HORMONAS

ESTEROIDEAS
Q.F. Ivan Miguel Quispe DIAZ
ESTROGENOS
CONCENTRACIONES
 BIOSINTESIS

Estrone -PubChem». National Center for Biotechnology Information. Consultado el 06-09-2009.

Helen Varney, Jan M. Kriebs, Carolyn L. Gegor. Varney's midwifery, Fourth Edition. Jones and Bartlett Publishers, 2004, p. 340.
ESTROGENOS MAS IMPORTANTES
DISTRIBUCION EN EL ORGANISMO
AGENTE ENDOCRINO METABOLICO
ESTROGENOS

ESTREVA : ESTRADIOL X
 INDICACIONES FDA
MENOPAUSIA IIb/B
 CANCER DE MAMA-
 ATROFIA VULVAR.
METASTASIS-PALIATIVO.
 ATROFIA VAGINAL.
 CARCINOMA DE
PROSTATA-AVANZADO-
 OSTEOPOROSIS.
PALIATIVO. IIb/B
POSTMENOPAUSICA PX. IIb/B
 DISMINUCION NIVEL
ESTROGENICO. I/B
SEGURIDAD: RAM COMUNES
0.5-13 % 5.7-56.7 % 17 %

SISTEMA SISTEMA PARCHE

TRANSDERMAL TRANSDERMAL TRANSDERMAL
SEGURIDAD: RAM COMUNES
20.2 /5-50% 1-8 % 6.5-17 %

GEL/SISTEMA SISTEMA SISTEMA

TRANSDERMAL TRANSDERMAL TRANSDERMAL
SEGURIDAD: RAM COMUNES
12.5/5-34.8 % 12.5/5-34.8 % 6.5-17 %

GEL/SISTEMA GEL/SISTEMA SISTEMA

TRANSDERMAL TRANSDERMAL TRANSDERMAL
SEGURIDAD: RAM COMUNES
SEGURIDAD: RAM GRAVES
CONTRAINDICACIONES
RECIENTE, ACTIVO, HISTORIA

Product Information: Vagifem(R) vaginal tablets, estradiol vaginal tablets. Novo Nordisk (per
FDA), Princeton, NJ, 2012.
Product Information: ELESTRIN(TM) topical gel, estradiol topical gel. DPT Laboratories, Ltd (Per
FDA), San Antonio, TX, 2012
Product Information: Evamist transdermal spray, estradiol transdermal spray. Ther-Rx
Corporation (per FDA), St. Louis, MO, 2011.
Product Information: ESTRACE(R) oral tablets, estradiol oral tablets. Warner Chilcott (US),Inc,
Rockaway, NJ, 2005.
Product Information: ESTRASORB(R) topical emulsion, estradiol topical emulsion. Espirit Pharma,
East Brunswick, NJ, 2006
Product Information: ESTRACE(R) vaginal cream, estradiol vaginal cream. Warner Chilcott
Company,Inc, Rockaway, NJ, 2007
 Product Information: Divigel(R) topical gel, estradiol topical gel. Upsher-Smith Laboratories, Inc.
(per FDA), Minneapolis, MN, 2012.
Product Information: VIVELLE(R) transdermal system, estradiol transdermal system. Novartis, East
Hanover, NJ, 2004.
CONTRAINDICACIONES
SOSPECHA, HISTORIA

 Product Information: Estraderm(R) transdermal system, estradiol transdermal system.

Novartis Pharmaceuticals Corporation (per FDA), East Hanover, NJ, 2012.
 Product Information: CLIMARA(R) transdermal patch, estradiol transdermal patch.
Bayer Healthcare Pharmaceuticals,Inc, Wayne, NJ, 2007.
Product Information: ALORA(R) transdermal patch, estradiol transdermal patch.
Watson Laboratories, Corona, CA, 2005.
Product Information: ESTRASORB(R) topical emulsion, estradiol topical emulsion.
Espirit Pharma, East Brunswick, NJ, 2006

ACTIVO, HISTORIA

Product Information: ELESTRIN(TM) topical gel, estradiol topical gel.

DPT Laboratories, Ltd (Per FDA), San Antonio, TX, 2012 .
Product Information: Evamist transdermal spray, estradiol transdermal
spray. Ther-Rx Corporation (per FDA), St. Louis, MO, 2011.
Product Information: ESTRACE(R) vaginal cream, estradiol vaginal
cream. Warner Chilcott Company,Inc, Rockaway, NJ, 2007.
CONTRAINDICACIONES
DIAGNOSTICO ANORMAL

Product Information: Vagifem(R) vaginal tablets, estradiol vaginal tablets. Novo

Nordisk (per FDA), Princeton, NJ, 2012.
Product Information: ESTRASORB(R) topical emulsion, estradiol topical emulsion.
Espirit Pharma, East Brunswick, NJ, 2006
Product Information: Evamist transdermal spray, estradiol transdermal spray. Ther-Rx
Corporation (per FDA), St. Louis, MO, 2011
Product Information: ESTRING(R) vaginal ring, estradiol vaginal ring. Pharmacia &
Uphjohn Company, New York, NY, 2007.

Product Information: Vagifem(R) vaginal tablets, estradiol vaginal

tablets. Novo Nordisk (per FDA), Princeton, NJ, 2012.
Product Information: ELESTRIN(TM) topical gel, estradiol topical gel.
DPT Laboratories, Ltd (Per FDA), San Antonio, TX, 2012.
Product Information: ESTRACE(R) oral tablets, estradiol oral tablets.
Warner Chilcott (US),Inc, Rockaway, NJ, 2005.
Product Information: ESTRING(R) vaginal ring, estradiol vaginal ring.
Pharmacia & Uphjohn Company, New York, NY, 2007.
CONTRAINDICACIONES
SOSPECHA, CONOCIDA

 Product Information: ESTRACE(R) vaginal cream, estradiol vaginal cream. Warner

Chilcott Company,Inc, Rockaway, NJ, 2007.
Product Information: ESTRACE(R) oral tablets, estradiol oral tablets. Warner Chilcott
(US),Inc, Rockaway, NJ, 2005.
Product Information: Divigel(R) topical gel, estradiol topical gel. Upsher-Smith
Laboratories, Inc. (per FDA), Minneapolis, MN, 2012
 FARMACOCINETICA
F:
Tópica-gel: Transdermal
ABSORCION
Difusión pasiva y vaginal,
buena

DIISTRIBUCION UPP: Alta

VD: Amplio

Hepático: CYP 3 A 4
Recirculación enterohepatica
METABOLISMO Estrona, estriol, sulfato

EXCRECION Renal: Principal

INTERACCIONES FARMACOLOGICAS

SOLO PRESENTA 14
INTERACCIONES
FARMACOLOGICAS DE
MODERADA
SEVERIDAD.
ACCION SOBRE EL SRAA
NEUROPROTECCION
NEUROPROTECCION
NEUROPROTECCION
CANCER DE MAMA
CANCER DE MAMA
EN LA ARTERIOSCLEROSIS
LDL/HDL
ANTIESTROGENOS
 ANTIESTROGENOS

TIPO I: TIPO II: ANTAGONISTAS

AGONISTAS/ANTAGONISTAS

TRIFENILETILENO:
Tamoxifeno, toremifeno FULVESTRANT

BENZOTIOFENO:
Raloxifeno
BENZOPIRANOS:
Levormeloxifeno
HIDRONAFTALENOS:
Trioxifeno
MODULADOR SELECTIVO DEL
RECEPTOR DE ESTROGENO
 INDICACIONES FDA
TAMOXIFENO RALOXIFENO TOREMIFENO
CANCER SENO, TX ADJ
IIa/A
CANCER SENO, ALTO RIESGO, PX
IIa/A
CARCINOMA SENO IN SITU, REDUCIR
INVASIVIDAD
IIa/B
NEOPLASIA MAMA MASCULINA,
METASTASIS
IIb/B
CANCER SENO, METASTASIS
IIa/B
CANCER SENO, INVASIVO,
POSTMENOPAUSIA, PX
IIa/B
CANCER SENO, INVASIVO,
POSTMENOPAUSIA-OSTEOPOROSIS, PX
IIb/B
POSTMENOPAUSIA-OSTEOPOROSIS
IIa/B
POSTMENOPAUSIA-OSTEOPOROSIS, PX
IIa/B
CANCER SENO, METASTASIS,RECEPTOR
ESTROGENICO POSITIVO O
IIa/B
DESCONOCIDO
SEGURIDAD-RAM COMUNES
TAMOXIFENO RALOXIFENO TOREMIFENO

FLUSHING MENOPAUSICO
41-80 %
PERIODO IRREGULAR 9-25 %
DESCENSO VAGINAL 13-30 % ++
SUDORACION +++ +++
CALAMBRES EN PIERNAS +++
EDEMA 5%
NAUSEA +++

MAREOS +++
 SEGURIDAD-RAM GRAVES
TAMOXIFENO RALOXIFENO TOREMIFENO
TVP 0.8 % 1%
CANCER DE SENO +
CATARATAS 7-8.7 %
CANCER UTERINO +
TROMBOCITOPENIA > 1.5 %
INCREMENTO AST/GOT 5-19 %
INCREMENTO FOSFATASA 8-19 %
ALCALINA
 CONTRAINDICACION
TAMOXIFENO RALOXIFENO TOREMIFENO
USO CONCOMITANTE
ANTICOAGULANTES +
CUMARINICOS

TVP
+ +
HIPERSENSIBILIDAD
+ +
EMBOLISMO PULMONAR
+ +
MADRES LACTANTES
+
EMBARAZO
+
HIPOMAGNESEMIA, no
corregida +
INTERACCIONES FARMACOLOGICAS
TAMOXIFENO RALOXIFENO TOREMIFENO
WARFARINA CONTRAINDICADO
RETRASADO
BUENO
INCREMENTO SANGRADO

FLUOURACILO MAYOR
RETRASADO
BUENO
TROMBOEMBOLISMO

FLUOXETINA RETRASADO
MAYOR
DEBIL
DISMINUYE
CONCENTRACION
TAMOXIFENO ACTIVO
 FARMACOCINETICA
TAMOXIFENO RALOXIFENO TOREMIFENO

ABSORCION Tmx 5 h, RAPIDO T max 3 h, alimentos no

F: 2 % influencian

DISTRIBUCION UPP: 95 % UPP: 99.5 %

METABOLISMO HEPATICO, EXTENSO, CYP 3 A, HEPATICO, EXTENSO, PRIMER HEPATICO, EXTENSIVO, CYP
2 C 9, 2 D 6. PASO 3 A 4.
N-DESMETIL-TAMOXIFENO CIRCULACION ENTEROHEPATICA

EXCRECION FECAL, PRINCIPALMENTE FECAL, PRINCIPALMENTE FECAL, PRINCIPALMENTE.

RENAL 10 %

TIEMPO DE VIDA MEDIA 5-7 d. 32.5 h 5d

14 d
RESISTENCIA A TAMOXIFENO