| Class | Selective binding agent |
|---|---|
| Chemistry |
γ-cyclodextrin |
| Routes of administration |
IV only |
| Absorption |
Minimal oral bioavailability (<4%) because of degradation by digestive enzymes |
| Solubility |
pKa= 2.82; reasonable water solubility |
| Distribution |
VOD=0.16-0.20 L/kg; minimally protein-bound |
| Metabolism |
Not really metabolised |
| Elimination |
Cleared renally (which means any nondepolarising agent captured by this molecule will also be cleared renally |
| Time course of action |
Elimination half-life is about 2 hours; onset of effect is within about 3 minutes |
| Target receptor |
Rocuronium molecules are the drug target |
| Mechanism of action |
The cyclodextrin is a funnel-shaped molecule with a lipophilic core that binds the steroid ring of aminosteroid agents and traps them, preventing them from having any further activity on the neuromuscular junction. |
| Clinical effects |
Reversal of nondepolarising blockade due to rocuronium, vecuronium, and to a lesser extent pancuronium. Also: may (rarely) cause bradycardia, QT prolongation, and anaphylaxis |
| Literature reference |
Bom (2009) |
| CICM details of understanding | Level 3 |
| Mentioned around Deranged Physiology | |
| Related SAQs |