Raloxifene Hydrochloride 60 mg Tablet, Film Coated
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Estrogen Agonist/Antagonist class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Raloxifene is used to prevent and treat osteoporosis (condition in which the bones become thin and weak and break easily) in postmenopausal (women who have experienced a change of life; end of menstrual periods) women. Raloxifene is also used to decrease the risk of developing invasive breast cancer (breast cancer that has spread outside of the milk ducts or lobules into the surrounding breast tissue) in postmenopausal women who are at high risk of developing this type of cancer or who have osteoporosis. Raloxifene cannot be used to treat invasive breast cancer or to prevent invasive breast ca...
Read the full MedlinePlus article ↗- It's related to estrogen but it's not the same thing. Raloxifene is what's called a SERM — it selectively acts like estrogen in your bones, which helps slow bone loss and keep your...
- What is raloxifene actually doing for me — is it like taking estrogen?
- You have a lot of flexibility here. Raloxifene can be taken at any time of day — morning, afternoon, or evening — whatever fits your routine best. You don't need to take it with fo...
- Can I take this with or without food, and does the time of day matter?
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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Anhydrous lactose is a milk sugar with no water content. It acts as a filler and binder in tablets and capsules, adding bulk and helping ingredients stick together.
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Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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Crospovidone is a synthetic polymer made from polyvinylpyrrolidone. It acts as a disintegrant, helping tablets break apart quickly in the stomach so the medicine dissolves and absorbs into the body.
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Hypromellose is a plant-based thickener made from cellulose. It's used in medicines as a binder to hold ingredients together, a coating for tablets, and a thickener for liquids.
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Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
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Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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Polyethylene glycol is a synthetic liquid or solid polymer used in medicines as a solvent, lubricant, and humectant. It helps dissolve active ingredients, reduces friction during manufacturing, and retains moisture in the final product.
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Polysorbate 80 is a synthetic emulsifier derived from sorbitol and oleic acid. It helps mix oil and water-based ingredients together in medications and improves how the product disperses in the body.
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Povidone is a synthetic polymer made from a plastic-like material. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in your stomach so the medicine can be absorbed.
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Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
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Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
11 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.236 | $11.80 / 50 tablet |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $0.4465 | $22.33 / 50 tablet |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Raloxifene Hydrochloride 60 mg 00093-7290-01 | Teva | 100 tablets | $0.236 | AB | Availability likely | — |
| Raloxifene hydrochloride 60 mg 00904-6902-04 | Major | 1 tablet | $0.236 | AB | Availability likely | — |
| Raloxifene Hydrochloride 60 mg 16714-0213-01 | NorthStar | 30 tablets | $0.236 | AB | Availability likely | — |
| Raloxifene hydrochloride 60 mg 43598-0505-01 | Dr.Reddys | 100 tablets | $0.236 | AB | Availability likely | — |
| Raloxifene Hydrochloride 60 mgthis 50268-0694-15 | AvPAK | 1 tablet | $0.236 | AB | Availability likely | — |
| Raloxifene Hydrochloride 60 mg 60687-0266-21 | American | 30 tablets | $0.236 | AB | Availability likely | — |
| Raloxifene Hydrochloride 60 mg 65162-0057-03 | Amneal | 30 tablets | $0.236 | AB | Availability likely | — |
| Raloxifene Hydrochloride 60 mg 65862-0709-01 | Aurobindo | 100 tablets | $0.236 | AB | Availability likely | — |
| Raloxifene Hydrochloride 60 mg 69097-0825-02 | Cipla | 30 tablets | $0.236 | AB | Availability likely | — |
| Raloxifene hydrochloride 60 mg 72241-0010-05 | Modavar | 100 tablets | $0.236 | AB | Availability likely | — |
| Evista 60 mg 00002-4184-02 | Eli | 100 tablets | — | AB | FDA listed | — |
| Raloxifene hydrochloride 60 mg 50090-6177-01 | A-S | 90 tablets | — | AB | FDA listed | — |
| Raloxifene Hydrochloride 60 mg 50090-7073-01 | A-S | 90 tablets | — | AB | FDA listed | — |
| Raloxifene hydrochloride 60 mg 50228-0306-20 | ScieGen | 2000 tablets | — | AB | FDA listed | — |
| raloxifene hydrochloride 60 mg 68462-0393-01 | Glenmark | 100 tablets | — | AB | FDA listed | — |
| Raloxifene hydrochloride 60 mg 71209-0082-01 | Cadila | 30 tablets | — | AB | FDA listed | — |
| Raloxifene hydrochloride 60 mg 71335-1460-01 | Bryant | 60 tablets | — | AB | FDA listed | — |
| Raloxifene Hydrochloride 60 mg 71335-1715-01 | Bryant | 60 tablets | — | AB | FDA listed | — |
| Raloxifene Hydrochloride 60 mg 71335-2059-01 | Bryant | 60 tablets | — | AB | FDA listed | — |
| Raloxifene hydrochloride 60 mg 71610-0053-60 | Aphena | 90 tablets | — | AB | FDA listed | — |
| Raloxifene Hydrochloride 60 mg 71610-0524-60 | Aphena | 90 tablets | — | AB | FDA listed | — |
| Raloxifene hydrochloride 60 mg 72162-2418-00 | Bryant | 1000 tablets | — | AB | FDA listed | — |
| Raloxifene Hydrochloride 60 mg 76282-0256-01 | Exelan | 100 tablets | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 50268-0694-15 You're viewing this | 50 BLISTER PACK in 1 BOX, UNIT-DOSE (50268-694-15) / 1 TABLET, FILM COATED in 1 BLISTER PACK (50268-694-11) | 2018-06-27 | Active |
📄 Full prescribing information FDA SPL
🚨 Boxed Warning ▾
WARNING--INCREASED RISK OF VENOUS THROMBOEMBOLISM AND DEATH FROM STROKE Increased risk of deep vein thrombosis and pulmonary embolism have been reported with raloxifene HCl (5.1) . Women with active or past history of venous thromboembolism should not take raloxifene HCl (4.1) . Increased risk of death due to stroke occurred in a trial in postmenopausal women with documented coronary heart disease or at increased risk for major coronary events.
Consider risk-benefit balance in women at risk for stroke ( 5.2 , 14.5 ). WARNING: INCREASED RISK OF VENOUS THROMBOEMBOLISM AND DEATH FROM STROKE See full prescribing information for complete boxed warning. Increased risk of deep vein thrombosis and pulmonary embolism have been reported with raloxifene HCl (5.1) .
Women with active or past history of venous thromboembolism should not take raloxifene HCl (4.1) . Increased risk of death due to stroke occurred in a trial in postmenopausal women with documented coronary heart disease or at increased risk for major coronary events. Consider risk-benefit balance in women at risk for stroke (5.2, 14.5) .
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Raloxifene HCl tablets, USP are an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. (1.1) Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (1.2) Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer.
(1.3) Important Limitations: Raloxifene HCl tablets, USP are not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer. (1.3)
1.1Treatment and Prevention of Osteoporosis in Postmenopausal Women Raloxifene hydrochloride (HCl) tablets, USP are indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1, 14.2) ] .
1.2Reduction in the Risk of Invasive Breast Cancer in Postmenopausal Women with Osteoporosis Raloxifene HCl tablets, USP are indicated for the reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis [see Clinical Studies (14.3) ] .
1.3Reduction in the Risk of Invasive Breast Cancer in Postmenopausal Women at High Risk of Invasive Breast Cancer Raloxifene HCl tablets, USP are indicated for the reduction in risk of invasive breast cancer in postmenopausal women at high risk of invasive breast cancer [see Clinical Studies (14.4) ] . The effect in the reduction in the incidence of breast cancer was shown in a study of postmenopausal women at high risk for breast cancer with a 5-year planned duration with a median follow-up of 4.3 years [see Clinical Studies (14.4) ] .
Twenty-seven percent of the participants received drug for 5 years. The long-term effects and the recommended length of treatment are not known. High risk of breast cancer is defined as at least one breast biopsy showing lobular carcinoma in situ (LCIS) or atypical hyperplasia, one or more first-degree relatives with breast cancer, or a 5-year predicted risk of breast cancer ≥1.66% (based on the modified Gail model).
Among the factors included in the modified Gail model are the following: current age, number of first-degree relatives with breast cancer, number of breast biopsies, age at menarche, nulliparity or age of first live birth. Healthcare professionals can obtain a Gail Model Risk Assessment Tool by dialing 1-800-545-5979. Currently, no single clinical finding or test result can quantify risk of breast cancer with certainty.
After an assessment of the risk of developing breast cancer, the decision regarding therapy with raloxifene HCl tablets, USP should be based upon an individual assessment of the benefits and risks. Raloxifene HCl tablets, USP does not eliminate the risk of breast cancer. Patients should have breast exams and mammograms before starting raloxifene HCl tablets, USP and should continue regular breast exams and mammograms in keeping with good medical practice after beginning treatment with raloxifene HCl tablets, USP.
Important Limitations of Use for Breast Cancer Risk Reduction There are no data available regarding the effect of raloxifene HCl tablets, USP on invasive breast cancer incidence in women with inherited mutations (BRCA1, BRCA2) to be able to make specific recommendations on the effectiveness of raloxifene HCl tablets, USP. Raloxifene HCl tablets, USP are not indicated for the treatment of invasive breast cancer or reduction of the risk of recurrence. Raloxifene HCl tablets, USP are not indicated for the reduction in the risk of noninvasive breast cancer.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION 60 mg tablet orally once daily. (2.1)
2.1Recommended Dosing The recommended dosage is one 60 mg raloxifene HCl tablet, USP daily, which may be administered any time of day without regard to meals [see Clinical Pharmacology (12.3) ] . For the indications in risk of invasive breast cancer the optimum duration of treatment is not known [see Clinical Studies (14.3, 14.4) ] .
2.2Recommendations for Calcium and Vitamin D Supplementation For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate. Postmenopausal women require an average of 1500 mg/day of elemental calcium. Total daily intake of calcium above 1500 mg has not demonstrated additional bone benefits while daily intake above 2000 mg has been associated with increased risk of adverse effects, including hypercalcemia and kidney stones.
The recommended intake of vitamin D is 400 to 800 IU daily. Patients at increased risk for vitamin D insufficiency (e.g., over the age of 70 years, nursing home bound, or chronically ill) may need additional vitamin D supplements. Patients with gastrointestinal malabsorption syndromes may require higher doses of vitamin D supplementation and measurement of 25-hydroxyvitamin D should be considered.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS 60 mg, white to off-white, elliptical shaped, film-coated tablets debossed with “AN057” on one side and plain on the other side. Tablets (not scored): 60 mg (3)
⛔ Contraindications ▾
4 CONTRAINDICATIONS Active or past history of venous thromboembolism, including deep vein thrombosis, pulmonary embolism and retinal vein thrombosis. (4.1) Pregnancy, women who may become pregnant and nursing mothers. (4.2, 8.1, 8.3)
4.1Venous Thromboembolism Raloxifene HCl, USP is contraindicated in women with active or past history of venous thromboembolism (VTE), including deep vein thrombosis, pulmonary embolism and retinal vein thrombosis [see Warnings and Precautions (5.1) ] .
4.2Pregnancy Raloxifene hydrochloride is contraindicated for use in pregnancy, as it may cause fetal harm [see Use in Specific Populations (8.1)].
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Venous Thromboembolism: Increased risk of deep vein thrombosis, pulmonary embolism and retinal vein thrombosis. Discontinue use 72 hours prior to and during prolonged immobilization. (5.1, 6.1) Death Due to Stroke: Increased risk of death due to stroke occurred in a trial in postmenopausal women with documented coronary heart disease or at increased risk for major coronary events.
No increased risk of stroke was seen in this trial. Consider risk-benefit balance in women at risk for stroke. (5.2, 14.5) Cardiovascular Disease: Raloxifene HCl should not be used for the primary or secondary prevention of cardiovascular disease.
(5.3, 14.5) Premenopausal Women: Use is not recommended. (5.4) Hepatic Impairment: Use with caution. (5.5) Concomitant Use with Systemic Estrogens: Not recommended.
(5.6) Hypertriglyceridemia: If previous treatment with estrogen resulted in hypertriglyceridemia, monitor serum triglycerides. (5.7)
5.1Venous Thromboembolism In clinical trials, raloxifene HCl-treated women had an increased risk of venous thromboembolism (deep vein thrombosis and pulmonary embolism). Other venous thromboembolic events also could occur. A less serious event, superficial thrombophlebitis, also has been reported more frequently with raloxifene HCl than with placebo.
The greatest risk for deep vein thrombosis and pulmonary embolism occurs during the first 4 months of treatment, and the magnitude of risk appears to be similar to the reported risk associated with use of hormone therapy. Because immobilization increases the risk for venous thromboembolic events independent of therapy, raloxifene HCl should be discontinued at least 72 hours prior to and during prolonged immobilization (e.g., post-surgical recovery, prolonged bed rest) and raloxifene HCl therapy should be resumed only after the patient is fully ambulatory.
In addition, women taking raloxifene HCl should be advised to move about periodically during prolonged travel. The risk-benefit balance should be considered in women at risk of thromboembolic disease for other reasons, such as congestive heart failure, superficial thrombophlebitis and active malignancy [see Contraindications (4.1) and Adverse Reactions (6.1) ] .
5.2Death Due to Stroke In a clinical trial of postmenopausal women with documented coronary heart disease or at increased risk for coronary events, an increased risk of death due to stroke was observed after treatment with raloxifene HCl. During an average follow-up of 5.6 years, 59 (1.2%) raloxifene HCl-treated women died due to a stroke compared to 39 (0.8%) placebo-treated women (22 versus 15 per 10,000 women-years; hazard ratio 1.49; 95% confidence interval, 1 to 2.24; p=0.0499). There was no statistically significant difference between treatment groups in the incidence of stroke (249 in raloxifene HCl [4.9%] versus 224 placebo [4.4%]).
Raloxifene HCl had no significant effect on all-cause mortality. The risk-benefit balance should be considered in women at risk for stroke, such as prior stroke or transient ischemic attack (TIA), atrial fibrillation, hypertension, or cigarette smoking [see Clinical Studies (14.5) ] .
5.3Cardiovascular Disease Raloxifene HCl should not be used for the primary or secondary prevention of cardiovascular disease. In a clinical trial of postmenopausal women with documented coronary heart disease or at increased risk for coronary events, no cardiovascular benefit was demonstrated after treatment with raloxifene for 5 years [see Clinical Studies (14.5) ] .
5.4Premenopausal Use There is no indication for premenopausal use of raloxifene HCl. Safety of raloxifene HCl in premenopausal women has not been established and its use is not recommended.
5.5Hepatic Impairment Raloxifene HCl should be used with caution in patients with hepatic impairment. Safety and efficacy have not been established in patients with hepatic impairment [see Clinical Pharmacology (12.3) ] .
5.6 Concomitant Estrogen Therapy The sa…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS Adverse reactions (>2% and more common than with placebo) include: hot flashes, leg cramps, peripheral edema, flu syndrome, arthralgia, sweating. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact AvKARE at 1-855-361-3993; email [email protected]; or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The data described below reflect exposure to raloxifene HCl in 8429 patients who were enrolled in placebo-controlled trials, including 6666 exposed for 1 year and 5685 for at least 3 years. Osteoporosis Treatment Clinical Trial (MORE) — The safety of raloxifene in the treatment of osteoporosis was assessed in a large (7705 patients) multinational, placebo-controlled trial.
Duration of treatment was 36 months, and 5129 postmenopausal women were exposed to raloxifene (2557 received 60 mg/day, and 2572 received 120 mg/day). The incidence of all-cause mortality was similar among groups: 23 (0.9%) placebo, 13 (0.5%) raloxifene HCl-treated (raloxifene 60 mg) and 28 (1.1%) raloxifene 120 mg women died. Therapy was discontinued due to an adverse reaction in 10.9% of raloxifene HCl-treated women and 8.8% of placebo-treated women.
Venous Thromboembolism: The most serious adverse reaction related to raloxifene HCl was VTE (deep venous thrombosis, pulmonary embolism and retinal vein thrombosis). During an average of study-drug exposure of 2.6 years, VTE occurred in about 1 out of 100 patients treated with raloxifene HCl. Twenty-six raloxifene HCl-treated women had a VTE compared to 11 placebo-treated women, the hazard ratio was 2.4 (95% confidence interval, 1.2, 4.5) and the highest VTE risk was during the initial months of treatment.
Common adverse reactions considered to be related to raloxifene HCl therapy were hot flashes and leg cramps. Hot flashes occurred in about one in 10 patients on raloxifene HCl and were most commonly reported during the first 6 months of treatment and were not different from placebo thereafter. Leg cramps occurred in about one in 14 patients on raloxifene HCl.
Placebo-Controlled Osteoporosis Prevention Clinical Trials — The safety of raloxifene has been assessed primarily in 12 Phase 2 and Phase 3 studies with placebo, estrogen and estrogen-progestin therapy control groups. The duration of treatment ranged from 2 to 30 months and 2036 women were exposed to raloxifene (371 patients received 10 to 50 mg/day, 828 received 60 mg/day and 837 received from 120 to 600 mg/day). Therapy was discontinued due to an adverse reaction in 11.4% of 581 raloxifene HCl-treated women and 12.2% of 584 placebo-treated women.
Discontinuation rates due to hot flashes did not differ significantly between raloxifene HCl and placebo groups (1.7% and 2.2%, respectively). Common adverse reactions considered to be drug-related were hot flashes and leg cramps. Hot flashes occurred in about one in four patients on raloxifene HCl versus about one in six on placebo.
The first occurrence of hot flashes was most commonly reported during the first 6 months of treatment. Table 1 lists adverse reactions occurring in either the osteoporosis treatment or in five prevention placebo-controlled clinical trials at a frequency ≥2% in either group and in more raloxifene HCl-treated women than in placebo-treated women. Adverse reactions are shown without attribution of causality.
The majority of adverse reactions occurring during the studies were mild and generally did not require discontinuation of therapy. Table 1: Adverse Reactions Occurring in Placebo-Controlled Osteoporosis Clinical Trials at a Frequency ≥2% and in More Raloxifene HCl-Treated (60 mg Once Daily) Women than Placebo-Treated Women a Treatment Prevention Raloxifene HCl N=2557 % Pl…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Cholestyramine: Use with raloxifene HCl is not recommended. Reduces the absorption and enterohepatic cycling of raloxifene. (7.1, 12.3) Warfarin: Monitor prothrombin time when starting or stopping raloxifene HCl. (7.2, 12.3) Highly Protein-Bound Drugs: Use with raloxifene HCl with caution. Highly protein-bound drugs include diazepam, diazoxide and lidocaine. Raloxifene HCl is more than 95% bound to plasma proteins. (7.3, 12.3)
7.1Cholestyramine Concomitant administration of cholestyramine with raloxifene HCl is not recommended. Although not specifically studied, it is anticipated that other anion exchange resins would have a similar effect. Raloxifene HCl should not be co-administered with other anion exchange resins [see Clinical Pharmacology (12.3) ] .
7.2Warfarin If raloxifene HCl is given concomitantly with warfarin or other warfarin derivatives, prothrombin time should be monitored more closely when starting or stopping therapy with raloxifene HCl [see Clinical Pharmacology (12.3) ] .
7.3Other Highly Protein-Bound Drugs Raloxifene HCl should be used with caution with certain other highly protein-bound drugs such as diazepam, diazoxide and lidocaine. Although not examined, raloxifene HCl might affect the protein binding of other drugs. Raloxifene is more than 95% bound to plasma proteins [see Clinical Pharmacology (12.3) ] .
7.4Systemic Estrogens The safety of concomitant use of raloxifene HCl with systemic estrogens has not been established and its use is not recommended.
7.5Other Concomitant Medications Raloxifene HCl can be concomitantly administered with ampicillin, amoxicillin, antacids, corticosteroids and digoxin [see Clinical Pharmacology (12.3) ] . The concomitant use of raloxifene HCl and lipid-lowering agents has not been studied.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Pediatric Use: Safety and effectiveness not established. (8.4)
8.1Pregnancy Pregnancy Category X. Raloxifene HCl should not be used in women who are or may become pregnant [see Contraindications (4.2) ] .
8.3Nursing Mothers Raloxifene HCl should not be used by lactating women [see Contraindications (4.2) ] . It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when raloxifene is administered to a nursing woman.
8.4Pediatric Use Safety and effectiveness in pediatric patients have not been established.
8.5Geriatric Use Of the total number of patients in placebo-controlled clinical studies of raloxifene HCl, 61% were 65 and over, while 15.5% were 75 and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Based on clinical trials, there is no need for dose adjustment for geriatric patients [see Clinical Pharmacology (12.3) ] .
8.6Renal Impairment Raloxifene HCl should be used with caution in patients with moderate or severe renal impairment [see Warnings and Precautions (5.8) and Clinical Pharmacology (12.3) ] .
8.7Hepatic Impairment Raloxifene HCl should be used with caution in patients with hepatic impairment [see Warnings and Precautions (5.5) and Clinical Pharmacology (12.3) ] . To report SUSPECTED ADVERSE REACTIONS, contact AvKARE at 1-855-361-3993; email [email protected]; or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
🤰 Pregnancy ▾
8.1Pregnancy Pregnancy Category X. Raloxifene HCl should not be used in women who are or may become pregnant [see Contraindications (4.2) ] .
🧒 Pediatric Use ▾
8.4Pediatric Use Safety and effectiveness in pediatric patients have not been established.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the total number of patients in placebo-controlled clinical studies of raloxifene HCl, 61% were 65 and over, while 15.5% were 75 and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Based on clinical trials, there is no need for dose adjustment for geriatric patients [see Clinical Pharmacology (12.3) ] .
🆘 Overdosage ▾
10 OVERDOSAGE In an 8-week study of 63 postmenopausal women, a dose of raloxifene HCl 600 mg/day was safely tolerated. In clinical trials, no raloxifene overdose has been reported. In postmarketing spontaneous reports, raloxifene overdose has been reported very rarely (less than 1 out of 10,000 [<0.01%] patients treated).
The highest overdose has been approximately 1.5 grams. No fatalities associated with raloxifene overdose have been reported. Adverse reactions were reported in approximately half of the adults who took ≥180 mg raloxifene and included leg cramps and dizziness.
Two 18-month-old children each ingested raloxifene 180 mg. In these two children, symptoms reported included ataxia, dizziness, vomiting, rash, diarrhea, tremor and flushing, as well as elevation in alkaline phosphatase. There is no specific antidote for raloxifene.
No mortality was seen after a single oral dose in rats or mice at 5000 mg/kg (810 times the human dose for rats and 405 times the human dose for mice based on surface area, mg/m 2 ) or in monkeys at 1000 mg/kg (80 times the AUC in humans).
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Raloxifene is an estrogen agonist/antagonist, commonly referred to as a selective estrogen receptor modulator (SERM). The biological actions of raloxifene are largely mediated through binding to estrogen receptors. This binding results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism).
The agonistic or antagonistic action of raloxifene depends on the extent of recruitment of coactivators and corepressors to estrogen receptor (ER) target gene promotors. Raloxifene appears to act as an estrogen agonist in bone. It decreases bone resorption and bone turnover, increases bone mineral density (BMD) and decreases fracture incidence.
Preclinical data demonstrate that raloxifene is an estrogen antagonist in uterine and breast tissues. These results are consistent with findings in clinical trials, which suggest that raloxifene HCl lacks estrogen-like effects on the uterus and breast tissue.
12.2Pharmacodynamics Decreases in estrogen levels after oophorectomy or menopause lead to increases in bone resorption and accelerated bone loss. Bone is initially lost rapidly because the compensatory increase in bone formation is inadequate to offset resorptive losses. In addition to loss of estrogen, this imbalance between resorption and formation may be due to age-related impairment of osteoblasts or their precursors.
In some women, these changes will eventually lead to decreased bone mass, osteoporosis and increased risk for fractures, particularly of the spine, hip and wrist. Vertebral fractures are the most common type of osteoporotic fracture in postmenopausal women. In both the osteoporosis treatment and prevention trials, raloxifene HCl therapy resulted in consistent, statistically significant suppression of bone resorption and bone formation, as reflected by changes in serum and urine markers of bone turnover (e.g., bone-specific alkaline phosphatase, osteocalcin and collagen breakdown products).
The suppression of bone turnover markers was evident by 3 months and persisted throughout the 36-month and 24-month observation periods. In a 31-week, open-label, radiocalcium kinetics study, 33 early postmenopausal women were randomized to treatment with once-daily raloxifene HCl 60 mg, cyclic estrogen/progestin (0.625 mg conjugated estrogens daily with 5 mg medroxyprogesterone acetate daily for the first 2 weeks of each month [hormone therapy]), or no treatment. Treatment with either raloxifene HCl or hormone therapy was associated with reduced bone resorption and a positive shift in calcium balance (-82 mg Ca/day and +60 mg Ca/day, respectively, for raloxifene HCl and -162 mg Ca/day and +91 mg Ca/day, respectively, for hormone therapy).
There were small decreases in serum total calcium, inorganic phosphate, total protein and albumin, which were generally of lesser magnitude than decreases observed during estrogen or hormone therapy. Platelet count was also decreased slightly and was not different from estrogen therapy.
12.3Pharmacokinetics The disposition of raloxifene has been evaluated in more than 3000 postmenopausal women in selected raloxifene osteoporosis treatment and prevention clinical trials, using a population approach. Pharmacokinetic data also were obtained in conventional pharmacology studies in 292 postmenopausal women. Raloxifene exhibits high within-subject variability (approximately 30% coefficient of variation) of most pharmacokinetic parameters.
Table 3 summarizes the pharmacokinetic parameters of raloxifene. Absorption — Raloxifene is absorbed rapidly after oral administration. Approximately 60% of an oral dose is absorbed, but presystemic glucuronide conjugation is extensive.
Absolute bioavailability of raloxifene is 2%. The time to reach average maximum plasma concentration and bioavailability are functions of systemic interconversion and enterohepatic cycling of raloxifene and its glucuronide metabo…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Raloxifene is an estrogen agonist/antagonist, commonly referred to as a selective estrogen receptor modulator (SERM). The biological actions of raloxifene are largely mediated through binding to estrogen receptors. This binding results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism).
The agonistic or antagonistic action of raloxifene depends on the extent of recruitment of coactivators and corepressors to estrogen receptor (ER) target gene promotors. Raloxifene appears to act as an estrogen agonist in bone. It decreases bone resorption and bone turnover, increases bone mineral density (BMD) and decreases fracture incidence.
Preclinical data demonstrate that raloxifene is an estrogen antagonist in uterine and breast tissues. These results are consistent with findings in clinical trials, which suggest that raloxifene HCl lacks estrogen-like effects on the uterus and breast tissue.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING
16.1How Supplied Raloxifene HCl tablets, USP, 60 mg, are supplied as white to off-white, elliptical shaped, film–coated tablets debossed with “AN057” on one side and plain on the other side. They are available as follows: NDC 50268-694-15 (10 tablets per card, 5 cards per carton) Dispensed in Unit Dose Package. For Institutional Use Only.
16.2Storage and Handling Store at controlled room temperature, 20º to 25ºC (68º to 77ºF) [ see USP]. The USP defines controlled room temperature as a temperature maintained thermostatically that encompasses the usual and customary working environment of 20º to 25ºC (68º to 77ºF); that results in a mean kinetic temperature calculated to be not more than 25ºC; and that allows for excursions between 15º and 30ºC (59º and 86ºF) that are experienced in pharmacies, hospitals and warehouses. Dispense in tight containers.
📋 Description ▾
11 DESCRIPTION Raloxifene HCl, USP is an estrogen agonist/antagonist, commonly referred to as a selective estrogen receptor modulator (SERM) that belongs to the benzothiophene class of compounds. The chemical structure is: The chemical designation is methanone, [6-hydroxy-2-(4-hydroxyphenyl)benzo[ b ]thien-3-yl]-[4-[2-(1-piperidinyl)ethoxy]phenyl]-, hydrochloride. Raloxifene HCl, USP has the molecular formula C 28 H 27 NO 4 S•HCl, which corresponds to a molecular weight of 510.05.
Raloxifene HCl, USP is an off-white to pale-yellow solid that is very slightly soluble in water. Raloxifene HCl, USP is supplied in a tablet dosage form for oral administration. Each raloxifene HCl tablet, USP contains 60 mg of raloxifene HCl, USP, which is the molar equivalent of 55.71 mg of free base.
Inactive ingredients include anhydrous lactose, crospovidone, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, povidone, silicon dioxide and titanium dioxide. Chemical Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION See FDA-approved Medication Guide . Physicians should instruct their patients to read the Medication Guide before starting therapy with raloxifene HCl and to reread it each time the prescription is renewed.
17.1Osteoporosis Recommendations, Including Calcium and Vitamin D Supplementation For osteoporosis treatment or prevention, patients should be instructed to take supplemental calcium and/or vitamin D if intake is inadequate. Patients at increased risk for vitamin D insufficiency (e.g., over the age of 70 years, nursing home bound, chronically ill, or with gastrointestinal malabsorption syndromes) should be instructed to take additional vitamin D if needed. Weight-bearing exercises should be considered along with the modification of certain behavioral factors, such as cigarette smoking and/or excessive alcohol consumption, if these factors exist.
17.2Patient Immobilization Raloxifene HCl should be discontinued at least 72 hours prior to and during prolonged immobilization (e.g., post-surgical recovery, prolonged bed rest), and patients should be advised to avoid prolonged restrictions of movement during travel because of the increased risk of venous thromboembolic events [see Warnings and Precautions (5.1) ] .
17.3Hot Flashes or Flushes Raloxifene HCl may increase the incidence of hot flashes and is not effective in reducing hot flashes or flushes associated with estrogen deficiency. In some asymptomatic patients, hot flashes may occur upon beginning raloxifene HCl therapy.
17.4Reduction in Risk of Invasive Breast Cancer in Postmenopausal Women with Osteoporosis or at High Risk of Invasive Breast Cancer Use of raloxifene HCl is associated with the reduction of the risk of invasive breast cancer in postmenopausal women. Raloxifene HCl has not been shown to reduce the risk of noninvasive breast cancer. When considering treatment, physicians need to discuss the potential benefits and risks of raloxifene HCl treatment with the patient.
Raloxifene HCl is not indicated for the treatment of invasive breast cancer or reduction of the risk of recurrence. Patients should have breast exams and mammograms before starting raloxifene HCl and should continue regular breast exams and mammograms in keeping with good medical practice after beginning treatment with raloxifene HCl. Manufactured for: AvKARE Pulaski, TN 38478 Mfg.
Rev. 12-2021-04 AV Rev. 01/24 (M) AvPAK
💬 Medication Guide ▾
Medication Guide Raloxifene (ra-LOX-i-feen) HCl Tablets for Oral Use Read the Medication Guide that comes with raloxifene HCl before you start taking it and each time you refill your prescription. The information may have changed. This Medication Guide does not take the place of talking with your doctor about your medical condition or treatment.
Talk with your doctor about raloxifene HCl when you start taking it and at regular checkups. What is the most important information I should know about raloxifene HCl? Serious and life-threatening side effects can occur while taking raloxifene HCl.
These include blood clots and dying from stroke: Increased risk of blood clots in the legs (deep vein thrombosis) and lungs (pulmonary embolism) have been reported with raloxifene HCl. Women who have or have had blood clots in the legs, lungs, or eyes should not take raloxifene HCl. Women who have had a heart attack or are at risk for a heart attack may have an increased risk of dying from stroke when taking raloxifene HCl.
1. Before starting raloxifene HCl, tell your doctor if you have had blood clots in your legs, lungs, or eyes, a stroke, mini-stroke (transient ischemic attack), or have an irregular heartbeat. 2.
Stop taking raloxifene HCl and call your doctor if you have: leg pain or a feeling of warmth in the lower leg (calf). swelling of the legs, hands, or feet. sudden chest pain, shortness of breath, or coughing up blood. sudden change in your vision, such as loss of vision or blurred vision. 3. Being still for a long time (such as sitting still during a long car or airplane trip or being in bed after surgery) can increase your risk of blood clots.
(See “What should I avoid if I am taking raloxifene HCl?” ) What is raloxifene HCl? Raloxifene HCl is a type of prescription medicine called a Selective Estrogen Receptor Modulator (SERM). Raloxifene HCl is for women after menopause, and has more than one use: • Osteoporosis: Raloxifene HCl treats and prevents osteoporosis by helping make your bones stronger and less likely to break. • Invasive Breast Cancer: If you have osteoporosis or are at high risk for breast cancer, raloxifene HCl can be used to lower your chance of getting invasive breast cancer.
Raloxifene HCl will not totally get rid of your chance of getting breast cancer. Your doctor can estimate your risk of breast cancer by asking you about risk factors, including: your age (getting older). family history of breast cancer in your mother, sister, or daughter. a history of any breast biopsy, especially an abnormal biopsy. You and your doctor should talk about whether the possible benefit of raloxifene HCl in lowering your chance of getting invasive breast cancer is greater than its possible risks.
Raloxifene HCl is not for use in premenopausal women (women who have not passed menopause). Who should not take raloxifene HCl ? Do not take raloxifene HCl if you: have or have had blood clots in your legs, lungs, or eyes.
Taking raloxifene HCl may increase the risk of getting blood clots. are pregnant or could become pregnant. Raloxifene HCl could harm your unborn child. are nursing a baby. It is not known if raloxifene HCl passes into breast milk or what effect it might have on the baby.
What should I tell my doctor before taking raloxifene HCl ? Raloxifene HCl may not be right for you. Before taking raloxifene HCl, tell your doctor about all your medical conditions, including if you: have had blood clots in your legs, lungs, or eyes, a stroke, mini-stroke (TIA/transient ischemic attack), or a type of irregular heartbeat (atrial fibrillation). have had breast cancer.
Raloxifene HCl has not been fully studied in women who have a history of breast cancer. have liver or kidney problems. have taken estrogen in the past and had a high increase of triglycerides (a kind of fat in the blood). are pregnant, planning to become pregnant, or breast-feeding (see “Who should not take raloxifene HCl ?” ). Tell your doctor about all medicines you ta…