Casodex, 50 mg 28 pcs
€59.93 €49.94
Casodex is an antitumor, antiandrogenic.
Pharmacodynamics
The anti-androgenic nonsteroidal drug. It is a racemic mixture, with predominantly the (R)-enantiomer having antiandrogenic activity. The drug has no other types of endocrine activity. Casodex® binds to androgen receptors and, without activating gene expression, suppresses the stimulating effect of androgens. This results in regression of prostate neoplasms.
In some patients, discontinuation of Cassodex may lead to the development of clinical antiandrogen withdrawal syndrome.
Pharmacokinetics
Intake
After oral administration is quickly and completely absorbed from the gastrointestinal tract. Concomitant ingestion does not affect absorption.
Distribution
Daily ingestion of 50 mg Cassodex has a Css (R)-enantiomer in plasma of about 9 µg/mL. At equilibrium, about 99% of all circulating enantiomers in the blood are the active (R)-enantiomer. When Casodex is taken daily, the plasma concentration of the (R)-enantiomer is increased about 10-fold due to a long T1/2, which allows Casodex to be taken once daily. Binding to plasma proteins is high (for the racemic mixture 96%, for the (R)-enantiomer 99.6%).
Metabolism
It is intensively metabolized in the liver by oxidation and formation of conjugates with glucuronic acid.
Excretion
The metabolites are excreted with urine and bile in approximately equal proportions. The (S)-enantiomer is eliminated much faster than the (R)-enantiomer, the T1/2 of the latter is about 7 days.
Pharmacokinetics in special clinical cases
The pharmacokinetics of (R)-enantiomer is not affected by age, impaired renal function, mild and moderate hepatic function. There is evidence that in patients with severe hepatic impairment the elimination of (R)-enantiomer from plasma is delayed. Cumulation of bicalutamide in the body may be observed in patients with moderate to severe hepatic impairment.
Indications
Disseminated prostate cancer (in combination with a GnRH analogue or with surgical castration).
Active ingredient
Composition
1 tablet contains:
Active ingredient:
bicalutamide 50 mg;
Associates:
lactose monohydrate,
sodium carboxymethyl starch,
povidone,
p> magnesium stearate,
purified water (evaporated during manufacture);
Composition of the shell:
Hypromellose, macrogol 300, titanium dioxide, purified water.
How to take, the dosage
Casodex® is indicated in adult men (including elderly) with advanced prostate cancer in combination with a GnRH analogue or surgical castration at a dose of 50 mg once daily. Treatment should be started simultaneously with initiation of GnRH analogue or surgical castration.
Patients with impaired renal function and with mild hepatic impairment do not require dose adjustment.
In patients with moderate to severe hepatic impairment, there may be increased cumulation of the drug.
Interaction
There are no data on pharmacodynamic or pharmacokinetic interactions between Casodex and GnRH analogues.
In in vitro studies, the (R)-enantiomer of Cassodex has been shown to be an inhibitor of CYP3A4 and to a lesser extent of CYP2C9, CYP2C19, CYP2D6. In clinical trials using phenazone as a marker of cytochrome P450 activity, no potential ability of Cassodex to interact with other drugs was found. However, when Casodex was used for 28 days with midazolam, the AUC of midazolam was increased by 80%.
Casodex is contraindicated with such drugs as terfenadine, astemizole and cisapride.
Caution should be exercised when prescribing Casodex together with cyclosporine or slow calcium channel blockers. It may be necessary to reduce the dose of these drugs, especially in case of potentiation or development of adverse reactions. Careful monitoring of cyclosporine plasma concentrations and the patient’s clinical condition is recommended after initiation or withdrawal of Cassodex.
With caution, concomitant use of Cassodex® and drugs that inhibit microsomal liver enzymes (e.g., cimetidine, ketoconazole) is recommended. Use of these combinations may lead to increased plasma concentrations of bicalutamide and possibly to an increased incidence of adverse reactions.
Casodex® potentiates the effect of coumarin-type indirect anticoagulants (including warfarin) because it can displace these drugs from their binding sites with proteins. It is recommended to monitor prothrombin time regularly when prescribing Kasodex to patients receiving coumarin-type indirect anticoagulants.
Special Instructions
The drug is metabolized in the liver. Given the possibility of delayed excretion of bicalutamide and cumulation of bicalutamide in patients with significant hepatic dysfunction, it is advisable to periodically assess liver function. Most changes in liver function occur within the first 6 months of treatment with Casodex.
Casodex® should be used with caution in patients with moderate to severe hepatic impairment.
Severe liver dysfunction is rare with Cassodex® (fatal cases have been reported).
In case of marked changes in liver function, Casodex should be discontinued.
In patients with disease progression with elevated prostate-specific antigen (PSA) levels, discontinuation of treatment with Casodex should be considered.
With the potential for inhibition of cytochrome P450 (CYP3A4) activity by Kasodex, caution should be exercised when concomitantly prescribing Kasodex with drugs primarily metabolized with CYP3A4.
In patients taking GnRH agonists, decreased glucose tolerance has been observed. This effect may lead to the development of diabetes mellitus or decreased glucose tolerance in patients with diabetes mellitus. Therefore, blood glucose concentrations should be monitored in patients taking Casodex® and GnRH agonists.
Impact on ability to drive vehicles and other mechanisms requiring high concentration
Drowsiness and dizziness may occur with use of Cassodex® and therefore caution should be exercised when driving motor transport or other moving machinery.
Contraindications
With caution: Use Xodex® in patients with hepatic impairment, lactose intolerance, lactase deficiency, and glucose/galactose malabsorption syndrome.
Side effects
Casodex® is well tolerated by most patients and only rarely does it have to be stopped because of the side effects it causes.
The pharmacological effects of Cassodex® may cause the following side effects.
Very common ( > 10%): gynecomastia (may persist even after stopping therapy, especially if the drug has been taken for a long time), breast soreness, hot flashes.
Often (â¥1%- < 10%): hot flashes*, anemia*, dizziness*, abdominal pain*, constipation*, nausea*, peripheral edema*, hematuria*, hepatotoxicity, transient increase in liver transaminases, cholestasis, and jaundice (the described changes in liver function were rarely rated as serious, were transient, and disappeared completely or diminished despite continuation of therapy or after drug withdrawal), decreased appetite, decreased libido, depression, somnolence, dyspepsia, flatulence, alopecia, hirsutism or hair regrowth, dry skin, skin itching, erectile dysfunction, chest pain, weight gain.
Rarely (â¥0.1%- < 1%): hypersensitivity reactions, angioedema, urticaria, interstitial lung disease (fatal cases reported), heart failure.
Very rare (â¥0.01%- < 0.1%): hepatic failure (fatal cases reported).
* – When concomitant use of Cassodex and GnRH analogues, side effects have been observed frequently.
Overdose
No cases of overdose in humans have been described.
There is no specific antidote, so if necessary symptomatic therapy is carried out.
Dialysis is ineffective because bicalutamide is firmly bound to proteins and is not excreted unchanged in the urine.
General supportive therapy and monitoring of vital body functions are indicated.
Pregnancy use
Casodex® is contraindicated in women and should not be administered to pregnant or lactating women.
Similarities
Weight | 0.016 kg |
---|---|
Shelf life | 5 years |
Conditions of storage | At a temperature not exceeding 30 °C |
Manufacturer | Corden Pharma GmbH, Germany |
Medication form | pills |
Brand | Corden Pharma GmbH |
Related products
Buy Casodex, 50 mg 28 pcs with delivery to USA, UK, Europe and over 120 other countries.