Biochem/physiol Actions
Bioavailable, acetylcholinesterase inhibitor with rapid onset and short duration of action.
Edrophonium chloride is a fast-acting, reversible and competitive inhibitor of acetylcholinesterase (AChE; Ki = 0.2, 0.2, and 0.4 μM in human red blood cells, purified calf forebrain, and octopus brain, respectively) with no effect on butyrylcholinesterase (BChE) activity. Edrophonium dispensing increases acetylcholine (ACh) levels in the neuromuscular junction to result in brief improvements in skeletal and muscular strength. Allosterically interacts with AChE-Serine103 and has a rapid onset of action occurring within 1 minute of administration and a short duration of action lasting 10 minutes with a very short half-life of 2–5 min (intravenous). Atropine, a competitive inhibitor of muscarinic receptors, is an ideal antidote for edrophonium.