Casodex
Casodex: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Casodex
ATX code: L02BB03
Active ingredient: bicalutamide (bicalutamide)
Manufacturer: S.p. A. Corden Pharma (Italy) for AstraZeneca Ltd (UK)
Description and photo update: 2019-13-08
Prices in pharmacies: from 1897 rubles.
Buy
Casodex is a non-steroidal antiandrogenic drug used to treat advanced prostate cancer.
Release form and composition
Casodex is produced in the form of film-coated tablets: biconvex, round, white, on one side there is an engraved logo in the form of a rounded arrow, on the other - "50" and "Cdx" (50 mg tablets) or "Casodex 150" (tablets of 150 mg), in blisters of 14 pcs., 2 blisters in a cardboard box.
The composition of 1 tablet includes:
- Active ingredient: bicalutamide - 50 or 150 mg;
- Auxiliary components (50/150 mg, respectively): lactose monohydrate - 61/183 mg, sodium carboxymethyl starch - 7.5 / 22.5 mg, povidone - 5/15 mg, magnesium stearate - 1.5 / 4.5 mg.
The composition of the shell (50/150 mg, respectively): hypromellose - 2.5 / 7.5 mg, macrogol 300 - 0.5 / 1.5 mg, titanium dioxide (E171) - 0.77 / 2.3 mg.
Pharmacological properties
Pharmacodynamics
Casodex is a racemic mixture characterized by non-steroidal antiandrogenic activity, predominantly of the (R) -enantiomer, and the absence of any other endocrine activity.
Casodex suppresses the stimulatory effect of androgens by binding to androgen receptors (without activating gene expression). As a result of this process, regression of prostate malignant tumors is achieved.
When you stop taking the drug, in some cases, a clinical syndrome of antiandrogen withdrawal may develop.
In the case of daily use of Casodex at a dose of 150 mg per day with immediate hormonal therapy or adjuvant therapy of locally advanced (T3 – T4, any N, M0 or any T, N +, M0) prostate cancer, the likelihood of disease progression and the appearance of bone metastases is significantly reduced.
In the case of locally advanced prostate cancer in the groups of patients who took Casodex at a dose of 150 mg as adjuvant or immediate therapy, in comparison with standard therapy (radiation therapy, surgical treatment), there was a trend towards an increase in life expectancy without symptoms of disease progression.
With locally advanced prostate cancer, patients who received Casodex at a dose of 150 mg during immediate monotherapy or adjuvant treatment in combination with radiation therapy, recorded an increase in life expectancy.
In locally advanced non-metastatic prostate cancer, the use of Casodex 150 mg compared to surgical castration did not show statistically significant differences in life expectancy and time to progression, with statistically significant benefits in physical condition and sexual function.
Pharmacokinetics
After oral administration, Casodex is absorbed from the gastrointestinal tract quickly and completely. Food intake does not affect absorption.
The (R) -enantiomer is excreted from the body much more slowly than the (S) -enantiomer, the half-life of the former is about 7 days.
In the case of daily administration of bicalutamide, due to the long half-life, the content of the (R) -enantiomer in the blood plasma increases approximately 10 times, which makes it possible to use the drug once a day.
In the case of daily administration of bicalutamide at a dose of 150 mg, the equilibrium concentration of the (R) -enantiomer in plasma is approximately 22 μg / ml, and at a dose of 50 mg, this figure is approximately 9 μg / ml. In the equilibrium state, the active (R) -enantiomer accounts for about 99% of all enantiomers circulating in the blood.
The pharmacokinetics of the (R) -enantiomer is not affected by age, the degree of renal dysfunction, and the presence of mild and moderate liver dysfunction in the patient. There is information about a slowdown in the elimination of the (R) -enantiomer from plasma in patients with severely impaired liver function.
For the racemic mixture, the bond with plasma proteins is 96%, and for the (R) enantiomer - 99.6%. It is actively metabolized in the liver due to oxidation and the formation of conjugates with glucuronic acid. Excretion of metabolites is carried out with bile and urine in approximately equal proportions.
The average content of the (R) -enantiomer in the semen of patients treated with Casodex at a dose of 150 mg is about 4.9 μg / ml. Potentially low amounts of bicalutamide (0.3 μg / kg) can be found in women after intercourse. This amount is below the concentration required for changes in fetal development in laboratory animals.
Indications for use
According to the instructions, Casodex is prescribed for the treatment of advanced prostate cancer (in combination with surgical castration or an analogue of gonadotropin-releasing hormone).
Contraindications
- Simultaneous use with astemizole, terfenadine, cisapride;
- Hypersensitivity to drug components.
Casodex is not prescribed for women and children.
The drug should be used with caution in patients with functional disorders of the liver, as well as with lactase deficiency, lactose intolerance and galactose / glucose malabsorption syndrome.
Instructions for the use of Casodex: method and dosage
Casodex is taken orally.
The drug is prescribed for adult men, including elderly patients, at 50 mg per day in combination with a gonadotropin-releasing hormone (GnRH) analog or with surgical castration (treatment should be started simultaneously).
Patients with mild liver dysfunction and renal dysfunction should not be adjusted.
In patients with severe and moderate functional impairment of the liver, the cumulation of Casodex may increase.
Side effects
During the use of Casodex, there may be violations from some body systems, manifested with different frequencies:
- Very often (≥10%): skin rash, gynecomastia (may persist even after stopping treatment, especially with prolonged use of the drug), asthenia, breast tenderness;
- Often (≥1% to <10%): drowsiness, dizziness, depression, anorexia, hot flashes, abdominal pain, itching, constipation, nausea, dyspepsia, weight gain, decreased appetite, dry skin, flatulence, hair regrowth, or alopecia, hirsutism, hematuria, decreased sex drive, erectile dysfunction, edema, chest pain, anemia, jaundice, increased activity of hepatic transaminases, hepatotoxicity;
- Uncommon (from ≥ 0.1% to <1%): angioedema, urticaria, hypersensitivity reactions, interstitial pulmonary diseases (there are data on cases with a fatal outcome);
- Rarely (from ≥ 0.01% to <0.1%): liver failure (there are data on cases with a fatal outcome).
Jaundice, cholestasis, and hepatic transaminase elevation were rarely considered serious. These disorders were of a transient nature and decreased or completely disappeared with continued treatment or after discontinuation of Casodex. Very rarely, while taking the drug, hepatic failure developed, but the cause-and-effect relationship has not been reliably established.
Overdose
Overdose cases in humans have not been recorded.
There is no specific antidote.
Treatment is symptomatic: general supportive therapy is prescribed, control of vital functions is shown. Dialysis is ineffective, since bicalutamide strongly binds to proteins and is not excreted unchanged in the urine.
special instructions
In patients with functional disorders of the liver during therapy, it is advisable to periodically assess liver function. In most cases, changes in liver function are observed during the first 6 months of therapy. With the development of severe disorders, treatment should be interrupted.
With the progression of the disease against the background of an increase in the level of prostate-specific antigen (PSA), it may be necessary to discontinue therapy.
Caution should be exercised while using Casodex with drugs that are mainly metabolized with the participation of CYP3A4.
With simultaneous use with coumarin anticoagulants, regular monitoring of prothrombin time is recommended.
Patients with lactose intolerance should take into account that each 50/150 mg tablet contains 61/183 mg of lactose monohydrate.
During the application of Casodex, dizziness and drowsiness may occur, which is why you need to be careful when driving or driving other moving machinery.
Application during pregnancy and lactation
It is forbidden to use Casodex to treat women.
Pediatric use
It is forbidden to use Casodex to treat children.
With impaired renal function
In case of impaired renal function, dose adjustment is not required.
For violations of liver function
In case of impaired liver function, the drug should be used with caution.
Drug interactions
With the simultaneous use of Casodex with some drugs, undesirable effects may occur:
- Slow calcium channel blockers, cyclosporine: potentiation or development of undesirable reactions (dose reduction may be required, it is recommended to carefully monitor the patient's clinical condition and the concentration of cyclosporine in the blood plasma);
- Medicines that inhibit liver microsomal enzymes (for example, ketoconazole, cimetidine): an increase in the concentration of bicalutamide in plasma and, possibly, an increase in the incidence of side effects (caution should be exercised with simultaneous use);
- Indirect anticoagulants of the coumarin series (including warfarin): enhancing their action (it is recommended to regularly monitor the prothrombin time).
Concomitant use of Casodex with terfenadine, cisapride and astemizole is contraindicated.
Analogs
Casodex analogs are: Areklok, Bikana, Bicalutamide, Bicalutamide-Teva, Bikalan, Bikalutera, Bikulid, Bilumid, Calumid, Flulem, Flutamide, Flutan, Flutazin, Flucine, Flutaplex, Flutapharm.
Terms and conditions of storage
Keep out of reach of children at temperatures up to 30 ° C.
Shelf life: Casodex 50 mg - 5 years, 150 mg - 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Casodex
Reviews of Casodex indicate that this drug is effective in the treatment of prostate cancer (it supports the hormone levels necessary for therapy).
According to user reports, the most common side effect when taking Casodex is liver impairment.
The price of Casodex in pharmacies
The approximate price for Casodex is: 28 tablets of 50 mg - 4500 rubles, 28 tablets of 150 mg - 7400 rubles.
Casodex: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Casodex 50 mg film-coated tablets 28 pcs. 1897 RUB Buy |
|
Casodex 150 mg film-coated tablets 28 pcs. RUB 4560 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
