Pharmacokinetics and pharmacodynamics of 25-mg estradiol implants in postmenopausal Mexican women.
OBJECTIVE
To assess the serum concentrations of estradiol (E2), estrone (E1), gonadotrophins, sex hormone-binding globulin, and lipids, and to determine degree of symptom relief after subcutaneous implantation of 25 mg estradiol in postmenopausal Mexican women.


METHODS
Fifteen postmenopausal, hysterectomized women participated in an open, observational study. Blood samples were obtained before implantation and at regular intervals during a study period of 24 weeks. Climacteric symptoms were evaluated by means of the Greene climacteric scale. Wilcoxon's test was performed on the paired results of pre-and postimplantation values.


RESULTS
Serum concentrations of E2 obtained after implantation were fairly constant, remaining within the early follicular range for the entire study period of 24 weeks, and were associated with significant symptom relief. A physiological, premenopausal E2:E1 ratio was achieved. No significant metabolic changes occurred. Side effects were estrogenic in nature and no removal of implant was required.


CONCLUSIONS
Subcutaneous implantation of 25 mg estradiol results in physiological, premenopausal estrogen concentrations in most women and is associated with considerable symptom relief without inducing significant adverse metabolic effects.
del Carmen Cravioto
M
M
Department of Reproductive Biology, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán, Mexico City, Mexico.
Larrea
F
F
Delgado
N E
NE
Escobar
A R
AR
Díaz-Sánchez
V
V
Domínguez
J
J
de León
R P
RP
D004958:Estradiol / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology*; D015914:Estrogen Replacement Therapy; D004970:Estrone / Q000097:blood; D005260:Female; D005640:Follicle Stimulating Hormone / Q000097:blood; D006801:Humans; D007986:Luteinizing Hormone / Q000097:blood; D008800:Mexico; D008875:Middle Aged; D017698:Postmenopause / Q000187:drug effects* / Q000502:physiology; D019736:Prostheses and Implants; D012738:Sex Hormone-Binding Globulin / Q000032:analysis
D012738:Sex Hormone-Binding Globulin; D004970:Estrone; D004958:Estradiol; D007986:Luteinizing Hormone; D005640:Follicle Stimulating Hormone