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83 Cards in this Set

  • Front
  • Back
what system synchronizes body fxns by conveying messages b/w specific tissues and cells?
the neuroendocrine system
what is the neuroendocrine system regulated by?
the hypothalamus and pituitary
what is the difference in time b/w genomic and non genomic effects?
genomic takes hours to days
while
non genomic takes seconds
what is the neuroendocrine systemis responsible for controlling in the body?
*growth
*metabolism
*reproduction
what horomones are made in the hypothalamus and then transported to post pituitary?
vasopressin and oxytocin
what are most hypothalamic hormones made of?
small proterins (peptides)
how do hypothalamic hormones and pituitary hormones exhibit there effects?
through a specific membrane receptor
what controls the sythesis and release of ant. pit hormones?
the hypothtalmaic releasing or inhibitng hormones
what are the hypothalamic regulatory hormones largely used for in medicine?
as diagnostic tools to deteremine different states of pituitary insufficiency
what are the pituitary hormone preparations used clinically for?
as replacement therapy for certain hormone deficient states and in treatment of certain hormorn related disorders
what is the only hypothalamicor pituitary hormone that is NOT a peptide
dopamine
how does being a peptide influence the method of administration?
they must be administered either sub q or intramuscularly or intranasally since they are rapidly degraded within the GI tract
describe the receptors for growth hormone and prolactin

what does hormone binding to these receptors cause?
they are similar single transmembrane peptides

binding activates an intracellular tyrosine kinase (JAK2) that causes phosphoyrlation of intracellular proteins thereby influencing gene regulation
what are all other hypothalamic and pituitary hormone receptors like? (not GH or prolactin)

what is activated
seven transmembrane domain serpentine peptides involved in the activation of G proteins
what does the activation of G proteins lead to?
*activation of adenylyl cyclase
*synthesis of cAMP,
*activation of protein kinases
*phosphorylation of intracellular proteins such as enzymes
what are the hypothalamic hormones?
1. Growth hormone releasing hormone-GHRH
2. Somatostatin (somatrotropin release inhibiting hormone)
3. Thyrotropin releasing hormone-TRH
4. Corticotropin releasing hormone (CRH)
5. GOnadotropin releasing hormone (GnRH or LHRH)
6. Dopamine(prolactin inhibiting hormone)
7. Oxytocin
8. Vasopressin
what is the natrual GHRH?

what is the synthetic?

how are these administered?
somatorelin is natural

sermorelin is synthetic

iv, sc, nasally
what is the clinical use of somatorelin/sermorelin?

what are adverse effects?
the cause of GH deficiency and to promote GH releease in GH deficient kids

facial flushing, injection pain, HA, n/v
what is does TRH do?

how many peptides is it?

what regulates the release or TRH
stimulates TSH from ant pituit. and also increases prolactin release

it is a tripeptide

it is regulated by thyroxine
what is the drug used as TSH?

what is it's clinical usefulness?

what are adverse effects?
Protirelin is drug

administered IV but rarely used in dx of hypo/hyper thyroid states

effects include nausea, flushign, light headed
what does CRH stimulate?

what is the drug used?
CRH stimulates ACTH and beta endorphin secretion from ant. pituitary

(ACTH leads to production of cortisol and androgens by adrneal cortex)

the drugs used is corticorelin
what is the clinical use of corticorelin

(hint: CRH)
diff. dx of Cushing syndrome and other adrenal disorders

*cushings has high levels of cortisol usually due to pituitary tumor

*adrenal disorders have ectopic secretion of cortisol (usually in lung
will acth release increase following CRH stimulation in is cause of excess cortisol is from nonpit tumor?


will ACTH increase if excess is due to pit. tumor (cushings)
NO


YES w/ cushings there is no neg feedback to pituitary
how is corticorelin administered and waht are side effects?
IV, facial flushing, midl dyspena and hypotension
what does gonadotropin releasing hormone stimulate?

what is natural drug used clinically?
GnRH stim. Gonadotropins from ant pit. (LH and FSH)

drug used clinically is Gonadorelin
why is gonadorelin administered in pulsatile doses and not continuously



what are clinical uses?
pulsed doses resemble physiologic cycle. if given continuously then then gonadotropin release is actually inhibited


clinical uses include infertility, amenorrhea, delayued puberty and cryptorchidism due to 1st degree hypothalamic hypogonadism
what are the GnRH analongs?
*Leuprolide
*Nafarelin(synarel)
*Histrelin
*Goserelin
*Triptorelin
how doe the GnRH analogs compare to gonadorelin in terms of potency and time of action?
they are more potent and longer acting
what are some clinical uses for the GnRH analogs?

(hint: they are administered conintuously)
continuous inhibition inhibits relase of LH and FSH from pit.

this suppression can be used to tx prostatic carcinoma, breast cancer in premenopausal females, ovarian cancer, uterine fibroids, endometriosis, precocious puberty, mastalgia and hirsutism

also in femles undergoing controlled ovarian hyperstim and in assisted reproduction tech
what are the GnRH adverese effects?
OSTEOPOROSIS, sweats, hot flashes, HA, depression, decresed libido and vag dryness
what are the GnRH antagonists?

what do they inhibit

what is the clinical use?
Cetrorelix and Ganirelix

they inhibit LH

clinically they inhibit premature LH surges in females undergoin CONTROLLED OVARIAN HYPERSTIM
what is the other name for Somatostatin release Inhibitng hormone?

why is somatostatin clinically worthless?
also called GH inhibiting hormone.

*also inhibits insulin

it is cliniclally worthelss due to the really short half life
what is the clinically used Somatostatin?

what is this drug used to tx?

what is the major adverse effect
Octreotide***(Sandostatin, Sandostatin LAR DEPOT)

used to treat:
-acromegaly
-carcinoid tumor
-bleeding due to esophageal varices

*DOES NOT provoke hyperglycemia

adverse effect is biliary disorders suc =ha s gallstones and bile sludge
what is is the prolactin inhibiting horomone?

why is this not a practical managment for hyper prolactinemia?
dopamine

is not practical b/c of it's peripheral actions and requirements of parenteral administration
what are the drugs used clinically that are D2 receptor agonists?

how are these drugs administered?
Bromocriptine and Cabergoline

administered PO
what are bromocriptine and cabergoline used to tx?
HYPERPROLACTINEMIA due to galactorrhea, amenorrhea, hypogonadism,infertility and breast tenderness

also tx prolactin secreting adenomas (prolactinomas)
what are drugs that can cause hyperprolactinemia (b/c they are D2 receptor antagonists)
older antipsychotic drugs such as phenothoazine and haloperidol

also drugs that deplete CNAS amine NT's such as RESERPINE
what are the anterior pituitary hormones
1. GH
2. TSH
3. Adrenocorticotropin ACTH
4. FSH
5, LH
6. Menotropins
7. Prolactin
what is the naturally occuring GH?

what are the synthetic?
Somatotropin is natural

Somatrem and Somatropin are synthetic
what is the mech of action of GH?


what is the target organ
Gh stimulates sythesis and relese of SOMATOMEDINS and promote cell proliferation, bone growth and cartilage synthesis

they also induce an insulin like effect followed by a peripheral insulin antagonistic effect

liver is target organ
what are the synthetic GH's (Somatrem and Somatropin) used clinically for?
tx GH deficiency

*hypopituitary dwarfism
*turners syndrome
*Prader-willi syndrome (short stature)
*AIDS assoc wasting/cachexia
what are the adverse effects and contraindications of Somatrem and somatropin?
adverse=intracranial HTN, pancreatitis, gynecomastia and myalgia

contraindicated in kids with closed epiphysis
what are two newer drugs used to tx GH failure, GH gene deletion or primary IGF-1 deficiency?

which is better and Y
Inrelex and Iplex

Iplex is better b/c is only needs to be administered once a day
what are adverse effects of iplex and increlex?
HYPOGLYCEMIA (less w/ iplex)
what is a GH antagonist?

wat is is used to tx?

what are adverse effects?
GH antagonist is Somavert

used to tx acromegaly

adverse is elevated hepatic enzymes
what is the natural thyroid stim horm drugs?

what is target organ

what does it regulate?

what is the release of this drug inhibited by
thyrotropin is naturally occuring glycoprotein hormone

target organ is thyroid

it regulates the thyroid fxn by stimulating adenlyl clclsae and prod of cAMP

it also increases iodine uptkae intho thyroid to controll sythesis and release of thyroid hormones T4 and T3
what is the main thyroid hormone? T3 or T4
T4 is main
what is the clinical use of thyrotropin?
as a diagnostic tool b/w primary and secondary hypothyroidism
if you give someon thyrotorpin and there is no effect on thyroid hormone release what does this indicate?
primary hypothyroidism due to hypothyroid glad itself not working
if you give thyrotropin and thryoid hormone increses what does this indicate?
it indicates secondary hypothyroidism due to pit not releasing TSH
what is thyrotropin alph used for?
a diagnostic tool for determining the recurrency of thryoid carcinoma
when is TSH (thyrotropin) contraindicated?
if person hs heart dz or adrenocortical insufficiency
what is target organ of ACTH?

what is teh mechanism of action?

what is the rate limiting step of adrneocorticoid sythsis?
the adrenal cortex

this peptid ehromone regulates release of glucorcorticoids and mineralocorticoids and androgens through the G protein/cAMP mechanism

cholesterol esterase
what are the ACTH drugs?

what is the clinical use?
*corticotropin-natural
*cosyntroprin is synthetic

COSYNTROPIN used to distinguish primary and secondary addison's dz
if cosyntropin is given and there is no effect on corticosteroid release what does this indicate?
that this is primary addison's due to adrenal gland not producing
if you give cosyntropin and there is increased relesae of corticosteroid what does this indicate?
that the pituitary is not making ACTH and is secondary Addison's disease
what what is the target organ of FSH?

what does is mechanism of action

what does it cause in females?

what does it cause in males?
gonads


Controls gonadal fxn through cAMP


females=gametogenesis and foliclar maturation

males=spermatogenesis
what are adverse effectes of FSH drugs?
females=ovarian enlargment

males=gynecomastia
what other hormone does FSH work with?
LH
what FSH drug is extracted from urine of postmenopausal women?

which FSH drugs are made through recom DNA?

what are the FSH drugs used to tx clinically?
from urin=Urofollitropin

from DNA=Follitropin alfa and beta

tx infertility
what is LH a major stimulant of?

what is the target organ?
major stimulant of gonadal steroid biosynthesis

target organ is gonads
what effect does LH have in females

in males?
in females reulates follicular development and induces ovulation, sythesis of pregesterone and androgens in corpus luteum

in males promotes biosythesis of testosterone
what are the three drugs used as clinical LH?
1. hCG(Pregnyl and Novarel)

2. hCG alfa (Ovidrel)

3. Lutropin alfa (Luveris)
what are the hCG's and Lutropin used to tx?
1. hypogonadism
2. infertility
3. cryptorchidism
what are adverse effects?

what are contraindications?
adverse=ovarian enlargement, gynecomastia, Prostate cancer

contraindicated in presence of adnrogen dependent neoplasms
what are menotropins?

where are they acquired from?

what is effect in males?

in females?
menotropins are partly degreaded FSH and LH

acquired from postmenopausal women

females=promote follicular growth and maturation

males=spermatogenesis
what are menotropin drugs used clinically?

what do they treat?

what are adverse effects?
drugs are Repronex and Menopur

treat infertility

adverse effects are ovarian enlargement and gynecomastia
what is prolactin responsible for?

what is target organ?

what can a deficiency of prolactin cause?

is there any current therapy for prolactin deficient patients?
primary hormone of lactation

target organ is breast

deficiency can cause hyporprolactinemia

NO
what can hyperprolactinemia lead to?

what is secretion of prolactin inhibited by?
galactorrhea and hyopgonadism

dopamine(dopamine blockers can cause hyperprolactinemia)
what are the Prolactin inhibiting drugs?

which is better?

what receptor do these drugs act on?

what are the active derivatives?
Bromocriptine and Cabergoline

Cabergoline is better b/c fewer side effects

act on dopamine D2 agonists

orally active ergot derivatives
what are clinical uses of bromocriptine and cabegoline?


which of these two drugs in not a hormone?
tx hyperprolactinemia and its manifestations

tx prolactin secreting adenomas, acromegaly and parkinsons

bromocriptine
what are the post pituitary drugs?
1. Vasopressin
2. Desmopressin
3. Oxytocin
how are post pit drugs administered?
parenterally since they aren'te peptides
what is vasopressin?

what does a deficiency result in?

what causes a release of vasopressen?
it is ADH, nonapeptide hormone

deficiency results in diabetes insipidis

released due to incresed plamsa tonicity or decreased blood pressure
what is synthetic ADH?

what effects does this drug exhibit
ARGIPRESSIN

exhibits both antidiureticV2 and vasopressor V1 effects
what are the the three types or receptrs and resulting effects that argipressin activates?
1. renal V2=increased water permeability in kidney

2. extrarenal V2=von willebrand factor and coag factor VIII release

3. V1 receptr=vascular smooth muscle vasoconstriction
what is the clinical use of argipressin?

what are contraindications?
tx pituitary diabetes insipidus

control bleeding from esophageal varices and colonic divertiula

C/I=CAD (b/c hyponatremia and vasoconstrtiction)

asthma(b/c bronchoconstriciton

and

epilepsy b/c tremor, hyponatrmia, water intoxication
what is a a vasopressin antagonist?

what are clinical uses?

what is adverse effect?
conivaptan

tx hyponatrmic states and SIADH

adverse effect in hypernatremia
what is desmopressing?

what are drug names?
desmopressin is a selective V2 receptor agonist that is a long acting synthetic VASOPRESSIN DERIV

drugs are DDAVP, stimate and minirin

clinically used to tx von willebrand dz and doag wih hemophilia A

tx also diabetes insipidus and nocturnal enuresis
what are clinical used of DDAVP, Stimate, Minirin ?
1. pit diabetes insipidus

2. von Willebrand dz and coag assoc with hemophilia A

3. nocturnal enuresis (bedwetting)
what does oxytocin do?
promote milk ejection

stimulant of uterine contraction

initiate labor
what are clinical uses?
*induce labor
*reinforce mild let down and releif of post partum breast engorgement

*control postpartum and postaboraiton utrerin hemorrhage
*induce therapeutic abortion
what are adverse effects?
(HTN crisis

H2o retention

uterine rupture and fetal death