Pharmacological properties Casodex 50 mg:
nonsteroidal antiandrogen, not having other hormonal activity. The drug – a racemic mixture in which the anti-androgenic activity exhibits only (R)-enantiomer. Binds to androgen receptors without activating gene expression, thereby inhibits the activity of androgens. The result is a regression of prostate tumors.
Well absorbed in the gastrointestinal tract after oral administration. Food intake did not affect the bioavailability of bicalutamide. (S)-enantiomer is eliminated from the body much faster than (R)-enantiomer, the latter a half-life of approximately 1 week.
With a daily intake of Casodex concentration (R)-enantiomer in plasma increased about 10 times due to prolonged half-life that allows you to take this medicine 1 time a day. With a daily intake of Casodex at 50 mg concentration of (R)-enantiomer in plasma is about 9 mg / ml, 150 mg – about 22 mg / ml. Moreover, almost 99% of the drug that is in systemic circulation is active (R)-enantiomer.
Pharmacokinetics of (R)-enantiomer does not depend on such factors as age, renal function and liver (with a slight to moderate its violation). In patients with severely impaired liver function elimination (R)-enantiomer of slowing down.
To a large extent bound to plasma proteins (racemate 96%, R-bicalutamide 99.6%). Extensively metabolized by oxidation and glyukuronidnyh conjugates. The metabolites are excreted in the urine and bile in approximately equal proportions.
INDICATIONS Casodex 50 mg:
indications for Casodex 50 mg. A common prostate cancer (late stage) is used to combine with releasing factor analog of luteinizing hormone (LH-RG) or surgical castration.
Indications for Casodex 150 mg. Locally advanced prostate cancer (T3-T4, any N, M0; T1-T2, N +, M0), as a separate drug or as an adjuvant therapy to radical prostatectomy or radiotherapy.
Locally progressive, nemetastaziruyuschy prostate cancer, in cases where surgical castration or other medical intervention is not considered appropriate or feasible.
APPLICATION Casodex 50 mg:
Casodex 50 mg. Men, including the elderly: 1 tablet (50 mg) per day. Treatment should be started simultaneously Casodex with the appointment of an analogue of LH-RG or surgical castration. Duration of treatment is determined by the physician.
Casodex 150 mg. Grown men, including the elderly: 1 tablet orally 150 mg 1 time per day.
Casodex 150 mg should be taken continuously for a minimum of 2 years or until the onset of changes in disease development.
Does not require dose adjustment of the drug in patients with renal failure and slightly severe impaired liver function.
Patients with moderate to severe liver dysfunction in order to avoid possible accumulation Casodex be used with caution.
CONTRAINDICATIONS Casodex 50 mg:
hypersensitivity to the drug. Casodex not appoint women and children.
Casodex should not be used in conjunction with terfenadine, astemizole, and cisapride.
Side effect Casodex 50 mg:
Casodex well tolerated by most patients and only in rare cases it has to cancel because they caused side effects.
Pharmacological effect could be due to Casodex anticipated effects, including flushing, itching, as well as breast tenderness and gynecomastia, the severity of which decreases after castration performed simultaneously. Sometimes, patients taking Casodex , there is abdominal pain, diarrhea, nausea, vomiting, fatigue, depression, alopecia restore hair growth, hematuria, decreased libido, dry skin.
In clinical trials Casodex were marked changes in the liver (increased transaminase levels, jaundice, cholestasis). These changes were mostly transient and disappeared completely or decreased in spite of continued therapy or after its termination.
In some cases, during treatment Casodex may develop liver failure, and the causal link between the development of side effects and treatment Casodex not been established.
In addition, clinical trials, while the application Casodex and analogue LHRH noted the following side effects (such as possible side effects of drug therapy, according to clinicians, with a frequency greater than or equal to 1%).
Cardio-vascular system: congestive heart failure.
From the digestive system: anorexia, dry mouth, dyspepsia, constipation, flatulence.
CNS: dizziness, headache, insomnia, somnolence, decreased libido.
The respiratory system: dyspnea.
Urogenital system: impotence, nocturia.
From the hemopoietic system: anemia.
Dermatological reactions: alopecia, rash, sweating, hirsutism.
From the Metabolic: diabetes mellitus, hyperglycemia, edema, or weight loss.
Other: abdominal pain, chest pain, pelvic pain, chills.
It should be noted, however, failed to reliably prove a causal relationship between these effects and the therapy, in addition, some of these effects often occur in elderly patients without the use of Casodex .
SPECIAL INSTRUCTIONS Casodex 50 mg:
Casodex as extensively metabolized by the liver, its excretion can be delayed in patients with severe hepatic impairment and this, in turn, can lead to accumulation Casodex . Therefore, such patients should be Casodex used with caution.
In therapy Casodex must conduct periodic tests of liver function. Most of these changes can be expected in the first 6 months of treatment Casodex .
In the event of severe disturbances of liver treatment Casodex should be discontinued.
Casodex inhibits cytochrome P450 (CYP 3A4), so you need to be careful in appointing Casodex with drugs metabolized CYP 3A4.
Patients with lactose intolerance should be taken into account that each tablet of 150 mg Casodex contains 183 mg lactose monohydrate.
Use during pregnancy and lactation.
Application Casodex contraindicated for women during pregnancy and lactation.
Children. Casodex is contraindicated in children.
Ability to influence to drive a car or operating other machines. It is unlikely to influence patients’ ability to Casodex drive vehicles or by other mechanisms. However, it should be noted that occasionally somnolence may occur. Patients who are taking this drug, you need to be careful.
INTERACTION Casodex 50 mg:
no data on the interaction Casodex and analogues of LH-RG.
Studies in vitro have demonstrated that R-bicalutamide inhibits CYP 3A4, to a lesser extent CYP 2C9, 2C19 and 2D6.
Although clinical studies with antipyrine, a marker of the activity of P450 did not confirm the possibility of interaction with Casodex , to use the drug for 28 days in patients receiving midazolam led to an increase in AUC values of midazolam by 80%. Therefore, the application Casodex with terfenadine, astemizole, and cisapride is contraindicated. You must be careful while appointing Casodex with cyclosporine or calcium channel blockers. May require dose reduction of these drugs. Patients taking cyclosporine should remain under medical supervision, especially early in treatment Casodex and its Abolition.
Be careful when appointing Casodex with drugs depressing the metabolism of drugs (cimetidine, ketoconazole). Theoretically, the appointment of such a combination can lead to increased concentration in the blood Kasodeksa and frequency of side effects.
Studies in vitro have shown that Casodex may displace warfarin anticoagulant coumarin from the places of its binding to plasma proteins. Therefore, the appointment Casodex in patients receiving coumarin anticoagulants, it is recommended to regularly monitor the prothrombin time.
OVERDOSAGE Casodex 50 mg
data on overdose in humans do not. No specific antidote, treatment is symptomatic. It is shown that maintenance therapy and monitoring of vital body functions. Dialysis is ineffective because the drug has a high degree of binding to plasma proteins.
