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At least 19 recordsLinked to original sources
PubMed1999

Effects of non-depolarizing neuromuscular blocking agents on norepinephrine release from human atrial tissue obtained during cardiac surgery.

We have studied the effect of non-depolarizing neuromuscular blocking agents, at concentrations present in serum during anaesthesia, on release of [3H]-norepinephrine ([3H]NE) from superfused atrial appendage obtained during cardiac surgery from 48 patients. Three of the neuromuscular blocking agents (pancuronium, gallamine and rocuronium), which are known to cause an increase in heart rate during anaesthesia, increased stimulation-evoked release of [3H]NE. In contrast, (+)tubocurarine and pipecuronium, neuromuscular blocking agents that do not cause tachycardia, did not affect release of NE. Org 9487 significantly enhanced release while SZ1677 was ineffective, even at concentrations higher than those expected after administration of a 2 x ED95 dose. Atropine enhanced release. These data suggest that the axon terminals of sympathetic nerves in human heart have muscarinic heteroreceptors whose activation by acetylcholine (ACh) released from the vagal nerve reduces release of NE. This action contributes to lowering of heart rate. Therefore, any neuromuscular blocking agent with antimuscarinic actions and capable of increasing the release of NE may produce tachycardia.

Analysis of Variance↗
PubMed2001

Muscle relaxants in paediatric day case surgery.

It has been estimated that more than 60% of all paediatric surgery is performed on a day case basis. The benefits of this type of surgery in children include reduced costs, avoidance of the stress of hospitalization and less disruption to family life. The growth of day surgery in children has been facilitated by the development of non-depolarizing neuromuscular blocking agents characterized by short and intermediate duration of action and fewer side-effects. The more rapid onset and shorter duration of action of non-depolarizing neuromuscular blocking agents in children should facilitate the use of these agents in place of succinylcholine for day case procedures.

Ambulatory Surgical Procedures↗
PubMed1999

Neuromuscular blocking agents in paediatric anaesthesia.

Neuromuscular blocking agents are used commonly in paediatric anaesthesia, both to facilitate tracheal intubation and during surgery. Paediatric patients differ from adults in certain pharmacokinetic and pharmacodynamic characteristics. However, because maturational changes in certain of these characteristics counterbalance, dosing requirements do not differ markedly with age. In general, onset is more rapid in paediatric patients than in adults. Succinylcholine is still used commonly in children, despite restrictions by regulatory authorities, because of its rapid onset and offset. However, newer non-depolarizing neuromuscular blocking agents, particularly mivacurium, rocuronium and rapacuronium, offer many of the advantages of succinylcholine without its severe adverse effects: rocuronium and rapacuronium have an onset comparable with that of succinylcholine whereas the onset of mivacurium is slightly longer. In addition, recovery from an intubating dose of either mivacurium or rapacuronium is nearly comparable with that of succinylcholine. If rapacuronium i.m. proves to have a rapid onset without prolonged duration, the remaining value of succinylcholine will diminish.

Adult↗
PubMed2004

Anaphylaxis during surgical and interventional procedures.

OBJECTIVE: To describe the current evidence-based knowledge of the causes, diagnostic evaluation, and treatment of patients with anaphylaxis associated with surgical and interventional procedures. DATA SOURCES: Articles published between 1966 and 2003 were identified in MEDLINE using the keywords anaphylactoid, anaphylaxis, anesthetics, antibiotics, cephalosporins, contrast media, colloids, flow cytometry, hypersensitivity, latex, neuromuscular depolarizing agents, neuromuscular nondepolarizing agents, penicillins, radioallergosorbent test, skin test, and vancomycin. Additional studies were identified from article reference lists. STUDY SELECTION: Relevant, peer-reviewed original research articles and reviews. RESULTS: Neuromuscular blocking agents, natural rubber latex, antibiotics, and induction agents are the most common causes of anaphylaxis during surgical and interventional procedures. Colloids, opioids, and radiocontrast media probably account for less than 10% of all reactions. Newer agents implicated in anaphylaxis include isosulphan blue and chlorhexidine. Skin tests are useful for evaluating allergic reactions to anesthetic agents and penicillins and for selecting alternative agents. Skin testing and specific IgE measurements for latex vary in allergen standardization and sensitivity and specificity, respectively. Flow cytometric allergen stimulation tests show promise in differentiating allergic from idiosyncratic ("pseudoallergic") reactions. Drug desensitization has been shown to be useful for penicillin anaphylaxis. Premedication with histamine receptor antagonists and corticosteroids helps prevent or attenuate radiocontrast media reactions. CONCLUSIONS: Anaphylaxis during surgical and interventional procedures may be difficult to evaluate because of the rapid, successive use of multiple drugs or diagnostic agents. Careful analysis of anesthetic records and diagnostic tests for all the putative agents are necessary to ensure a complete evaluation.

Anaphylaxis↗
PubMed1991

Clinical pharmacology of the neuromuscular blocking agents.

Neuromuscular blocking agents are among the most commonly used drugs during general anesthesia. They compete with acetylcholine and interfere with the transmission of nerve impulses resulting in skeletal muscle relaxation. Based on their mechanism of action, neuromuscular blocking agents are classified as either depolarizing or nondepolarizing. Succinylcholine is a short-acting depolarizing agent. Commonly used nondepolarizing agents are curare (long-acting), pancuronium (long-acting), atracurium (intermediate-acting), and vecuronium (intermediate-acting). Neuromuscular blocking agents are used clinically to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery. This article provides an overview of the physiology of the neuromuscular transmission and summarizes our current knowledge on the use of these agents during general anesthesia.

Atracurium↗
PubMed1990

Clinical observations on the neuromuscular blocking action of Org 9426, a new steroidal non-depolarizing agent.

The neuromuscular blocking effects of Org 9426, the 2-morpholino, 16-allyl-pyrrolidino derivative of the 3-desacetoxy analogue of vecuronium have been investigated in anaesthetized patients. Based on data from a pilot study, two doses, 250 and 500 micrograms kg-1 (estimated as the ED90 and 2 x ED90, respectively) were chosen. Org 9426 appeared to be six to eight times less potent than vecuronium and showed a faster rate of development of neuromuscular block, with good to excellent intubation conditions within 60 s after administration of a dose of 500 micrograms kg-1. The duration of action and the recovery index appeared to be similar to those of vecuronium. Side effects were not noted. Org 9426 may have advantages over existing non-depolarizing neuromuscular blocking agents with respect to rate of development of good intubating conditions, and is stable in aqueous solutions.

Adolescent↗
PubMed1998

Neuromuscular blocking and cardiovascular effects of Org 9487, a new short-acting aminosteroidal blocking agent, in anaesthetized animals and in isolated muscle preparations.

This study was undertaken to investigate the neuromuscular blocking profile and cardiovascular effects of Org 9487, a new aminosteroidal, non-depolarizing, neuromuscular blocking agent structurally related to vecuronium, in anaesthetized animals and in isolated muscle preparations. In in vitro functional assays of neuromuscular blocking activity, Org 9487 was between eight and 15 times less potent than vecuronium. In cats and monkeys the potency of Org 9487 was approximately one-seventh and one-twentieth, respectively, that of vecuronium. In both species, Org 9487 induced rapidly developing (onset times between 1.5 min and 1.9 min) neuromuscular paralysis, which was shorter-lasting than that of vecuronium and similar in time course to suxamethonium. The vagal: neuromuscular blocking dose ratio for Org 9487 was 3 and ganglion block was seen only at approximately 20 times the neuromuscular blocking dose. There was no evidence in the rat that Org 9487, administered at doses up to 3 mg kg-1, inhibited noradrenaline re-uptake. In anaesthetized dogs, Org 9487 (3 x 90% blocking dose) induced only relatively small and transient haemodynamic effects. The administration of clinically relevant doses of neostigmine or pyridostigmine shortened the time-course profile of Org 9487, even when administered during profound neuromuscular block. In animals, Org 9487 is a low potency, nondepolarizing neuromuscular blocking agent with a time course profile similar to that of suxamethonium. Although Org 9487 is less selective than vecuronium for the neuromuscular junction, it is unlikely to produce prohibitive cardiovascular side effects in man.

Adrenergic alpha-Agonists↗
PubMed1998

Neuromuscular blocking agents in the neurosurgical intensive care unit.

The long-term administration of neuromuscular blocking (NMB) agents in the ICU has increased in frequency the last several years. NMB agents in the ICU patient facilitate intubation and ventilatory support, decrease oxygen demand and consumption, facilitate bedside procedures and diagnostics, and potentially decrease intracranial pressure. However, NMB agents have extensive adverse effect profiles and require close monitoring. Two major classes of NMB agents exist: depolarizing and nondepolarizing. Depolarizing NMB agents work by mimicking the effect of acetylcholine at the nicotinic cholinergic receptor. Continuous depolarization inhibits repolarization, resulting in paralysis. Nondepolarizing NMB agents induce muscle paralysis by their competitive antagonism at the nicotinic cholinergic receptor. The neurosurgeon must be aware that NMB agents are paralytics only and should only be used in patients who are sedated and receiving adequate analgesia. Appropriate drug selection demands a thorough knowledge and understanding of each patient's neurologic, metabolic, and cardiovascular status and the hemodynamic, autonomic, pharmacokinetic, pharmacodynamic, and cost profiles of the NMB agents.

Humans↗
PubMed1975

Pre- and postjunctional neuromuscular blockade by carbachol.

Carbachol, when applied to the bathing Ringer solution of frog sartorius muscles, caused depolarization of the endplate and a blockade of endplate potentials (EPP's), miniature EPP's (mepp's) and the iontophoretic acetylcholine potential. In muscles treated with an analog of hemicholinium-3, alpha, alpha'bis(dimethylammonium acetaldehyde diethylacetal)-p-p'-diacetylbiphenyl dibromide (DMAE), depolarization of the endplate by carbachol was blocked and the blockade by carbachol of the iontophoretic acetylcholine potential was prevented. These responses to carbachol were attributed to a postjunctional action that was antagonized by DMAE. In contrast, the blockade by carbachol of EPP's and mepp's was enhanced in DMAE-treated muscles at a time when carbachol-induced depolarization was blocked. This response to carbachol was attributed to a pre-junctional action. Carbachol either blocked transmitter release by a mechanism that was insensitive to DMAE or enhanced the prejunctional blocking actions of DMAE. Succinylcholine had actions similar to carbachol. DMAE prevented depolarization by succinylcholine but enhanced neuromuscular blockade by succinylcholine. SKF 525-A (beta-diethylaminoethyl diphenylpropylacetate hydrochloride), like DMAE, prevented depolarization but not transmission blockade caused by carbachol.

Acetylcholine↗
PubMed1972

Action of some bisquaternary derivatives of phthalic acids and related substances on neuromuscular transmission.

1. All the bisquaternary derivatives of terephthalic acid with three methyl groups on each nitrogen atom (PK-107, PK-95, PK-97 and PK-126) were depolarizing neuromuscular blocking agents. The most active was the compound PK-97, in which the two quaternary groups are separated by sixteen atoms and are about 20 A (2 nm) apart. Activity was reduced many fold either by decreasing the separation to twelve atoms or by increasing it to eighteen atoms. It was also reduced several hundred fold when one trimethylammonium group in PK-97 was replaced by a hydrogen atom (as in PK-119).2. The presence and position of the ester groups in these compounds is important; depolarizing activity is in most cases greatest when the ester groups are the same distance from the quaternary nitrogen atoms as in acetylcholine, that is, in carbolonium, sebacoyldicholine and PK-154. The monoquaternary analogues of carbolonium and sebacoyldicholine are appreciably active, having between about one-tenth to one-fifth of the activity of their bisquaternary analogues.3. The relationships between the structure and activity of these compounds are discussed, particular consideration being given to the structure of the chain separating the quaternary groups and the arrangement of acetylcholine receptors on cells and of esterbinding groups within these receptors.

Acetylcholine↗
PubMed1981

Muscle relaxants in infants and children.

In the first 2 years of life there is physical and biochemical maturation of the neuromuscular junction of man. With this maturation there is an increase in the neuromuscular reserve (margin of safety) of the infant and a change in the contractile properties of skeletal muscle. On a weight basis neonates and young infants are resistant to both depolarizing and non-depolarizing muscle relaxants; when dosage is calculated on the basis of surface area neonates and young infants are not resistant to succinylcholine, but appear sensitive to non-depolarizing relaxants. Variation in extracellular fluid volume probably explains these differences in apparent resistance. Data relating recovery of neuromuscular transmission to plasma or tissue bath concentrations of dTc are conflicting. Awareness of the clinical response of neonates and infants to muscle relaxants and awareness of the non-neuromuscular blocking properties of relaxants in infants and children permits the use of these anesthetic adjuncts in patients of any age.

Adolescent↗
PubMed1999

A large simple randomized trial of rocuronium versus succinylcholine in rapid-sequence induction of anaesthesia along with propofol.

BACKGROUND: Rocuronium has an onset of action more rapid than other non-depolarizing neuromuscular blocking agents, but it is unclear whether it and succinylcholine give equivalent intubating conditions during rapid-sequence induction of anaesthesia. We performed this study to answer the question--are there clinically relevant differences between the use of rocuronium and succinylcholine to secure acceptable intubating conditions during rapid-sequence induction of anaesthesia with propofol? METHODS: Anaesthesia was induced using propofol 2.5 mg/kg in 349 ASA physical status grade I-IV patients who were undergoing either elective or emergency surgery. Propofol was followed immediately by either rocuronium 0.6 or 1 mg/kg or succinylcholine 1.0 mg/kg (randomly selected). Fifty seconds after the end of muscle relaxant injection laryngoscopy was performed and intubating conditions were graded by an experienced anaesthetist blind to the muscle relaxant allocation. This study design was selected so that a 10% difference in clinically acceptable intubating conditions between drugs would be detectable. RESULTS: In this setting rocuronium 1.0 mg/kg provided superior intubating conditions compared with rocuronium 0.6 mg/kg. The incidence of clinically acceptable intubating conditions with rocuronium 1.0 mg/kg and succinylcholine 1.0 mg/kg was 93.2% and 97.1% respectively, the difference being -3.9% (95% C.I. -9.7% to 1.9%). CONCLUSION: Rocuronium 1.0 mg/kg given along with propofol in a rapid-sequence induction of anaesthesia is clinically equivalent to succinylcholine 1.0 mg/kg.

Adolescent↗
PubMed2005

Development of ultra short-acting muscle relaxant agents: history, research strategies, and challenges.

Author has reviewed the literature and his own work related to the chemistry, pharmacology, and clinical aspects of new muscle relaxants. Emphasis has been placed on the basic science concepts and technologies (e.g. structure-activity relationships, nicotinic receptor pharmacology, and investigation of side effects) behind the development of rapidly and short acting nondepolarizing muscle relaxants.

Anaphylaxis↗
PubMed1992

The use of muscle relaxants in the intensive care unit.

Neuromuscular blocking agents are frequently used in the Intensive Care Unit to facilitate tracheal intubation and the application of continuous paralysis. This review will focus on various conditions of the critically ill patient such as multi-organ dysfunction, acid-base and electrolyte imbalance, prolonged immobility, multiple drug interactions and specific disease/injury processes that may affect the pharmacokinetic and pharmacodynamic behaviour of muscle relaxants. As such, due to the complex nature of the critically ill patients, the effects of neuromuscular blocking agents are unpredictable. Therefore, guidelines regarding their administration and the methodology and requirement for continuous bedside monitoring of neuromuscular function will be presented.

Humans↗