Pharmacology of Thyroid

PHARMACOLOGY OF
THYROID GLANDS
dr. Siti Syarifah, M.Biomed
Fakultas Kedokteran
Universitas Sumatera Utara
Medan, April 2022
INTRODUCTION
Due to its anatomic prominence thyroid

was one of the first of the endocrine
glands to be associated with the clinical
conditions caused by its malfunctions
Thyroid Gland Physiology
Synthesis and secretion of thyroid hormones.
Metabolism of Thyroid Hormones
TH  circulates bound to plasma

protein 
1. Thyroid binding globulin (TBG)
2. Transthyretin.
T4 : predominant in the blood, but
T3 : has 4 times the physiologic activity
of T4 on target tissues.
Peripheral metabolism of thyroxine
Enzymes for deiodination : 
iodothyronine 5’ – deiodinase.
3 subtypes
1. Type I deiodinase
- expressed in the liver and kidneys.
- important for converting T4 to T3 in
the serum.
2. Type II deiodinase
- expressed in pituitary, brain and
brown fat.
- located intra cellularly
- Converted T4 to T3 locally.
3. Type III deiodinase
- responsible for T4 and T3
degradation.
T4 presence in blood acts like a buffer or
reservoir for thyroid hormone effect.
t ½ T4 in plasma :  6 days
t ½ T3 :  1 days
 Changes in thyroid hormone –

regulated functions caused by
pharmacologic intervention are generally
not observed for a period of 1 to 2 weeks.
HYPOTHALAMIC – PITUITARY –
THYROID AXIS
MECHANISM OF T.H. ACTION
EFFECTS OF T.H.
T.H. are responsible for optimal :

- Growth
- Development
of all body tissues
- Function
- Maintenance
Excess  thyrotoxicosis or hyperthyroidism.
Inadequate  hypothyroidism
T.H. is important in infancy for growth
and development of the nervous
system
Congenital deficiency of TH.
Cretinism  mental retardation

In adult :
TH regulates general body metabolism and
energy expenditure, and also some enzymes :
- Na+ - K+ - ATPase
- For catabolic and anabolic  body
temperatur increases
- Resemble the effects of symphathetic
stimulation.
Low level of TH.
- Lethargy
- Myxedema  - Hypometabolic
- Dry skin
- Coarse voice
- Cold intolerance
TREATMENT OF HYPERTHYROIDISM
Inhibitors of Iodide uptake
- Perchlorate (Cl O4-)
- Thiocyonate (SCN-) 
- Pertechnetate
Compete with iodide for uptake
via Na+/ I- symporter.
Iodide for TH synthesis

- Effect not appear for over a week
- Can cause aplastic anaemia
- Thioamine is more effective.

- Be careful for radioopaque
contrast
Inhibition of organification and
hormone release.
I. Iodides radioactive
1. 131 I-  a radioactive iodide isotope, emits
strongly -rays toxic to cells.
 Na+ / I- channel cannot distinguish
131 I- from 127 I-
131I- will destroy the thyroid gland.

Concern 
- May develop to hypothyroidism
- Long-term side-effect : thyroid cancer ?
I. IODIDE
2. Stable inorganic iodide  high levels of
iodide inhibit synthesis & release 
Wolff – Chaikoff effect
- reversible, transient
not useful for long-term theraphy.
- Reduces the size & vascularisation of
the thyroid gland
- Often administered before gland

surgery
II. THIOAMINES
Mekanisme kerja :
1. Competes with thyroglobulin (TG)
for oxidized iodide in process that
is catalyzed by the enzyme thyroid
peroxidase
2. Iodinated thioamine may also bind
to TG  TH
TH production  TSH upregulation 
thyroid gland stimulation
Thyroid gland hypertrophy
goiter
Thiomanies referred to as goitrogens.

Thioamines pharmacokinetics
Prophylthiouracil Methimazole
Abs. - rapid,  peak of - Variable
absorb in  1 hour
Bioavail, - 50 – 80% - Complex
Vol. Dist. - Total body water - id
- Accum. in thyroid - id
Metab. - Glucuronidation - id
Excr. - Kidney - id but.
slower
t½ - 1,5 hours - 6 hours
Dose : 6 – 8 hours Single dose
Propylthiouracil
- Prototype of thioamine.
- Inhibit thyroid peroxidase
- Can also inhibit peripheral T4 to T3
conversion.
- Can also deplete the level of
prothrombin.
Methimazole.
- Inhibit iodide oxidized in thyroid gland
- Is reported to cause fetal defects.
- More potent than PTU  hypothroidism.
Carbamizole: degraded to methamizole in the
body
Inhibitors of Peripheral thyroid hormone
metabolism
- Propylthiouracil *
-  - adrenergic blockers.
- Radiocontrast agents.
 - adrergic blockers.
- Symptoms of thyrotoxicosis mimic those of
sympathetic stimulation :
- Sweating
- Tremor
- Nervousness
- Tachycardia
Propranolol : most widely used and studied.
Esmolol : preferred because
- Rapid onset of action
- Short t ½ (9 minutes).
Radiocontrast agents :
- Iodinated contrast agents :

- Ipodate
P.O.
- Iopanoic acid
- Diatrizoate  I. V.
- Rapidly inhibit T4 to T3 conversion by

inhibiting 5’ – deiodinase.
TREATMENT OF HYPOTHYROIDISM
T3 or T4 ?
More active
 Lower activity but is the most
TH in blood
as a buffer
 t ½ of T4 6 days  single dose
Preparation available :
I. THYROID AGENTS :
- Levothyroxine (T4): chemically stable,
uniform potency, inexpensive
- Liothyronine (T3)
- Liotrix (a combination of a 4 : 1 ratio of
T 4 : T 3)
- Thyroid desiccated
Side Effects with Thyroid replacement therapy
- Symptomatic thyrotoxicosis
- Subclinical thyrotoxicosis ( with an
increase in bone loss)
- Atrial tachyarrhytmias
- Heart failure
- Myocardial Infarction
- Angina pectoris
II. ANTI THYROID AGENTS
1. Propyl thiouracil (PTU)

2. Methimazole (Tapazole)
3. Iodide (131I) sodium
4. Ipodate sodium
5. Potassium Iodide
- generic oral sol.
- Lugol’s solution :
- 100 mg/ml KY + 50 mg/ml iodine.
CONCLUSION
 The thyroid gland plays a vital role in the maintenance of a
normal basal metabolism in the human body. Therefore,
abnormalities in thyroid hormone levels can have far-
reaching effects on various body systems, organs and
tissues.
 Typically, such abnormalities fall into one of two

categories: hypo- or hyperthyroidism, and require effective
treatment to either replace the deficient levels of T4 in the
bloodstream or to antagonise excessive levels of
circulating thyroid hormone.

Pharmacology of Thyroid

Uploaded by

Copyright:

Available Formats

Pharmacology of Thyroid

Uploaded by

Document Information

Copyright

Available Formats

Share this document

Share or Embed Document

Sharing Options

Did you find this document useful?

Is this content inappropriate?

Copyright:

Available Formats

Pharmacology of Thyroid

Uploaded by

Copyright:

Available Formats

PHARMACOLOGY OF

dr. Siti Syarifah, M.Biomed

Due to its anatomic prominence thyroid

TH  circulates bound to plasma

 Changes in thyroid hormone –

T.H. are responsible for optimal :

Excess  thyrotoxicosis or hyperthyroidism.

Congenital deficiency of TH.

Cretinism  mental retardation

Iodide for TH synthesis

- Thioamine is more effective.

131I- will destroy the thyroid gland.

Wolff – Chaikoff effect

- Often administered before gland

Thyroid gland hypertrophy

Thiomanies referred to as goitrogens.

Abs. - rapid,  peak of - Variable

- Iodinated contrast agents :

- Rapidly inhibit T4 to T3 conversion by

1. Propyl thiouracil (PTU)

 Typically, such abnormalities fall into one of two

You might also like