Raloxifene 60mg Tablets
WARNING: This drug may raise the chance of blood clots. Do not take this drug if you have a blood clot or have had blood clots in the past. Talk with your doctor.This drug may raise the chance of dying from stroke in people with heart disease or who have a risk for heart disease. Talk with your doctor. @ COMMON USES: It is used to treat or prevent soft, brittle bones (osteoporosis) in patients who have been through menopause (change of life).It is used to help prevent breast cancer after menopause in people who have soft, brittle bones (osteoporosis) or in those with a higher chance of getting breast cancer.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Selective Estrogen Receptor Modulator (SERM)
Pharmacologic Class
Selective Estrogen Receptor Modulator (SERM)
Pregnancy Category
Category X
FDA Approved
Dec 1997
DEA Schedule
Not Controlled
Overview
What is this medicine?
Raloxifene is a medication used by postmenopausal women to prevent and treat osteoporosis (thinning bones) and to reduce the risk of invasive breast cancer. It works by acting like estrogen in some parts of the body, like bones, to keep them strong, but blocks estrogen's effects in other parts, like the breast.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food. Continue taking it even if you feel well, unless your doctor or healthcare provider advises you to stop.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding bathrooms. Keep all medications in a safe location, out of reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. If you have questions about disposal, consult your pharmacist. You may also want to check if there are drug take-back programs available in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food. Continue taking it even if you feel well, unless your doctor or healthcare provider advises you to stop.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding bathrooms. Keep all medications in a safe location, out of reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. If you have questions about disposal, consult your pharmacist. You may also want to check if there are drug take-back programs available in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
Lifestyle & Tips
- Ensure adequate intake of calcium and vitamin D through diet or supplements.
- Engage in regular weight-bearing exercise (e.g., walking, jogging, dancing) as recommended by your doctor.
- Avoid prolonged periods of immobility, especially after surgery or during long travel.
- Quit smoking and limit alcohol intake, as these can negatively impact bone health.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
60 mg orally once daily
Dose Range:
60 - 60 mg
Condition-Specific Dosing:
Osteoporosis Prevention and Treatment:
60 mg orally once daily
Reduction in Risk of Invasive Breast Cancer in Postmenopausal Women with Osteoporosis:
60 mg orally once daily
Reduction in Risk of Invasive Breast Cancer in Postmenopausal Women at High Risk for Invasive Breast Cancer:
60 mg orally once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required
Moderate:
No dose adjustment required
Severe:
Use with caution; limited data available. Consider potential for increased exposure.
Dialysis:
Not studied; use with caution. Raloxifene is highly protein-bound and unlikely to be removed by dialysis.
Hepatic Impairment:
Mild:
Use with caution; increased exposure expected.
Moderate:
Not recommended; significantly increased exposure expected.
Severe:
Not recommended; significantly increased exposure expected.
Pharmacology
Mechanism of Action
Raloxifene is a selective estrogen receptor modulator (SERM) that acts as an estrogen agonist in some tissues (e.g., bone, lipid metabolism) and an estrogen antagonist in others (e.g., breast, uterus). In bone, it decreases bone resorption and increases bone mineral density. In the breast, it inhibits estrogen-stimulated growth of breast cancer cells. It does not stimulate the endometrium.
Pharmacokinetics
Absorption:
Bioavailability:
2%
Tmax:
Approximately 6 hours (for raloxifene and its glucuronide metabolites)
FoodEffect:
Food does not significantly affect absorption or systemic exposure.
Distribution:
Vd:
2348 L/kg (apparent volume of distribution)
ProteinBinding:
Approximately 98-99% (primarily to albumin and alpha1-acid glycoprotein)
CnssPenetration:
Limited
Elimination:
HalfLife:
27.7 hours (for raloxifene and its glucuronide metabolites)
Clearance:
Not available (due to extensive first-pass metabolism)
ExcretionRoute:
Primarily fecal (approximately 93% of dose), with less than 6% excreted in urine.
Unchanged:
Less than 0.2% (in urine)
Pharmacodynamics
OnsetOfAction:
Bone effects: Not immediately apparent; BMD changes typically observed after 6-12 months of therapy.
PeakEffect:
Bone effects: Peak BMD increase typically seen after 2-3 years of continuous therapy.
DurationOfAction:
Effects persist as long as therapy is continued; bone density benefits may diminish upon discontinuation.
Safety & Warnings
BLACK BOX WARNING
Increased Risk of Venous Thromboembolism (VTE) and Cardiovascular Events. Raloxifene increases the risk of deep vein thrombosis (DVT), pulmonary embolism (PE), and retinal vein thrombosis. Raloxifene should be discontinued at least 72 hours prior to and during prolonged immobilization (e.g., surgery, prolonged bed rest). Raloxifene also increases the risk of death due to stroke in postmenopausal women with established coronary heart disease (CHD) or at increased risk for CHD.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Change in balance
+ Drooping on one side of the face
+ Blurred eyesight
Changes in vision
Breast-related symptoms, such as:
+ Lump in the breast
+ Breast pain or soreness
+ Nipple discharge
+ Enlarged breasts
Vaginal bleeding that is not normal
Swelling in the arms or legs
Depression
Signs of a blood clot, such as:
+ Chest pain or pressure
+ Coughing up blood
+ Shortness of breath
+ Swelling, warmth, numbness, change of color, or pain in a leg or arm
+ Trouble speaking or swallowing
Other Possible Side Effects
Most people do not experience severe side effects, and some may not have any side effects at all. However, if you notice any of the following symptoms, contact your doctor or seek medical help if they bother you or do not go away:
Hot flashes
Leg cramps
Flu-like symptoms
Excessive sweating
Headache
Upset stomach
Stomach pain or diarrhea
Muscle or joint pain
Trouble sleeping
Weight gain
* Signs of a common cold
Reporting Side Effects
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Change in balance
+ Drooping on one side of the face
+ Blurred eyesight
Changes in vision
Breast-related symptoms, such as:
+ Lump in the breast
+ Breast pain or soreness
+ Nipple discharge
+ Enlarged breasts
Vaginal bleeding that is not normal
Swelling in the arms or legs
Depression
Signs of a blood clot, such as:
+ Chest pain or pressure
+ Coughing up blood
+ Shortness of breath
+ Swelling, warmth, numbness, change of color, or pain in a leg or arm
+ Trouble speaking or swallowing
Other Possible Side Effects
Most people do not experience severe side effects, and some may not have any side effects at all. However, if you notice any of the following symptoms, contact your doctor or seek medical help if they bother you or do not go away:
Hot flashes
Leg cramps
Flu-like symptoms
Excessive sweating
Headache
Upset stomach
Stomach pain or diarrhea
Muscle or joint pain
Trouble sleeping
Weight gain
* Signs of a common cold
Reporting Side Effects
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Sudden leg pain, swelling, or tenderness (especially in the calf)
- Sudden chest pain, shortness of breath, or coughing up blood
- Sudden vision changes or loss
- Sudden severe headache
- Weakness or numbness on one side of the body
- Difficulty speaking or understanding speech
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the symptoms you experienced.
If you are taking cholestyramine, colestipol, or estrogen, as these medications may interact with this drug.
Your reproductive status:
+ If you have not yet gone through menopause or are still able to become pregnant.
+ If you are pregnant or think you may be pregnant. Do not take this medication if you are pregnant.
If you are breast-feeding or plan to breast-feed.
* If you are male, as this medication is not approved for use in men.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without consulting your doctor first.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the symptoms you experienced.
If you are taking cholestyramine, colestipol, or estrogen, as these medications may interact with this drug.
Your reproductive status:
+ If you have not yet gone through menopause or are still able to become pregnant.
+ If you are pregnant or think you may be pregnant. Do not take this medication if you are pregnant.
If you are breast-feeding or plan to breast-feed.
* If you are male, as this medication is not approved for use in men.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without consulting your doctor first.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Your doctor may advise you to stop taking this drug before undergoing certain types of surgery. If you need to stop taking this medication, your doctor will provide guidance on when to resume taking it after your surgery or procedure.
Regular breast exams are crucial, and your doctor will recommend the frequency of these exams. Additionally, you will need to perform breast self-exams as instructed by your doctor. It is important to discuss any concerns or questions you have with your doctor.
Be aware that this medication may cause elevated triglyceride levels. If you have a history of high triglyceride levels, inform your doctor. It is also vital to undergo regular blood tests and bone density checks as directed by your doctor.
To minimize potential risks, limit your alcohol consumption. If you are a smoker, consult with your doctor about the best course of action. If you anticipate being immobile for extended periods, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor, as prolonged immobility may increase your risk of developing blood clots. When traveling, make an effort to get up and move around as frequently as possible.
To maximize the effectiveness of this medication, it is recommended to use it in conjunction with calcium and vitamin D supplements, as well as engage in weight-bearing exercises like walking or physical therapy. Adhere to the diet and exercise plan outlined by your doctor.
It is crucial to note that this medication may harm an unborn baby if taken during pregnancy. If you become pregnant or suspect you may be pregnant while taking this medication, contact your doctor immediately.
Regular breast exams are crucial, and your doctor will recommend the frequency of these exams. Additionally, you will need to perform breast self-exams as instructed by your doctor. It is important to discuss any concerns or questions you have with your doctor.
Be aware that this medication may cause elevated triglyceride levels. If you have a history of high triglyceride levels, inform your doctor. It is also vital to undergo regular blood tests and bone density checks as directed by your doctor.
To minimize potential risks, limit your alcohol consumption. If you are a smoker, consult with your doctor about the best course of action. If you anticipate being immobile for extended periods, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor, as prolonged immobility may increase your risk of developing blood clots. When traveling, make an effort to get up and move around as frequently as possible.
To maximize the effectiveness of this medication, it is recommended to use it in conjunction with calcium and vitamin D supplements, as well as engage in weight-bearing exercises like walking or physical therapy. Adhere to the diet and exercise plan outlined by your doctor.
It is crucial to note that this medication may harm an unborn baby if taken during pregnancy. If you become pregnant or suspect you may be pregnant while taking this medication, contact your doctor immediately.
Overdose Information
Overdose Symptoms:
- Leg cramps
- Dizziness
- Nausea
- Vomiting
What to Do:
There is no specific antidote for raloxifene overdose. Management should be supportive and symptomatic. Contact a poison control center immediately (e.g., 1-800-222-1222) or seek emergency medical attention.
Drug Interactions
Major Interactions
- Systemic Estrogens (e.g., conjugated estrogens, estradiol): Concomitant use is not recommended due to potential for additive effects and increased risk of adverse events.
- Warfarin: May decrease prothrombin time (PT) and increase INR. Monitor INR closely.
Moderate Interactions
- Cholestyramine: Significantly reduces raloxifene absorption and systemic exposure. Avoid concomitant use.
- Ampicillin: May decrease raloxifene absorption, though clinical significance is generally minor.
- Diazepam: No significant interaction, but theoretical competition for protein binding sites.
Monitoring
Baseline Monitoring
Bone Mineral Density (BMD)
Rationale: To establish baseline and assess need for therapy.
Timing: Prior to initiation of therapy
Lipid Profile (Total Cholesterol, LDL, HDL, Triglycerides)
Rationale: Raloxifene can affect lipid levels; establish baseline.
Timing: Prior to initiation of therapy
Liver Function Tests (ALT, AST, Bilirubin)
Rationale: To assess baseline hepatic function, especially given hepatic metabolism.
Timing: Prior to initiation of therapy
Complete Medical History and Physical Exam
Rationale: To identify risk factors for VTE or other contraindications.
Timing: Prior to initiation of therapy
Routine Monitoring
Bone Mineral Density (BMD)
Frequency: Every 1-2 years
Target: Maintain or improve T-score
Action Threshold: Significant decline in BMD or new fracture despite therapy
Signs and Symptoms of Venous Thromboembolism (VTE)
Frequency: Continuously (patient education)
Target: Absence of symptoms
Action Threshold: Development of leg pain/swelling, chest pain, shortness of breath, vision changes
Lipid Profile
Frequency: Periodically, as clinically indicated
Target: Within healthy ranges
Action Threshold: Significant adverse changes in lipid profile
Symptom Monitoring
- Leg pain, swelling, tenderness, or redness (signs of DVT)
- Sudden chest pain, shortness of breath, coughing up blood (signs of PE)
- Sudden vision loss or changes, sudden severe headache, weakness or numbness on one side of the body, difficulty speaking (signs of stroke)
- Hot flashes
- Leg cramps
- Peripheral edema
Special Patient Groups
Pregnancy
Contraindicated in women who are or may become pregnant. Raloxifene can cause fetal harm when administered to a pregnant woman. Based on animal studies, it may cause developmental abnormalities.
Trimester-Specific Risks:
First Trimester:
High risk of fetal harm (e.g., developmental abnormalities, reproductive tract malformations)
Second Trimester:
High risk of fetal harm
Third Trimester:
High risk of fetal harm
Lactation
Contraindicated in lactating women. It is not known whether raloxifene is excreted in human milk. However, raloxifene is an estrogen antagonist and could inhibit lactation. Potential for serious adverse reactions in a breastfed infant.
Infant Risk:
High (potential for inhibition of lactation, unknown effects on infant)
Pediatric Use
Safety and effectiveness have not been established in pediatric patients. Not indicated for use in premenopausal women or pediatric patients.
Geriatric Use
No specific dose adjustment is required based on age. However, older women, especially those with pre-existing cardiovascular disease or risk factors, may be at increased risk for venous thromboembolic events and stroke. Use with caution and careful risk-benefit assessment.
Clinical Information
Clinical Pearls
- Raloxifene is a good option for postmenopausal women with osteoporosis who also have a high risk of breast cancer, as it offers benefits for both conditions.
- It is important to counsel patients on the signs and symptoms of VTE and stroke and to seek immediate medical attention if they occur.
- Patients should be advised to discontinue raloxifene at least 72 hours prior to and during prolonged immobilization (e.g., surgery, long-distance travel).
- Unlike estrogen therapy, raloxifene does not cause endometrial proliferation and is not associated with an increased risk of endometrial cancer.
- Common side effects include hot flashes and leg cramps, which may be bothersome for some patients.
Alternative Therapies
- Bisphosphonates (e.g., alendronate, risedronate, zoledronic acid)
- Denosumab
- Teriparatide
- Abaloparatide
- Romosozumab
- Calcitonin
- Estrogen therapy (for osteoporosis, but with different risk/benefit profile)
Cost & Coverage
Average Cost:
Varies widely, typically $50-$200 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which is a crucial resource for patients. Please read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or other healthcare provider for guidance. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.