Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1. Pharmacodynamic properties:
Pharmacotherapeutic group: Sex and urogenital system hormones
ATC Code: G03DA04

UTROGESTAN, which contains micronised progesterone, significantly raises plasma progesterone concentrations after oral use. It therefore corrects progesterone deficiencies.

Pharmacokinetic Properties

        5.2. Pharmacokinetic properties

Oral administration

Blood concentrations of progesterone rise from the first hour after dosing and the highest plasma concentrations are found 1 to 3 hours after dosing. Because of the hormone tissue retention time, the daily dosage appears to need to be divided into two separate doses 12 hours apart in order to achieve hormone exposure throughout the 24 hour period.

Metabolism: the plasma and urinary metabolites are identical to those found following physiological secretion from the ovarian corpus luteum: in plasma these are mostly 20-alpha hydroxy delta-4 pregnenolone and 5-alpha dihydroprogesterone. 95% of urinary excretion is in the form of glycuronoconjugated metabolites, the major one of which is 3 alpha-5 beta pregnanediol (pregnandiol).

Vaginal administration

Elevation of blood progesterone levels starts from the first hour onwards, with peak plasma levels observed 1 to 3 hours after administration.

At the average recommended dose, stable physiological levels of plasma progesterone, similar to those obtained during the luteal phase of a normal, ovulatory menstrual cycle, can be reached and maintained.

Thus, Utrogestan Vaginal soft capsules induce adequate endometrial maturity, promoting the implantation of a potential embryo.
At higher doses, increased gradually, this route of administration makes it possible to achieve blood progesterone levels similar to those observed during the first trimester of pregnancy.

Metabolism: plasma and urinary metabolites are identical to those found during physiological secretion of corpus luteum in the ovaries: in plasma, its main metabolites are 20-alpha-hydroxy-delta-4-pregnenolone and 5-alpha-dihydroprogesterone. Urinary elimination occurs at a rate of 95% in the form of glucuronide-conjugated metabolites, the main one being 3-alpha-5-beta pregnanediol (pregnandiol).