Reduces the concentration of testosterone and other androgens in the serum below the indicators that can be obtained during treatment with agonists Liu liberina or after orchiectomy. This is due to the selective inhibition of the enzyme , which is required for the biosynthesis of androgens. The concentration of prostate-specific antigen (PSA) is a biomarker for patients with prostate cancer,in patients taking part in clinical trials, major drug , were not allowed to use spironolactone, since its molecules bind to androgen receptors and PSA levels can increase.
The analgesic effect of
proportion of patients who have observed a palliative analgesic effect was significantly higher than when using the drug Zitiga ® , compared with the placebo group. Moreover, compared with patients receiving placebo in lesser proportion of patients receiving the drug Zitiga ® , it marked progression of pain.
The risk of skeletal-related events
compared with the placebo group at the lower proportion of patients receiving the drug , there have been cases of bone lesions, which were classified as pathological fracture, spinal compression, palliative radiation bone, bone surgery.
The pharmacokinetics of abiraterone acetate and abiraterone was examined in healthy volunteers, in patients with advanced metastatic prostate cancer and non-cancer patients with renal or hepatic insufficiency. Abiraterone acetate in vivo rapidly converted to abiraterone, which is an inhibitor of androgen biosynthesis.
Oral administration of the drug primobolan only cycle fasted abiraterone time to maximum plasma concentration is approximately 2 hour. The drug with food as compared to taking the drug on an empty stomach, leads to 10-fold increase in the area under the curve “concentration-time» (AUC) and 17-fold increase in maximum concentration abiraterone (Cmax), depending on the fat ingested food. Whereas normal diversity of content and composition of meals, taking medication with food has the ability to provide a variety of systemic exposure. Therefore, the drug should not be taken with food.
Binding to plasma proteins labeled with 14 C-abiraterone is 99.8%. Apparent volume of distribution is about 5,630 liters, which indicates that abiraterone actively distributed in peripheral tissues.
Oral administration of 14 C-abiraterone acetate in capsules, abiraterone acetate hydrolyzed to abiraterone, which in turn undergoes metabolism, including sulfation, hydroxylation and oxidation, mainly in the liver. Most circulating 14 C-abiraterone (approximately 92%) is in the form of abiraterone metabolites. Of the 15 detectable primobolan only cycle metabolites for each of the two major metabolites – abiraterone sulphate and N-oxide abiraterone sulphate – accounted for 43% of the total radioactivity.
According to studies conducted in healthy volunteers, the mean half-life of abiraterone in plasma is approximately 15 hours. When taken orally, labeled 14 C-abiraterone acetate at a dose of 1 g of about 88% of the radioactive dose is excreted through the intestine and about 5% is excreted by the kidneys. The main substance found in feces, were unchanged abiraterone acetate and abiraterone (approximately 55% and 22% of the administered dose, respectively).
Special patient groups
Patients with hepatic impairment
The pharmacokinetics of abiraterone has been studied in patients with mild to moderate hepatic insufficiency (class A and B in Child-Pugh classification, respectively) and in healthy volunteers. Abiraterone systemic exposure after a single oral administration at a dose of 1 g was increased by approximately 11% in patients with mild hepatic impairment and by 260% in patients with moderate hepatic impairment.Abiraterone average half-life is increased to approximately 18 hours in patients with mild hepatic failure and up to about 19 hours in patients primobolan only cycle with moderate hepatic impairment. For patients with mild degree of liver failure, the dose correction is not required. Zitiga The drug is not recommended for patients with moderate or severe hepatic insufficiency (class B or C according to Child-Pugh), since in this case it is impossible to predict the required dose adjustment. Therefore Zitiga drug should be used with caution in patients with impaired liver function moderate only if the benefit clearly outweighs the potential risk.Zitiga The drug should not be prescribed to patients with severe impairment of liver function. Patients who in the course of therapy with developed hepatotoxicity may require temporary removal of the drug, and dose adjustment.
Patients with renal insufficiency
The pharmacokinetics of abiraterone were compared in patients with end-stage renal disease receiving hemodialysis, the standard scheme, and in patients with normal renal function. Systemic exposure to abiraterone acetate after oral administration at a dose of 1 g in patients with end-stage renal disease receiving hemodialysis, did not increase. It should be used with caution in drug Zitiga ® to patients with cancer of the prostate in violation of severe renal function, since clinical data on the use of the drug Zitiga ® in these patients are missing.
Effects on the QT interval
was found effect on QT / QTc interval. That drug Zitiga ® has no significant
The drug Zitiga ® in combination with prednisone for the treatment of metastatic castrate-resistant prostate cancer.
- Hypersensitivity to the active ingredient or any excipient of the drug;
- Children under the age of 18 years;
- Severe liver dysfunction.
- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
- It should be used with caution in drug Zitiga ® to patients with cancer of the prostate in violation of severe renal function, since clinical data on the use of the drug Zitiga ® in these patients are missing.
- Caution should be exercised when treating patients whose condition may deteriorate with increasing blood pressure or development of hypokalemia, for example, patients with heart failure, with recent myocardial infarction or ventricular arrhythmias; left ventricular ejection fraction less than 50%, heart failure III-IV NYHA functional class classification.
Dosing and Administration
The recommended daily dose of the drug Zitiga ® is 1 g (4 tablets of 250 mg), 1 per day for 1 hour before meals or 2 hours after a meal. The tablets should be swallowed whole, without chewing, with a small amount of water. Preparation Zitiga ® is used together with low doses of prednisolone. The recommended dose of prednisone 10 mg / day.
The drug Zitiga ® should not be taken with food.
Within 1 hour after taking the drug is not suitable for eating.
Before starting treatment with primobolan only cycle , every 2 weeks during the first three months of treatment, followed by a monthly measurement of the activity of serum transaminases and bilirubin. Blood pressure, the concentration of potassium in the blood and the degree of fluid retention should be evaluated monthly. Omitting the regular daily dose Zitiga ® , prednisolone next day should take the normal dose of the drug missed.
Dose adjustment in patients with impaired hepatic function
dose adjustment in patients with impaired mild liver function is not required. No data on the efficacy and safety of abiraterone acetate when repeated use in patients with impaired liver or moderate to severe function (class B or C according to Child-Pugh), so it is impossible to predict the required dose adjustment. The drug Zitiga ® should be used with caution in patients with impaired liver function moderate, and only if the benefit clearly outweighs the potential risk. The drug Zitiga ® should not be administered to patients with impaired liver function severe.
If in the course of treatment, the patient developed symptoms of hepatotoxicity (increased activity of alanine aminotransferase or aspartate aminotransferase 5 times the upper limit of normal or bilirubin concentration of 3 times the upper limit of normal), treatment should be discontinued immediately until full normalization of liver function.
Repeated therapy in patients with liver function normalized indexes can be started with a reduced dose of 500 mg (two tablets) once daily. In this case, control of serum transaminases and bilirubin should be performed at least every two weeks for three months, and then – on a monthly basis. If the symptoms of hepatotoxicity occur when receiving doses of 500 mg, the drug therapy Zitiga ® should be discontinued.
If the patient at any time during therapy develop severe hepatotoxicity (ALT or AST activity exceeds the upper limit of normal to 20 times), the drug Zitiga ® should be discontinued, the re-appointment of the drug in such patients is not possible.
Special patient groups
Use in patients with hepatic insufficiency
For patients with pre-treatment violation mild liver function (class A classification Child-Pugh) correction dose is not required. The drug Zitiga ® should be used with caution in patients with impaired liver function moderate, and only if the benefit clearly outweighs the potential risk. The drug Zitiga ® should not be administered to patients with hepatic impairment, severe, class B and C according to Child-Pugh classification.
Use in patients with renal insufficiency
For patients with impaired renal function dose adjustment is required. However, caution should be prescribed the drug Zitiga ® to patients with cancer of the prostate in violation of severe renal function, since clinical data on the use of the drug Zitiga ® in these patients are missing.
For children, use of the drug Zitiga ® irrelevant, because this age group is not prostate cancer. buy anabolic steroids online bruce lee’s workout anabolic steroids online uk