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Brand Name :
Casodex
(China) [Available]Synonyms :
Bicalutamide
Class :
Antineoplastics, Antiandrogen;
Brand Name :
Casodex
(China) [Available]Synonyms :
Bicalutamide
Class :
Antineoplastics, Antiandrogen;
Dosage Forms & Strengths
When bicalutamide is combined with an LHRH analog:
50
mg
Orally
once a day
Dose Adjustments
Renal Dose Adjustments
No adjustment required
Liver Dose Adjustments
Caution recommended.
When both drugs are combined, there may be an increased effect of flibanserin by affecting hepatic or intestinal enzyme CYP3A4 metabolism
when both drugs are combined, there may be an increased effect of Lomitapide by affecting hepatic or intestinal enzyme CYP3A4 metabolism
when both drugs are combined, there may be an increased effect of Lonafarnib by affecting hepatic or intestinal enzyme CYP3A4 metabolism
abiraterone acetate and niraparib
may decrease the diagnostic effect of antiandrogens
may decrease the level by affecting hepatic enzyme CYP3A4 metabolism
may decrease the level by affecting hepatic enzyme CYP3A4 metabolism
may decrease the level by affecting hepatic enzyme CYP3A4 metabolism
may decrease the level by affecting hepatic enzyme CYP3A4 metabolism
When both drugs are combined, there may be an increased risk of adverse effect
when both drugs are combined, there may be an increased risk of adverse effect
when both drugs are combined, there may be an increased risk of adverse effect
when both drugs are combined, there may be an increased risk of adverse effect
may enhance cisapride's serum concentration
It may enhance the levels when combined with tamsulosin by affecting CYP3A4 metabolism
It may diminish its effectiveness when combined with flotufolastat F-18
When alprazolam and bicalutamide is used together, this leads to reduction in the alprazolam’s metabolism
When bicalutamide is used together with fluconazole, this leads to reduction in the bicalutamide metabolism
When bicalutamide is used together with capsaicin, this leads to enhanced risk or seriousness of methemoglobinemia
When bicalutamide is used together with allylestrenol, this leads to a reduction in the bicalutamide metabolism
When bicalutamide is used together with oleandomycin, this leads to enhanced concentration serum of bicalutamide
When bicalutamide is used together with patupilone, this leads to enhanced concentration serum of bicalutamide
When bicalutamide is used together with ridaforolimus, this leads to enhanced concentration serum of bicalutamide
the metabolism of digitoxin can be diminished when combined with bicalutamide
when both drugs combine bicalutamide will increase effect of ifosfamide by affecting the enzyme CYP3A4 metabolism.
when both drugs are combined, there may be an increased metabolism of bicalutamide
increases serum level of cabazitaxel by affecting the enzyme CYP3A4
it increases the effect or level of palbociclib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
may increase the hypertensive effect of hypertension-associated agents
the serum concentration of bicalutamide can be elevated when combined with remacemide
Actions and Spectrum:
Actions:
Androgen Receptor Binding: In prostate cancer cells, bicalutamide binds to androgen receptors in competition with androgens such as testosterone and dihydrotestosterone (DHT). Bicalutamide blocks androgens from activating these receptors by attaching itself to them.
Frequency defined
>10%
Dyspnea (13%)
Nausea (15%)
Infection (18%)
Pelvic pain (21%)
Constipation (22%)
Asthenia (22%)
Back pain (25%)
General pain (35%)
Hot flashes (53%)
1-10%
Headache (7%)
Flu like symptoms (7%)
Vomiting (8%)
Hypertension (8%)
Chest pain (8%)
UTI (9%)
Rash (9%)
Gynecomastia (9%)
Black Box Warning
Take caution with diabetic patient.
Contraindication/Caution:
Contraindications
Pregnancy and breastfeeding
Hypersensitivity
Cautions
Gynecomastia and breast pain
Severe liver injury
Inhibition of spermatogenesis is reported
Pregnancy & breastfeeding:
Pregnancy consideration:
Contraindicated in pregnant women.
Breastfeeding warnings:
No data is available regarding the excretion of drugs in breast milk.
Pregnancy category:
Pharmacology:
Bicalutamide is an example of a non-steroidal anti-androgen drug which is mainly used widely in treatment of prostate cancer.
Pharmacodynamics:
Anti-androgen Activity:
Bicalutamide compete with testosterone and other androgens to bind to the receptor sites on the castration resistant prostate cancer cells. This inhibition inhibits the androgen dependent pathway responsible for the growth and survival of prostate cancer cells.
Pharmacokinetics:
Absorption
When administered orally, bicalutamide is readily absorbed.
The drug has a peak plasma time of 31 hours.
Distribution
Bicalutamide is mostly attached to albumin, accounting for 96% of its protein bound state.
Metabolism
In the liver, bicalutamide is extensively metabolised, mostly by cytochrome P450 enzymes, especially CYP3A4.
Excretion and Elimination
Approximately 42% of a dosage of bicalutamide is expelled mostly through feces, while approximately 36% is removed by urine.
There is an estimated 5.8-day elimination half-life.
Administration:
Bicalutamide is available in the form of tablets and is usually administered through the oral route irrespective of food. It is significant to adhere to the directions given by the doctor or pharmacist and not to take more than the prescribed dose.
Patient information leaflet
Generic Name: bicalutamide
Bicalutamide: bye-ka-LOO-ta-mide
Why do we use bicalutamide?
Bicalutamide is most used to treat Prostate Cancer. It falls under the category of nonsteroidal antiandrogens; it inhibits the functioning of androgens; including testosterone. Because androgens would stimulate the development of the prostate cancer cells, bicalutamide will reduce or halt the growth of the cancer.
Bicalutamide is most useful where the cancer has progress to other parts of the body (Advanced prostate cancer) mainly through metastatic prostate cancer.
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