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Raloxifene is formulated for treatment of osteoporosis, it also reduces risk of breast cancer in postmenopausal women with osteoporosis.

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Generic Raloxifene Information

Introduction

Raloxifene is a selective estrogen receptor modulator (SERM) used principally to prevent and treat osteoporosis in post‑menopausal women. In the United Kingdom it is prescribed under the women's health portfolio and is also approved to reduce the risk of invasive breast cancer in certain high‑risk groups. The active compound is raloxifene, and it is widely available as a generic alternative to the original brand‑name product Evista® (manufactured by Eli Lilly).

What is Raloxifene?

Raloxifene is the generic version of Evista®, containing the same active compound raloxifene. It belongs to the SERM class, which exerts estrogen‑like effects on bone while antagonising estrogen receptors in breast and uterine tissue. Generic raloxifene is produced by several certified manufacturers worldwide and is marketed in the UK as a cost‑effective option for the same therapeutic indications.

How Raloxifene Works

  • Receptor selectivity – Raloxifene binds to estrogen receptors (ERα and ERβ) with tissue‑specific activity. In bone, it mimics estrogen, promoting osteoblast activity and reducing osteoclast‑mediated resorption. In breast and uterus, it blocks estrogen signalling, limiting proliferative stimulation.

  • Bone turnover – By decreasing osteoclast recruitment and activation, raloxifene lowers markers of bone resorption (e.g., serum C‑telopeptide). This results in a net gain in bone mineral density (BMD), particularly at the lumbar spine and hip.

  • Pharmacokinetics – After oral administration, raloxifene is absorbed slowly (peak plasma concentrations in 4–6 h). It undergoes extensive first‑pass glucuronidation; the parent drug reaches a steady state after about 2 weeks of daily dosing. The elimination half‑life is approximately 28 hours, allowing once‑daily dosing.

Conditions Treated with Raloxifene

  • Post‑menopausal osteoporosis – Raloxifene is licensed for the primary and secondary prevention of vertebral fractures in women with low BMD (T‑score ≤ ‑2.5) or with a history of fragility fractures. In the UK, osteoporosis affects ~3 million women over 50, representing a significant public‑health burden.

  • Reduction of invasive breast cancer risk – For post‑menopausal women at increased risk (e.g., those with a strong family history, previous atypical hyperplasia, or high‑risk genetic profiles), raloxifene reduces the incidence of estrogen‑receptor‑positive breast cancer by about 38 % in long‑term studies.

  • Off‑label use for cardiovascular risk – While not approved for this purpose, early trials suggested modest improvements in lipid profiles (decrease in LDL‑cholesterol). Current UK guidance does not recommend raloxifene for primary cardiovascular prevention.

Who is Raloxifene For?

  • Post‑menopausal women with osteoporosis – Particularly those who cannot tolerate bisphosphonates, have contraindications to hormone replacement therapy, or prefer a medication without uterine stimulation.

  • Women at elevated risk of ER‑positive breast cancer – Those who meet NICE criteria for chemoprevention and who have no active breast disease.

  • Patients with contraindications to estrogen therapy – Because raloxifene does not increase endometrial thickness, it is suitable for women with a history of endometrial hyperplasia or cancer.

  • Not appropriate for – Premenopausal women, men, pregnant or lactating individuals, and patients with established venous thromboembolism (VTE) or severe hepatic impairment.

Risks, Side Effects, and Interactions

Common

  • Hot flushes
  • Leg cramps or musculoskeletal pain
  • Nausea or abdominal discomfort
  • Mild headache

Rare

  • Menstrual irregularities (spotting, breakthrough bleeding)
  • Elevated liver enzymes (transaminases)
  • Dyspepsia or gastro‑oesophageal reflux

Serious

  • Venous thromboembolism (VTE) – Deep vein thrombosis or pulmonary embolism. The risk is higher in women with a personal or family history of clotting disorders, obesity, or prolonged immobilisation.
  • Stroke – Ischaemic events have been reported, particularly in patients with pre‑existing cerebrovascular disease.
  • Severe allergic reactions – Anaphylaxis, angioedema, or cutaneous rash requiring immediate medical attention.
Drug–Drug Interactions
  • Anticoagulants (warfarin, direct oral anticoagulants) – Raloxifene may potentiate anticoagulant effects; INR monitoring is advised when used concomitantly.
  • CYP3A4 inducers (rifampicin, carbamazepine, St John’s wort) – May reduce raloxifene plasma concentrations, diminishing efficacy.
  • CYP3A4 inhibitors (ketoconazole, erythromycin) – Potentially increase exposure; dose adjustment is usually not required but clinical vigilance is recommended.
  • Hormone therapy or estrogen‑containing contraceptives – Counteracts raloxifene’s antagonist effect on breast and uterine tissue, reducing its protective benefit.

Practical Use: Dosing, Missed Dose, Overdose

  • Standard dosing – The usual adult dose for osteoporosis and breast‑cancer risk reduction is 60 mg (one tablet) taken orally once daily, with or without food.

  • Missed dose – If a dose is forgotten, take it as soon as remembered on the same day. Do not take a double dose the following day.

  • Overdose – Acute overdose of raloxifene is unlikely to be life‑threatening but may cause nausea, vomiting, or dizziness. If an overdose is suspected, seek emergency medical advice; supportive care and observation are the primary interventions.

  • Precautions

    • Avoid initiating raloxifene in women with active VTE or uncontrolled hypertension.
    • Alcohol can increase clotting risk; moderate consumption is advised.
    • Periodic monitoring of BMD, lipid profile, and liver function tests is recommended.

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FAQ

  • Is raloxifene available in both brand‑name and generic forms in the UK?
    Yes. The original brand‑name product is Evista®, produced by Eli Lilly. Multiple generic manufacturers supply raloxifene tablets that contain the identical active ingredient, offering a more affordable alternative.

  • What does a raloxifene tablet look like?
    Generic tablets are typically round, white to off‑white, and may be film‑coated. Imprint codes vary by manufacturer; common markings include “60 mg” and a manufacturer logo.

  • Does raloxifene require special storage conditions?
    The medication should be stored at controlled room temperature (15 °C–30 °C), protected from moisture and direct sunlight. No refrigeration is needed.

  • Can raloxifene be taken with calcium or vitamin D supplements?
    Yes, co‑administration is common and does not affect raloxifene absorption. In fact, calcium and vitamin D are routinely prescribed alongside to maximise bone health benefits.

  • Are there any known differences in formulation between EU and US raloxifene products?
    The active ingredient and therapeutic dose (60 mg) are identical. Inactive excipients may differ slightly, reflecting regional manufacturing preferences, but these variations do not alter efficacy or safety.

  • What is the recommended interval for bone‑density monitoring while on raloxifene?
    NICE advises a baseline dual‑energy X‑ray absorptiometry (DXA) scan, followed by reassessment after 2–3 years of consistent therapy, or sooner if clinical risk factors change.

  • Can raloxifene affect results of hormone‑related laboratory tests?
    Raloxifene may modestly raise sex‑hormone‑binding globulin (SHBG) levels, potentially interfering with assays that measure free estradiol. Clinicians typically interpret results in the context of SERM therapy.

  • Is it safe to travel internationally with raloxifene tablets?
    Yes, provided you carry the medication in its original packaging with a copy of the prescription (or a legitimate import licence) and keep it in your carry‑on luggage to avoid temperature extremes.

  • Does raloxifene interact with herbal products such as black cohosh or red clover?
    Limited data exist, but both herbs possess estrogenic activity and could theoretically diminish raloxifene’s antagonist effects in breast tissue. It is prudent to discuss any complementary medicines with a healthcare professional.

  • What is the historical significance of raloxifene’s development?
    Raloxifene emerged from the 199s SERM research programme aimed at separating estrogen’s beneficial bone effects from its proliferative actions on breast and uterus. Clinical trials such as the MORE (Multiple Outcomes of Raloxifene Evaluation) and STAR (Study of Tamoxifen and Raloxifene) established its dual role in osteoporosis prevention and breast‑cancer risk reduction.

Glossary

Selective Estrogen Receptor Modulator (SERM)
A class of compounds that act as estrogen agonists in some tissues (e.g., bone) and antagonists in others (e.g., breast, uterus), providing tissue‑specific therapeutic effects.
Bone Mineral Density (BMD)
A measurement of mineral content (mainly calcium) in bone, expressed as grams per square centimetre, used to assess fracture risk and monitor osteoporosis treatment.
Venous Thromboembolism (VTE)
The formation of blood clots in the venous system, encompassing deep‑vein thrombosis and pulmonary embolism, conditions that carry serious morbidity if untreated.

⚠️ Disclaimer

The information provided about raloxifene is for general knowledge only. It does not replace professional medical consultation. All treatment decisions should be made under the supervision of a qualified healthcare provider. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to raloxifene for individuals who may have limited availability through traditional pharmacies, prescription‑based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication.

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