Thyroid and Anti-thyroid drugs Flashcards

1
Q

function Thyroid gland?

A
  • It regulates optimal growth,
    development,
    body temperature
    energy level.
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2
Q

Transport of iodide into thyroid gland by

A

Sodium/Iodide symporter

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3
Q

Transport of iodide at the apical membrane is by a transport enzyme

A

Pendrin

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4
Q

Oxidation of iodide to iodine is done at the apical membrane by

A

thyroidal peroxidase (TPO)

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5
Q

T3, T4, MIT, and DIT are released from thyroglobulin by

A

exocytosis and proteolysis

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6
Q

Transport of T3 &T4 in plasma; bound to

A

thyroxine-binding globulin

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7
Q

Metabolism of T4 is by to T3 and rT3

A

5 deiodinase enzyme

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8
Q

Abnormal thyroid stimulation occurs in Grave’s disease by TSH receptor antibody (stimulatory) that results in

A

thyrotoxicosis and ophthalmopathy

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9
Q

Mechanism of action of Thyroid hormones

A

enters the nucleus (TRa & TRβ)
activates gene transcription
formation of messenger RNA
alteration of protein synthesis

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10
Q

Levo thyroxine (T4)

A

Lack of allergens
Drug of choice

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11
Q

Lio thyronine (T3)

A

Greater cardio-toxicity
Used for short-term suppression of TSH

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12
Q

Desiccated thyroid

A

Protein antigenicity ↑

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13
Q

Liotrix

A

(T4:T3)= (4:1)

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14
Q

Clinical Uses of hyperthyroidism drugs

A

 Loss of thyroid cells (Hypothyroidism)
◦ thyroid surgery
◦ radioactive iodine treatment
 Iodine deficiency (endemic goitre)
 Congenital hypothyroidism
 Hashimoto’s thyroiditis (autoimmune destruction)

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15
Q

Adverse effects of hyperthyroidism drugs

A

Early stage= angina, MI, arrhythmias
Later stage= hyperthyroidism

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16
Q

Causes of Hyperthyroidism

A
  1. Grave’s disease
  2. goiter
  3. Sub-acute thyroiditis; viral infection
17
Q

Drugs treatment of hyperthyroidism

A

1- Thioamides
2- Iodide salts/ Iodine
3- Radioactive iodine (131I)
4- B-adrenoceptor antagonists

18
Q

(Thioamides) Propylthiouracil (PTU)

A

used in pregnancy because highly protein-bound

19
Q

T or F (Thioamides) Methimazole is 10 times more potent than PTU

A

T

20
Q

Mechanism of action of Thioamides

A

 Inhibit thyroid peroxidase
 Block iodine organification
 Block coupling of iodo-tyrosine residues
 PTU inhibit peripheral conversion of T4→T3

21
Q

Adverse effects of Thioamides

A

agranulocytosis
Hepatitis (PTU) that can be fatal, and cholestatic jaundice (MTZ).
maculopapular rash

22
Q

Methimazole is preferred over PTU because it has a

A

longer half-life and a lower incidence of adverse effects

23
Q

Iodide salts/Iodine

A
  • Lugol’s solution (iodine and potassium iodide)
  • Saturated solution of potassium iodide.
24
Q

Clinical Uses of Iodide salts/Iodine

A

1- thyroidectomy
2- severe hyperthyroidism

24
Q

Mechanism of action of Iodide salts/Iodine

A

(inhibit thyroglobulin proteolysis)
inhibit iodide organification
decrease the size, vascularity, and fragility of the thyroid gland

25
Q

Adverse effects of Iodide salts/Iodine

A

Iodism: acne-form rash, swollen salivary glands, mucous membrane
ulcerations, conjunctivitis, metallic taste, rhinorrhea, bleeding disorder and drug fever.

26
Q

Reasons for limited use of Iodide salts/Iodine

A
  • increases thyroid stores of iodine
  • prevent the use of radioactive iodine
  • thyrotoxicosis
  • cross placenta
27
Q

Clinical uses of Radioactive Iodine - 131

A

Thyrotoxicosis & thyroid carcinoma

28
Q

Disadvantages (ADR) Radioactive Iodine - 131

A

Since it crosses the placenta it is contraindicated during pregnancy and lactation