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Steroids Dec 2021Vecuronium bromide (Piperidinium, 1-[(2β,3α,5α,16β,17β)-3,17-bis(acetyloxy)-2-(1-piperidinyl)androstan-16-yl]-1-methyl-, bromide; Norcuron®) has been extensively...
Vecuronium bromide (Piperidinium, 1-[(2β,3α,5α,16β,17β)-3,17-bis(acetyloxy)-2-(1-piperidinyl)androstan-16-yl]-1-methyl-, bromide; Norcuron®) has been extensively used in anesthesiology practice as neuromuscular blocking agent since its launch on the market in 1982. However, a detailed crystallographic and NMR analysis of its advanced synthetic intermediates is still lacking. Hence, with the aim of filling this literature gap, vecuronium bromide was prepared starting from the commercially available 3β-hydroxy-5α-androstan-17-one (epiandrosterone), implementing some modifications to a traditional synthetic procedure. A careful NMR study allowed the complete assignment of the H, C, and N NMR signals of vecuronium bromide and its synthetic intermediates. The structural and stereochemical characterization of 2β,16β-bispiperidino-5α-androstane-3α,17β-diol, the first advanced synthetic intermediate carrying all the stereocenters in the final configuration, was described by means of single-crystal X-ray diffraction and Hirshfeld surface analysis, allowing a detailed conformational investigation.
Topics: Crystallography, X-Ray; Magnetic Resonance Spectroscopy; Models, Molecular; Molecular Structure; Neuromuscular Blocking Agents; Vecuronium Bromide
PubMed: 34655596
DOI: 10.1016/j.steroids.2021.108928 -
Dimensions of Critical Care Nursing :... 1999
Topics: Critical Care; Drug Interactions; Drug Monitoring; Humans; Neuromuscular Nondepolarizing Agents; Vecuronium Bromide
PubMed: 10640038
DOI: No ID Found -
Canadian Journal of Anaesthesia =... May 1989
Topics: Adolescent; Anesthesia; Cyclosporins; Drug Interactions; Female; Humans; Neuromuscular Junction; Vecuronium Bromide
PubMed: 2566392
DOI: 10.1007/BF03010782 -
Journal of Cardiothoracic and Vascular... Apr 1992
Topics: Cardiac Surgical Procedures; Humans; Injections, Intramuscular; Pediatrics; Vecuronium Bromide
PubMed: 1348964
DOI: 10.1016/1053-0770(92)90231-u -
Veterinary Ophthalmology Sep 2002Topical vecuronium bromide (Norcuron) and combinations with atropine and phenylephrine, were evaluated as mydriatics in juvenile double-crested cormorants (Phalacrocorax...
Topical vecuronium bromide (Norcuron) and combinations with atropine and phenylephrine, were evaluated as mydriatics in juvenile double-crested cormorants (Phalacrocorax auritus). Nine cormorants were treated with each of four protocols: 1% atropine; 4 mg/mL vecuronium bromide (total 0.16 mg/eye); atropine with vecuronium; and atropine, 2.5% phenylephrine, followed by vecuronium. Drugs were applied topically at 15-min intervals (0.01 mL/drop). Pupil diameter was measured manually every 15 min with a pupil gauge calibrated to the nearest 0.5 mm. No effect was observed with atropine alone. Average +/- SD peak pupil diameter for vecuronium, atropine/vecuronium, and atropine/phenylephrine/vecuronium were 5.4 +/- 1.1 mm, 5.7 +/- 0.8 mm and 6.2 +/- 0.4 mm, respectively; and duration of peak diameters were 38 +/- 28 min, 79 +/- 71 min and 103 +/- 58 min, respectively. The combined atropine, phenylephrine and vecuronium provided the most consistent dilation with larger average pupil size and longer average duration. No side-effects from vecuronium were observed in these birds.
Topics: Animals; Animals, Wild; Atropine; Birds; Drug Therapy, Combination; Mydriatics; Ophthalmic Solutions; Phenylephrine; Pupil; Vecuronium Bromide
PubMed: 12236864
DOI: 10.1046/j.1463-5224.2002.00231.x -
Journal of Perianesthesia Nursing :... Aug 2000Rapacuronium bromide (Raplon; Organon Inc, West Orange, NJ) is a new, fast-onset, short-duration surgical muscle relaxant. While anesthesia providers are learning how to...
Rapacuronium bromide (Raplon; Organon Inc, West Orange, NJ) is a new, fast-onset, short-duration surgical muscle relaxant. While anesthesia providers are learning how to use this new relaxant, PACU nurses must become aware of the potential problems associated with rapacuronium. This article compares and contrasts the effects of succinylcholine and rapacuronium.
Topics: Humans; Neuromuscular Nondepolarizing Agents; Postanesthesia Nursing; Vecuronium Bromide
PubMed: 11235463
DOI: 10.1053/jpan.2000.9470 -
Drugs Nov 1999Rapacuronium bromide (rapacuronium) is an aminosteroid, nondepolarising neuromuscular blocking agent (NMBA). At the recommended dose for endotracheal intubation (1.5... (Review)
Review
UNLABELLED
Rapacuronium bromide (rapacuronium) is an aminosteroid, nondepolarising neuromuscular blocking agent (NMBA). At the recommended dose for endotracheal intubation (1.5 mg/kg), an intravenous bolus of rapacuronium has a rapid onset (approximately 1.2 to 1.8 minutes) and short duration of action (10.2 to 16.5 minutes) in adults undergoing elective surgery. Rapacuronium 1.5 mg/kg produced clinically acceptable intubating conditions in 68 to 89% of these patients at about 1 minute after administration. The onset, extent and duration of action and clinical efficacy of an intubating dose of rapacuronium appeared to be similar in the general adult population, adult patients with renal or hepatic dysfunction, patients undergoing Caesarean section, and elderly, paediatric or obese adult patients. Onset time with rapacuronium 1.3 to 2.5 mg/kg (0.9 to 1.8 minutes) was similar to or slower than that with a 1 mg/kg dose of the depolarising NMBA suxamethonium chloride (0.8 to 1.2 minutes). Intubating conditions were clinically acceptable about I minute after administration in 86 to 100% of patients with rapacuronium 1.3 to 2.5 mg/kg compared with in 88 to 97% of patients with suxamethonium chloride 1 or 1.5 mg/kg. Spontaneous recovery was slower with rapacuronium than with suxamethonium chloride, but neostigmine 0.04 or 0.05 mg/kg administered 2 or 5 minutes after rapacuronium 1.3 or 1.5 mg/kg accelerated recovery. In the few available comparative clinical trials, rapacuronium 1.5 mg/kg appeared to have a more rapid onset of action than the nondepolarising NMBAs mivacurium chloride 0.25 mg/kg, rocuronium bromide 0.45 or 0.6 mg/kg or vecuronium bromide 0.07 mg/kg, and a shorter duration of action than rocuronium bromide 0.45 or 0.6 mg/kg or vecuronium bromide 0.07 mg/kg. Additional boluses (< or =3) of rapacuronium 0.5 or 0.55 mg/kg after an intubating bolus of 1.5 mg/kg provided continued skeletal muscle relaxation during short surgical procedures in adult patients. However, these patients may recover more slowly than those who receive a single bolus of the drug. Bronchospasm was the most common treatment-related adverse event with rapacuronium 0.3 to 3 mg/kg (3.4% of adult patients). Tachycardia, injection site reaction and hypotension were also reported in small proportions of patients (1.6, 1.1 and 0.9%). The overall incidence of drug-related adverse events was similar with rapacuronium 1.5 or 2.5 mg/kg or suxamethonium chloride 1 mg/kg (8 vs. 6%) but bronchospasm, tachycardia and injection site reaction tended to occur more often with rapacuronium.
CONCLUSIONS
At the recommended dose of 1.5 mg/kg, the nondepolarising NMBA rapacuronium has a rapid onset and short duration of action. It may provide a nondepolarising alternative to suxamethonium chloride for endotracheal intubation. Rapacuronium may be preferred over rocuronium bromide, vecuronium bromide or mivacurium chloride in this indication.
Topics: Animals; Clinical Trials as Topic; Humans; Intubation, Intratracheal; Neuromuscular Nondepolarizing Agents; Vecuronium Bromide
PubMed: 10595867
DOI: 10.2165/00003495-199958050-00011 -
Anaesthesia Apr 1993
Topics: Androstanols; Drug Interactions; Hemodynamics; Humans; Neuromuscular Nondepolarizing Agents; Rocuronium; Scopolamine; Vecuronium Bromide
PubMed: 8098589
DOI: 10.1111/j.1365-2044.1993.tb06973.x -
Anesthesia and Analgesia Mar 2002
Topics: Bronchial Spasm; Child; Humans; Neuromuscular Nondepolarizing Agents; Vecuronium Bromide
PubMed: 11867361
DOI: 10.1097/00000539-200203000-00001 -
British Journal of Anaesthesia Aug 1988
Topics: Bradycardia; Humans; Intraoperative Complications; Vecuronium Bromide
PubMed: 2901271
DOI: 10.1093/bja/61.2.240-b