Burckhardt P
Département de médecine interne, CHUV, Lausanne.
Schweiz Med Wochenschr. 1999 Dec 11;129(49):1926-30.
The term "SERM" stands for "Selective Estrogen Receptor Modulators", substances which act on certain organs as oestrogen agonists and on other organs as oestrogen antagonists. They can exert the known oestrogen-like effects on bone and lipids without exerting any action on the endometrium and the breast, a potentially ideal profile for postmenopausal hormone replacement treatment. Long known are clomifen, an ovulation stimulator, and tamoxifen, used for secondary prevention in breast cancer. Tamoxifen prevents postmenopausal bone loss as efficiently as hormone replacement treatment, and lowers blood lipids and the coronary risk, but increases the risk of endometrial cancer; for this reason it cannot be used in the prevention of postmenopausal osteoporosis. Raloxifen stimulates neither the endometrium nor the mammary gland, and probably even lowers the risk of breast cancer. Its relatively mild but significant effect on BMD (+ 2-3%/2 years) is sufficient for prevention, and in osteoporotics goes along with a substantial decrease in vertebral fracture incidence (by about 50%) comparable to the effect of other treatments. As in hormone replacement treatment, thromboembolism and leg cramps occur more frequently. Therefore, raloxifen can be used in women free of climacteric symptoms for the prevention and treatment of postmenopausal osteoporosis with no increased risk of phlebitis, alone or in combination with calcium, vitamin D, bisphosphonates and calcitonin; in future it may also be useful in male osteoporosis.
术语“SERM”代表“选择性雌激素受体调节剂”,这类物质在某些器官上作为雌激素激动剂起作用,而在其他器官上作为雌激素拮抗剂起作用。它们可以对骨骼和脂质发挥已知的雌激素样作用,而对子宫内膜和乳腺不产生任何作用,这对于绝经后激素替代治疗来说是一种潜在的理想特性。长期以来为人所知的克罗米芬是一种排卵刺激剂,他莫昔芬则用于乳腺癌的二级预防。他莫昔芬预防绝经后骨质流失的效果与激素替代治疗一样有效,还能降低血脂和冠心病风险,但会增加子宫内膜癌的风险;因此它不能用于预防绝经后骨质疏松症。雷洛昔芬既不刺激子宫内膜也不刺激乳腺,甚至可能降低乳腺癌风险。它对骨密度有相对温和但显著的影响(2年内增加2 - 3%),足以用于预防,对于骨质疏松症患者,它能使椎体骨折发生率大幅降低(约50%),与其他治疗效果相当。与激素替代治疗一样,血栓栓塞和腿部痉挛更频繁发生。因此,雷洛昔芬可用于没有更年期症状的女性,用于预防和治疗绝经后骨质疏松症,不会增加静脉炎风险,可单独使用或与钙、维生素D、双膦酸盐和降钙素联合使用;未来它可能对男性骨质疏松症也有用。