Pituitary Pharmacology

The anterior pituitary produces GH, TSH, ACTH, Prolactin, and FSH/LH.
The posterior pituitary stores and releases ADH and oxytocin, both produced in the hypothalaus.
Reducing GH secretion
GH production is stiulated by GH!H and inhibited by somatostatin. "le#ated GH causes acroe$aly.
GH stiulates peripheral production o% IGF-1, which is used to guage GH levels.
GH!H is used dia$nostically to deterine GH reser#es in the anterior pituitary.
All GH anta$onists except Pegvisomant act centrally to bloc& GH secretion.
''Soatostatin (S!)F* is used to reduce GH secretion by GH'producin$ tuors.
''+ctreotide (Sandostatin* is a somatostatin analogue with longer half life. )t norali,es )GF'- in
./0 o% patients. Side e%%ects include gallstones and G) syptos.
''Caber$oline is a dopaine'li&e a$ent that norali,es )GF'- in 120 o% patients.
''Pegvisomant is a GH antagonist that prevents dimeriation of the GH receptor. Thus, it acts
peripherally to bloc& the action o% GH, rather than centrally to bloc& the synthesis o% GH.
This norali,es )GF'- in 3/0 o% patients.
(!ayond reo#ed ia$e sho4in$ pe$#isoant anta$oni,in$ GH'receptor dieri,ation.*
Reducing Prolactin secretion
Prolactin secretion is priarily under inhibitory control by dopamine.
Prolactinoas express the D1 dopaine receptor, so they are susceptible to inhibition by dopaine.
Dopainer$ic a$ents reduce prolactin synthesis/secretion as 4ell as shrin& prolactinoa tuors.
''5roocriptine non'selecti#ely binds D- and D1 receptors.
''Caber$oline selecti#ely binds D1 receptors, so it has %e4er side e%%ects.
''Per$olide non'selecti#ely binds D- and D1 receptors. )t treats Par&inson6s and prolactinoas.
Reducing Gonadotropin secretion
Gonadotropins contribute to precocious puberty, prostate cancer, and endoetriosis by boostin$
sex horone production. 5loc&in$ $onadotropins causes cheical castration.
Gonadotropins include LH and FSH, 4hich are secreted by the pituitary only in response to
pulsatile Gn!H stimulation" #ontinuous Gn!H stimulation down-regulates secretion$
''Leuprolide is a Gn!H analo$ue that causes cheical castration a%ter a transient rise in
$onadotropin le#els.
ADH pharmacology and the treatment of diabetes insipidus
''L'ar$inine #asopressin is 7ust noral ADH. )t has a short hal% li%e.
''Desopressin (dDA8P* is an %&H analogue with much longer half life and greater specificity.
)GF'-
Patients should experience polyuria each tie be%ore ta&in$ their next dose. This ensures
that the dDA8P has 4orn o%%, 4hich protects a$ainst overdose. +#erdose o% dDA8P
causes dan$erous euvolemic hyponatremia.