Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2019 Publisher: Besins Healthcare, Avenue Louise 287, B-1050 Brussels, Belgium
Pharmacotherapeutic group: Sex hormones and modulators of the genital system; Progestogens; Pregnen-(4) derivatives
ATC code: G03DA04
Progesterone is a natural progestogen, the main hormone of the corpus luteum and the placenta. It acts on the endometrium by converting the proliferating phase to the secretory phase. Utrogestan 100mg Capsules have all the properties of endogenous progesterone, in particular gestagenic, antiestrogenic, slightly anti-androgenic and antialdosterone effects.
As estrogens promote the growth of the endometrium, unopposed estrogens increase the risk of endometrial hyperplasia and cancer. The addition of progesterone greatly reduces the estrogen-induced risk of endometrial hyperplasia in non-hysterectomised women.
Micronised progesterone is absorbed by the digestive tract. Pharmacokinetic studies conducted in healthy volunteers have shown that after oral administration of 2 capsules (200mg), plasma progesterone levels increased to reach the Cmax of 13.8ng/ml +/- 2.9ng/ml in 2.2 /- 1.4 hours. The elimination half-life observed was 16.8/- 2.3 hours.
Progesterone is approximately 96%-99% bound to serum proteins, primarily to serum albumin (50%-54%) and transcortin (43%-48%).
Urinary elimination is observed for 95% in the form of glycuroconjugated metabolites, mainly 3 α, 5 β–pregnanediol (pregnandiol).
Progesterone is metabolised primarily by the liver. The main plasma metabolites are 20 α hydroxy- ∆ 4 α-prenolone and 5 α-dihydroprogesterone. Some progesterone metabolites are excreted in the bile and these may be deconjugated and further metabolised in the gut via reduction, dehydroxylation and epimerisation. The main plasma and urinary metabolites are similar to those found during the physiological secretion of the corpus luteum.
The pharmacokinetics of micronized progesterone is independent of the dose administered. Although there were some inter-individuals variations, the same individual pharmacokinetic characteristics were maintained over several months permitting appropriate individual adaptation of the posology and indicating predictable responses to the drug.
As per adults above.
Nonclinical data revealed no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity to reproduction and development.
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