Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
72 Cards in this Set
- Front
- Back
|
What are two examples of somatotropon agonists?
|
serostim
genotropin |
|
|
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?
|
hypoglycemia
|
|
|
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 arthralgia myalgia 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)
|
GH
serotonin gastrin VIP motilin |
|
|
what are 3 short term adverse effects of somatostatin?
|
nausea
diarrhea bloating |
|
|
what are 2 long term adverse effects of somatostatin?
|
gallstones
hypo-/hyperglycemia |
|
|
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?
|
gonadorelin
gosrelin nafarelin |
|
|
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)
|
IM
Sub-q 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
endometriosis precocious puberty |
|
|
what are GnRH agonists contraindicated in in women? (2)
|
pregnancy
breast feeding |
|
|
what are 4 adverse side effects of GnRH agonists in women?
|
headache/nausea
light headedness menopause-like symptoms reduced bone density |
|
|
what are 5 adverse side effects of GnRH agonists in men?
|
hot flashes
edema gynecomastia decreased libido decreased bone density |
|
|
what are 2 examples of GnRH antagonists?
|
ganirelix
centrorelix |
|
|
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?
|
nausea
headache 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?
|
urofollitropin
|
|
|
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?
|
propasi
pregnyl |
|
|
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 seizure death |
|
|
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
arrythmias MI peripheral ischemia |
|
|
what are 4 uses for vasopresin?
|
polyuria/polydipsea
hypernatremia 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
|
