ReportPharmacokinetics of topical calcineurin inhibitors in adult atopic dermatitis: A randomized, investigator-blind comparison
Section snippets
Study design
This was a randomized, investigator-blind, parallel-group, multicenter trial. Adult patients with moderate to severe AD (Investigators' Global Assessment8 [IGA] score of 3-5) affecting at least 30% of the total body surface area (TBSA) received twice-daily treatment with either pimecrolimus or tacrolimus for 13 days. An investigator-blind design was used because the formulation differences between the two study treatments made it impossible to conduct the study in a double-blind manner.
Patients
Patients
Patients
A total of 37 patients was randomized at 6 centers in the United States to receive either pimecrolimus (n = 18) or tacrolimus (n = 19). Baseline demographics are shown in Table I. In general, the two treatment groups had similar baseline demographic characteristics, with some slight imbalances in the proportion of women (12 of 18 in the pimecrolimus group and 17 of 19 in the tacrolimus group) and mean body weight (83 kg in the pimecrolimus group and 71.9 kg in the tacrolimus group). The mean
Discussion
Previously published studies have demonstrated that systemic absorption through the skin in most patients with AD who were treated with topical calcineurin inhibitors is negligible. Concentrations of the active compound in the blood were low or undetectable, even in the most susceptible patients, such as those with extensive disease and high body area to mass ratios, and pediatric patients.2, 3, 4, 5, 6, 7 However, significant absorption of topical tacrolimus has been reported in patients with
References (23)
- et al.
Tacrolimus ointment for the treatment of atopic dermatitis in adult patients: part II, safety
J Am Acad Dermatol
(2001) - et al.
Tacrolimus (FK506) ointment for atopic dermatitis: a phase I study in adults and children
J Am Acad Dermatol
(1998) - et al.
A randomized, vehicle-controlled trial of tacrolimus ointment for treatment of atopic dermatitis in children: pediatric tacrolimus study group
J Allergy Clin Immunol
(1998) - et al.
Disease management of atopic dermatitis: a practice parameter. Joint task force on practice parameters, representing the American Academy of Allergy, Asthma and Immunology, the American College of Allergy, Asthma and Immunology, and the Joint Council of Allergy, Asthma and Immunology. Work group on atopic dermatitis
Ann Allergy Asthma Immunol
(1997) - et al.
Update on therapy of atopic dermatitis
J Allergy Clin Immunol
(1999) - et al.
Percutaneous absorption of drugs used in atopic eczema: pimecrolimus permeates less through skin than corticosteroids and tacrolimus
Int J Pharm
(2004) - et al.
Topical immunomodulators for atopic dermatitis
Curr Opin Pediatr
(2002) - et al.
First experience of topical SDZ ASM 981 in children with atopic dermatitis
Br J Dermatol
(2001) - et al.
Systemic exposure, tolerability, and efficacy of pimecrolimus cream 1% in atopic dermatitis patients
Arch Dis Child
(2003) - et al.
Low systemic exposure after repeated topical application of pimecrolimus (Elidel, SD Z ASM 981) in patients with atopic dermatitis
Dermatology
(2002)
Validation of the Eczema Area and Severity Index for atopic dermatitis in a cohort of 1550 patients from the pimecrolimus cream 1% randomized controlled clinical trials program
Br J Dermatol
Cited by (55)
Topical treatments for atopic dermatitis (eczema): Systematic review and network meta-analysis of randomized trials
2023, Journal of Allergy and Clinical ImmunologyGuidelines of care for the management of atopic dermatitis in adults with topical therapies
2023, Journal of the American Academy of DermatologyManagement of Allergic Skin Disorders in Pregnancy
2023, Immunology and Allergy Clinics of North AmericaCitation Excerpt :Systemic absorption of topical tacrolimus is low, and available data suggest the risk of congenital defects is not increased.2,17 Although topical pimecrolimus is absorbed even less,18 its FDA label currently says not to use because of lack of experience. Topical tacrolimus is recommended because of a large amount of existing data and may be preferable to TCS especially for use on the face and areas prone to striae formation.2
Cancer risk with topical calcineurin inhibitors, pimecrolimus and tacrolimus, for atopic dermatitis: a systematic review and meta-analysis
2023, The Lancet Child and Adolescent HealthAtopic dermatitis and pregnancy
2022, Journal of Allergy and Clinical ImmunologyCitation Excerpt :Although an increased risk of prematurity has been demonstrated, it may be associated with maternal disease.55 Furthermore, because of the large size of the molecules, systemic absorption of tacrolimus and pimecrolimus is considered to be very low.56,57 Although not approved for use during pregnancy, topical calcineurin inhibitors can be recommended for the face, intertriginous areas, and thigh skin, where the use of TCSs is not favorable due to the risk of striae formation (Fig 5).49
Topical Calcineurin Inhibitors
2020, Comprehensive Dermatologic Drug Therapy, Fourth Edition
Funding source: Novartis Pharmaceuticals Corp.
Disclosure: Ms Chon and Dr Abrams are employees of Novartis Pharmaceuticals Corp. Dr Paul is an employee of Novartis Pharma AG.