Hypothalamic and Pituitary Hormones DSA Flashcards
somatotropin
GH
octreotride
somatostatin analog
pegvisomant
GH antagonist
bromocriptin
dopamine agonist
cabergoline
dopamine agonist
vasopressin
ADH
desmopressin
vasopressin receptor agonist
neurons of posterior pituitary
supraoptic nuclei
paraventricular nuclei
synthesize arginine vasopressin or oxytocin
GH signaling
JAK/STAT
single chain proteins
PRL signaling
JAK/STAT
single chain proteins
thyrotropin
TSH
TSH signaling
GPCRs
dimeric proteins
FSH signaling
GPCRs
dimeric proteins
LH signaling
GPCRs
dimeric proteins
ACTH signaling
GPCRs
cleaved from precursor beta endorphin
single peptide
TSH release
regulated by TRH
LH and FSH release
regulated by GnRH
ACTH release
regulated by CRH
TSH and TRH release
negative feedback from T4 and T3
FSH, LH, and GnRH release
negative feedback from estrogen/progesterone (F) and androgens (M)
ACTH and CRH release
negative feedback from cortisol
GH release
stimulated by GHRH
inhibited by somatostatin
somatostatin
negative feedback on GH release
GH release
inhibited by GH and IGF-1
PRL release
negative feedback from dopamine via D2 receptors
disruption of hypothalamohypophysial portal vessels
increase PRL
decrease ACTH, GH, LH, FSH, TSH
target organ of GH
liver, muscle, bone, kidney
IFG-1 mediator
somatotropin
aka GH
ACTH target organ
adrenal cortex
glucocorticoid, mineralocorticoid, androgen release
GnRH release
endogenous - pulsatile - stimulates LH and FSH
continuously as drug - inhibit LH and FSH
somatropin
recombinant human form of rhGH
GH function
stimulates long bone growth
anabolic effects in muscle
catabolic effects in lipid cells
GH and IGF-1 on insulin
GH reduces insulin sensitivity
IGF-1 losers serum glucose and reduces insulin
GH deficiency in children
rhGH
-permits children with short stature to achieve normal height
GH deficiency in adults
generalized obesity, reduced muscle mass, asthenia, reduced cardiac output
tx with rhGH reverses many of these symptoms
GH treatment of kids with short stature
prader-willi
turner
noonan
idiopathic short stature
wasting in AIDS patients
GH tx
adverse effects of GH in kids
rare - intracranial HTN - vision changes, HA, N/V
scoliosis otitis media turner syndrome hypothyroidism pancreatitis gynecomastia
adverse effects of GH in adults
peripheral edema
myalgias
arthralgias
carpal tunnel syndrome
known active malignancy
contraindication for GH
mecasermin
recombinant IGF-1
in children with rare IGF-1 deficiency not responsive to GH - due to mutation in GH receptor
subQ admin**
adverse of mecasermin
hypoglycemia
so just eat before
anterior pituitary adenoma secreting GH
tx - GH antagonist
can cause acromegaly in adults and gigantism in children
MOA of pegvisoman
GH receptor antagonist
somatostatin analog MOA
suppression of GH secretion
dopamine receptor agonist
can be used to suppress GH secretion
somatostatin function
inhibit release of GH, TSH, glucagon, insulin, gastrin
octreotide
somatostatin analog
45x more potent than SST in inhibiting GH release and 2x as potent in reducing insulin secretion
octreotide admin
subQ
adverse effects of octreotide
N/V, abdominal cramping, flatulence steatorrhea bulky bowel movements gallstones cardiac effects vit B12 deficiency
lanreotide
SST analog
-approved for tx of acromegaly
pegvisomant MOA
GH receptor antagonist
tx of acromegaly
pegvisomant more effective than SST analogs
male hyperPRL
loss of libido and infertility
female hyperPRL
galactorrhea and amenorrhea
inhibition of PRL
dopamine agonists
hypogonadims and infertility with hyper PRL
result from inhibition of GnRH release
bromocriptin MOA
dopamine D2 receptor agonist
ergot derivative
cabergoline MOA
dopamine D2 receptor agonist
ergot derivative
cabergoline
dopamine agonist
longer half life, higher affinity, and greater selectivity for D2 receptors
lower incidence of side effects
pregnancy desired
bromocriptine preferred
as dopamine agonist
adverse of dopamine agonists
bromocriptine and cabergoline
nausea, HA, light headed, orthostatic HTN, fatigue
psych sx occasionally
macroadenoma during pregnancy continue
microadenoma during pregnancy stop therapy
postpartum lactation
do not recommend dopamine agonists
increased incidence of stroke and coronary thrombosis
oxytocin
stimulate uterine contraction
elicits milk ejection
differs from vasopressin at positions 3 and 8 out of 9 AA peptide
desmopressin
long acting synthetic analog of vasopressin
with minimal V1 receptor activity and an antidiuretic to pressor ratio 4000x that of vasopressin
vasopressin MOA
activate V1 and V2 receptors
-GPCRs
V1 - smooth muscle cells of vascular - vasoconstriction
V2 - renal tubules - increased water permeability in collecting tubule
extrarenal V2 - regulate release of coag factor VIII and vWF
pituitary diabetes insipidus tx
vasopressin and desmopressin
coagulopathy in hem A and vWF disease tx
desmopressin
vasopressin CIs
CAD - vasoconstriction
overdose of vasopressin
hyponatremia
-seizures
conivaptan
vasopressin antagoninst
tolvaptan
vasopressin antagonist
more selective for V2