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
Blocks Iodine organification
Inhibits peripheral
conversion of T4 to T3
Methimazole Inhibits TPO
Blocks Iodine organification
Liver injury
agranulocytosis
Tapdin 5,20 mg tab Agranulocytosis
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