DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

Table 11–2
Classification of Neuromuscular Blocking Agents
TIME OF CLINICAL
CHEMICAL PHARMACOLOGICAL ONSET DURATION MODE OF
AGENT CLASS PROPERTIES (MIN) a (MIN) a ELIMINATION
Succinyl Dicholine ester Ultrashort 0.8-1.4 6-11 Hydrolysis
choline duration; by plasma
(ANECTINE, depolarizing cholinesterases
others)
D-Tubocurarine b Natural alkaloid Long duration; 6 80 Renal and hepatic
(cyclic benzyl- competitive elimination
isoquinoline)
Metocurine b Benzylisoquinoline Long duration; 4 110 Renal elimination
competitive
Atracurium Benzylisoquinoline Intermediate 3 45 Hofmann
(TRACRIUM, duration; elimination;
others) competitive hydrolysis by
plasma esterases
Cisatracurium Benzylisoquinoline Intermediate 2-8 45-90 Hofmann and
(NIMBEX) duration; renal elimination
competitive
Doxacurium b Benzylisoquinoline Long duration; 4-8 120 Renal elimination
competitive
Mivacurium Benzylisoquinoline Short duration; 2-3 15-21 Hydrolysis by
competitive
plasma
cholinesterases
Pancuronium Ammonio steroid Long duration; 3-4 85-100 Renal and hepatic
(generic) competitive elimination
Pipecuronium b Ammonio steroid Long duration; 3-6 30-90 Renal elimination;
competitive
hepatic
metabolism and
clearance
Rocuronium Ammonio steroid Intermediate 0.9-1.7 36-73 Hepatic
(ZEMURON, duration; elimination
others)
competitive
Vecuronium Ammonio steroid Intermediate 2-3 40-45 Hepatic and renal
(NORCURON, duration; elimination
others)
competitive
Gantacurium c Asymmetric Ultra-short 1-2 5-10 Cysteine adduction
mixed-onium duration, and ester
chlorofumarate competitive hydrolysis
a
Time of onset and clinical duration achieved from dose ranges in Table 11–3.
b D-Tubocurarine, doxacurium, metocurine, and pipecuronium are no longer available in the U.S.
c
Gantacurium is in investigational status.
of vagal responses, and histamine release. The prototypical ammonio
steroid, pancuronium, induces virtually no histamine release;
however, it blocks muscarinic receptors, and this antagonism is
manifested primarily in vagal blockade and tachycardia. Tachycardia
is eliminated in the newer ammonio steroids, vecuronium and
rocuronium.
The benzylisoquinolines appear to be devoid of vagolytic and
ganglionic blocking actions but show a slight propensity to cause
histamine release. The unusual metabolism of the prototype compound
atracurium and its congener mivacurium confers special indications
for use of these compounds. For example, atracurium’s
disappearance from the body depends on hydrolysis of the ester