Chemical formula: C₂₂H₃₂O₃ Molecular mass: 386.524 g/mol PubChem compound: 6279
Medroxyprogesterone acetate when administered parenterally at the recommended dose to women, inhibits the secretion of gonadotropins which, in turn, prevents follicular maturation and ovulation and causes thickening of cervical mucus which inhibits sperm entry into the uterus.
Medroxyprogesterone acetate exerts anti-oestrogenic, anti-androgenic and antigonadotrophic effects.
Medroxyprogesterone acetate has actions and uses similar to those of progesterone.
Medroxyprogesterone acetate has minimal androgenic activity compared to progesterone and virtually no oestrogenic activity.
Progestogens are used in the treatment of dysfunctional uterine bleeding, secondary amenorrhoea and endometriosis.
Medroxyprogesterone acetate is rapidly absorbed from the G-I tract with a single oral dose of 10-250 mg. The time taken to reach the peak serum concentration (Tmax) was 2-6 hours and the average peak serum concentration (Cmax) was 13-46.89 mg/ml.
Unmetabolised medroxyprogesterone acetate is highly plasma protein bound. Medroxyprogesterone acetate is metabolised in the liver.
Medroxyprogesterone acetate is primarily metabolised by faecal excretion as glucuronide conjugated metabolite.
Metabolised medroxyprogesterone acetate is excreted more rapidly and in a greater percentage following oral doses than after aqueous intramuscular injection.
Parenteral medroxyprogesterone acetate (MPA) is a long acting progestational steroid. The long duration of action results from its slow absorption from the injection site. Immediately after injection of 150 mg/ml MPA, plasma levels were 1.7 ± 0.3 nmol/l. Two weeks later, levels were 6.8 ± 0.8 nmol/l. Concentrations fell to the initial levels by the end of 12 weeks. At lower doses, plasma levels of MPA appear directly related to the dose administered. Serum accumulation over time was not demonstrated. Medroxyprogesterone acetate is eliminated via faecal and urinary excretion. Plasma half-life is about six weeks after a single intramuscular injection. At least 11 metabolites have been reported. All are excreted in the urine, some, but not all, conjugated.
No data held.
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