raloxifene (Evista)
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Introduction
Tradename: raloxifene.
Indications
- prevention & treatment of osteoporosis*
- reduces risk of vertebral fractures, RR=0.65[9]
- 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
Tabs: 60 mg
Pharmacokinetics
- rapidly absorbed after oral administration
- 60% absorption of oral dose
- extensive pre-systemic glucuronidation
- absolute bioavailability is 2%
- may be administered without regard to meals
- volume of distribution 2348 L/kg
- protein binding > 95%
- binds to albumin & alpha-1 acid glycoprotein
- elimination 1/2 life of 28 hours
- glucuronide eliminated the feces
elimination via liver
protein binding = >95 %
1/2life = 28 hours
Adverse effects
- leg cramps
- hot flashes
- increased risk of thrombosis, RR=1.44[7][9]
- uterine cramps
- increased risk of fatal stroke, RR=1.47[9]
- NOT associated with increased risk of uterine bleeding or endometrial cancer[6]
- cataracts[11]
Drug interactions
- warfarin: coadministration of raloxifene may diminish prothrombin time by 10%
- cholestyramine causes a 60% reduction in raloxifene levels after a single dose
- ampicillin & amoxicillin decrease raloxifene levels
Mechanism of action
- estrogen receptor agonist/antagonist
- does not stimulate uterus or breast tissue
- decreases vertebral fractures by up to 50% in women who take it for 3 years
- reduces homocysteine serum levels[3]
- improves lipid patterns
More general terms
Additional terms
References
- ↑ The Prescriber's Letter, vol 6 #11, Nov 1999
- ↑ Prescriber's Letter 8(8):46, 2001
- ↑ 3.0 3.1 Solomon D. In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 12-15, 2001
- ↑ Prescriber's Letter 9(3):16 2002
- ↑ Physician's Desk Reference (PDR) 56th edition, 2002
- ↑ 6.0 6.1 6.2 6.3 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 - ↑ 7.0 7.1 7.2 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: https://www.ncbi.nlm.nih.gov/pubmed/15458908
- ↑ 8.0 8.1 Prescriber's Letter 12(2): 2005 Role of Raloxifene in Breast Cancer Prevention: CORE Results Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=210214&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 9.0 9.1 9.2 9.3 9.4 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: https://www.ncbi.nlm.nih.gov/pubmed/16837676
Stefanick ML Risk-benefit profiles of raloxifene for women N Engl J Med 2006; 355:190 PMID: https://www.ncbi.nlm.nih.gov/pubmed/16837684 - ↑ 10.0 10.1 Prescriber's Letter 14(10): 2007 Evista (Raloxifene) Approved for Breast Cancer Prevention Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=231012&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 11.0 11.1 11.2 Medical Knowledge Self Assessment Program (MKSAP) 18, American College of Physicians, Philadelphia 2018