Clomifene Other names: Chlomaphene Chloramifene Chloramiphene Cisclomiphene Zuclomiphene

The ovulatory response to 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 tablets 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.

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.

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.