Thyroid & Antithyroid Drugs
• Thyroid gland secretes thyroid hormones
Triiodothyronine (T3)
Thyroxine (T4)
calcitonin
Pharmacological actions of thyroid
hormons
• On carbohydrate metabolism
• ↑ Glycogenolysis
• ↑ Gluconeogenesis
• ↑ Glucose absorption from GIT
• Enhance glycolysis (Rapid uptake of glucose
by the cells)
• Net result – Increased blood glucose levels
On protein metabolism-
↑ protein catabolism
On fat metabolism
↑ mobilisation of fat
Oxidation of fatty acids
On BMR-
↑ Basal metabolic rate
• On growth-
↑ growth
On GIT-
Increase appetite and food intake
↑ rate of secretion of digestive juice
↑ GI motility
On CVS-
↑ tissue sensitivity to catecholamines
↑ cardiac output
On nervous system
Excitable effect
Plays a role in development of brain in fetal and 1st
few weeks of postnatal life.
Muscle weakness due to protein catabolism
Synthesis of thyroid hormone
• Transport of iodide into thyroid gland by
Sodium iodide symporter
Oxidation of iodide by thyroperoxidase to
iodine.
Tyrosine in thyroglobulin is iodinated and forms
monoiodo tyrosine(MIT) and
diiodotyrosine(DIT).
• Iodotyrosine condensation within
thyroglobulin molecule
MIT+ DIT→ Triiodo thyronine(T3)
DIT+DIT → Thyroxine T4
T4,T3,MIT and DIT are rekeased from
thyroglobulin by exocytosis & proteolysis of
thyroglobulin.
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• Thyroid hormones (T4 % T3) transported in
plasma.
• They bound to protein thyroxine binding
globulin in reversible manner.
• Only about 0.04% of total T4 & 0.4% T3 exist
in the free form.
Thyroid drugs
• Levothyroxine (L-T4)
• Levothyronine (T3)
• They produce all the effects via binding to
nuclear receptors,which induce new protein
generation which produce effects
Use- short term suppression of TSH
Used to treat hypothyroidism.
Antithyroid drugs
• Classification
1.Thioamides
Ex: propylthiouracil
Methimazole
Carbimazole
Anion inhibitors
Ex: Perchlorate
Thiocyanate
• Iodinated contrast media:
Ex: Diatriazoate
Iohexol
Iodides:
Ex; KI & NaI
Rdioactive Iodine:
Ex: I 131
• Thioamides prevent hormone synthesis by
inhibiting the thyroid peroxidase catalized
reactions and blocking iodine organification.
• Blocks coupling of iodotyrosines
• Propylthiouracil and methimazole inhibits
peripheral deiodination T4 & T3.
• Their effect requires 4 weeks
• Carbimazole & methimazole are teratogenic
• Propylthiouracil is safe in pregnancy
Adverse effects
• An altered sense of taste and smell occurs
with methimazole.
• Maculopapular pruritic rash is most common
• Hepatitis and cholestatic jaundice can be fatal.
Clinical use
Used in thyrotoxicosis
For preoperatively to make euthyroid
Anion Inhibitors
• Block uptake of iodine by the gland through
competitive inhibition of the iodide transport
mechanism
• Potassium iodide block thyroidal reuptake of
iodide in patients with iodide iduced
hyperthyroidism
• Potassium perchlorate is rarely
used,associated with aplastic anaemia.
Iodides-Inhibitors of hormone release
• They inhibit organification
• Hormone release
• Decrease size and vascularity of the
hyperplastic gland.
Clinical use:
• Prophylaxis in endemic goiter
• Preparation for thyroidectomy
Adverse effects
Acute: swelling of lip, eyelid, face,edema of
larynx, fever, joint pain and thrombocytopenia
Chronic: ulcers in the mouth, salivation,
lacrimation, burning sensation in the mouth,
rhinorrhoea and GI intolerence
Radioactive iodine
Used for treatment of thyrotoxicosis
As a diagnostic tool for thyroid function test
