| Class | Noradrenaline/dopamine reuptake inhibitor |
|---|---|
| Chemistry |
Aminoketone |
| Routes of administration |
Oral only |
| Absorption |
Oral absorption is close to 100%; bioavailability is about 20% but this does not matter as the first pass metabolite is active |
| Solubility |
pKa 7.9; highly soluble in both water and lipid |
| Distribution |
VOD=19L/kg; 84% protein bound |
| Metabolism |
Hepatic metabolism by CYP2B6, into an active metabolite (hydroxybupropion) |
| Elimination |
The majority of parent drug and metabolites are eliminated in the urine as glycine conjugates |
| Time course of action |
Elimination half-life is about 18 hours |
| Target receptor |
Serotonin reuptake transport protein (SCL6A4, or SERT) as well as dopamine reuptake transporter (DAT) |
| Mechanism of action |
By inhibiting the reuptake of serotonin and dopamine from the synaptic cleft, SSRI/SDRI drugs increase monoamine neurotransmission, which is thought to be involved in mood regulation. |
| Clinical effects |
Dry mouth, constipation, headache, nausea, insomnia and weight loss. The most common reason for discontinuation is apparently "an unpleasant state variously described as a crazy feeling". |
| Literature reference |
Foley et al (2006) |
| CICM details of understanding | Not specifically listed in the CICM syllabus |
| Mentioned around Deranged Physiology | |
| Related SAQs |