Nicotinic Receptor Antagonists Flashcards
Non-depolarising blockers
Vecuronium / Pancuronium
MOA
Reversible competitive antagonism at muscle-type nicotinic receptors. Inhibits binding of ACh to the
receptors at the muscle end-plate. End-plate potential fails to reach the threshold for initiation and
propagation of the action potential along the muscle Fiber. Action reversed by anticholinesterases
(e.g. neostigmine)
Vecuronium / Pancuronium
Abs/Distrb/Elim
Given i.v.
Half-life 2–3h.
Substantial renal excretion (duration increased in renal failure).
Vecuronium / Pancuronium
Clinical use
In general anaesthesia – aids tracheal intubation, provides muscle relaxation for general surgery and
aids mechanical ventilation
Vecuronium / Pancuronium
Adverse effects
Tachycardia (muscarinic antagonist action).
Vecuronium / Pancuronium
Special point
Tubocurarine is the archetypal non-depolarizing neuromuscular blocker, but it has more side effects,
such as bronchoconstriction due to histamine release, and is now rarely used.