ACTUALIZACION SOBRE EL OLMESARTAN MEDOXOMIL




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ACTUALIZACION SOBRE EL OLMESARTAN MEDOXOMIL

(especial para SIIC © Derechos reservados)
El olmesartán medoxomil es un bloqueante específico del receptor AT 1 de acción prolongada con excelentes efectos para el descenso de la presión arterial, solo y especialmente en combinación con un diurético.
chrysant9.jpg Autor:
Steven G Chrysant
Columnista Experto de SIIC

Institución:
Oklahoma Cardiovascular and Hypertension Center - University of Oklahoma School of Medicine


Artículos publicados por Steven G Chrysant
Recepción del artículo
10 de Marzo, 2006
Aprobación
20 de Marzo, 2006
Primera edición
6 de Octubre, 2006
Segunda edición, ampliada y corregida
7 de Junio, 2021

Resumen
El olmesartán medoxomil es un bloqueante del receptor de la angiotensina II (BRA) que ha sido aprobado por la US Food and Drug Administration (FDA) para el tratamiento de la hipertensión. Es una prodroga que se absorbe rápidamente y es hidrolizada completamente en el tracto gastrointestinal a su metabolito activo, olmesartán (RNH-6270). El olmesartán es muy selectivo para el receptor tipo 1 (AT1) de la angitensina II, al cual se une completamente y de forma irreversible. Tiene muy poca afinidad, si es que tiene alguna, por los otros subtipos de receptores AT2 y AT4. Luego de la administración oral, en animales o humanos, la concentración máxima de la droga en sangre se alcanza dentro de un tiempo máximo de dos horas, aproximadamente. Luego es eliminado lentamente a través de la orina y materia fecal. Su vida media es de 13 horas aproximadamente, lo que lo hace adecuado para la administración en una sola toma diaria. El olmesartán medoxomil administrado por vía oral en una dosis diaria única de 20 a 40 mg demostró un significativo descenso de la presión arterial (PA) en pacientes hipertensos. En estudios clínicos con un diseño correcto, el olmesartán medoxomil presentó una acción antihipertensiva similar a las otras drogas antihipertensivas. Algunos estudios comparativos con otros BRA informaron que el olmesartán medoxomil tiene una acción antihipertensiva superior a las dosis equivalentes de losartán, valsartán, irbesartán y candesartán. Además, su efecto antihipertensivo se potencia considerablemente con la combinación de bajas dosis de diurético. También, al igual que otros BRA, el olmesartán medoxomil demostró un excelente perfil de seguridad.

Palabras clave
Olmesartán medoxomil, BRA, hipertensión, tratamiento, diurético, combinación


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Abstract
Olmesartan medoxomil is an angiotensin II (Ang II) receptor blocker (ARB) that has been approved by the US Food and Drug Administration (FDA) for the treatment of hypertension. It is a prodrug that is rapidly absorbed and completely hydrolyzed in the gastrointestinal tract into its active metabolite, olmesartan (RNH-6270). Olmesartan is highly selective for the Ang II type 1 receptor (AT1) to which it binds completely and insurmountably. It has very little affinity, if any, for the other receptor subtypes AT2 and AT4. After oral administration, in animals and humans, it achieves a maximal blood drug concentration within a maximal time of approximately two hours. It is then slowly eliminated in the urine and feces. His half-life is approximately 13 hours, which makes it suitable for once-daily administration. Olmesartan medoxomil given orally in single daily doses of 20 to 40 mg has demonstrated significant BP lowering effects in hypertensive patients. In well designed clinical trials, olmesartan medoxomil has demonstrated similar antihypertensive actions to the other antihypertensive drugs. Comparative studies with other ARBs have shown that olmesartan medoxomil has superior antihypertensive action to equivalent doses of losartan, valsartan, irbesartan and candesartan. In addition, its antihypertensive effect is greatly enhanced with its combination with a low-dose diuretic. Also, like the other ARBs, olmesartan medoxomil has demonstrated an excellent safety profile.

Key words
Olmesartan medoxomil, ARB, hypertension, treatment, diuretic, combination


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Clasificación en siicsalud
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Especialidades
Principal: Cardiología
Relacionadas: Atención Primaria, Farmacología, Geriatría, Medicina Familiar, Medicina Farmacéutica, Medicina Interna



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Steven G. Chrysant, Oklahoma Cardiovascular and Hypertension Center - University of Oklahoma School of Medicine, OK 73132, 5850 W. Wilshire Blvd., Oklahoma, EE.UU.
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