How is the action of succinylcholine terminated?
Succinylcholine is rapidly metabolized by
plasma cholinesterase (pseudocholinesterase) to succinylmono-choline and
choline. When 1 mg/kg of succinylcholine is injected intravenously, about 90%
is metabolized within 1 minute, so very little of the drug actually reaches the
neuromuscular junction.
Plasma cholinesterase has no effect on
succinylcholine once it has reached the neuromuscular junction. The action of
succinylcholine at the neuromuscular junction is terminated when
succinylcholine moves away from the neuromuscular junction, which occurs when
its concentra-tion gradient has reversed. When succinylcholine is first
injected, its concentration is greatest in the plasma and lowest at the
neuromuscular junction. As succinylcholine is metabolized in the serum and
extracellular space, its concentration declines and succinylcholine diffuses
away from the junction along this reversed gradient, and the clinical effect
(block) of succinylcholine decreases. The onset of blockade from 1 mg/kg is
typically 1 minute, while the normal duration of block is 5–8 minutes. Plasma
cholinesterase is produced in the liver under genetic con-trol. Its production
is related to a pair of allelic genes EU and EU. The
enzyme has a half-life of 5–12 days.
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