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Endocrine- Pharm > Hypothalamic/Pituitary Hormones > Flashcards

Hypothalamic/Pituitary Hormones Flashcards

1
Q

What is the MOA of somatotropin?

A

Somatropin is a direct agonist of the growth hormone receptor stimulating gene expression e.g. IGF1

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2
Q

Somatotropin: indications?

A 
HRT for children w GH deficiency
Other conditions of small stature
Prader-willi syndrome
Turner’s syndrome
Noonan’s syndrome
Chronic renal insufficiency
Idiopathic short stature
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3
Q

Somatotropin: adverse effects?

A

Children:
Idiopathic intracranial HTN
Increased intraocular pressure
Development of insulin resistance

Adults:
Peripheral edema
Arthralgias
Carpal tunnel
Parathesis
Worsening glucose intolerance
Acute pancreatitis
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4
Q

Somatotropin: contra-indications?

A 
Contraindications:
Active malignancy
Uncontrolled diabetes
Proliferative retinopathy
Children with closed epiphyses
Prader-willi with severe obesity 
and/or respiratory obstruction
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5
Q

Mescarmin: MOA?

A

Recombinant IGF1

Is a downstream effector of GH-bypasses GHR defects and/or anti-GH Abs

Activates the IGF1R

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6
Q

Mescarmin: indications?

A

Children with impaired growth non-responsive to GH

e.g. mutations in GHR or downstream signaling pathway, neutralizing antibodies to GH, or IGF-1 gene defects (v. rare)

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7
Q

Mescarmin: adverse effects?

A

Hypoglycemia

Intracranial hypertension

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8
Q

Mescarmin: contraindications?

A

Active malignancy

Children with closed bone epiphyses

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9
Q

Name two somatostatin analogues

A

Octreotide

Lanreotide

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10
Q

Octreotide/Lanreotide: MOA?

A

Octreotide/Lanreotide are somatostatin receptors agonists

Stimulate pathways that inhibit production of GH

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11
Q

Octreotide/lanreotide: indications?

A

GH excess
Gigantism
Acromegaly

Other clinical uses
Esophageal varices
Carcinoid syndrome
Gastrinoma
glucagonoma
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12
Q

Octreotide/lanreotide: adverse effects?

A

Nausea/Diarrhea (~50%)
Gallstones (~25%)
Suppresses TSH (monitor for hypothyroidism
low risk- typically only transient effect)
Bradycardia & cardiac arrhythmias

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13
Q

Pegvisomant: MOA?

A

Direct antagonist of the growth hormone receptor

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14
Q

Pegvisomant: indications?

A

GH excess
Gigantism
Acromegaly

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15
Q

Name two dopamine agonists

A

Cabergoline

Bromocriptine

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16
Q

Bromocriptine/Cabergoline: MOA?

A

Direct agonists of D2 dopamine receptors

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17
Q

Bromocriptine/Cabergoline: indications?

A

Hyperprolactinemia

Other uses;
At high doses- treatment of acromegaly/gigantism

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18
Q

Bromocriptine/Cabergoline: adverse effects?

A

Nausea/headache
Orthostatic hypertension
Psychiatric symptoms

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19
Q

Name 5 gonadotropin releasing hormone agonists

A 
Leuprolide
Goserlin
Buserlin
Triptorelin
Naferelin
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20
Q

What is the MOA of Leuprolide/Goserlin/Buserlin/Triptorelin/Naferelin?

A

Sustained activation of GnRH receptor inhibits

release of gonadotropins

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21
Q

Leuprolide/Goserlin/Buserlin/Triptorelin/Naferelin: indications?

A

Controlled ovarian stimulation
Palliative therapy of hormone-dependent tumors
Suppression of inappropriate growth of hormone-dependent tissues e.g. endometriosis & fibroids
Treatment of precocious puberty
Suppression of endogenous puberty in gender dysmorphic adolescents

22
Q

GnRH agonists/antagonists contraindications?

A

Pregnancy

23
Q

Name three GnRH antagonists

A

Ganirelix
Cetrorelix
Degarelix

24
Q

Ganirelix, Cetrorelix, Degarelix: MOA?

A

Antagonize GnRH receptor –> reduce gonadotropin release

25
Q

Ganirelix/Cetrerelix: indication?

A

Control ovarian stimulation

26
Q

Degarelix: indication?

A

Advanced prostate cancer

27
Q

GnRH antagonists/agonists: adverse effects?

A 
Side effects associated with gonadal hormone deprivation
e.g. hot flashes
Decreased bone density
Vaginal dryness/atrophy
Erectile dysfunction
28
Q

Name the exogenous FSH/LH

A

hMG

29
Q

Name the exogenous FSH

A

Urofollitropin

30
Q

Name the recombinant FSH

A

Follitropan alpha/beta

31
Q

What is the MOA of FSH and hMG in females?

A

FSH and hMG stimulates follicular development

32
Q

What is the MOA of HCG in females?

A

HCG triggers ovulation via the LH receptor

33
Q

What is the MOA of HCG in males?

A

HCG stimulates endogenous testosterone production in males via stimulation of the LH receptor

34
Q

What are the indications of exogenous gonadotropins?

A

Infertility treatment in anovulatory women
Ovarian hyperstimulation
Male infertility in hypogonadotopic hypogonadism

35
Q

What are side effects of exogenous HCG in men?

A

Gynecomastia

36
Q

What are the side effects of exogenous FSH and HCG in women?

A

Multiple pregnancies

Ovarian hyperstimulation

37
Q

What is the MOA of oxytocin?

A

Acts through cognate GPCR expressed on uterine SMC and breast

38
Q

What are the indications for oxytocin?

A

Induction of labor

Treatment of uterine atony (failure of uterus to contract following delivery)

39
Q

What are the adverse effects of oxytocin at low vs. very high levels

A

Low; excessive stimulation of uterine contractions –> fetal distress, placental abruption or uterine rupture

High: off-target activation of vasopressin receptors leading to excessive fluid retention

40
Q

What is synthetic vasopressin called?

A

Desmopressin

41
Q

What is the MOA of desmopressin?

A

Selectively activates V2 vasopressin receptors in the kidney to promote water reabsorption

Activates V2 receptors on endothelial cells to release vWF

Long acting!

42
Q

Desmopressin: indications?

A

Central diabetes insipidus
Nocturnal enuresis
Minor bleeding in minor hemophilia and von willebrand’s disease

43
Q

Desmopressin: adverse effects?

A

Headache, hyponatremia

Acute thrombotic events- very rare

44
Q

Vasopressin: MOA

A

Direct full agonist of both V1 and V2 receptors

45
Q

What is the only indication of vasopressin?

A

Second line agent used in treatment of vasodilatory shock refractory to epinephrine

46
Q

What are the adverse effects of vasopressin

A

Hyponatremia, cardiac arrhythmia, low cardiac output, atrial fibrillation

47
Q

Name two vasopressin antagonists

A

Tolvaptan, Conivaptan

48
Q

Conivaptan: MOA

A

V1 and V2 antagonist- promotes increased water excretion and raises serum Na+

49
Q

Tolvaptan: MOA

A

Selectively antagonizes V2 receptors

50
Q

What is the indication for conivaptan and tolvaptan?

A

Hypervolemic hyponatremia- due to SIADH

51
Q

Which -vaptan is associated with liver hepatotoxicity?

A

Tolvaptan

Endocrine- Pharm (6 decks)

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