1 - TOPICAL CALCINEURIN INHIBITORS Flashcards
Topical calcineurin inhibitors are free of the adverse effects of topical corticosteroids I.e. atrophy, striae, potential hypothalamo-pituitary-adrenal axis suppression
True
Cyclosporine (a calcineurin inhibitor) lacks topical activity because its large molecular weight results in poor epidermal penetration
True
Tacrolimus and pimecrolimus have lower molecular weights (than the oral calcineurin inhibitor cyclosporine) and so can penetrate inflamed skin
True
Tacrolimus is a macrolide produced by the soil bacterium Streptomyces tsukubaensis
True
Tacrolimus’s structure and mechanism of action are similar to those of cyclosporine
True
Tacrolimus and pimecrolimus prevents cytokine production and blocks T cell activation and proliferation
True
Topical tacrolimus is FDA approved as second line therapy for the short term and non-continuous chronic treatment of moderate to severe atopic dermatitis in immunocompetent adults
True
Topical tacrolimus for atopic dermatitis is as effective as moderately potent topical corticosteroids for the trunk and extremities, and superior in efficacy to mild potency corticosteroids for the face and neck
True
Chronic atopic dermatitis lesions of the face and flexures are most justified for treatment with topical calcineurin inhibitors
True (topical calcineurin inhibitors have comparatively superior/similar potency to a TCS that would not have been used on the face/flexures due to risk of TCS adverse effects)
Tacrolimus 0.1% ointment is similar in efficacy to topical corticosteroids of class I (superpotent) and class II/III (high) potency
True
Once the atopic dermatitis has stabilised, proactive maintenance treatment with Tacrolimus 2 or 3 times weekly can significantly prevent flares in paediatric and adult patients
True
Tacrolimus ointment may reduce the number of flares and prolonged the time to first flare in atopic dermatitis
True
Topical Tacrolimus is more effective than pimecrolimus in adult atopic dermatitis patients
True
Topical tacrolimus and Pimecrolimus have similar safety and tolerability profile
True
Use of topical tacrolimus ointment in oral lichen planus can result in systemic absorption, though clinically significant adverse events associated with systemic absorption have not been observed
True
The efficacy of topical tacrolimus ointment in oral lichen planus is at least equal to those of topical clobetasol propionate 0.05% ointment (superpotent Class I TCS)
True
Although there have been 2 cases of oral SCC in oral lichen planus patients after treatment with tacrolimus ointment, further studies will clarify if there is a causal relationship
True
Topical tacrolimus 0.03% ointment is generally for paediatric patients and the 0.1% ointment is generally for adult patients
True
Topical tacrolimus 0.1% ointment is almost as efficacious as clobetasol propionate 0.05% ointment (superpotent class I TCS) in vitiligo on the face
True
Tacrolimus 0.1% ointment has a defined role in facial, inverse and genital psoriasis
True
Topical tacrolimus and pimecrolimus, either as monotherapy or combined with oral hydroxychloroquine is effective in cutaneous lupus erythematosus
True (topical tacrolimus and pimecrolimus was equal to clobetasol propionate 0.05% ointment in facial LE)
Topical tacrolimus 0.1% ointment and pimecrolimus 1% cream is useful in seborrheic dermatitis
True
Open studies have shown favourable results with topical tacrolimus in the treatment of Rosacea
True
Tacrolimus 0.1% ointment has shown favourable results in morphea (localised scleroderma)
True
Topical tacrolimus may result in local application site irritation
True
The localised application site irritation due to topical tacrolimus is transient and decreases in prevalence over time
True
Both topical tacrolimus and pimecrolimus are absolutely contraindicated in individuals with hypersensitivity to the active drug or components of the ointment/cream
True
Both topical tacrolimus and pimecrolimus are relatively contraindicated in children less than 2 years of age
True
Both topical tacrolimus and pimecrolimus are absolutely contraindicated in individuals with an active skin infection at the site to be treated
True
Exposure to topical tacrolimus or pimecrolimus is not associated with an increase in the overall cancer rate
True
The use of topical tacrolimus may be associated with an increased risk of T-cell lymphoma
True (although this may be inconclusive as another study found no increased risk of lymphoma in patients treated with topical calcineurin inhibitors, and that patients with atopic dermatitis itself was associated with an increased lymphoma risk although this study did not find any cases of lymphoma in topical calcineurin inhibitors users)
There is a theoretical risk that topical calcineurin inhibitors may cause lymphoma, although available data on lymphoma following topical calcineurin inhibitor use are inconsistent and insufficient to draw a conclusion about the causal role
True
Available data have found no evidence indicating that skin cancer is associated with topical calcineurin inhibitor use
True
Combining UVB and tacrolimus seems to have a limited direct photocarcinogenic potential on keratinocytes compared to UVB alone
True
Systemic absorption of topical tacrolimus in atopic dermatitis is low and not clinically significant
True (although marked systemic absorption has been observed in Netherton’s syndrome)
Patients with Netherton’s syndrome treated with topical tacrolimus are at risk for systemic absorption of topical tacrolimus
True (serum levels elevated, although no signs or symptoms of toxicity have been observed) - tacrolimus can be switched to pimecrolimus
Topical tacrolimus may cause enhanced facial flushing after alcohol ingestion
True
Topical Tacrolimus may cause Rosacea-like dermatitis
True (although ironically topical tacrolimus has shown favourable results in Rosacea)
Topical tacrolimus may cause acne
True
Topical tacrolimus may cause reactivation of HPV infection
True
Pimecrolimus is a semi synthetic derivative of the macrolide ascomycin, with a similar structure to that of tacrolimus
True
Pimecrolimus appears to have a role in atopic dermatitis of the head and neck
True
The need for topical corticosteroids for atopic dermatitis on the head and neck is reduced with pimecrolimus cream
True
Intervention with Pimecrolimus cream at the first signs and symptoms of a subsequent recurrence of atopic dermatitis reduced the number of flares/prevented progression to flares requiring topical corticosteroids
True
The efficacy of pimecrolimus 1% cream in oral lichen planus is equal to topical Triamcinolone Acetonide 0.1% paste (moderately potent Class IV/V TCS)
True
Pimecrolimus 1% cream + NB-UVB is superior to placebo + NB-UVB for facial vitiligo lesions
True
Pimecrolimus 1% cream is equal in efficacy to mometasone furoate 0.1% cream (High potency Class II/III TCS) and clobetasol propionate 0.05% ointment (Superpotent Class I TCS) for facial vitiligo lesions
True
The role of pimecrolimus in inverse psoriasis is inconclusive
True (unlike tacrolimus, which has shown clear benefit for facial, genital and inverse psoriasis)
Pimecrolimus 1% cream has comparable efficacy to ketoconazole for seborrheic dermatitis, but adverse effects appeared more with pimecrolimus
True
Pimecrolimus 1% cream is effective in corticosteroid-induced Rosacea
True
Topical Pimecrolimus has successfully treated Netherton’s syndrome
True (increased absorption and systemic toxicity from topical tacrolimus)
There is no increase of systemic absorption of topical pimecrolimus with increasing body surface area treated
True (and no drug related systemic adverse events)
The order of decreasing potency for topical calcineurin inhibitors are Tacrolimus 0.1% > Tacrolimus 0.03% > Pimecrolimus 1%
True
Topical pimecrolimus has not been associated with drug related systemic events
True
The use of pimecrolimus cream results in minimal systemic absorption
True
Topical pimecrolimus does not increase the risk of malignancy
True (this risk is unclear with topical tacrolimus and lymphoma due to mixed data)
Topical pimecrolimus may cause enhancement of molluscum contagiosum
True
