thyroid and antithyroid Flashcards
function of thyroid peroxidase
oxidation and organification of iodide AND coupling of mono-iodotyrosine and diodotyrosine
DIT + DIT - T4
DIT + MIT - T2
thyroid hormone fxn
bone growth and CNS development
enhance B1 receptors in heart = increase CO/HR/SV/contractility
Increase BMR via Na/K ATPase
Increase glycogenolysis, gluconeogenesis, lipolysis
thyroglobulin proteins affected by pregnancy and OCP
TBG increases
action of reverse T3
binds T3 receptors and blocks T3 receptors
unknown pharmalogical fxn
what kind of pathway do TRH, TSH, and T3/T4 use?
TRH = IP3 TSH = cAMP T3/4 = intranuclear receptor binding
control gene expression
what drugs can cause primary hypothyroidism
lithium
amiodarone
levothyroxine
T4
liothyronine
T3
not used too frequently
thyroid preparations MOA
stimulation of nuclear receptors = gene expression with RNA formulation and protein synthesis
thyroid preparation use
hypothyroidism
cretinism
off label as weight loss supplements
thyroid preparation kinetics
T4 –> T3 = T3 is much more potent
any inducers can increase metabolism of thyroid hormones
thyroid prep AE
thyrotoxicosis:
sweating, warm skin, inc appetite, dyspnea, tachycardic, weight loss, menstrual irregularity, infertile, increased deep tendon reflexes
drugs used in hyperthyroidism
1) thioamides
2) iodine/salts
3) 131 Iodide
4) beta blocker
5) diatrizoate, glucocorticoids
propylthiouracil
thioamide
inhibits both TPO and 5-deiodinase = decreases drops in T3 AND T4
reserved for pt who are intolerant to methimazole
used in thyroid storm (b/c dec both T3 and T4)
used in 1st trimester (less teratogen than methimazole)
methimazole
thioamide
inhibits only TPO
thioamide MOA
inhibit thyroid peroxidase, iodine organification, and conversion of T4 to T3
proprylthiouracil inhibits both thyroid peroxidase and 5-deiodinase
methimazole inhibits TPO only
thioamide PK
slow onset - not inhibited preformed T4/T3 - takes 2 to 3 weeks
methimazole - 1x daily
PTU - 3x daily
both pass placental barrier
thioamide AE
agranulocytosis
hepatitis
hypothyroidism
lugol’s solution
iodide
iodide + potassium iodidie
potassium iodide
iodide
saturated solution
Iodides MOA
inhibition of thyroid hormone synthesis = dec organification and release via brief TPO inhibition
cannot use long term use - thyroid escapes effects after 14 days = “wolff Chaikoff effect”
wolff chaikoff effect
“escape effect”
loss of efficacy of iodides b/c thyroid loses TPO inhibition after 14 days
if continued – multinodular goiter
iodides use
pre-op for thyroidectomy = decreases size, fragility, and vascularity of tumor
PTU + b blocker + iodides = used for thyrotoxic crisis
Jod Basedow phenomenon
multinodular goiter that develops with continued use after wolff chaikoff effect
iodides AE
wolf chaikoff
chronic iodide intoxications
anaphylactoid = angioedema,
larygneal swelling
brassy taste
burning of teeth and gums
enlargement of parotid and maxillary glands
radioactive iodidne
taken up and sequestered by thyroid gland = damages tissue through emission of toxic beta rays
radioactive iodidne use
hyperthyroidism
Grave’s
if refractory to other drugs
contraindicated in pregnant and nursing females
**only medication that causes permanent reduction in thyroid activity
radioactive iodine AE
sore throat
hypothyroidism
nonselective B blockers used
propranolol
nadolol
esmolol
B blocker MOA
competitively blocks B receptors - inhibit T4 to T3 conversion
B blocker use
thyroid storm/toxicosis, tremor, stage fright
b blocker AE
bronchospasm
AV block
HF
nadolol: longer action that propanolol, less CNS effects
esmolol: shorter acting - used for intra-operative thyroid storm
B blocker alternative in asthma pt
CCB: dilitazem and verapamil
amiodarone
structurally similar to thyroxine
iodine assoc hyperthyroidism or autoimmune med inflam - use steroids
hypothyroidism - give levothyroxine
iohexol/diatrizoate
suppress T4 to T3
rapidly reduces T3 concentration in thyrotoxicosis
lithium
inhibits release of hormones and thyroid enlarges
drugs that inhibit conversion of T4 to T3
1) steroids
2) propranolol
3) amiodarone
4) diatrizoate and iohexol