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Thyroid
Pharm
68
Medical
Kindergarten
04/27/2010

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Term
What are the steps in thyroid hormone synthesis?
Definition
Active uptake of iodide, Incorporation into Thyroglobulin by thyroidal peroxidase, Thyroglobulin molecule contains T4,T3,T2 and T1, TSH stimulates proteolysis of Thyroglobulin molecule into secreted T3 and T4
Term
What happens to T3 and T4 once in the blood stream?
Definition
Both are avidly bound to plasma proteins some T4 is converted to T3
Term
What enzyme is responsible for incorportation of Iodide to the Thyroglobulin molecule?
Definition
Thyroidal Peroxidase
Term
How much of the circulating T3 is actually converted from T4?
Definition
60%
Term
What reaction converts T4 to T3 peripherally?
Definition
Deiodization
Term
What enzyme is responsible for the Deiodization of T4 to T3 and where does it occur?
Definition
5'deiodinase found mainly in the Kidney and Liver
Term
What is the fate of T3 and T4?
Definition
They are both conjugated with Glucuronic and Sulfuric Acid which is secreted in the bile
Term
How are T3 and T4 excreted?
Definition
They are conjugated with Glucuronic acid and Sulfuric Acid which are released into the BIle in the lIver
Term
What is the MOA of Perchlorate and Thiocyanate?
Definition
Blocks active Iodidne uptake by the Thyroid Gland
Term
Which drugs inhibit thyroidal peroxidase?
Definition
Iodides, Propylthiouracil and Methimazole
Term
Does Iodide inhibit the secretion of Thyroid Hormone?
Definition
Yes
Term
What enzyme do Ipodate
Definition
Beta-Blockers, Propylthiouracil and Corticosteroids inhibit?,5'Deiodinase
Term
What drug blocks both Thyroidal Peroxidase and 5'Deiodinase?
Definition
Propylthiouracil
Term
What is Thyroxine?
Definition
T4
Term
What is Triiodothyronine?
Definition
T3
Term
What is the result of deiodinization of T4 at the 5' position?
Definition
Reverse T3
Term
Is reverse T3 active?
Definition
No
Term
What is the result of 5'-deiodinase-1 on T4?
Definition
Converted into active T3 which is more potent that T4
Term
How much more potent is T3 than T4?
Definition
5-10x, T4 is often considered a prohormone
Term
What enzyme is responsible for the conversion of T4 into T3 in the liver?
Definition
5'deiodinase-1
Term
What is the effect of TSH on thyroid release of T3 and T4?
Definition
Increases
Term
Which Hormone caused decreased T3 and $ secretion?
Definition
Somatostatin from the Hypothalamus
Term
Is TSH kept in relatively constant concentrations throughout the day?
Definition
Yes
Term
What do Thyroid Hormones regulate?
Definition
Development and Growth
Term
What effect does Thyroid Hormone have on O2 consumption and Protein Synthesis?
Definition
Increases Both
Term
What are the two thyroid hormones recepter found in a heterocomplex?
Definition
Thyroid Hormone Receptor and the Retinoid X Receptor
Term
Are thyroid Horomones bound to binding proteins in circulation?
Definition
Yes avidly
Term
Where are the Thyroid Receptors located?
Definition
In the Nucleus
Term
What is the kinetics of Thyroid Hormone effect activation?
Definition
Slow onset and Slow Offset due to work in the Nucleus
Term
What are some causes of hypothyroidism?
Definition
Hashimotos, Radiation, Congenital, Iodine Def., Drug Induced
Term
What drug reduces TSH secretion causing Hypothyroidism?
Definition
Ocreotide
Term
What drugs can inhibit Thyroid Hormone release?
Definition
Iodine itself, Amiodarone and Lithium
Term
How do bile resins such as Colestyramine cause hypothyroidism?
Definition
They can bind Thyroxine making it less bioavailable
Term
What drugs can inhibit peripheral conversion of T4 to T3 causing hypothyroidism?
Definition
Glucocorticoids and Beta-blockers
Term
What is the gold standard for treating hypothyroidism caused by anything other the drug induced?
Definition
Synthroid-Synthetic Thyroxin (T4)
Term
What is the problem with Synthroid?
Definition
It is inherently unstable when exposed to heat or light
Term
What is the main side effect associatted with Synthroid?
Definition
Cardiac Dysarthrythmias cause by the beta-adrenergic response
Term
What treatment is associatted with an increase in HR
Definition
Sweating, and Tremors?,Synthroid
Term
What can the increased cardiac work caused by over medication with Synthroid lead to?
Definition
Increased work leads to increased oxygen demands and if not met can turn into Angina
Term
What is the most senstive way to check Synthroids activity as you prescribe it?
Definition
Monitor TSH levels, also ask the patient how they feel
Term
A 45 year old is taking I-thyroxine following her thyroidectomy. Her physician tells her to take the medications at a different time of the day than one of her other medications. The most likely reason for this is:
Definition
The INtestional absorption of I-Thyroxine can be quite variable and is affected by certain medications
Term
What is a common cause of Hyperthyroidism?
Definition
Graves disease
Term
What types of drugs are used to treat hyperthyroidism?
Definition
Ionic Inhibitors, Iodine containing compounds
Term
What is the MOA of Lugol's Solution?
Definition
It is an Iodide containing compound which is concentrated in the Thyroid and prevents Thyroid Hormone Secretion
Term
What is Lugol's solution composed of?
Definition
5% iodine and 10% potassium iodine
Term
What drug is used priot to a thyroidectomy or to prevent the uptake of radioactive Iodine by the thyroid?
Definition
Lugol's Solution
Term
How long does the preventative effects of Lugols Solution last?
Definition
Short lived due to gland escaping inhibiton after a couple weeks
Term
What is radioactive iodine 131 used to treat?
Definition
Hyperthroidism,It destroys the Tyroid Gland by Beta Radiation
Term
How is Radioactive Iodine dosed? And can it be used while pregnant?
Definition
Given as a single dose of 5-15 millicuries, and No not used in pregnancy
Term
Why is radioactive iodine not used in pregnant women?
Definition
It will cross the placenta and be concentrated in the Fetal Thyroid causing its destruction
Term
What percentage of patients given radioactive iodine wind up with Hypothyroidism?
Definition
80% and 20% of those will require thyroid hormone supplementation
Term
Why is radioactive iodine only prescribed to patient over the age of 35?
Definition
There is a concern that patients will develop cancer later in life
Term
What are the tow thionamides?
Definition
Propylthiouracil and Methamizole
Term
How do the thionamides
Definition
Propylthiouracil and Methamizole work to treat hyperthyroidism?,Inhibit Thyroid Peroxidase
Term
What other enzyme can Propylthiouracil inhibit causing a double effect?
Definition
5'thiodinase-1 which converts T4 to T3
Term
What drugs can reduce thyroid immunity which can lead to a remission of Graves disease and removal of medication?
Definition
Propythiouracil and Methamizole
Term
What are the side effects of the Thionamides?
Definition
Rash, Fever, Arthralgia, and agranulocytosis
Term
Which drug can cause a serious agranulocytosis?
Definition
The Thionamides, Propylthiouracil and Methamizole
Term
Does Propylthiouracil cross the placenta or into breast milk?
Definition
No so can be used during pregnancy
Term
What drug is the 3rd leading cause of drug induced liver failure?
Definition
Propythiouracil
Term
What is a less hepatotoxic option than Propylthiouracil?
Definition
Methimazole, it will only cause reversible jaundice
Term
When is Propythiouracil use warranted?
Definition
During a Thyroid storm brough about by 5'deiodinase-1 or during pregnancy
Term
Which drugs can lead to remission and removal of medication for a hyperthyroidism patient?
Definition
Prophylthiouracil or Methimazole
Term
What is the Beta-antagonist used for treatment of hyperthyroidism?
Definition
Propanolol
Term
Why do the Thionamides take a few weeks to become effective?
Definition
The thyroid has a couple week supply of thyroid hormone it can continue to secret
Term
What are the symptoms of hyperthyroidism?
Definition
Tremors, anxiety, palpatations and a racing heart
Term
Which drug can immediately eliminate some of these symptoms?
Definition
Propanolol which blocks the sympathetic effects of Hyperthyroidism
Term
When should use of Propanolol be discontinued?
Definition
After the couple week store of Thyroid hormone is used up and Thionamides can take effect
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