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34 Cards in this Set
- Front
- Back
What organ is responsible for Iodine organification?
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Thyroid peroxidase!
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Tyrosine residues of thyroglobulin (storage form of TH) are iodinated in the gland to form what?
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MIT(monoiodotyrosie) and DIT (diiodotyrosine)
note: T3 = MIT + DIT T4 = DIT x2 |
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High levels of iodide or thyroid hormones have what effect on TSH and TRH?
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Inhibition through negative feedback
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What cell releases the thyroid stimulating immunoglobulins that cause an increase in TH levels in pts with Graves Disease?
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Lymphocytes
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High levels of iodide have what effect of TH synthesis and release?
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inhibit synthesis and release by inhibiting iodination of tyrosine
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What causes nontoxic hypothyroidism ?
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lack of iodine,
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What is the mechanism of action of TH ?
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Enters cell => T4 converted to T3 => dimerization of steroid receptor complex => T3 activated dimers interact with DNA response elements => synthesis of RNA.
note: NO heat shock proteins! |
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What are the therapeutic uses of thyroid hormones?
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-Replacement therapy in hypothyroid individuals (myxedema)
- Pituitary TSH suppresion (thyroid carcinoma, Hashimoto's thyroiditis, diffuse non-toxic goiter) -Differential diagnosis of hyperthyroidism |
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Which drug is the treatment of choice for myxedema? It is T4 converted to T3 and has a long half life?
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Levothyroxine (Synthroid, Levoxyl, Levothroid, Tirosint, Unithroid)
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Which drug is used in patients with myxedema that can't convert T4 to T3?
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Liothyronine (Cytomel, Triosat)
- Triostat is given IV in hospital, Cytomel is given orally. - it is more potent, faster acting, shorter duration, more expensive. |
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What is the ratio of T3:T4 in Liotrix?
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4:1 of T4 to T3
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Which drugs are used to manage myxedema coma?
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IV Triostat or IV Levothyroxine
-levothyroxine is not as fast |
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What converts T4 to T3 in target cells, liver, and kidneys?
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5'deiodinase
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What are the effects of Phenytoin, Phenobarbital, and Rifambin on overall effect of thyroid hormones?
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DECREASE effect due to increase in cytochrome P450.
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What is the half life of T4 and T3?
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T4- 7 days
T3 - 1 day ( more free in plasma so it gets degraded ) |
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T/F: Patients with longstanding hypothyroidism should be given lower doses of T4 because they are extremely sensitive to the effects on the heart.
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True
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What is the clinical use of Radioactive iodine (I131)?
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It is used to remove the thyroid gland in thyrotoxicosis or thyroid carcinoma through beta particles given off by radioactive iodine.
- Favored in patients over 21 - Adv: no surgery, permanent, doesn't endager other tissue - Disadv: Delayed hypothyroidism so pt has to take t3/4 supplements |
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What drugs inhibit thyroid hormone synthesis (not release)?
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Thiomides -Propylthiouracil and Metimazole (Tapozole)
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What is the mechanism of Thioamides like Propylthiouracil and Methimazole?
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- Block thyroid peroxidase -> block iodine organification (oxidation reaction for iodinationof tyrosine residues of thyroglobulin)
- Blocks coupling of DIT and MIT (T3) -High dose PTU blocks conversion of T4 to T3 |
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Why are Propylthiouracil and Methimazole NOT effective in management of thyroid storm alone?
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Slow onset of action and equires 3-4 weeks for full effectW
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What is the safest antuthyroid drug to administer to a pregnant woman because it is less likely to cross the placenta and enter breast milk?
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Propylthiouracil (PTU)
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What are the adverse side effects of Propylthiouracil and Methimazole?
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- SEVERE IMMUNE REACTIONS SUCH AS AGRANULOCYTOSIS !
- skin rash, edema, hepatotoxicity, jaundice, nephritic, arthralgia, nausea, vomiting, drug fever |
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What is the mechanism of action of Lugol's strong iodine and Saturated solution of potassium iodide (SSKI)?
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-Inhibit BOTH organification and release of thyroid hormone
-Reduce both size and vascularity of hyperplastic thyroid (beneficial for prior to thyroidectomy) -Rapid onset (2-7 days) and transient effects (wear off so rarely given alone) |
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What is the clinical use of Lugol's strong iodine and Saturated solution of potassium iodide (SSKI)?
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-Management of "thyroid storm"
-Severe thyrotoxicosis - Surgical resection preparation |
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What is the mechanism of action of Diatrizoate (Hypaque) and Ihexol (omnipaque)?
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- Decrease conversion of T4 to T3 via 5'deiodinase in liver, kidney, and other peripheral tissue
- Inhibits thyroid hormone release through feedback inhibition |
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What is the clinical use of Diatrizoate (Hypaque) and Ihexol (omnipaque)?
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Rapid decrease in T3 levels in thyrotoxicoses or thyroid storm in Emergency situation
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What drugs are useful in managing manifestations of thyrotoxicosis such as tachycardia?
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B-Blockers
-note: Propranolol also inhibits 5'deiodinase |
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What is the mechanism of action of Lugol's strong iodine and Saturated solution of potassium iodide (SSKI)?
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-Inhibit BOTH organification and release of thyroid hormone
-Reduce both size and vascularity of hyperplastic thyroid (beneficial for prior to thyroidectomy) -Rapid onset (2-7 days) and transient effects (wear off so rarely given alone) |
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What is the clinical use of Lugol's strong iodine and Saturated solution of potassium iodide (SSKI)?
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-Management of "thyroid storm"
-Severe thyrotoxicosis - Surgical resection preparation |
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What is the mechanism of action of Diatrizoate (Hypaque) and Ihexol (omnipaque)?
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- Decrease conversion of T4 to T3 via 5'deiodinase in liver, kidney, and other peripheral tissue
- Inhibits thyroid hormone release through feedback inhibition |
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What is the clinical use of Diatrizoate (Hypaque) and Ihexol (omnipaque)?
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Rapid decrease in T3 levels in thyrotoxicoses or thyroid storm in Emergency situation
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What drugs are useful in managing manifestations of thyrotoxicosis such as tachycardia?
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B-Blockers
-note: Propranolol also inhibits 5'deiodinase (t4->t3) |
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If Beta-Blockers are contraindicated, that is used to manage manifestation of thyroid storm?
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Calcium channel blockers - Diltiazem (Cardizem)
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What is the therapy indicated for a patient with "thyroid storm" ?
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-Proponolol or Diliazem to control manifestations
- SSKI or Lugol's to inhibit release - PTU or Methimazole to inhibit synthesis - Supportive - cool patient down. |