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Active ingredients
Bicalutamide
Release form
Pills
Composition
Bicalutamide 150 mg; Auxiliary substances: magnesium aluminometasilicate - 30 mg, sodium carboxymethyl starch - 12 mg, magnesium stearate - 6 mg, ludipress - 402 mg.; Film coating composition: Opadry II yellow 85F32733 - 24 mg, including polyvinyl alcohol - 35-49%, talc - 9.8-25%, macrogol 3350 - 7.35-35.2%, titanium dioxide and iron oxide yellow - 15.15-30%.
Pharmacological effect
Antiandrogenic nonsteroidal agent. By binding to receptors that have affinity for androgens, it inhibits the activity of androgens, as a result of which a regression of the prostate tumor is observed. Does not possess other types of endocrine activity.
Pharmacokinetics
After ingestion 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 the formation of glucuronide conjugates.; It is excreted in the form of metabolites in urine and bile in approximately equal proportions.; Cumulation of bicalutamide in the body is possible.
Indications
Prostate cancer - as part of a combination therapy with a GnRH analogue or with surgical castration.
Contraindications
Simultaneous administration with terfenadine, astemizole, cisapride; children's age, hypersensitivity to bikalutamidu.; Do not prescribe to female patients.
Use during pregnancy and lactation
Do not prescribe to female patients.
Dosage and administration
Individual, depending on the indications and treatment regimen.
Side effects
On the part of the endocrine system: hot flashes, breast tenderness and gynecomastia, decreased libido.; On the part of the digestive system: abdominal pain, diarrhea, nausea, vomiting, increased transaminase levels, jaundice, cholestasis.; On the part of the CNS: asthenia, depression are possible. ; Dermatological reactions: alopecia, restoration of hair growth, itching, dry skin.; Other: hematuria.
Overdose
Cases of overdose in humans are not described. There is no specific antidote. Symptomatic treatment. Dialysis is not effective because bicalutamide binds strongly to proteins and is not excreted in the urine unchanged. General supportive therapy and monitoring of vital body functions is shown.
Interaction with other drugs
When bicalutamide is 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 undesirable reactions is possible. 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 bicalu tamid may displace the coumarin anticoagulant warfarin from plasma protein binding sites.
special instructions
Use with caution in patients with moderately severe and severe liver dysfunction, because possible cumulation of bicalutamide in the body. During the period of treatment requires regular monitoring of liver function. In the case of the development of severe changes, it is necessary to stop taking bicalutamide.