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PHARM 3 > Hypothalamic/Pituitary Hormones > Flashcards

Hypothalamic/Pituitary Hormones Flashcards

1
Q

what receptors are activated by growth hormone

A

JAK/STAT superfamily

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2
Q

what receptors are activated by prolactin

A

JAK/STAT

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3
Q

what receptors are activated by TSH

A

GPCR

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4
Q

what receptors are activated by FSH

A

GPCR

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5
Q

what receptors are activated by LH

A

GPCR

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6
Q

what receptors are activated by ACTH

A

GPCR

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7
Q

what is the primary target of GHRH?

A

Growth hormone –> IGF-1 (mediates most of response)

acts on liver, muscle, bone, kidney

**notably also acts on some insulin receptors - causing insulin like effects

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8
Q

what are the effects of GH on GFR, insulin and adipocytes?

A

increase GFR

anti-insulin: decrease glucose utilization, inc lipolysis - receptors become unresponsive with long term use of GH d/t overproduction of insulin – NIDDM like state

stimulate pre-adipocyte differentiation into adipocytes

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9
Q

somatropin vs somatrem?

A

somatropin = recombinant GH

somatrem = GH analog

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10
Q

use of recombinant GH

A

peds patients with:

  • GH deficient
  • chronic renal failure
  • Noonan syndrome
  • Prader Wili
  • Turner
  • idiopathic short stature

GH deficient in adults
Wasting in HIV pt
Short bowel syndrome

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11
Q

Recombinant GH AE

A

scoliosis during rapid growth

  • hypothyroidism
  • intracranial HTN - fatal AE (can increase CSF production)
  • otitis media - in Turner pt
  • pancreatitis, gynecomastia, nevus growth
  • diabetic syndrome with chronic use

Adult AE:
- peripheral edema, myalgias, carpal tunnel syndrome

  • peripheral retinopathy
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12
Q

Recombinant GH contraindication

A

p450 inducer

pt with malignancy = may increase growth of tumor

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13
Q

Mecasermin

A

IGF-1 analog

recombinant IGF-1 and human IGF-binding protein 3

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14
Q

Mecasermin use

A

mutated GH-R, neutralizing GH antibodies

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15
Q

mecasermin AE

A

hypoglycemia - eat before/after to counter AE

intracranial HTN

elevated liver enzymes

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16
Q

treatment for GH secreting tumors

A

seen as acromegaly or gigantism (if occurs in childhood)

1) GH-r antagonist
2) somatostatin analog
3) dopamine-r agonist

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17
Q

Pegvisomant

A

GH-r antagonist

prevent dimerization of receptor - still allows for receptor binding

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18
Q

ocreotide

A

somatostatin analog

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19
Q

ocreotide MOA

A

inhibits release of GH, TSH, glucagon, insulin, gastrin

  • more potent than somatostatin**
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20
Q

ocreotide AE

A

n/v cramps, steatorrhea

constipation

biliary sludge/gallstones

bradycardia

B12 deficiency - w/long term use

pain at injection site

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21
Q

bromocriptine

A

dopamine agonist

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22
Q

cabergoline

A

dopamine agonist

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23
Q

use of bromocriptine/cabergoline

A

adenomas that secrete excess prolactin

*oral/vaginal insert

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24
Q

bromocriptine/cabergoine use

A

hyperprolactinemia

acromegaly

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25
Q

bromocriptine/cabergoline aE

A

nausea, headache, lightheadedness, orthostatic hypotension
(bromocriptine»cabergoline)

psych manifestations

high dose - cold induced peripheral vasospasms

pulmonary infiltrates with high dosage

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26
Q

use of gonadotrophins

A

infertility – stimulate spermatogenesis or induce ovulation

27
Q

menotropins

A

hMG = purified extract of FSH and LH

28
Q

follitropin

A

recombinant FSH

29
Q

urofollitropin

A

uFSH = purified human FSH extract

30
Q

choriogonadotropin alpha

A

(rhCG) recombinant hCG given SC

31
Q

gonadotropin MOA

A

act through GPCRs

32
Q

tx male infertility

A

FSH and LH both required if hypogonadal

hCG alone

urofollitropin, rFSH, rLH

33
Q

AE gonadotropins

A

ovarian hyperstimulation

multiple pregnancies

headache, depression, precocious puberty

male – gynecomastia

34
Q

gonadorelin

A

gonadotropin releasing hormone synthetic

35
Q

goserelin

A

GnRH analog - (more potent than gonadorelin)

36
Q

leuprolide

A

GnRH analog(more potent than gonadorelin)

37
Q

nafarelin

A

GnRH analog(more potent than gonadorelin)

38
Q

pulsatile vs sustained nonpulsatile administration of GnRH analogs

A

pulsatile = required to stimulate LH and FSH release

nonpulsatile = inhibits FSH and LH release – leads to hypogonadism

39
Q

GnRH analog use

A

suppression =
controlled ovarian hyperstimulation - suppress endogenous LH surge

endometriosis = reducing exposure to cyclical changes in estrogen and progesterone

uterine fibroids

prostate cancer

precocious puberty

adv breast/ovarian cancer
tx amenorrhea, PCOD
thinning of endometrial lining (pre-op endometrial ablation)

stimulation =
female/male infertility
diagnosis of LH responsiveness

40
Q

gonadorelin AE

A

hypersensitivity
pituitary apoplexiy and blindness
headache, light headed ness

41
Q

GnRH analog AE

A

menopausal sxs
depression
diminshed libido
vaginal dyrness

contraindicated in pregnant and breast feeding women

men: hot flushes, sweats, gyenocmastia, decreased hematocrit

42
Q

cetrorelix

A

competitive antagonist of GnRH receptors

43
Q

ganirelix

A

competitive antagonist of GnRH receptor

44
Q

GnRH receptor antagonist use

A

suppress gonadotropin production = prevent LH surge during controleld ovarian hyperstimulation

45
Q

corticotropin

A

ACTH analog

46
Q

cosyntropin

A

ACTH analog

47
Q

ACTH analog MOA

A

act via MC2r (inc cAMP) stimulate adrenal cortex = release glucocorticoids and androgen precursors

ACTH released from pituitary in pulses - highest in am, lowest in pm

cortisol suppresses release

48
Q

ACTH use

A

differentiate between primary and secondary insufficiency

infantile spasm/West Syndrome treatment

49
Q

ACTH AE

A

glucocorticoids

50
Q

Oxytocin low dose vs high dose

A

low dose: increases force, frequency of contractions

high dose: sustained contractions, weak antidiuretic and pressor activity

contraction of myoepithelial cells surrounding mammary alveoli = milk ejection

51
Q

oxytocin IV vs IM use

A

IV: intitiation and augmentation of labor

IM: post partum bleeding

52
Q

oxytocin clinical application

A

1) labor induction
2) augment normal labor
3) control uterine hemorrhage

53
Q

oxytocin AE

A

excessive uterine contraction stimulation

activation of vasopressin receptors

if bolus administration = hypotension

54
Q

oxytocin contraindications

A

fetal distress, premature
abnormal fetal presentation
uterine rupture predisposition

55
Q

atosiban

A

oxytocin antagonist

56
Q

atosiban use

A

pre-term labor = not used in US

57
Q

Vasopressin

A

ADH agonist

58
Q

Desmopressin

A

ADH agonist
long acting synthetic analog of vasopression

minimal V1 activity

59
Q

Vasopressin PD/PK

A

2 receptos activated

V1R = vascular SM = vasoconstriction
V2R = renal tubule cells = inc water permeability, water reabsorption

shorter t 1/2 with vasopressin rather than desmopressin

60
Q

Vasopressin use

A

diabetes insipidis
esophagal varice bleeding
colonic diverticular bleeding

61
Q

desmopressin use

A

coagulapathy in hemophilia A and vWB disease

62
Q

vasopressin AE

A

overdosage = hyponatremia, seizures

63
Q

conivaptan

A

vasopressin antagonist

used in pt with hyponatremia d/t elevated vasopressin

high affinity for V1, V2

PHARM 3 (21 decks)

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