| Class | Glucocorticoid |
|---|---|
| Chemistry |
Steroid |
| Routes of administration |
Oral or IV |
| Absorption |
70-100% oral bioavailability |
| Solubility |
pKa=12.42; lipid soluble; available as water-soluble salts for IV injection |
| Distribution |
VOD=0.65L/kg; 65% protein-bound (mainly to albumin) |
| Metabolism |
Metabolised extensively in the liver |
| Elimination |
Inactive metabolites are eliminated in the urine |
| Time course of action |
Half-life 4-5 hours (though biological activity persist for 36-72 hours) |
| Target receptor |
Glucocorticoid receptor, which is a cytoplasmic and nuclear receptor, that regulates gene transcription and protein synthesis (but some actions are also attributed to membrane-bound receptors and nongenomic pathways) |
| Mechanism of action |
A combination of genomic effects and nongenomic effects, where some (medium and long term) activity is mediated by the regulation of protein synthesis, and some more immediate effects are mediated by the interference in cell membrane function, intracellular second messenger systems and membrane-bound glucocorticoid receptors |
| Clinical effects |
- Immunosuppression (decreased granulocyte and lymphocyte activity) |
| Literature reference |
Czock et al (2019) |
| CICM details of understanding | Level 2 |
| Mentioned around Deranged Physiology | |
| Related SAQs |