| Class | SSRI |
|---|---|
| Chemistry |
Synthetic derivative of naphthalenamine
|
| Routes of administration |
Oral only |
| Absorption |
Complete but slow absorption (6-8 hrs); almost 100% bioavailability
|
| Solubility |
pKa 9.16; poorly water-soluble
|
| Distribution |
VOD = 20L/kg; extremely highly protein-bound (99%)
|
| Metabolism |
Hepatic metabolism, mainly by N-demethylation to from an extremely long-lived metabolite (with about 10% of the potency of the parent drug, and a half-life of about 100 hours)
|
| Elimination |
50% of the metabolites are renally excreted, and 50% of them are eliminated in the faeces, suggesting that there is some biliary excretion.
|
| Time course of action |
Half life is about 26 hours
|
| Target receptor |
Serotonin reuptake transport protein (SCL6A4, or SERT), for which it has a very high affinity |
| Mechanism of action |
By inhibiting the reuptake of serotonin from the synaptic cleft, SSRIs increase serotonergic neurotransmission, which is thought to be involved in mood regulation. |
| Clinical effects |
Agitation, diarrhoea, loss or gain of weight, vertigo; risk of serotonin syndrome with overdose |
| Literature reference |
Hiemke & Härtter (2000) |
| CICM details of understanding | Not specifically listed in the CICM syllabus |
| Mentioned around Deranged Physiology | |
| Related SAQs |