Raloxifene
SERM · postmenopausal osteoporosis
Third-party optionBy the Layer Nutrition editorial team · How the atlas classifies the 664 molecules
What this medicine is for
Raloxifene is a medicine in the « SERM (postmenopausal osteoporosis) » category. This medicine strengthens bone solidity and reduces the risk of fracture.
Specifically, for Raloxifene: Strengthens bone in postmenopausal women. Its conditions of use depend on the situation, within the framework set by the doctor.
Under which brands it is found
In France, about 8 reimbursable presentations containing Raloxifene are recorded. It is found under several brand names and as generics.
- Evista
- Raloxifene Arrow
- Raloxifene Biogaran
- Raloxifene Cristers
- Raloxifene Eg
- Raloxifene Teva
- Raloxifene Viatris
- Raloxifene Zentiva
Original brand-name products and generics deliver the same active substance; the choice between them is made with your doctor or pharmacist.
On the plate: calcium and vitamin D
Raloxifene acts on bone, but it does not make up for a deficiency in calcium or vitamin D. Yet the absorption and retention of calcium decline after menopause. Diet is the first lever to support the skeleton, alongside your treatment.
Calcium is a major component of bone. It is found in dairy products such as milk, cheese and yogurt, in canned sardines and salmon eaten with their bones, and in certain green vegetables such as kale and broccoli. Spreading these sources across the day helps meet needs that rise with age.
Vitamin D plays a complementary role: it helps the body absorb calcium, and a deficiency in it promotes osteoporosis. It comes mainly from egg yolks, oily fish and fortified foods such as milk, cereals and yogurt. Pairing the two on the plate gives calcium the means to be truly taken up.
How raloxifene works
Raloxifene belongs to the family of selective estrogen receptor modulators, the SERMs. Its distinctive feature lies in that word, selective: depending on the tissue, it behaves differently at the estrogen receptor. In bone, it acts as an agonist, meaning that it mimics estrogen. In the uterus and the breast, by contrast, it behaves as an antagonist, blocking the receptor.
This dual action explains its place in postmenopausal women. In bone, it slows bone resorption, the stage where old bone is broken down, and it reduces the biochemical markers of remodeling. The result can be measured: bone mineral density increases. Raloxifene does not build new bone, it slows the loss of it.
What the body does with the drug
Raloxifene follows an unusual metabolic path. It is not transformed by the cytochrome P450 enzymes, the liver enzymes responsible for breaking down many medications. Instead, it undergoes extensive glucuronide conjugation: the liver and the intestine attach glucuronide molecules to it to make it soluble. This particular pathway limits the CYP-type interactions that are common with other treatments.
Its pharmacokinetics also explain why a once-daily dose is enough. Raloxifene and its glucuronides continually interconvert through reversible metabolism and an enterohepatic cycle, a back-and-forth between the liver and the intestine. This recycling extends the elimination half-life to 27.7 hours. Absolute bioavailability remains low, around 2 percent, and raloxifene circulates 95 percent bound to plasma proteins.
Why it is prescribed
Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women. After menopause, the drop in estrogen accelerates bone loss and weakens the skeleton. By mimicking estrogen in bone, raloxifene partly makes up for this loss of protection and reduces the risk of vertebral fracture.
It has a second indication, tied to its antagonist action in the breast: reducing the risk of invasive breast cancer in certain postmenopausal women at high risk. The choice between raloxifene and other osteoporosis treatments depends on each woman's profile, on her bone and vascular risk factors, and is decided together with the physician.
How to take it day to day
The dosing is simple: one 60 mg tablet by mouth, once a day. You can take it at any time of day, with or without food, which leaves plenty of freedom to fit it into a routine. Consistency matters more than timing: a steady daily dose maintains the effect on bone.
Raloxifene acts on bone but does not correct a deficiency in calcium or vitamin D. If your dietary intake is insufficient, a calcium and vitamin D supplement is recommended in addition to the treatment. Like any osteoporosis treatment, it should not be stopped on your own initiative: bone loss resumes as soon as it is stopped, and that decision rests with the physician.
The effects to know about
Hot flashes affect 9.7 percent of women taking raloxifene 60 mg, compared with 6.4 percent on placebo. Leg cramps affect 7.0 percent of women, compared with 3.7 percent on placebo. Flu-like syndrome is reported in 13.5 percent, compared with 11.4 percent on placebo, and peripheral edema in 5.2 percent, compared with 4.4 percent.
The important risk to know about is vascular. Raloxifene increases the risk of venous thromboembolism, roughly 1 case per 100 treated patients: in the MORE trial, 26 cases on raloxifene versus 11 on placebo, giving a hazard ratio of 2.4 (95 percent confidence interval of 1.2 to 4.5). A boxed warning flags this risk of deep vein thrombosis and pulmonary embolism, as well as an increased risk of death from stroke in women with coronary heart disease or at high risk of it.
Contraindications, interactions and monitoring
Some situations rule out raloxifene. It is contraindicated in case of a history or an active episode of venous thromboembolism, and during pregnancy or breastfeeding. A planned long trip spent sitting still or a hospital stay with bed rest is worth mentioning to the physician, because such situations raise the venous risk.
Two interactions call for caution. Cholestyramine, a drug that binds bile acids, reduces the absorption and the enterohepatic cycle of raloxifene: the two should not be taken together. With warfarin, an anticoagulant, raloxifene can alter prothrombin time, a measure of coagulation that then needs to be monitored. Follow-up of the treatment combines measuring bone density over time with attention to these vascular signals.
Sources
Related molecules
To explore within the « Bones and joints » family and its neighbours.
See the entire « Bones and joints » family · Back to the atlas
Supplements to consider
Beyond the plate, a single isolated nutrient can be worth discussing, to confirm with your doctor or pharmacist. Here is which one and in which form.
Calcium
Calcium is the most abundant mineral in the body, involved in bone health. Calcium citrate is well absorbed, including away from meals, whereas carbonate requires an acidic environment for its absorption.
Preferred form calcium citrate (does not depend on gastric acidity)
Vitamin D3 (cholecalciferol)
Vitamin D is a fat-soluble vitamin. The D3 form (cholecalciferol) is the one adopted by most guidelines. It is better absorbed when taken during a meal that contains fats.
Preferred form D3 (cholecalciferol), during a fatty meal
Frequently asked questions
What are the side effects of raloxifene?
The package leaflet notably lists hot flushes, leg cramps, flu-like symptoms and possible swelling of the limbs. The most closely monitored risk involves venous thromboembolic events, such as phlebitis. For the full list and what applies to you, refer to the leaflet and speak with your doctor or pharmacist.
What are the contraindications of raloxifene?
Raloxifene is notably contraindicated in people with a history of, or a risk of, venous thromboembolic events, and it is usually stopped during prolonged immobilization. These situations need to be assessed case by case. Check the contraindications in the leaflet and confirm your situation with your doctor.
Does raloxifene have any drug interactions?
For example, the leaflet flags an interaction with cholestyramine, which can reduce the absorption of raloxifene, as well as caution with certain oral anticoagulants. Report all of your treatments, including over-the-counter ones. Your pharmacist or doctor is best placed to check your combinations.
Does raloxifene cause weight gain?
Weight gain is not described as a characteristic effect of raloxifene in its leaflet, even though swelling of the lower limbs can occur. If you notice a change in weight that worries you, talk to your doctor rather than adjusting anything on your own.
Do you need calcium and vitamin D during osteoporosis treatment?
The raloxifene summary of product characteristics recommends considering calcium and vitamin D intake when diet does not sufficiently cover your needs, since these two nutrients support bone metabolism. This is a nutrition point that supports the overall care, not a treatment in itself. A vitamin D blood test and a review of your dietary intake with your doctor help determine whether a supplement is useful.
Which form of calcium and vitamin D is best if diet falls short?
For vitamin D, the best documented form is cholecalciferol (vitamin D3). For calcium, calcium citrate is regarded as well absorbed and largely independent of stomach acidity, while calcium carbonate remains a common option to take with a meal. Whether a supplement is worthwhile and which form to choose depend on your actual intake and a possible blood test, decided with your doctor.
Ces réponses portent sur le volet nutritionnel. Pour toute question sur votre médicament, la notice et votre médecin ou pharmacien font foi.