Drug Detail:Raloxifene (Raloxifene [ ra-lox-i-feen ])
Drug Class: Hormones / antineoplastics Selective estrogen receptor modulators
1. How it works
- Raloxifene decreases bone resorption and turnover and may be used for the treatment or prevention of osteoporosis.
- Raloxifene is not a hormone but it works by mimicking the action of estrogen on bones while at the same time blocking the effect of estrogen on other tissues.
- Raloxifene belongs to the class of medicines known as estrogen agonist/antagonists (also called selective estrogen receptor modulators [SERMs]).
2. Upsides
- May be used for the treatment or prevention of osteoporosis in postmenopausal women.
- May also be given to lower the risk of invasive breast cancer in postmenopausal women with osteoporosis, or other postmenopausal women at risk of invasive breast cancer.
- Long-term use of raloxifene does not carry the same risk to breast and womb tissue associated with estrogen-based hormone therapies.
- Raloxifene is usually taken as a once-daily dose.
- Raloxifene is available as a generic and under the brand name Evista.
3. Downsides
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Hot flashes, joint or muscle pain, difficulty sleeping, weight gain, increased vaginal discharge, gastrointestinal complaints (such as indigestion, bloating, gas, nausea), flu-like syndromes, infection, sinusitis, and a rash.
- Raloxifene has only been tested in postmenopausal women.
- May increase the risk of blood clots that occur in the leg (deep vein thrombosis), lung (pulmonary embolism), or eye. May also increase the risk of stroke; the risk is higher in women with coronary heart disease, diabetes, high blood pressure, high cholesterol, going through menopause, who smoke, or who are overweight.
- Raloxifene may increase the incidence of hot flushes and leg cramps.
- May not be as effective as bisphosphonates or estrogen at preventing bone loss.
- Although raloxifene may be used to reduce the risk of invasive breast cancer in postmenopausal women, it does not treat breast cancer and is not a cancer medicine.
- May not be suitable for some people, including those with a history of blood clots, cardiovascular disease, liver or kidney disease, high triglycerides, with a history of breast cancer, or who take certain medications (such as warfarin, statins, or estrogen replacement therapy). Avoid raloxifene in women who are pregnant or breastfeeding.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Tips
- May be taken with or without food.
- Your doctor may advise you to take supplements such as calcium or vitamin D while you are taking raloxifene. Take them as directed.
- Keep your appointments with your doctor, even if you feel well. An appointment is how your doctor can check that raloxifene is effective for you and how you are tolerating raloxifene.
- If you have surgery scheduled, tell your doctor you are taking raloxifene because it may need to be temporarily discontinued about three days before surgery if you will be experiencing periods of inactivity or bed rest. Also, tell your doctor if you are planning to go on a long trip or plane flight and will be inactive for long periods.
- Tell your doctor if you experience any vaginal bleeding, breast pain or enlargement, or swelling of the hands or feet. Seek urgent medical help if you experience any shortness of breath, calf pain, or chest pain.
- Weight-bearing exercise can help osteoporosis and you should talk to your doctor about exercises that are recommended.
- Raloxifene should only be given to postmenopausal women but if you inadvertently become pregnant during treatment tell your doctor immediately.
5. Response and effectiveness
- Research has shown that raloxifene significantly and consistently suppressed bone turnover within three months and this persisted for the duration of the trial (24 or 36 months).
- Decreases in levels of other minerals, such as total calcium, total protein, albumin, and inorganic phosphate were small and less than that typically seen with estrogen or hormone therapy.
- Spine and hip bone mineral density increased by 2-3% with raloxifene administration.
6. Interactions
Medicines that interact with raloxifene may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with raloxifene. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with raloxifene include:
- anticoagulants, such as warfarin
- cholestyramine and colestipol
- diazepam
- diazoxide
- estrogen preparations
- levothyroxine
- lidocaine
- ospemifene
- tranexamic acid.
Note that this list is not all-inclusive and includes only common medications that may interact with raloxifene, You should refer to the prescribing information for raloxifene for a complete list of interactions.