304
Endothelial function is associated with cardiac risk fac-
tor status.
1
Estrogen administration induces positive ef-
fects on endothelial function and on blood flow in
normal and atherosclerotic arteries in nonhuman pri-
mates and in postmenopausal women.
2-4
Estrogen recep-
tors, which are present in the vascular endothelium, play
an integral role, especially in the generation of nitric
oxide.
5
Selective estrogen receptor modulators (SERMs)
have estrogen-agonistic actions in some tissues and estro-
gen-antagonist actions in others. Estrogen-like actions in
arteries have been reported for several different SERMs,
including raloxifene, in human cell culture and animal
studies
6-8
and for tamoxifen and droloxifene in post-
menopausal women.
9
Two recent reports of the effects of
raloxifene on endothelial function in healthy post-
menopausal women are discrepant; one report shows a
significant increase in blood flow–mediated vasodilation
after raloxifene, and the other report shows no signifi-
cant improvement.
10,11
Brachial artery imaging
12
and laser Doppler veloci-
metry (LDV)
13
have been used to assess endothelial
function. There is a close relation between endothelium-
dependent vasomotor responses in the human coronary
and peripheral circulations.
14
We therefore used these
techniques simultaneously to assess the effects of ralox-
ifene on brachial artery and microcirculatory endothelial
responses in healthy postmenopausal women in a ran-
domized, double-blind, placebo-controlled crossover
trial.
Material and methods
Subjects. Twenty healthy postmenopausal women were
enrolled, of whom 1 was subsequently deemed ineligible
because of undisclosed Raynaud’s phenomenon; the re-
maining cohort of 19 women was studied. Postmenopausal
From the Departments of Obstetrics and Gynecology
a
and Epidemiology
and Public Health,
b
Yale University School of Medicine, and the Yale
Prevention Research Center.
c
Supported by Eli Lilly and Company, Indianapolis, Ind.
Received for publication May 17, 2002; revised July 12, 2002; accepted
September 23, 2002.
Reprint requests: Philip M. Sarrel, MD, Yale-Griffin Prevention Re-
search Center, 130 Division St, Derby, CT 06418. E-mail: philip.sar-
rel@Yale.edu
© 2003, Mosby, Inc. All rights reserved.
0002-9378/2003 $30.00 + 0
doi:10.1067/mob.2003.28
Raloxifene and endothelial function in healthy
postmenopausal women
Philip M. Sarrel, MD,
a
Haq Nawaz, MD, MPH,
b,c
Wendy Chan, MPH,
c
Melissa Fuchs, MD,
b
and David L. Katz, MD, MPH
b,c
New Haven and Derby, Conn
OBJECTIVE: The purpose of this study was to determine the effects of raloxifene on endothelial function in
healthy, postmenopausal women.
STUDY DESIGN: This was a randomized, double-blind, placebo-controlled crossover trial. Subjects (n = 19;
mean age, 61 years) underwent endothelial function testing at baseline and after treatment with placebo or
raloxifene (60 mg per day for 6 weeks).
RESULTS: Brachial artery diameter change (flow-mediated dilation) increased 5.0% with placebo and 8.56%
with raloxifene (SE = 1.83, P = .03) in response to a hyperemic stimulus; an adjustment of this response for a
variation in stimulus intensity resulted in greater discrimination (P = .009). The ratio of area under the curve
response to area under the curve reference with the use of laser Doppler measures was 1.18 for placebo
and 1.28 for raloxifene (P = .05). Flow-mediated dilation and area under the curve ratio correlated signifi-
cantly (r = 0.33, P = .04).
CONCLUSION: Treatment with raloxifene enhanced endothelial-mediated dilation in brachial arteries and
digital vessels in healthy, postmenopausal women.A potential mechanism for a cardioprotective effect of
raloxifene is suggested and warrants further study. (Am J Obstet Gynecol 2003;188:304-9.)
Key words: Endothelial response, raloxifene, healthy postmenopausal women
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