Description

Simple

A medication used to prevent bone loss and treat breast cancer in postmenopausal women.

Clinical

A selective estrogen receptor modulator that is used to prevent and treat osteoporosis and reduce the risk of invasive breast cancer in high-risk postmenopausal women.

Overview

Raloxifene is a second generation selective estrogen receptor modulator (SERM) that mediates anti-estrogenic effects on breast and uterine tissues, and estrogenic effects on bone, lipid metabolism, and blood coagulation.[6,12] Exhibiting tissue-specific effects distinct from [estradiol], raloxifene is the first of the benzothiophene group of antiestrogens to be labelled a SERM.[7] Available in many countries worldwide, raloxifene was initially approved by the FDA in December, 1997 under the market name Evista® for the management and prevention of osteoporosis in postmenopausal women and reduction in risk for invasive breast cancer in postmenopausal women with osteoporosis or those who are at high risk for invasive breast cancer. However, it has a negligible effect on altering the development and progression of breast cancer itself.[label] The most common causes of osteoporosis include postmenopausal deficiency of estrogen and age-relate... Read more

Pharmacology

Indication

Indicated for the prevention and treatment of osteoporosis in postmenopausal women, as well as prevention and treatment of corticosteroid-induced bone loss.[label]

Indicated for the reduction in the risk of invasive breast cancer in postmenopausal women with osteoporosis or postmenopausal women w... Read more

Pharmacodynamic

Raloxifene belongs to the selective estrogen receptor modulator (SERM) drug class that exhibits estrogenic effects on bone and lipid metabolism while mediating anti-estrogenic effects on uterine endometrium and breast tissues.[ Read more

Mechanism of action

Raloxifene is a selective estrogen receptor modulator that acts as both an estrogen agonist and antagonist via differential effects on the tissue-specific estrogen receptors. Based on the findings of competitive binding assays, raloxifene displays binding affinity that is similar to that of [estradi... Read more

Absorption

Raloxifene is well absorbed from the gastrointestinal tract, with approximately 60% fo the drug being absorbed following oral administration.[ Read more

Protein binding

About 95% of raloxifene and its glucuronide metabolites are bound to plasma proteins.[label] Although this is a relatively high protein binding profile, _in vitro_ studies suggest that raloxifene and its metabolites do not significantly interact with binding of highly protein-bound drugs.[ Read more

Volume of distribution

Following oral administration of single doses randing from 30 to 150 mg in postmenopausal women, the volume of distribution was about 2348 L/kg. Following oral administration of multiple doses, the value increased to 2853 L/kg. Raloxifene is widely distributed in the tissues. It is not known whether... Read more

Clearance

Following intravenous administration, raloxifene was shown to be cleared at a rate approximating hepatic blood flow. The apparent oral clearance is reported to be 44.1 L/kgxhr. The clearance can range from 40 to 60L/kgxhr following chronic dosing. In healthy postmenopausal women receiving multiple o... Read more

Half life

The average plasma elimination half-life of raloxifene ranges from 27 to 32 hours.[7, Read more

Route of elimination

Raloxifene predominantly undergoes fecal excretion, with less than 0.2% of the dose being excreted in the urine as unchanged form of the compound and less than 6% of the dose being excreted as glucuronide conjugates. Co-administration with [cholestyramine], a bile acid sequestrant, was shown to redu... Read more

Toxicity

**LD50 and Overdose**

The oral LD50 value in rats is > 5000 mg/kg, which is about 810 times the human dose.[MSDS] In monkeys, no mortality was seen after a single oral dose of 1000 mg/kg.[label] No cases of raloxifene overdose have been reported during clinical trials. A rar... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Hot Flashes US
  • postmenopausal
  • Kind: experimental
    • Percent: 24.6
  • Kind: placebo
    • Percent: 18.3
  • Clinical Trial
    Arthralgia US
    • postmenopausal
  • Kind: experimental
    • Percent: 15.5
  • Kind: placebo
    • Percent: 14
  • Clinical Trial
    Infection US
    • postmenopausal
  • Kind: experimental
    • Percent: 15.1
  • Kind: placebo
    • Percent: 14.6
  • Clinical Trial
    Flu syndrome US
    • postmenopausal
  • Kind: experimental
    • Percent: 14.6
  • Kind: placebo
    • Percent: 13.5
  • Clinical Trial
    Peripheral Edema US
    • postmenopausal
  • Kind: experimental
    • Percent: 14.1
  • Kind: placebo
    • Percent: 11.7
  • Clinical Trial
    Flu syndrome US
    • postmenopausal
  • Kind: experimental
    • Percent: 13.5
  • Kind: placebo
    • Percent: 11.4
  • Clinical Trial
    Muscle Spasms US
    • postmenopausal
  • Kind: experimental
    • Percent: 12.1
  • Kind: placebo
    • Percent: 8.3
  • Clinical Trial
    Arthralgia US
    • postmenopausal
  • Kind: experimental
    • Percent: 10.7
  • Kind: placebo
    • Percent: 10.1
  • Clinical Trial
    Sinusitis US
    • postmenopausal
  • Kind: experimental
    • Percent: 10.3
  • Kind: placebo
    • Percent: 6.5
  • Clinical Trial
    Rhinitis US
    • postmenopausal
  • Kind: experimental
    • Percent: 10.2
  • Kind: placebo
    • Percent: 10.1
  • Clinical Trial
    Hot Flashes US
    • postmenopausal
  • Kind: experimental
    • Percent: 9.7
  • Kind: placebo
    • Percent: 6.4
  • Clinical Trial
    Bronchitis US
    • postmenopausal
  • Kind: experimental
    • Percent: 9.5
  • Kind: placebo
    • Percent: 8.6
  • Clinical Trial
    Cough increased US
    • postmenopausal
  • Kind: experimental
    • Percent: 9.3
  • Kind: placebo
    • Percent: 9.2
  • Clinical Trial
    Headache US
    • postmenopausal
  • Kind: experimental
    • Percent: 9.2
  • Kind: placebo
    • Percent: 8.5
  • Clinical Trial
    Weight Gain US
    • postmenopausal
  • Kind: experimental
    • Percent: 8.8
  • Kind: placebo
    • Percent: 6.8
  • Clinical Trial
    Nausea US
    • postmenopausal
  • Kind: experimental
    • Percent: 8.8
  • Kind: placebo
    • Percent: 8.6
  • Clinical Trial
    Nausea US
    • postmenopausal
  • Kind: experimental
    • Percent: 8.3
  • Kind: placebo
    • Percent: 7.8
  • Clinical Trial
    Sinusitis US
    • postmenopausal
  • Kind: experimental
    • Percent: 7.9
  • Kind: placebo
    • Percent: 7.5
  • Clinical Trial
    Hot Flashes US
    • postmenopausal
  • Kind: experimental
    • Percent: 7.8
  • Kind: placebo
    • Percent: 4.7
  • Clinical Trial
    Myalgia US
    • postmenopausal
  • Kind: experimental
    • Percent: 7.7
  • Kind: placebo
    • Percent: 6.2
  • Clinical Trial
    Pharyngitis US
    • postmenopausal
  • Kind: experimental
    • Percent: 7.6
  • Kind: placebo
    • Percent: 7.2
  • Clinical Trial
    Diarrhea US
    • postmenopausal
  • Kind: experimental
    • Percent: 7.2
  • Kind: placebo
    • Percent: 6.9
  • Clinical Trial
    Leg cramps US
    • postmenopausal
  • Kind: experimental
    • Percent: 7
  • Kind: placebo
    • Percent: 3.7
  • Clinical Trial
    Depression US
    • postmenopausal
  • Kind: experimental
    • Percent: 6.4
  • Kind: placebo
    • Percent: 6
  • Clinical Trial
    Cough increased US
    • postmenopausal
  • Kind: experimental
    • Percent: 6
  • Kind: placebo
    • Percent: 5.7
  • Clinical Trial
    Dyspepsia US
    • postmenopausal
  • Kind: experimental
    • Percent: 5.9
  • Kind: placebo
    • Percent: 5.8
  • Clinical Trial
    Leg cramps US
    • postmenopausal
  • Kind: experimental
    • Percent: 5.9
  • Kind: placebo
    • Percent: 1.9
  • Clinical Trial
    Rash US
    • postmenopausal
  • Kind: experimental
    • Percent: 5.5
  • Kind: placebo
    • Percent: 3.8
  • Clinical Trial
    Insomnia US
    • postmenopausal
  • Kind: experimental
    • Percent: 5.5
  • Kind: placebo
    • Percent: 4.3
  • Clinical Trial
    Pharyngitis US
    • postmenopausal
  • Kind: experimental
    • Percent: 5.3
  • Kind: placebo
    • Percent: 5.1
  • Clinical Trial
    Peripheral Edema US
    • postmenopausal
  • Kind: experimental
    • Percent: 5.2
  • Kind: placebo
    • Percent: 4.4
  • Clinical Trial
    Vomiting US
    • postmenopausal
  • Kind: experimental
    • Percent: 4.8
  • Kind: placebo
    • Percent: 4.3
  • Clinical Trial
    Cystitis US
    • postmenopausal
  • Kind: experimental
    • Percent: 4.6
  • Kind: placebo
    • Percent: 4.5
  • Clinical Trial
    Vaginitis US
    • postmenopausal
  • Kind: experimental
    • Percent: 4.3
  • Kind: placebo
    • Percent: 3.6
  • Clinical Trial
    Vertigo US
    • postmenopausal
  • Kind: experimental
    • Percent: 4.1
  • Kind: placebo
    • Percent: 3.7
  • Clinical Trial
    Urinary Tract Infection US
    • postmenopausal
  • Kind: experimental
    • Percent: 4
  • Kind: placebo
    • Percent: 3.9
  • Clinical Trial
    Arthritis US
    • postmenopausal
  • Kind: experimental
    • Percent: 4
  • Kind: placebo
    • Percent: 3.6
  • Clinical Trial
    Chest Pain US
    • postmenopausal
  • Kind: experimental
    • Percent: 4
  • Kind: placebo
    • Percent: 3.6
  • Clinical Trial
    Fever US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.9
  • Kind: placebo
    • Percent: 3.8
  • Clinical Trial
    Tendon disorder US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.6
  • Kind: placebo
    • Percent: 3.1
  • Clinical Trial
    Vomiting US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.4
  • Kind: placebo
    • Percent: 3.3
  • Clinical Trial
    Cholelithiasis US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.3
  • Kind: placebo
    • Percent: 2.6
  • Clinical Trial
    Leukorrhea US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.3
  • Kind: placebo
    • Percent: 1.7
  • Clinical Trial
    Cystitis US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.3
  • Kind: placebo
    • Percent: 3.1
  • Clinical Trial
    Peripheral Edema US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.3
  • Kind: placebo
    • Percent: 1.9
  • Clinical Trial
    Gastrointestinal Disorder US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.3
  • Kind: placebo
    • Percent: 2.1
  • Clinical Trial
    Uterine disorder US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.3
  • Kind: placebo
    • Percent: 2.3
  • Clinical Trial
    Endometrial Disorder US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.1
  • Kind: placebo
    • Percent: 1.9
  • Clinical Trial
    Sweating US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.1
  • Kind: placebo
    • Percent: 1.7
  • Clinical Trial
    Flatulence US
    • postmenopausal
  • Kind: experimental
    • Percent: 3.1
  • Kind: placebo
    • Percent: 2.4
  • Clinical Trial

    Contraindications

    • Sex Group: female
    • Regions: US
    • Age Groups:
      • postmenopausal
      • premenopausal
    • Patient Conditions:
        • Name: Nursing Women
        • Drugbank Id: DBCOND0050656
    • Sex Group: female
    • Regions: US
    • Age Groups:
      • postmenopausal
      • premenopausal
    • Patient Conditions:
        • Name: Potential for pregnancy
        • Drugbank Id: DBCOND0108358
        • Name: Pregnancy
        • Drugbank Id: DBCOND0018394
    • Sex Group: female
    • Regions: US
    • Age Groups:
      • postmenopausal
    • Patient Conditions:
        • Name: Venous Thromboembolism
        • Drugbank Id: DBCOND0000676
        • Name: Pulmonary Embolism
        • Drugbank Id: DBCOND0027915
        • Name: Deep Vein Thrombosis
        • Drugbank Id: DBCOND0029964
        • Name: Retinal Vein Thrombosis
        • Drugbank Id: DBCOND0037936

    Food Interactions

    Avoid excessive or chronic alcohol consumption. Excessive and chronic alcohol consumption may be associated with vitamin D deficiency.

    Take with or without food. The absorption is unaffected by food.