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Pharmacology > Endocrine Pharmacology: Hypothalamus & Pituitary > Flashcards

Endocrine Pharmacology: Hypothalamus & Pituitary Flashcards

1
Q

What stucture of the hypothalamus secretes ADH (vasopressin) and oxytocin?

A

Supraooptic and paraventricular nuclei

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2
Q

What are the hormones released by the anterior pituitary gland?

A

TSH, ACTH, FSH, LH, GH, PRL

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3
Q

What are the hormones released by the posterior pituitary gland?

A

Oxytocin & Vasopressin (ADH)

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4
Q

What is the receptor of GH & PRL?

A

JAK/STAT

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5
Q

What is the receptor of GHRH, TSH, FASH, LH, ACTH, & Vasopressin?

A

Gs

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6
Q

What is receptor of Dopamine, SST?

A

Gi-coupled GPCRs

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7
Q

What is the receptor of GnRH, Ocytocin & Vasopressin 1A&B?

A

Gq coupled GPCRs

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8
Q

How are we able to diagnose GH deficiency? Explain

A

Injecting exogenou GH into the body. If GH levels increase (Hypothalamic disorder), GH levels remain low (anterior pituitary problem)

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9
Q

How would you describe Peptide hormones?

A

unbound in the plasma, receptor is at the cell membrane (lipophobic), fast onset of effects

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10
Q

What are the different peptide hormones?

A

Pituitary hormones, hypothalamic releasinghormones, Insulin, Glucagon, Calcitonin, PTH

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11
Q

How would you describe steroid hormones?

A

Protein-bound in plasma, receptors are in the cytoplasm (lipophilic), slow onset of effects

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12
Q

How would you describe AA derivatives of hormones that function like steroids?

A

Protein-bound, receptor is at the nucleus (lipophilic), and slow onset of effects

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13
Q

What are examples of AA derived hormones that act like steroids?

A

T3, T4

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14
Q

How would you describe AA derived hormones that function like peptides?

A

Unbound in plasma, receptor is at the cell membrane (lipophobic), and fast onset of effects

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15
Q

What are the diff hormones derived from AA and function like peptides?

A

Dopamine, Epinephrine & NRE

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16
Q

What classification of drugs are used to tx giganistism & dwarfism?

A

GH & GH regulators

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17
Q

What are the 4 GH regulators?

A

Somatostatin, GH, Mecasermin, & Pegivosomant

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18
Q

What is a GH-inhibiting hormones from the hypothalamust that inhibits Gastrin release from G cels & histamine release from enterochromaffin cells?

A

Somatostatin

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19
Q

What cells secrete Somatostatin?

A

D cells of the pancrease & D cells of the GI tract

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20
Q

What is the effect of Somatostain releae?

A

Inhibition of GH, TSH, Insulin, Glucagon, Gastrin & Other GI hormone release

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21
Q

What are the 2 SST analogs and which of them has less side efefcts, longer DOA, more potent & has less rebound hypersecretion?

A

2 Analogs: Octreotide & Lanretoide
Which of them: Octreotide

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22
Q

What conditions are SST analogs used for?

A

Acromegaly, Giganitism, Hormone-secreting tumors & Bleeding esophageal varices

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23
Q

What is a significant AE of SST analogs?

A

Gallstone

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24
Q

What are the direct & indirect effects of GH?

A

DIrect effects: INC lipolysis & blood sugar + anti-insulin effects
Indirect effects: Skeletal growth, INC cell proliferation, INC protein anabolism

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25
Q

What is the only preparation of GH?

A

Somatropin

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26
Q

What are the therapeutic uses of Somatropin?

A

GH deficient children & adults (Prader-Willi syndromes, CKD in pedia px, SGA babies <2yo)

Non-GH deficient/Idiopathic short stature children

Wasting in AIDS px

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27
Q

What are the AE of Somatropin?

A

Children (rare): Intracranial HPN, Scoliosis & Hypothyroidism

adults: Peripheral edema, MYALAGIA, ARTHRALGIA

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28
Q

What GH agonist is used for children unresponsive to GH therapy and stimulates skeletal muscle growth, AA transpo, protein synthesis, & cell proliferation?
What is a significant AE of this drug?

A

Mecasermin

Hypoglycemia

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29
Q

What is a GH receptor antagonist blocks peripheral effects of GH causing DEC of IGF-1 used for patients w/ Acromegaly who are unresponsive to Somatostatin analogs?

What is a common AE in Pegvisomant?

A

Pegvisomant

CHange in liver function test

30
Q

What is the main use of drugs that antagonize or mimic gonadostropins?

A

Infertility

31
Q

What is the physiologic process of GnRH release from the hypothalamus?

A

Controls the release and synthesis of FSH & LH

32
Q

What determines the effect of GnRH analogs? How so?

A

On how they are administered

If administered in pulsatile matter —> stimulates synthesis and release of Gonadotropin —> mimics physiologic release of GnRH

If administered continuously —> inhibits synthesis & release of Gonadotropin

33
Q

What are the therapeutic uses of GnRH analogs?

A

Pituitary stimulation
Suppression of Gonadotropins

34
Q

In what conditions do we use GnRH analogs?

A

Hypogonadotropic hypogonadism —> male/female infertility

Initiate ovulation in Assisted Reproductive Technology procedures —> triggers ovulation

35
Q

In what conditions are GnRH analogs used for suppression of Gonadotropins?

A

Endometriosis
Central precocious puberty
Prostatic/Breast cancer & Uterine Leiomyoma
Assisted Reproductive Technology
Early pubertal transgender adolescents

36
Q

How do GnRH analogs affect ART to suppress Gonadotropins?

A

Inhibition of endogenou LH surge to prevent premature ovulation —> DEC ART cycle cancellation rates —> INC pregnancy rates

37
Q

What are the diff preparations of GnRH analogs?

A

-relin = “release”
LeuproRELIN - PH available
GosereRELIN - PH available
TriptoRELIN
NafaRELIN

38
Q

What is the common AE of GnRH analogs?

A

Biphasic response

39
Q

What is the MOA of GnRH antagonist?

A

Directly blocks GnRH receptors in the APG preventing effects of endogenou GnRH

40
Q

What are the preparations of GnRH antagonists?

A

-relix = “antagonize”
CetroRELIX
GaniRELIX
DegaRELIX

41
Q

For what are GnRH antagonists used for?

A

To suppress secretion of Gonadotropin
Female infertility, Adv prostate cancer, & Endometriosis

42
Q

What drugs are used for advanced prostate cancer , Female infertility, & Endometriosis?

A

-x = “antagonize”

Elagolix - Endometriosis
Abarelix & Degarelix = Advanced prostate cancer
Ganirelix & Cetrorelix = Suppress LH surge that can prematurely trigger ovulation —> tx female infertility

43
Q

What is the most common AE of GnRH antagonist?

A

Nausea & headache
Estrogen/Androgen-deprivation: Hot flash, sweats, depression, decreased libido

44
Q

What are the functions of FSH?

A

Stimulates gamotegenesis
Stimulates steroid production —> Estradiol & Testosterone production

45
Q

What are the functions of LH?

A

Regulation of gonadal steroid hormone production

46
Q

What gonadotropic hormone stimulates ovarian corpus lutem to produce progesterone —> maintains placenta?

A

HCG

47
Q

Where is hCG secreted from?

A

Synctiotrophobalts from the placenta

48
Q

What are the diff preparations of FSH?

A

-pin
MentroPIN - postmenopausal women
UrofollitroPIN - taken from urine of postmeonopausal women
RFSH - purified recombinant form of FSH

49
Q

What are the pure preparations of LH used as LH analogs?

A

HCG
RhCG
RLH/Lutropin

50
Q

What are the different uses of Gonadotropin hormone analogs?

A

Female infertility
Male infertility
Cryptorchidism - undescended testes of a boy

51
Q

What type of male infertility disorders cause the need for Gonadotropin hormone analogs?

A

HYPERgonadotropic/Primary Hypogonadism
HYPOgonadotrpoic/Secondary Hypogonadism

52
Q

What are the AEs of Gonadotropin hormone analogs?

A

Multiple pregnancies
Ovarian Hyperstimulation
Headache & Depression
Gycenomastia

53
Q

What happens during assisted reproductive technology? Explain the process.

A
  1. Start w/ FSH preparation —> stimualte folicular growth and steroidal genesis
  2. LH may be added especially in hypogonadotropic women for adequate estrogen production
  3. Follicles grow —> Estrogen production INC —> Premature ovulation —> GnRH agonist/antagonist given —> Harvest egg at proper time

If GnRH agonist —> start early before start of FSH tx bcos of initial rise in Gn secretion

If GnRH antagonist —> start on Day 7 —> immediate effects

  1. Follicular #s and size monitors through ultrasound —> ideal size obtained —> LH prep (hCG) given —> final oocyte maturation —> Progesterone given (improved uterine receptivity)
  2. Egg retrieval after 34-46hrs —> eggs are incubated w/ sperm —> embryo egg is inserted to uterine cavity
54
Q

What are the diff dopamine agonists?

A

BromocriptINE (Parlodel) —> most improtant

Carbergoline
Quinagolide

55
Q

What is the MOA of dopamine agonists?

A

Diba Dopamine inhibits PRL? Sooo….

It inhibts PRL release from the anterior pituitary gland

Acts on D2 receptors

56
Q

What are the therapeutic uses for Dopamine agonists?

A

Hyperprolactinemia
Inhibit physiologic lactation
Parkinsons’ disease
Acromegaly
Diabetes

57
Q

What are the preparations of Dopamine agonists and which drug is improtant for a specific condition?

A

Bromocription & Cabergoline

Bromocriptione - postpartum women who do not intend to breastfeed

58
Q

What is the stimulus for Oxytocin & what are its effects?

A

Stimulus: Infant suckling & Cervical dilation

Effects:
- Uterine contraction
- Milk ejection (lactating women)
- Weak antidiuretic @ high concentrations

59
Q

What are the therapeutic uses of Oxytocin?

A

Ocytocin challenge test/Contraction stress test
Induce labor
Augment uterine contractions
Prevent/Tx Postpartum hemorrhage
Not really used for impaired milk ejection

60
Q

What is the preparation of Oxytocin?

A

Demoxytocin (IV/IM)

61
Q

What are the AEs of Oxytocin administration?

A

Uterine rupture
Fetal death
Abruptio placentae —> premature separation of the placenta, compromising fetal blood supply
Hypotension in bolus doses

62
Q

What are the C/Is of Oxytocin?

A

Fetal distress
Prematurity
Cephalopelic disproportion
Abnormal fetal presentation
Placental abruption worsens the condition
Predisposition to uterine rupture

63
Q

What are the uses for Oxytocin antagonist?

A

Tocolysis in preterm labor
Relax uterine muscles —> delayed labor

64
Q

What is the preparation of Oxytocin antagonist?

A

Atosiban (Tractocile)

65
Q

In what condition can we secrete ADH/Vasopressin?

A

If INC plasma tonicity, LOW BP —> INC ADH —> antidiuresis, H2O retention —> INC BP

66
Q

What are the 2 types of Vasopressin/ADH receptors?

A

V1 (Gq) - vascular smooth muscles —> vasoconstriction
V2 (Gs) - acts in renal tubule cells —> free H2O reabsoription in CTs

67
Q

What are the types of preparation of Vasopressin? Which of those 2 is long-acting?

A

Desmopressin (oral) —> LONG ACTING
Vasopressin (Parenteral)

68
Q

What are the therapeutic uses of Vasopressin?

A

Diabetes insipidus
Noctorunal enuresis
Hemophilia A, vWD
Bleeding esophageal varices

69
Q

What are the common AE of vasopressin & its C/I?

A

GIT disturbance, headache, overdose,

C/I: px w/ CAD

70
Q

What are the 2 Vasopressin antagonist?

A

ConiVAPTAN
TolVAPTAN

71
Q

What is the therapeutic use of Conivaptan? AE? C/I?

A

Use: Hypervolemic/Euvolemic hyponatremia (hospitalized px)

AE: Orthostatic hypotension

C/I: Hypovolemic hyponatremia

Produces water diuresis

72
Q

What are the uses, AEs, & C/Is of Tolvaptan?

A

Uses:
- HF when other diuretics don’t work
- Hypervolemic/Euvolemic hyponatrmia
- SIADH

AEs: Thirst, dry mouth, nausea, polyuria, Liver toxicity

C/I: Liver disease

Pharmacology (19 decks)

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