Thyroid and Antithyroid Drugs
Hypothalamus- organ in the brain as well as
anterior pituitary gland (adenohypothesis)
- ones producing TRH (Thyroid releasing
hormone) which will stimulate the anterior
pituitary gland in order to release TSH
(thyroid stimulating hormone) which will
stimulate thyroid gland to secretes thyroid
hormones called T3 (triiodothyronine) and T4
(tetraiodothyronine/ thyroxine)
How does the thyroid gland or the follicular
cells of the thyroid gland produce T3 and T4?
In the thyroid gland,
1) Transport of Iodide ions
The iodide will go through a transporter called
Sodium Iodide Symporter (NIS)
What is a symporter?
When substance A goes inside the cell
substance B will also go inside through a
transporter.
2) Iodide will enter another gate channel
called Pendrin as a form of regulation.
Some people locked pendrin or has not
enough Pendrin called pendrin syndrome
3) When iodide comes inside the cell or
thyroid gland, it will deoxidize by thyroid
peroxidase (TPO). It will deoxidize from iodide
to iodine.
4) From iodine, it will now bind to tyrosine
residue in the thyroglobulin molecule that is
found inside the thyroid gland. Process is
called organification. When it binds to the
residues, you’ll have MIT
(Monoiodothyronine) and DIT
(Diiodothyronine), or your T3 and T4.
5) They will be Proteolyse or
cleave/breakdown. Most of them are restored
and recycle in iodine. But T4 and T3 are
usually released.
6) T3 and T4 will go in the blood.It will go to
peripheral tissues to target different organs
including the brain, muscles, heart, the GI
tract, lungs, and so on)
7) When T4 and T3 are already in the blood.
Some T4’s converted to T3 by an enzyme
called D1, D2, or D3. But mostly D2 which
strands for deodinases.
- Most of the thyroid gland released are T4’s
(Thyroxine).
- Due to conversion of T4 to T3, many T3’s are
seen in the blood.
T3’s is more active and potent than T4.
Drugs affecting the synthesize, inhibition of
our thyroid
Substances/drugs that may inhibit and
release of thyroid hormones
Anions,
iodides, thioamides,
iodides- blocks proteolysis,
radiation therapy,
beta blockers,
some drugs such as corticosteroids and
amiodarone (antiarrythmic drugs)
Thyroid hormones and others:
Quantity released: T4>T3
Due to conversion of D1 and D2
Potency: T4<T3
TPO (thyroid peroxidase)-- converts iodide to
iodine is stimulated by TSH-- steps for thyroid
hormone synthesis.
D1, D2 converts T4 to T3, removes iodine
that’s why deodinase
D3 produces rT3 (inactive)
T4 is absorbed in the duodenum and ileum
T3 is almost completely absorbed
TBG (Thyroid binding globulin)
In order for T4 and T3 to be active, they
should be in their free forms.
Hyperthyroidism:
Increased metabolic rate (agitated, irritable,
weight loss, palpitation, reproductive system:
amnorhhea, infertility, you’re sweating while
others are not. Heat intolerance
Hypothyroidism:
Lack of T3 and T4 hormones causes a patient
to be slow and low. Mental retardation,
cretinism, obese, slow in action. You’re cold
when others are not. Cold intolerance
Thyroid Preparations:
Thyroid hormones can be detrimental in the
management of obesity, abnormal vaginal
bleeding, or depression if thyroid hormone
levels are normal.
Half-life: Levothyroxine (T4) > Liothyronine
(T3)
There is a mixture of two called Liothrix but
not used anymore
Potency: Levothyroxine < Liothyronine
T3 should be avoided in pts with cardiac
disease. Since T3 is super potent and it is
active more than T4; cause palpitation; stress
to the heart.
Use T3 with caution for patients with
comorbidities (heartfailure, surgeries, MI,
etc.)
- All thyroid drugs are detrimental unless it is
really needed (fatal if administered if there’s
no problem)
- Preparation of choice for replacement
therapy: Levothyroxine
- Hyperthyroidism: almost similar to
SYMPATHETIC NERVOUS SYSTEM response
- Hypothyroidism: associated with
PARASYMPATHETIC response.

Antithyroid Agents (Thiamides/Anion

Inhibitors/Iodides/Radioactive iodine)
Goiter- enlargement of thyroid gland.
- It needs surgery
- Almost all the time, it needs surgery
(sometimes it cause difficulty in breathing;
trachea is compressed) ; compressed of blood
vessels in the periphery. These are
anastimosis or branch of aorta that’s why
they are large arteries.
- Butterfly shaped
- Can be caused by hyper or hypothyroidism
or genetics ( Carcinoma)
- Overactivity of thyroid gland.
Thiamides
Methimazole, PTU
- Inhibit thyroid peroxidase reactions
(conversion of iodide to iodine)
Organification (blocks binding of iodine to the
tyrosine residues of the thyroglobulin
molecule) and peripheral deamination of T4
and T3 (PTU) (inhibits conversion)
- These drugs (thiamines) collectively
interferes with the synthesis of thyroid
hormones and not release.
-Thiamides
-Methimazole is the DOC for adults and
children
-Potency: Methimazole > PTU
- PTU is used in pregnant pts, thyroid storm,
pts who cannot tolerate methimazole.
- PTU is used in pregnant patient suffering
from thyroid problems
-Methimazole readily crosses the placental
barrier
- The fetus may also experience
hypothyroidism
PTU>Methimazole (P-pregnant)
- Both of them are teratogenic but
methimazole is more teratogeic because it
can induce hypothyroidism in fetus (cretinism)
- Leads to mental retardation and other
symptoms.