ATC Group: L02AE Gonadotropin releasing hormone analogues

Buserelin is a synthetic peptide. It is a superactive analogue of natural gonadotrophin releasing hormone (gonadorelin, LHRH or GNRH). After an initial stimulation of gonadotrophin release, it down-regulates the hypothalanic-pituitary-gonadal axis.

Goserelin is a synthetic analogue of naturally occurring LHRH. On chronic administration goserelin results in inhibition of pituitary LH secretion leading to a fall in serum testosterone concentrations in males and serum estradiol concentrations in females.

Histrelin is a gonadotropin releasing hormone (GnRH) agonist and an inhibitor of gonadotropin secretion when given continuously. It is indicated for the treatment of children with central precocious puberty (CPP). However, continuous administration of histrelin acetate causes a reversible down-regulation of the GnRH receptors in the pituitary gland and desensitization of the pituitary gonadotropes.

Leuprorelin is inactive when given orally due to poor membrane permeability and an almost complete inactivation by intestinal proteolytic enzymes. Leuprorelin has potent LHRH agonist properties when given during short-term and intermittent therapy, however, when administered in a continuous, nonpulsatile manner, LHRH analogs induce inhibition of gonadotropin secretion and suppression of testicular steroidogenesis.

Triptorelin is a decapeptide analogue of GnRH which initially stimulates release of pituitary gonadotropins.