Estrogen replacement is often advised for postmenopausal women to prev
ent menopausal symptoms, osteoporosis and heart disease. However, litt
le information is available concerning the half-life of estradiol (E-2
) in postmenopausal women. This study was designed to determine the ha
lf-life and metabolism of transdermal E-2. A prospective clinical stud
y of 8 healthy postmenopausal women was performed in the Clinical Rese
arch Center of the Brigham and Women's Hospital. A transdermal E-2 pat
ch 0.10 mg was placed on the abdominal wall. Thirteen hours later, aft
er an overnight fast, the E-2 patch was removed and frequent blood sam
pling was performed over 6 h. Serum samples were assayed for E-2, estr
one (E-1) and estrone sulfate (E1S). Serum samples were taken before E
-2 patch placement, for 30 min before patch removal, and for 6 h after
patch removal. The basal E-2 level of women prior to use of transderm
al E-2 was 19 +/- 2 pg/ml (mean +/- SE). Thirteen hours after transder
mal E-2 placement, steady state levels had been reached, with a mean E
-2 of 112 +/- 6 pg/ml. The mean half-life of E-2 after removal of tran
sdermal E-2 was 161 min (range 107-221 min). There was a direct relati
onship between the subjects' weight and the half-life of E-2 (r = 0.79
, p = 0.02). Mean basal E-1 levels were 23 +/- 5 pg/ml and mean E-1 st
eady-state levels after E-2 patch placement were 39 +/- 0.6 pg/ml. E1S
levels rose from mean basal levels of 1.5 +/- 0.3 ng/ml to mean stead
y-state levels of 3.1 +/- 0.1 ng/ml after placement of the E-2 patch.
The apparent half-life of E-2 after discontinuing a transdermal E-2 pa
tch is 2.7 h or 161 min.