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72 Cards in this Set

  • Front
  • Back
What are two examples of somatotropon agonists?
What is the MOA of somatropin?
identical to native GH
exerts it effects directly on adipocytes and indirectly on anabolic and growth-promoting effects through increases in IGF-1 and tyrosine kinase family receptors
what is the clinical use for somatropin in children?
diagnosed deficiencies (often hypothalamic) usually seen as short stature and low age-adjusted velocity
what is the clincal use for somatropin in adults?
often pituitary defects associated with the CV system, bone, and psychological issues
also approved for AIDS associated wasting
what is protropin?
an example of somatrem, a GH with an additional methionine group at the amino terminus
what is sermorelin?
a GHRH agonist
what is geref?
a semorelin, a GHRH agonist
what is the MOA of semorelin?
corresponds to the first 29 amino acids of the secreted GHRH but is somewhat less effective than somatropin
what is the problem with semorelin?
it will not be effective in patients who have a defective GHRH receptor
what is increlex?
a recombinant IGF-1
what is mecasermin?
a recombinant IGF-1
what are recombinant IGF-1s used for? (2)
to treat patients with a mutation in the GH receptor
it will indirectly stimulate anabolic and growth-promoting effects through the increased synthesis of IGF-1
what is the main side effect of recombinant IGF-1?
what are 3 adverse side effects of growth hormones in children?
idiopathic intracranial htn
possible increased incidence of leukemia
too rapid growth can cause slipped epiphysis or scoliosis
what are 5 adverse effects of growth hormones in adults?
peripheral edema
carpal tunnel syndrome
increased incidence associated with increased age and/or obesity
what is ocreotide?
a somatostatin agonist
what is the moa of ocreotide?
synthetic octapeptide with actions similar to somatostatin but with a longer half life
selectively binds the 2 somatostatin and inhibits the secretion of numerous hormones including GH
what type of receptor does somatostatin use?
Gi GPCR that prevents the release of GH by decreasing cAMP and Ca++
what hormones does somatostatin inhibit? (5)
what are 3 short term adverse effects of somatostatin?
what are 2 long term adverse effects of somatostatin?
what is pegvisomant and what is an example of one?
a GH receptor antagonist
ex, somavert
What is the MOA of pegvisomant?
it is a mutant of the GH molecule that binds itself to the GH receptor dmer and include internalization without activating the receptor
does pegvisomant have direct or indirect actions?
both due to GH or IGF-1 receptor activation
when should pegvisomant not be used?
if transaminases are elevated so check for liver function
how is the prolactin receptor activated?
dimerization of two monomeric subunits promoted by prolactin leading to the activation of JAK-STAT signal transduction pathway
what are dopamine receptor agonists used for? (3)
prolactin-secreting adenomas
decreased dopamine release
renal failure
how do dopamine receptor agonists work?
usually used to stop the growth of prolactin secreting hormones by binding to D2 receptors (which are usually Gi coupled receptors) and prevent the release of prolactin-containing granules
what are 2 examples of dopamine receptor agonists?
bromocriptine (parlodel)
pergolide (permax)
what are 4 adverse effects of dopamine receptor agonists?
nausea (may be so bad people stop taking the drug)
postural hypotension due to vasodilatory effects on renal vascular beds
nasal congestion
CNS effects
what is Cabergoline?
a dopamine receptor agonist similar to bromocriptine but with a much lower tendency to cause nausea
what is dostinex?
cabergoline, a dopamine receptor agonist similar to bromocriptine but with a much lower tendency to cause nausea
what are 3 examples of GnRH agonists?
What effect do the modifications to GnRH agnosits have?
give them a longer half life than GnRh
What happens when GnRH is administered in a non-pulsatile manner?
LH and FSH are induced for the first 7-10 days (flare) and then subsequent administration will inhibit their release
what are GnRH agonists used most often for?
to suppress gonadotropin release
how can GnRH agnosist be administered? (3)
nasal spray
how are GnRH agonists used to stimulate female infertility?
to precipitate an LH surge and ovulation
how are GnRH agonists used to stimulate male infertility?
using pulsatile gondorelin
what are GnRH agonists used to inhibit? (3)
prostate cancer
precocious puberty
what are GnRH agonists contraindicated in in women? (2)
breast feeding
what are 4 adverse side effects of GnRH agonists in women?
light headedness
menopause-like symptoms
reduced bone density
what are 5 adverse side effects of GnRH agonists in men?
hot flashes
decreased libido
decreased bone density
what are 2 examples of GnRH antagonists?
what is the MOA of GnRH antagonists?
competitive antagonists used to prevent LH surge during ovarian hyperstimulation
what are 2 advantages of GnRH antagonists?
duration of admin is shorter
less negative impact on ovarian response to gonadotropin stimulation
what are 3 adverse effects of GnRH antagonists?
ovarian hyperstimulation syndrome (when used along with gonadotropins)
what is the MOA of LH agonists? (3)
increases androgen production and in combination with FSH enhances steroidogensis
if pregnancy occurs, LH controls estrogen and progesterone during the luteal phase to prevent the onset of menses
main stimulus for testosterone in men
what is Lutropin?
an LH agonist
how is lutropin to be used?
only for use with follitropin alpha for stimulation of follicular development in infertile women with profound LH deficiency
what does FSH do? (2)
directs ovarian follicle development and in combination with LH enhances steroidogenesis
primary regulator of steroidogenesis
what FSH agonists has been extracted from the urine of postmenopausal women?
what are 2 FSH agonists that are recombinant but have a shorter half life?
follitropin alpha and beta
what are 2 hCG agonists isolated from the urine of pregnant women?
what is a recombinant hCG?
choriogonadotropin alfa
what are 4 adverse effects of gonadotropins (LH, FSH, hCG)?
ovarian hyperstimulation
multiple pregnancies
complications in pregnancy
headache, depression, edema
where is oxytocin synthesized?
hypothalamus and transported via axons to the posterior pituitary
what type of receptor does oxytocin use?
Gq coupled GPCR
what happens when an oxytoxin receptor is activated? (3)
increase in intracellular Ca2+ which contracts the muscles of the myometrium
activated PLC which results in prostaglandins to further contraction
contraction of myoepithelial cells surrounding alveoli for milk ejection
what are the effects of oxytocin at higher concentrations?
vasopressor and antidiuretic effects
what is pitocin?
synthetic oxytocin used to induce labor and prevent bleeding post partum
what can pitocin toxicity cause? (3)
fetal distress
placental abruption
uterine rupture
what effect can pitocin have on blood pressure? (4)
vasopressin activation can lead to
fluid retention
heart failure
what does vasopressin activate? (2)
both Gq-coupled V1 receptors in the vasculature
Gs-coupled V2 receptor in the collecting tubules
what effect does vasopressin's V2-like receptor have?
activity at extrarenal sites regulates the release of coagulation factor VIII and von-wilebrand
what is desmopressin?
a long acting vasopressin analog
what receptors does desmopressin have the most effect at?
V2 where it leads to resoprtion of water in the collecting tubules
what is a side effect of both vasopressin and desmopressin?
abdominal cramping
what are 4 unique side effects of vasopressin (that desmopressin does not have)
increased BP
peripheral ischemia
what are 4 uses for vasopresin?
bedtime desmopressin for nocturnal enuresis
esophageal variceal bleeding
what is conivaptan?
a vasopressin antagonist that acts at the V1 and V2 receptors
what can conivaptan be used for?
treat hyponatremia associated with elevated levels of vasopressin