Thyroid and Anti-thyroid drugs Flashcards
function Thyroid gland?
- It regulates optimal growth,
development,
body temperature
energy level.
Transport of iodide into thyroid gland by
Sodium/Iodide symporter
Transport of iodide at the apical membrane is by a transport enzyme
Pendrin
Oxidation of iodide to iodine is done at the apical membrane by
thyroidal peroxidase (TPO)
T3, T4, MIT, and DIT are released from thyroglobulin by
exocytosis and proteolysis
Transport of T3 &T4 in plasma; bound to
thyroxine-binding globulin
Metabolism of T4 is by to T3 and rT3
5 deiodinase enzyme
Abnormal thyroid stimulation occurs in Grave’s disease by TSH receptor antibody (stimulatory) that results in
thyrotoxicosis and ophthalmopathy
Mechanism of action of Thyroid hormones
enters the nucleus (TRa & TRβ)
activates gene transcription
formation of messenger RNA
alteration of protein synthesis
Levo thyroxine (T4)
Lack of allergens
Drug of choice
Lio thyronine (T3)
Greater cardio-toxicity
Used for short-term suppression of TSH
Desiccated thyroid
Protein antigenicity ↑
Liotrix
(T4:T3)= (4:1)
Clinical Uses of hyperthyroidism drugs
Loss of thyroid cells (Hypothyroidism)
◦ thyroid surgery
◦ radioactive iodine treatment
Iodine deficiency (endemic goitre)
Congenital hypothyroidism
Hashimoto’s thyroiditis (autoimmune destruction)
Adverse effects of hyperthyroidism drugs
Early stage= angina, MI, arrhythmias
Later stage= hyperthyroidism
Causes of Hyperthyroidism
- Grave’s disease
- goiter
- Sub-acute thyroiditis; viral infection
Drugs treatment of hyperthyroidism
1- Thioamides
2- Iodide salts/ Iodine
3- Radioactive iodine (131I)
4- B-adrenoceptor antagonists
(Thioamides) Propylthiouracil (PTU)
used in pregnancy because highly protein-bound
T or F (Thioamides) Methimazole is 10 times more potent than PTU
T
Mechanism of action of Thioamides
Inhibit thyroid peroxidase
Block iodine organification
Block coupling of iodo-tyrosine residues
PTU inhibit peripheral conversion of T4→T3
Adverse effects of Thioamides
agranulocytosis
Hepatitis (PTU) that can be fatal, and cholestatic jaundice (MTZ).
maculopapular rash
Methimazole is preferred over PTU because it has a
longer half-life and a lower incidence of adverse effects
Iodide salts/Iodine
- Lugol’s solution (iodine and potassium iodide)
- Saturated solution of potassium iodide.
Clinical Uses of Iodide salts/Iodine
1- thyroidectomy
2- severe hyperthyroidism
Mechanism of action of Iodide salts/Iodine
(inhibit thyroglobulin proteolysis)
inhibit iodide organification
decrease the size, vascularity, and fragility of the thyroid gland
Adverse effects of Iodide salts/Iodine
Iodism: acne-form rash, swollen salivary glands, mucous membrane
ulcerations, conjunctivitis, metallic taste, rhinorrhea, bleeding disorder and drug fever.
Reasons for limited use of Iodide salts/Iodine
- increases thyroid stores of iodine
- prevent the use of radioactive iodine
- thyrotoxicosis
- cross placenta
Clinical uses of Radioactive Iodine - 131
Thyrotoxicosis & thyroid carcinoma
Disadvantages (ADR) Radioactive Iodine - 131
Since it crosses the placenta it is contraindicated during pregnancy and lactation