Antiestrógenos

Clasificación

Se deben considerar varias clases principales de antiestrógenos. Los LOS Neisseria medicamentos prototípicos de cada clase se indican con un asterisco (*).

• Moduladores selectivos de los LOS Neisseria receptores de estrógeno (SERM, por sus siglas en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum inglés):
  • Actividad antagonista (i.e., antiestrogénica) en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum algunos tejidos y actividad agonista (i.e., estrogénica) en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum otros tejidos
  • Agentes:
    • Tamoxifeno*
    • Raloxifeno
    • Ospemifeno
    • Bazedoxifeno
    • Citrato de clomifeno
• Reguladores descendentes selectivos de los LOS Neisseria receptores de estrógeno (SERD, por sus siglas en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum inglés):
  • También conocidos como antagonistas estrogénicos puros
  • Solo tienen actividad antagonista.
  • Agentes:
    • Fulvestrant Fulvestrant An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. Antiestrogens* (el único compuesto aprobado por la FDA)
    • Actualmente, se están desarrollando y/o experimentando ensayos clínicos con varios compuestos adicionales.
• Inhibidores de la aromatasa:
  • Anastrozol*
  • Letrozol
  • Exemestano
• Otros:
  • Análogos de la hormona liberadora de gonadotropina (GnRH):
    • Leuprolida
    • Ganirelix Ganirelix Antiestrogens
    • Elagolix Elagolix Antiestrogens
  • Andrógenos: danazol Danazol A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders. Antiestrogens
  • Progestágenos

Moduladores Selectivos de los Receptores de Estrógeno y Reguladores Descendentes Selectivos de los Receptores de Estrógeno

Mecanismo de acción de los LOS Neisseria SERM

Tamoxifeno, raloxifeno, ospemifeno, bazedoxifeno y citrato de clomifeno:

• Se unen competitivamente a los LOS Neisseria receptores de estrógeno (ER, por sus siglas en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum inglés)
• Tanto la actividad agonista como la antagonista dependen del tejido diana:
  • Actividad antiestrogénica en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum la mama
  • Tienden a tener actividad estrogénica (i.e., agonista) en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum:
    • Útero
    • Huesos
    • Hígado
• Receptores de estrógeno:
  • Situados en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum el núcleo ( en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum lugar de la membrana celular)
  • Actúan como factores de transcripción dependientes de ligandos (cuando el estrógeno es el ligando requerido para la unión al AL Amyloidosis ADN).
  • Cuando el estrógeno se une al AL Amyloidosis ER, el complejo ER-estrógeno se une a los LOS Neisseria elementos de respuesta al AL Amyloidosis estrógeno (ERE) en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum la región promotora de los LOS Neisseria genes Genes A category of nucleic acid sequences that function as units of heredity and which code for the basic instructions for the development, reproduction, and maintenance of organisms. DNA Types and Structure diana.
  • La unión al AL Amyloidosis ERE puede activar o reprimir la expresión del gen específico.
• No se comprende completamente cómo los LOS Neisseria efectos de los LOS Neisseria SERM difieren entre los LOS Neisseria tejidos.
• Teoría: El complejo SERM-ER interactúa con los LOS Neisseria diferentes cofactores presentes en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum los LOS Neisseria diferentes tejidos.

Mecanismo de acción de los LOS Neisseria SERD

Fulvestrant Fulvestrant An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. Antiestrogens:

• Un antagonista competitivo de alta afinidad que evita que el estrógeno se una al AL Amyloidosis ER
• Similar al AL Amyloidosis ligando de estrógeno endógeno → compite con el estrógeno para unirse al AL Amyloidosis dominio de unión al AL Amyloidosis ligando del ER.
• Actividad antagonista pura del ER sin tener actividad agonista
• Produce un complejo dentro del núcleo celular (sitio donde se encuentra el ER), que provoca la regulación descendente de los LOS Neisseria receptores de estrógeno.
• Efectos dependientes de la dosis (e.g., a dosis más alta de fulvestrant Fulvestrant An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. Antiestrogens → mayor regulación descendente)
• Sin estimulación estrogénica → se inhibe el crecimiento tumoral dependiente de hormonas.

Efectos fisiológicos

Los LOS Neisseria SERM actúan como agonistas estrogénicos en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum algunos tejidos y como antagonistas estrogénicos en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum otros.

Efectos fisiológicos de los LOS Neisseria SERD:

El fulvestrant Fulvestrant An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. Antiestrogens tiene efectos puramente antiestrogénicos en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum los LOS Neisseria tejidos. Los LOS Neisseria efectos fisiológicos clave incluyen:

• ↓ Estimulación estrogénica de la mama
• ↓ BMD
• Supresión del crecimiento endometrial

Farmacocinética

• Absorción:
  • Se absorben rápidamente cuando se administran por vía oral.
  • La mayoría tienen baja biodisponibilidad (< 10%).
• Distribución:
  • Ampliamente distribuidos
  • Altamente unidos a proteínas (principalmente a la albúmina, no a la globulina fijadora de hormonas sexuales)
• Metabolismo:
  • Metabolismo hepático
  • Tamoxifeno: vía CYP2D6 y CYP3A4 CYP3A4 Class 3 Antiarrhythmic Drugs (Potassium Channel Blockers)/CYP3A5 a metabolitos activos más potentes
  • Raloxifeno: Se somete a un extenso metabolismo de primer paso a conjugados de glucurónido.
  • Bazedoxifeno: metabolismo hepático (no a través de la vía de las enzimas CYP)
  • Ospemifeno: vía CYP3A4 CYP3A4 Class 3 Antiarrhythmic Drugs (Potassium Channel Blockers), CYP2C9 CYP2C9 A cytochrome p-450 subtype that has specificity for acidic xenobiotics. It oxidizes a broad range of important clinical drugs that fall under the categories of nonsteroidal anti-inflammatory agents; hypoglycemic agents; anticoagulants; and diuretics. Anticoagulants y CYP2C19
  • Fulvestrant Fulvestrant An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. Antiestrogens: vía CYP3A4 CYP3A4 Class 3 Antiarrhythmic Drugs (Potassium Channel Blockers) a metabolitos activos
• Excreción:
  • Principalmente fecal
  • Vida media: generalmente larga:
    • Tamoxifeno: 5–7 días
    • Raloxifeno y bazedoxifeno: aproximadamente 30 horas
    • Fulvestrant Fulvestrant An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. Antiestrogens: aproximadamente 40 días

Indicaciones

Las indicaciones principales de cada medicamento se indican con un asterisco (*):

• Cáncer de mama y otros problemas de mama:
  • Agentes:
    • Tamoxifeno*
    • Raloxifeno
    • Fulvestrant Fulvestrant An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. Antiestrogens*
  • Tratamiento adyuvante en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum el cáncer de mama
  • Carcinoma ductal in situ ( DCIS DCIS Proliferation of cytologically malignant cells within the mammary ductal system, with no invasion of the surrounding stroma Breast Cancer, por sus siglas en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum inglés)
  • Reducción del riesgo profiláctico en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum individuos de alto riesgo
  • Ginecomastia (crecimiento de los LOS Neisseria senos en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum los LOS Neisseria hombres)
  • Mastalgia severa ( dolor Dolor Inflammation en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum los LOS Neisseria senos)
• Prevención y tratamiento de la osteoporosis Osteoporosis Osteoporosis refers to a decrease in bone mass and density leading to an increased number of fractures. There are 2 forms of osteoporosis: primary, which is commonly postmenopausal or senile; and secondary, which is a manifestation of immobilization, underlying medical disorders, or long-term use of certain medications. Osteoporosis posmenopáusica:
  • Raloxifeno*
  • Bazedoxifeno*
• Otros síntomas de la menopausia :
  • Bazedoxifeno: síntomas vasomotores* (e.g., sofocos, sudoraciones nocturnas)
  • Ospemifeno: sequedad vaginal*
• Esterilidad:
  • Clomifeno: para la inducción de la ovulación*
  • Tamoxifeno:
    • Para la inducción de la ovulación en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum pacientes con cáncer de mama
    • Para la infertilidad por factores masculinos idiopáticos
• Pubertad precoz (e.g., síndrome de McCune-Albright):
  • Tratamiento de 1.ra línea: inhibidores de la aromatasa
  • Agentes de 2.da línea:
    • Tamoxifeno
    • Fulvestrant Fulvestrant An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. Antiestrogens

Efectos secundarios

• Sofocos (común con todos los LOS Neisseria SERM y los LOS Neisseria SERD)
• Tromboembolismo venoso ( VTE VTE Obstruction of a vein or veins (embolism) by a blood clot (thrombus) in the bloodstream. Hypercoagulable States, por sus siglas en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum inglés) (una preocupación con todos los LOS Neisseria agentes):
  • Trombosis venosa profunda
  • Embolia pulmonar
• Tumores y lesiones uterinas (tamoxifeno, ospemifeno, clomifeno):
  • Carcinoma endometrial
  • Carcinoma uterino (sarcoma)
  • Pólipos endometriales
  • Hiperplasia endometrial
  • Fibromas uterinos
• Efectos oculares (tamoxifeno)
• Otros efectos secundarios comunes (todos los LOS Neisseria agentes):
  • Edema Edema Edema is a condition in which excess serous fluid accumulates in the body cavity or interstitial space of connective tissues. Edema is a symptom observed in several medical conditions. It can be categorized into 2 types, namely, peripheral (in the extremities) and internal (in an organ or body cavity). Edema
  • Mareo
  • Malestar gastrointestinal
  • Espasmos musculares
  • Artralgias/ dolor Dolor Inflammation de huesos

Contraindicaciones

• Hipersensibilidad
• Antecedentes o VTE VTE Obstruction of a vein or veins (embolism) by a blood clot (thrombus) in the bloodstream. Hypercoagulable States actual
• Embarazo
• Sangrado vaginal inexplicable
• Terapia concomitante con warfarina (tamoxifeno)
• Utilice con precaución en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum pacientes con insuficiencia hepática.

Inhibidores de la Aromatasa

Descripción general

Los LOS Neisseria inhibidores de la aromatasa evitan la conversión de testosterona en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum estrógeno, el cual es un proceso conocido como aromatización. Los LOS Neisseria medicamentos de esta clase incluyen anastrozol, letrozol y exemestano. Los LOS Neisseria medicamentos se utilizan más comúnmente en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum el tratamiento del cáncer de mama posmenopáusico.

Mecanismo de acción

• Los LOS Neisseria inhibidores de la aromatasa inhiben la acción de la aromatasa:
  • Anastrozol y letrozol: Se unen reversiblemente a la aromatasa.
  • Exemestano: Se une irreversiblemente a la aromatasa.
• Conducen a una ↓ en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum los LOS Neisseria niveles de estrógeno en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum mujeres posmenopáusicas:
  • El estrógeno estimula el crecimiento tumoral en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum muchos cánceres de mama.
  • El efecto general de los LOS Neisseria inhibidores de la aromatasa:
    • Disminuye la masa tumoral.
    • Retrasa la progresión en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum tumores sensibles a las hormonas.
• Aromatasa:
  • La enzima clave requerida en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum la síntesis de estrógeno
  • Convierte los LOS Neisseria andrógenos en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum estrógenos:
    • Bloqueo de la testosterona → estradiol Estradiol The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. Noncontraceptive Estrogen and Progestins
    • Bloqueo de la androstenediona → estrona
  • Ubicada dentro de:
    • Células de la granulosa en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum los LOS Neisseria ovarios (sitio principal de producción de estrógenos en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum las mujeres premenopáusicas)
    • Mamas
    • Tejido adiposo
    • Glándulas suprarrenales
    • Cerebro
    • Hueso
• ¿Por qué se usan los LOS Neisseria inhibidores de la aromatasa en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum mujeres posmenopáusicas?:
  • Antes de la menopausia, el eje hipotálamo-hipófisis-ovario (HPO, por sus siglas en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum inglés) es funcional y responde correctamente.
  • Inhibición de la producción de estrógeno gonadal → ↓ estrógeno circulante → menor inhibición de:
    • GnRH
    • Hormona folículoestimulante ( FSH FSH A major gonadotropin secreted by the adenohypophysis. Follicle-stimulating hormone stimulates gametogenesis and the supporting cells such as the ovarian granulosa cells, the testicular sertoli cells, and leydig cells. Fsh consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle)
    • Hormona luteinizante ( LH LH A major gonadotropin secreted by the adenohypophysis. Luteinizing hormone regulates steroid production by the interstitial cells of the testis and the ovary. The preovulatory luteinizing hormone surge in females induces ovulation, and subsequent luteinization of the follicle. Luteinizing hormone consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle)
  • Menor inhibición de GnRH, FSH FSH A major gonadotropin secreted by the adenohypophysis. Follicle-stimulating hormone stimulates gametogenesis and the supporting cells such as the ovarian granulosa cells, the testicular sertoli cells, and leydig cells. Fsh consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle y LH LH A major gonadotropin secreted by the adenohypophysis. Luteinizing hormone regulates steroid production by the interstitial cells of the testis and the ovary. The preovulatory luteinizing hormone surge in females induces ovulation, and subsequent luteinization of the follicle. Luteinizing hormone consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle → ↑ GnRH, FSH FSH A major gonadotropin secreted by the adenohypophysis. Follicle-stimulating hormone stimulates gametogenesis and the supporting cells such as the ovarian granulosa cells, the testicular sertoli cells, and leydig cells. Fsh consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle y LH LH A major gonadotropin secreted by the adenohypophysis. Luteinizing hormone regulates steroid production by the interstitial cells of the testis and the ovary. The preovulatory luteinizing hormone surge in females induces ovulation, and subsequent luteinization of the follicle. Luteinizing hormone consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle → estimulan a los LOS Neisseria ovarios para ↑ la producción de andrógenos.
  • El eje HPO se «apaga» en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum la menopausia con el cese de la función ovárica.
  • Los LOS Neisseria sitios extragonadales continúan produciendo estrógeno capaz de estimular el cáncer de mama en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum mujeres posmenopáusicas → los LOS Neisseria inhibidores de la aromatasa inhiben la producción de estrógeno.

Farmacocinética

Anastrozol, letrozol:

• Absorción (ambos):
  • Buena absorción por vía oral
  • Absorción rápida
  • El grado de absorción no se ve VE Ventilation: Mechanics of Breathing afectado por los LOS Neisseria alimentos.
• Unión a proteínas (ambos): débil a moderada
• Metabolismo:
  • Metabolismo hepático a metabolitos inactivos
  • Anastrozol: a través de la desalquilación N, hidroxilación y glucuronidación
  • Letrozol: vía CYP3A4 CYP3A4 Class 3 Antiarrhythmic Drugs (Potassium Channel Blockers) y CYP2A6
• Excreción (ambos):
  • Principalmente fecal (10% orina)
  • Vida media: aproximadamente 2 días

Exemestano:

• Absorción:
  • Moderadamente bien absorbido después de la administración oral
  • ↑ Posprandial
• Distribución:
  • Ampliamente distribuido en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum los LOS Neisseria tejidos
  • El 90% se une a proteínas (principalmente a la albúmina y a la glucoproteína ácida 𝛂₁).
• Metabolismo:
  • Metabolismo hepático extenso a metabolitos inactivos
  • A través de la oxidación y reducción del CYP3A4 CYP3A4 Class 3 Antiarrhythmic Drugs (Potassium Channel Blockers) del grupo 17-ceto
• Excreción:
  • Dividido aproximadamente entre la orina (principalmente como metabolitos) y las heces
  • Vida media: aproximadamente 24 horas

Indicaciones

• Cáncer de mama avanzado en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum mujeres posmenopáusicas
• Reducción del riesgo de cáncer de mama en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum mujeres posmenopáusicas
• Uso fuera de indicación en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum cánceres recurrentes de ovario y útero
• Indicaciones adicionales para el letrozol:
  • Infertilidad: agente de 1.ra línea para la inducción de la ovulación en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum mujeres anovulatorias con síndrome de ovario poliquístico (SOP)
  • Pubertad precoz periférica (e.g., síndrome de McCune-Albright)

Efectos secundarios

• Sofocamientos
• Disfunción sexual (típicamente debido a la vaginitis atrófica)
• Osteoporosis Osteoporosis Osteoporosis refers to a decrease in bone mass and density leading to an increased number of fractures. There are 2 forms of osteoporosis: primary, which is commonly postmenopausal or senile; and secondary, which is a manifestation of immobilization, underlying medical disorders, or long-term use of certain medications. Osteoporosis/ osteopenia Osteopenia Osteoporosis: ↓ BMD y ↑ riesgo de fracturas
• Efectos músculo-esqueléticos:
  • Artralgia/ dolor Dolor Inflammation de huesos
  • Rigidez articular
  • Mialgias
  • Síndrome del túnel carpiano
• Edema Edema Edema is a condition in which excess serous fluid accumulates in the body cavity or interstitial space of connective tissues. Edema is a symptom observed in several medical conditions. It can be categorized into 2 types, namely, peripheral (in the extremities) and internal (in an organ or body cavity). Edema periférico
• Malestar gastrointestinal:
  • Náuseas/vómitos
  • Diarrea/estreñimiento
  • Dolor Dolor Inflammation abdominal
• Aumento de peso
• Hipercolesterolemia
• Eventos cardiovasculares isquémicos ( los LOS Neisseria estudios son mixtos):
  • Probable ↑ riesgo en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum personas con enfermedades cardiovasculares preexistentes
  • ↑ Riesgo en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum comparación con el tamoxifeno (probablemente no un gran ↑ riesgo en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum comparación con un placebo Placebo Any dummy medication or treatment. Although placebos originally were medicinal preparations having no specific pharmacological activity against a targeted condition, the concept has been extended to include treatments or procedures, especially those administered to control groups in clinical trials in order to provide baseline measurements for the experimental protocol. Epidemiological Studies)
  • Los LOS Neisseria eventos pueden incluir:
    • Angina de pecho
    • Infarto agudo del miocardio
    • Accidente cerebrovascular isquémico

Contraindicaciones

• Hipersensibilidad
• Embarazo
• Lactancia
• Estado premenopáusico para su uso en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum el tratamiento del cáncer de mama

Análogos de la Hormona Liberadora de Gonadotropina

Descripción general

• La GnRH es un componente clave del eje HPO:
  • El hipotálamo libera GnRH.
  • La GnRH estimula la liberación de FSH FSH A major gonadotropin secreted by the adenohypophysis. Follicle-stimulating hormone stimulates gametogenesis and the supporting cells such as the ovarian granulosa cells, the testicular sertoli cells, and leydig cells. Fsh consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle y LH LH A major gonadotropin secreted by the adenohypophysis. Luteinizing hormone regulates steroid production by the interstitial cells of the testis and the ovary. The preovulatory luteinizing hormone surge in females induces ovulation, and subsequent luteinization of the follicle. Luteinizing hormone consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle de la hipófisis anterior.
  • La FSH FSH A major gonadotropin secreted by the adenohypophysis. Follicle-stimulating hormone stimulates gametogenesis and the supporting cells such as the ovarian granulosa cells, the testicular sertoli cells, and leydig cells. Fsh consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle y LH LH A major gonadotropin secreted by the adenohypophysis. Luteinizing hormone regulates steroid production by the interstitial cells of the testis and the ovary. The preovulatory luteinizing hormone surge in females induces ovulation, and subsequent luteinization of the follicle. Luteinizing hormone consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle estimulan el ovario, que produce estrógeno y progesterona.
• La GnRH se libera de forma pulsátil desde el hipotálamo.
• Los LOS Neisseria análogos de GnRH se unen a los LOS Neisseria receptores de GnRH en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum la hipófisis.
• Tanto los LOS Neisseria agonistas como los LOS Neisseria antagonistas suprimen la liberación de FSH FSH A major gonadotropin secreted by the adenohypophysis. Follicle-stimulating hormone stimulates gametogenesis and the supporting cells such as the ovarian granulosa cells, the testicular sertoli cells, and leydig cells. Fsh consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle y LH LH A major gonadotropin secreted by the adenohypophysis. Luteinizing hormone regulates steroid production by the interstitial cells of the testis and the ovary. The preovulatory luteinizing hormone surge in females induces ovulation, and subsequent luteinization of the follicle. Luteinizing hormone consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle, lo que lleva a la supresión de:
  • Desarrollo folicular
  • Ovulación
  • Producción de estrógeno y progesterona
• No deben utilizarse como método anticonceptivo.
• Los LOS Neisseria efectos secundarios son similares a los LOS Neisseria otros antiestrógenos:
  • Sofocamientos
  • Sudoración nocturna
  • Cambios de humor Humor Defense Mechanisms
  • Sequedad vaginal
  • Pérdida ósea (el tratamiento a menudo se limita a < 6 meses)

Agonistas de la GnRH

Leuprolida:

• La exposición continua ( en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum lugar de la exposición pulsátil) a la GnRH suprime la FSH FSH A major gonadotropin secreted by the adenohypophysis. Follicle-stimulating hormone stimulates gametogenesis and the supporting cells such as the ovarian granulosa cells, the testicular sertoli cells, and leydig cells. Fsh consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle y la LH LH A major gonadotropin secreted by the adenohypophysis. Luteinizing hormone regulates steroid production by the interstitial cells of the testis and the ovary. The preovulatory luteinizing hormone surge in females induces ovulation, and subsequent luteinization of the follicle. Luteinizing hormone consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle → ↓ desarrollo del folículo → ↓ estrógeno.
• Crea una «menopausia médica» reversible hasta que los LOS Neisseria efectos desaparezcan.
• La supresión toma algunos días → las personas a menudo experimentan «brotes» de síntomas antes de la mejoría.
• Administrada como inyecciones IM cada 1 a 3 meses
• Indicaciones:
  • Pubertad precoz central
  • Tratamiento a corto plazo (< 6 meses) de los LOS Neisseria fibromas uterinos:
    • Reduce el tamaño del fibroma antes de la cirugía.
    • Detiene el sangrado menstrual abundante para dar tiempo a la corrección de la anemia Anemia Anemia is a condition in which individuals have low Hb levels, which can arise from various causes. Anemia is accompanied by a reduced number of RBCs and may manifest with fatigue, shortness of breath, pallor, and weakness. Subtypes are classified by the size of RBCs, chronicity, and etiology. Anemia: Overview and Types antes de la cirugía.
    • Suprime los LOS Neisseria síntomas hasta que ocurra la menopausia natural en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum mujeres perimenopáusicas.
  • Tratamiento a corto plazo (< 6 meses) de la endometriosis Endometriosis Endometriosis is a common disease in which patients have endometrial tissue implanted outside of the uterus. Endometrial implants can occur anywhere in the pelvis, including the ovaries, the broad and uterosacral ligaments, the pelvic peritoneum, and the urinary and gastrointestinal tracts. Endometriosis (e.g., para «desgastar» los LOS Neisseria implantes antes de comenzar con los LOS Neisseria anticonceptivos hormonales como tratamiento a largo plazo)
  • Tratamiento de cáncer de próstata avanzado

Antagonistas de la GnRH

Ganirelix Ganirelix Antiestrogens, elagolix Elagolix Antiestrogens:

• Bloquean competitivamente los LOS Neisseria receptores de GnRH en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum la hipófisis.
• Suprimen la liberación de FSH FSH A major gonadotropin secreted by the adenohypophysis. Follicle-stimulating hormone stimulates gametogenesis and the supporting cells such as the ovarian granulosa cells, the testicular sertoli cells, and leydig cells. Fsh consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle y LH LH A major gonadotropin secreted by the adenohypophysis. Luteinizing hormone regulates steroid production by the interstitial cells of the testis and the ovary. The preovulatory luteinizing hormone surge in females induces ovulation, and subsequent luteinization of the follicle. Luteinizing hormone consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity. Menstrual Cycle para prevenir la ovulación.
• No tienen la «llamarada» asociada con los LOS Neisseria agonistas de GnRH.
• Indicaciones:
  • Ganirelix Ganirelix Antiestrogens: Se utiliza como parte de los LOS Neisseria tratamientos de fertilidad durante los LOS Neisseria ciclos ovulatorios controlados (se administran otros medicamentos para desarrollar folículos y desencadenar la ovulación).
  • Elagolix Elagolix Antiestrogens:
    • Endometriosis Endometriosis Endometriosis is a common disease in which patients have endometrial tissue implanted outside of the uterus. Endometrial implants can occur anywhere in the pelvis, including the ovaries, the broad and uterosacral ligaments, the pelvic peritoneum, and the urinary and gastrointestinal tracts. Endometriosis
    • Dispareunia (relaciones sexuales dolorosas)

Andrógenos y Progestágenos

• Los LOS Neisseria andrógenos y las progestinas sintéticas (estructuralmente similares a los LOS Neisseria andrógenos) se oponen al AL Amyloidosis estrógeno en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum el tejido endometrial.
• Suprimen el crecimiento endometrial → causan un adelgazamiento del tejido endometrial.
• Debido a los LOS Neisseria efectos secundarios androgénicos, los LOS Neisseria andrógenos rara vez se utilizan para el tratamiento en EN Erythema nodosum is an immune-mediated panniculitis (inflammation of the subcutaneous fat) caused by a type IV (delayed-type) hypersensitivity reaction. It commonly manifests in young women as tender, erythematous nodules on the shins. Erythema Nodosum mujeres.
• Las progestinas son un componente principal de la mayoría de los LOS Neisseria anticonceptivos hormonales.
• Indicaciones:
  • Anticoncepción
  • Condiciones que mejoran cuando se suprime el crecimiento endometrial:
    • Endometriosis Endometriosis Endometriosis is a common disease in which patients have endometrial tissue implanted outside of the uterus. Endometrial implants can occur anywhere in the pelvis, including the ovaries, the broad and uterosacral ligaments, the pelvic peritoneum, and the urinary and gastrointestinal tracts. Endometriosis
    • Dismenorrea
    • Sangrado menstrual abundante
    • Hiperplasia endometrial

Comparación de Medicamentos