Targretin

DRUG DESCRIPTION

Targretin® (bexarotene) is a member of a subclass of retinoids that selectively activate retinoid X receptors (RXRs). These retinoid receptors have biologic activity distinct from that of retinoic acid receptors (RARs). Each soft gelatin capsule for oral administration contains 75 mg of bexarotene.

The chemical name is 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl) ethenyl] benzoic acid, and the structural formula is as follows:

Targretin® (bexarotene) capsules  Structural Formula Illustration

Bexarotene is an off-white to white powder with a molecular weight of 348.48 and a molecular formula of C24H28O2. It is insoluble in water and slightly soluble in vegetable oils and ethanol, USP.

Each Targretin® (bexarotene) capsule also contains the following inactive ingredients: polyethylene glycol 400, NF, polysorbate 20, NF, povidone, USP, and butylated hydroxyanisole, NF. The capsule shell contains gelatin, NF, sorbitol special-glycerin blend, and titanium dioxide, USP.

What are the possible side effects of bexarotene (Targretin)?

If you experience any of the following serious side effects, stop taking bexarotene and seek emergency medical attention:

  • an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives); or
  • symptoms of pancreatitis (inflammation of the pancreas) such as persistent nausea, vomiting, and abdominal or back pain.

Other, less serious side effects may be more likely to occur. Continue to take bexarotene and talk to your doctor if you experience:

    ...

Read All Potential Side Effects and See Pictures of Targretin »

What are the precautions when taking bexarotene (Targretin)?

Before taking bexarotene, tell your doctor or pharmacist if you are allergic to it; or to other retinoids such as isotretinoin, acitretin, etretinate, tretinoin; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

This medication should not be used if you have certain medical conditions. Before taking this medicine, consult your doctor or pharmacist if you have: pancreatitis.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: frequent alcohol use, cataracts, high blood fats (high cholesterol/triglyceride), diabetes, gallbladder disease, liver problems, thyroid problems (e.g.,...

Read All Potential Precautions of Targretin »


Targretin Consumer (continued)

SIDE EFFECTS: Headache, tiredness, nausea, vomiting, dry skin, diarrhea, or trouble sleeping may occur. If any of these effects persist or worsen, notify your doctor.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

This medication can frequently increase the level of "bad" fats (cholesterol/triglyceride) in your blood. Your doctor will order blood tests to measure these fats. If your blood fat levels get too high, your bexarotene dose may need to be lowered or stopped, or you may need to start cholesterol medication.

This medication can cause an underactive thyroid (hypothyroidism). Tell your doctor immediately if any of these symptoms of low thyroid occur: unusual weight gain, feeling cold, constipation, slow heartbeat, low on energy. Your doctor will order a blood test and may start you on thyroid medication.

Tell your doctor immediately if any of these unlikely but serious side effects occur: stomach pain, swelling of the hands/feet, muscle pain/stiffness/cramps, fast/pounding heartbeat.

Tell your doctor immediately if any of these rare but very serious side effects occur: severe abdominal/back/stomach pain, persistent nausea/vomiting, dark urine, vision changes, yellowing eyes and skin.

This medication can lower the body's ability to fight an infection. Notify your doctor promptly if you develop any signs of an infection such as fever, chills, or persistent sore throat.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice the following symptoms of an allergic reaction: rash, itching/swelling (especially of the face/tongue/throat), dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking bexarotene, tell your doctor or pharmacist if you are allergic to it; or to other retinoids such as isotretinoin, acitretin, etretinate, tretinoin; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

This medication should not be used if you have certain medical conditions. Before taking this medicine, consult your doctor or pharmacist if you have: pancreatitis.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: frequent alcohol use, cataracts, high blood fats (high cholesterol/triglyceride), diabetes, gallbladder disease, liver problems, thyroid problems (e.g., hypothyroidism).

This medication may make you more sensitive to the sun. Avoid prolonged sun exposure, tanning booths, and sunlamps. Use a sunscreen and wear protective clothing when outdoors.

Because this medication can lower your body's ability to fight an infection, wash your hands frequently to prevent the spread of infection.

This medication must not be used during pregnancy. If you become pregnant or think you may be pregnant, inform your doctor immediately. (See also Warning section.)

It is not known if this drug passes into breast milk. Due to the possible harm to the nursing infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.


Targretin Patient Information Including Side Effects

Brand Names: Targretin

Generic Name: bexarotene (Pronunciation: beks AIR oh teen)

  • What is bexarotene (Targretin)?
  • What are the possible side effects of bexarotene (Targretin)?
  • What is the most important information I should know about bexarotene (Targretin)?
  • What should I discuss with my healthcare provider before using bexarotene (Targretin)?
  • How should I use bexarotene (Targretin)?
  • What happens if I miss a dose (Targretin)?
  • What happens if I overdose (Targretin)?
  • What should I avoid while using bexarotene (Targretin)?
  • What other drugs will affect bexarotene (Targretin)?
  • Where can I get more information?

What is bexarotene (Targretin)?

The exact way bexarotene works is unknown, but it is believed to inhibit the growth of tumor cells.

Bexarotene is used to treat skin lesions of cutaneous T-cell lymphoma (CTCL) in patients who have not responded to or not tolerated other therapies.

Bexarotene may also be used for purposes other than those listed in this medication guide.

What are the possible side effects of bexarotene (Targretin)?

If you experience any of the following serious side effects, stop taking bexarotene and seek emergency medical attention:

  • an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives); or
  • symptoms of pancreatitis (inflammation of the pancreas) such as persistent nausea, vomiting, and abdominal or back pain.

Other, less serious side effects may be more likely to occur. Continue to take bexarotene and talk to your doctor if you experience:

  • an increase in fats in the blood (blood lipids) such as cholesterol or triglycerides (blood tests will detect this);
  • a underactive thyroid (blood tests will detect this);
  • blood problems;
  • headache;
  • fatigue;
  • weakness or loss of strength;
  • swelling;
  • rash;
  • dry skin;
  • infections;
  • nausea; or
  • diarrhea.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side effects to FDA at 1-800-FDA-1088.

What is the most important information I should know about bexarotene (Targretin)?

Avoid prolonged exposure to sunlight or artificial ultraviolet light (e.g. sunlamps). Bexarotene may increase the sensitivity of your skin to sunlight. Use a sunscreen and wear protective clothing when exposure to the sun is unavoidable.

Do not take bexarotene if you are pregnant or if you could become pregnant. Bexarotene is in the FDA pregnancy category X. This means that bexarotene will cause birth defects in an unborn baby. You must take a pregnancy test and have negative results within one week before starting treatment with bexarotene, and a pregnancy test should be repeated monthly during treatment. Bexarotene should be started on the second or third day of a normal menstrual period. Also, you will need to use two reliable forms of birth control at the same time for one month before starting treatment with bexarotene, during treatment with bexarotene, and for at least 1 month following the end of your treatment. If you become pregnant, stop using birth control, or miss your menstrual period, immediately stop taking bexarotene and notify your doctor. Men taking bexarotene with sexual partners who are pregnant, possibly pregnant, or who could become pregnant, must use condoms during sexual intercourse while using bexarotene and for at least one month after the last dose of bexarotene.

Swallow each capsule whole. Do not chew them, dissolve them in liquid, or allow them to dissolve in your mouth.

Your doctor will want to monitor the levels of lipids (triglycerides and cholesterol) and thyroid hormones in your blood periodically during treatment with bexarotene. Treatment may be necessary if your cholesterol or triglyceride levels become elevated, or if your thyroid hormone levels are low.

Grapefruit and grapefruit juice may interact with bexarotene. The interaction could have potentially dangerous effects. Discuss the use of grapefruit and grapefruit juice with your doctor. Do not increase or decrease the amount of grapefruit products in your diet without first talking to your doctor.

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