Last Updated on May 23, 2023
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What is bicalutamide?
Bicalutamide is a non-steroidal antiandrogen used to treat prostate cancer. It used to be approved only in combination with other forms of therapy, but is now used as a single therapy (especially in the early stages). Here you can read all about the effects and use of bicalutamide, side effects and other important facts.
How does bicalutamide work?
The prostate is a sexual gland found only in male mammals that secretes a secretion that is part of the sperm. It is located under the bladder and surrounds the urethra. Prostate growth is controlled by the male sex hormones (androgens) testosterone and dihydrotestosterone (a derivative of testosterone).
Random mutations (genetic changes) in the genetic material of prostate cells can cause them to start to grow uncontrollably – this is called prostate cancer. Its growth depends on a supply of testosterone and dihydrotestosterone, so treatment tries to block the receptors for these hormones on the prostate cells. This is done with so-called “anti-androgens” such as bicalutamide.
In the early stages of the disease, bicalutamide alone can stop the growth of the tumour. In advanced stages, another treatment (surgical removal of the prostate, radiotherapy, hormone therapy, chemotherapy) is often added.
Absorption, degradation and elimination of bicalutamide
Once taken by mouth, the drug is absorbed into the bloodstream through the intestines. It is metabolised in the liver in different ways, and about half of it is excreted in the stool and urine. Excretion is very slow, and after a week only about half of the active ingredient has been removed from the body.
When should you use bicalutamide?
Bicalutamide is approved for use alone or in combination for the treatment of prostate cancer.
Scientific studies have shown that low-dose bicalutamide can be used successfully to treat unwanted hair growth (hirsutism) in women. However, it is not approved for this use (known as off-label use).
How to take bicalutamide?
The drug is only available in tablet form, depending on the type of therapy, 50 milligrams or 150 milligrams of bicalutamide taken once a day at the same time of day and independently of meals. The treatment lasts a long time.
What are the side effects of bicalutamide?
More than ten per cent of patients treated with bicalutamide show side effects in the form of chest tightness, breast growth, weakness, water retention in the subcutaneous tissue and blood in the urine.
In addition, between one in ten and one in a hundred patients treated with bicalutamide experience side effects such as erectile dysfunction, pelvic pain, chills, drowsiness, liver dysfunction, sweating, increased hair growth, itching, diabetes, weight gain and loss, heart failure and heart attack.
What should I watch for when taking bicalutamide?
There are no known interactions with the drugs commonly used in combination therapy for prostate cancer (such as LHRH analogues).
Because bicalutamide is extensively metabolised in the liver, it blocks enzymes that break down other substances, which can lead to a significant increase in their blood levels. For this reason, bicalutamide should not be taken together with drugs for allergies (such as terfenadine, astemizole), immunosuppressants (such as cyclosporine) and calcium channel blockers (such as nifedipine, verapamil, diltiazem, used for heart disease).
Conversely, other drugs inhibit the breakdown of bicalutamide which accumulates in the body. This includes antifungals (such as ketoconazole) and heartburn medicines (such as cimetidine).
Patients taking anticoagulants (such as warfarin and phenprocoumon) should have their coagulation monitored at the start of treatment with bicalutamide, as their coagulation levels may change.
As bicalutamide has a major effect on the hormonal balance of the body, it must not be taken by pregnant or breastfeeding women, children or adolescents under the age of 18.
Blood levels of bicalutamide should be monitored in patients with severe liver impairment.
How to buy Bicalutamide online over the counter UK?
In the UK, all products containing bicalutamide are available only on prescription from a doctor.
How long has bicalutamide been around?
Non-steroidal antiandrogens were first discovered in the 1970s. The approval of the first drug of this substance group, flutamide, in 1989 in the US. However, it is noticed early on that flutamide is degraded relatively rapidly and the liver very heavily used. Its successor, bicalutamide, was approved in the US in 1995 and has a much longer duration of action and improved liver compatibility. Now that the patent has expired, there are many affordable generic versions of bicalutamide on the market.