Gynecology Book

http://www.fpnotebook.com/

EvistaAka: Raloxifene, Droloxifene, Idoxifene, Toremifene, Selective Estrogen Receptor Modulator, SERM

Advertisement

  1. See Also
    1. Tamoxifen
  2. Mechanism
    1. Positive Estrogen effects
      1. Stimulates bone mineralization
      2. Improves lipid profile
    2. Anti-Estrogenic effects
      1. No breast stimulation
      2. No uterine stimulation
  3. Indication
    1. Osteoporosis Prevention in postmenopausal women
    2. Hormone Replacement in postmenopausal women
      1. Beyond hot flash stage
      2. Estrogen Replacement contraindicated (Breast Cancer)
  4. Advantages
    1. No Uterine endometrial stimulation (unlike Estrogen)
      1. Does not require concurrent Progestin use
    2. Does not stimulate breast tissue (unlike Estrogen)
      1. No breast swelling, tenderness, or pain
      2. No data yet on Breast Cancer
    3. Increases Bone Mineral Density
      1. Modest effect (1-2%) at hip, spine, and long bones
      2. Not as effective as Estrogen Replacement
    4. Positive lipid effects
      1. Lowers LDL 10-12%
      2. Lowers Total Cholesterol 6-7%
    5. 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
  5. Disadvantages
    1. Expensive: $65/month (Premarin is $20/month)
    2. Anti-Estrogen effects (Hot Flashes)
  6. Adverse Effects
    1. Hot Flashes (24.6%)
    2. Leg cramps (5.9%)
    3. Increased Deep Vein Thrombosis and thromboembolism risk
      1. More likely to occur in first 4 months of treatment
      2. Similar to risk with Estrogen Replacement
  7. Dosing
    1. Raloxifene 60 mg PO qd
  8. Reference
    1. Delmas (1997) N Engl J Med 337:1641
    2. Scott (1999) Am Fam Physician 60:1131

droloxifene (C0047498)

Definition (NCI)A phenolic analogue of tamoxifen, a nonsteroidal selective estrogen receptor modulator (SERM). Droloxifene competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA. The result is a reduction in DNA synthesis and cellular response to estrogen. (NCI)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC038345
English3-hydroxytamoxifen, droloxifene, meta-hydroxytamoxifen
Parent ConceptsSelective Estrogen Receptor Modulators (C0732611)
SourcesMSH, MTH, NCI
Derived from the NIH UMLS (Unified Medical Language System)


Toremifene (C0076836)

Definition (MSH)A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue.
Definition (NCI)An anticancer drug that belongs to the family of drugs called antiestrogens. Toremifene blocks the effect of the hormone estrogen in the body. It may help control some cancers from growing, and it may delay or reduce the risk of cancer recurrence.
Definition (PDQ)A nonsteroidal triphenylethylene antiestrogen. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator (SERM). This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene also has intrinsic estrogenic properties, which are manifested according to tissue type or species. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41103&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41103&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1256" NCI Thesaurus)
Definition (NCI)A nonsteroidal triphenylethylene antiestrogen. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator (SERM). This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene also has intrinsic estrogenic properties, which are manifested according to tissue type or species. (NCI04)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD017312
EnglishTOR, Toremifene, TOREMIFENE PREPARATION
Spanishtoremifeno
Parent ConceptsTamoxifen (C0039286), Selective Estrogen Receptor Modulators (C0732611), [AN500] ANTINEOPLASTIC HORMONES (C0991595), Estrogen Antagonists (C0014930), Drug allergen (C1320237)
SourcesMSH, MTH, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


pyrrolidino-4-iodotamoxifen (C0139560)

Definition (NCI)A drug that blocks the effects of estrogen.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC071362
English4-iodopyrrolidinotamoxifen, idoxifene, Pyr-I-Tam, pyrrolidino-4-iodotamoxifen
Parent ConceptsSelective Estrogen Receptor Modulators (C0732611)
SourcesMSH, NCI, PDQ
Derived from the NIH UMLS (Unified Medical Language System)


Raloxifene (C0244404)

Definition (CSP)a selective estrogen receptor modulator; has both agonist and antagonist estrogen action.
Definition (NCI)A drug that belongs to the family of drugs called selective estrogen receptor modulators (SERMs) and is used in the prevention of osteoporosis in postmenopausal women. Raloxifene is also being studied as a cancer prevention drug.
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)
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)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD020849
EnglishKeoxifene, RALOX, Raloxifene, RALOXIFENE PREPARATION
Spanishraloxifeno
Parent ConceptsEstrogen Antagonists (C0014930), Estrogens, Synthetic (C0014941), Selective Estrogen Receptor Modulators (C0732611), Tamoxifen (C0039286), [HS900] HORMONES/SYNTHETICS/MODIFIERS, OTHER (C0991612), Bone resorption inhibitor (C0521941), Drug allergen (C1320237)
SourcesCSP, MSH, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Evista (C0720318)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD020849
EnglishELi Lilly Brand of Raloxifene, Evista, Lilly Brand of Raloxifene, Raloxifene Lilly Brand
SourcesCSP, MSH, NCI, PDQ, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Selective Estrogen Receptor Modulators (C0732611)

Definition (NCI)(sel-EK-tiv ESS-tro-jen re-SEP-tor MOD-yew-lay-tor) SERM. A drug that acts like estrogen on some tissues but blocks the effect of estrogen on other tissues. Tamoxifen and raloxifene are SERMs.
Definition (NCI)Selective estrogen receptor modulator. A drug that acts like estrogen on some tissues but blocks the effect of estrogen on other tissues. Tamoxifen and raloxifene are SERMs.
Definition (MSH)A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63)
Definition (CSP)structurally diverse group of compounds distinguished from estrogen by their ability to bind and activate the estrogen receptor, but act as either an estrogen agonist or antagonist depending on the tissue type and hormonal milieu; classified as either first generation because they demonstrate estrogen agonist properties in the endometrium or second generation based on their patterns of tissue specificity.
ConceptsPharmacologic Substance (T121)
MSHD020845
EnglishESTROGEN RECEPT MODULATORS SELECTIVE, SELECTIVE ESTROGEN RECEPT MODULATORS, Selective Estrogen Receptor Modifying Agents, Selective estrogen receptor modulator, Selective Estrogen Receptor Modulators, Selective oestrogen receptor modulator, SERM, SERM - Selective estrogen receptor modulator, SERM - Selective oestrogen receptor modulator, SERMs
Spanishmodulador selectivo de receptor de estrogeno, modulador selectivo del receptor de estrogeno, modulador selectivo del receptor estrogenico
Parent ConceptsHormones (C0019932), Estrogen Receptor Modulators (C0752229), Estrogen Antagonists (C0014930), Chemopreventive Agent (C1516463), Steroid Receptor Modulators (C1373061), Synthetic antiestrogen (C0521963), Sex Hormones/Modifiers (C1579311)
SourcesCSP, MSH, NCI, NDFRT, SCTSPA, SNOMEDCT, USPMG
Derived from the NIH UMLS (Unified Medical Language System)



Navigation Tree