Bicalutamide Canon, 50 mg 30 pcs

Pharmacodynamics

Anti-androgenic nonsteroidal agent. By binding to receptors that have an affinity for androgens, it suppresses androgen activity, as a result of which regression of the prostate tumor is observed. It has no other endocrine activity.

Pharmacokinetics

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

The binding to plasma proteins is 96%. It is extensively metabolized in the liver by oxidation and formation of glucuronide conjugates.

Extracted as metabolites with urine and bile in approximately equal proportions.

Cumulation of bicalutamide in the body is possible.

Indications

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

Pharmacological effect

Pharmacodynamics

Antiandrogenic non-steroidal drug. By binding to receptors with affinity for androgens, it suppresses the activity of androgens, resulting in regression of the prostate tumor. Does not have 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%. Intensively metabolized in the liver by oxidation and the formation of glucuronide conjugates.

It is excreted in the form of metabolites in urine and bile in approximately equal proportions.

Bicalutamide may accumulate in the body.

Special instructions

Use with caution in patients with moderate to severe liver dysfunction, because accumulation of bicalutamide in the body is possible.

During treatment, regular monitoring of liver function is required. If severe changes develop, you should stop taking bicalutamide.

Active ingredient

Bicalutamide

Composition

Active ingredient:

bicalutamide 50 mg.

Excipients:

corn starch 35 mg,

croscarmellose sodium 6.5 mg,

lactose monohydrate 44.3 mg,

povidone 3.2 mg,

sodium stearyl fumarate 1 mg.

Film shell composition:

Opadry II white 4 mg.

Pregnancy

Not prescribed for female patients.

Contraindications

Simultaneous use with terfenadine, astemizole, cisapride;
childhood;
hypersensitivity to bicalutamide;
not prescribed to female patients.

Side Effects

From the endocrine system: hot flashes, breast tenderness and gynecomastia, decreased libido.

From the digestive system: abdominal pain, diarrhea, nausea, vomiting, increased transaminase levels, jaundice, cholestasis.

From the side of the central nervous system: asthenia, depression are possible.

Dermatological reactions: alopecia, hair regrowth, itching, dry skin.

Other: hematuria.

Interaction

When bicalutamide was used for 28 days while taking midazolam, the AUC of midazolam increased by 80%.

With simultaneous use of bicalutamide with cyclosporine or calcium channel blockers, potentiation or development of adverse reactions is possible.

It is theoretically possible to increase the concentration of bicalutamide in the blood plasma when used simultaneously with inhibitors of microsomal liver enzymes, which may be accompanied by an increase in the incidence of adverse reactions.

In vitro studies have shown that bicalutamide can displace the coumarin anticoagulant warfarin from plasma protein binding sites.

Overdose

Cases of overdose in humans have not been described. There is no specific antidote.

Treatment is symptomatic. Dialysis is not effective, since bicalutamide is tightly bound to proteins and is not excreted unchanged by the kidneys.

General supportive therapy and monitoring of vital body functions are indicated.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Manufacturer

Kanonpharma production CJSC, Russia