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Management of GI and Endocrine Conditions > Lecture 23 - Chemistry of Thyroid Treatments > Flashcards

Lecture 23 - Chemistry of Thyroid Treatments Flashcards

1
Q

Two thyroid hormones?

A

Thyroxine (T4)

Triiodothyronine (T3)

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2
Q

How are thyroid hormones transported in the blood?

A

bound to proteins

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3
Q

How active are thyroid proteins?

A

active in unbound form and have function in almost all cells

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4
Q

What does the thyroid gland convert tyrosine to?

A

monoiodotyrosine (MIT) and diiodotyrosine (DIT)

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5
Q

What do TSH and TRH act as?

A

a system to regulate production of T3 and T4

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6
Q

What converts T4 to T3

A

5’- deionase enzyme

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7
Q

MIT and DIT give?

A

T3

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8
Q

DIT and DIT give?

A

T4

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9
Q

How do disease states alter the thyroid system?

A

by changing the chemistry

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10
Q

Hypothyroidism?

A

underproduction of the thyroid hormones

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11
Q

Hypothyroidism causes?

A

insufficient iodine in the diet, Hashimoto’s thyroiditis, inflammation to the thyroid gland (lymphocytic thyroiditis)

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12
Q

Hyperthyroidism?

A

overproduction of the thyroid hormones

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13
Q

Hyperthyroidism causes?

A

overactive thyroid gland producing excess thyroid hormones

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14
Q

Hypothyroidism treatment?

A

levothyroxine and liothyronine

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15
Q

Levothyroxine physiochemistry?

A

log P = 7.4

pKa = 10, 9, 4

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16
Q

Liothyronine physiochemistry?

A

log P = 6

pKa = 10, 9, 4

17
Q

What allows conversion of levothyroxine and liothyronine to salts?

A

The carboxylic acid functional group

18
Q

How are levothyroxine and liothyronine given?

A

orally to replace deficient thyroid hormones

can be given by IM injection if required

19
Q

How do anti thyroid drugs work?

A

by preventing the synthesis of thyroid hormones

20
Q

Carbimazole physiochemistry?

A

log P = 0.3

21
Q

What is carbimazole?

A

a prodrug

converted to methimazole

22
Q

Methimazole physiochemistry?

A

log P = -0.3

23
Q

What does carbimazole lose to become methimazole?

A

the methyl group and the ester group, this decreases the log P

24
Q

What does active methimazole do?

A

inhibits thyroid peroxidases which convert tyrosine to MIT and DIT

25
Q

What does no MIT and DIT mean?

A

no T3 and T4

26
Q

Propythiouracil physiochemistry?

A

Log P = 0.4

27
Q

How does propythiouracil work?

A

inhibits thyroid peroxidases which convert tyrosine to MIT and DIT

28
Q

What else does propythiouracil do?

A

inhibits 5’-deionase enzymes helping to stop T3 biosynthesis

29
Q

How are carbimazole and propythiouracil administered?

A

as tablets

Management of GI and Endocrine Conditions (24 decks)

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