TH and Anti-Thyroid agents French Flashcards
What is TSH stimulated and inhibited by?
Stim by: hypothalamic TRH
Inhib by: somatostatin, DA, glucocorticoids (stress)
pts who are on lithium ions for ani-manic therapy can show hyper or hypothyroidism? How?
HYPOthyroidism
- inhibits cAMP generation → less uptake of iodine → hence blocks action of TSH
Iodide organification is achieved via which enzyme? What else does this enzyme do?
Thyroid peroxidase
I- oxidized and incorporated into tyrosine residues (MIT, DIT) on Tg molecules
It also is involved in coupling the MIT + DIT on Tg
How is T4 and T3 released from the thyroid gland?
via proteolysis
TRH aka _____
Pharmacodynamics
Uses
Protirelin
activ PLC → ↑ IP3 → ↑intracellular Ca2+
Test for pituitary reserve of TSH if suspected hypo or hyperthyroidism
Thyrotropin
Pharmacodynamics
Uses
TSH
stimulates cAMP production → increased Iodide uptake + TH production
Uses: therapy for metastatic thyroid carcinoma
Most common cause of hypothyroidism
autoimmune thyroiditis (Hashimotos)
- glandular destruction due to cell-antibody mediated damage
- nontender thyroid
Why does pregnancy require increased T4 dose?
due to increased levels of TBG (via elevated estrogen) and placental metabolism of T4-T3
Sign of end stage untreated hypothyroidism and is an acute medical emergency
Myxedema coma
- hyponatremia, hypoglycemia, hypothermia, shock, death
Things that increase binding of free T4 to TBG
Estrogen (increases levels of TBG)
SERMs (Selective estrogen receptor modulators)
Tamoxifen
Things that Decrease binding of free T4 to TBG
Salicylates
Antiseizure meds
Where is the majority of circulating T3 that is utilized derived from and where? What about T3 that is used in brain and pituitary?
Derived from T4 in the liver
T3 that is utilized by pit+brain is derived locally
Drugs that inhibit 5’deiodinase which converts T4 → T3
Glucocorticoids
Beta-adrenergic receptor antagonist
Propylthiouracil
↑
→↓ ←
α β
v
Most common form of hyperthyroidism
Graves disease
- results from thyroid stimulation by autoantibodies that mimic TSH
- see exophthalmos and pretibial myxedema