Casodex coated pills 150mg N28
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Active ingredients
Bicalutamide
Release form
Pills
Composition
1 tab.: Bicalutamide 150 mg. Additional substances: lactose monohydrate - 183 mg, sodium carboxymethyl starch - 22.5 mg, povidone - 15 mg, magnesium stearate - 4.5 mg. Shell composition: hypromellose - 7.5 mg, macrogol 300 - 1.5 mg, titanium dioxide (E171 ) - 2.3 mg.
Pharmacological effect
Antiandrogenic nonsteroid drug. It is a racemic mixture, with predominantly (R) -enantiomer having antiandrogenic activity. The drug does not possess other types of endocrine activity. Casodex binds to androgen receptors and, while not activating gene expression, inhibits the stimulating effect of androgens. As a result, prostate neoplasia regression occurs. In some patients, discontinuation of Casodex can lead to the development of clinical antiandrogen withdrawal syndrome. When Casodex is administered in a daily dose of 150 mg daily to treat patients with locally advanced (T3-T4, any N, M0 or any T, N +, M0) cancer of the prostate gland, as an immediate hormone therapy or as an adjuvant therapy, significantly reduces the risk of disease progression and bone metastases. In local-p Spread of prostate cancer tends to improve life expectancy without signs of disease progression in groups of patients taking Casodex 150 mg as an immediate or adjuvant therapy compared with standard therapy (surgical treatment, radiation therapy). Increased life expectancy among patients with locally advanced prostate cancer, receiving Casodex at a dose of 150 mg as an immediate monotherapy and as an adjuvant Antenna treatment in combination with radiation therapy. The use of Casodex at a dose of 150 mg compared with surgical castration in patients with locally advanced non-metastatic prostate cancer did not reveal a statistically significant difference in life expectancy and time to progression with a statistically significant advantage of sexual function and physical condition .
Pharmacokinetics
AbsorptionAfter ingestion is rapidly and completely absorbed from the gastrointestinal tract.Simultaneous ingestion of food does not affect absorption. DistributionWhen daily administration of Casodex at a dose of 150 mg of Css (R) enantiomer in plasma is about 22 μg / ml. At equilibrium, about 99% of all enantiomers circulating in the blood is the active (R) enantiomer. When Casodex is taken daily, the concentration of (R) enantiomer in plasma increases by about 10 times due to prolonged T1 / 2, which allows Casodex to be administered 1 time / day Plasma proteins are high (96% for racemic mixture, 99.6% for (R) -enantiomer). The average concentration of (R) -enantiomer in the semen of men who received Casodex 150 mg is 4.9 mcg / ml. The amount of bicalutamide that can potentially be detected in women after sexual intercourse is low and is approximately 0.3 mcg / kg (the value of this indicator is lower than that required for changes in fetal development in laboratory animals). Metabolism is extensively metabolized in the liver by oxidation and the formation of conjugates with glucuronic acid. WithdrawalMetabolites are excreted in urine and bile in approximately equal proportions. (S) -enantiomer is eliminated from the body much faster (R) -enantiomer, T1 / 2 of the last about 7 days. Farmacokin Ethics in special clinical situations. The pharmacokinetics of (R) -enantiomer are not affected by age, renal dysfunction, mild and moderate liver dysfunction. There is evidence that in patients with severely dysfunctioning liver function, elimination of (R) -enantiomer from plasma slows down. patients with moderate and severe hepatic impairment may experience cumulation of bicalutamide in the body
Indications
- locally advanced prostate cancer as an immediate monotherapy or as adjuvant therapy in combination with radical prostatectomy or radiation therapy; - locally advanced non-metastatic prostate cancer as monotherapy in cases where surgical castration or other medical interventions are unacceptable or inapplicable.
Contraindications
- simultaneous use with terfenadine, astemizole, cisapride; - hypersensitivity to bicalutamide and other components of the drug; Casodex is not prescribed to women and children. Casodex is used with caution in patients with impaired liver function, with lactose intolerance, lactase deficiency and glucose / galactose malabsorption syndrome .
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
Casodex is contraindicated in women and should not be given to pregnant or lactating women.
Dosage and administration
Casodex is prescribed to adults and elderly men at a dose of 150 mg 1 time / day. Casodex should be taken for a long time, at least for 2 years. If there is evidence of disease progression, the drug should be discontinued. Patients with impaired renal function and with mild hepatic impairment do not need dose adjustment. Patients with moderate and severe impaired liver function may experience increased drug accumulation.
Side effects
Except where otherwise indicated, the incidence of side effects was calculated according to studies of Kasodex early prostate cancer monotherapy. Very often (≥10%): gynecomastia (may persist even after cessation of therapy, especially when taking the drug for a long time), chest pain glands, skin rash, asthenia. Often (≥1% - <10%): depression, anorexia, dizziness, drowsiness, hot flushes, itching, abdominal pain, constipation, dyspepsia, flatulence, alopecia or hair regrowth, g irsutism, dry skin, hematuria, nausea, decreased sexual desire, erectile dysfunction, chest pain, edema, weight gain, increased activity of hepatic transaminases, hepatotoxicity, jaundice, anemia, decreased appetite. Often (≥ 0.1% - <1%) : hypersensitivity reactions, angioedema, urticaria, interstitial lung disease (fatal cases reported). * Rarely (≥ 0.01% - <0.1%): hepatic failure (fatal cases reported). * Increased hepatic trance activity az, cholestasis and jaundice rarely assessed as serious, were transient, completely disappeared or decreased with continued therapy or after drug discontinuation. Very rarely, in the setting of bicalutamide, liver failure developed, but the causal relationship between the development of liver failure and treatment with Casodex has not been reliably established. * According to the post-marketing use of the drug.
Overdose
Cases of overdose in humans are not described. Specific antidote does not exist, therefore, if necessary, conduct symptomatic therapy.Dialysis is ineffective 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
There are no data on the pharmacodynamic or pharmacokinetic interaction between Casodex and GnRH analogues. In vitro studies have shown that Casodex's (R) -enantiomer is an inhibitor of CYP3A4, to a lesser extent CYP2C9, CYP2C19, CYP2D6. The potential ability of Casodex to interact with other drugs was not detected. However, when using Casodex for 28 days while taking midazolam AUC, midazolam increased by 80%. Simultaneous use of Casodex with drugs such as terfenadine, astemizole, and cisapride is contraindicated. Caution should be taken when taking Casodex along with cyclosporine or calcium channel blockers. It may be necessary to reduce the dose of these drugs, especially in the case of potentiation or the development of adverse reactions. After the start of use or withdrawal of Casodex, careful monitoring of the plasma cyclosporine concentration and the patient’s clinical condition is recommended. Simultaneous administration of Casodex and drugs that inhibit microsomal drug oxidation (cimetidine, ketoconazole) may lead to an increase in plasma bicalutamide concentration and, possibly, an increase in the incidence of undesirable reactions. Casodex enhances the effect of the indirect coumarin anticoagulants (warfarin), because can displace these drugs from their protein binding sites.
special instructions
Considering the possibility of slowing down the excretion of bicalutamide and the cumulation of bicalutamide in patients with impaired liver function, it is advisable to periodically assess liver function. Most changes in liver function occur during the first 6 months of treatment with Casodex. If pronounced changes in liver function develop, you must stop taking Casodex. Patients with disease progression amid elevated levels of prostate-specific antigen (PSA) should consider stopping Casodex. the administration of Kasodex to patients receiving coumarin anticoagulants,It is recommended that prothrombin time be regularly monitored. Considering the possibility of casodex inhibiting cytochrome P450 (CYP3A4) activity, caution should be exercised when simultaneously prescribing Casodex with drugs mainly metabolized with CYP3A4. Patients with lactose intolerance need to be informed that each Casodex 150 mg tablet contains 18 lactose monohydrate. Impact on the ability to drive vehicles and control mechanisms. When using Casodex can be observed onlivost and dizziness, and therefore caution should be exercised when driving vehicles or other moving machinery.