17 The thyroid Flashcards
17.01 THYROID HORMONE SUPPRESSION
Carbimazole, propylthiouracil - actions
gradually decreases thyroid hormone output and thus reduces signs and symptoms of thyrotoxicosis
17.01 THYROID HORMONE SUPPRESSION
Carbimazole, propylthiouracil - MOA
reduces the synthesis of thyroid hormones by inhibiting thyroperoxidase which normally iodinates tyrosyl residues in thyroglobulin to give the precursors of T3 and T4
17.01 THYROID HORMONE SUPPRESSION
Carbimazole, propylthiouracil - abs/distrib/elim
given orally
carbimazole is converted to methimazole, plasma half-life 6-15h
17.01 THYROID HORMONE SUPPRESSION
Carbimazole, propylthiouracil - clinical use
hyperthyroidism
the clinical response may take several weeks because the thyroid stores of hormone need to be depleted and T4 has a long half-life
17.01 THYROID HORMONE SUPPRESSION
Carbimazole, propylthiouracil - adverse effects
agranulocytosis (rare - incidence 0.1–1.2%)
rashes (more common)
joint pains
17.02 THYROID HORMONE REPLACEMENT
Levothyroxine (synthetic T4); similar: liothyronine (T3) - actions
increased metabolism of carbohydrates, proteins and fats
increase in basal metabolic rate
17.02 THYROID HORMONE REPLACEMENT
Levothyroxine (synthetic T4); similar: liothyronine (T3) - MOA
the drug enters cells and is converted to T3, which enters the nucleus and binds to a thyroid hormone receptor
the complex activates transcription, resulting in the generation of mRNA and the synthesis of proteins and enzymes responsible for the metabolic actions of T4
17.02 THYROID HORMONE REPLACEMENT
Levothyroxine (synthetic T4); similar: liothyronine (T3) - abs/distrib/elim
given orally
long half-life
an IV formulation of liothyronine is available
17.02 THYROID HORMONE REPLACEMENT
Levothyroxine (synthetic T4); similar: liothyronine (T3) - clinical use
hypothyroidism
liothyronine injection is used for myxoedema coma
17.02 THYROID HORMONE REPLACEMENT
Levothyroxine (synthetic T4); similar: liothyronine (T3) - adverse effects
nervousness, palpitations, insomnia, heat intolerance, weight loss
17.02 THYROID HORMONE REPLACEMENT
Levothyroxine (synthetic T4); similar: liothyronine (T3) - special points
best given on an empty stomach since some foods can interfere with absorption