Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:3.1.3.16 (calcineurin)
 17,112 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The development of topical calcineurin inhibitors resulted in a significant improvement in the treatment of inflammatory skin diseases such as atopic dermatitis. In addition, an excellent amelioration of pruritus could be observed. Other itchy dermatoses such as chronic irritative hand dermatitis, rosacea, graft-versus-host-disease, renal pruritus, lichen sclerosus, prurigo simplex, prurigo nodularis, scrotal eczema, and inverse psoriasis also have been treated successfully with pimecrolimus and tacrolimus. The antipruritic effect currently is believed to be related to the inhibition of inflammatory cytokines. Furthermore, recent investigations indicate a release of neuropeptides from sensory nerve fibers and degranulation of mast cells mediated by pimecrolimus and tacrolimus. Similar effects have been observed during capsaicin treatment. These findings may provide a possible explanation for initially observed calcineurin inhibitors related side-effects such as burning and pruritus. Moreover, the antipruritic potency may be related to a direct effect on nerve fibers leading to suppression of itch mediated by unknown mechanisms.
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PMID:[Antipruritic effects of pimecrolimus and tacrolimus]. 1271 60

Therapeutic options for rosacea include topical agents, oral therapies, laser and light treatments, and surgical procedures. Topical therapies play a critical role in the treatment of patients with papulopustular rosacea and erythematotelangiectatic rosacea, and have the ability to effectively minimize certain manifestations of the disease, including papules, pustules, and erythema. The 3 primary agents for the topical treatment of rosacea are metronidazole, azelaic acid, and sodium sulfacetamide-sulfur. Each of these therapies is approved for the treatment of rosacea and has been validated by multiple studies. Additional topical therapies including benzoyl peroxide, clindamycin, retinoids, topical steroids, calcineurin inhibitors, and permethrin are not approved for the treatment of rosacea and play variable roles in the management of this condition.
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PMID:Topical therapies for rosacea. 1646 88

Steroid-induced erythema in rosacea is a therapeutic challenge because of its tendency to rebound and the local characteristics of the facial skin. We describe 3 cases of steroid-induced rosacea with the typical history of steroid abuse with tachyphylaxis. Steroids with increasing potency had to be used with increasing frequency in the course of treatment in order to achieve a response. Acute exacerbations followed any attempt at withdrawal. The steroid treatment was discontinued and therapy with pimecrolimus cream 1% twice daily initiated. This brought rapid and marked improvement within a few days. The cases show that the calcineurin antagonist pimecrolimus offers an effective and well-tolerated therapy option in the acute therapy of steroid-aggravated facial dermatoses.
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PMID:[Steroid-aggravated rosacea: successful therapy with pimecrolimus]. 1687 34

The topical calcineurin inhibitors (TCIs) pimecrolimus and tacrolimus are approved for atopic dermatitis but have additional potential in other inflammatory skin diseases. This article reviews their clinical use in non-atopic dermatitis diseases. In seborrheic dermatitis, asteatotic eczema, and contact dermatitis, TCIs are of great benefit and can compete with topical corticosteroids. In psoriasis, TCIs have shown clinical efficacy and safety in facial and intertriginous lesions. Further investigations into possible combinations of TCIs with other established treatments such as UVB irradiation in this disorder are necessary. Initial studies in cutaneous lupus erythematosus have been promising, whereas the response in rosacea and rosacea-like eruptions has been mixed. TCIs have been associated with good clinical responses in oral lichen planus and anogenital lichen sclerosus et atrophicus. In vitiligo, TCIs are associated with some degree of repigmentation, with better results being seen in children and in facial and neck areas. TCIs have a synergistic effect with UVB irradiation in vitiligo. There is a long list of small series and case reports documenting use of TCIs in various other skin conditions that warrant further validation. Although the established mode of action of TCIs is T-cell control, other effects also need to be considered. Specifically, TCIs reduce pruritus and erythema, which cannot be explained by T-cell interactions, and further investigations are needed in these fields.
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PMID:The role of topical calcineurin inhibitors for skin diseases other than atopic dermatitis. 1749 44

The introduction of topical calcineurin inhibitors resulted in a significant improvement in the treatment of atopic dermatitis. In addition, rapid amelioration of pruritus could be observed. In case reports, other pruritic dermatoses such as chronic irritative hand dermatitis, rosacea, graft-versus-host-disease, and lichen sclerosus were also treated successfully with pimecrolimus and tacrolimus. Twenty patients were treated with tacrolimus and pimecrolimus in a surveillance study to evaluate efficacy in pruritus and prurigo. Eighteen of 20 patients responded to therapy. Best results were obtained in localized and generalized pruritus while in prurigo nodularis only a subgroup of patients showed an improvement of pruritus. Further controlled studies are necessary to confirm these results.
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PMID:Treatment of pruritic diseases with topical calcineurin inhibitors. 1836 May 95

Many options exist for the treatment of rosacea, including topical and systemic therapies, laser and light-based therapies, and surgical procedures. A classification system for rosacea identifies 4 subtypes (i.e., erythematotelangiectatic, papulopustular, phymatous, and ocular), which may help guide therapeutic decision-making. The goals of therapy include reduction of papules, pustules, erythema, physical discomfort, and an improvement in quality of life. Standard topical treatment agents include metronidazole, azelaic acid, and sodium sulfacetamide-sulfur. Second line therapies include benzoyl peroxide, clindamycin, calcineurin inhibitors, and permethrin.
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PMID:Rosacea and its topical management. 1933 Feb 70

Pimecrolimus has been approved for more than five years for the treatment of atopic dermatitis in Germany. An important difference in the safety profile of this drug compared with topical corticosteroids is the lack of potential side effects which are often observed upon prolonged use of topical corticosteroids (skin atrophy, steroid-induced rosacea or perioral dermatitis). Even after prolonged use in sensitive skin areas, no tolerance to this drug is induced, in contrast to that seen with topical corticosteroids. The most common side effect of pimecrolimus is burning. Placebo-controlled studies suggest that pimecrolimus is associated with a slightly increased incidence of herpes simplex infections. Compared with topical corticosteroids, pimecrolimus does not increase the overall incidence of skin infections (including recurrent herpes simplex infections). So far, clinical studies with pimecrolimus have not shown any evidence of an increased risk of malignancy. The analysis of spontaneously reported adverse events has also not shown any evidence of malignancy caused by pimecrolimus. This corresponds with the results of a case-control study from a large U.S. database. According to the German guidelines on atopic dermatitis, topical calcineurin inhibitors are indicated when topical corticosteroids are not indicated or when an anticipated lengthy treatment course would lead to inevitable side effects. On sensitive areas such as face, intertriginous regions and scalp, they are preferred as first-line choice over topical corticosteroids
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PMID:Topical use of pimecrolimus in atopic dermatitis: update on the safety and efficacy. 1965 Aug 20

There are many options for the treatment of acne rosacea, including topical and systemic therapies, laser and light-based therapies, and surgical procedures. A classification system for rosacea identifies 4 subtypes (ie, erythematotelangiectatic, papulopustular, phymatous, and ocular), which may help guide therapeutic decision making. Until recently, the pathophysiology of acne rosacea has been poorly understood and limited to descriptions of factors that exacerbate or improve this disorder. Recent molecular studies suggest that an altered innate immune response is involved in the pathogenesis of the vascular and inflammatory disease seen in patients with rosacea. These findings may help explain the benefits of current treatments and suggest new therapeutic strategies helpful for alleviating this disease. The goals of therapy include reduction of papules, pustules, erythema, physical discomfort, and an improvement in quality of life. Standard topical treatment agents include metronidazole, azelaic acid, and sodium sulfacetamide-sulfur. Second-line therapies include benzoyl peroxide, clindamycin, calcineurin inhibitors, and permethrin. There are also various systemic therapy options.
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PMID:Updates on the pathophysiology and management of acne rosacea. 1982 Feb 88

Rosacea is one of the most common dermatoses of adults. In recent years many studies have contributed to a better understanding of the pathophysiology of rosacea. They suggest that an altered innate immune response is involved in the vascular and inflammatory manifestations seen in rosacea. A good understanding of the disease and its special features is necessary for the differential diagnosis of the many clinical subtypes and for a stage- and phase-specific treatment approach. Topical treatments that are widely accepted are metronidazole and azelaic acid; agents under investigation that show promise include permethrin, calcineurin inhibitors and sulfur compounds. For systemic therapy antibiotics (tetracyclines, macrolides) and recently doxycycline in anti-inflammatory rather than anti-microbial dosages are used, as well as isotretinoin in severe cases. Findings such as rhinophyma and telangiectases can be treated using different laser systems or dermabrasion. This article gives an overview regarding rosacea, a challenging condition with multiple therapeutic options.
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PMID:[Rosacea 2009 : new advances in pathophysiology, clinical staging and therapeutic strategies]. 1995 73

Topical corticosteroids have been the mainstay of treatment for atopic dermatitis (AD) over the last decade, especially in the setting of acute flares. However, heavy and prolonged use of topical corticosteroid is undesirable as it is associated with side effects such as, skin atrophy, telangiectasia, striae, steroid-induced dermatoses, rosacea, acne exacerbation, and in some severe and rare cases, systemic effects such as hypothalamic-pituitary-adrenal axis suppression, growth retardation and ocular problems. Non-steroidal ant-inflammatory agents specific for the treatment of AD (topical calcineurin inhibitors, or TCIs) are now available and they are a viable alternative to topical corticosteroids in treating dermatitis of the face, neck, eyelids, and intertriginous areas where there is a greater risk of the steroid-induced side effects. More recently, medical device emollients have entered the marketplace. These medical devices provide, but are not limited to, anti-oxidant, anti-protease, anti-inflammatory activity, and aid in restoring the natural balance of lipids, which is one of the causes of the epidermal abnormalities seen with AD. The present study evaluated the short-term effectiveness and appeal of a non-steroidal medicated device foam as compared to pimecrolimus cream 1% in the treatment of AD within a wide age group of subjects with active disease at baseline. In this study, both pimecrolimus and the medical device foam exhibited efficacy in mild-to-moderate AD. Primary efficacy was measured by IGA. After four weeks of treatment with the medical device foam, 82% of target lesions were scored "clear" (0) or "almost clear" (1) compared to 71% of target lesions under the pimecrolimus arm. This study confirmed that pimecrolimus cream 1% and the medical device foam work well in the treatment of AD in both adults and children with no associated adverse effects.
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PMID:Bilateral comparison study of pimecrolimus cream 1% and a ceramide-hyaluronic acid emollient foam in the treatment of patients with atopic dermatitis. 2163 8


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