Thyroid Pharm Flashcards
Explain the synthesis of thyroid hormone?
In the thyroid gland, there are many follicles. Each follicle has a lumen surrounded by a layer of epithelium. Inside the lumen, thyroglobulin is waiting to be iodinated by iodine. As the thyroid gland takes up iodide, it is oxidized to iodine by peroxidase. Then the iodine iodinates the tyrosine residues of thyroglobulin, making DIT and MIT. Two moles of DIT with thyroglobulin gives us T4 and one MIT and one DIT with thyroglobulin gives us T3.
What three agents can block iodine from iodinating thyroglobulin?
Iodide, thioamides, and PTU
What two agents can block the production of T4 and T3 after getting DIT and MIT?
Thioamide and PTU
What agent can block proteolysis of T3 and T4?
Iodide
What 5 major agents can block peripheral conversion of T4 to T3?
Radiocontrast media, beta blockers, corticosteroids, amiodarone, and PTU
What are the two fates of T4 once in peripheral circulation?
Deiodinated to T3 or inactivated
What is the relationship between CYP 450s and thyroid hormone?
Drugs that induce CYP 450 activity increase metabolism of thyroid hormone
Of T3 and T4, which one is used as the thyroid replacement therapy of choice and why?
T4. Lower cost, more stable and longer half life.
What do we use for short term suppression of TSH?
T3
3 ways we reduce thyroid activity and the effect of thyroid hormone?
Block production, block interaction with target tissue, destroy thyroid gland with radiation or surgery.
If anti thyroid medicine is required for a pregnant lady, how do we use the two?
PTU for first semester, methimazole for second and third trimesters
4 functions of thioamides?
Blocks oxidation of iodide, blocks iodination of tyrosine residues, blocks coupling of MIT and DIT to form t3 and t4, and blocks peripheral conversion of t4 to t3.
What is the most common adverse effect of thioamides?
Rash with system effects like fever, nausea and GI problems.
What is a unique adverse effect more common to PTU and one more common to meth?
Hepatitis
Jaundice
What is the most serious complication of using a thioamide, even thought it is more rare?
Huge drop in white blood cell count.