Dosing and uses of Protopic (tacrolimus ointment)
Adult dosage forms and strengths
ointment
- 0.03%
- 0.1%
Atopic Dermatitis
0.03% or 0.1% ointment: Apply thin layer to affected area q12hr; discontinue treatment when symptoms have cleared; if no improvement within 6 weeks, reassess diagnosis
Pediatric dosage forms and strengths
ointment
- 0.03%
- 0.1%
Atopic Dermatitis
<2 years old: Not recommended
2-15 years: 0.03% ointment: Apply thin layer to affected area q12hr
>15 years: Apply 0.03% or 0.1% ointment as thin layer to affected area q12hr; discontinue treatment when symptoms have cleared; if no improvement within 6 weeks, reassess diagnosis
Protopic (tacrolimus ointment) adverse (side) effects
>10%
Burning sensation (43-58%)
Pruritus (41-46%)
Flu-like symptoms (23-31%)
Skin erythema (12-28%)
Headache (5-20%)
Postmarketing Reports
CNS: Seizures
Infections: Bullous impetigo, osteomyelitis, septicemia
Neoplasms: Lymphomas, basal cell carcinoma, squamous cell carcinoma, malignant melanoma
Renal: Acute renal failure in patients with or without Netherton’s syndrome, renal impairment
Skin: Rosacea, application site edema
Warnings
Black box warnings
Rare cases of malignancy reported (although causal relationship not identified)
Avoid long-term use and limit application to areas of atopic dermatitis
Not indicated for use in children <2 yr
Only 0.03% ointment indicated for children aged 2-15 years
Contraindications
Hypersensitivity
Age <2 yr
Cautions
Preferably use as second-line agents for short-term & intermittent treatment in unresponsive to, or intolerant of other treatments
Do not use with occlusive dressings
May be associated with development of lymphadenopathy
Not for application in areas with active viral or bacterial infections
Acute renal failure reported (rare)
Potential risk of lymphoma and skin cancer
Not recommended in patients having skin conditions with a skin barrier defect where there is the potential for increased systemic absorption of tacrolimus (eg, Netherton's syndrome, lamellar ichthyosis, generalized erythroderma, cutaneous graft vs host disease)
Pregnancy and lactation
Pregnancy category: C
Lactation: Not known whether tacrolimus is distributed in milk following topical administration to skin
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Protopic (tacrolimus ointment)
Mechanism of action
Unknown; inhibits T-cell activation by binding to intracellular protein FKBP-12 and complexes with calcineurin dependent proteins
Pharmacokinetics
Absorption: No systemic absorption detected
Bioavailability: 0.5%
