Advantages of raloxifene over alendronate or estrogen on nonreproductive and reproductive tissues in the long-term dosing of ovariectomized rats

Journal of Pharmacology and Experimental Therapeutics

Volumn 279, Issue 1, 1996, Pages 298-305

  Sato, Masahiko ^a   Bryant, Henry U ^a   Iversen, Philip ^a   Helterbrand, Jeff ^a   Smietana, Frank ^a   Bemis, Kerry ^a   Higgs, Richard ^a   Turner, Charles H ^b   Owan, Ichiro ^b   Takano, Yuichi ^b   Burr, David B ^b  

^a ELI LILLY AND COMPANY   (United States)

^b INDIANA UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALENDRONIC ACID; ETHINYLESTRADIOL; RALOXIFENE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BODY WEIGHT; BONE ATROPHY; BONE DENSITY; CHOLESTEROL BLOOD LEVEL; CONTROLLED STUDY; ESTROGEN THERAPY; FEMALE; HORMONE SUBSTITUTION; MOUSE; NONHUMAN; ORAL DRUG ADMINISTRATION; OSSIFICATION; OVARIECTOMY; PRIORITY JOURNAL; SUBCUTANEOUS DRUG ADMINISTRATION; UTERUS WEIGHT;

EID: 12644279864     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (34)

1. AZUMA, Y., SATO, H., OUE, Y., OKABE, K., OHTA, T., TSUCHIMOTO, M. AND KIYOKI, M.: Alendronate distributed on bone surfaces inhibits osteoclastic bone resorption in vitro and in experimental hypercalcemia models. Bone 16: 235-245, 1995.
2. BLACK, L. J., JONES, C. D. AND FACONE, J. R.: Antagonism of estrogen action with a new benzothiophene derived antiestrogen. Life Sci. 32: 1031-1036, 1983.
3. BLACK, L. J., SATO, M., ROWLEY, E. R., MAGEE, D. E., BEKELE, A., WILLIAMS. D. C., CULLINAN, G. J., BENDELE, R., KAUFFMAN, R. F., BENSCH, W. R., FROLIK, C., TERMINE, J. AND BRYANT, H. U.: Raloxifene (LY139481 HCl) prevents bone loss and reduces serum cholesterol without causing uterine hypertropy in ovariectomized rats. J. Clin. Invest. 93: 63-69, 1994.
4. DEMPSTER, D. W. AND LINDSAY, R.: Pathogenesis of osteoporosis Lancet 341: 797-801, 1993.
5. DEVOR, M., BARRETT-CONNER, E., RENVALL, M., FEIGAL, D. AND RAMSDELL, J.: Estrogen replacement therapy and the risk of venous thrombosis. Am. J. Med. 92: 275-282, 1992.
6. DRAPER, M. W., FLOWERS, D. E., HUSTER, W. J. AND NEILD, J. A.: Effects of raloxifene (LY139481 HCl) on biochemical markers of bone and lipid metabolism in healthy postmenopausal women. In Proceedings of the 4th International Symposium on Osteoporosis, ed. by C. Arnaud and K. Harper, March 27-April 2, 1993. Hong Kong (Abstract), pp. 119-121.
7. DUPONT, W. D. AND PAGE, D. L.: Menopausal estrogen replacement therapy and breast cancer. Arch. Int. Med. 151: 67-72, 1991.
8. EVANS, G., BRYANT, H. U., MAGEE, D., SATO, M. AND TURNER, R. T.: The effects of raloxifene on tibia histomorphometry in ovariectomized rate. Endocrinology 134: 2283-2288, 1994.
9. FLEISCH, H.: Bisphosphonates- pharmacology and use in the treatment of tumour-induced hypercalcaemic and metastatic bone disease. Drugs 42: 919-944, 1991.
10. HAMMOND, C. B., JELOVSEK, F. R., LEE, K. L., CREASMAN, W. T. AND PARKER, R. T.: Effects of long term estrogen therapy. I. Metabolic effects. Am. J. Obstet. Gynecol. 133: 525-536, 1979.
11. LIBERMAN U. A., WEISS S. R., BROLL J., MINNE H. W., QUAN H., BELL N. H., PORTALES J. R., DOWNS R. W., DEQUEKER J., FAVUS M., SEEMAN E., RECKER R. R., CAPIZZI T., SANTORA A. C., LOMBARDI A., SHAH, R. V., HIRSCH L. J., AND KARPF D. B.: Effect of oral alendronate on bone mineral density and the incidence of fractures in postmenopausal osteoporosis. N. Engl. J. Med. 333: 1437-43, 1995.
12. LIN, J. H., CHEN, I. W. AND DELUNA, F. A.: Nonlinear kinetics of alendronate, plasma protein binding and bone uptake. Drug Metab. Dispos. 22: 400-405, 1994a.
13. LIN, J. H., CHEN, I. W. AND DELUNA, F. A.: On the absorption of alendronate in rats. J. Pharm. Sci. 83: 1741-1746, 1994b.
14. LINDSAY, R.: Prevention and treatment of osteoporosis Lancet 341: 801-805, 1993.
15. PAPAPOULOS, S. E., LANDMAN, J., BIJVOET, O. L. M., LOWIK, C. W. G. M., VALKEMA, R., PAUWELS, E. K. J. AND VERMEIJ, P.: The use of bisphosphonates in the treatment of osteoporosis. Bone 13: suppl. 1, S41-S49, 1992.
16. PARFITT, A. M., DREZNER, M. K., GLORIEUX, F. H., KANIS, J. A., MALLUCHE, H., MEUNIER, P. J., OTT, S. M. AND RECKER, R. R.: Bone histomorphometry: Standardization of nomenclature, symbols, and units. J. Bone Miner. Res. 2: 595-610, 1987.
17. QUIGLEY, M. E. T., MARTIN, P. L., CURNIER, A. M. AND BROOKS, P.: Estrogen therapy arrests bone loss in elderly women. Am. J. Obstet. Gynecol. 156: 1516-1523, 1987.
18. RODAN, G. A., SEEDOR, J. G. AND BALENA, R.: Preclinical pharmacology of alendronate. Osteoporos. Int. 3: S7-S12, 1993.
19. SAHNI, M., GUENTHER, H. L., FLEISCH, H., COLLIN, P. AND MARTIN, T. J.: Bisphosphonates act on rat bone resorption through the mediation of osteoblasts. J. Clin. Invest 91: 2004-2011, 1993.
20. SATO, M. AND GRASSER, W.: Effects of bisphosphonates on isolated rat osteoclasts as examined by reflected light microscopy. J. Bone Miner. Res. 5: 31-40, 1990.
21. SATO, M., GRASSER, W., ENDO, N., AKINS, R., SIMMONS, H., THOMPSON, D. D., GOLUB, E. AND RODAN, G. A.: Bisphosphonate action: Alendronate localization in rat bone and effects on osteoclast ultrastructure. J. Clin. Invest. 88: 2095-2105, 1991.
22. SATO, M., MCCLINTOCK, C., KIM, J., TURNER, C., BRYANT, H., MAGEE, D. AND SLEMENDA, C.: Dual-energy X-ray aborptiometry of raloxifene effects on the lumbar vertebrae and femora of ovariectomized rats. J. Bone Miner. Res. 9: 715-724, 1994.
23. SATO, M., KIM, J., SHORT, L. L., SLEMENDA, C. W. AND BRYANT, H. U.: Longitudinal and cross-sectional analysis of raloxifene effects on tibiae from ovariectomized aged rats. J. Pharmacol. Exp. Ther. 272: 1252-1259, 1995.
24. SCHALKOFF, R. J.: Digital Image Processing and Computer Vision, Wiley, New York, 1989.
25. SCHENK, R., MESZ, W. A, MUHLBAUER, R., RUSSELL, R. AND FLEISCH, H.: Effect of EHDP and Cl2 MDP on the calcification and resorption of cartilage and bone in the tibial epiphysis and metaphysis of rats. Calcif. Tissue Res. 11: 196-214, 1973.
26. SHEN, V., MENG, X., LIANG, X., BIRCHMAN, D., WU, D., LINDSAY, R. AND DEMPSTER, D.: Increased trabecular thickness without an accompanying increase in trabecular plate number or connectivity can completely restore cancellous bone strength in estrogen deficient rats (Abstract). J. Bone Miner. Res. 10: S356, 1995.
27. SMITH, D. C., PRENTICE, R., THOMPSON, D. J. AND HERRMANN, W. L.: Association of exogenous estrogen and endometrial carcinoma. N. Engl. J. Med. 293: 1164-1167, 1975.
28. STAMPFER, M. J., COLDITZ, G. A., WILLET, W. C., MANSON, J. E., ROSNER, B., SPEIZER, F. E. AND HENNEKENS, C. H.: Postmenopausal estrogen therapy and cardiovascular disease: Ten-year follow-up from the nurses' health study. N. Engl. J. Med. 325: 756-762, 1991.
29. STEINBERG, K. K., THACKER, S. B. AND SMITH, S. C.: A meta-analysis of the effect of estrogen replacement therapy on the risk of breast cancer. J. Am. Med. Assoc. 265: 1985-1990, 1991.
30. TOOLAN, B. C., SHEA, M., MYERS, E., BORCHERS, R., SEEDOR, J., QUARTUCCIO, H., RODAN, G. AND HAYES, W.: Effects of 4-amino-1-hydroxybutylidene bisphosphonate on bone biomechanics in rats. J. Bone Miner. Res. 7: 1399-1406, 1992.
31. TURNER, C., SATO, M. AND BRYANT, H. U.: Raloxifene preserves bone strength and bone mass in ovariectomized rats. Endocrinology 135: 2001-2005, 1994.
32. VESEY, M. P.: Exogenous hormones in the aetiology of cancer in women. J. R. Soc. Med. 77: 542-549, 1984.
33. WEISS, N. S., URE, C., BALLARD, J. H., WILLIAMS, A. R. AND DALING, J. R.: Decreased risk of fractures of the hip and lower forearm with postmenopausal use of estrogen. N. Engl. J. Med. 303: 1195-1198, 1980.
34. ZIEL, H. K. AND FINKLE, W. D.: Increased risk of endometrial carcinoma among users of conjugated estrogens. N. Engl. J. Med. 293: 1167-1170, 1975.