Kruse - Thyroid and Antithyroid Drugs DSA Flashcards
Longer half life: T4 or T3? Which is more potent?
T4 (7 days) > T3 (1 day).
T3 is more potent, but T4 is preferred therapy for hypothyroidism as thyroid replacement.
T4 and T3 absorption may be affected by myxedema with ileus, but not by mild ____?
hypothyroidism
Agents that inhibit conversion of T4 to T3 (via inhibition of 5’-deiodinase in cytoplasm) and increase reverse-T3 (inactive) levels.
Radiocontrast agents iopanoic acid and ipodanate
***Amiodarone, B-blockers, Corticosteroids
Patients experiencing ____ are administered agents that inhibit T4 to T3 conversion to reduce T3 levels?
Thyroid storm (thyrotoxic crisis)
What drugs decrease T4 absorption?
What instructions should be given to someone who is taking T4?
Cholestyramine, colestipol, cipirofloxin, PPI, ferrous sulfate, bran, soy, coffee, antacids (aluminum hydroxide, calcium carbonate)
-Instruct to take on an empty stomach
Drugs that induce hepatic CYP450s, thus increasing metabolism of T4 and T3 are ____.
Rifampin, rifabutin, phenobarbital, carbamazepine, phenytoin, imatinib, protease inhibitors
Advantages of T4 (levothyroxine) for thyroid replacement therapy
Stability, low cost, lack of allergic foreign protein, easy lab measurement of serum levels, long 1/2 life –> 1x/day dose
Agents that interfere with production of thyroid hormone
- Thioamides (block iodide organification/oxidation in the thyroid)
- Anion inhibitors (block thyroid uptake of iodide)
- Iodide (inhibit organification, decrease size/vascularity of gland)
Agents that modify tissue response to thyroid hormone
?
Thyroid gland destruction with radiation or surgery
Radioactive iodine
Name the thioamides and function.
Methimazole, Propylthiouracil (PTU)
Used for hyperthyroidism
MOA of methimazole and Propylthiouracil (PTU)
Inhibit thyroidal peroxidase-catalyzed reactions and BLOCKS IODIDE ORGANIFICATION (Inhibit TH synthesis by blocking oxidation of iodide in the thyroid gland.)
Two pregnant woman have hyperthyroidism and need agents that interfere with production of thyroid hormone. One is in her 1st trimester, one is in her 2nd/3rd trimester. What drug is given to each?
1st trimester, give PTU
2nd/3rd trimester, give methimazole
Methimazole and Propylthiouracil (PTU) - half lives and dosing.
Methimazole - half life = 6hrs; 1x/day dose
Propylthiouracil (PTU) - half life = 1.5 hours; 3-4x/day dose
How does PTU MOA differ from methimazole?
PTU blocks peripheral conversion of T4 to T3, allowing for a significantly greater fall in T3 concentration.
Most common adverse effects of methimazole and propylthiouracil (PTU).
Maculopapular pruritic rash with possible fever, nausea, GI distress