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Gestrinone, a synthetic trienic 19-norsteroid, inhibits the pituitary gland. It exerts its activity at the level of gonadotrophin release.
Gonadotrophin inhibition appears early, as from the first month if the treatment is initiated on the first day of the ovulatory cycle. The subsequent suppression of ovarian secretions entails a rapid inactivation atrophy of endometrial and ectopic endometrial tissue.
This gonadotrophin inhibiting action is fully reversible.
Apart from its anti-pituitary activity, gestrinone exhibits anti-progesterone and anti-estrogenic properties at the cellular receptor level of the endometrium as well as the extra-uterine ectopic implants as well as other estrogen and progesterone dependent tissue. Gestrinone may produce androgenic effects.
Elimination half-life is about 24 hours. Plasma levels, 3 days after administration, represent only 5% of the maximum concentration, steady state is reached from the second administration thus avoiding any risk of accumulation under normal conditions of use.
Gonadotrophin inhibition appears early, as from the first month if the treatment is initiated on the first day of the ovulatory cycle. The subsequent suppression of ovarian secretions entails a rapid inactivation atrophy of endometrial and ectopic endometrial tissue.
This gonadotrophin inhibiting action is fully reversible.
Apart from its anti-pituitary activity, gestrinone exhibits anti-progesterone and anti-estrogenic properties at the cellular receptor level of the endometrium as well as the extra-uterine ectopic implants as well as other estrogen and progesterone dependent tissue. Gestrinone may produce androgenic effects.
Elimination half-life is about 24 hours. Plasma levels, 3 days after administration, represent only 5% of the maximum concentration, steady state is reached from the second administration thus avoiding any risk of accumulation under normal conditions of use.
