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Endocrine > 180. Pituitary/Thyroid/Adrenal Pharmacology > Flashcards

180. Pituitary/Thyroid/Adrenal Pharmacology Flashcards

1
Q

Vasopressin binds this GPCR that then couples to Gq/PLC

Leads to vascular effects:
- IP3 –> calcium release –> vasoconstriction

CNS effects:

  • bonding
  • depression
A

V1 receptor

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2
Q

Can be used for its anti-cancer actions:

  • decrease lymphocytes
  • can promote cancer cell differentiation

Used in combination w/ chemo of hematologic malignancies

A

Prednisone (glucocorticoids)

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3
Q

Modified mutant form of GH that acts as a GH receptor antagonist

Allows receptor dimerization but blocks subsequent signaling, thus prevents activation of JAK-STAT pathway and secretion of IGF-1 from liver

Used to treat acromegaly

A

Pegvisomant

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4
Q

Adverse effects:

  • increases in liver transaminases
  • lipohypertrophy
  • possible loss of negative feedback, resulting in growth of GH-secreting adenomas
  • compulsive behavior
A

Pegvisomant

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5
Q

Desmopressin prefers which receptor over which other one?

A

V2&raquo_space;» V1

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6
Q

Vasopressin synthetic analog

A

Desmopressin

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7
Q

Adverse effects:

  • arthralgias, myalgias
  • peripheral edema
  • carpal tunnel
  • intracranial HTN
  • insulin resistance (sometimes improved sensitivity d/t reduced visceral fat)
A

GH

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8
Q

Act mainly through nuclear receptors to regulate genes
- interact with response elements as heterodimers

B1: liver
B2: hypothalamus
Alpha-1: heart
Alpha-2: inactive binding form

A

Thyroid hormones

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9
Q

2 things that negatively regulate GH

A

Dopamine and somatostatin

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10
Q

Inhibits thyroglobulin proteolysis and hormone release

Adverse effects:

  • cross placenta and can cause fetal hypothyroidism
  • not useful for long-term treatment
A

KI

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11
Q

Most toxic steroid synthesis blocker

Used to treat carcinomas

A

Mitotane

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12
Q

Blocks cholesterol side chain cleavage

A

Aminoglutethimide

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13
Q

Gamma and beta emitter

Administered orally; absorption is rapid

Trapped, incorporated, deposited in colloid

Released beta particles cause necrosis of follicular cells

Half life is 8 days, which most gone by 2 months

Synthesis needs to be blocked so that there is no release of radioactive hormone and precursors

Not used in pregnant or nursing women

A

I-131

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14
Q

Levothyroxine is which thyroid hormone

A

T4

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15
Q

GH antagonist that is more potent than somatostatin in inhibiting GH secretion

Acts through somatostatin receptors, GPCRs that use Gi

Activates K+ channels and protein phosphotyrosine phosphates

Short duration, requires multiple doses per day through IV or SC

Long acting analog = lanreotide

A

Octreotide

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16
Q

Used to determine the etiology of hypofunction (low glucocorticoids)

Blocking 11-hydroxylase will decrease glucocorticoid production, thus decreasing negative feedback, and increasing ACTH secretion

Used to determine the extent to which the pituitary can be stimulated
- manipulating feedback pathway

A

Metyrapone test

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17
Q

Can cause hepatoxicity but is the drug to treat pregnant patients

A

PTU

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18
Q

Acute loss of adrenal function requires __ w/ salt and water

A

Glucocorticoids

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19
Q

Used to induce labor under restricted conditions:

  • when early vaginal delivery is indicated (eclampsia)
  • when labor is protracted or arrested

Control postpartum uterine hemorrhage

A

Oxytocin

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20
Q

Liver:
- promote conservation of glucose (glycogen synthesis); stimulate gluconeogenesis (insulin antagonistic effect)

CT:
- decerase protein synthesis, promote protein breakdown resulting in muscle wasting, thinning of skin, osteoporosis

Adipose tissue:
- fat redistribution, truncal obesity

A

Glucocorticoids

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21
Q

Thyroid hormones should be prescribed as:
__ for pregnant patients

__ for elderly and pts w/ CAD

A

Higher

Lower

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22
Q

For myxedema coma, T3 is administered through __ or else thyroid hormones are orally effective

A

IV

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23
Q

Used as suppressive therapy after thyroidectomy for malignancy

A

Thyroid hormones

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24
Q

Adverse effects:

  • hypoglycemia
  • lipohypertrophy
  • intracranial HTN
  • slipped epiphyses
  • scoliosis

Contraindicated in pts w/ active or suspected neoplasia
- cancer patients

A

IGF-1 agonists

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25
Q

Type of CAH

Low glucocorticoids
High ACTH
Increased secretion of mineralocorticoids and androgens

Steroid replacement of glucocorticoid

A

11-hydroxylase deficiency

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26
Q

Used for:

  • replacement in children w/ GH deficiency
  • Other causes of short stature: Turner’s, Prader-Willi, Chronic renal insufficiency, idiopathic short stature)
  • AIDS-wasting or malabsorption
A

GH treatment

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27
Q

Vasopressin receptor antagonists used to treat SIADH

A

Conivaptan and tolvaptan

- tolvaptan is more selective fo V2 receptors but can be hepatotoxic

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28
Q

Adverse effects:

  • nausea and bloating
  • gallstones
  • bradycardia (affects cardiac conduction)
A

Octreotide

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29
Q

Promote growth and normalize metabolism in IGF-1 deficiency resistant to GH

A

Mecasermin (IGF-1 agonist)

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30
Q

Control tachycardia, hypertension, A-Fib, during the acute phase of thyrotoxicosis

Control BP chronically

Weak inhibitor of peripheral T4 –> T3 conversion

A

Propranolol

31
Q

Secreted in response to decreased blood pressure and hypertonicity (hypernatremia)

Raises BP and promotes water reabsorption

Master regulator of fluid homeostasis

A

Vasopressin (ADH)

32
Q

Vasopressin receptor that increases factor VIII and vWF

A

V2 receptor

33
Q

Activates GPCRs on smooth muscle for contraction
- Gq –> PLC –> Ca2+ - calmodulin - myosin

Promotes release of prostaglandins and leukotrienes
- important for smooth muscle control

A

Oxytocin

34
Q

Adverse effects:

  • uterine rupture, fetal distress
  • activation of vasopressin receptors at high dose d/t structural similarity
A

Oxytocin

35
Q

Therapies for __:

  • surgery to resect glands
  • I-131 radiation
  • thionamides
  • sympatholytic agents (Beta-blockers)
  • KI
A

Hyperthyroidism

36
Q

Used to determine the etiology of hypofunction (low glucocorticoids)

Exogenous ACTH will stimulate adrenal secretion if the adrenal insufficiency is due to inadequate ACTH secretion (pituitary insufficiency), but not if the insufficiency is d/t adrenal failure

A

ACTH test

37
Q

Contains IGF-1 and the IGF-1 binding protein IGFBP-3, which prolongs the half-life

A

Mecasermin rinfabate

38
Q

Used to stop bleeding in hemophilia A and von Willebrand’s disease

A

Desmopressin

39
Q

Treatment of central diabetes insipidus

Stop bleeding from esophageal varices

A

Vasopressin

40
Q

Stimulates longitudinal growth of bone until epiphyseal plate closure

Increases muscle mass

Decreases central adiposity

Reduces sensitivity to insulin

A

Growth hormone

41
Q

Most glucocorticoids are inactivated in the __

A

Liver

42
Q

Most common treatment of adrenal hyperfunction (2 things)

Can be primary - adrenal adenoma, carcinoma - or secondary to increased ACTH - pituitary adenoma, ectopic ACTH

A

Surgery or radiation

43
Q

Adverse effects:

  • weight loss
  • excessive sweating
  • diarrhea
  • anxiety
  • headaches
  • palpitations, angina
  • coronary and cerebral thromboses

Chronic excess can result in muscle weakness, anemia, infertility, high output cardiac failure, bone loss, insulin resistance

A

Thyroid hormones

44
Q

Adrenal steroids interact with receptors in the cytoplasm, resulting in the release of __

This exposes the DNA binding domain of receptor and allows translocation to the nucleus

A

Hsp90

45
Q

T4 is the preparation of choice in most situations: why?

A 
More convenient dosage (QD - longer half-life) 
Lower risk (less potent)
46
Q

Inhibits:

  • GH secretion
  • TSH secretion
  • ACTH secretion
  • glucagon secretion
  • gastrin secretion
  • insulin secretion

Uses:

  • acromegaly
  • other hormone-secreting tumors
  • secretory diarrhea from chemo
  • “dumping syndrome” after gastric surgery
A

Octreotide

47
Q

Can be used for anti-inflammatory and immunosuppressive actions:

  • decrease synthesis of prostaglandins and leukotrienes (inflammatory cytokines)
  • decrease lymphocytes, monocytes, eosinophils, basophils
  • decrease Ab production and Ag processing
  • decrease scar formation

Useful in palliative treatment of RA, lupus, and other systemic and local inflammatory disorders

A

Hydrocortisone

48
Q

Recombinant peptide that is identical to native human GH and used to treat GH deficiency

A

Somatropin

49
Q

Semisynthetic ergot alkaloids

Mechanism:

  • selective dopamine D2 receptor agonists
  • mimic effects of dopamine to inhibit GH production and secretion
  • even more effective in inhibiting prolactin
A

Cabergoline and bromocriptine

50
Q

Treatment for nephrogenic diabetes insipidus

  • can be caused congenitally or by drugs like lithium
  • decreases urine output through a paradoxical path
A

Thiazides

51
Q

ACTH deficiency requires __ replacement

A

Glucocorticoid

52
Q

Glucocorticoid receptor antagonist

A

Mifepristone

53
Q

Addison’s disease:

  • characteristics include muscle weakness and low BP
  • requires replacement of what??
A

Mineralocorticoids and glucocorticoids

54
Q

Adverse effects:

  • undesired vasoconstriction, especially in pts w/ CAD
  • nausea, abdominal cramps, HAs, and allergic reactions
A

Vasopressin

55
Q

Recombinant form of IGF-1

A

Mecasermin

56
Q

Critical for development of the CNS and skeletal system

Metabolic: optimize energy metabolism and reproductive function

Cardiac: inotropic and chronotropic effects; potentiate effects of sympathomimetic amines

Hepatic: increase cholesterol metabolism; effects on glucose metabolism cause insulin resistance

Skeletal: possibly promote osteoporosis

A

Thyroid hormones

57
Q

GH acts through homodimeric __-__ linked membrane receptors

JAK is then activated which activates STAT proteins –> go to nucleus to be transcription factors

A

tyrosine-kinase

58
Q

Steroids need to be tapered off after the drug is no longer needed to control symptoms to avoid __ __

Can ruin the feedback system overall and the pituitary will no longer secrete ACTH

A

Adrenal insufficiency

59
Q

Type of CAH

Low glucocorticoids and mineralocorticoids
High ACTH
Increased secretion of androgens

Steroid replacement of mineralocorticoids and glucocorticoids

A

21-hydroxylase deficiency

60
Q

Adverse effects:

  • pruritic rash, arthralgia most common
  • agranulocytosis
A

Thionamides

61
Q

Uses:

  • acromegaly
  • hyperprolactinemia and galactorrhea

Orally effective

A

Cabergoline

62
Q

Uses related to anti-inflammatory, immunosuppressive, anticancer actions requires supraphysiologic concentrations

A

Glucocorticoids

63
Q

Used to determine the etiology of hyperfunction (high glucocorticoids)

Potent glucocorticoid is used that will not interfere with assays for endogenous glucocorticoids to test whether the response is suppressible

Test will usually suppress ACTH from pituitary adenomas, but not ectopic ACTH

A

Dexamethasone Test

64
Q

Abnormal growth of bone and cartilage is characteristic of __

Treatments include surgery, radiation, and drugs

A

Acromegaly

65
Q

__ deficiency during childhood and adolescence results in short stature, decreased muscle mass, and increased body fat

A

GH

66
Q

Blocks multiple steps in the steroid synthesis pathway

A

Ketoconazole

67
Q

Kidney:
- increase calcium excretion

Immune system:
- decrease antibody production, antigen processing, decrease lymphocytes, cytokines, and prostaglandins

GI:
- cause thinning of mucus, increase acid and pepsin secretion, decrease calcium absorption

A

Glucocorticoids

68
Q

Adverse effects:

  • nausea and vomiting
  • HA
  • orthostatic hypotension
  • rare effects: nasal congestion, digital vasospasm, hallucinations, psychoses, nightmares, congestion
  • has been associated with valvular heart disease
A

Cabergoline

69
Q

Vasopressin binds this GPCR that then couples to Gs/adenylate cyclase, increase cAMP, PKA

Increases water reabsorption from collecting duct through insertion and stabilization of aquaporin-containing vesicles (Aquaporin 2)

A

V2 receptor

70
Q

Blocks 11-hydroxylase

A

Metyrapone

71
Q

Inhibit TPO, blocking iodination and couplng

__ also inhibits peripheral conversion of T4 to T3

Slow onset, 3-4 weeks, because stored hormone can still be released

A

Thionamides (methimazole and PTU)

PTU

72
Q

GH analog with an additional methionine which prolongs its half-life

A

Somatrem

73
Q

Most of the actions of GH are mediated through hepatic production of __

  • can also be stimulated by other agents
  • __ and GH can down-regulate GH secretion
A

IGF-1

Endocrine (26 decks)

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