| Class | Thyroid hormone |
|---|---|
| Chemistry |
Iodinated tyrosine derivative |
| Routes of administration |
IV (but could still be given orally) |
| Absorption |
97% oral bioavailability |
| Solubility |
pKa=8.4; reluctantly soluble in water |
| Distribution |
VOD = 1.8L/kg; less protein-bound than T4 (30 times less affinity for thyroxine-binding globulin) |
| Metabolism |
Metabolised by deiodination, by tissue deiodinases |
| Elimination |
Metabolites are further deiodinated into various inactive iodinated compounds. In overdose, some hepatic metabolism occurs, which results in enterohepatic recirculation |
| Time course of action |
Half-life 6-10 hours |
| Target receptor |
Thyroid hormone receptors, mainly nuclear receptors which act as transcription factors, tghough some are transmembrane and some are cytosolic |
| Mechanism of action |
Endocytosis by a variety of transmembrane transporters, and which binds to nuclear transcription factors to perform a variety of functions. Some actions are probably also performed by cytoplasmic and transmembrane receptors, which mediate more acute effects |
| Clinical effects |
Cardiovascular effects (acts as inodilator) |
| Literature reference |
X-gen pharmaceuticals PI document |
| CICM details of understanding | Level 3 |
| Mentioned around Deranged Physiology | |
| Related SAQs |