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Avita Azərbaycan Karyera Məhsullarımız Partnyorlarımız
Dermatologiya / Ametazon
Pubmed

J Biol Chem. 2012 Mar 21. [Epub ahead of print]

Deciphering modern glucocorticoid cross-pharmacology using ancestral corticosteroid receptors.

Kohn JADeshpande KOrtlund EA.

Source

Emory University, United States.

Abstract

Steroid receptors (SRs) are the largest family of metazoan transcription factors, and control genes involved in development, endocrine signaling, reproduction, immunity, and cancer. The entire hormone-receptor system is driven by a molecular switch triggered by the binding of small lipophilic ligands (1,2). This makes the SRs ideal pharmaceutical targets, yet even the best clinically approved synthetic steroidal agonists are prone to cross-reactivity and off-target pharmacology. The mechanism underlying this promiscuity is derived from the fact that SRs share common structural features derived from their evolutionary relationship. More often than not, rational attempts to probe SR drug selectivity via mutagenesis fail even when high quality structural and functional data is available, due to the fact that important mutations often result in nonfunctional receptor. This highlights the fact that steroid receptors suffer from instability preventing in depth mutational analysis and hampering crystallization of key receptor-ligand complexes. We have taken a unique approach to address this problem by using a resurrected ancestral protein to determine the structure of a previously intractable complex, identifying the structural mechanisms that confer activation and selectivity for a widely used glucocorticoid,mometasone furoate (MOF). Moreover, we identify a single residue located outside of the ligand binding pocket that controls MOF antagonism vs. agonism in the human mineralocorticoid receptor.

http://www.ncbi.nlm.nih.gov/pubmed/22437833

 

 

 

Lik Sprava. 2011 Apr-Jun;(3-4):29-40.

[Atopic dermatitis: a modern view of pediatricians and pediatric allergologist].

[Article in Ukrainian]

Okhotnikova OM.

Abstract

The article presents the views of pediatric allergologist on the problem of atopic dermatitis/ atopic eczema in children. Atopic dermatitis (AD) is considered from a modern viewpoint of allergic 'march', which is characteristic (typical) for children with atopy. These data indicate to systemic nature of atopic 'march', the first step of which is atopic eczema. Further evolution of atopic dermatitis leads to a transformation of it in other atopic diseases--allergic rhinitis and bronchial asthma; this fact indicates that immunopathological disorders are united in these diseases and it conditions the possibility of prevention. It has taken into consideration the systemic nature of atopic diseases, combined therapy is great important and has to include not only basic local therapy, in particular topical corticosteroids (mometasone furoate--Elokom) during the exacerbation, and the systematic elimination of trigger factors, diet, the removal of the digestive system dysfunctions and the imbalance of vitamins. A long-time systemic basic therapy by H1-antihistamines of second generation, such as desloratadine (Aerius) takes a special place in the treatment of atopic dermatitis.

http://www.ncbi.nlm.nih.gov/pubmed/22416361

 

 

 

Skin Pharmacol Physiol. 2012 Feb 17;25(3):133-141. [Epub ahead of print]

Bioavailability, Antipsoriatic Efficacy and Tolerability of a New Light Cream with Mometasone Furoate 0.1%

Korting HCSchöllmann CWillers CWigger-Alberti W.

Source

Department of Dermatology and Allergology, Ludwig Maximilian University, Munich, Germany.

Abstract

Mometasone furoate, a potent glucocorticoid (class III) with a favorable benefit/risk ratio, has emerged as a standard medication for the treatment of inflammatory skin disorders. The purpose of the investigation presented here was to determine the noninferiority of a topical mometasone formulation, a light cream (O/W 60/40 emulsion) with mometasone furoate 0.1% (water content of 33%) versus marketed comparators. Using the vasoconstrictor assay, a strong blanching effect of the new cream (called Mometasone cream) comparable to that of a mometasone comparator, a fatty cream withmometasone furoate 0.1%, could be demonstrated. Thus, the topical bioavailability of the active ingredient mometasone furoate (0.1%) was regarded to be similar for Mometasone cream and the mometasone comparator. Using the psoriasis plaque test, a strong antipsoriatic effect comparable to that of the mometasone comparator was found for Mometasone cream after 12 days of occlusive treatment. A nearly identical reduction in the mean infiltrate thickness and similar mean AUC values were noted with both formulations confirmed by clinical assessment data. The noninferiority ofMometasone cream to its active comparator with respect to the AUC of change to baseline in infiltrate thickness was demonstrated. Both medications were well tolerated. Overall, Mometasone cream and the mometasone comparator showed similar efficacy and tolerability. Mometasonecream, in addition to its high potency and good tolerability, provides the properties of a light cream, which might make this new medication particularly suitable for application on acutely inflamed and sensitive skin.

Copyright © 2012 S. Karger AG, Basel.

http://www.ncbi.nlm.nih.gov/pubmed/22353786

 

 

 

Br J Dermatol. 1999 May;140(5):882-6.

Long-term, intermittent treatment of chronic hand eczema with mometasone furoate.

Veien NKOlholm Larsen PThestrup-Pedersen KSchou G.

Source

The Dermatology Clinic, Vesterbro 99, DK-9000 Aalborg, Denmark. veien@dadlnet.dk

Abstract

Chronic hand eczema can be incapacitating, and there is little knowledge of the efficacy and safety of long-term treatment with topical corticosteroids. We compared the efficacy and safety of two different schedules for the treatment of chronic hand eczema with a potent topical corticosteroid, mometasone furoate. In a prospective, open, randomized trial, 120 patients with chronic hand eczema were treated daily withmometasone furoate fatty cream until the dermatitis cleared or for a maximum of 9 weeks. Those who cleared were randomized to treatment for up to 36 weeks with mometasone furoate on Sunday, Tuesday and Thursday (group A), mometasone furoate on Saturday and Sunday (group B) or no further corticosteroid treatment (group C). In the event of relapse, patients were permitted daily treatment with mometasone furoate for 3 weeks on two separate occasions. For 50 of 106 randomized patients, daily treatment for 3 weeks controlled their dermatitis; 29 needed 6 weeks and 27 needed 9 weeks of treatment. During the maintenance phase, 29 of 35 (83%) in group A, 25 of 37 (68%) in group B and nine of 34 (26%) in group C had no recurrences (P = 0.001, chi2-test). Side-effects were minimal. It is concluded that long-term, intermittent treatment of chronic hand eczema withmometasone furoate fatty cream is effective and safe.

http://www.ncbi.nlm.nih.gov/pubmed/10354026

 

 

 

Eur J Dermatol. 1998 Sep;8(6):421-6.

Mometasone furoate decreases adhesion molecule expression in psoriasis.

Berti ECerri AMarzano AVRichelda RBianchi BCaputo R.

Source

Institute of Dermatological Science, University of Milan, IRCCS Ospedale Maggiore, Milan, Italy.

Abstract

The topical corticosteroids are widely used in the treatment of moderate psoriasis, because of their usefulness for reducing inflammation and controlling itching. The therapeutic effect of corticosteroids in different cutaneous inflammatory diseases may be partially explained by their varying ability to block in vitro the synthesis of different cytokines, which play a pivotal role in epidermal hyperproliferation and leukocyte recruitment into the skin. The purpose of the present investigation was to further elucidate the mode of action of mometasone furoate, a medium-high potency, topical corticosteroid, on adhesion molecules, cytokines and cytokine receptor expression in psoriatic skin. Using an immunohistochemical assessment, we examined lesional skin biopsies from ten psoriatic patients before treatment and after 1 and 3 weeks of therapy. The overexpression of alpha 2, alpha 3, alpha 6, and beta 1 integrins detected in the spinous layer of untreated psoriatic skin was significantly decreased after therapy in 8 out of 10 cases, characterized by only partial clinical remission. In the remaining patients, a disappearance of the above integrin reactivity paralleling the disappearance of psoriatic lesions was induced by the treatment. With the exception of GM-CSF, no or only marginal effects of mometasone furoateon the cytokine and cytokine receptor system were observed. A significant reduction of the positive immunostaining with anti-ICAM-1 and ICAM-2 monoclonal antibodies on dermal vascular endothelial cells was also seen. Thus, our findings indicate that the therapeutic effects of mometasone furoate in psoriasis are mediated principally by decreasing adhesion molecule expression and to a lesser degree by inhibiting cytokine synthesis.

http://www.ncbi.nlm.nih.gov/pubmed/9729054

 

 

 

Clin Ther. 1997 Jul-Aug;19(4):701-9.

Mometasone furoate 0.1%-salicylic acid 5% ointment twice daily versus fluocinonide 0.05% ointment twice daily in the management of patients with psoriasis.

Medansky RSCuffie CATanner DJ.

Source

Schering-Plough Research Institute, Kenilworth, New Jersey, USA.

Abstract

This study compared the clinical efficacy and safety of the combination agent mometasone furoate 0.1%-salicylic acid 5% ointment with those of the single agent fluocinonide 0.05% ointment, each applied twice daily for 21 days, in the treatment of patients with moderate to severe plaque psoriasis. Forty adult patients were included in this single-center, randomized, double-masked, intraindividual, bilateral-paired comparative trial. Two similar, bilaterally symmetrical target lesions on the trunk, arms, or legs of each patient were selected for treatment and evaluation. One lesion was treated with mometasone furoate 0.1%-salicylic acid 5% ointment, and the other was treated with fluocinonide 0.05% ointment, both twice daily for 21 days. Treatment was randomly assigned to the right or left side of the body. Signs of psoriasis (ie, erythema, induration, and scaling) and overall clinical response were evaluated and scored on days 4, 8, 15, and 22 and compared against baseline. Patients were asked to evaluate the treatments for efficacy and acceptability at each visit. The primary efficacy parameter was the mean percentage of improvement in total sign scores for the target lesions. Safety was evaluated based on clinical observation and patients' reports. Beginning with day 15, statistically significant differences favoringmometasone furoate 0.1%-salicylic acid 5% ointment over fluocinonide 0.05% ointment were seen in individual and total sign scores, as well as in overall global clinical response. On day 15, 20 patients expressed a preference for one treatment over the other, and 20 patients made no distinction between the two. Of those who expressed a preference, significantly more patients believed mometasone furoate 0.1%-salicylic acid 5% ointment to be better than fluocinonide 0.05% ointment. On day 22, of 25 patients who expressed a preference, significantly more patients thought mometasone furoate 0.1%-salicylic acid 5% ointment was better than fluocinonide 0.05% ointment. No adverse events were recorded for either treatment group. The combination mometasone furoate 0.1%-salicylic acid 5% ointment was significantly more efficacious than and equally as safe as fluocinonide 0.05% ointment in the management of patients with plaque psoriasis and was preferred by a greater number of patients.

http://www.ncbi.nlm.nih.gov/pubmed/9377614

 

 

Australas J Dermatol. 1991;32(2):85-91.

Safety and efficacy of mometasone furoate cream in the treatment of steroid responsive dermatoses.

Kelly JWCains GDRallings MGilmore SJ.

Source

Alfred Hospital, Melbourne.

Abstract

The safety and efficacy of once daily application of mometasone furoate cream 0.1% was determined by comparison with twice daily applications of betamethasone dipropionate cream 0.05% in a single blind, dual centre, randomized study in patients with a variety of steroid-responsive inflammatory dermatoses, the most common of which was psoriasis. Morning plasma cortisol levels revealed little adrenal suppression in either of the two study groups and there was no significant difference between the two groups. Routine laboratory investigations showed no trends in values outside the normal ranges that were of clinical significance. Less skin atrophy was seen in the group treated with mometasone furoate. In comparison to the betamethasone dipropionate treated group, those treated with mometasone furoate exhibited only slight evidence of skin atrophy, and this was not observed before four to twelve weeks of treatment. Eighteen percent of patients using mometasone reported adverse reactions but all were of limited duration and did not persist despite continued application of the drug. Nine percent of patients using betamethasone dipropionate reported adverse effects. Both drugs were found to be highly effective with no significant difference between the two groups at the termination of the treatment period. Of importance is the fact that whilst mometasone furoate is found to be a highly effective treatment for a variety of steroid-responsive dermatoses, this drug has only a limited potential for production of local and systemic side effects. Thus, a high margin of safety can be expected for patients using this drug.

http://www.ncbi.nlm.nih.gov/pubmed/1781761

 

Clinical dermatology

Thomas P. Habif

MANAGEMENT.

When a patient does not respond as predicted or becomes worse while using topical corticosteroids, all topical treatment should be stopped. If corticosteroid therapy is absolutely necessary, one of the corticosteroids with a low sensitizing potential (e.g., mometasone furoate [Elocon], fluticasone propionate [Cutivate], betamethasone esters) could be used, and then only in an ointment base to avoid other allergens.

Thomas P. Habif, MD Adjunct Professor of Medicine (Dermatology), Dartmouth Medical School, Hanover, NH, USA Copyright © 2010

 

 

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