| Class | Non-depolarising NMJ blocker |
|---|---|
| Chemistry |
Aminosteroid |
| Routes of administration |
IV or IM only |
| Absorption |
Poor absorption; minimal oral bioavailability |
| Solubility |
pKa=7.4; good water solubility |
| Distribution |
VOD= 0.2L/kg, 82% protein-bound |
| Metabolism |
Minimal metabolism (less than 1%) |
| Elimination |
10-20% cleared by the liver, 80-90% cleared by the kidney |
| Time course of action |
Half-life 110 minutes |
| Target receptor |
Nicotinic acetylcholine receptors at the neuromuscular junction |
| Mechanism of action |
Nondepolarising neuromuscular junction blocker (competitive antagonist of acetylcholine); by binding to the nicotinic acetylcholine receptor, this agent blocks the binding of acetylcholine, and prevents the cation channel from opening, thus preventing the depolarisation of the motor endplate. |
| Clinical effects |
Nondepolarising neuromuscular junction blockade; also: |
| Literature reference |
Buckett et al (1968) |
| CICM details of understanding | Level 2 |
| Mentioned around Deranged Physiology | |
| Related SAQs |