Nh. Bjarnason et al., TIBOLONE - INFLUENCE ON MARKERS OF CARDIOVASCULAR-DISEASE, The Journal of clinical endocrinology and metabolism, 82(6), 1997, pp. 1752-1756
Tibolone, a synthetic steroid with estrogenic, androgenic, and progest
ogenic properties relieves climacteric symptoms and prevents postmenop
ausal bone loss. The influence of tibolone treatment on coagulation, f
ibrinolysis, and lipid metabolism was investigated in 91 healthy late
postmenopausal women. They were randomly assigned in a double-blind, p
lacebo-controlled 2-year study to receive either tibolone 1.25 mg (n =
36, 29 completed) or 2.5 mg (n = 35, 28 completed) or placebo (n = 20
, 13 completed). The biochemical markers of lipid metabolism, fibrinol
ysis, and coagulation were measured every 3 months. In both tibolone g
roups a similar (similar to 30%) decrease in high density lipoprotein
cholesterol and a corresponding lowering of apolipoprotein A-1 (P < 0.
001) was detected. Also serum total cholesterol and triglycerides were
reduced (similar to 15%; P < 0.01), whereas low density lipoprotein c
holesterol, apolipoprotein B, and lipoprotein(a) were unaffected by ti
bolone. The two dose levels of tibolone resulted in a similar, marked
lowering (similar to 30%) of tissue plasminogen activator and plasmino
gen activator inhibitor activity as compared with placebo (P < 0.001).
Plasminogen increased (similar to 15%; P < 0.001) in both groups. Fib
rinogen was lowered (P < 0.01) in the low-dose group, and antithrombin
III remained unchanged. The overall effect on hemostatic factors of t
he present doses of tibolone in healthy, late postmenopausal women ten
ds towards increased fibrinolysis and unchanged coagulation. This may
be beneficial and might theoretically counterbalance the potentially n
egative effect of the decrease in high density lipoprotein cholesterol
.