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    Está indicado para: – Tratamiento de cáncer de mama. – Reducción en la incidencia de cáncer de mama en mujeres con alto riesgo. Las mujeres con alto riesgo son aquellas con al menos 35 años de edad y con riesgo mayor o igual a 1.67% (calculado con el modelo de Gail) de desarrollar cáncer de mama en los siguientes cinco años. Después de la administración oral, tamoxifeno se absorbe rápidamente, obteniéndose concentraciones séricas máximas dentro de las primeras 4-7 horas. Después de cuatro semanas de tratamiento con 40 mg/día, se consiguen concentraciones de estado estable (alrededor de 300 ng/m L). El fármaco se une fuertemente a las proteínas como la albúmina sérica ( 99%). Se metaboliza por hidroxilación, desmetilación y conjugación, generando varios metabolitos que poseen un perfil farmacológico similar al compuesto original, contribuyendo así al efecto terapéutico. Se excreta principalmente por las heces y una vida media de eliminación de aproximadamente siete días fue calculada para el propio medicamento, mientras que para su principal metabolito circulante, el N-desmetiltamoxifeno, es de 14 días. En un estudio clínico donde niñas cuyas edades oscilaban entre 2 y 10 años, con síndrome Mc Cune Albright (SMA), que recibieron 20 mg de tamoxifeno una vez al día durante 12 meses, presentaron una disminución en la eliminación dependiente de la edad así como un incremento en la exposición (AUC), (con valores hasta 50% más altos en los pacientes más jóvenes) en comparación con los adultos. Tamoxifen is a popular and powerfully effective Selective Estrogen Receptor Modulator (SERM) that is often referred to as an anti-estrogen. However, while being an antagonist it is also an agonist as it will actually act as estrogen in certain parts of the body while acting as an anti-estrogen in other areas. As one of the oldest SERM’s on the market that is still regularly used medicinally. Tamoxifen, officially known as Tamoxifen Citrate, was first developed in 1961 by ICI now Astra Zeneca under the trade name Nolvadex. The SERM was developed to treat breast cancer, specifically hormone-responsive breast cancer. However, it has also been effectively used in breast cancer prevention. Then we have anabolic steroid users, and it was long ago discovered that Tamoxifen had a place among such individuals.

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