Lb. Barradell et D. Mctavish, HISTRELIN - A REVIEW OF ITS PHARMACOLOGICAL PROPERTIES AND THERAPEUTIC ROLE IN CENTRAL PRECOCIOUS PUBERTY, Drugs, 45(4), 1993, pp. 570-588
Histrelin is a synthetic gonadotrophin-releasing hormone (GnRH) agonis
t which, when administered over a prolonged period, suppresses the rel
ease of gonadotrophins.from the anterior pituitary. Data from clinical
trials undertaken in small numbers of patients with idiopathic centra
l precocious puberty have demonstrated that histrelin 8 to 10 mug/kg/d
ay administered subcutaneously desensitises the anterior pituitary to
gonadotrophin secretion within 3 months, ablating the pubertal gonadot
rophin response to GnRH stimulation and reducing circulating gonadal s
ex steroid levels. When histrelin is administered to treat central pre
cocious puberty, the rate of secondary sexual maturation is slowed and
in some cases there is a reversal of maturation which occurs before i
nitiation of treatment. Of equal importance, histrelin therapy appears
to have decelerating effects on skeletal maturation, allowing more st
atural growth; an increase in final adult height is predicted from ava
ilable data, but will need to be confirmed in long term.follow-up stud
ies currently being undertaken. The most common adverse event reported
during histrelin therapy was a skin reaction at the site of subcutane
ous injection. Few patients have discontinued therapy because of any a
dverse event. Although experience with histrelin is limited, the absen
ce of effective clinically available alternatives and the demonstrated
efficacy of histrelin justifies its place as a first-line therapy for
patients with central precocious puberty.