II. Indications
- Osteoporosis Prevention in postmenopausal women
-
Hormone Replacement in postmenopausal women
- Beyond hot flash stage
- Estrogen Replacement contraindicated (Breast Cancer)
- Breast Cancer Prevention in post-menopausal women
- Breast Cancer risk >1.66% in 5 years
III. Contraindications
- Venous Thromboembolism
- Perioperative period
- Prolonged immobilization (discontinue 72 hours before expected immobilization)
- History of Cerebrovascular Accident (CVA) or Transient Ischemic Attack (TIA)
- Pregnancy
IV. Mechanism
- See Selective Estrogen Receptor Modulator
- Positive Estrogen effects
- Stimulates bone mineralization
- Improves lipid profile
- Anti-Estrogenic effects
- No Breast stimulation
- No uterine stimulation
V. Dosing
- Raloxifene 60 mg orally daily
- Course of 5 years if used for breast Cancer Prevention
VI. Adverse Effects
- See Selective Estrogen Receptor Modulator
- Precautions
- Thromboembolism and Cardiovascular Risk are FDA black box warnings
-
Venous Thromboembolism (DVT, PE)
- More likely to occur in first 4 months of treatment
- Similar to risk with Estrogen Replacement
-
Cerebrovascular Accident
- Avoid in Coronary Artery Disease or cardiovascular disease risk factors
-
Hot Flashes (Anti-Estrogen effects)
- See Hot Flashes for management
- Avoid symptomatic management with agents contraindicated following Breast Cancer
- Avoid Estrogen and Phytoestrogens
- Other effects
VII. Safety
- Avoid in pregnancy
- Avoid in Lactation
VIII. Drug Interactions
IX. Efficacy
- Lower efficacy than Tamoxifen for breast Cancer Prevention (but lower Venous Thromboembolism, Endometrial Cancer Risks)
- No Uterine endometrial stimulation (unlike Estrogen)
- Does not require concurrent Progestin use
- Does not stimulate Breast tissue (unlike Estrogen)
- No Breast swelling, tenderness, or pain
- No data yet on Breast Cancer
- Increases Bone Mineral Density
- Modest effect (1-2%) at hip, spine, and long bones
- Not as effective as Estrogen Replacement
- Positive lipid effects
- Lowers LDL 10-12%
- Lowers Total Cholesterol 6-7%
- Helps stabilize pelvic floor
- Protects against Uterine Prolapse
- Decreases Incidence of Urinary Incontinence
- Reduces pelvic surgery rate by 50%
- Goldstein (2001) Obstet Gynecol 98:91-6 [PubMed]
X. Resources
Images: Related links to external sites (from Bing)
Related Studies
| raloxifene (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| RALOXIFENE HCL 60 MG TABLET | Generic | $0.28 each |
Ontology: Raloxifene (C0244404)
| Definition (NCI_NCI-GLOSS) | The active ingredient in a drug used to reduce the risk of invasive breast cancer in postmenopausal women who are at high risk of the disease or who have osteoporosis. It is also used to prevent and treat osteoporosis in postmenopausal women. It is also being studied in the prevention of breast cancer in certain premenopausal women and in the prevention and treatment of other conditions. Raloxifene blocks the effects of the hormone estrogen in the breast and increases the amount of calcium in bone. It is a type of selective estrogen receptor modulator (SERM). |
| Definition (NCI) | A selective benzothiophene estrogen receptor modulator (SERM). Raloxifene binds to estrogen receptors (ER) as a mixed estrogen agonist/antagonist; it displays both an ER-alpha-selective partial agonist/antagonist effect and a pure ER-beta-selective antagonist effect. This agent functions as an estrogen agonist in some tissues (bones, lipid metabolism) and as an estrogen antagonist in others (endometrium and breasts), with the potential for producing some of estrogen's beneficial effects without producing its adverse effects. (NCI04) |
| Definition (CSP) | a selective estrogen receptor modulator; has both agonist and antagonist estrogen action. |
| Definition (MSH) | A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue. |
| Definition (PDQ) | A selective benzothiophene estrogen receptor modulator (SERM). Raloxifene binds to estrogen receptors (ER) as a mixed estrogen agonist/antagonist; it displays both an ER-alpha-selective partial agonist/antagonist effect and a pure ER-beta-selective antagonist effect. This agent functions as an estrogen agonist in some tissues (bones, lipid metabolism) and as an estrogen antagonist in others (endometrium and breasts), with the potential for producing some of estrogen's beneficial effects without producing its adverse effects. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43109&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43109&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1518" NCI Thesaurus) |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D020849 |
| SnomedCT | 109029006, 419530003 |
| LNC | LP171633-3 |
| English | Methanone, (6-hydroxy-2-(4-hydroxyphenyl)benzo(b)thien-3-yl)(4-(2-(1-piperidinyl)ethoxy)phenyl)-, raloxifene, [6-Hydroxy-2-(4-hydroxyphenyl)-benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone, raloxifene (medication), Raloxifene, Raloxifene [Chemical/Ingredient], RALOXIFENE, Raloxifene (substance), RALOX, Keoxifene, Raloxifene (product) |
| Spanish | raloxifeno (producto), raloxifeno (sustancia), raloxifeno, Raloxifeno |
| Swedish | Raloxifen |
| Czech | raloxifen |
| Finnish | Raloksifeeni |
| Russian | RALOKSIFEN, РАЛОКСИФЕН |
| Italian | Keoxifene, Raloxifene |
| Polish | Raloksyfen |
| Japanese | ケオキシフェン, ラロキシフェン |
| French | Raloxifène |
| German | Raloxifen |
| Portuguese | Raloxifeno |
Ontology: Evista (C0720318)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D020849 |
| English | ELi Lilly Brand of Raloxifene, Lilly Brand of Raloxifene, Raloxifene Lilly Brand, evista, Evista |
