Hypothalmic, Pituitary & Thyroid Hormone Pharmacology Flashcards

1
Q

3 types of Anterior Pituitary Hormones

A

1) Growth hormone agonists and antagonists
2) Gonadotropin agonists and antagonists
3) Prolactin antagonists

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2
Q

2 types of posterior pituitary hormones

A

1) Oxytocin agonists

2) Vasopressin agonists and antagonists

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3
Q

what are agonists used for?r

A

replacement of hormone deficiency

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4
Q

what are antagonists used for?

A

excess pituitary hormone production

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5
Q

What are releasing hormones predominatly used for?

A

diagnostic testing

not used as medications because if the gland does not work it is easier to give target gland hormone than the hormone from the hypothalamus or pituitary

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6
Q

List the Anterior Pituitary Hormones

A

1) Growth hormone (GH)
2) Growth hormone antagonists
3) LH/FSH
4) GnRH agonists and analogues
5) Dopamine or analogues

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7
Q

List posterior pituitary hormones

A

1) oxytocin

2) vasopressin

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8
Q

Growth Hormone

A

Somatotropin

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9
Q

Somatotropin effects

A
  • linear bone growth
  • stimulat erythropoietin
  • increases lipolysis
  • regulates blood nutrient levels
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10
Q

How is human GH made?

A

recombinant DNA

SQ 3-7 times/week

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11
Q

How does somatotropin work best?

A

works best when short stature is due to GH deficiency

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12
Q

What is a MUST requirment of using somatotropin?

A

height MUST use before closure of epiphyseal plates

2 years after menses
20 yo-boys

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13
Q

What age group has less adverse side affects with somatotropin?

A

children

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14
Q

ADRs of somatotropin

A

Children: arthralgia, edema, HA, leg/muscle pain

Adults: arthralgia, back pain, carpal tunnel syndrome, edema, HA, stiffness, upper respiratory infections

INCREASES DEATH IN TERMINAL PTS.

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15
Q

Use of Growth Hormone Antagonists

A

to treat GH excreting pituitary adenomas

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16
Q

Growth Hormone antagonist

A

Somatostatin, octreotide

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17
Q

Somatostatin

A

excreted by hypothalmus and pancreas

inhibits release of GH, glucogon, insulin, and gastrin

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18
Q

Rx somatostatin

A

Octreotide

longer half life than somatostatin

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19
Q

Clinical Uses of Octreotide

A
  • acromegaly
  • GH producing adenomas
  • rare cancers like gastrinomas and insulinomas
  • esophageal bleeding
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20
Q

How is Octreotide administered

A

injectable

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21
Q

ADRs of Octreotide

A
  • GI
  • Arrhythmias
  • hypothyroidism
  • decrease glucose
  • biliary tract disorders
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22
Q

FSH/LH/hCG

A

hCG- human chorionic gonadotropin is produced by the placenta, close to FSH

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23
Q

what does hCG stimulate?

A

FSH receptors

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24
Q

What is the use of hCG?

A

infertility
stimulates spermatogenesis in men and ovulation in women
used in IVF

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25
Q

GnRH Agonists & Analgues

A

Gonadotropin Releasing Hormone

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26
Q

What are the two ways of giving GnRH

A
  • pulsatile fashion causes release of FSH/LH

- a sustained/continuous way it inhibits release of FSH/LH

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27
Q

What is the effect of GnRH if given in a pulsatile fashion?

A

release of FSH/LH

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28
Q

What is the effect of GnRH if given in a sustained fashion?

A

inhibits the release of FSH/LH

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29
Q

Leuprolide (Lupron)

A

pallative care prostate cancer

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30
Q

Goserelin (Zoladex)

A

breast and prostate cancer

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31
Q

Histrelin (Vantus)

A

precocious puberty

32
Q

Nafarelin (Synarel)

A

endometriosis

33
Q

Uses for GnRH sustained use

A

Prostate, Breast, and Ovarian Cancer

it causes -hypogonadism- down regulates receptors then decreases secretion of FSH and LH. THis causes hypogonadism because now there is no stimulation of the gonads, The body sees no estrogen or testosterone.

Controlled ovarian hyperstimulation

Prevent FSH from working, then stop it when you want ovulation

Endometriosis-blocks FSH/LH-supresses estrogen- prevents stimulation of endometrial cells

Uterine fibroids-same mechanism of endometriosis

34
Q

ADRs GnRH agonists

A

HA
meopause symptoms
androgen deprivation in men

35
Q

Use of Dopamine Analogues

A

supress prolactin in hyperolacinemia produced by adenomas

Acromegaly

36
Q

RXs of Dopamine Agonists

A
  • Bromocriptine (Parlodel)
  • Cabergoline (Dostinex)
  • Pergolide
37
Q

ADRs of Dopamine Analogues

A
Nausea, 
Constipation 
HA
Light-headedness 
Orthostatic hypotension 
Fatigue
38
Q

Posterior Pituitary Hormone List

A

Oxytocin (Pitocin)

Vasopressin (Pitressin) & Desmopressin (DDAVP) a long acting analogue of vasopressin

39
Q

Oxytocin Uses

A

causes sustained contractions of uterus

  • Induce labor
  • Augment protracted labor
  • Postpartum control of uterine hemorrhage
40
Q

Oxytocin Toxicity

A

fetal distress, placental abruption or uterine rupture

fluid retention, water intoxication

41
Q

Oxytocin Contraindications

A

fetal distress, prematurity, abnormal fetal presentation, cephalopelvic disproportion

42
Q

Vasopressin and Desmopressin

A

Antidiuretic effects and vasopressor (increase BP) effects

43
Q

MOA of vasopressin and Desmopressin

A

increase cAMP in renal tubules leads to increased H2) absorption-> increase Von Willebrand factor-> shortend apTT and bleeding time

44
Q

Clinical Uses of Posterior Pituitary Hormones

A
  • Diabetes insipidus
  • esophageal bleeding
  • Hemophilia A or von Wilebrands disease
  • need to elevate BP
  • nocturnal enuresis
45
Q

ADRs of Vasopressin and Desmopressin

A

HA, nausea, abdominal cramps, agitation and allergic reactions

46
Q

Contraindications of Vasopress and Desmopressin

A
  • Hyponatremia and seizures
  • vasoconstriction=CAD
  • Renal Impairment
47
Q

RXs for Synthetic Thyroid supplements

A
  • Levothyroxine (T4): Synthroid (Drug of Choice)
  • Liothyronine (T3): Cytomel
  • Liotrix (T3 and T4 mix): Thyrolar
48
Q

RXs for animal thyroid supplements

A
  • Desiccated thyroid: Armour Thyroid

- T3 & T4 mix: Natur-Throid

49
Q

Anti-thyroid agents

A
  • Methimzazole

- propylthiouracil

50
Q

Thyroid Gland

A

Thyroid releaseing hormone released from hypothalmus , hits pituitary, which release thyroid stimulating hormone, thyroid then releases t3 and t4, once t3 and t4 are release there is a negative feedback system to the hypothalmus and the pituitary

T3 is the active form so body will convert the t4 to the t3

51
Q

Use of thyroid Supplements

A

Used when thyroid gland does not produce enough thyroid on its own

52
Q

Synthetic thyroid supplements

A
  • Levothyroxine (T4): Synthroid (Drug of Choice)
  • Liothyronine (T3): Cytomel
  • Liotrix (T3 and T4 mix): Thyrolar
53
Q

Animal Thyroid Supplements

A
  • Desiccated thyroid: Armour Thyroid

- T3 & T4 mix: Natur-Throid

54
Q

Pharmacokinetics Thyroid Supplements

A
  • Oral thyroxine (T4) and Liothyronine (T3) are both well absorbed
  • give on empty stomach, morning 30 min before breakfast or 4 hours after dinner

Give IV in sever hypothyoidism

55
Q

myxedema coma

A

severe hypothyroidism

56
Q

MOA Thyroid Supplements

A

Free thyroxine (T4) enters cell, changed to T3, and affects metabolism

57
Q

Which thyroid is stornger?

A

T3. Has 4 times the strength as T4.

T3 works days after administration

58
Q

What is thyroid hormone needed for?

A

It is needed for optimal growth, function, and maintinance of tissues.

59
Q

Levothyroxine (Synthroid) (T4)

A

-1st choice- stable, low cost, long half life

25mg-300mcg 88-150 average

60
Q

Liothyronine (Cytomel)

A

-4x more potent
short hald life and need to be dosed multiple times a day
5mcg and 25mcg pills

61
Q

When to use T3?

A

If your body has trouble converting T4 to T3

62
Q

Liotrix (Thyrolar)

A

Mix of T4 and T3
4:1
tries to mimic body

63
Q

Sunthroid=Armour Thyroid

A
Desiccated from animals
used less bc of hypersensitivity
MEASURED IN GRAINS
1 Grain=65 mcg
1 Grain Armour=100 mcg levothyroxine
64
Q

What is the clinical use of thyroid supplements?

A

Hypothyroidism- biggest use

65
Q

Monitoring Thyroid Drug Therapy

A
  • done with serum levels of TSH or T4
  • TSH tells you how much thyroid the pituitary is seeing
  • not enough thyroid available TSH is high (b/c thyroid not seeing enough)
  • too much thyroid TSH is low
66
Q

how often do you measure thyroid therapy?

A

4-8 weeks

67
Q

ADRs of thyroid overtreatment

A
osteoporosis
tachyarrhythmias
angina
 MI
 hyperthyroidism
68
Q

What are the two ways drugs deal with hyperthyroidism?

A
  • Interfere with production of thyroid

- Modify tissue response to hormones

69
Q

Two drugs that interfere with thyroid production.

A
  • Methimazole (Tapazole)

- Propylthiouracil (PTU)

70
Q

MOA of -Methimazole (Tapazole) and Propylthiouracil (PTU)

A
  • inhibit synthesis of thyroid hormones

- block T4->T3 conversion

71
Q

Pharmokinetics of Methimazole (Tapazole) and Propylthiouracil (PTU)

A
  • accumulate in thyroid gland so serum half-life is short but effect lasts a long time
  • Cross placenta
  • CAN CAUSE FETAL HYPOTHYROIDISM
  • slow onset- reduce symptoms- 4-6 months
72
Q

Which is more potent, Methimazole or Propylthiouracil (Thioureas)?

A

Methimazole-10x

73
Q

ADRs of Methimazole & Propylthiouracil (Thioureas)

A
-HEPATOTOXICITY-BLACK BOX
rash
lupus like symptoms
fever
arthralgia
agranulocytosis- early in therapy
74
Q

Agents that inhibit symptoms of thyoidtocixosis

A

Beta Blockers

they dont change thyroid levels they just help symptoms

palpitations, tachycardia, tremors, anxiety

75
Q

Beta Blockers used in thyrrotoxicosis

A

propanol

nadolol