| Class | 5-HT3 receptor antagonist |
|---|---|
| Chemistry |
Carbazole |
| Routes of administration |
IV, IM, s/c |
| Absorption |
Rapidly and completely absorbed, bioavailability ~ 60% |
| Solubility |
pKa 9.4, freely soluble in water |
| Distribution |
VOD=2.4 L/kg, 65% protein-bound |
| Metabolism |
Undergoes extensive hepatic metabolism, mainly by CYP 1A1 |
| Elimination |
Clearance is almost completely hepatic; only some minimal amount is eliminated by the kidneys |
| Time course of action |
Half life of 9 hours, but the duration of effect is over 24 hours |
| Target receptor |
5-HT3 serotonin receptor antagonist - which are ligand-gated cation channels and which mainly conduct depolarising sodium and potassium currents |
| Mechanism of action |
Main mechanism of antiemetic activity is the antagonism of 5-HT3 ligand-gated cation channels at the chemoreceptor trigger zone. No anticholinergic or antidopaminergic effects, and therefore no effects on gastric motility or nausea related to vertigo |
| Clinical effects |
#NAME? |
| Literature reference |
Plosker & Goa, 1991 |
| CICM details of understanding | Not specifically listed in the CICM syllabus |
| Mentioned around Deranged Physiology | |
| Related SAQs |