Update on Raloxifene: Mechanism of Action, Clinical Efficacy, Adverse Effects, and Contraindications

@article{Gizzo2013UpdateOR,
  title={Update on Raloxifene: Mechanism of Action, Clinical Efficacy, Adverse Effects, and Contraindications},
  author={Salvatore Gizzo and Carlo Saccardi and Tito Silvio Patrelli and Roberto Berretta and Giampiero Capobianco and Stefania di Gangi and Antonio Vacilotto and Anna Bertocco and Marco Noventa and Emanuele Ancona and Donato D'Antona and Giovanni Battista Nardelli},
  journal={Obstetrical \& Gynecological Survey},
  year={2013},
  volume={68},
  pages={467–481}
}
Raloxifene is the only selective estrogen receptor modulator approved for long-term treatment in the prevention of osteoporotic fractures and for the reduction of invasive breast cancer risk in postmenopausal women. The demonstrated beneficial effects on bone and mammalian tissue led clinical and molecular research to focus mainly on these organs, giving less attention to all other systemic effects. The aim of this review was to evaluate all described systemic effects of raloxifene… 
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References

SHOWING 1-10 OF 55 REFERENCES
Raloxifene hydrochloride.
  • K. Snyder, N. Sparano, J. M. Malinowski
  • Medicine, Biology
    American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists
  • 2000
TLDR
Raloxifene is an alternative to traditional hormone replacement therapy for the prevention and treatment of osteoporosis in selected postmenopausal women and seemed to reduce the risk of breast cancer and positively influenced blood lipid markers of cardiovascular disease.
Recommendations for raloxifene use in daily clinical practice in the Swiss setting
TLDR
The clinical profiles of postmenopausal women expected to benefit most from therapy with raloxifene were characterized based on published scientific evidence to date and a board of Swiss experts in the fields of menopause and metabolic bone diseases agreed about translating these insights into daily practice.
Effects of raloxifene on serum lipids and coagulation factors in healthy postmenopausal women.
TLDR
Raloxifene favorably alters biochemical markers of cardiovascular risk by decreasing LDL-C, fibrinogen, and lipoprotein(a), and by increasing HDL2-C without raising triglycerides.
Safety and Adverse Effects Associated With Raloxifene: Multiple Outcomes of Raloxifene Evaluation
TLDR
Raloxifene was associated with an increased risk for venous thromboembolism, but there was no increase risk for cataracts, gallbladder disease, endometrial hyperplasia, or endometrian cancer.
Randomized control study of the effects of raloxifene on serum lipids and homocysteine in older women.
TLDR
The results of this study show that raloxifene at a dose of 60 mg/d reduces serum concentrations of low-density lipoprotein cholesterol and total cholesterol in healthy older women and may have a favorable effect on the incidence of cardiovascular disease in older women.
Prevention of osteoporosis and uterine effects in postmenopausal women taking raloxifene for 5 years
TLDR
The main objectives of these analyses are to compare the effect of 5 years of treatment with raloxifene (60 mg/day) with placebo in terms of the likelihood of developing osteoporosis and to evaluate the effect on the endometrium and incidence of vaginal bleeding.
Long-term safety and efficacy of raloxifene in the prevention and treatment of postmenopausal osteoporosis: an update
TLDR
Raloxifene is effective to prevent and treat postmenopausal vertebral osteoporosis, with reduction of spine fractures and, in post-hoc analyses, non-spine fractures in high-risk subjects and the overall risk-benefit profile is favorable.
Raloxifene modulates interleukin-6 and tumor necrosis factor-alpha synthesis in vivo: results from a pilot clinical study.
TLDR
The data show that RAL can modulate circulating levels of cytokines involved in osteoclastogenesis and bone resorption, suggesting that modulation of soluble factors could play a pivotal role in the mechanisms of the osteoprotective effect of RAL.
Reduced incidence of invasive breast cancer with raloxifene among women at increased coronary risk.
TLDR
Raloxifene reduces risk of invasive ER-positive breast cancer regardless of a woman's baseline breast cancer risk but does not reduce risk of noninvasive or ER-negative breast cancers.
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