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34 Cards in this Set

  • Front
  • Back
What organ is responsible for Iodine organification?
Thyroid peroxidase!
Tyrosine residues of thyroglobulin (storage form of TH) are iodinated in the gland to form what?
MIT(monoiodotyrosie) and DIT (diiodotyrosine)

note:
T3 = MIT + DIT
T4 = DIT x2
High levels of iodide or thyroid hormones have what effect on TSH and TRH?
Inhibition through negative feedback
What cell releases the thyroid stimulating immunoglobulins that cause an increase in TH levels in pts with Graves Disease?
Lymphocytes
High levels of iodide have what effect of TH synthesis and release?
inhibit synthesis and release by inhibiting iodination of tyrosine
What causes nontoxic hypothyroidism ?
lack of iodine,
What is the mechanism of action of TH ?
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!
What are the therapeutic uses of thyroid hormones?
-Replacement therapy in hypothyroid individuals (myxedema)

- Pituitary TSH suppresion (thyroid carcinoma, Hashimoto's thyroiditis, diffuse non-toxic goiter)

-Differential diagnosis of hyperthyroidism
Which drug is the treatment of choice for myxedema? It is T4 converted to T3 and has a long half life?
Levothyroxine (Synthroid, Levoxyl, Levothroid, Tirosint, Unithroid)
Which drug is used in patients with myxedema that can't convert T4 to T3?
Liothyronine (Cytomel, Triosat)

- Triostat is given IV in hospital, Cytomel is given orally.

- it is more potent, faster acting, shorter duration, more expensive.
What is the ratio of T3:T4 in Liotrix?
4:1 of T4 to T3
Which drugs are used to manage myxedema coma?
IV Triostat or IV Levothyroxine

-levothyroxine is not as fast
What converts T4 to T3 in target cells, liver, and kidneys?
5'deiodinase
What are the effects of Phenytoin, Phenobarbital, and Rifambin on overall effect of thyroid hormones?
DECREASE effect due to increase in cytochrome P450.
What is the half life of T4 and T3?
T4- 7 days
T3 - 1 day ( more free in plasma so it gets degraded )
T/F: Patients with longstanding hypothyroidism should be given lower doses of T4 because they are extremely sensitive to the effects on the heart.
True
What is the clinical use of Radioactive iodine (I131)?
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
What drugs inhibit thyroid hormone synthesis (not release)?
Thiomides -Propylthiouracil and Metimazole (Tapozole)
What is the mechanism of Thioamides like Propylthiouracil and Methimazole?
- 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
Why are Propylthiouracil and Methimazole NOT effective in management of thyroid storm alone?
Slow onset of action and equires 3-4 weeks for full effectW
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?
Propylthiouracil (PTU)
What are the adverse side effects of Propylthiouracil and Methimazole?
- SEVERE IMMUNE REACTIONS SUCH AS AGRANULOCYTOSIS !

- skin rash, edema, hepatotoxicity, jaundice, nephritic, arthralgia, nausea, vomiting, drug fever
What is the mechanism of action of Lugol's strong iodine and Saturated solution of potassium iodide (SSKI)?
-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)
What is the clinical use of Lugol's strong iodine and Saturated solution of potassium iodide (SSKI)?
-Management of "thyroid storm"

-Severe thyrotoxicosis

- Surgical resection preparation
What is the mechanism of action of Diatrizoate (Hypaque) and Ihexol (omnipaque)?
- Decrease conversion of T4 to T3 via 5'deiodinase in liver, kidney, and other peripheral tissue

- Inhibits thyroid hormone release through feedback inhibition
What is the clinical use of Diatrizoate (Hypaque) and Ihexol (omnipaque)?
Rapid decrease in T3 levels in thyrotoxicoses or thyroid storm in Emergency situation
What drugs are useful in managing manifestations of thyrotoxicosis such as tachycardia?
B-Blockers

-note: Propranolol also inhibits 5'deiodinase
What is the mechanism of action of Lugol's strong iodine and Saturated solution of potassium iodide (SSKI)?
-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)
What is the clinical use of Lugol's strong iodine and Saturated solution of potassium iodide (SSKI)?
-Management of "thyroid storm"

-Severe thyrotoxicosis

- Surgical resection preparation
What is the mechanism of action of Diatrizoate (Hypaque) and Ihexol (omnipaque)?
- Decrease conversion of T4 to T3 via 5'deiodinase in liver, kidney, and other peripheral tissue

- Inhibits thyroid hormone release through feedback inhibition
What is the clinical use of Diatrizoate (Hypaque) and Ihexol (omnipaque)?
Rapid decrease in T3 levels in thyrotoxicoses or thyroid storm in Emergency situation
What drugs are useful in managing manifestations of thyrotoxicosis such as tachycardia?
B-Blockers

-note: Propranolol also inhibits 5'deiodinase (t4->t3)
If Beta-Blockers are contraindicated, that is used to manage manifestation of thyroid storm?
Calcium channel blockers - Diltiazem (Cardizem)
What is the therapy indicated for a patient with "thyroid storm" ?
-Proponolol or Diliazem to control manifestations

- SSKI or Lugol's to inhibit release

- PTU or Methimazole to inhibit synthesis

- Supportive - cool patient down.