Muscle-relaxant properties of a steroid bis-quaternary ammonium salt

Biggs, Rosemarie S.; Davis, M.; Wien, R.

doi:10.1007/bf02150684

Cited by 28 publications

(13 citation statements)

References 4 publications

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“…This situation was first reported for the bisquaternary amino-steroid, dipyrandium, which matched suxamethonium's short duration in the chicken, rabbit and cat but was almost three times longer in duration in the Rhesus monkey and in man (Briggs et al, 1964: Mushin and Mapleson, 1964: Bamford et al, 1976. rabbit, cat) in determining the duration of a~tion of neuromuscular blocking agents.…”

Section: Acrylic Acidsupporting

confidence: 54%

Muscle Relaxants

1995

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Originally published by Springer-Verlag Tokyo in 1995. Softcover reprint ofthe hardcover lst edition 1995 This work is subject to copyright. AII rights are reserved, whether the whole or part of the material is concerned, specifically the rights of translation, reprinting, reuse of iIIustrations, recitation, broadcasting, reproduction on microfilms or in other ways, and st<;>rage in data banks. The use of registered names, trademarks, etc. in this publication does not imply, even in the absence of a specific statement, that such names are exempt from the relevant protective laws and regulations and therefore free for general use. Product Iiability: The publisher can give no guarantee for information about drug dosage and application thereof contained in this book. In every individual case the respective user must check its accuracy by consulting other pharmaceuticalliterature. PrefaceThe Fifth International Neuromuscular Meeting was held in Tokyo from November 17 through 20, 1994, and it was my privilege to chair these proceedings. It might seem to some that everything that can be said about the pharmacology of neuromuscular blocking agents (NBA) and their antagonists, the clinical use of NBAs, and the anatomy and physiology of neuromuscular receptor sites has already been said. From the beginning of the meeting, it became clear, not surprisingly, that such is not the case.It was a tortuous path from the first recorded clinical use of a curariform substance by Lawen in 1912 to the introduction of Intocostrin by Griffith in Canada, as reported in a 1942 issue of Anesthesiology. The practice of anesthesiology and surgery was changed forever. It was to be many years before a clear understanding of the neuromuscular junction (NMJ) and receptor pharmacology emerged. Prejunctional and post junctional actions of NBAs can now be differentiated and these data are clearly presented in these proceedings. The effects of catecholamine stress, burns, immobilization, and endotoxicosis as well as those from chronic infusions of curare and succinylcholine on NMJ pertubations have been elucidated. Recent studies utilizing the tools of molecular biology have helped to explain both prolonged blockade and sudden, lethal hyperkalemia following the administration of succinylcholine.Special considerations are addressed for administering NBAs to children, the elderly, and those with impaired renal and hepatic function. The relationship between the pharmacokinetics of d-Tubocurarine (dTc) , vecuronium, and atracurium and the volume of distribution in children is discussed, as is the decreased prejunctional acetylcholine stores in neonates and infants. In the elderly, elimination of NBAs (except for atracurium and, possibly, pipecuronium) is delayed due to decreased plasma clearance. In this respect, atracurium is unique since its half-life is independent of either renal or hepatic function. Elimination pathways of the new steroidal NBAs have not been established. The reader will be reminded, however, that the influence of hepatic disease ...

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Section: Acrylic Acidsupporting

confidence: 54%

Muscle Relaxants

1995

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“…There has been some speculation about the neuromuscular blocking properties of bisquaternary steroids (Alauddin & Martin-Smith, 1962;Alauddin, Caddy, Lewis, Martin-Smith & Sugrue, 1965), and the effects of several compounds have been described in detail (Quevauviller & Laine, 1960;Khuong Huu-Laine & Pinto-Scognamiglio, 1964;Biggs, Davis & Wien, 1964;Alauddin et al, 1965). However, little work has been published on the influence of stereoisomerism on the properties of 3,17-bisquaternary steroids.…”

Section: Discussionmentioning

confidence: 99%

“…The discovery of the curarizing properties of the bisquaternary steroidal alkaloid, malouetine chloride, 3,3,20a-bisdimethylamino-5a-pregnane bismethochloride (1) (Quevauviller & Laine, 1950), prompted the syntheses in our research laboratories of several series of androstane-3,17-and pregnane-3,20-bisquatemary ammonium salts based upon the relatively rigid steroid skeleton (Biggs, Davis & Wien, 1964). The use of a steroid nucleus to confer rigidity has been discussed by Alauddin & Martin-Smith (1962) and by Stenlake (1963), and the syntheses and activity of some bisquaternary steroids have been independently reported (Khuong Huu-Laine & Pinto-Scognamiglio, 1964;Alauddin, Caddy, Lewis, Martin-Smith & Sugrue, 1965).…”

mentioning

confidence: 99%

Neuromuscular Blocking Properties of Stereoisomeric Androstane‐3, 17‐bisquaternary Ammonium Salts

Bamford

Biggs

Davis

et al. 1967

British Journal of Pharmacology and Chemotherapy

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“…The May and Baker group focused in 1963 on 3b, 17b-dipyrrolidin-1 H -yl-5a-androstane bis-methiodide, M&B 9105, later called dipyrandium (Fig. 1C) [21]. The relaxant action in man of dipyrandium chloride (M&B 9105A) was tested by Mushin and Mapleson in 1964 [22].…”

mentioning

confidence: 99%

Prelude to pancuronium and vecuronium

McKenzie

2000

Anaesthesia

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SummaryThe discovery of the neuromuscular blocking activity of malouetine isolated from Malouetia bequaertiana Woodson by Quevauviller and Laine Â in 1960 stimulated interest in aminosteroids as potential neuromuscular blockers. Alauddin (a pharmacist) and Martin-Smith (a medicinal chemist) began research in this area, which was then taken up by pharmaceutical companies. Pure pancuronium was synthesised in 1964 by Savage and his co-workers, directed by Hewett. Pharmacologists headed by Buckett discovered that pancuronium was far more potent than dtubocurarine and had minimal side-effects. Buckett quickly recognised the value of pancuronium, and his persistence resulted in successful clinical trials, followed by the commercial launch of pancuronium in 1968. Vecuronium was synthesised, tested and the studies published by Buckett, Hewett and Savage in 1973, but this was before anaesthetists called for a`clean muscle relaxant' and, furthermore, it was unstable in aqueous solution. Hence, it was only promoted for clinical trials six years later.

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Muscle-relaxant properties of a steroid bis-quaternary ammonium salt

Cited by 28 publications

References 4 publications

Muscle Relaxants

Muscle Relaxants

Neuromuscular Blocking Properties of Stereoisomeric Androstane‐3, 17‐bisquaternary Ammonium Salts

Prelude to pancuronium and vecuronium

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