Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. They are metabolised, primarily in the liver.
Absorption is dependent on many drug-related factors including: intrinsic properties of the steroid itself; concentration of the drug (increased concentration generally leads to more drug being absorbed but may plateau at higher concentrations); vehicle used (optimized or augmented vehicles > ointments or gels > creams or lotions); duration of exposure; frequency of application; combination with other products that break down the skin barrier and increase absorption (e.g., salicylic acid, urea). Patient-related factors that influence absorption include: patient age (infants and children absorb topical medications more quickly and to a greater degree than adults, and have a greater total skin surface to body weight ratio; the elderly have thinner skin and absorb drug more readily); disruption of the skin due to inflammation or disease (e.g., absorption increased in atopic dermatitis); total skin area treated; skin site treated (absorption is much greater from thin-skinned areas such as scalp, face, eyelid, axilla, and scrotum than from areas with thicker skin such as forearm, knee, elbow, palm and sole); absorption is increased with increased temperature or humidity of the skin or the environment; occlusion of the treated skin (via plastic wrap, oily vehicles, dressings, tape, diapers, tight-fitting clothing, etc.) can increase absorption up to 10-fold.
来源:DrugBank
吸收、分配和排泄
消除途径
克洛贝松及其代谢物通过尿液排出。
Clobetasone and its metabolites are excreted in urine.
来源:DrugBank
吸收、分配和排泄
分布容积
由于循环水平远低于检测水平，因此需要使用药效学终点来评估外用皮质类固醇的系统暴露。
The use of pharmacodynamic endpoints for assessing the systemic exposure of topical corticosteroids is necessary due to the fact that circulating levels are well below the level of detection.
[EN] COMPOUNDS USEFUL AS CSF1 MODULATORS<br/>[FR] COMPOSÉS UTILES EN TANT QUE MODULATEURS DU FACTEUR 1 DE STIMULATION DE COLONIES
申请人：REDX PHARMA PLC
公开号：WO2016051193A1
公开（公告）日：2016-04-07
This invention relates to novel compounds and to pharmaceutical compositions comprising the novel compounds. More specifically, the invention relates to compounds useful as Colony Stimulating Factor 1 Receptor (cFMS) modulators (e.g. cFMS inhibitors). This invention also relates to processes for preparing the compounds, uses of the compounds in treatment and methods of treatment employing the compounds. Specifically, the invention relates to the use of the compounds for the treatment of cancer and autoimmune diseases.
Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
[EN] BORON-CONTAINING RHO KINASE INHIBITORS<br/>[FR] INHIBITEURS DE LA RHO KINASE CONTENANT DU BORE
申请人：PERCIPIAD INC
公开号：WO2021011873A1
公开（公告）日：2021-01-21
The present invention provides boron-containing isoquinoline compounds as protein kinase-modulating compounds. These compounds are useful as neuroprotective and neuro-regenerative agents for the amelioration of glaucoma and other ocular neuropathies.
[EN] ISOTHIAZOLOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS<br/>[FR] ANTI-INFECTIEUX A BASE D'ISOTHIAZOLOQUINOLONES ET DE SELS CORRESPONDANTS
申请人：ACHILLION PHARMACEUTICALS INC
公开号：WO2005019228A1
公开（公告）日：2005-03-03
The invention provides compounds and salts of Formula (I) and Formula (II): which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula (I) and Formula (II). The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula (I) and Formula (II) disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula (I) or Formula (II) and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula (I) or Formula (II) as the only active agent or may contain a combination of a compound of Formula (I) or Formula (II) and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
Described herein is the FLAP inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin-3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, including solvates, and polymorphs thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.
