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
GnRH Agonists & Analgues
Gonadotropin Releasing Hormone
26
What are the two ways of giving GnRH
- pulsatile fashion causes release of FSH/LH | - a sustained/continuous way it inhibits release of FSH/LH
27
What is the effect of GnRH if given in a pulsatile fashion?
release of FSH/LH
28
What is the effect of GnRH if given in a sustained fashion?
inhibits the release of FSH/LH
29
Leuprolide (Lupron)
pallative care prostate cancer
30
Goserelin (Zoladex)
breast and prostate cancer
31
Histrelin (Vantus)
precocious puberty
32
Nafarelin (Synarel)
endometriosis
33
Uses for GnRH sustained use
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
ADRs GnRH agonists
HA meopause symptoms androgen deprivation in men
35
Use of Dopamine Analogues
supress prolactin in hyperolacinemia produced by adenomas Acromegaly
36
RXs of Dopamine Agonists
- Bromocriptine (Parlodel) - Cabergoline (Dostinex) - Pergolide
37
ADRs of Dopamine Analogues
``` Nausea, Constipation HA Light-headedness Orthostatic hypotension Fatigue ```
38
Posterior Pituitary Hormone List
Oxytocin (Pitocin) Vasopressin (Pitressin) & Desmopressin (DDAVP) a long acting analogue of vasopressin
39
Oxytocin Uses
causes sustained contractions of uterus - Induce labor - Augment protracted labor - Postpartum control of uterine hemorrhage
40
Oxytocin Toxicity
fetal distress, placental abruption or uterine rupture fluid retention, water intoxication
41
Oxytocin Contraindications
fetal distress, prematurity, abnormal fetal presentation, cephalopelvic disproportion
42
Vasopressin and Desmopressin
Antidiuretic effects and vasopressor (increase BP) effects
43
MOA of vasopressin and Desmopressin
increase cAMP in renal tubules leads to increased H2) absorption-> increase Von Willebrand factor-> shortend apTT and bleeding time
44
Clinical Uses of Posterior Pituitary Hormones
- Diabetes insipidus - esophageal bleeding - Hemophilia A or von Wilebrands disease - need to elevate BP - nocturnal enuresis
45
ADRs of Vasopressin and Desmopressin
HA, nausea, abdominal cramps, agitation and allergic reactions
46
Contraindications of Vasopress and Desmopressin
- Hyponatremia and seizures - vasoconstriction=CAD - Renal Impairment
47
RXs for Synthetic Thyroid supplements
- Levothyroxine (T4): Synthroid (Drug of Choice) - Liothyronine (T3): Cytomel - Liotrix (T3 and T4 mix): Thyrolar
48
RXs for animal thyroid supplements
- Desiccated thyroid: Armour Thyroid | - T3 & T4 mix: Natur-Throid
49
Anti-thyroid agents
- Methimzazole | - propylthiouracil
50
Thyroid Gland
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
Use of thyroid Supplements
Used when thyroid gland does not produce enough thyroid on its own
52
Synthetic thyroid supplements
- Levothyroxine (T4): Synthroid (Drug of Choice) - Liothyronine (T3): Cytomel - Liotrix (T3 and T4 mix): Thyrolar
53
Animal Thyroid Supplements
- Desiccated thyroid: Armour Thyroid | - T3 & T4 mix: Natur-Throid
54
Pharmacokinetics Thyroid Supplements
- 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
myxedema coma
severe hypothyroidism
56
MOA Thyroid Supplements
Free thyroxine (T4) enters cell, changed to T3, and affects metabolism
57
Which thyroid is stornger?
T3. Has 4 times the strength as T4. | T3 works days after administration
58
What is thyroid hormone needed for?
It is needed for optimal growth, function, and maintinance of tissues.
59
Levothyroxine (Synthroid) (T4)
-1st choice- stable, low cost, long half life | 25mg-300mcg 88-150 average
60
Liothyronine (Cytomel)
-4x more potent short hald life and need to be dosed multiple times a day 5mcg and 25mcg pills
61
When to use T3?
If your body has trouble converting T4 to T3
62
Liotrix (Thyrolar)
Mix of T4 and T3 4:1 tries to mimic body
63
Sunthroid=Armour Thyroid
``` Desiccated from animals used less bc of hypersensitivity MEASURED IN GRAINS 1 Grain=65 mcg 1 Grain Armour=100 mcg levothyroxine ```
64
What is the clinical use of thyroid supplements?
Hypothyroidism- biggest use
65
Monitoring Thyroid Drug Therapy
- 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
how often do you measure thyroid therapy?
4-8 weeks
67
ADRs of thyroid overtreatment
``` osteoporosis tachyarrhythmias angina MI hyperthyroidism ```
68
What are the two ways drugs deal with hyperthyroidism?
- Interfere with production of thyroid | - Modify tissue response to hormones
69
Two drugs that interfere with thyroid production.
- Methimazole (Tapazole) | - Propylthiouracil (PTU)
70
MOA of -Methimazole (Tapazole) and Propylthiouracil (PTU)
- inhibit synthesis of thyroid hormones | - block T4->T3 conversion
71
Pharmokinetics of Methimazole (Tapazole) and Propylthiouracil (PTU)
- 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
Which is more potent, Methimazole or Propylthiouracil (Thioureas)?
Methimazole-10x
73
ADRs of Methimazole & Propylthiouracil (Thioureas)
``` -HEPATOTOXICITY-BLACK BOX rash lupus like symptoms fever arthralgia agranulocytosis- early in therapy ```
74
Agents that inhibit symptoms of thyoidtocixosis
Beta Blockers they dont change thyroid levels they just help symptoms palpitations, tachycardia, tremors, anxiety
75
Beta Blockers used in thyrrotoxicosis
propanol | nadolol