Raloxifene is a SERM drug with both bone protection and breast cancer risk reduction. It is mainly used for postmenopausal women, with good tissue selectivity and safety. It is one of the important treatment options for risk management of osteoporosis combined with breast cancer.

1、 Drug name

1. Common name: Raloxifene

2. Product Name: EVISTA ®

2、 Indications

EVISTA ® It is an estrogen agonist/antagonist (selective estrogen receptor modulator, SERM) suitable for:

1. Treatment and prevention of osteoporosis in postmenopausal women.

2. Reduce the risk of invasive breast cancer in postmenopausal women with osteoporosis.

3. Reduce the risk of invasive breast cancer in postmenopausal women with a high risk of invasive breast cancer.

Important use restrictions: EVISTA is not applicable to the treatment of invasive breast cancer, reducing the risk of recurrence of breast cancer or reducing the risk of non invasive breast cancer.

3、 Specifications and characteristics

Tablets, each containing 60 milligrams of raloxifene hydrochloride (equivalent to 55.71 milligrams of free base)

4、 Main components

Active ingredient: Raloxifene hydrochloride.

5、 Usage and dosage

1. Recommended dosage: Take one tablet (60mg) once a day orally.

2. Medication time: It can be taken at any time of the day without considering meals.

3. Calcium and vitamin D supplementation: When treating or preventing osteoporosis, if the daily intake is insufficient, calcium and/or vitamin D should be supplemented. Postmenopausal women need an average of 1500 milligrams of elemental calcium per day. The recommended daily intake of vitamin D is 400-800IU.

6、 Dose adjustment

For specific populations (such as those with liver and kidney dysfunction), please refer to the "Special Population Medication" section for usage recommendations.

7、 Medication precautions

1. Missed dose: The general principle is that if you remember that it is close to the next dose, you should skip the missed dose and take the next dose according to the original plan. Do not take double the dose.

2. Vomiting: When vomiting occurs, it is not recommended to take additional medication and wait until the next scheduled medication time.

3. Co administration with food: May or may not be co administered with food. High fat foods increase absorption but do not result in clinically significant systemic exposure changes.

4. Activity restriction period: EVISTA should be discontinued at least 72 hours before and during planned long-term inactivity (such as postoperative recovery or long-term bed rest), and medication should be resumed after the patient is fully active. Patients should be advised to engage in regular activities during prolonged travel.

5. Breast examination: Regular breast examinations and mammography should be conducted in accordance with good medical practice before and during EVISTA treatment.

8、 Medication for special populations

1. Pregnant women: Do not use. EVISTA may cause harm to the fetus. Women of childbearing age should take effective contraceptive measures during the period of use and when plasma drugs can be tested after discontinuation of medication.

2. Breastfeeding women: not applicable to women of childbearing age. There is currently no information indicating whether raloxifene is present in human milk.

3. Children: Safety and efficacy have not yet been established.

4. Elderly people (≥ 65 years old): No need to adjust dosage. No overall differences in safety or efficacy were observed in clinical studies compared to young patients.

5. Pre menopausal women: Not recommended for use, safety and efficacy have not yet been established.

6. Patients with liver and kidney dysfunction: Patients with liver dysfunction should use it with caution. Mild liver dysfunction patients may have elevated plasma drug concentrations. Patients with moderate to severe renal insufficiency should use it with caution, as male patients with renal insufficiency have elevated plasma drug concentrations. It is recommended to monitor adverse reactions in this population.

9、 Adverse reactions

1. Common adverse reactions (incidence>2% and higher than placebo group) include:

Hot flashes: One of the most common adverse reactions, especially in the early stages of treatment.

Leg spasms.

Peripheral edema.

Influenza syndrome.

Joint pain.

Sweating.

2. Serious risk:

Venous thromboembolism: including increased risk of deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis. The risk is highest in the first 4 months of treatment.

Lethal stroke: In a trial targeting postmenopausal women with coronary heart disease or increased risk of coronary heart disease, an increased risk of death due to stroke was observed in the EVISTA group (1.2% vs. 0.8%). For women at risk of stroke, it is necessary to weigh the risks and benefits.

10、 Contraindications

1. Active or previous history of venous thromboembolism, including deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis.

2. Pregnant women.

11、 Drug interactions

1. Kaolaienamine (and other anion exchange resins): Not recommended for combination use. It will significantly reduce the absorption and enterohepatic circulation of raloxifene.

2. Warfarin: When starting or stopping EVISTA treatment, prothrombin time should be monitored more closely.

3. Other high protein binding drugs, such as diazepam, diazepam, and lidocaine, should be used in combination with caution. The binding rate of raloxifene to plasma proteins exceeds 95%, which may affect the protein binding of other drugs.

4. Systemic estrogen: Not recommended for combination use, safety has not been established.

12、 Storage method

1. Store at a controlled room temperature of 20 ° C to 25 ° C (68 ° F to 77 ° F).

2. Allow brief fluctuations between 15 ° C and 30 ° C (59 ° F and 86 ° F).

Raloxifeneinformation