Raloxifene

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Evista, Optruma; Belgium: Evista; Bulgaria: Evista; Cyprus: Evista; Czech Republic: Evista, Optruma; Denmark: Evista; Estonia: Evista, Optruma; Finland: Evista; France: Evista, Optruma; Germany: Evista, Optruma; Greece: Evista, Optruma; Hungary: Evista, Optruma; Ireland: Evista, Optruma, Raloxiep; Italy: Evista, Optruma; Latvia: Evista, Optruma; Lithuania: Optruma; Luxembourg: Evista, Optruma; Malta: Evista, Optruma; Netherlands: Evista, Optruma; Poland: Celvista, Evista, Optruma; Portugal: Evista, Optruma, Raloxifeno; Romania: Evista, Optruma; Slovakia: Evista, Optruma; Slovenia: Evista, Optruma; Spain: Evista, Optruma; Sweden: Evista, Optruma; UK: Evista.

North America

Canada: Evista, Raloxifene; USA: Evista.

Latin America

Argentina: Evista, Ketidin, Raxeto; Brazil: Evista; Mexico: Evista.

Asia

Japan: Evista.

Drug combinations

Chemistry

Raloxifene Hydrochloride: C~28~H~27~NO~4~S HCl. Mw: 510.04. (1) Methanone, [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-, hydrochloride; (2) 6-Hydroxy-2-(p-hydroxyphenyl)benzo[b]thien-3-yl-p-(2-piperidinoethoxy)phenyl ketone, hydrochloride. CAS-82640-04-8; CAS-84449-90-1 (raloxifene)(1988).

Pharmacologic Category

Estrogen Agonist-Antagonists; Selective Estrogen Receptor Modulator. Bone Resorption Inhibitors. (ATC-Code: G03XC01).

Mechanism of action

Affects some, but not all, of the same receptors as estrogen, and in some instances, antagonizes or blocks estrogen. Acts like estrogen to prevent bone loss and has potential to block some estrogen effects in breast and uterine tissues. Decreases bone resorption, increasing bone mineral density and decreasing fracture incidence.

Therapeutic use

Prevention and treatment of osteoporosis in postmenopausal women. Risk reduction for invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women with high risk for invasive breast cancer.

Pregnancy and lactiation implications

Raloxifene should not be used by pregnant women or by women planning to become pregnant. Contraindicated in nursing women.

Unlabeled use

Contraindications

History of or current venous thromboembolic disorders (including DVT, PE, and retinal vein thrombosis). Pregnancy. Breast-feeding.

Warnings and precautions

Risk of death due to stroke may be increased in women with coronary heart disease or in women at risk for coronary events (use with caution in cardiovascular disease). Do not use for prevention of cardiovascular disease. Use with caution in history of cervical/uterine carcinoma, and in hepatic impairment. Women with history of elevated triglycerides in response to treatment with oral estrogens (or estrogen/progestin) may develop elevated triglycerides when treated with raloxifene. Use with caution in moderate-to-severe renal impairment. May increase risk for DVT or PE (use with caution in patients at high risk for venous thromboembolism). Use contraindicated in history of or current venous thromboembolic disorders. Use with caution in unexplained uterine bleeding. Use with systemic estrogen therapy not recommended. Not indicated for treatment of invasive breast cancer, reduction of risk of recurrence of invasive breast cancer, or reduction of risk of noninvasive breast cancer. Efficacy (for breast cancer risk reduction) in women with inherited BRCA1 and BRCA1 mutations not established. Discontinue at least 72 hours prior to and during prolonged immobilization (postoperative recovery or prolonged bedrest).

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