Bicalutamide – Uses, Dosage, Side Effects, Interaction

Indications

  • For treatment (together with surgery or LHRH analog) of advanced prostatic cancer.
  • Bicalutamide is a nonsteroidal antiandrogen similar in structure to flutamide that is used widely in the therapy of prostate cancer and has been linked to rare instances of liver injury.
  • Bicalutamide/ 50 mg daily is indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D2 metastatic carcinoma of the prostate.

Use in Cancer

Bicalutamide is approved to treat:

Bicalutamide is also being studied in the treatment of other types of cancer.

Contraindications

  • are allergic to bicalutamide or any ingredients of the medication
  • have early-stage (localized) prostate cancer and would otherwise undergo watchful waiting
  • diabetes
  • anemia
  • a type of inflammation of the lung called interstitial pneumonitis
  • damage to the liver and inflammation
  • liver problems
  • abnormal liver function tests
  • pregnancy

Dosage

Strengths: 50 mg

Prostate Cancer

  • In combination with an LHRH analog: 50 mg orally once a day (morning or evening)

Side Effects

The Most Common

  • hot flashes or flushing
  • bone, back, or pelvic pain
  • muscle weakness
  • muscle or joint pain
  • headache
  • shortness of breath
  • increased blood pressure
  • swelling of the hands, feet, ankles, or lower legs
  • cough
  • constipation
  • nausea
  • vomiting
  • abdominal pain
  • diarrhea
  • gas
  • change in weight (loss or gain)
  • loss of appetite
  • dizziness
  • pain, burning, or tingling in the hands or feet
  • difficulty sleeping
  • feeling of uneasiness or dread
  • rash
  • sweating
  • inability to get or keep an erection
  • need to urinate frequently during the night
  • bloody urine
  • painful or difficult urination
  • frequent and urgent need to urinate
  • difficulty emptying bladder
  • painful or swollen breasts

More Common

  • yellowing of the skin or eyes
  • pain in the upper right part of the stomach
  • extreme tiredness
  • unusual bleeding or bruising
  • lack of energy
  • upset stomach
  • loss of appetite
  • flu-like symptoms
  • dull or sharp side pain
  • chest pain
  • flatulence (passing gas)
  • hair loss or decreased hair regrowth
  • hot flashes
  • impotence or reduction in sexual desire
  • increased sensitivity of the skin to sun; increased risk of sunburn
  • indigestion

Rare

  • abdominal pain
  • blood in the urine
  • chest pain
  • severe itching
  • signs of anemia (low red blood cells; e.g., dizziness, pale skin, unusual tiredness or weakness, shortness of breath)
  • signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
  • signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
  • symptoms of high blood sugar (e.g., frequent urination, increased thirst, excessive eating, unexplained weight loss, poor wound healing, infections, fruity breath odour)
  • symptoms of heart failure (e.g., tiredness, shortness of breath especially when lying down, swelling of the feet or ankles)
  • pain or tenderness in stomach
  • signs of a heart attack (e.g., chest pain or pressure, pain extending through shoulder and arm, nausea and vomiting, sweating)
  • symptoms of lung problems (e.g., shortness of breath, painful breathing, sudden shortness of breath, cough, fever)
  • symptoms of a serious allergic reaction (e.g., hives, shortness of breath, difficulty swallowing, swelling of the face, lips, tongue or throat)

Drug Interaction

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Pregnancy and Lactation

US FDA pregnancy category: Not assigned.

Pregnancy

This drug is contraindicated in females. This drug is contraindicated in pregnant women because it can cause fetal harm. Drugs that have caused, are suspected to have caused or may be expected to cause, an increased incidence of human fetal malformations or irreversible damage. These drugs may also have adverse pharmacological effects. Accompanying texts should be consulted for further details.

Breastfeeding

This drug is contraindicated in females; therefore, it is contraindicated in lactation. Excreted into human milk: Unknown

Excreted into animal milk: Yes
The effects in the nursing infant are unknown.

How should this medicine be used?

Bicalutamide comes as a tablet to take by mouth. It is usually taken with or without food once a day, either in the morning or evening. Take bicalutamide at around the same time every day. You should begin taking bicalutamide on the same day you begin injecting the luteinizing hormone-releasing hormone. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take bicalutamide exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Bicalutamide along with the luteinizing hormone-releasing hormone may help stop the growth and spread of cancer cells but does not cure prostate cancer. Continue to take both bicalutamide and the luteinizing hormone-releasing hormone even if you feel better. Do not stop taking these medications without talking to your doctor.

What special precautions should I follow?

Before taking bicalutamide,

  • tell your doctor and pharmacist if you are allergic to bicalutamide, any other medications, or any of the ingredients in bicalutamide tablets. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: alprazolam (Xanax); anticoagulants (‘blood thinners’) such as warfarin (Coumadin); aripiprazole (Abilify); buspirone (Buspar); calcium channel blockers such as amlodipine (Norvasc), diltiazem (Cardizem, Dilacor, Tiazac), felodipine (Plendil), nifedipine (Adalat, Procardia), nisoldipine (Sular), and verapamil (Calan, Covera, Isoptin, Verelan); chlorpheniramine; cholesterol-lowering medications (statins) such as atorvastatin (Lipitor), lovastatin (Mevacor), and simvastatin (Zocor); clarithromycin (Biaxin); cyclosporine (Neoral, Sandimmune); diazepam (Valium); erythromycin (E.E.S., E-Mycin, Erythrocin); HIV protease inhibitors such as indinavir (Crixivan), ritonavir (Norvir), and saquinavir (Invirase, Fortovase); methadone (Dolophine); midazolam (Versed); pimozide (Orap); quinidine (Quinidex, Quinaglute); quinine; sildenafil (Viagra); tacrolimus (Prograf); tamoxifen (Nolvadex); telithromycin (Ketek); trazodone (Desyrel); triazolam (Halcion); and vincristine (Vincasar). Many other medications may also interact with bicalutamide, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
  • tell your doctor if you have or have ever had liver disease.
  • you should know that bicalutamide is only for use in men. If taken by pregnant women, bicalutamide can cause abnormalities in the fetus. Women who are or may become pregnant should not take bicalutamide. If you take bicalutamide while you are pregnant, call your doctor immediately.

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Abnormal heart rhythm: Bicalutamide can cause changes to the normal rhythm of the heart, called QT prolongation. QT prolongation is a serious life-threatening condition. If you are at risk for heart rhythm problems (e.g., have heart failure, angina, low potassium or magnesium levels; have congenital long QT syndrome; or are taking medications that can prolong the QT interval, such as quinidine, procainamide, amiodarone, sotalol, flecainide), discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Anemia: Bicalutamide may cause low levels of red blood cells. If you experience symptoms of reduced red blood cell count (anemia) such as shortness of breath, feeling unusually tired, or pale skin, contact your doctor as soon as possible.

Your doctor will do blood tests regularly to monitor the number of specific types of blood cells, including red blood cells, in your blood.

Diabetes: Bicalutamide may cause an increase in blood sugar levels. People with diabetes may find it necessary to monitor their blood sugar more frequently while using this medication.

If you have diabetes or are at risk for developing diabetes, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Drowsiness/reduced alertness: This medication may cause drowsiness. Do not drive, operate machinery, or perform other hazardous tasks until you have determined how this medication affects you.

Heart disease: The risk of heart attack or heart failure is increased for people taking bicalutamide. If you have risk factors for heart disease (obesity, high blood cholesterol, smoking), discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Liver function: Bicalutamide is broken down by the liver. Liver disease or reduced liver function may cause this medication to build up in the body, causing side effects. If you have liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. Your doctor may want to test your liver function regularly with blood tests while you are taking this medication.

This medication may also cause liver problems. Contact your doctor immediately if you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin.

Lung disease: Rarely, and particularly when higher doses are used, cases of interstitial lung disease have been reported with this medication. If you experience any symptoms of lung problems such as breathing difficulties, wheezing, cough, fever, or shortness of breath, contact your doctor immediately.

Osteoporosis: Long-term use of bicalutamide has been shown to cause reduced bone strength and may increase the risk of bone fractures. If you have osteoporosis or are at increased risk of developing osteoporosis, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Sensitivity to sunlight: This medication may increase the sensitivity of the skin to sunlight, increasing the risk of sunburn. Avoid exposure to sunlight for long periods of time, particularly between the hours of 10 am and 2 pm, while you are taking this medication and for 7 days after completing treatment. Wear a broad-spectrum sunscreen and lip balm with an SPF of 50 or greater. If you notice any unusual skin rash or peeling, contact your doctor immediately.

Children: The safety and effectiveness of this medication have not been determined for children.

References

  1. https://pubchem.ncbi.nlm.nih.gov/compound/Bicalutamide
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    The data from CAS Common Chemistry is provided under a CC-BY-NC 4.0 license, unless otherwise stated.
  9. Bicalutamide [USAN:USP:INN:BAN]
    ChemIDplus Chemical Information Classification
  10. CompTox Chemicals Dashboard Chemical Lists
  11. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
  12. NCI Thesaurus Tree
  13. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
  14. LICENSE
    The content of the MoNA database is licensed under CC BY 4.0.
  15. LICENSE
    Data: CC-BY 4.0; Code (hosted by ECI, LCSB): Artistic-2.0
    NORMAN Suspect List Exchange Classification
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