Bicalutera (Tablets) Instructions for Use

Instructions
Dosage forms

ATC Code

L02BB03 (Bicalutamide)

Active Substance

Bicalutamide (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antiandrogenic drug with antitumor activity

Pharmacotherapeutic Group

Antineoplastic agent, antiandrogen

Pharmacological Action

Bicalutamide is a nonsteroidal antiandrogen. By binding to receptors with affinity for androgens, it suppresses androgen activity, resulting in regression of prostate tumor. It does not possess other types of endocrine activity.

Pharmacokinetics

After oral administration, it is well absorbed from the gastrointestinal tract. Food intake does not affect bioavailability.

Plasma protein binding is 96%. It is extensively metabolized in the liver by oxidation and formation of glucuronide conjugates.

It is excreted as metabolites in urine and bile in approximately equal proportions.

Accumulation of bicalutamide in the body is possible.

Indications

Prostate cancer – as part of combination therapy with a GnRH analogue or with surgical castration.

ICD codes

Open the list of ICD codes

ICD-10 code	Indication
C61	Malignant neoplasm of prostate

ICD-11 code	Indication
2C82.Y	Other specified malignant neoplasms of the prostate gland
2C82.Z	Malignant neoplasms of prostate, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Administer one 50 mg tablet once daily, at the same time each day, with or without food.

Initiate treatment concurrently with a GnRH analogue; the timing of the first dose should align with the initiation of GnRH analogue therapy or at least 3 days before surgical castration.

Continue treatment for as long as clinically indicated by the patient’s response and tolerability; do not adjust the dose for mild to moderate hepatic impairment, but exercise increased caution.

Adverse Reactions

Observe for hot flashes, breast pain, and gynecomastia; these are very common endocrine effects. Monitor for decreased libido.

Commonly reported gastrointestinal effects include nausea, vomiting, diarrhea, and abdominal pain; monitor liver function tests for elevated transaminases, jaundice, and cholestasis.

Asthenia and depression may occur. Dermatological reactions can include alopecia, hair regrowth, pruritus, and dry skin. Hematuria has also been reported.

Drug Interactions

Exercise caution with concomitant use of drugs metabolized by CYP3A4, such as midazolam, as bicalutamide can increase their exposure; monitor for increased effects.

Theoretically, co-administration with strong CYP3A4 inhibitors may increase bicalutamide plasma concentrations, potentially increasing adverse reactions.

In vitro, bicalutamide can displace coumarin anticoagulants like warfarin from protein binding sites; monitor INR closely upon initiation or discontinuation. Use with cyclosporine or calcium channel blockers may potentiate adverse reactions.

Contraindications

Hypersensitivity to bicalutamide or any excipient of the drug.
Concomitant use with terfenadine, astemizole, or cisapride is contraindicated.
Do not use in women, particularly those who are or may become pregnant, or during lactation.
Contraindicated in children and adolescents.

Overdose

No specific antidote exists; manage with symptomatic and supportive care. Consider gastric lavage if ingestion was recent.

Monitor for increased severity of known adverse reactions, particularly related to the liver. Dialysis is unlikely to be effective due to high protein binding.

Tablets

Individual, depending on the indications and treatment regimen.

Use in Pregnancy and Lactation

Not prescribed for female patients.

Use in Hepatic Impairment

Use with caution in patients with moderate and severe hepatic impairment, as accumulation of bicalutamide in the body is possible.

Regular monitoring of liver function is required during treatment. In case of severe changes, bicalutamide should be discontinued.

Pediatric Use

The drug is not prescribed to children.

Special Precautions

Use with caution in patients with moderate and severe hepatic impairment, as accumulation of bicalutamide in the body is possible.

Regular monitoring of liver function is required during treatment. In case of severe changes, bicalutamide should be discontinued.

Storage Conditions

Store at 15°C (59°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.

Medical Disclaimer