The maximum concentration rosuvastatin reached after approximately 5 hours after oral masteron ingestion. The absolute bioavailability – about 20%. Distribution .Rosuvastatin is stored mainly in the liver, the main organ of synthesis and oral masteron. . Plasma protein binding (mostly to albumin) is about 90%. Metabolism . Biotransformiroetsa to a small extent (about 10%), as a non-core substrate for the metabolic enzymes cytochrome .
The basic isoenzyme involved in the metabolism of rosuvastatin is in the metabolism are involved to a lesser extent. The main metabolites identified are dismetil and lactone metabolites. N-dismetil approximately 50% less active than rosuvastatin lactone pharmacologically inactive metabolites. Over 90% of the pharmacological activity inhibiting circulating reductase inhibitor rosuvastatin is provided, the rest – its metabolites. Excretion . Approximately 90% of rosuvastatin dose is excreted unchanged in the feces. The remaining part is excreted in urine. The half-life not change with increasing dose.
Mean plasma clearance value of approximately . As with otherredukazy in the process of “hepatic” capture rosuvastatin involved anionic membrane transporter , performs an important role in the hepatic elimination of rosuvastatin.
Gender and age did not have a clinically meaningful effect on the pharmacokinetics of rosuvastatin. Comparative studies on the pharmacokinetics of rosuvastatin in Japanese and Chinese patients living in Asia, showed approximately twofold increase in the average area values under the curve “concentration-time»oral masteron, in comparison with indicators of the Europeans living in Europe and Asia. There was no influence of genetic factors and environmental factors on the resulting differences in the pharmacokinetic parameters. Pharmacokinetic analysis among the various ethnic groups of patients showed no clinically relevant differences among Europeans, Hispanics, blacks or African Americans. In patients with mild to moderate renal insufficiency, the value of the plasma concentration of rosuvastatin or the N-dismetila does not change. In patients with severe renal insufficiency (clearance creatinine (KK) <30 ml / min) rosuvastatin plasma concentration of 3-fold higher concentration and N-dismetila 9 times higher than in healthy volunteers. The concentration of rosuvastatin in the blood plasma of patients on hemodialysis were approximately 50% higher than in healthy volunteers. In patients with different stages of liver failure were found to increase the T ½ rosuvastatin (patients with a score of 7 or less on the scale of Child-Pugh). In 2 patients with points 8 and 9 on the Child-Pugh marked increase in T ½ , at least 2 times. Experience in the use of rosuvastatin in patients with a score of higher than 9 on the scale of Child-Pugh is absent.
Indications for use:
- Primary hypercholesterolaemia (type IIa including family getereozigotnuyu giperholestreinemiyu) hypercholesterolemia or mixed (type 116) as an adjunct to diet when diet and other non-pharmacological treatments (eg exercise, weight loss) are insufficient;
- homozygous familial hypercholesterolemia oral masteron as an adjunct to diet and other holesterinsnizhayuschey therapy or in cases where such therapy is not appropriate to the patient.