Thyroid, Antithyroid Drugs

DR.dr.Asep Sukohar,M.Kes
Pharmacology and Therapy
Faculty of Medicine Lampung University
 Site of action
Pharmacokinetics

Pharmacodynamics

Duration Of action

Cost

Dosage
 Thyroid Hormone
synthesis & secretion
Secretes
Triiodothyronin (T3)
Thyroxin (T4)
Calcitonin

Uptake of iodide ion

Stimulated by TSH
Inhibited by Potassium Perchlorate

Iodination

I I2
I2 + Thyroglobulin MIT and DIT
Inhibited by methimazole & PTU
 Release
Condensation

To act in the tissues T4

T3 + I
DIT and MIT Enter the Inhibited by
T3 and T4 general PTU and
Inhibited by circulation adrenergic
Methimazole Inhibited by antagonist
and PTU Iodide
Stimulated
by TSH
 Functions of Thyroid hormone

Facilitates normal growth and maturation

Maintains the level of metabolism

Hepatic glycogenolysis
glucose storage
Inhibit gluconeogenesis
Inhibit lypolysis
Plasma amino acid
 Thyroid dysfunction

Thyroid hormone resistance & TSH secretion

Hashimotos Thyroiditis
Hypothyroidism Myxoedema
Pituitary disease

Overproduction of endogenous H
Hyperthyroidism Exposure to excess exogenous H
 Drug for Hypothyroidism
Levothyroxine
Isomer T4 , some are converted to T3
Long half life
Steady state : 6 - 8 weeks
Toxicity hyperthyroidism: Arrhythmia, tachycardia, anginal pain, etc.
Precautions: Heart disease

Liothyronine (L- Triiodothyronine sodium)

Isomer T3
OOA > rapid; DOA > shorter
RODA: p.o, iv
Indication:
- severe hypothyroidism
- 5-deiodinase deficiency: cannot convert T4
to T3
CI & AR =Levothyroxine

Liotrix (T3 &T4)

Thyroid USP & Thyroglobulin

 Treatment of Hyperthyroidism

Thioureylenes / Carbimazole, methimazole,

Thionamides (>< propylthiouracil
synthesis)

Iodide, potassium perchlorate

Anion inhibitors (><
release)

Propranolol, atenolol, etc.

Beta- adrenoceptor
antagonist (>< action)

Surgical
Radioiodine (removal Destruction by radioactive iodine (131I)
thyroid gld.) which emitted beta particles
 Inhibiting hormone synthesis

Methimazole

Carbimazole (active metabolite of

Methimazole)

Propylthiouracil

Effectiveness is delayed until stored hormone

is depleted
Not effective for thyroid storm/crisis
Adverse effects: agranulocytosis, rash, edema
 Blockade Hormone release
Drugs: Iodide

Combined with PTU or Methimazole

Effective for thyroid storm

Administered prior to surgery

Decreases the vascularity of the gland

Not useful for long-term therapy

Adverse reactions:
Ulceration of mucous membranes
Metallic taste in the mouth
rashes
 Blocking the action

T3 : active form in the tissue

To act in the tissues T4 T3

inhibited by PTU and adrenergic antagonist

adrenergic antagonist also normalizes

heart beat
THANKS

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Dan seandainya pohon-pohon di bumi menjadi pena dan lautan (menjadi
tinta), ditambahkan kepadanya tujuh lautan (lagi) setelah (kering)nya,
niscaya tidak akan habis-habisnya (dituliskan) kalimat-kalimat Allah
 QUESTION (EXAMPLE)

A patient, woman 30 years old, complain that

she feels palpitation after she takes a drug
which is used to relieve her illness. Which one
of this drugs that cause the woman symptom
?
A. Methimazole
B. Levothyroxine
C. Iodide
D. PTU
E. Propanolol
 QUESTION (EXAMPLE)

A patient, woman 30 years old, complain that

she feels palpitation after she takes a drugs
which is used to relieve her illness. Which one
of this drugs that cause the woman symptom
?
A. Methimazole
B. Levothyroxine
C. Iodide
D. PTU
E. Propanolol
 QUESTION (EXAMPLE)

Mrs. Laila, 25 years old, will has thyroidektomi

operation. For decreasing the bleeding while
operation, a surgeon gives Mrs. Laila a drug
prior the operation. What is the name of this
drug?
A. Methimazole
B. Carbimazole
C. Iodide
D. PTU
E. Propanolol

 QUESTION (EXAMPLE)

Mrs. Laila, 25 years old, will has thyroidektomi

operation. For decreasing the bleeding while
operation, a surgeon gives Mrs. Laila a drug
prior the operation. What is the name of this
drug?
A. Methimazole
B. Carbimazole
C. Iodide
D. PTU
E. Propanolol

 QUESTION (EXAMPLE)

Mrs. Novi, 26 years old, complain that she had metalic

tasted in the mouth after she had taken a drug for
relieve her illness. Since 1 years ago, she had
hyperthyroidism and has been taking this drug. What is
the name of a drug which can cause her symptom ?
A. Methimazole
B. Carbimazole
C. Iodide
D. PTU
E. Propanolol
 QUESTION (EXAMPLE)

Mrs. Novi, 26 years old, complain that she had metalic

tasted in the mouth after she had taken a drug for
relieve her illness. Since 1 years ago, she had
hyperthyroidism and has been taking this drug. What is
the name of a drug which can cause her symptom ?
A. Methimazole
B. Carbimazole
C. Iodide
D. PTU
E. Propanolol
 QUESTION (EXAMPLE)

What is the drug which can be used safely

by pregnant woman in the first semester ?
A. Propiltiourasil (PTU).
B. Methymazole
C. Iodide
D. Radioactive iodide
E. Thiocyanate (SCN)
 QUESTION (EXAMPLE)

What is the drug which can be used safely

by pregnant woman in the first semester ?
A. Propiltiourasil (PTU).
B. Methymazole
C. Iodide
D. Radioactive iodide
E. Thiocyanate (SCN)