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Pharm Exam 5 > 63: Thyroid/Antithyroid Drugs > Flashcards

63: Thyroid/Antithyroid Drugs Flashcards

1
Q

iodide uptake into thyroid gland by the…

A

sodium iodide symporter

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2
Q

oxidation of iodide to iodine

A

peroxidase mediated

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3
Q

iodination of tyrosine molecules within..

A

thyroglobulin molecule
“iodide organification”

can either be MIT or DIT

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4
Q

MIT + DIT =

DIT + DIT =

A

T3

T4

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5
Q

most thyroid hormone is released as…

A

T4

majority is bound to thyroxine-binding globulin in blood

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6
Q

without thyroid hormone bound..

A

receptor is bound to tyroid response element and corepressors to INHIBIT gene transcription

T3 will bind directly to monomer of TR but T4 needs to be converted to T3 (5’ deiodinase)

with T3 bound to TR, retinoid x receptor and TR form hetero-dimer and increase gene trx

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7
Q

hypothalamus releases TRH –>

A

pituitary gland –> TSH –> thyroid –> T3 and T4

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8
Q

high T3 and T4 ______ secretion of TRH and TSH

A

inhibit - negative feedback loop

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9
Q

high iodide concentrations _____ thyroid hormone synthesis

A

inhibit (short term)

low promote

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10
Q

impact of TH on sympathetics?

A
  • increase B adrenergic receptors

- decrease alpha adrenergic receptors

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11
Q

impact of TH on growth and development?

A
  • brain development, neurogenesis

- bone growth and skeletal maturation through activation of osteoblast/clast

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12
Q

impact of TH on thermogenics?

A
  • increase energy consumption resulting in heat production
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13
Q

impact of TH on respiratory system?

A
  • increase O2 consumption in most tissues, thereby increasing CO2 formation –> RR increases
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14
Q

impact of TH on CNS?

A
  • rapidity of thinking and reasoning

- effect spinal cord synapses that control m. tone

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15
Q

impact of TH on GI?

A

increase secretions and motility

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16
Q

impact of TH on skin and hair?

A
  • growth promotion of hair, skin, nails

- prevent accumulation of glycosaminoglycans in interstitial space

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17
Q

impact of TH on cardiovascular?

A
  • increase HR
  • increase force of contraction
  • increase Co
  • increase blood volume
  • decrease vascular resistance

(due to changes in gene expression of prtns including b-adrenergic receptors)

18
Q

impact of TH on metabolism?

A
  • decrease circulating cholesterol by increases LDL and lipolysis
  • increase absorption of carbs, increase glycolysis, increase gluconeogenesis, increase insulin secretion
  • increase prtn synthesis and catabolism
  • increase need and usage of vit
  • *increase basal metabolic rate
19
Q

s/s hyperthyroidism

A 
increase BP
tachycardia
sweating
tremors
rapid growth
heat intolerance
high RR
increased breakdown muscle
weight loss
weakness and fatigue
insomnia
diarrhea
*exopthalmos
20
Q

grave’s disease

A

hyperthyroidism (autoimmune)

autoantibodies stimulate TSH receptors and increase the production of T3 and T4
*TSH levels will be low

21
Q

s/s hypothyroidism

A 
delayed development
bradycardia
cold intolerance
hypoventilation
depression
*puffy eyes
sleepy 
increased body weight
dry and scaly skin
atherosclerosis
22
Q

cretinism

A

congenital defect - primary hypothyroidism

  • lack of thyroid development, lack of TSH receptor, lack of TH synthesis
23
Q

Hashimotos disease

A

autoimmune primary hypothyroidism

may see initial hyperthyroidism with release from glands being destroyed

24
Q

iodide deficiency

A

primary hypothyroidsim

impaired hormone production

observe goiter

25
Q

why is levothyroxine tx of choice for hypothyroidism?

A
  • stable
  • low cost
  • easily measured
  • long half life
  • similar to normal physiology
26
Q

liothyronine

A

T3 agonist

more potent, but shorter half-life

27
Q

thyroid storm

A

acute episode of thyroid activity brought on by stress in a pt with undiagnosed/untreated hyperthyroidism

28
Q

excess iodide –>

A

normally will inhibit hormone production but with underlying disease can cause hyperthyroidism

29
Q

thioamides =

A

methimazole
propylthiouracil

  • contra in preggers
  • rash/GI side effects
30
Q

MOA methimazole and propylthiouracil

A

inhibit peroxidase, iodination, and coupling of iodotyrosines

concentrate in thyroid gland

31
Q

BBW for propylthiouracil

A

hepatitis

32
Q

treat thyroid storm with which thioamide

A

propylthiouracil because faster absorption

33
Q

iodides =

A

potassium iodide
lugol’s solution

can be used for thyroid storm

34
Q

MOA iodide

A

inhibit hormone release by inhbiting proteolysis of Tgb

35
Q

side effects of iodides

A

“sick” feeling

only work 2-8 wks

withdrawal = thyrotoxicosis

36
Q

MOA radioactive iodine

A

b ray destroy parenchymal cells of thyroid

gamma rays pass through tissue and detect concentration of RAI remaining in thyroid gland

37
Q

anion inhibitors

A

perchlorate
pertechnetate
thiocyanate

38
Q

adverse effect perchlorate

A

aplastic anemia

39
Q

MOA perchlorate, pertechnetate, thiocyanate

A

competitively inhibit the uptake of iodide via Na/I transporter

40
Q

MOA propanolol

A 
beta blcoker (Cardioprotective in thyroid storm)
 blocks T4--> T3

cant be used with athma, hypotension, bradycardia

41
Q

MOA diltiazem

A

calcium channel blocker

control tachycardia in asthmatic

42
Q

MOA barbiturates and bile acid sequestrants

A

increase T4 metabolism

increase T4 excretion

Pharm Exam 5 (11 decks)

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