Pimecrolimus: Skin disposition after topical administration in minipigs in vivo and in human skin in vitro

Gschwind, Hans‐Peter; Waldmeier, Felix; Zollinger, Markus; Schweitzer, A.; Grassberger, Maximilian A.

doi:10.1016/j.ejps.2007.09.004

Cited by 20 publications

(15 citation statements)

References 18 publications

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“…Moreover, pimecrolimus is more lipophilic and binds with higher affinity to structural skin proteins than tacrolimus, having a lower penetration rate in the dermis and a minor systemic biodisponibility [15]. …”

Section: Discussionmentioning

confidence: 99%

Topical Pimecrolimus as a New Optional Treatment in Cutaneous Sarcoidosis of Lichenoid Type

Tammaro

Abruzzese

Narcisi

et al. 2014

Case Reports in Dermatological Medicine

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Section: Discussionmentioning

confidence: 99%

Topical Pimecrolimus as a New Optional Treatment in Cutaneous Sarcoidosis of Lichenoid Type

Tammaro

Abruzzese

Narcisi

et al. 2014

Case Reports in Dermatological Medicine

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“…One might argue that drug concentrations are too low in vivo to be able to detect a change at 48 h. Topically applied pimecrolimus has also been shown to be able to act quickly in vivo , as it causes a rapid and detectable decrease in skin microcirculation by 72 h 29 . In addition, studies show that pimecrolimus penetrates the stratum corneum quickly (maximum concentration within 30 min) and that this concentration is not elevated with multiple dosing 30 . The dermal concentration found after a single application of 1% pimecrolimus cream in pigs is approximately 2 μg g −1 (2·5 μmol L −1 ) 30 .…”

Section: Discussionmentioning

confidence: 99%

“…In addition, studies show that pimecrolimus penetrates the stratum corneum quickly (maximum concentration within 30 min) and that this concentration is not elevated with multiple dosing 30 . The dermal concentration found after a single application of 1% pimecrolimus cream in pigs is approximately 2 μg g −1 (2·5 μmol L −1 ) 30 . Even considering extensive protein binding, this concentration is well above the subnanomolar concentrations needed for pimecrolimus to inhibit T‐cell function in patients with atopic dermatitis 31 .…”

Section: Discussionmentioning

confidence: 99%

The direct cellular target of topically applied pimecrolimus may not be infiltrating lymphocytes

Fiorentino¹,

Chen²,

Stewart³

et al. 2011

British Journal of Dermatology

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“…[56] Topical pimecrolimus was associated with a lower rate of permeation through healthy human skin, compared with topical tacrolimus [57,58] and topical corticosteroids. [56] Topical pimecrolimus was associated with a lower rate of permeation through healthy human skin, compared with topical tacrolimus [57,58] and topical corticosteroids.…”

Section: Absorption and Distributionmentioning

confidence: 99%

“…[61] In in vitro studies, pimecrolimus was almost exclusively metabolized by cytochrome P450 (CYP) 3A4. [56] Pimecrolimus is mainly eliminated via the fecal route. [56] Pimecrolimus is mainly eliminated via the fecal route.…”

Section: Metabolism and Eliminationmentioning

confidence: 99%

Topical Pimecrolimus

Yang¹,

Curran²

2009

Pediatric Drugs

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Topical pimecrolimus 1% cream (Elidel) [hereafter referred to as topical pimecrolimus] is a nonsteroidal alternative in the treatment of pediatric atopic dermatitis. In vehicle-controlled, short-term, continuous-use trials in pediatric patients with mild to moderate atopic dermatitis, topical pimecrolimus was effective in treating disease symptoms. Topical pimecrolimus was effective in preventing disease flares and reducing the need for topical corticosteroids in longer term, intermittent-use trials. In addition, topical pimecrolimus was associated with improvements in the health-related quality of life (HR-QOL) of pediatric patients with atopic dermatitis and their parents. In vehicle-controlled trials, topical pimecrolimus was generally as well tolerated as vehicle. Topical pimecrolimus showed similar efficacy to topical tacrolimus 0.03% ointment (hereafter topical tacrolimus) in a short-term, continuous-use trial and the two agents had a generally similar tolerability profile. Although comparative data between topical pimecrolimus and topical corticosteroids are lacking in pediatric patients, and the long-term tolerability (beyond 1-2 years) of topical pimecrolimus is yet to be established, topical pimecrolimus is a useful agent in the management of pediatric patients with mild to moderate atopic dermatitis who do not achieve satisfactory treatment with other topical pharmacologic treatments, including topical corticosteroids.

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Pimecrolimus: Skin disposition after topical administration in minipigs in vivo and in human skin in vitro

Cited by 20 publications

References 18 publications

Topical Pimecrolimus as a New Optional Treatment in Cutaneous Sarcoidosis of Lichenoid Type

Topical Pimecrolimus as a New Optional Treatment in Cutaneous Sarcoidosis of Lichenoid Type

The direct cellular target of topically applied pimecrolimus may not be infiltrating lymphocytes

Topical Pimecrolimus

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