Optruma (Raloxifene)
Selective Estrogen Receptor Modulator for Postmenopausal Osteoporosis
Quick Facts About Optruma
Key Takeaways About Optruma (Raloxifene)
- Prevents vertebral fractures: Raloxifene significantly reduces the risk of vertebral fractures in postmenopausal women with osteoporosis, although a reduction in hip fracture risk has not been demonstrated
- Non-hormonal alternative: As a SERM, raloxifene provides estrogen-like bone protection without stimulating breast or uterine tissue, offering a different risk profile compared to hormone replacement therapy
- Blood clot risk: Raloxifene increases the risk of venous thromboembolism (deep vein thrombosis and pulmonary embolism); it must not be used in women with a history of blood clots
- Cholesterol benefit: Raloxifene lowers total cholesterol and LDL cholesterol, potentially offering additional cardiovascular benefit
- Not for menopausal symptoms: Raloxifene does not relieve hot flushes or other menopausal symptoms – in fact, hot flushes are a common side effect
What Is Optruma and What Is It Used For?
Optruma contains the active substance raloxifene hydrochloride, a selective estrogen receptor modulator (SERM) used to treat and prevent osteoporosis in women who have gone through menopause. It reduces the risk of vertebral fractures by slowing bone loss and maintaining bone mineral density.
Osteoporosis is a condition in which the bones become thin, weak, and fragile, making them more susceptible to fracture. It is particularly common in women after menopause, when levels of the female hormone estrogen decline significantly. This decline in estrogen accelerates bone resorption (the breakdown of bone tissue), leading to a progressive loss of bone mineral density. Over time, this can result in fractures, particularly in the vertebrae (spine), hip, and wrist, even with minimal trauma.
Raloxifene belongs to a group of non-hormonal medicines called selective estrogen receptor modulators (SERMs). These drugs are designed to act differently on estrogen receptors in different tissues. In bone and in lipid metabolism, raloxifene mimics the protective effects of estrogen – it slows down bone resorption, helps maintain bone mineral density, and reduces total cholesterol and LDL cholesterol (the “bad” cholesterol). However, in breast and uterine tissue, raloxifene acts as an estrogen antagonist, meaning it blocks estrogen’s stimulating effects. This selective action gives raloxifene a favourable benefit–risk profile compared to traditional hormone replacement therapy.
Clinical studies have demonstrated that raloxifene reduces the risk of vertebral fractures in postmenopausal women with osteoporosis. The landmark MORE (Multiple Outcomes of Raloxifene Evaluation) trial showed that raloxifene reduced the risk of new vertebral fractures by approximately 30–50% over three years, depending on whether patients had pre-existing vertebral fractures. However, a reduction in the risk of hip fractures has not been demonstrated in clinical trials. For this reason, raloxifene is generally considered more appropriate for postmenopausal women at moderate risk of fracture, particularly vertebral fracture, rather than those at high risk of hip fracture.
Although osteoporosis may produce no symptoms in its early stages, it can lead to significant clinical consequences over time, including back pain, loss of height, and a stooped posture (kyphosis). By maintaining bone density and reducing fracture risk, Optruma helps preserve skeletal integrity, mobility, and quality of life in postmenopausal women.
Raloxifene was first approved by the European Medicines Agency (EMA) and the US Food and Drug Administration (FDA) in the late 1990s. It is included in major international guidelines for osteoporosis management, including those from the International Osteoporosis Foundation (IOF), the American Association of Clinical Endocrinologists (AACE), and the National Institute for Health and Care Excellence (NICE). Your doctor may also recommend calcium and vitamin D supplements alongside raloxifene to optimise bone health.
What Should You Know Before Taking Optruma?
Before starting Optruma, inform your doctor about any history of blood clots, liver or kidney disease, unexplained vaginal bleeding, or if you are pregnant or breastfeeding. Optruma is strictly for postmenopausal women and must not be used during pregnancy.
Contraindications
You should not take Optruma if any of the following apply to you:
- History of blood clots – including deep vein thrombosis (DVT), pulmonary embolism (PE), or retinal vein thrombosis, whether currently active or in the past
- Allergy to raloxifene or any of the other ingredients in the tablet (listed in the “What Does Optruma Contain?” section below)
- Possibility of pregnancy – Optruma is intended only for postmenopausal women. If there is any chance you could become pregnant, do not take this medicine, as raloxifene may harm an unborn child
- Liver disease – including cirrhosis, mildly impaired liver function, or cholestatic jaundice (jaundice caused by bile duct problems)
- Severe kidney problems – your doctor will assess whether raloxifene is safe for you if you have impaired kidney function
- Unexplained vaginal bleeding – your doctor must investigate the cause of any unexplained vaginal bleeding before you start treatment
- Active endometrial cancer – experience with raloxifene in women with active uterine cancer is limited, and its use in this setting is not recommended
Warnings and Precautions
Talk to your doctor or pharmacist before taking Optruma if any of the following apply to you:
- Prolonged immobilisation – if you are wheelchair-bound, need to be hospitalised, or must remain in bed for an extended period (for example, after surgery or during a serious illness), your risk of blood clots is increased. Your doctor may advise you to stop taking Optruma at least 72 hours before planned surgery or prolonged immobilisation and not to restart until you are fully mobile again
- History of cerebrovascular events – if you have had a stroke, transient ischaemic attack (TIA), or if your doctor has told you that you are at high risk of stroke, discuss the benefits and risks of raloxifene carefully with your doctor
- Liver disease – even if you do not have a contraindication, your doctor may want to monitor liver function during treatment
- Breast cancer – experience with raloxifene in women with breast cancer is limited. Discuss the potential benefits and risks with your doctor
- Estrogen therapy – if you are currently taking or have recently taken estrogen replacement therapy, inform your doctor, as the combination may not be appropriate
Raloxifene is unlikely to cause vaginal bleeding. Therefore, any vaginal bleeding that occurs while you are taking Optruma is unexpected and should be investigated by your doctor promptly.
Optruma does not help with menopausal symptoms such as hot flushes. In fact, hot flushes are one of the most commonly reported side effects of raloxifene. If you are experiencing significant menopausal symptoms, talk to your doctor about alternative treatment options.
Pregnancy and Breastfeeding
Optruma is indicated exclusively for postmenopausal women and must not be taken by women who are still able to become pregnant. Raloxifene may cause harm to a developing foetus. If you suspect that you may be pregnant, do not take Optruma and consult your doctor immediately.
Do not take Optruma during breastfeeding. The active substance may pass into breast milk, and the potential effects on a nursing infant have not been established.
Driving and Operating Machinery
Optruma has no or negligible effect on the ability to drive or operate machinery. No special precautions are required in this regard.
Lactose Content
Optruma tablets contain lactose. If your doctor has told you that you have an intolerance to certain sugars (such as lactose), contact your doctor before taking this medicine.
How Does Optruma Interact with Other Drugs?
Optruma can interact with several medications, including anticoagulants (such as warfarin), cholestyramine, and digitalis heart medications. Always inform your doctor about all medicines you are taking, including over-the-counter products and supplements.
Although raloxifene does not have extensive drug interactions compared to some other medications, there are several clinically important interactions that can affect its safety and efficacy. Always tell your doctor about all medications, supplements, and herbal products you are currently taking or plan to take.
Major Interactions
| Drug | Category | Effect | Recommendation |
|---|---|---|---|
| Warfarin | Anticoagulant | Raloxifene may alter warfarin metabolism, potentially affecting prothrombin time (INR) | Monitor INR closely when starting or stopping raloxifene; dose adjustment of warfarin may be needed |
| Cholestyramine | Bile acid sequestrant (lipid-lowering) | Cholestyramine significantly reduces the absorption and enterohepatic recycling of raloxifene, reducing its effectiveness by approximately 60% | Avoid concomitant use; if both are required, separate administration times by at least 4–6 hours |
| Estrogen / HRT | Hormone replacement | Concurrent use with systemic estrogen has not been studied and is not recommended; potential for opposing pharmacological effects | Do not use raloxifene concurrently with systemic estrogen therapy |
Moderate Interactions
| Drug | Category | Effect | Recommendation |
|---|---|---|---|
| Digitalis glycosides (digoxin) | Cardiac glycoside | Raloxifene may alter digoxin levels, though clinically significant interactions are uncommon | Monitor digoxin levels and clinical response; dose adjustment may be needed |
| Other anticoagulants | Blood thinners | Potential additive effects on coagulation parameters | Monitor coagulation parameters when initiating or discontinuing raloxifene |
| Highly protein-bound drugs | Various | Raloxifene is >95% protein-bound; theoretically may compete for binding sites with other highly protein-bound drugs such as diazepam, diclofenac, or ibuprofen | Clinical significance is generally low; no routine dose adjustments needed, but report any unusual effects to your doctor |
| Levothyroxine | Thyroid hormone | SERMs may affect thyroid hormone binding proteins | Monitor thyroid function tests if taking concurrently; dose adjustment may be required |
Raloxifene lowers total cholesterol and LDL cholesterol. However, it generally does not affect triglycerides or HDL cholesterol (“good” cholesterol). Your doctor may want to discuss this with you if you have previously taken estrogen and experienced significantly elevated triglyceride levels, as the effect may differ from that of estrogen therapy.
What Is the Correct Dosage of Optruma?
The recommended dose of Optruma is one 60 mg tablet taken once daily, at any time of day, with or without food. The tablet should be swallowed whole and not crushed or split. Your doctor may also recommend calcium and vitamin D supplements.
Always take Optruma exactly as your doctor has told you. If you are unsure, check with your doctor or pharmacist. The dosage regimen for raloxifene is straightforward – there is only one strength available (60 mg), and the dose is the same for all patients.
Postmenopausal Women
Dose: 60 mg once daily
Route: Oral (swallow whole with water)
Timing: At any time of day, with or without food. Taking it at the same time each day helps you remember.
Duration: Your doctor will advise how long to continue. Long-term treatment is typically required for osteoporosis management.
Elderly Patients
Dose: 60 mg once daily (no dose adjustment required)
No dose adjustment is necessary for elderly patients. Raloxifene has been studied extensively in older postmenopausal women and the standard 60 mg dose applies regardless of age.
Children and Adolescents
Not indicated: Optruma is not intended for use in children or premenopausal women. It is approved exclusively for postmenopausal women.
How to Take the Tablet
The tablet is designed for oral use. Swallow it whole with or without water. Do not crush, split, or chew the tablet before taking it. A split or crushed tablet may taste unpleasant, and you risk receiving an incorrect dose. Your doctor may also advise you to take calcium tablets and vitamin D supplements to support bone health during treatment.
Missed Dose
If you forget to take a tablet, take one as soon as you remember and then continue as normal. Do not take a double dose to make up for a forgotten one. If it is nearly time for your next dose, skip the missed dose and take the next one at the usual time.
Overdose
If you have taken more Optruma than you should, contact your doctor or pharmacist immediately. Symptoms of overdose may include leg cramps and dizziness. There is no specific antidote for raloxifene overdose; treatment is supportive and symptomatic. In the event of a suspected overdose, seek medical advice without delay.
Stopping Optruma
Do not stop taking Optruma without first talking to your doctor. It is important that you continue taking Optruma for as long as your doctor prescribes. The medicine can only treat or prevent your osteoporosis if you continue to take the tablets consistently. Your doctor will help you determine the appropriate duration of treatment based on your individual risk factors and bone density assessments.
What Are the Side Effects of Optruma?
The most common side effects of Optruma are hot flushes, flu-like symptoms, gastrointestinal discomfort, and increased blood pressure. A more serious but less common risk is blood clots (venous thromboembolism). Most side effects are mild and tend to diminish over time.
Like all medicines, Optruma can cause side effects, although not everybody gets them. The majority of side effects seen with raloxifene have been mild. Understanding the frequency and nature of potential side effects can help you recognise them early and discuss any concerns with your healthcare provider.
- Pain, swelling, or redness in one leg (possible deep vein thrombosis)
- Sudden shortness of breath, chest pain, or coughing up blood (possible pulmonary embolism)
- Sudden vision changes or loss of vision in one eye (possible retinal vein thrombosis)
- Sudden severe headache, weakness on one side, difficulty speaking, or confusion (possible stroke)
- Signs of a severe allergic reaction: swelling of the face, lips, tongue, or throat; difficulty breathing; severe skin rash
Very Common
May affect more than 1 in 10 people
- Hot flushes (vasodilation)
- Flu-like symptoms
- Gastrointestinal symptoms (nausea, vomiting, abdominal pain, stomach discomfort)
- Increased blood pressure
Common
May affect up to 1 in 10 people
- Headache, including migraine
- Leg cramps
- Peripheral oedema (swelling of hands, feet, and legs)
- Gallstones (cholelithiasis)
- Rash
- Mild breast symptoms (pain, swelling, tenderness)
Uncommon
May affect up to 1 in 1,000 people
- Deep vein thrombosis (DVT) – blood clots in the legs
- Pulmonary embolism (PE) – blood clots in the lungs
- Retinal vein thrombosis – blood clots in the eye
- Superficial venous thrombophlebitis (redness and tenderness around a vein)
- Arterial blood clots (including stroke) and increased risk of death from stroke
- Decreased platelet count (thrombocytopenia)
Rare
May affect fewer than 1 in 1,000 people
- Elevated liver enzyme levels in blood tests
The risk of venous thromboembolism is the most clinically significant adverse effect of raloxifene. The relative risk is approximately 2–3 times that of untreated women, which is similar to the risk associated with oral estrogen therapy. Risk factors for thromboembolism include a personal or family history of blood clots, prolonged immobilisation, recent surgery, obesity, and certain medical conditions. If you experience any signs of a blood clot, seek emergency medical attention immediately.
If you experience any side effects not listed here, or if any side effect becomes severe, contact your doctor or pharmacist. Reporting suspected side effects helps ensure ongoing monitoring of the medicine’s benefit–risk balance.
How Should You Store Optruma?
Store Optruma in its original packaging at room temperature, away from children. Do not freeze. Do not use after the expiry date on the packaging.
Keep Optruma out of the sight and reach of children. Store the medicine in its original packaging to protect it from moisture and light. Do not freeze.
Do not use Optruma after the expiry date stated on the packaging after “EXP”. The expiry date refers to the last day of the stated month. Check the date regularly and discard any expired medication.
Do not flush unused tablets down the toilet or dispose of them in household waste. Return any unused or expired medicines to your pharmacy for safe disposal. These measures help protect the environment from pharmaceutical contamination.
What Does Optruma Contain?
Each Optruma tablet contains 60 mg of raloxifene hydrochloride (equivalent to 56 mg raloxifene) as the active ingredient, along with several inactive ingredients including lactose.
Active Ingredient
The active substance is raloxifene hydrochloride. Each film-coated tablet contains 60 mg of raloxifene hydrochloride, which is equivalent to 56 mg of raloxifene (the free base form).
Inactive Ingredients (Excipients)
The other ingredients are:
- Tablet core: Povidone, polysorbate 80, lactose, lactose monohydrate, crospovidone, magnesium stearate
- Film coating: Titanium dioxide (E171), polysorbate 80, hypromellose, macrogol 400, carnauba wax
- Printing ink: Shellac, propylene glycol, indigo carmine (E132)
Lactose Content
This medicine contains lactose. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicine.
Tablet Appearance and Packaging
Appearance: Optruma tablets are white, oval, film-coated, and marked with “4165”.
Pack sizes: Blister packs containing 14, 28, or 84 tablets, or plastic bottles containing 100 tablets. Not all pack sizes may be available in all countries.
Marketing Authorisation Holder
Eli Lilly Nederland B.V., Orteliuslaan 1000, 3528 BD Utrecht, The Netherlands.
How Does Optruma Work in the Body?
Raloxifene selectively binds to estrogen receptors in different tissues, producing estrogen-like effects on bone (reducing resorption) and on lipid metabolism (lowering LDL cholesterol), while blocking estrogen’s effects on breast and uterine tissue. This targeted action is the hallmark of selective estrogen receptor modulators (SERMs).
When a woman reaches menopause, her ovaries stop producing significant amounts of estrogen. Estrogen plays a critical role in maintaining bone health by suppressing osteoclast activity (the cells that break down bone). With declining estrogen levels, the rate of bone resorption increases relative to bone formation, leading to a net loss of bone mineral density. This imbalance is the fundamental mechanism underlying postmenopausal osteoporosis.
Raloxifene binds to estrogen receptors (both ERα and ERβ) but, unlike estrogen itself, it activates different downstream signalling pathways depending on the tissue. In bone tissue, raloxifene acts as an estrogen agonist: it reduces osteoclast-mediated bone resorption, helps preserve bone mineral density, and reduces the risk of vertebral fractures. In lipid metabolism, it similarly acts as an agonist, lowering total cholesterol and LDL cholesterol levels.
In breast tissue and uterine (endometrial) tissue, however, raloxifene acts as an estrogen antagonist. It blocks estrogen’s proliferative effects on these tissues, which is why it does not increase the risk of breast cancer or endometrial cancer – a concern associated with some forms of hormone replacement therapy. In fact, clinical data from the MORE and RUTH trials suggest that raloxifene may reduce the incidence of invasive estrogen receptor–positive breast cancer in postmenopausal women.
Pharmacokinetic Profile
After oral administration, raloxifene is rapidly absorbed from the gastrointestinal tract. However, it undergoes extensive first-pass glucuronidation, which reduces its absolute bioavailability to approximately 2%. Despite this low bioavailability, the drug achieves effective clinical concentrations because it is administered as a relatively high dose (60 mg).
Raloxifene is highly protein-bound (>95%), primarily to albumin and α1-acid glycoprotein. It has a large volume of distribution and is metabolised in the liver via glucuronide conjugation. The parent compound is not metabolised by cytochrome P450 enzymes, which reduces the potential for drug interactions compared to many other medications. The elimination half-life is approximately 27.7 hours, supporting once-daily dosing. The drug and its metabolites are primarily excreted in the faeces, with less than 6% eliminated in urine.
Frequently Asked Questions About Optruma
Optruma contains the active substance raloxifene and is used to treat and prevent osteoporosis (bone thinning) in postmenopausal women. It reduces the risk of vertebral fractures by mimicking some of the beneficial effects of estrogen on bone without the associated risks to breast and uterine tissue. It belongs to a class of non-hormonal medicines called selective estrogen receptor modulators (SERMs).
The most common side effects of Optruma (affecting more than 1 in 10 people) are hot flushes (vasodilation), flu-like symptoms, gastrointestinal symptoms such as nausea, vomiting, abdominal pain and stomach discomfort, and increased blood pressure. Common side effects (affecting up to 1 in 10 people) include headache, leg cramps, peripheral oedema, gallstones, rash, and mild breast symptoms. Most side effects are mild and tend to diminish over time.
Yes, Optruma can increase the risk of blood clots, including deep vein thrombosis (DVT), pulmonary embolism, and retinal vein thrombosis. This is an uncommon side effect (affecting 1 to 10 in 1,000 people). You should not take Optruma if you have a history of blood clots, and you should inform your doctor before any planned surgery or prolonged immobilisation, as these situations increase clot risk. Seek immediate medical attention if you experience leg pain, swelling, sudden shortness of breath, or vision changes.
No, Optruma does not help with menopausal symptoms such as hot flushes. In fact, hot flushes are one of the most common side effects of Optruma, reported by more than 1 in 10 users. Optruma is designed specifically to protect bone density and reduce fracture risk, not to treat vasomotor or other menopausal symptoms. If you are experiencing problematic menopausal symptoms, discuss alternative treatments with your doctor.
Optruma (raloxifene) is a selective estrogen receptor modulator (SERM), not a hormone. Unlike HRT, raloxifene selectively mimics estrogen’s effects on bone and cholesterol while blocking estrogen’s stimulating effects on breast and uterine tissue. This means it does not increase the risk of breast cancer or endometrial cancer – concerns associated with some forms of HRT. However, unlike HRT, Optruma does not relieve menopausal symptoms and may actually worsen hot flushes. Both raloxifene and HRT carry a risk of venous thromboembolism.
Yes, and your doctor will likely recommend it. Adequate calcium and vitamin D intake is essential for bone health and complements the effects of raloxifene on bone. Most international guidelines recommend 1,000–1,200 mg of calcium and 800–2,000 IU of vitamin D daily for postmenopausal women at risk of osteoporosis. You can obtain calcium from dietary sources (dairy products, fortified foods, leafy green vegetables) or supplements, and vitamin D primarily from sunlight exposure and supplements.
References
This article is based on the following international medical guidelines and peer-reviewed sources. All medical claims have evidence level 1A, the highest quality of evidence based on systematic reviews of randomised controlled trials.
- Ettinger B, Black DM, Mitlak BH, et al. Reduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with raloxifene: results from a 3-year randomized clinical trial (MORE). JAMA. 1999;282(7):637–645. doi:10.1001/jama.282.7.637
- Barrett-Connor E, Mosca L, Collins P, et al. Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women (RUTH trial). New England Journal of Medicine. 2006;355(2):125–137. doi:10.1056/NEJMoa062462
- European Medicines Agency (EMA). Optruma (raloxifene) – Summary of Product Characteristics. EMA product information database. Accessed January 2026.
- Kanis JA, Cooper C, Rizzoli R, Reginster JY. European guidance for the diagnosis and management of osteoporosis in postmenopausal women. Osteoporosis International. 2019;30(1):3–44. doi:10.1007/s00198-018-4704-5
- International Osteoporosis Foundation (IOF). IOF Compendium of Osteoporosis. 2nd edition. IOF; 2019.
- Camacho PM, Petak SM, Binkley N, et al. American Association of Clinical Endocrinologists/American College of Endocrinology Clinical Practice Guidelines for the Diagnosis and Treatment of Postmenopausal Osteoporosis – 2020 Update. Endocrine Practice. 2020;26(Suppl 1):1–46.
- National Institute for Health and Care Excellence (NICE). Bisphosphonates for treating osteoporosis. NICE technology appraisal guidance [TA464]. Updated 2023.
- World Health Organization (WHO). WHO Model List of Essential Medicines – 23rd list. Geneva: WHO; 2023.
Editorial Team
This article has been written and reviewed by the iMedic Medical Editorial Team, a group of licensed specialist physicians with expertise in endocrinology, clinical pharmacology, and women’s health.
Medical Writers
Board-certified physicians specialising in endocrinology, bone metabolism, and clinical pharmacology with documented academic and clinical experience.
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Independent review board ensuring clinical accuracy, adherence to international guidelines (IOF, AACE, NICE, WHO), and evidence level 1A standards.
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