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bexarotene bexarotene

 
  Trade/other name(s)
Targretin
 
  Pronunciation: bex-air-uh-teen  
  Why would this drug be used?
Bexarotene capsules are used to treat skin lesions caused by cutaneous T-cell lymphoma that did not respond to prior systemic treatment. The 1% topical gel (for use on the skin) is used to treat early stage skin lesions of cutaneous T-cell lymphoma that no longer responds to other treatments.
 
  How does this drug work?
Bexarotene is a retinoid used in molecular targeted therapy. A retinoid occurs naturally in the body and helps regulate, or control, the gene functions that help cells grow and divide. Bexarotene "activates" certain retinoid receptors on the cancer cell. The "turned on" receptor works with other substances to control cancer cell growth and division.
 
  Before taking this medicine

Tell your doctor:
 
 
  • If you are allergic to anything, including medicines, dyes, additives, or foods.
  • If you have any medical conditions such as liver disease (including hepatitis), kidney disease, or diabetes. These conditions may require that your medicine dose, regimen, or timing be changed.
  • If you have ever had pancreatitis or gallbladder disease. Bexarotine can cause these problems or make them worse.
  • If you have high triglycerides or cholesterol (lipids or fats) in the blood. This drug can raise these levels higher.
  • If you drink a lot of alcohol. You are more likely to have problems with your liver or pancreas while on this drug.
  • If you are pregnant, trying to get pregnant, or if there is any chance of pregnancy. This drug may cause birth defects if either the male or female is taking it at the time of conception or during pregnancy. Men and women who are taking this drug need to use 2 kinds of birth control during treatment and for a month after treatment is done. It is important to check with your doctor about what kinds of birth control can be used with this medicine.
  • If you are breast-feeding. The drug may pass into breast milk and harm the baby. Breast feeding is not recommended while you are taking bexarotene.
  • About any other prescription or over-the-counter medicines you are taking, including vitamins and herbs.
 
  Interactions with other drugs
If gemfibrozil is taken with bexarotene it can increase blood levels of bexarotene and raise the risk of side effects.

Bexarotene can increase the risk of low blood sugar if you are taking medicine for diabetes, such as insulin, pioglitazone (Actos), rosiglitazone (Avandia), acetohexamide (Dymelor), chlorpropamide (Diabinese), glimepiride (Amaryl), glipizide (Glucotrol), glyburide (DiaBeta), tolazamide (Tolinase), or tolbutamide (Orinase).

Vitamin A supplements from animal sources (such as fish liver oil) can cause toxic levels of Vitamin A in the body when taken during treatment with bexarotene. Do not take more than 4000 or 5000 IU of Vitamin A per day while on bexarotene. Vitamin A precursors from vegetable sources (such as beta carotene) are not a problem.

Bexarotene can cause large amounts of DEET (from insect repellant) to be absorbed through the skin and get into your blood.

Ketoconazole may cause bexarotene to build up in the body, which worsens the chance of serious side effects. Limited testing for these kinds of drug interactions with bexarotene is available, but drugs that cause problems when given with similar medicines include cimetidine, erythromycin, verapamil, diltiazem, cyclosporine, and others.

Anti-seizure medicines such as carbamazepine, phenobarbital, and phenytoin can cause the body to get rid of bexarotene too quickly, so that it doesn't work well. Rifampin and rifabutin (TB drugs) can do the same thing.

Certain medicines that are used for infection, pain, inflammation, high blood pressure, and mental illness may increase the risk of blood problems if taken with bexarotene. Check with your doctor, nurse, or pharmacist about the other medicines, vitamins, herbs, and supplements you are taking.

 
  Interactions with foods
Grapefruit or grapefruit juice can raise the level of this drug in your body. This can worsen any bad effects the drug may have on you and may increase its action in a harmful way. Check with your doctor, nurse, or pharmacist about whether other foods may be a problem.
 
 
Tell all the doctors, dentists, nurses, and pharmacists you visit that you are taking this drug.


 
  How is this drug taken or given?
Bexarotene is taken as a capsule by mouth with food. The dose of bexarotene depends on your size. To start, you will take the drug every day,( for up to 97 weeks) until a response is seen Sometimes the bexarotene dose needs to be lowered if you have a lot of side effects. If the side effects go away on a lowered dose, then your doctor may try to slowly increase the dose again.

Do not break, chew, or dissolve capsules, and do not handle any that have been broken. If you get any of the capsule's contents on your skin, wash it off with soap and water and call your doctor or pharmacist for further instructions.

Bexarotene also comes in the form of a gel that can be used on skin lesions. Usually, it is applied every other day for the first week, once a day the next week, then increased each week until it is being used 4 times a day. Apply just enough to cover the lesion. You can spread the gel with a cotton swab or your fingers. If you use your fingers, wash your hands thoroughly afterward so that none of the medicine gets into your eyes, nose, or mouth. Never use the gel near mucous membranes (eyes, nose, mouth, rectal area, or vagina). Wait until the gel completely dries before covering it with clothing. Do not bandage the area where the gel is applied unless your doctor tells you to do so.

Take this drug exactly as directed by your doctor. If you do not understand the instructions, ask your doctor or nurse to explain them to you. Keep the medicine in a tightly closed container out of heat, light, and humidity, and out of the reach of children and pets.

 
  Precautions
Sunlight, sun lamps, and tanning beds can cause severe sunburn while you are using bexarotene.

Bexarotene capsules may cause cataracts in your eyes. Make sure that you tell your doctor right away if your vision changes during treatment.

Your doctor will likely test your blood throughout your treatment, looking for possible effects of the drug on blood counts or on other body organs, such as increased triglycerides and total cholesterol, decreased HDL, increased blood levels of liver function, decreased blood levels of thyroid function, increased LDH, and decreased white blood cells.. Based on the test results, you may be given medicines to help treat any effects. Your doctor may also need to reduce or delay your next dose of this drug, or even stop it altogether.

Report signs of low thyroid function, such as weight gain, tiredness, slowed thinking, skin dryness, constipation, feeling cold all the time, low energy, or joint pain or stiffness.

You may have to take medicine to lower your blood lipid levels or to get your thyroid hormone levels back to normal while you are taking bexarotene. Usually your doctor monitors these blood values closely. Changes in blood lipid level and thyroid function generally go back to normal after the treatment is finished.

This drug can increase your chance of getting an infection. Be sure to let your doctor or nurse know right away if you have any signs of infection, such as fever (100.5° or higher), shaking chills, pain when passing urine, a new cough, or bringing up sputum.

This drug may increase your risk of bleeding. Speak with your doctor before taking any drugs or supplements that might affect your body's ability to stop bleeding, such as aspirin or aspirin-containing medicines, warfarin (Coumadin), or vitamin E. Tell your doctor right away if you have unusual bruising, or bleeding such as nosebleeds, bleeding gums when you brush your teeth, or black, tarry stools.

Do not get any immunizations (vaccinations), either during or after treatment with this drug, without your doctor's OK. This drug may affect your immune system, which could make vaccinations ineffective, or could even lead to serious infections. Try to avoid contact with people who have recently received a live virus vaccine, such as the oral polio vaccine or smallpox vaccine. Check with your doctor about this.

Call your doctor if you have nausea, vomiting, pain in your back or abdomen, or appetite loss. These can be signs of pancreatitis, a dangerous complication.

Report rash, severe pain at application site (gel), or peeling of skin right away.

 
 
Possible side effects
 
  Common
  • increased blood lipid levels (fasting triglycerides, cholesterol)*
  • decreased blood HDL cholesterol ("good cholesterol") level
  • low thyroid function, which may require treatment*
  • headache
  • diarrhea
  • itching (gel)
  • rash (gel)*
  • pain at application site (gel)*
 
  Less common
  • weakness or listlessness
  • flu-like symptoms
  • low white blood cells with increased risk of infection*
  • back pain*
  • rash
  • abdominal pain*
  • peeling of skin
  • fever and chills*
  • hair loss
  • difficulty sleeping
  • swelling of the hands, feet or ankles
 
  Rare
  • increased blood level of liver function tests, possible liver damage
  • nausea*
  • vomiting*
  • pancreatitis*
  • loss of appetite*
  • bleeding*
  • cataracts*
  • allergic reaction, with trouble breathing, skin welts, itching, dizziness, or swelling of the face, mouth, or throat
  • birth defects if taken during pregnancy, or if pregnancy occurs up to a month after taking the drug

*See "Precautions" section for more detailed information

 
 
There are other side effects not listed above that can also occur in some patients. Tell your doctor or nurse if you develop these or any other problems.
 
 
 
  FDA approval
Yes - first approved in 1999
 
 
 
  Disclaimer: This information does not cover all possible uses, actions, precautions, side effects, or interactions. It is not intended as medical advice, and should not be relied upon as a substitute for talking with your doctor, who is familiar with your medical needs.  


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