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raloxifene (Evista)

Tradename: raloxifene. Indications: 1) prevention & treatment of osteoporosis* - reduces risk of vertebral fractures, RR=0.65 [9] 2) reduces risk of invasive breast cancer RR=0.56 [6,9,10] (see MORE-CORE trial [7,8] & STAR trial) * indicated only for women who cannot take estrogen [6] Contraindications: - history of or risk for deep vein thrombosis Dosage: - 60 mg PO QD - stop hormone replacement (estrogens) for 1 month prior to starting raloxifene Tabs: 60 mg Pharmacokinetics: 1) rapidly absorbed after oral administration 2) 60% absorption of oral dose 3) extensive pre-systemic glucuronidation 4) absolute bioavailability is 2% 5) may be administered without regard to meals 6) volume of distribution 2348 L/kg 7) protein binding > 95% -> binds to albumin & alpha-1 acid glycoprotein 8) elimination 1/2 life of 28 hours 9) glucuronide eliminated the feces Adverse effects: 1) leg cramps 2) hot flashes 3) increased risk of thrombosis, RR=1.44 [7,9] - lower risk than with tamoxifen [11] 4) uterine cramps 5) increased risk of fatal stroke, RR=1.47 [9] 6) NOT associated with increased risk of uterine bleeding or endometrial cancer [6] 7) cataracts [11] Drug interactions: 1) warfarin: coadministration of raloxifene may diminish prothrombin time by 10% 2) cholestyramine causes a 60% reduction in raloxifene levels after a single dose 3) ampicillin & amoxicillin decrease raloxifene levels Mechanism of action: 1) estrogen receptor agonist/antagonist 2) does not stimulate uterus or breast tissue 3) decreases vertebral fractures by up to 50% in women who take it for 3 years 4) reduces homocysteine serum levels [3] 5) improves lipid patterns

Interactions

drug interactions

Related

MORE-CORE trial Study of Tamoxifen And Raloxifene (STAR)

General

estrogen antagonist

Properties

MISC-INFO: elimination route LIVER protein-binding >95% 1/2life 28 HOURS

Database Correlations

PUBCHEM correlations

References

  1. The Prescriber's Letter, vol 6 #11, Nov 1999
  2. Prescriber's Letter 8(8):46, 2001
  3. Solomon D. In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 12-15, 2001
  4. Prescriber's Letter 9(3):16 2002
  5. Physician's Desk Reference (PDR) 56th edition, 2002
  6. Geriatrics Review Syllabus, American Geriatrics Society, 5th edition, 2002-2004 - Geriatric Review Syllabus, 8th edition (GRS8) Durso SC and Sullivan GN (eds) American Geriatrics Society, 2013
  7. Journal Watch 24(22):167-68, 2004 Grady D, Ettinger B, Moscarelli E, Plouffe L Jr, Sarkar S, Ciaccia A, Cummings S; Multiple Outcomes of Raloxifene Evaluation Investigators. Safety and adverse effects associated with raloxifene: multiple outcomes of raloxifene evaluation. Obstet Gynecol. 2004 Oct;104(4):837-44. PMID: 15458908
  8. Prescriber's Letter 12(2): 2005 Role of Raloxifene in Breast Cancer Prevention: CORE Results Detail-Document#: 210214 (subscription needed) http://www.prescribersletter.com
  9. Barrett-Connor E et al, Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women. N Engl J Med 2006; 355:125 PMID: 16837676 - Stefanick ML Risk-benefit profiles of raloxifene for women N Engl J Med 2006; 355:190 PMID: 16837684
  10. Prescriber's Letter 14(10): 2007 Evista (Raloxifene) Approved for Breast Cancer Prevention Detail-Document#: 231012 (subscription needed) http://www.prescribersletter.com
  11. Medical Knowledge Self Assessment Program (MKSAP) 18, American College of Physicians, Philadelphia 2018