RESUMO
El pilar principal de tratamiento de las inflamaciones oculares tanto postquirúrgicas como endógenas, se basa en el uso de esteroides. Aunque estos medicamentos son efectivos, su empleo no está exento de riesgos como la hipertensión ocular y la aceleración de la formación de la catarata, principalmente en el caso de los esteroides más fuertes como la prednisolona y la betametasona. Esta revisión estuvo encaminada a la profundización del conocimiento sobre la bioquímica y el desarrollo del difluprednate, nueva droga esteroidea sintética de alta potencia, cuyo uso está aprobado por la Food and Drug Administration FDA para el tratamiento del edema macular después de la cirugía del segmento anterior. Se analizaron algunos aspectos de este medicamento off-label como la farmacocinética, el metabolismo, la distribución ocular del medicamento y utilidad en las fases I, II y III de ensayos clínicos sobre su utilización en pacientes con inflamaciones posoperatorias, tanto del segmento anterior como posterior y con uveítis anterior
The main pillar of the treatment of both the postsurgical and endogenous eye inflammations is based on the use of steroids. Although these drugs are effective, their use has risks such as ocular hypertension and accelerated formation of cataracts, fundamentally in the case of stronger steroids such as prednisolone and betamethasone. This review was aimed at expanding the knowledge on biochemistry and the development of difluprednate, a new highly potent synthetic steroidal drug that has been approved by the Food and Drug Administration FDA to treat macular edema after the anterior segment surgery. Some aspects of this off-label drug were analyzed such as pharmacokinetics, metabolism, ocular distribution of drug and usefulness in phases I, II and II of clinical assays on the use of these drugs in patients with postoperative inflammations both in the anterior and the posterior segments and with anterior uveitis
Assuntos
Humanos , Edema Macular/tratamento farmacológico , Esteroides/farmacocinética , Esteroides/uso terapêutico , Segmento Anterior do Olho/cirurgiaRESUMO
El asma bronquial es una entidad que va en aumento. Basta leer el porcentaje de artículos de Neumología que cubren el tema. Costa Rica no escapa a esta tendencia y en los últimos años han aumentado los artículos nacionales sobre el asma. Sin embargo, un tema poco conocido es el asma resistente a esteroides. Dado que la interacción de los glucocorticoides, con el receptor correspondiente es vital para intentar entender la acción de dichas drogas en asma, y dado que, también lo es, para entender el asma resistente a esteroides, nosotros procedemos a discutir los mecanismos bioquímicos e inmunológicos de dicha unión y los eventos fisiopatológicos que son necesarios para comprender la entidad. Por razones de objetivos y de espacio solo se discuten marginalmente los medicamentos que se están utilizando en esta forma compleja del asma
Assuntos
Humanos , Asma/complicações , Asma/tratamento farmacológico , Asma/terapia , Esteroides/administração & dosagem , Esteroides/uso terapêutico , Esteroides/farmacocinética , Costa RicaRESUMO
Se hace una revisión sobre los esteroides, invitando al médico general a olvidar el mito de que los esteroides son "veneno" y que solo son de uso privativo de los especialistas. La mayoría de errores que se comenten en la práctica diaria son por la ignorancia sobre el manejo de estos medicamentos que a través de la historia siguen demostrando ser armas importantísimas en el manejo de muchas patologías sobre todo en aquellas que son de origen "autoinmune".
Assuntos
Esteroides/química , Esteroides/farmacocinética , Esteroides/farmacologia , Esteroides/uso terapêuticoRESUMO
The use of fecal steroid analysis to assess gonadal and adrenal function in primates has rapidly increased in recent years due to the ability to collect feces from nonhuman primates living in wild conditions. These techniques offer an exciting new potential for enhancing our knowledge of the endocrine status of free-living animals. Prior to using these techniques under field conditions, it is important to determine the diurnal variation of fecal excreted steroids for assessing possible time limitations on fecal collections. The following study investigates the diurnal frequency of defecation and patterns of steroid levels excreted in feces from four female common marmosets, Callithrix jacchus, living in a family group. These females represented three reproductive conditions: early pregnancy, ovarian cycling, and noncycling (postpubertal). Cortisol, estradiol, and progesterone were extracted and analyzed by enzyme immunoassay. Diurnal variations in steroid levels were found by ANOVA for cortisol and progesterone but not for estradiol. Significantly higher levels of cortisol were found in the afternoon, while the reverse was found for progesterone. All females showed the same pattern of steroid level change, except for cortisol in the pregnant female. Since all females defecated within the first hour after they awoke in the morning, this time was determined to be the most effective time to collect feces. The consistency of our findings reinforces the usefulness of this approach for studying reproductive and adrenocortical function in marmosets and also indicates that fecal collection should be limited to either morning or afternoon collections.
Assuntos
Callithrix/fisiologia , Prenhez/fisiologia , Esteroides/farmacocinética , Córtex Suprarrenal/fisiologia , Animais , Ritmo Circadiano , Fezes/química , Feminino , GravidezRESUMO
Con la introducción de los esteroides para su uso tópico en la década de los cincuenta, el tratamiento de una gran variedad de enfermedades inflamatorias de la piel cambió radicalmente. Desde entonces se han desarrollado diversos esteroides en un intento por aumentar la potencia y disminuir los efectos colaterales de los mismos. Sus efectos se basan en actividades antiinflamatorias-inmunosupresoras, antiproliferativas y vasoconstrictoras, secundarias a la unión del esteroide y su receptor con el DNA. Para ejercer sus efectos, el esteroide debe dejar el vehículo aplicado y difundir en la piel y a través de los tejidos hacia la circulación sistémica. Su absorción depende del vehículo, la técnica de aplicación y el sitio anatómico en el que utilice. Actualmente se ha definido las dermatosis que tienen buena, moderada o pobre respuesta al uso de esteroides y existen algunas indicaciones precisas para su administración. Sin embargo, el uso de esteroides se puede acompañar de efectos secundarios bien identificados, que se minimizan cuando se administran en las dermatosis en las que su utilidad está bien definida, y se siguen las guías adecuadas para su uso
Assuntos
Mecanismo de Ação do Medicamento Homeopático , Dermatologia , Vias de Administração de Medicamentos , Esteroides , Esteroides/efeitos adversos , Esteroides/farmacocinética , Esteroides/uso terapêuticoRESUMO
Los lazaroides constituyen una serie de nuevos compuestos esteroides carentes de actividad Glucocorticoide, que han sido desarrollados para el tratamiento agudo de las lesiones traumáticas o isquemicas del Sistema nervioso Central (SNC) los cuales tienen un poder cerebroprotector superior al de los compuestos glucocorticoides que actualmente se conocen. Son capaces de inhibir las relaciones de lipoperoxidación de las membranas que se generan posterior a la lesión del SNC En esta revisión se analizan su mecanismo de acción, así como su utilidad en los procesos inflamatorios, traumáticos, infecciosos y degenerativos del SNC, igualmente se analiza su beneficio en la preservación de organos a ser transplantados y la conservación de la sangre y sus derivados
Assuntos
Antioxidantes/terapia , Isquemia Encefálica/terapia , Esteroides/administração & dosagem , Esteroides/farmacocinética , Esteroides/uso terapêuticoRESUMO
The effect of progesterone and six other C21-deoxysteroids on renal sodium retention by male adrenalectomized rats was compared with the effect exerted by the natural corticoids aldosterone, 11-deoxycorticosterone, and corticosterone. Steroids were active in the following order: aldosterone > 11,19-oxidoprogesterone > 5 alpha H-3,20-pregnanedione > or = 5 beta H-3,20-pregnanedione > progesterone = 11-ketoprogesterone > 6,19-oxidoprogesterone = 11-keto-6,19-oxidoprogesterone > or = corticosterone. All C21-deoxysteroids, except 11,19-oxidoprogesterone, exhibited parabolic log dose-response functions, indicating an effect that opposes renal sodium retention at high doses. 11,19-Oxidoprogesterone and the natural corticoids exhibited normal, exponential, log dose-response curves. Diverse geometric parameters related to molecular planarity were calculated and their correlation with biopharmacological properties was attempted. The best linear regression was obtained for correlation of the concavity of log dose-response parabolas (second-order coefficients) of C21-deoxysteroids with the C3 = O/ring D angle of these molecules. A good linear regression could also be obtained for correlation of the affinity of C21-deoxysteroids, except 11,19-oxidoprogesterone, for purified type I mineralocorticoid receptors with those angles. The latter correlation deteriorated upon incorporation of the affinity data for the three natural corticoids, due to similar affinities of these hormones for type I mineralocorticoid receptors, but could be restored when the binding data for the unpurified, corticosterone-binding globulin-containing stage of the receptors were considered. In vivo binding data followed the same trend as that for unpurified receptors.
Assuntos
Rim/efeitos dos fármacos , Rim/metabolismo , Sódio/metabolismo , Esteroides/farmacologia , Glândulas Suprarrenais/fisiologia , Glândulas Suprarrenais/cirurgia , Adrenalectomia , Aldosterona/metabolismo , Aldosterona/farmacocinética , Aldosterona/farmacologia , Animais , Citosol/metabolismo , Desoxicorticosterona/metabolismo , Desoxicorticosterona/farmacocinética , Desoxicorticosterona/farmacologia , Meia-Vida , Masculino , Conformação Molecular , Potássio/metabolismo , Progesterona/análogos & derivados , Progesterona/metabolismo , Progesterona/farmacocinética , Progesterona/farmacologia , Ratos , Ratos Sprague-Dawley , Receptores de Esteroides/metabolismo , Sódio/farmacocinética , Esteroides/metabolismo , Esteroides/farmacocinética , TrítioAssuntos
Anti-Inflamatórios/administração & dosagem , Corticosteroides , Corticosteroides/administração & dosagem , Corticosteroides/farmacocinética , Corticosteroides/farmacologia , Corticosteroides/uso terapêutico , Dermatologia , Dermatopatias/prevenção & controle , Dermatopatias/terapia , Dermatopatias/tratamento farmacológico , Esteroides , Esteroides/administração & dosagem , Esteroides/farmacocinética , Esteroides/farmacologia , Esteroides/metabolismo , Esteroides/uso terapêutico , FarmacologiaRESUMO
Some details about the function of natural and synthetical hormonas are reviewed, particularly estrogens as ethynyl estradiol and its 3, Methyl ether (mestranol); its peripheral concentration vs tissular hormonal contents, a relationship of biological importance as the first step in its hormonal action and the cumulative local effects that could explain some intra and extracellular phenomena.
Assuntos
Congêneres do Estradiol/farmacocinética , Adulto , Endométrio/metabolismo , Congêneres do Estradiol/metabolismo , Etinilestradiol/farmacocinética , Feminino , Humanos , Histerectomia , Esteroides/farmacocinética , Distribuição TecidualRESUMO
The ability of adrenal corticosteroids to both suppress inflammation and compromise host defenses has been well documented. Recenthy, a series of in vitro and in vivo experiments, based on our new knowledge of the cell biology of inflammation and biochemestry of the pagocytic cell itself, has provided new insights into the mechanism of steroid action in the inflammatory process. Evidence is presented thst pharmacologic doses of steroids arecapable of inhibiting each of the steps in phagocyte-micro-organism interaction: chemotaxi, recognition and opsonization, phagocytosis, membrane fusion, and degranulation. In addition, steroid alteration of posphagocytic superoxide production, hydrogen peroxide generation, and prostaglandin and thromboxane synthesis is described. Yhe anti-inflammatory effects of aspirin andindomethacin can be explained almost entirely by virtue of their ability to inhibit cyclo-oxygenase, this preventing the transformation of arachidonic acid to both prostaglandins and thromboxanes. The cortisol-induced inhibition of endoperoxides, prostaglandins, and thromboxanes (at a site proximal to the release of arachidonic acid) may well explain those anti-inflammatory actions that cortisone shares with aspirin. However, patients treated with nonsteroidalanti-inflammatory agents effectively combat infections. In contrast, corticosteroids have more profound effects, as can be seen by the inhibition of superxide production, with the subsequent decrease in hydrogen peroxide generation and the diminution in release of the antibacterial lysosomal bydrolases within the phagocyte vacuole, Thus, corticosteroids interfere with the killing of micro-organisms. This new understanding of the pharmacologic action of cortisol on phagecytic cells explains, we believe, how glucocorticoids alleviate inflammation while, at the same time, they permit multiplication of the offending micro-organism within the phagocyte.