Following oral administration of a single dose of 300 mg of bioavailability is about 13%. Communication with plasma proteins – high (98%) and remains constant after reaching masteron 100 therapeutic blood plasma concentration. The degree of binding to plasma proteins is not dependent on gender, age, liver function, and does not change with slightly expressed or moderate renal insufficiency, but may be reduced in severe renal insufficiency. The maximum concentration of the drug is determined 1-2 hours after ingestionn.
The half-life (T1 / 2) – 5-9 hours.
It writes mainly in unchanged form – through the intestines of 90%, the kidneys – 7%. A small portion (less than 2%) excreted by the kidneys in the form of glucuronides. 20% of the concentration in the urine is atsilglyukuronid eprosartan and 80% – unmodified drug. Virtually accumulates. Body weight, gender and race did not influence the pharmacokinetics of eprosartan. In patients younger than 18 years old pharmacokinetics has not been studied.
In old age, Cmax and AUC values increase on average in 2 times, which, however, does not require correction dosing regimen.
In liver failure value AUC (but not Cmax) increased on average by 40%, which does not require correction dosing regimen.
When eprosartan in patients with moderate chronic renal failure (creatinine clearance (CC) from 30 to 59 ml / min.), The 30%, and severe (creatinine clearance from 5 to 29 ml / min.) – 50% higher as compared with healthy volunteers.
: Hypersensitivity to the drug; pregnancy; lactation; age of 18 years (effectiveness and safety have been established); hemodynamically significant bilateral renal artery stenosis and stenosis of the artery to a solitary kidney.
Lactose intolerance, lactase deficiency or masteron 100 syndrome malabsorption (product contains lactose monohydrate).
Severe chronic heart failure (III-IV functional class NYHA classification); bilateral renal artery stenosis, renal artery stenosis only, reduction in blood volume (CBV) (including from vomiting, diarrhea, high doses of diuretics); renal failure (creatinine clearance less than 60 mL / min).
The company has no data on the safety in patients with end-stage renal failure, and in patients on hemodialysis.
Application of pregnancy and lactation
is not recommended to use pregnancy. Use of the drug masteron 100 is contraindicated in the second and third trimesters of pregnancy. Except when continuing therapy is regarded as vital, patients planning pregnancy should go to reception alternative antihypertensive agents with established safety features for use in pregnancy. Therapy should be discontinued immediately after the establishment of pregnancy, and, if necessary, alternative therapy should be started. It is known that angiotensin II receptor antagonist therapy during the second and third trimesters of pregnancy is toxic to the fetus (worsening of renal function, oligohydramnios, delayed ossification of the skull bones) and newborn (renal failure, hypotension, hyperkalemia). If the start of treatment the must be in the second trimester of pregnancy, it is recommended to carry out ultrasonic testing condition of the skull and renal function in the fetus. Newborns whose mothers took the , should be carefully monitored for detection of arterial hypotension.
Lactation: Data on the penetration of eprosartan passes into breast milk is not. If necessary, use of the masteron 100 lactation, breast-feeding should be discontinued.