Thyroid Gland
Location:
•Butterfly-shaped gland located in the front of the
neck, just below the Adam’s apple (larynx).
•Wrapped around the trachea (windpipe).
Structure:
•Two lobes (right and left) connected by a thin piece
of tissue called the isthmus.
Functions of the Thyroid Gland:
[Link] Metabolism: Controls the rate at which cells use energy.
[Link] and Development: Especially important for brain development in infants.
[Link] of Body Temperature.
[Link] Heart Rate, Blood Pressure, and Digestion.
[Link] Regulation: Through calcitonin (minor role).
Hormones Produced by the Thyroid
1. Thyroxine (T4) 2. Triiodothyronine (T3)
•Full name: Tetraiodothyronine •Full name: Triiodothyronine
•Contains 4 iodine atoms. •Contains 3 iodine atoms.
•Secreted in larger amounts (~80% of •Secreted in smaller amounts (~20%).
thyroid output). •Biologically more active (3-4 times more
•Less active, serves as a prohormone potent than T4).
that gets converted to T3 in tissues. •Most of the T3 is produced by conversion of T4
Synthesis of T3 and T4: Functions of T3 and T4:
[Link] Trapping: Thyroid cells actively [Link] Basal Metabolic Rate (BMR): Energy
transport iodide from the blood. consumption rises.
[Link] of Iodide: Iodide is oxidized to [Link] Synthesis and Degradation: Muscle
iodine. turnover.
[Link] of Tyrosine: Iodine attaches to [Link] & Lipid Metabolism: Enhances
tyrosine residues on thyroglobulin (TG). glucose absorption, lipolysis.
1. Forms Monoiodotyrosine (MIT) and [Link] Rate & Cardiac Output: Increases
Diiodotyrosine (DIT) sensitivity to catecholamines (epinephrine).
[Link] Reaction: [Link]: Heat production.
1. MIT + DIT = T3 [Link] Development: Critical in fetal and
2. DIT + DIT = T4 neonatal stages.
[Link]: Hormones stored in colloid as part [Link] Growth and Maturation.
of thyroglobulin. [Link] Health: Normal ovulation and
[Link]: On stimulation, T3 and T4 are spermatogenesis.
cleaved from thyroglobulin and released into
the bloodstream.
ANTI-THYROID DRUGS
1. Thioamides ( thyroid hormone synthesis inhibitor)
2. Iodides
3. Radioactive Iodine
4. Beta – Blockers
Class Example(s) Mechanism
Thioamides PTU, Methimazole PTU inhibits T4→T3
Iodides Lugol's Inhibit hormone release
Radioactive Iodine Iodine-131 Destroys thyroid tissue
Beta Blockers Propranolol Block β effects, inhibit T4→T3 (high dose)
Propylthiouracil (PTU)
Mechanism of Action (MOA):
1. Inhibits Thyroid Peroxidase (TPO):
•Blocks:
• Oxidation of iodide (I⁻) to iodine (I⁰)
• Iodination of tyrosine residues on thyroglobulin
• Coupling of iodotyrosine residues (MIT + DIT → T3, DIT + DIT → T4)
•Result: Decreases synthesis of both T3 and T4.
2. Inhibits Peripheral Conversion of T4 to T3:
•Unique to PTU (not seen with Methimazole)
•Reduces the active hormone (T3) in tissues.
Pharmacokinetics
Parameter Details
Absorption Rapid oral absorption
Onset Slow onset; takes 2-4 weeks for clinical effect (due to preformed T3/T4 stores)
Metabolism Liver metabolism (glucuronidation)
Excretion Renal (as inactive metabolites)
Half-life ~1-2 hours (shorter than Methimazole)
Therapeutic Uses:
[Link]
Graves' disease (autoimmune hyperthyroidism)
[Link] storm (life-threatening complication of untreated or poorly controlled
hyperthyroidism, characterized by an extreme excess of circulating thyroid hormones
(T3 and T4), leading to multi-organ dysfunction.)
[Link]-induced hyperthyroidism
1. Preferred in the 1st trimester due to lower teratogenic risk
Carbimazole
Mechanism of Action (MOA):
1. Inhibits Thyroid Peroxidase (TPO) enzyme, preventing:
•Oxidation of iodide (I⁻) to iodine (I⁰)
•Iodination of tyrosine residues
•Coupling of iodotyrosine residues (MIT + DIT → T3, DIT + DIT → T4)
2. Inhibits new thyroid hormone synthesis (T3 & T4)
•No effect on preformed hormones already stored in the thyroid gland
•No significant effect on peripheral T4 to T3 conversion (unlike PTU)
Feature Carbimazole (CBZ) Propylthiouracil (PTU)
Class Thionamide / Thioamide Thionamide / Thioamide
Prodrug Yes — converts to Methimazole No — Active form
Inhibits thyroid peroxidase (TPO), blocks Inhibits TPO and blocks peripheral T4 →
Mechanism of Action
hormone synthesis only T3 conversion
Half-life Long (~6–10 hours) Short (~1–2 hours)
Dosing frequency Once daily due to long half-life Multiple doses daily (3–4 times/day)
Rarely first-line except in specific
Preferred in general use Yes, first-line in most cases worldwide
situations
2nd & 3rd trimesters (less 1st trimester only (lower teratogenic
Preferred in pregnancy
hepatotoxicity, but mild teratogenic) risk but hepatotoxic)
Hepatotoxicity risk Lower Higher, can cause severe liver failure
Yes (can cause fetal
Crosses placenta Yes
hypothyroidism/goiter)
Use in lactation Safe with monitoring Safe with monitoring
Liver metabolism Hepatic Hepatic
Less commonly used except in thyroid
Availability Widely used globally
storm/pregnancy
Cost and convenience Cheaper, once-daily, better compliance More expensive, less convenient dosing
Lugol’s Iodine Solution
Mechanism of Action
When administered in high doses, Lugol’s Iodine or KI:
[Link] Thyroid Hormone Synthesis:
1. Blocks organification of iodide (iodination of tyrosine)
2. Prevents synthesis of T3 & T4
[Link] Hormone Release:
1. Stops pre-formed thyroid hormone secretion
2. Rapid reduction in circulating T3/T4 levels
[Link] Thyroid Vascularity and Size:
1. Reduces gland blood flow and size, especially useful pre-surgery
Pharmacokinetics
Parameter Details
Absorption Rapidly absorbed from the GI tract
Distribution Accumulates in thyroid and salivary glands
Metabolism Minimal, mostly unchanged
Excretion Excreted via kidneys
Onset of Action 24-48 hours
Therapeutic Uses (Indications): Adverse Effects
Sore throat
1. Pre-operative preparation for thyroidectomy in Mettalic Taste
Graves' disease — reduces vascularity and size Burning in mouth/throat
2. Thyroid storm / thyrotoxic crisis — rapid hormone
release block Increased salivation
3. Radiation emergencies (KI only) — blocks GI upset
radioactive iodine uptake
4. Adjunct to anti-thyroid drugs in severe
hyperthyroidism
Radioactive Iodine (I-131)
Mechanism of Action (MOA):
1. I-131 is actively taken up by the thyroid gland via the sodium-iodide symporter
2. Emits beta particles (destructive) and gamma rays (diagnostic/monitoring)
3. Beta radiation destroys thyroid follicular cells:
•Causes progressive fibrosis of the gland
•Reduces hormone production (T3/T4)
4. Gamma rays are used for scanning but have no therapeutic role.
Pharmacokinetics Therapeutic Uses (Indications):
Parameter Details
Absorption Rapidly absorbed orally [Link] (Graves’ disease)
Distribution Selectively taken up by thyroid follicular cells [Link] multinodular goiter
Metabolism Radioactive decay (half-life ~8 days) [Link] cancer (as high-dose
Excretion Urine, saliva, sweat, feces adjuvant therapy post-surgery)
Onset of [Link] scanning (low dose)
Slow — clinical effect in 4-8 weeks
Action
