Hypothalamic and pituitary pharm Flashcards
Gs hormones
beta-adrenergic LH, FSH, TSH glucagon PTH, PTHrP ACTH GHRH, CRH histamine serotonin
Gi hormones
alpha-adrenergic Ach (muscarinic) opioids serotonin cannabinoid somatostatin
Gq hormones
TRH, GnRH
amines
peptides
protanoids
TK hormones
insulin and IGF-I
serine kinase hormones
TGF-beta
Gs
stimulates AC -> increased cAMP
Gi
inhibits AC -> decreased cAMP
opens cardiac K channels decreasing HR
Go
in brain
not fully understood
Gq
activates PLC -> increases ITP and DAG -> increases intracellular Ca
insulin receptor
TK dimerization -> MAP, PI3, RAS
cytokine receptor linked kinases
Jak/Stat
GH
PRL
Nuclear Rs
regulate gene transcription ( L activated TF)
steroid hormones (E, T, androgen, Progesterone, TH, retionic acid, vit D)
48 NRs in human genome
synthetic GH
somatropin
IGF-I agonist
mecasermin
somatostatin analogs
octreotide
lanreotide
GH antagonists
pegvisomant
dopamine agonists
bromocriptine
cabergoline
vasopressin R agonisits
vassopressin
desmopressin
vasopressin R antagonisits
conivaptan
tolvaptan
somatropin PD
growth mediated thru IGF-I
anabolic effects in mm
catabolic effects in lipids
mixed effects on CHO metabolism
somatropin uses
GH deficiency
pediatric patients with short stature (prader-willi, turners, noonan, idopathic short stature)
other uses of somatropin
chronic wasting in AIDs
short bowel syndrome
banned by olympic committee and professional sports
rBovine GH used in cattle
mecasermin
recombinant IGF-I
mecaasermin rinfabate includes binding protein to increase half-ife
uses of mecasermin
IGF-I deficiency not responsive to GH
children with GH gene deletions or who have developed AbS
most common adverse effect of mecasermin
hypoglycemia
somatostatin analogs
reduce secretion of GH
GHR antagonists
block action of GH at R
somatostatin
inhibits release of GH as well as glucagon, insulin, gastrin)
exogenous has very short duration of action
somatostatin analogs
more potent then somatostain at inhibiting GH and insulin secretion
somatostatin analog uses
Tx of ant pituitary adenomas that secrete GH (acromegaly, gigantism)
adverse effects of somatostatin analogs
nausea, vomiting, GI (steatorrhea, gallstones), cardiac (sinus bradycardia, conduction disturbances)
Pegvisomant MOA
GH R antagonist
more effective then somatostatin analogs
prolactin
direct action in target tissues via Jak/STAT
no preparations are available
D2R agonists can decrease endogenous production
D2R agonists
Gi
decrease prolactin secretion
D2R agonist uses
hyperprolactinemia
acromegaly
parkinson
adverse effects of D2R agonisits
nausea, HA, light headedness, orthostatic hypotension, fatigue
desmopressin
longer half life then vasopressin
uses of vasopressin
neurogenic DI
hemophilia A
vWD
uses of vasopressin antagonistis
hypervolemic or euvolemic hyponatremia