Bicalutamide is a racemic mixture of a non-steroidal antiandrogenic activity predominantly (R) -enantiomer, has no other endocrine anavar for sale anavar for sale activity. Bicalutamide binds to the androgen receptor and without activating gene expression, inhibits the stimulatory effect of androgens. The result is a regression of prostate tumors. In some patients receiving bicalutamide cessation may result in the development of clinical “antiandrogen withdrawal syndrome.”
After intake of rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect absorption.
In the equilibrium state, about 99% of total circulating enantiomers of the active (R) enantiomer.
In pharmacokinetics (R) -enantiomer does not affect the age, renal impairment, mild to moderate hepatic dysfunction. There is evidence that patients with severely impaired liver function slows down the elimination of enantiomer from plasma.
The connection to plasma proteins is high (for a racemic mixture of for the enantiomer is extensively metabolized in the liver (by oxidation and glucuronic acid conjugates). Metabolites are excreted by the kidneys and intestines in approximately equal proportions.
- Hypersensitivity to bicalutamide and / or other components of the drug;
- simultaneous with terfenadine, astemizole, and cisapride;
- Kalumid® should not be given to anavar for sale women and children.
With caution : liver dysfunction; lactase deficiency, lactose intolerance, glucose-galactose malabsorption (in the dosage form of the drug contains lactose) ..
Dosage and administration Adult males (including the elderly) : When the prevalence of prostate cancer in combination with a GnRH analogue or surgical castration , inside of 50 mg once daily. Treatment with Kalumid ® should be started simultaneously with the start of the reception, analogue of GnRH IPT surgical castration. In locally advanced prostate cancer : the interior of 150 mg once a day. Kalumid ®should be taken for a long time, for at least 2 years. If signs of progression of the disease taking the drug should be discontinued. Renal function : Dosage adjustment is not required. Violations of the liver : in mild abnormal liver function Dose adjustment is not required. In patients with moderate and severe hepatic impairment increased accumulation of the drug can be observed Kalumid ® .
The pharmacological action of bicalutamide may condition the following side effects:
- very frequently (> 10%): gynecomastia (may persist even after the cessation of therapy, particularly in the case of taking the drug for a long time), thoracic pain glands, “tides” of blood to the face;
- frequent ( > 1% and <10%): diarrhea, nausea, transient increase in activity of “liver” transaminases, cholestasis and jaundice (described liver function changes are rarely rated as serious, they were transient in nature, completely disappeared or decreased with continued therapy or after cancellation drug) anavar for sale, pruritus, asthenia; when use of the drug in a daily dose of 150 mg – alopecia or hair regrowth, decreased libido, sexual dysfunction, weight gain.
- rare ( > 0.1% – <1%): hypersensitivity reactions, including angioedema and urticaria, interstitial lung disease; angina pectoris, prolongation of the interval QT, cardiac arrhythmias; when use of the drug in a daily dose of 150 mg, abdominal pain, depression, dyspepsia, hematuria
- very rarely ( > 0.01% – <0.1%): vomiting, dry skin (when using the drug in a daily dose of 150 mg of dry skin – there is often), liver failure (cause-and-effect relationship – with taking bicalutamide significantly is not installed), thrombocytopenia .
With simultaneous use of bicalutamide and GnRH analogues can also be observed -Follow side effects with frequency. > 1% (causal connection with taking the drug is not installed, some of the noted side effects occurred in elderly patients): Since the cardiovascular system : the heart failure. From the digestive system : anorexia, dry mouth, dyspepsia, dysphagia, constipation, flatulence. From the nervous system : dizziness, headache, insomnia, somnolence. respiratory system : shortness of breath. From the urinary system : nocturia, polyuria. From the hematopoietic system : anemia, leukopenia. On the part of the skin and its appendages : alopecia, rash, sweating, hirsutism. From the laboratory anavar for sale parameters : hyperglycemia, increased activity of “liver” transaminases. Other : abdominal pain, chest pain , pelvic pain, decrease or increase in body weight, edema, diabetes, fever.
Overdose cases are not described in humans. There is no specific antidote.
Treat symptomatically. Dialysis is not effective, since bicalutamide is closely associated with proteins and excreted by the kidneys unchanged. Shown general supportive treatment and monitoring of vital body functions.
Interaction with other medicinal products
There are no data on the pharmacokinetic or pharmacodynamic interactions between bicalutamide and GnRH analogues.
In in vitro studies have shown that the (R) enantiomer of bicalutamide inhibit SYP ZA4, to a lesser extent affecting the activity of CYP 2C9, 2C19 and 2D6. The potential ability of bicalutamide to interact with others: drugs are found, however, when using bicalutamide for 28 days, patients receiving midazolam, area anavar for sale under the curve “concentration-time» (AUC) midazolam is increased by 80%.
Incompatible with terfenadine, astemizole , cisapride.
caution should be exercised when administering the drug Kalumid ® simultaneously with cyclosporine or calcium channel blockers. You may need to decrease the dose of these drugs, particularly in the case or potentiation of side effects. After the start of the use or discontinuation Kalumid ® recommend close monitoring of cyclosporine plasma concentrations and clinical condition of the patient.
The simultaneous use of the drug Kalumid ® and drugs that inhibit the microsomal oxidation of drugs, such as cimetidine or ketoconazole may result in increased concentrations of the drug Kalumid® plasma, and possibly an increase in the incidence of adverse effects.
Increases the coumarin anticoagulants, including warfarin (competition for protein binding).
tablets film-coated, 50 mg. 15 tablets in a blister of PVC / AL.
2 or 6 blisters with instruction on use in carton box.
Store at temperatures not above 30 ° C.
Keep out of reach of children!