Progesterone acts on progesterone receptors throughout the body, including in the breast, uterus, central nervous system, and cardiovascular system. Two effects matter most for the indications biio. uses Prometrium for.
The first is direct progesterone receptor activity, which counterbalances the effects of unopposed oestrogen — relevant for cyclical symptoms, perimenopausal patterns, and combined hormone therapy. In women on oestrogen therapy with a uterus, progesterone is essential to protect the uterine lining from oestrogen-driven hyperplasia.
The second is the effect of allopregnanolone, a progesterone metabolite produced when progesterone is taken orally. Allopregnanolone is a positive modulator of the GABA-A receptor, producing a calming, sleep-supporting effect. The oral capsule route maximises allopregnanolone production due to the gut and liver first-pass metabolism pathway. This is why Prometrium is dosed at night — the sedating effect is intentional when used for sleep, and is the reason daytime dosing is not used. In some patients it is important to note that there may be a allopregnanolone sensitivity, where the opposite effects occur, your risk for this occuring will be discussed with you and advice on how to manage this will also be discussed.
RECEPTOR ACTIVITY
Acts directly on progesterone receptors, counterbalancing the effects of unopposed oestrogen.
PROTECTS THE LINING
On oestrogen therapy with a uterus, progesterone is essential to protect the lining from hyperplasia.
ALLOPREGNANOLONE · GABA-A
The oral route produces a calming, sleep-supporting metabolite — best taken at night.
A SENSITIVITY TO NOTE
A minority have allopregnanolone sensitivity — the opposite effect. biio. will assess your risk and how to manage it.