Which among the following is TRUE about Clomiphene?
High-Yield Explanation
Clomiphene is an antiestrogen. These compounds are distinguished from the Selective estrogen receptor modulators(SERMs) in that they are pure antagonists in all tissues studied. Clomiphene citrate is a potent anti-estrogen that primarily is used for treatment of anovulation in the setting of an intact hypothalamic--pituitary axis and adequate estrogen production (e.g., PCOS). By inhibiting the negative feedback effects of estrogen at hypothalamic and pituitary levels, clomiphene increases follicle-stimulating hormone (FSH) levels--typically by ~50%--and thereby enhances follicular maturation. Clomiphene s approved for the treatment of infeility in anovulatory women. Clomiphene increases gonadotropin secretion and stimulates ovulation. It increases the amplitude of LH and FSH pulses without changing pulse frequency. This suggests that the drug is acting largely at the pituitary level to block inhibitory actions of estrogen on gonadotropin release from the gland and/or is somehow causing the hypothalamus to release larger amounts of GnRH per pulse. Ref: Levin E.R., Hammes S.R. (2011). Chapter 40. Estrogens and Progestins. In L.L. Brunton, B.A. Chabner, B.C. Knollmann (Eds), Goodman & Gilman's The Pharmacological Basis of Therapeutics, 12e.