THYROID and ANTITHYROID DRUGS
The hypothalamic-
pituitary-thyroid axis
Mechanism of Thyroid hormone
Biosynthesis of Thyroid
Hormone
Action of Thyroid hormones
Etiology and Pathogenesis of
hypothyroidism
Disorders of the Thyroid
Hypothyroidism
• Myxedema Coma
• Management with the use of thyroid
hormones
Hyperthyroidism
• Thyrotoxicosis
• Grave’s disease
• Can be controlled by: antithyroid drugs,
surgical thyroidectomy, destruction of
thyroid gland
Manifestations of Thyrotoxicosis and Hypothyroidism
Thyroid Function test
SYNTHETIC THYROID HORMONES
Levothyroxine – DOC
Brands:
Eltroxin – 25,50,100,150 mcg tab
Thydin – 12.5, 25,50,100,150 mcg tab
Eltroxin – 50 mcg tab
Liothyronine
Dosing Recommendations
IV (Myxedema coma)
200-500 mcg
Oral (hypothyroidism)
Adult: initially, 50-100 mcg
Child: 10-15 mcg/kg/day
Elderly: > 50 yo, initially 25-50 mcg/day
Patient Counselling
Toxicity is directly related to hormone levels
Should be taken on an empty stomach. Take
60 min before meals, 4 hrs after meal or at
bedtime
Antithyroid drugs
Thioamides
o Propylthiouracil, methimazole, carbimazole
Anion inhibitors
o Perchlorate, pertechnetate and thiocyanate
Iodides
o Lugol’s solution, potassium iodide
Radioactive Iodine
Adrenoreceptor blocking agents
o Propranolol, metoprolol and atenolol
Thioamides
Drug MOA Brands ADR
PTU Inhibits TPO Liver injury
Blocks Iodine organification agranulocytosis
Inhibits peripheral
conversion of T4 to T3
Methimazole Inhibits TPO Tapdin 5,20 mg tab Agranulocytosis
Blocks Iodine organification Tapazole 5,20 mg tab Pregnancy category D
Carbimazole Prodrug Neomercazole 5,20
mg tab
Neomerdin 5,20 mg
tab
Thiamazole Strumazole 10,30 mg
Anion inhibitors
Block uptake of iodide by the gland through
competitive inhibition of the iodide transport
mechanism
Useful for iodide-induced hyperthyroidism
Rarely used due to its association with
aplastic anemia
Iodides
Major anti-thyroids before introduction of
thioamides
Preparations: Lugol’s, KI, Iodine
Rarely used as sole therapy
Mechanism:
Inhibit organification and hormone release
Decrease the size and vascularity of
hyperplastic gland
Indication
Thyroid storm
Pre-operative preparation for thyroid surgery
Protection of thyroid against fallout in the
event of a nuclear accident
Iodine excess causing
thyroid defects
Wolff-chaikoff effect
Jod-Basedow phenomenon
Radioactive Iodine
I-131 is the only isotope used for the
treatment of thyrotoxicosis
Mechanism: destruction of thyroid gland
After oral administration, it is rapidly
absorbed, concentrated by the thyroid and
incorporated into storage follicles
Destruction of thyroid parenchyma occurred
within 6-12 weeks
Adrenoreceptor blocking
agents
Mechanism
o block the peripheral effects of thyroid hormone
o Block the peripheral conversion of T4 to T3
Can cause clinical improvement of
hyperthyroid symptoms but do not typically
alter thyroid hormone levels
Indications
It is preferred drug for:
o Patients > 21 y/o who are not pregnant/breast-
feeding
o Debilitated, cardiac or elderly who are poor
surgical risks
o Patients failing to respond to drug therapy
o Patient who had ADRs with other treatments
o Patients with recurrence after thyroid surgery
