Time of maximum concentration after administration. Food does not affect the bioavailability of sunitinib. Binding of sunitinib and anavar vs winstrol its main metabolite plasma protein was 95 and 90%, respectively, without an explicit dependence on the concentration in the range . The magnitude of the estimated volume of distribution in tissues. Metabolism sunitinib performs basically isoenzyme , cytochrome enzyme, resulting in a major active metabolite, which is further metabolized by the same isoenzyme .
The proportion of the active metabolite is 23-37% of the area under “concentration-time” curve . Sunitinib appears mainly in the feces (61%); via the kidneys in the form of the drug and its metabolites derived approximately 16% of the administered dose. Total clearance when administered reached 34-62 l / hr. After a single oral administration in healthy volunteers sunitinib and its main active metabolite of 40-60 and 80-110 hours, respectively. Repeated daily application comes 3-4-fold accumulation of sunitinib and 7-10-fold accumulation of its major metabolite. The equilibrium concentrations of sunitinib and its primary active metabolite are achieved within 10-14 days. By day 14, the total concentration of sunitinib and its main active metabolite in plasma is 62,9-101 ng / ml.
Repeated daily application or repeated cycles with different dosing regimen no significant changes in the pharmacokinetics of sunitinib and its main active metabolite detected. Age, weight, creatinine clearance, race, gender, or evaluation according to the classification East combined group oncologists anavar vs winstrol did not have a clinically significant effect on the pharmacokinetics of the drug and its active metabolite. Body weight and quality of life: a population pharmacokinetic analysis showed that there is no need to correct the initial dose based on body weight and quality of life for the scale. Gender: Available data show that the apparent clearance of sunitinib in women may be 30% lower than males but this difference does not require correction of the initial dose of sunitinib.
Indications for use :
- gastrointestinal stromal tumors in the absence of the effect of imatinib treatment due to resistance or intolerance;
- common and / or metastatic renal cell carcinoma in patients who have not previously received a specific treatment;
- common and / or metastatic renal cell carcinoma with no effect on cytokine therapy.Contraindications
- Hypersensitivity to sunitinib or to other components of the drug;
- Pregnancy and lactation;
- Children’s age (efficacy and safety of the drug anavar vs winstrol in children has not been established).Precautions
Sunitinib should be used with caution in patients with prolongation of the interval in history, in patients receiving antiarrhythmic drugs, or patients with relevant cardiac disease, bradycardia, or electrolyte disturbances, as well as in patients with renal or hepatic insufficiency. It requires caution and reduce the dose of sunitinib while taking potent inhibitors of C isoenzyme, which can increase the concentration of sunitinib plasma.
Dosage and administration .
Inside. The drug is independent of food intake.
The recommended dose of the per day orally for 4 weeks followed by an interval of 2 weeks (02.04 mode). A full treatment cycle is thus 6 weeks.
If the drug was omitted to make up the missed dose should not be. The patient should take the usual prescribed dose of the drug the following day.
Depending on individual tolerance and safety of daily can be reduced or increased by 12.5 mg, and should be no more than 87.5 mg, and not less than 37.5 mg . Use in children: efficacy and safety of the in children has not been established. Use in elderly patients: dosage adjustment is not required. Use in patients with impaired hepatic function: with an increase in the activities of anavar vs winstrol levels above the upper limit of normal in less than 2.5 times or, in case of increase of these indicators as a result of the underlying disease, less than 5 times the dose adjustment is required. Use in patients with impaired renal function: when the concentration of serum creatinine less than 2 times the upper limit of normal dose adjustment not required.