Duinum Mechanism of Action

Pharmacotherapeutic group: Ovulation stimulants, synthetic, Sex hormones and modulators of the genital system. ATC code: G03GB02.
Pharmacology: Pharmacodynamics: Mechanism of action: The ovulatory response to cyclic clomifene therapy is mediated through increased output of pituitary gonadotrophins, which in turn stimulates the maturation and endocrine activity of the ovarian follicle.
Pharmacodynamic effects: Clomifene is a triarylethylene compound (related to chlorotrianisene and triparanol). It is a non-steroidal agent which stimulates ovulation in a high percentage of appropriately selected anovulatory women.
Pharmacokinetics: Orally administered ¹⁴C labelled clomifene citrate was readily absorbed when administered to humans. Cumulative excretion of the ¹⁴C label by way of urine and faeces averaged about 50% of the oral dose after 5 days in 6 subjects, with mean urinary excretion of 7.8% and mean faecal excretion of 42.4%. A mean rate of excretion of 0.73% per day of the ¹⁴C dose after 31 days to 35 days and 0.45% per day of the ¹⁴C dose after 42 days to 45 days was seen in faecal and urine samples collected from 6 subjects for 14 to 53 days after clomifene citrate ¹⁴C administration. The remaining drug/metabolites may be slowly excreted from a sequestered enterohepatic recirculation pool.
Toxicology: Preclinical safety data: Carcinogenicity: Prolonged use of clomifene may increase the risk of developing ovarian cancer.
Long term toxicity studies in animals have not been performed to evaluate the carcinogenic potential of clomifene.
Mutagenicity: Mutagenic potential of clomifene has not been evaluated.