Unit 5 - Thyroid and Antithyroid Drugs Flashcards Preview

MSII Pharmacology > Unit 5 - Thyroid and Antithyroid Drugs > Flashcards

Flashcards in Unit 5 - Thyroid and Antithyroid Drugs Deck (13):

how does iodine get into the thyroid?

through an Na-I symporter
-since there is high extracellular Na+, and an Na/K pump keeps intracellular Na+ low, I can get inside at a constant rate


what are diseases caused by defective Na-I smporters?

-symporter gene mutation - congenital hypothyroidism
-autoimmune (Hashimoto's) thyroiditis) - Ab against the symporter itself


what are the steps to thyroid hormone synthesis?

1. iodination of tyrosine to make DIT
2. addition of two DIT together to make T4 (thyroxin)

both are done by thyroid peroxidase enzyme


how are thyroid hormones secreted?

iodinated thyroglobulin (T4) travels thru apical membrane to follicular cell in endosome, which combines with lsosome to free the T4 molecules, and diffuse into blood thru basal membrane
-free T4 binds with thyroxin-binding globulin for travel thru blood


how is gene expression of thyroid hormones regulated?

T4 converts to T3 (more potent and lipophilic) to pass membranes to nucleus
-TH receptor (heterodimer made of TR monomer and RXR monomer), which is bound to TH response element (TRE)
-T3 binds TH-RXR-TRE complex to exert expression


what are physiological effects of TH?

-O2 consumption
-metabolism of fat, CHO, PRO, vits
-secretion and breakdown of other hormones
-growth and differentiation


what can Hashimoto's thyroiditis be caused by?

-production of Ab against thyroid peroxidase, Na-I symporter, or thyroglobulin or TSH receptor


what is myxedema?

severe form of hypothyroidism, especially in older women


what are problems associated with treating hypothyroidism with hormone replacement therapies?

1. contains T3 (acts rapidly, causes variable blood levels)
2. varies in potency (not stable products, hard to control dose)
3. some patients are allergic to animal products


what are 2 reasons TH replacement therapy is used?

1. replace function of gland
2. prevent further growth of thyroid tissue


when should readjustment of TH dosage be done?

after 4-6 weeks of therapy with proper clinical and laboratory evaluation (serum levels of T4 and TSH)


relationship between thyroid hormone and pregnancy?

a pregnant hypothyroid patient getting TH therapy needs to be monitored carefully
-too high or low levels could cause abnormal development


what are strategies for hyperthyroid treatment?

1. subtotal thyroidectomy + replacement of T4
2. irradiate thyroid gland (I-131) + replacement of T4
-I-131 is specific for thyroid, so not too much toxicity)
3. inhibit thyroid peroxidase activity (antithyroid drugs)
4. interfere with thyroid hormone facilitation of sympathetic activity (B-blockers)