Dienogest
When ATH:
G03FA15
Pharmacokinetics
After oral dienogest is rapidly and completely absorbed from the gastrointestinal tract. Cmax achieved through 2.5 no. The absolute bioavailability of dienogest 96% and stored in combination with ethinylestradiol.
Pharmacokinetics dienogesta is not dependent on the level of GSPS. Daily admission concentration in serum is increased 1,3 times, reaching equilibrium condition during the first half of cycle treatment.
Distribution
About 10% dienogest is in a free form in plasma, about 90% – nonspecifically bound to albumin. Dienogest does not bind to specific transport proteins – globulin, sex hormone binding (SHBG), and corticosteroid svyazыvayushtim globulinom (KSG), – and, so, Testosterone does not displace from its association with SHBG and cortisol in connection with the DRG. Unlikely, dienogest that affects the physiological processes of transport of endogenous steroids.
Dienogest slightly accumulates with daily intake. Average concentration in plasma is about 30 ng / ml after three cycles of treatment.
Metabolism
Effect “first pass” minor. Dienogest predominantly metabolized by hydroxylation, gidrogenizacii, conjugation and flavoring into inactive metabolites.
Deduction
T1/2 is about 9 h in single dose and about 10 h at multiple dose.
After a single dose 1 Janine Bean total clearance of dienogest 3.6 l / h and marginally reduced to 2.8 l / h after three cycles of treatment.
Value excretion of dienogest in the urine and feces of 3.2 after ingestion 0.1 dienogest mg / kg body weight.
After oral administration about 86% of the dose is excreted 6 days. Most of this amount (about 42%) is displayed for the first 24 no, mainly, urine.
