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MECANISMOS DE ACCION IMPLICADOS EN LOS EFECTOS ANTIDIABETICOS DE LAS TIAZOLIDINEDIONAS

(especial para SIIC © Derechos reservados)
El mecanismo de acción responsable de los efectos antidiabéticos de las tiazolidinedionas radica en la aparente paradoja que existe entre la utilización de fármacos antidiabéticos que favorecen la adipogénesis para el tratamiento de la diabetes tipo 2, cuando el factor de riesgo más importante para el desarrollo de esta patología es la obesidad.
vazquezca9.jpg Autor:
Manuel Vázquez-carrera,
Columnista Experto de SIIC

Institución:
Unidad de Farmacología Facultad de Farmacia Barcelona, España

Artículos publicados por Manuel Vázquez-carrera,
Coautores
Mireia Jové Godino*  Anna Planavila** 
Licenciada en Farmacia, Universidad de Barcelona*
Licenciada en Biología, Universidad de Barcelona**
Recepción del artículo
21 de Abril, 2004 		Aprobación
2 de Septiembre, 2004
Primera edición
27 de Octubre, 2004 		Segunda edición, ampliada y corregida
7 de Junio, 2021

MECANISMOS DE ACCION IMPLICADOS EN LOS EFECTOS ANTIDIABETICOS DE LAS TIAZOLIDINEDIONAS

Resumen
Las tiazolidinedionas (TZD), también llamadas glitazonas, son una nueva clase de fármacos antidiabéticos que han sido introducidos recientemente para el tratamiento de la diabetes mellitus tipo 2. Las TZD fueron la primera clase de compuestos identificados como ligandos de los receptores activados por proliferadores de peroxisomas γ (peroxisome proliferator-activated receptors, PPAR). La participación de los PPARγ en los efectos farmacológicos de las TZD se basó en estudios que demostraron una excelente correlación entre el efecto hipoglucemiante de estos fármacos y su afinidad por PPARγ. Aunque el músculo es responsable de la utilización de hasta un 80% de la glucosa estimulada por la insulina, se considera que el tejido adiposo es el lugar de acción principal de las TZD. Respecto del mecanismo de acción responsable de los efectos antidiabéticos de las TZD, recientes estudios realizados en animales parecen explicar la aparente paradoja que existe entre la utilización de fármacos antidiabéticos que favorecen la adipogénesis para el tratamiento de la diabetes tipo 2, cuando el factor de riesgo más importante para el desarrollo de esta patología es la obesidad. El objetivo de este artículo es revisar los estudios más relevantes realizados para determinar el mecanismo de acción de las TZD antidiabéticas.

Palabras clave
Tiazolidinedionas, diabetes tipo 2, PPARγ, tejido adiposo, músculo esquelético


Artículo completo
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Extensión:  +/-9.12 páginas impresas en papel A4
Exclusivo para suscriptores/assinantes

MECHANISMS OF ACTION INVOLVED IN THE ANTIDIABETIC EFFECTS OF THIAZOLIDINEDIONES

Abstract
Thiazolidinediones (TZD), also called glitazones, are a new class of antidiabetic drugs that have recently been introduced as therapeutic agents for the treatment of type 2 diabetes mellitus. TZD were the first class of compounds to be identified as peroxisome proliferator-activated receptors (PPAR) γ-ligands. The involvement of PPARγ in the pharmacological effects of TZD was supported by studies showing an excellent correlation between the hypoglycemic action of these drugs and their affinity for PPARγ. Despite this evidence, the site of action and the molecular mechanism of TZD remains unclear. Although up to 80% of insulin-stimulated glucose disposal in humans occurs in skeletal muscle, the primary site of action of TZD is thought to be the adipose tissue. Regarding the mechanism of action responsible for the antidiabetic effects of TZD, recent studies performed in animals seem to explain the apparent paradox that lies in using antidiabetic drugs that promote adipogenesis for the treatment of type 2 diabetes, when the major risk factor for the development of this pathology is obesity. The aim of the present article is to review the most relevant studies performed in the search for establishing the mechanism of action of antidiabetic TZD.

Key words
Thiazolidinediones, type 2 diabetes mellitus, PPARγ, adipose tissue, skeletal muscle

Clasificación en siicsalud
Artículos originales > Expertos de Iberoamérica >
página   www.siicsalud.com/des/expertocompleto.php/

Especialidades
Principal: Endocrinología y Metabolismo
Relacionadas: Bioquímica, Farmacología, Inmunología, Medicina Farmacéutica, Nutrición



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Enviar correspondencia a:
Vázquez-Carrera, Manuel
Patrocinio y reconocimiento:
Los estudios realizados en el Departamento de Farmacología y Química Terapéutica fueron subvencionados por la Fundació Privada Catalana de Nutrició i Lípids (FPCNL) y por el Ministerio de Ciencia y Tecnología de España (SAF00-0201, SAF 2003-01232 y BFI02-05167). También agradecemos a la Generalitat de Catalunya la subvención 2001SGR00141. Mireia Jové recibió una beca FPI del Ministerio de Ciencia y Tecnología de España. Anna Planavila cuenta con una beca de la División IV de la Universidad de Barcelona.
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