Comparative Pharmacology of Cisatracurium (51W89), Atracurium, and Five Isomers in Cats

@article{Wastila1996ComparativePO,
  title={Comparative Pharmacology of Cisatracurium (51W89), Atracurium, and Five Isomers in Cats},
  author={William B. Wastila and R. B. Maehr and Geoffrey L. Turner and D A Hill and M. Phil and John J. Savarese},
  journal={Anesthesiology},
  year={1996},
  volume={85},
  pages={169-177}
}
Background Atracurium has four chiral centers and the marketed product is a mixture of ten optical and geometric isomers. Six of the isomers were prepared and evaluated for neuromuscular blocking activity and autonomic effects in anesthetized cats. This study reports the comparative pharmacology of the six isomers and atracurium that led to the selection of one isomer, cisatracurium (Nimbex, 51W89) for clinical development. Methods Purpose bred cats, anesthetized with alpha-chloralose (80 mg/kg… 
The use of the nondepolarizing neuromuscular blocking drug cis-atracurium in dogs.
TLDR
Cis-atracurium is an effective neuromuscular blocking agent in the dog, although its potency varies, and may prove useful in dogs with impaired renal and or hepatic function.
Cisatracurium besilate. A review of its pharmacology and clinical potential in anaesthetic practice.
TLDR
Comparisons with vecuronium provide some indication of the potential of cisatracurium besilate as an intermediate-duration neuromuscular blocking agent but further comparisons with other like agents are required to define precisely its relative merits.
COMPARISON OF EFFICACY OF ATRACURIUM VERSUS CISATRACURIUM IN PATIENTS UNDERGOING SURGERIES UNDER GENERAL ANAESTHESIA
TLDR
2 x ED 95 dose of Atracurium is more effective neuromuscular blocking agent than 2 x ED95 dose of Cisatracurum providing rapid onset of action with similar duration of action, stable hemodynamic status and with no associated signs of histamine release.
Comparison of the cardiovascular effects of cisatracurium and vecuronium in patients with coronary artery disease
TLDR
In patients with coronary artery disease, rapid cisatracurium boluses and vecuronium (6×ED95) result in minor, clinically insignificant haemodynamic side effects.
Dose-response relationships for edrophonium and neostigmine antagonism of atracurium and cisatracurium- induced neuromuscular block
  • M. Naguib, W. Riad
  • Medicine
    Canadian journal of anaesthesia = Journal canadien d'anesthesie
  • 2000
TLDR
Although there were differences at five minutes, neostigmine:edrophonium potency ratios at 10 min, were similar in both relaxants studied, and nestigmine was equally effective against atracurium and cisatracuria with respect to TI recovery.
Comparison of the car- diovascular effects of cisatracurium and vecuro- nium in patients with coronary artery disease
TLDR
In patients with coronary artery disease, rapid cisatracurium boluses and vecuronium (6xED9s) result in minor, clinically insignificant haemodynamic side effects.
Cisatracurium Besilate
TLDR
Comparisons with vecuronium provide some indication of the potential of cisatracurium besilate as an intermediate-duration neuromuscular blocking agent but further comparisons with other like agents are required to define precisely its relative merits.
Pharmacodynamic and Pharmacokinetic Study on the Neuromuscular Blocking Action of Rapacuronium: a Comparison with Other Muscle Relaxants
TLDR
Rapacuronium can be considered a valid alternative to succinylcholine and had no observed cardiovascular effect.
Preclinical Pharmacology of GW280430A (AV430A) in the Rhesus Monkey and in the Cat: A Comparison with Mivacurium
TLDR
These experiments show a much shorter neuromuscular blocking effect and much-reduced side effects in the case of GW280430A vis-à-vis mivacurium, and suggest further evaluation in human subjects.
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References

SHOWING 1-10 OF 14 REFERENCES
The Clinical Neuromuscular Pharmacology of 51W89 in Patients Receiving Nitrous Oxide/Opioid/Barbiturate Anesthesia
TLDR
51W89 is a potent nondepolarizing neuromuscular blocking agent that shows noncumulative intermediate‐duration neuromUScular blocking pharmacodynamics and is well tolerated in patients undergoing elective surgical procedures.
Pharmacodynamic effects of 51W89, an isomer of atracurium, in children during halothane anaesthesia.
TLDR
51W89 is regarded as a promising, non-cumulative, intermediate-acting neuromuscular blocking agent the effects of which can be antagonized easily by neostigmine.
Structure: action Relationships Among Some Desacetoxy Analogues of Pancuronium and Vecuronium in the Anesthetized Cat
TLDR
Results showed that the greater neuromuscular blocking potency of pancuronium and vecuronium is lost after removal of one or both of the acetylcholine moieties, and it is suggested that a nondepolarizing equivalent of suxamethonium, when discovered, may necessarily be a drug of relatively low potency.
The Cardiovascular Effects and Histamine‐releasing Properties of 51W89 in Patients Receiving Nitrous Oxide/Opioid/Barbiturate Anesthesia
TLDR
51W89 is a benzylisoquinolinium‐type, nondepolarizing muscle relaxant that does not affect plasma histamine concentrations in healthy patients undergoing elective surgical procedures.
Cardiovascular and neuromuscular effects of dimethyl tubocurarine in anaesthetized cats and rhesus monkeys.
TLDR
The need remains for a drug resembling dimethyl tubocurarine in its highly specific action at the neuromuscular junction, but with a much shorter duration of action.
Pancuronium, gallamine, and d-tubocurarine compared: is speed of onset inversely related to drug potency?
  • A. Kopman
  • Medicine, Biology
    Anesthesiology
  • 1989
TLDR
The hypothesis that nondepolarizing neuromuscular blocking agents of low potency may have a more rapid onset of action than that seen with agents of high potency is supported.
The Pharmacokinetics of Atracurium Isomers In Vitro and in Humans
TLDR
The short half-life isomers of atracurium could be of practical usefulness in the future and require care in interpretation, as this isomer group contains isomer groups of widely varying rates of decomposition.
The Autonomic Margins of Safety of Metocurine and d‐Tubocurarine in the Cat
TLDR
The combination of higher neuromuscular blocking potency and weaker autonomic effect gives metocurine a much higher autonomic margin of safety than d-tubocurarine in the cat.
Effects on non-depolarizing neuromuscular blocking agents on peripheral autonomic mechanisms in cats.
TLDR
The absence of cardiovascular effects after the administration of neuromuscular blocking doses of Dimethyl tubocurarine would support its more extensive clinical use, but the need remains for a short-acting muscle relaxant with properties similar to those of dimethyl tubOCurarine.
Iontophoretic study of speed of action of various muscle relaxants.
The speed of action of nondepolarizing muscle relaxants is inversely related to potency. The hypothesis that this effect occurs at the end plate was tested in a frog (Rana pipiens) cutaneous pectoris
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