressive products. Cases of spontaneous abortion have been reported.
In rats and rabbits systemic tacrolimus has been shown to cause embryofoetal toxicity which demonstrated maternal toxicity.
Schaefer advises that topical use of tacrolimus on small surfaces is permissible when no alternatives exist.
The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Lactation
Use with caution in breastfeeding.
Human data demonstrate that tacrolimus is excreted into breast milk. Detrimental effects on the newborn cannot be excluded. Tacrolimus presents a low risk to the nursing infant because it is poorly absorbed after topical application on the maternal skin. The infant's skin must not come into direct contact with the areas of the skin that have been treated. The treated breasts should be washed before the infant is breastfed.
Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1
Counselling
Advise patients to consult a doctor if symptoms persist or worsen for after two weeks.
Advise patients on appropriate sun protection methods, such as minimisation of the time in the sun, use of a sunscreen product and covering of the skin with appropriate clothing.
Emollients should not be applied to the same area within two hours of applying tacrolimus ointment. Advise patient that consumption of alcohol may lead to flushing or irritation of the treated skin.
Side Effects
Acne
Alcohol intolerance
Burning sensation
Dysaesthesia
Eczema herpeticum
Erythema at application site
Folliculitis
Herpes infections
Herpes simplex
Hyperaesthesia
Impetigo
Infection (application site)
Irritation at application site
Kaposi's varicelliform eruption
Lymphadenopathy
Lymphoma
Oedema at application site
Pain at application site
Paraesthesia
Pruritus
Rash
Rosacea
Sensation of warmth
Skin carcinoma
Upper respiratory tract infection
Overdosage
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Further Information
Last Full Review Date: February 2013
Reference Sources
British National Formulary, 64th Edition (2012) Pharmaceutical Press, London.
BNF for Children (2012-2013) Pharmaceutical Press, London.
Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 2nd edition (2007) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.
Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.
Martindale: The Complete Drug Reference, 37th edition (2011) ed. Sweetman, S. Pharmaceutical Press, London.
Medications and Mothers' Milk, 14th Edition (2010) Hale, T. Hale Publishing, Amarillo, Texas.
Summary of Product Characteristics: Protopic 0.1% ointment. Astellas Pharma Ltd. Revised January 2013.
Summary of Product Characteristics: Protopic 0.03% ointment. Astellas Pharma Ltd. Revised June 2018.
US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
Available at: https://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT
Tacrolimus. Last revised: January 15, 2013
Last accessed: February 11, 2013
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