Absorption After oral administration, the time to reach maximum concentration (Cmax) of aliskiren in plasma is 1-3 hours and the absolute bioavailability of – 2.6%. Simultaneous eating reduces Cmax and area under the curve “concentration-time» of aliskiren, but it does not significantly affect the pharmacodynamics of the drug. Therefore aliskiren can be used regardless of the meal.Increased of aliskiren has a linear dependence on the dose range from 75 to 600 mg. The equilibrium concentration of aliskiren plasma levels achieved between the 5- and 7-day daily administration at one time per day and remains constant masterone with increasing initial dose 2 times.
After oral aliskiren evenly distributed in the body. Following intravenous administration, the mean volume of distribution at steady state is approximately 135 liters, indicating a significant extravascular distribution of aliskiren. The drug is moderately bound to plasma proteins (47-51%), irrespective of the concentration.
Metabolism and excretion
The average half-life of aliskiren is 40 hours (ranging from 34 to 41 hours). The drug is derived mainly unaltered through the intestine (91%). About 1.4% of an oral dose is metabolized with the participation of isoenzyme CYP3A4. After oral administration, about 0.6% of aliskiren excreted by the kidneys. Following intravenous administration, the mean plasma clearance is approximately 9 l / h.
Pharmacokinetics in special patient groups Patients over the age of 65 years When using aliskiren in patients over 65 years of correction dose is not required.
And patients with impaired renal function
The pharmacokinetics of aliskiren has been studied in patients with renal impairment of varying degrees. AUC and Smaxaliskirena indicators in patients with renal insufficiency after a single application and after reaching equilibrium concentration increased in 0.8-2 times compared with healthy individuals. However, the correlation between the above changes and the degree of renal impairment have been identified.
: Hypersensitivity to aliskiren or any other masterone component of the formulation. Efficacy and safety of Rasileza in children and adolescents under the age of 18 years, in patients with severely impaired renal function (creatinine> 150 umol / L for women and> 177 umol / L – for men and / or glomerular filtration rate less than 30 mL / min), with nephrotic syndrome, renovascular hypertension, and during regular hemodialysis, as well as with impaired liver function severe (more than 9 points on a scale Child-Pyuga) have not been established.
Caution should be exercised when administering the drug to patients with unilateral or bilateral renal artery stenosis or stenosis of the artery to a solitary kidney diabetes, reduced the volume of circulating blood, hyponatremia, hyperkalemia, or in patients after kidney transplantation.
Safety of Rasileza in patients with bilateral renal artery stenosis or stenosis of the artery to a solitary kidney has not been established.
Application of pregnancy and lactation
is insufficient data on the safety of use in pregnant not. The use of drugs during pregnancy, have a direct impact on the can cause the development of the pathology of the fetus and newborn, as well as lead to their death. As well as other means of having a direct impact on the should not be used during pregnancy and in women planning a pregnancy. Before the appointment of drugs that affect the the physician should inform patients of childbearing age about the possibility of a potential risk to the fetus in the application of these drugs during pregnancy. If pregnancy occurs during treatment masterone receiving the drug should be discontinued immediately.
It is not known whether aliskiren passes into breast milk. The question of the discontinuation Rasileza patient, breast-feeding, your doctor should be considered taking into account the benefit of therapy for the mother and the possible risk to the child. At the time of treatment Rasilezom should stop breastfeeding.