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Clormadinona ¿Todas Las Progestinas Son Iguales?

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Clormadinona ¿Todas Las Progestinas Son Iguales? ¿Todas las progestinas son iguales? DR. GUILLERMO LUIS CARPIO PERTIERRA GERENTE MÉDICO SALUD FEMENINA GRÜNENTHAL …Recordemos Fases del Ciclo Femenino (28 días) 1 2 3 4 5 6 7 8 9 1 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 Regla Fase estrogénica o proliferativa Fase lútea o progestacional O v La fase estrogénica o proliferativa se u La fase lútea o progestacional se l caracteriza por: a caracteriza por: • Elevación de FSH c • Elevación de LH i • Elevación de progesterona • Elevación de estrógenos ó • En el ovario, el folículo crece hasta 2.5 n • Se forma el cuerpo amarillo dentro del cm folículo roto para preparar al endometrio para recibir al huevo fecundado Papel de los estrógenos en el cuerpo de la mujer https://www.urmc.rochester.edu/encyclopedia/content.aspx?contenttypeid=85&contentid=P03652 Los estrógenos en el cuerpo de la mujer Cerebro ◦ Ayudan a mantener la temperatura corporal ◦ Ayudan a retrasar la pérdida de memoria Corazón e hígado ◦ Influyen en el metabolismo de las grasas y del colesterol protegiendo de las arterias de las placas de ateroma. ◦ Tienen efecto protector en los vasos sanguíneos de forma que disminuyen el riesgo de infarto de miocardio y de accidente vascular cerebral. Mamas ◦ Estimula el desarrollo de los senos en la pubertad y prepara a las glándulas para la producción de leche durante el embarazo Ovarios ◦ Estimula el comienzo de los ciclos menstruales (menarca), una indicación de que el sistema reproductivo de una niña ha madurado Útero ◦ Estimula su maduración durante la niñez ◦ Ayuda a preparar al útero para nutrir al feto en desarrollo Vagina ◦ Estimulan la producción de flujo vaginal de forma que evita la sequedad Huesos ◦ Ayudan a fijar el calcio en los huesos, evitando la acción de los osteoclastos y con ellos la osteoporosis Otros ◦ Determinan el acúmulo de grasa típicamente femenino en las caderas y alrededor de las mamas ◦ Son los responsables de la aparición del vello en la pubertad https://www.urmc.rochester.edu/encyclopedia/content.aspx?contenttypeid=85&contentid=P03652 La progesterona en el cuerpo de la mujer Cerebro ◦ Efecto sobre el cerebro responsable de los cambios de humor típicos de las diferentes fases del ciclo menstrual ◦ Influye también en la temperatura corporal aumentando en medio grado aproximadamente la temperatura después de la ovulación Mamas ◦ Efecto sobre las mamas produciendo una congestión de éstas, responsable del aumento de volumen y de la mayor sensibilidad de las mamas los días previos a la regla ◦ Favorece la maduración de los acinos y glándulas mamarias durante el embarazo Riñones ◦ Efecto sobre el riñón, disminuyendo la eliminación de agua y líquidos y por tanto aumentando la retención de líquidos en las mamas Sistema gastrointestinal ◦ Relaja el músculo liso, provocando así disminución en la motilidad intestinal y vaciamiento gástrico. Esto se traduce en “hinchazón” abdominal y también en estreñimiento Útero ◦ Induce la formación de glándulas en el endometrio uterino para la producción de glucógeno Vagina ◦ Modifica el moco cervical, volviéndolo grumoso ◦ Aumenta la vascularidad local ¿Qué es una PROGESTINA ? Las progestinas son un grupo de compuestos químicamente diversos con una multiplicidad de acciones sobre el progestágeno, así como el estrógeno, andrógeno, mineralocorticoide, glucocorticoide y otros receptores. Es una sustancia sintética que tiene efectos similares a la hormona progesterona Datos históricos de las progestinas sintéticas ▪ México jugó un papel muy importante en la síntesis de progestinas . ▪ En 1951 se sintetizó la noretisterona. ▪ Esto permitió la evaluación clínica de los primeros anticonceptivos orales. ¿Cómo actúan las progestinas en la anticoncepción? o Inhibiendo la ovulación según la dosis o Suprime el pico de LH y FSH que ocurre a la mitad del ciclo. Es importante recordar que el efecto anticonceptivo lo ofrece la progestina, el estrógeno se agrega para garantizar un sangrado regular mensual o Modificando las características del moco cervical, volviéndolo grumoso o Volviendo al endometrio no apto para la anidación o Al inhibir a los receptores para progesterona en el endometrio, aumenta el endometrio tisular y disminuye el número de glándulas y de edema estromal. o Reduciendo la motilidad tubárica, así como la motilidad de los cilios tubáricos ¿Cuáles son las progestinas en los anticonceptivos de Be Pink? Clormadinona Desogestrel Etonogestrel Nomegestrol Clasificación de los progestágenos Progesterona Naturales Progestágenos Retroprogesterona Dihidroprogesterona Progesterona Sódica Sintéticos Micronizada 17α 19 Nortestosterona 19 Norprogesterona SPRM’S* 17 Hidroxiespironolactona Hidroxiprogesterona Acetato de ESTRANOS Acetato de Acetato de Ulipristal Medroxiprogesterona - Acetato de Nomegestrol Asoprinil Drospirenona Noretindrona NETA Acetato de Nestorona Mifepristona Clormadinona Noretinodrel Trimegestona Lonaprisan Acetato de Linestrenol Promegestona Onapristona Ciproterona Diacetato de Medrogestona Etinodiol Acetato de Telapristona GONANOS Levonorgestrel Desogestrel Gestodeno Norgestimato Etonogestrel Norgestrel Dienogest • Modulador selectivo del receptor de progesterona • “Selective progesterone receptor modulator” Progesterona sintética Pregnanos Derivados Derivados Derivados 17α- Espironolactona Hidroxiprogesterona 19-Nor 19-Nortestosterona Potencia baja 19-Norprogesterona 19-Nortestosterona 19-Nortestosterona 17-Hidroxiespironolactona Gonanos Sin efecto Norpregnanos Estranos Gonanos Acción androgénico Baja potencia Primera generación Segunda generación Tercera generación antimineralocorticoide Alta potencia Alta potencia Alta potencia Acción androgénica Menos androgénico Noretisterona Acetado de Demegestona Medroxiprogesterona Promegestona Noretindrona Drospirenona Acetato de megestrol Nesterona Acetato de Noretisterona Desogestrel Gestodeno Norgestrel Acetato de Trimegestona Linestrenol Etonogestrel Norgestimato Clormadinona Dienogest Acetato de Nomegestrol Eacetato de etinodiol Levonorgestrel Acetato de Ciproterona Noretinodrel Guerra, J. A., López-Muñoz, F., & Álamo, C. (2013). Progestins in combined contraceptives. Journal of Experimental & Clinical Medicine, 5(2), 51-55. Nuevas Progestinas Características específicas PROGESTINA CARACTERISTICA NOTABLE Dienogest Antiandrogénica Drospirenona Antimineralocorticoide Nomegestrol Altamente antigonadotrópica Trimegestona Altamente progestacional Nestorona Altamente progestacional y antigonadotropica Ninguna progestina nueva es androgénica o estrogénica Sitruk-Ware R. New Progestogens A Review of Their Effects in Perimenopausal and Postmenopausal Women. Drugs Aging 2004; 21 (13): 865-883 Los primeros progestágenos y los actuales 1,2 Los progestágenos varían en cuanto a la selectividad por el receptor de progesterona (RP): Actividad Actividad Actividad Actividad androgénica mineralocorticoide glucocorticoide estrogénica • Pérdida de • Pérdida de sodio • Retención de • Acné respuesta y agua sal y agua estrogénica • Retención de • Hirsutismo potasio • Desequilibrio • ↓ presión arterial lipídico 1. Speroff L and Fritz MA. Oral contraception. In: Clinical Gynecologic Endocrinology and Infertility; Philadelphia: Lippincott Williams & Wilkins, 2005:861–942. 2. Sitruk-Ware R. Maturitas. 2008;61:151–157. Efectos de las Progestinas Progesterone, TMG, DYDR CPA, Agonista CMA Puro DNG CMA = Acetato de clormadinona Efecto Efecto ENG Antiestrogenico DSG Antiandrogenico CPA = Acetato de ciproterona parcial parcial LNG DNG = Dienogest DYDR = Dihidrogesterona Efecto Estrogénico Efecto DRSP = Drospirenona parcial Androgenico DSG = Desogestrel parcial GSD = Gestodeno NETA LNG, DSG, NMG = Acetato de Nomegestrol Efecto GST LNG = Levonorgestrel Glucocorticoide Efecto DSG, NG, parcial AntimineraloGSD- MPA = Acetato de medroxiprogesterona corticoide NETA = Acetato de noretindrona MPA parcial MGA NG = Norgestrel DRSP TMG = Trimegestona ENG = Etonorgestrel Schneider, H. P. "The role of antiandrogens in hormone replacement therapy." Climacteric: the journal of the International Menopause Society 3 (2000): 21-27. Efectos colaterales de las progestinas ▪ Actividad progestacional ▪ Efecto: Adelgazamiento del endometrio ▪ Uso principal: Contraposición a la proliferación endometrial estrogénica ▪ Actividad antigonadotrópica ▪ Efecto: Bloqueo del mecanismo de retroalimentación de FSH y LH, provocando anovulación ▪ Uso principal: Anticoncepción al evitar la anovulación ▪ Actividad anti-androgénica ▪ Efecto: Inhibición de la conversión de colesterol a testosterona vía inhibición de la actividad de la 3 beta hidroxiesteroide deshidrogenasa ▪ Uso principal: Acné, piel seborreica Vásquez-Awad, D., Palacios, S., De Melo, N. R., Gómez-Tabares, G., & de Mola, R. L. (2014). Anticonceptivos orales combinados: Guías Latinoamericanas. Medicina, 36(2), 136-149. Efectos colaterales de las progestinas ▪ Actividad anti-mineralocorticoide ▪ Efecto: Actúa en las glándulas suprarrenales oponiéndose al efecto de la hormona antidiurética, la cual es encargada del metabolismo del sodio y potasio además de la retención de líquidos ▪ Uso principal: Disminución de retención de agua haciendo las veces de un diurético menor ▪ Actividad glucocorticoide ▪ Efecto: Actúa en las glándulas suprarrenales, participando en la formación de cortisol, cortisona y corticosterona, hormonas que participan en la regulación del metabolismo de carbohidratos, actividad inmunosupresora y metabolismo intermedio de las grasas y proteínas ▪ Uso principal: Se trata de un efecto colateral, no tiene un uso específico ▪ Actividad anti-estrogénica
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