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Raloxifene

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Raloxifene, Evista

  • See Also
  1. Tamoxifen
  2. Selective Estrogen Receptor Modulator
  • Indications
  1. Osteoporosis Prevention in postmenopausal women
  2. Hormone Replacement in postmenopausal women
    1. Beyond hot flash stage
    2. Estrogen Replacement contraindicated (Breast Cancer)
  3. Breast Cancer Prevention in post-menopausal women
    1. Breast Cancer risk >1.66% in 5 years
  • Contraindications
  1. Venous Thromboembolism
  2. Perioperative period
  3. Prolonged immobilization (discontinue 72 hours before expected immobilization)
  4. History of Cerebrovascular Accident (CVA) or Transient Ischemic Attack (TIA)
  5. Pregnancy
  • Mechanism
  1. See Selective Estrogen Receptor Modulator
  2. Positive Estrogen effects
    1. Stimulates bone mineralization
    2. Improves lipid profile
  3. Anti-Estrogenic effects
    1. No Breast stimulation
    2. No uterine stimulation
  • Dosing
  1. Raloxifene 60 mg orally daily
    1. Course of 5 years if used for breast Cancer Prevention
  • Adverse Effects
  1. See Selective Estrogen Receptor Modulator
  2. Precautions
    1. Thromboembolism and Cardiovascular Risk are FDA black box warnings
  3. Venous Thromboembolism (DVT, PE)
    1. More likely to occur in first 4 months of treatment
    2. Similar to risk with Estrogen Replacement
  4. Cerebrovascular Accident
    1. Avoid in Coronary Artery Disease or cardiovascular disease risk factors
  5. Hot Flashes (Anti-Estrogen effects)
    1. See Hot Flashes for management
    2. Avoid symptomatic management with agents contraindicated following Breast Cancer
      1. Avoid Estrogen and Phytoestrogens
  6. Other effects
    1. Leg Cramps
    2. Hypertriglyceridemia
  • Safety
  1. Avoid in pregnancy
  2. Avoid in Lactation
  • Drug Interactions
  1. Cholestyramine
    1. Avoid with Raloxifene (reduces absorption)
  2. Warfarin
    1. Raloxifene affects INR (monitor)
  3. Highly Protein-Bound Drugs (e.g. Diazepam, Diazoxide, and Lidocaine)
    1. Raloxifene is also highly Protein bound (95%), affecting the serum level of other drugs
  • Efficacy
  1. Lower efficacy than Tamoxifen for breast Cancer Prevention (but lower Venous Thromboembolism, Endometrial Cancer Risks)
  2. No Uterine endometrial stimulation (unlike Estrogen)
    1. Does not require concurrent Progestin use
  3. Does not stimulate Breast tissue (unlike Estrogen)
    1. No Breast swelling, tenderness, or pain
    2. No data yet on Breast Cancer
  4. Increases Bone Mineral Density
    1. Modest effect (1-2%) at hip, spine, and long bones
    2. Not as effective as Estrogen Replacement
  5. Positive lipid effects
    1. Lowers LDL 10-12%
    2. Lowers Total Cholesterol 6-7%
  6. Helps stabilize pelvic floor
    1. Protects against Uterine Prolapse
    2. Decreases Incidence of Urinary Incontinence
    3. Reduces pelvic surgery rate by 50%
    4. Goldstein (2001) Obstet Gynecol 98:91-6 [PubMed]
  • Resources
  1. Raloxifene (DailyMed)
    1. https://www.dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ad3ef791-ac90-4f66-8da6-95b31e4c3eb6
  • Reference
  1. Delmas (1997) N Engl J Med 337:1641-7 [PubMed]
  2. Scott (1999) Am Fam Physician 60:1131-9 [PubMed]