| Class | Tricyclic antidepressant |
|---|---|
| Chemistry |
Tricyclic
|
| Routes of administration |
Oral only |
| Absorption |
Rapidly and completely absorbed; 52% oral bioavailability due to first pass effect
|
| Solubility |
pKa 10.47; insoluble in water
|
| Distribution |
VOD=21L/kg; 93% protein bound
|
| Metabolism |
Hepatic metabolism mainly by CYP2D6 into breakdown products which all have some degree of antidepressant activity
|
| Elimination |
All metabolites are renally eliminated
|
| Time course of action |
Elimination half-life of around 26 hours
|
| Target receptor |
Reuptake proteins (NET and SERT), and postsynaptic alpha-adrenergic receptors, cholinergic receptors and histamine receptors |
| Mechanism of action |
Multiple mechanisms of effect, mostly related to the inhibition of reuptake of noradrenaline and serotonin by interference with the function of SERT and NET transport proteins |
| Clinical effects |
Sedation, hypotension, anticholinergic side effects, sodium channel blockade in overdose |
| Literature reference |
Norman et al (1981) |
| CICM details of understanding | Not specifically listed in the CICM syllabus |
| Mentioned around Deranged Physiology | |
| Related SAQs |