Raloxifene

Brand names of raloxifene

  • Evista

Regulating the formation and destruction of bones is one of the many actions that are performed by the hormone estrogen. Two medical conditions that could cause a decrease in estrogen levels in women are the removal of ovaries and post menopausal effects. Lower levels of estrogen lead to osteoporosis which results in loss of bone density and weak bones.

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Though not at par with estrogen, raloxifene helps to increase bone density and reduce bone turnover. As bones become stronger women with osteoporosis will see reduction in fractures with intake of raloxifene.

Raloxifene affects some tissues in the body just like estrogen but not others, and not with the same intensity. Raloxifene reduces "bad" cholesterol levels in the blood that is low density lipoprotein (LDL) but does not increase high density lipoprotein or "good" cholesterol and that is why raloxifene is also called a "selective estrogen receptor modulator."

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Things you need to tell your physician before taking raloxifene

If you are allergic to raloxifene then you must tell your doctor or pharmacist about it before you start taking this medicine. Moreover you need to speak to your pharmacist in detail about some inactive ingredients which could be present in this medication and which could lead to allergic reactions.

Raloxifene is to be avoided in certain medical conditions, so before taking the medication speak to your doctor if you have a history of blood clotting in conditions like deep venous thrombosis, pulmonary embolism and in retinal vein thrombosis.

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Blood clot risk could increase with physical inactivity. The doctor is likely to discontinue the medication at least 3 days before surgery and if there is a long period of inactivity as there is likely to be less movement because of bed rest after surgery. Raloxifene should not be restarted unless active routine movements are on track like before. When you are travelling for long periods ensure that you walk or at least keep moving periodically so that blood flows freely through the body.

If you have a medical history then it should be brought to your pharmacist's or doctor's notice before you begin taking raloxifene especially if you have suffered from kidney or liver disease, high blood pressure, heart or blood vessel diseases like  congestive heart failure, atrial fibrillation, transient ischemic attack, stroke, high blood cholesterol levels, history of high levels of triglycerides or blood fat because of treatment with estrogen and also if you smoke.

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Raloxifene could harm the unborn fetus and so it should not be taken during pregnancy and in the event that you become pregnant or if you think you might be pregnant then the doctor should be notified immediately. There is no relevant data that lets us know if this medication is passed into breast milk but breast feeding should be avoided. It is best to discuss it with your doctor if you are breast feeding.

Usage

Raloxifene is used to treat and prevent osteoporosis in women after menopause. Strengthening bones reduces the risk of fractures as bone mass is preserved. Raloxifene acts like estrogen in some parts of the body but is mostly different from some other hormones like progestin.

The advantage raloxifene has over estrogen is that it does not stimulate uterine tissue lining (endometrium) to grow and so the risk of cancer in the uterus is reduced and the risk of invasive breast cancer, which could occur in women after menopause, is also decreased. However it cannot be used to treat hot flushes, which are symptoms of menopause. Raloxifene should not be taken by women who have yet to reach menopause and neither should children be given this medication. It is also not recommended for the prevention of heart disease.

How to use raloxifene

Before you start taking raloxifene and each time you get a refill you must read the medication guide that is always available with the pharmacist. Any further questions would need consultation with the doctor or pharmacist.

Unless the doctor has given other directions raloxifene is taken orally in the mouth, most often once a day with food or without it. To get the maximum benefit from the medication take it regularly and it works best if you take it at the same time every day.

Sufficient amounts of calcium and vitamin D should be included in your diet. Consult the doctor or pharmacist who can advise you if they see a need for you to take calcium or vitamin D supplements.

Raloxifene can be easily absorbed through the skin and lungs and so women who are pregnant should avoid coming into contact with the medication and should also ensure they do not breathe the dust from tablets if they want to keep their unborn child safe.

How raloxifene works

Certain cells in the body reabsorb minerals and other bone components so broken down bone can be reformed anew as a process where healthy bone tissues are remodelled continuously. The activity of these cells that resorb bone is suppressed when raloxifene is taken and so bone tissue breakdown is slower than the formation of new bone and so both bone density and strength are preserved.

After menopause estrogen levels decrease and this causes increase in the speed of bone resorption leading to faster bone loss. Initially this bone loss is faster because the parallel increase in bone formation in not adequate enough to counter resorptive loss of bone. Another reason for the imbalance between resorption and formation, besides loss of estrogen, could be due to the impairment of osteoblasts or precursors, due to age. The changes that some women will eventually have to deal with after menopause are osteoporosis, decrease in bone mass, risk of fractures in the spine, hip and wrist. Most osteoporotic fractures experienced are of a vertical nature.

Raloxifene is a selective estrogen receptor modulator (SERM) and it mediates by biologically binding itself to estrogen receptors. This mediation causes certain estrogenic pathways to become active while others are blocked. In this way it is both an estrogen agonist and also an estrogen antagonist.

On taking raloxifene, biochemical markers of bone turnover and bone resorption are both reduced to levels they were at before menopause. These changes are visible in reduced levels of serum and urine in bone turnover markers, reduction in bone resorption as observed through radio calcium kinetic studies. Also seen is an increase in bone mineral density (BMD) and the incidence of fractures perceptibly declines.

Side effects

Common
Less common

Possible interactions

Phytoestrogens absorbed from soy or other plants could work to complement raloxifene. A synthetic flavonoid, ipriflavone, is being investigated for osteoporosis as it could reduce bone resorption by cutting osteoclast use and encouraging osteoblast functioning.

Most people require between 1,000 mg to 1,500 mg of calcium a day. There is about 200 mg of calcium in an average American's diet, so you must ensure that you are taking enough calcium in your diet as well as vitamin D and also soaking in adequate amounts of sunshine. Calcium that is effervescent as it turns into a solution is absorbed more quickly then calcium in other forms. This helps in the prevention of osteoporosis. However you must watch out if you are taking soda as a beverage as phosphorous intake should be controlled.

Storage instructions

Raloxifene is easily stored at room temperature between 68-77°F which is 20-25°C and for brief periods of time it can be stored between 59-86°F or 15-30°C. The medicine should not be stored in the bathroom and should be kept away from heat and moisture and out of reach of children and pets.

Flushing medicine down the toilet or pouring it into the drain may not be the correct way of disposing unused medication, unless advised to do so. Consult your pharmacist or your area waste disposal company as to how to safely dispose medicine which has expired or is not needed anymore.

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