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Pharmacology > Endocrine Pharmacology: Hypothalamus & Pituitary > Flashcards

Endocrine Pharmacology: Hypothalamus & Pituitary Flashcards

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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
What is the only preparation of GH?
Somatropin
26
What are the therapeutic uses of Somatropin?
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
27
What are the AE of Somatropin?
Children (rare): Intracranial HPN, Scoliosis & Hypothyroidism adults: Peripheral edema, MYALAGIA, ARTHRALGIA
28
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?
Mecasermin Hypoglycemia
29
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?
Pegvisomant CHange in liver function test
30
What is the main use of drugs that antagonize or mimic gonadostropins?
Infertility
31
What is the physiologic process of GnRH release from the hypothalamus?
Controls the release and synthesis of FSH & LH
32
What determines the effect of GnRH analogs? How so?
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
What are the therapeutic uses of GnRH analogs?
Pituitary stimulation Suppression of Gonadotropins
34
In what conditions do we use GnRH analogs?
Hypogonadotropic hypogonadism —> male/female infertility Initiate ovulation in Assisted Reproductive Technology procedures —> triggers ovulation
35
In what conditions are GnRH analogs used for suppression of Gonadotropins?
Endometriosis Central precocious puberty Prostatic/Breast cancer & Uterine Leiomyoma Assisted Reproductive Technology Early pubertal transgender adolescents
36
How do GnRH analogs affect ART to suppress Gonadotropins?
Inhibition of endogenou LH surge to prevent premature ovulation —> DEC ART cycle cancellation rates —> INC pregnancy rates
37
What are the diff preparations of GnRH analogs?
-relin = “release” LeuproRELIN - PH available GosereRELIN - PH available TriptoRELIN NafaRELIN
38
What is the common AE of GnRH analogs?
Biphasic response
39
What is the MOA of GnRH antagonist?
Directly blocks GnRH receptors in the APG preventing effects of endogenou GnRH
40
What are the preparations of GnRH antagonists?
-relix = “antagonize” CetroRELIX GaniRELIX DegaRELIX
41
For what are GnRH antagonists used for?
To suppress secretion of Gonadotropin Female infertility, Adv prostate cancer, & Endometriosis
42
What drugs are used for advanced prostate cancer , Female infertility, & Endometriosis?
-x = “antagonize” Elagolix - Endometriosis Abarelix & Degarelix = Advanced prostate cancer Ganirelix & Cetrorelix = Suppress LH surge that can prematurely trigger ovulation —> tx female infertility
43
What is the most common AE of GnRH antagonist?
Nausea & headache Estrogen/Androgen-deprivation: Hot flash, sweats, depression, decreased libido
44
What are the functions of FSH?
Stimulates gamotegenesis Stimulates steroid production —> Estradiol & Testosterone production
45
What are the functions of LH?
Regulation of gonadal steroid hormone production
46
What gonadotropic hormone stimulates ovarian corpus lutem to produce progesterone —> maintains placenta?
HCG
47
Where is hCG secreted from?
Synctiotrophobalts from the placenta
48
What are the diff preparations of FSH?
-pin MentroPIN - postmenopausal women UrofollitroPIN - taken from urine of postmeonopausal women RFSH - purified recombinant form of FSH
49
What are the pure preparations of LH used as LH analogs?
HCG RhCG RLH/Lutropin
50
What are the different uses of Gonadotropin hormone analogs?
Female infertility Male infertility Cryptorchidism - undescended testes of a boy
51
What type of male infertility disorders cause the need for Gonadotropin hormone analogs?
HYPERgonadotropic/Primary Hypogonadism HYPOgonadotrpoic/Secondary Hypogonadism
52
What are the AEs of Gonadotropin hormone analogs?
Multiple pregnancies Ovarian Hyperstimulation Headache & Depression Gycenomastia
53
What happens during assisted reproductive technology? Explain the process.
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 4. Follicular #s and size monitors through ultrasound —> ideal size obtained —> LH prep (hCG) given —> final oocyte maturation —> Progesterone given (improved uterine receptivity) 5. Egg retrieval after 34-46hrs —> eggs are incubated w/ sperm —> embryo egg is inserted to uterine cavity
54
What are the diff dopamine agonists?
BromocriptINE (Parlodel) —> most improtant Carbergoline Quinagolide
55
What is the MOA of dopamine agonists?
Diba Dopamine inhibits PRL? Sooo…. It inhibts PRL release from the anterior pituitary gland Acts on D2 receptors
56
What are the therapeutic uses for Dopamine agonists?
Hyperprolactinemia Inhibit physiologic lactation Parkinsons’ disease Acromegaly Diabetes
57
What are the preparations of Dopamine agonists and which drug is improtant for a specific condition?
Bromocription & Cabergoline Bromocriptione - postpartum women who do not intend to breastfeed
58
What is the stimulus for Oxytocin & what are its effects?
Stimulus: Infant suckling & Cervical dilation Effects: - Uterine contraction - Milk ejection (lactating women) - Weak antidiuretic @ high concentrations
59
What are the therapeutic uses of Oxytocin?
Ocytocin challenge test/Contraction stress test Induce labor Augment uterine contractions Prevent/Tx Postpartum hemorrhage Not really used for impaired milk ejection
60
What is the preparation of Oxytocin?
Demoxytocin (IV/IM)
61
What are the AEs of Oxytocin administration?
Uterine rupture Fetal death Abruptio placentae —> premature separation of the placenta, compromising fetal blood supply Hypotension in bolus doses
62
What are the C/Is of Oxytocin?
Fetal distress Prematurity Cephalopelic disproportion Abnormal fetal presentation Placental abruption worsens the condition Predisposition to uterine rupture
63
What are the uses for Oxytocin antagonist?
Tocolysis in preterm labor Relax uterine muscles —> delayed labor
64
What is the preparation of Oxytocin antagonist?
Atosiban (Tractocile)
65
In what condition can we secrete ADH/Vasopressin?
If INC plasma tonicity, LOW BP —> INC ADH —> antidiuresis, H2O retention —> INC BP
66
What are the 2 types of Vasopressin/ADH receptors?
V1 (Gq) - vascular smooth muscles —> vasoconstriction V2 (Gs) - acts in renal tubule cells —> free H2O reabsoription in CTs
67
What are the types of preparation of Vasopressin? Which of those 2 is long-acting?
Desmopressin (oral) —> LONG ACTING Vasopressin (Parenteral)
68
What are the therapeutic uses of Vasopressin?
Diabetes insipidus Noctorunal enuresis Hemophilia A, vWD Bleeding esophageal varices
69
What are the common AE of vasopressin & its C/I?
GIT disturbance, headache, overdose, C/I: px w/ CAD
70
What are the 2 Vasopressin antagonist?
ConiVAPTAN TolVAPTAN
71
What is the therapeutic use of Conivaptan? AE? C/I?
Use: Hypervolemic/Euvolemic hyponatremia (hospitalized px) AE: Orthostatic hypotension C/I: Hypovolemic hyponatremia Produces water diuresis
72
What are the uses, AEs, & C/Is of Tolvaptan?
Uses: - HF when other diuretics don’t work - Hypervolemic/Euvolemic hyponatrmia - SIADH AEs: Thirst, dry mouth, nausea, polyuria, Liver toxicity C/I: Liver disease

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