Loading...
Loading...
Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Raloxifene Hydrochloride
Generic Name
Raloxifene Hydrochloride
Active Ingredient
RaloxifeneCategory
Other
Salt Form
Hydrochloride
Variants
19
Different strengths and dosage forms
| Strength | Form | Route | NDC |
|---|---|---|---|
| 60 mg/1 | TABLET, FILM COATED | ORAL | 68462-393 |
| 60 mg/1 | TABLET, FILM COATED | ORAL | 0904-6902 |
| 60 mg/1 | TABLET, FILM COATED | ORAL | 71335-1715 |
References used for this content
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Raloxifene Hydrochloride, you must consult a qualified healthcare professional.
| 60 mg/1 | TABLET, FILM COATED | ORAL | 50090-7073 |
| 60 mg/1 | TABLET, COATED | ORAL | 72162-2418 |
| 60 mg/1 | TABLET, FILM COATED | ORAL | 0093-7290 |
| 60 mg/1 | TABLET, FILM COATED | ORAL | 65162-057 |
| 60 mg/1 | TABLET, COATED | ORAL | 72241-010 |
| 60 mg/1 | TABLET, COATED | ORAL | 50090-6177 |
| 60 mg/1 | TABLET, FILM COATED | ORAL | 71335-1460 |
| 60 mg/1 | TABLET, FILM COATED | ORAL | 71335-2059 |
| 60 mg/1 | TABLET, FILM COATED | ORAL | 76282-256 |
+ 7 more variants
Detailed information about Raloxifene Hydrochloride
Raloxifene is a selective estrogen receptor modulator (SERM) used to treat and prevent osteoporosis in postmenopausal women and reduce the risk of invasive breast cancer in high-risk populations.
The standard dosage for Raloxifene is consistent across all approved indications, simplifying the treatment regimen for patients and providers.
Clinical trials, such as the MORE (Multiple Outcomes of Raloxifene Evaluation) trial, utilized this 60 mg daily dose to demonstrate significant reductions in vertebral fracture risk. There is no evidence that increasing the dose beyond 60 mg provides additional clinical benefit, and higher doses may increase the risk of adverse events.
Raloxifene is not approved for use in pediatric patients. Its safety and efficacy have not been established in children or adolescents. Because the drug's mechanism involves the modulation of estrogen receptors, which are critical for growth and development, its use in a pediatric population could have significant and unpredictable effects on bone maturation and hormonal balance.
For patients with mild to moderate renal (kidney) impairment, no specific dose adjustment is typically required. However, Raloxifene should be used with extreme caution in patients with severe renal impairment. Data in this population are limited, and because the drug can affect systemic mineral balance, close monitoring by a healthcare provider is essential.
Raloxifene is extensively metabolized in the liver. In patients with hepatic (liver) impairment (such as cirrhosis), safety and efficacy have not been fully established. Clinical studies have shown that plasma concentrations of Raloxifene can be significantly higher in patients with liver dysfunction. Therefore, Raloxifene is generally not recommended for patients with moderate to severe hepatic impairment.
No dose adjustment is necessary based solely on age. Clinical trials included a significant number of women over the age of 65 and 75, and no overall differences in safety or effectiveness were observed between these patients and younger postmenopausal women. However, older patients may be at a higher baseline risk for venous thromboembolism (VTE), which requires careful consideration.
To ensure the best results and safety, follow these administration guidelines:
If you miss a dose of Raloxifene, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and return to your regular schedule. Do not double the dose to catch up. Consistency is key to the long-term effectiveness of the medication in protecting bone density and reducing cancer risk.
Reports of Raloxifene overdose are rare. In clinical trials, daily doses up to 600 mg (ten times the standard dose) were administered for several weeks and were generally well-tolerated. However, an acute overdose may lead to an increase in side effects, particularly leg cramps and dizziness. In children, accidental ingestion has resulted in symptoms such as ataxia (lack of muscle coordination), dizziness, vomiting, and rash.
In the event of a suspected overdose, contact your local poison control center or seek emergency medical attention immediately. Treatment is generally supportive, as there is no specific antidote for Raloxifene.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop taking the medication without first consulting your medical team.
Raloxifene is generally well-tolerated, but because it blocks estrogen in certain parts of the body, it can cause symptoms similar to those experienced during menopause. The most frequently reported side effects include:
Raloxifene is a potent medication that requires careful screening before initiation. Patients must be aware that while it protects bones and reduces breast cancer risk, it does not provide the same benefits as estrogen for menopausal symptoms (like vaginal dryness or hot flashes) and carries significant vascular risks.
In certain situations, the risks of Raloxifene are so high that the drug must NEVER be used. These include:
FDA Category X. Raloxifene is strictly contraindicated in women who are or may become pregnant. In animal studies, Raloxifene caused significant fetal abnormalities, including issues with bone development and delayed parturition (birth). Because Raloxifene is only indicated for postmenopausal women, pregnancy should not occur during its use. If a woman becomes pregnant while taking this drug, she must stop immediately and be apprised of the potential hazard to the fetus.
It is not known whether Raloxifene is excreted in human milk. However, many drugs are excreted in human milk, and the potential for serious adverse reactions in nursing infants is high. Furthermore, as an anti-estrogen, Raloxifene may interfere with the hormonal regulation of milk production (lactation). Use in nursing mothers is not recommended.
Raloxifene is not approved for use in children. The safety and effectiveness have not been established in any pediatric population. Estrogen receptors play a vital role in the closing of growth plates in bones; therefore, using a SERM in children could lead to stunted growth or other developmental skeletal issues.
Raloxifene is a Selective Estrogen Receptor Modulator (SERM). Its biological actions are mediated through binding to estrogen receptors alpha (ERα) and beta (ERβ). This binding induces a specific conformational change in the receptor, which then dictates how the receptor interacts with DNA and various co-regulatory proteins.
In the bone, Raloxifene acts as an agonist. It inhibits the activity of osteoclasts, the cells responsible for bone resorption. This leads to a decrease in the rate of bone turnover and an increase in bone mineral density. In the breast and uterus, it acts as an antagonist. It prevents the binding of natural estrogen to its receptors, thereby inhibiting the growth of estrogen-dependent tissues. This is why it can reduce the risk of ER-positive breast cancer without increasing the risk of uterine cancer.
Raloxifene decreases bone resorption, as evidenced by decreases in serum and urine markers of bone turnover (e.g., bone-specific alkaline phosphatase, osteocalcin). These markers typically decrease to levels seen in premenopausal women within 3 to 6 months of starting therapy. Raloxifene also has favorable effects on lipid metabolism, lowering total and LDL cholesterol without significantly affecting HDL or total triglycerides (unless a pre-existing sensitivity exists).
Common questions about Raloxifene Hydrochloride
Raloxifene is primarily used for the prevention and treatment of osteoporosis in postmenopausal women, helping to increase bone density and reduce the risk of spinal fractures. Additionally, it is FDA-approved to reduce the risk of invasive breast cancer in postmenopausal women who are at high risk or have osteoporosis. It works by mimicking estrogen's beneficial effects on bone while blocking estrogen's potentially harmful effects on breast tissue. It is important to note that Raloxifene is not a treatment for existing breast cancer, but rather a preventive measure for those at risk. Your doctor will determine if you meet the criteria for these specific uses based on your medical history and bone density scores.
The most common side effects reported by women taking Raloxifene include hot flashes, leg cramps, and joint pain. Hot flashes are particularly common during the first few months of treatment because the drug blocks estrogen receptors in the brain's temperature-regulating center. Some women also experience swelling in the hands or feet (peripheral edema) and flu-like symptoms. While these side effects are generally manageable, they can be bothersome for some patients. If these symptoms become severe or persist, you should discuss them with your healthcare provider. Most side effects do not require stopping the medication, but your doctor can offer strategies to manage them.
There is no known direct interaction between Raloxifene and alcohol that would make drinking unsafe in moderation. However, heavy alcohol consumption is a significant risk factor for developing osteoporosis and can increase your risk of falling and sustaining a fracture. Since Raloxifene is prescribed to protect your bones, excessive drinking may counteract the benefits of the medication. It is generally recommended to limit alcohol intake to one drink per day or less to support overall bone health and general wellness. Always check with your doctor to see if your specific health conditions require you to avoid alcohol entirely.
No, Raloxifene is strictly contraindicated during pregnancy and is classified by the FDA as Category X. This means that studies in animals or humans have demonstrated that the drug can cause significant fetal abnormalities and birth defects. Raloxifene is only intended for use in postmenopausal women who are no longer able to become pregnant. If you are a woman of childbearing age, you should not take this medication. If you inadvertently take Raloxifene and suspect you are pregnant, you must stop the medication immediately and contact your healthcare provider for guidance on the potential risks to the fetus.
Raloxifene begins to affect bone turnover markers within the first few weeks of treatment, but the full clinical benefits for bone density are typically measured over a longer period. Most doctors will perform a follow-up bone density (DEXA) scan after 1 to 2 years of continuous use to assess the medication's effectiveness. For breast cancer risk reduction, the protective effects are cumulative and are based on long-term daily use as seen in clinical trials lasting five years or more. It is essential to take the medication consistently every day as prescribed to achieve these long-term health outcomes. Do not expect immediate changes in how you feel, as the drug's primary benefits are internal.
Yes, Raloxifene can be stopped suddenly without causing a withdrawal syndrome or immediate physical illness. Unlike some medications that require a tapering period, Raloxifene does not cause a 'rebound' effect. However, once you stop taking the drug, its protective effects on your bones will begin to fade, and your rate of bone loss will likely return to what it was before you started treatment. This could increase your risk of fractures over time. You should always talk to your doctor before stopping Raloxifene so they can recommend other ways to protect your bone health or manage your breast cancer risk.
If you miss a dose of Raloxifene, you should take it as soon as you remember on that same day. However, if you do not remember until the following day, you should skip the missed dose entirely and simply take your next regularly scheduled dose. You should never take two doses at the same time to make up for a missed one, as this could increase your risk of side effects like leg cramps. To help you remember your medication, try taking it at the same time each day, such as with breakfast or before bed. Consistency is the most important factor in ensuring the drug works effectively.
Weight gain is listed as a potential side effect in clinical trials, but it occurred at a rate very similar to women taking a placebo (a sugar pill). In the large MORE trial, there was no significant difference in average weight change between women taking Raloxifene and those who were not. Some women may experience mild fluid retention (edema), which can feel like weight gain or cause clothes to fit more tightly. If you notice a sudden or significant increase in weight, or if you have swelling in your legs and ankles, you should contact your doctor. They can determine if the weight change is related to the medication or another underlying health issue.
Raloxifene can be taken with many common medications, but there are some important exceptions. It should not be taken with bile acid sequestrants like cholestyramine, as these prevent Raloxifene from being absorbed. It also should not be used alongside systemic estrogen replacement therapy. If you are taking warfarin (a blood thinner), your doctor will need to monitor your blood clotting time more frequently, as Raloxifene can interfere with warfarin's effects. Because Raloxifene is highly protein-bound, it may interact with other highly bound drugs like diazepam or naproxen. Always provide your doctor with a complete list of all prescriptions, over-the-counter drugs, and supplements you use.
Yes, Raloxifene is available as a generic medication and is also sold under the brand name Evista. The generic version contains the same active ingredient (Raloxifene Hydrochloride) and is required by the FDA to meet the same standards for safety, strength, and effectiveness as the brand-name drug. Generic Raloxifene is typically much less expensive than the brand-name version and is covered by most insurance plans and Medicare. If you have concerns about switching between the brand and generic versions, you should discuss them with your pharmacist or healthcare provider, though they are considered therapeutically equivalent.
Other drugs with the same active ingredient (Raloxifene)
While rare, some side effects of Raloxifene are life-threatening. You must be vigilant for the following symptoms:
> Warning: Stop taking Raloxifene and call your doctor immediately if you experience any of these.
Long-term use of Raloxifene (over several years) is generally considered safe for bone health and breast cancer risk reduction. However, the risk of blood clots remains elevated throughout the duration of therapy. Unlike estrogen therapy, Raloxifene does not appear to increase the risk of uterine (endometrial) cancer or heart disease, though it also does not provide cardiovascular protection.
The FDA has issued a "Black Box Warning" for Raloxifene, the highest level of alert for serious risks.
Report any unusual symptoms to your healthcare provider immediately. Regular follow-ups are necessary to assess the ongoing risk-benefit ratio of the medication.
Raloxifene significantly increases the risk of blood clots during periods of prolonged immobility. You must stop taking Raloxifene at least 72 hours (3 days) before any scheduled surgery or any period where you will be confined to a bed or chair for a long time (such as a long flight). Do not restart the medication until you are fully mobile again. Discuss this with your surgeon well in advance of any procedure.
Before starting Raloxifene, your doctor should evaluate your risk for stroke. This includes checking for high blood pressure (hypertension), smoking status, history of a "mini-stroke" (TIA), or heart rhythm issues like atrial fibrillation. If you have a high risk of stroke, the risks of Raloxifene may outweigh the benefits.
Because the liver is the primary site of Raloxifene metabolism, patients with liver disease (cirrhosis, hepatitis) may experience dangerously high levels of the drug in their system. Raloxifene is generally avoided in these patients.
In women with a history of high triglycerides (fats in the blood) in response to oral estrogen therapy, Raloxifene may cause a further increase in triglyceride levels. Your doctor may need to monitor your lipid profile during treatment.
To ensure safety, the following monitoring is typically recommended:
Raloxifene does not typically cause drowsiness or cognitive impairment. However, if you experience dizziness or vision changes, you should avoid driving or operating heavy machinery until you know how the medication affects you.
There is no known direct interaction between alcohol and Raloxifene. However, excessive alcohol consumption is a risk factor for osteoporosis and can increase the risk of falls and fractures. It is generally advised to limit alcohol intake to support overall bone health.
There is no evidence of a withdrawal syndrome or a need to taper Raloxifene. If you stop taking it, the bone-protective effects will gradually wear off over time, and your bone loss rate will return to that of a postmenopausal woman not taking the drug. Always consult your doctor before stopping the medication to discuss alternative bone-protection strategies.
> Important: Discuss all your medical conditions, especially any history of blood clots or heart disease, with your healthcare provider before starting Raloxifene.
Raloxifene does not typically interfere with standard laboratory tests. However, it can lower total cholesterol and LDL cholesterol levels (which is generally considered a positive side effect) and may slightly increase levels of certain clotting factors, though these are not usually measured in routine blood work.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter pain relievers and vitamins.
These conditions require a careful risk-benefit analysis by a specialist:
While there is no direct cross-sensitivity with other SERMs (like tamoxifen or toremifene), patients who have had severe adverse reactions to other benzothiophene derivatives should use Raloxifene with caution. Always inform your pharmacist of any previous drug allergies.
> Important: Your healthcare provider will evaluate your complete medical history, including any history of smoking or vascular disease, before prescribing Raloxifene.
In clinical trials, no overall differences in safety or effectiveness were observed between patients over 65 and younger postmenopausal women. However, the baseline risk for stroke and venous thromboembolism increases with age. Therefore, while no dose adjustment is needed, healthcare providers should perform regular vascular risk assessments in geriatric patients. The risk of falls and subsequent fractures should also be managed holistically alongside Raloxifene therapy.
Raloxifene is not significantly cleared by the kidneys (less than 0.2% in urine). However, the drug can influence systemic mineral metabolism. While no dose adjustment is required for mild to moderate impairment, the drug has not been sufficiently studied in patients with a GFR (Glomerular Filtration Rate) below 30 mL/min. Caution is advised.
Safety in patients with hepatic impairment has not been established. In a single-dose study, Raloxifene concentrations were 2.5 times higher in patients with child-pugh class A cirrhosis compared to healthy controls. Use is generally not recommended in patients with moderate to severe hepatic impairment.
> Important: Special populations require individualized medical assessment and frequent monitoring to ensure the safest possible outcomes.
| Parameter | Value |
|---|---|
| Bioavailability | ~2% (due to extensive first-pass glucuronidation) |
| Protein Binding | ~95% (Albumin and α1-acid glycoprotein) |
| Half-life | 27.7 to 32.5 hours |
| Tmax | ~6 hours |
| Metabolism | Hepatic (Glucuronidation; non-CYP) |
| Excretion | Fecal (>95%), Renal (<0.2%) |
Raloxifene is the primary representative of the SERM class used for bone health. Other drugs in this class include Tamoxifen (used primarily for breast cancer treatment) and Bazedoxifene (used in combination with estrogens for menopause symptoms).