Raloxifene – Oral Route

Raloxifene is similar to an estrogen drug and works by lowering the concentration of bad cholesterols in the blood.

Overview

Raloxifene is a prescription-only medication that is given to women that have passed through the menopause to prevent their bones thinning. The drug can also treat bones that have already begun thinning. It is a similar substance to an estrogen, the female sex hormone, and stops bone loss that can occur in post-menopausal women.

Estrogen is a hormone that is produced by the ovaries and helps to keep the bones healthy and strong. When a woman goes through the menopause, she loses a large amount of estrogen as the ovaries stop producing the hormone. This can then cause brittle or soft bones, leading to a condition called osteoporosis. The effects of osteoporosis can be prevented or controlled by using an estrogen replacement, which slows down the loss of bone and improves the way the body stores and retains calcium (which contributes to strong and healthy bones).

Raloxifene works by acting like an estrogen, preventing the loss of bone. It lowers the concentration of bad cholesterols (low density lipoprotein cholesterol). It does not, however, increase the concentration of good cholesterol (which helps to improve bone density).

Raloxifene is a medication that is more suited to control the loss of bone density. It is not as effective at increasing bone density as some other drugs, such as conjugated estrogens. It also does not treat some of the common symptoms of the menopause, such as hot flushes, and it does not provide stimulation to the uterus or breast.

This medication is also used to decrease the chance of a post-menopausal woman developing invasive breast cancer later in life.

Raloxifene is also sold and marketed under the brand name Evista in the United States.

Conditions treated

  • Osteoperosis
  • Prevention of osteoporosis

Type of medication

  • Tablet

 

Side effects

Some patients that start taking Raloxifene could experience various side effects. Although most are not serious, there are some that may require medical attention. Not everyone will experience all of the side effects listed – in fact most people only experience one or two, or none at all – and they will usually subside on their own after a few days. Side effects are most commonly experienced as a result of the body not being used to a new drug being in its system. Therefore, side effects will usually happen at the start of a treatment plan.

Common side effects include:

  • Hot flushes or feeling faint
  • Headaches
  • Dizziness or feeling like the room is spinning
  • Nausea or vomiting
  • Pain in the stomach
  • Pain in the leg
  • Painful joints
  • Excessive sweating, even when it is not particularly warm

There are some side effects that, although rare, can be very harmful to patients. Those that experience any of the below complications must seek medical advice at once. It is likely that the patient will require medical treatment and may need to stop taking Raloxifene.

  • Sudden and severe headache
  • Confusion, anxiety, disorientation or difficulty speaking
  • Loss of balance
  • Pain in the chest
  • Persistent coughing or wheezing
  • Difficulty breathing or short, sharp breaths
  • Change in heart rate, usually an increase or irregularities
  • Sudden feeling of weakness or numbness, particularly on one side of the body
  • High fever, flu-like symptoms or chills
  • Severe sore throat
  • Body aches
  • Tenderness, pain or swelling in the breast
  • A lump in the breast
  • Severe pain in the lower back
  • Vaginal bleeding or spotting that is unusual in any way

Dosage

This medication should be taken exactly as your doctor recommends. Patients should not attempt to alter their own doses and should speak to their doctor if they think that the medicine is not working. Your individual dosage will depend on a number of things, such as your medical history, the severity of your bone condition, your likelihood of developing osteoporosis and any other drugs that you may be taking.

The medication should be taken once per day, at the same time every day if possible. You can take Raloxifene with or without a meal.

Your medication will be provided in blister packets of 15 tablets. Most are labeled according to the day of the week to make it easier to keep track of when you last took a dose.

The usual dosage of Raloxifene prescribed to patients without any other medical complications is 60 mg. Each tablet will contain 60 mg, so you will only need to take one dose per day.

Doctors may also recommend that patients add supplements of vitamin D and calcium to their daily dosage. These natural substances help strengthen the bones and help prevent the body from developing osteoporosis.

Interactions

There are certain drugs that should not be taken at the same time. This is because they can cause an interaction when mixed together, and this can cause several unwanted or even unknown side effects in the human body. Not all drug interactions are dangerous, and some may mean that you just need an altered dose of either medication. However, those that have major interactions should be avoided as a combination. There are several drugs that have a major interaction with Raloxifene. See the list of these drugs and their brand names below. Be sure to tell your doctor if you are taking these, as it will probably mean that Raloxifene is not a suitable treatment for you if your other medications cannot be altered:

  • Bexarotene
  • Carfilzomib
  • Pomalidomide
  • Thalomid (thalidomide)
  • Tranexamic acid
  • Cyklokapron (tranexamic acid)
  • Pomalyst (pomalidomide)
  • Revlimid (lenalidomide)
  • Targretin (bexarotene)
  • Thalidomide
  • Kyprolis (carfilzomib)
  • Lenalidomide
  • Lysteda (tranexamic acid)

Warnings

Risk of deep vein thrombosis

Women that have a history of this condition should not take Raloxifene. The drug increases the risk of the patient developing the condition – there have been various reports through medical studies of cases of deep vein thrombosis and pulmonary embolism.

Increased risk of death from stroke

There is also an increased risk of death from suffering a stroke for patients that are taking this medication. Raloxifene is therefore unsuitable for post-menopausal women that have a history of stroke. This risk is more prevalent in women that have documented coronary heart disease or are at a greater risk of major coronary health complications.

Breast cancer

A higher risk of developing breast cancer has also been identified in patients that have taken Raloxifene. The drug should not be taken by those that have the condition, are at risk of developing the condition, or have had one or more first-degree relatives with the condition. Patients should monitor their breasts regularly for lumps and report any abnormalities to a doctor immediately.

Pregnancy and breast feeding

Although this medication is unlikely to be used in women of childbearing age, it should not be used in women who are pregnant or think they may be pregnant. The medicine can cause birth defects and can cause harm to the fetus in human pregnancy. If you become pregnant while taking this medication, you must tell your doctor immediately.

It is not known whether Raloxifene passes into breast milk. However, it is not advisable to take this medication while you are breast feeding.

Surgery

If you require surgery while you are taking this medication, you should stop taking it for 72 hours prior to the operation. You should also notify any doctor that is involved in your operation that you are taking Raloxifene.

Disease interactions

Before you start taking Raloxifene, you need to tell your doctor if you have any other health conditions or diseases. This is because taking Raloxifene could be harmful to those conditions, aggravating them or causing dangerous interactions. Tell your doctor about any of the following:

  • Heart disease
  • High blood pressure
  • History of TIA
  • High triglycerides
  • Breast cancer
  • Coronary artery disease
  • Liver disease
  • Kidney disease
  • History of stroke

Menopause

This drug is intended for use in women that have gone through the menopause already. If you have not yet gone through the menopause, you should let your medical provider know, and a different medication may be provided to you.

Activity

You should remain active while taking Raloxifene. Undergoing regular exercise is the best way to stay healthy while taking the medication, as well as also helping it to work to its maximum capacity. You should not sit still for long periods of time, particularly during travel; try to move around every now and then. This drug is generally not suitable for those that are inactive or immobile.

Smoking and alcohol

It is not advisable to smoke while you are taking Raloxifene. Smoking can increase the risk of developing health complications that are related to Raloxifene.

It is also recommended that alcohol intake is kept to a minimum while taking this medicine. Taking Raloxifene and alcohol can increase the risk of adverse reactions such as headaches, nausea, vomiting, dizziness and loss of judgment.

Storage

Raloxifene is a tablet and is therefore most effective when stored in dry, temperate conditions. Try to keep your tablets at room temperature (around 20 to 25 degrees centigrade) and do not keep them close to heat sources like radiators, or near to ovens or stoves. Also, keep the tablets in their box, away from direct sunlight. If they have been supplied with a drying agent, leave this in the box with the tablets at all times and do not throw it away.

Summary

Raloxifene is a popular and reliable choice for those that are suffering from brittle or soft bones as a result of having been through the menopause. There are many clinical studies that show the drug to be safe, effective and suitable as a long-term treatment against the prevention of osteoporosis. As a result, Raloxifene has been a medication of choice for doctors for many years.

The drug has very few major interactions, particularly compared to some of its alternative counterparts; therefore, it offers greater flexibility to patients that may need to take additional prescription or over the counter medications for other purposes.

Despite being generally safe and effective, compared to some of its counterparts, there are some risks that have been identified in taking Raloxifene. The drug comes with an increased risk of death by stroke, breast cancer and deep vein thrombosis, and therefore may be unsuitable for patients with a history of these conditions, or a vulnerability to contracting them. Although side effects are usually minor or non-existent for those taking Raloxifene, the patient should be monitored closely for any signs of more serious conditions developing.

Patients can also help to decrease their risks of suffering side effects or health complications by telling their doctors about their full medical history and any other drugs they may be taking.

Raloxifene is usually prescribed to patients along with other medications, dietary supplements such as calcium, and a healthy lifestyle. To protect the body against osteoporosis and to keep bones strong and healthy, the patient must also make the effort to engage in regular exercise and consume foods that are high in vitamin D and calcium. Provided Raloxifene is taken according to its specific instructions, it can improve the quality of life for post-menopausal women with signs of brittle bones and can help them to stay comfortable and active for longer.

 

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Last Reviewed:
January 31, 2018
Last Updated:
January 27, 2018
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