Tacrolimus

Registered South African indications:

• Moderate to severe atopic dermatitis

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to macrolides

Cautions

• Pregnancy
• Breastfeeding
• Hepatic impairment
• Elderly
• Ultraviolet light exposure
• Skin barrier defect
• Prolonged use
• Local immunosuppression 
• Malignancy, potentially malignant or premalignant lesions
• Immunodeficiency
• Skin infections
• Contact with eyes and mucous membranes
• Occlusive dressings

Forms avail. in SA and covered in this monograph: oin

Atopic dermatitis

• Topical (oin): Flare: 0.1% oin. Apply small quantity to affected area, 12hrly; Maintenance: Apply small quantity to affected area, dly twice a week; Ensure 2-3 days between applications

Treatment should be given until clearance of the lesion

An attempt should be made to reduce the frequency of application or use the lower strength (0.03%) if continued use is required

Can be used on all areas of body except mucous membranes

Treatment should not be continued on a long-term basis

Only apply emolient >2hrs after application of tacrolimus

Paed. forms avail. in SA and covered in this monograph: oin

Atopic dermatitis

Younger than 2 years

• Not established for use

Older than 2 years

• Topical (oin): Flare: 0.03% oin. Apply small quantity to affected area, 12hrly for up to 3 weeks; Then reduce to daily; Maintenance: Apply small quantity to affected area, dly twice a week; Ensure 2-3 days between applications

Treatment should be given until clearance of the lesion

An attempt should be made to reduce the frequency of application if continued use is required

Can be used on all areas of body except mucous membranes

Treatment should not be continued on a long-term basis

Only apply emolient >2hrs after application of tacrolimus

Pregnancy

• Caution
• There are no adequate data from the use of tacrolimus ointment in pregnant women. Studies in animals have shown reproductive toxicity following systemic administration. The potential risk for humans is unknown
• Tacrolimus ointment should not be used during pregnancy unless clearly necessary

Breastfeeding

• Caution; not recommended
• Human data demonstrate that, after systemic administration, tacrolimus is excreted into breast milk
• Although clinical data have shown that systemic exposure from application of tacrolimus ointment is low, breastfeeding during treatment with tacrolimus ointment is not recommended

Renal Impairment

• No dose adjustment recommended

Hepatic Impairment

• Caution; no dose adjustment recommended 

Elderly

• Caution; no information available
• 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

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Paraesthesia
• Dysaesthesia
• Hyperaesthesia

Endocrine and Metabolic Disorders

• Alcohol intolerance

Skin and Subcutaneous Tissue Disorders

• Pruritus
• Acne
• Rosacea
• Lentigo
• Application site reaction

Immune, Blood and Lymphatic System Disorders

• Eczema herpeticum
• Folliculitis
• Herpes simplex
• Herpes virus infection
• Kaposi's varicelliform eruption
• Ophthalmic herpes Infection

Emollients

None routine

Tacrolimus inhibits calcium-dependent signal transduction pathways in T cells, preventing transcription and synthesis of interleukins and other cytokines. It has also been shown to inhibit release of inflammatory mediators from skin mast cells, basophils and eosinophils.

Ointment (per g) 0,3mg

• Protopic 0.03% (Adcock Ingram) originator

Ointment (per g) 1mg

• Protopic 0.1% (Adcock Ingram) originator

Also available in the following forms: Capsule and injection