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Intubationsbedingungen mit Org 9487
No full textDie Studie vergleicht die Intubationsbedingungen nach Applikation von Org 9487, einem neuen aminosteroidalen, nicht-depolarisierenden Muskelrelaxans, Succinylcholin und Placebo. 60 Patienten nahmen an der Doppel-Blind-Studie teil. Nach Einleitung der Narkose erfolgte eine Relaxation entweder mit 1,5 mg/kgKG Org 9487, 1 mg/kgKG Succinylcholin oder Placebo. Nach 60 Sekunden erfolgte die Intubation. Es wurde kein signifikanter Unterschied zwischen Intubationsbedingungen nach Succinylcholin und nach Org 9487 festgestellt. Die Rate klinisch akzeptabler Intubationsbedingungen lag nach Succinylcholin höher. Die Inzidenz unerwünschter Ereignisse war nach Org 9487 größer bei Succinylcholin. Als Nebenwirkungen nach Org 9487 traten lokale Intoleranz an der Injektionsstelle, leichte Tachykardie und Hypotonie auf. Succinylcholin ist nach wie vor das qualitativ bessere und zu bevorzugende Muskelrelaxans für eine Blitzintubation. Mittels Org 9487 sind jedoch annähernd gute Ergebnisse zu erreichen
Intubationsbedingungen mit Org 9487
No full textDie Studie vergleicht die Intubationsbedingungen nach Applikation von Org 9487, einem neuen aminosteroidalen, nicht-depolarisierenden Muskelrelaxans, Succinylcholin und Placebo. 60 Patienten nahmen an der Doppel-Blind-Studie teil. Nach Einleitung der Narkose erfolgte eine Relaxation entweder mit 1,5 mg/kgKG Org 9487, 1 mg/kgKG Succinylcholin oder Placebo. Nach 60 Sekunden erfolgte die Intubation. Es wurde kein signifikanter Unterschied zwischen Intubationsbedingungen nach Succinylcholin und nach Org 9487 festgestellt. Die Rate klinisch akzeptabler Intubationsbedingungen lag nach Succinylcholin höher. Die Inzidenz unerwünschter Ereignisse war nach Org 9487 größer bei Succinylcholin. Als Nebenwirkungen nach Org 9487 traten lokale Intoleranz an der Injektionsstelle, leichte Tachykardie und Hypotonie auf. Succinylcholin ist nach wie vor das qualitativ bessere und zu bevorzugende Muskelrelaxans für eine Blitzintubation. Mittels Org 9487 sind jedoch annähernd gute Ergebnisse zu erreichen
Comparison of vecuronium with ORG 9487 and their interaction
Get PDFPurpose: To compare the pharmacodynamic behaviour of vecuronium with that of ORG 9487, we measured the time-course of action of equipotent doses of ORG 9487 and vecuronium and investigated their mutual interaction when given in succession. Methods: Sixty ASA I-II patients were anaesthetized with thiopentone, fentanyl, halothane and nitrous oxide and assigned randomly to four groups. Each patient received an initial dose (ID) of either vecuronium (V) or OPG 9487 (O) followed by maintenance doses (MDn) of either V or O (ID/MD: O/O, V/O, O/V and V/V. The time course of action was measured mechanomyographically, determining the duration until 25% recovery of the single twitch (DUR25). Results: The onset time of an ID of ORG 9487 was shorter than that of an ID of vecuronium (96 vs 203 sec, P <0.001). The DUR25 of the ID of ORG 9487 was less than half that of vecuronium (10.7 +/- 2.8 vs 28.8 +/- 6.1 min, P <0.001). The DUR25 of MD1 and MD2 of ORG 9487 were shorter than those of vecuronium (O/O: 7.3 +/- 2.8 and 8.5 +/- 2.4 min; V/O: 12.7 +/- 3.3 and 11.5 +/- 3.5 min, vs O/V: 16.4 +/- 4.5 and 20.6 +/- 4.7 min; V/V: 8.8 +/- 3.0 and 20.1 +/- 3.8 min, respectively, P <0.05). An ID of vecuronium prolonged the DUR25 of MD1 and MD2 of ORG 9487 (P <0.05). Conclusion: ORG 9487 is a muscle relaxant with a shorter duration of action than vecuronium. Maintenance doses of ORG 9487 are also shorter acting than roughly equipotent maintenance doses of vecuronium, irrespective of which relaxant is given initially
Comparison of vecuronium with ORG 9487 and their interaction
No full textPurpose: To compare the pharmacodynamic behaviour of vecuronium with that of ORG 9487, we measured the time-course of action of equipotent doses of ORG 9487 and vecuronium and investigated their mutual interaction when given in succession.Methods: Sixty ASA I-II patients were anaesthetized with thiopentone, fentanyl, halothane and nitrous oxide and assigned randomly to four groups. Each patient received an initial dose (ID) of either vecuronium (V) or OPG 9487 (O) followed by maintenance doses (MDn) of either V or O (ID/MD: O/O, V/O, O/V and V/V. The time course of action was measured mechanomyographically, determining the duration until 25% recovery of the single twitch (DUR25).Results: The onset time of an ID of ORG 9487 was shorter than that of an ID of vecuronium (96 vs 203 sec, P <0.001). The DUR25 of the ID of ORG 9487 was less than half that of vecuronium (10.7 +/- 2.8 vs 28.8 +/- 6.1 min, P <0.001). The DUR25 of MD1 and MD2 of ORG 9487 were shorter than those of vecuronium (O/O: 7.3 +/- 2.8 and 8.5 +/- 2.4 min; V/O: 12.7 +/- 3.3 and 11.5 +/- 3.5 min, vs O/V: 16.4 +/- 4.5 and 20.6 +/- 4.7 min; V/V: 8.8 +/- 3.0 and 20.1 +/- 3.8 min, respectively, P <0.05). An ID of vecuronium prolonged the DUR25 of MD1 and MD2 of ORG 9487 (P <0.05).Conclusion: ORG 9487 is a muscle relaxant with a shorter duration of action than vecuronium. Maintenance doses of ORG 9487 are also shorter acting than roughly equipotent maintenance doses of vecuronium, irrespective of which relaxant is given initially.</p
Neuromuscular blocking and cardiovascular effects of Org 9487, a new short-acting aminosteroidal blocking agent, in anaesthetized animals and in isolated muscle preparations
No full textItem does not contain fulltextThis 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 reuptake. In anaesthetized dogs, Org 9487 (3 × 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.13 p
Time course of action and endotracheal intubating conditions of Org 9487, a new short-acting steroidal muscle relaxant; a comparison with succinylcholine
No full textIn a randomized study, we evaluated lag time (time from the end of injection of muscle relaxant until the first depression of the train-of-four response [TOF]), onset time (time from the end of injection of muscle relaxant until the maximum depression of the first twitch of the TOF [T1]), neuromuscular block, and endotracheal intubating conditions at 1 min after 1 mg/kg succinylcholine (n = 15) and 1.5 mg/kg Org 9487 (n = 30). Two minutes after administration of Org 9487, 15 of the 30 patients received neostigmine for reversal. Recovery of neuromuscular block after succinylcholine, Org 9487 without and Org 9487 with neostigmine were compared using the time until T1 was 90% for the succinylcholine group, and the time until TOF was 70% for the Org 9487 groups. Neuromuscular transmission was monitored mechanomyographically. Onset time was similar (67 [20] and 83 [38] s for succinylcholine and Org 9487, respectively) and endotracheal intubating conditions were also similar after both muscle relaxants. Times until clinically sufficient recovery of neuromuscular block induced by succinylcholine (time until T1 = 90%:10.6 [3.31 min) and Org 9487 with neostigmine (time until TOF = 70%: 11.6 [1.4] min) were not different. In contrast, in the Org 9487 without neostigmine group, more time was required until complete recovery (24.1 [6.2] min) (P <0.05). In conclusion, Org 9487 is a muscle relaxant suitable for endotracheal intubation and short-lasting interventions
Pharmacodynamics and pharmacokinetics of an infusion of Org 9487, a new short-acting steroidal neuromuscular blocking agent
No full textWe have evaluated in 10 anaesthetized patients the time course of action, infusion requirements, reversibility and pharmacokinetics of Org 9487. Org 9487 was administered as a bolus dose of 1.5 mg kg(-1), followed by an infusion to maintain a block of 75-85 % for 60 min. After recovery from the bolus dose, a mean dose of Org 9487 3.4 (SD 1.0) mg kg(-1) h(-1) was administered to maintain a mean neuromuscular block of 83 (3) %. During the final 15 min of infusion, the infusion requirements were 2.5 (1.1) mg kg(-1) h(-1). In the five patients who were allowed to recover spontaneously, a TOF ratio of 0.7 was reached 37.9 (12.4) min after stopping the infusion of Org 9487. In the five patients who received neostigmine, a TOF ratio of 0.7 was reached after 14.5 (6.1) min. Plasma clearance was 8.5 (30 %) ml kg(-1) min(-1). Volume of distribution at steady state was 293 (55 %) ml kg(-1). Terminal half life and mean residence time were 71.7 (34 %) and 33.4 (31 %) min, respectively. The concentration of the 3-OH metabolite remained relatively low. Urinary excretion of Org 9487 and its metabolites was 22 % in 24 h. In conclusion, a 1-h infusion of the short-acting drug Org 9487 changed its time course characteristics gradually from that of a short acting neuromuscular blocking agent to that of a neuromuscular blocker with an intermediate duration of action
Cardiovascular effects of Org 9487 under isoflurane anaesthesia in man
No full textpeer reviewedThe cardiovascular effects of Org 9487 during isoflurane anaesthesia have been evaluated using three doses around its ED90 for neuromuscular blockade, i.e. 1 mg kg-1, 2 mg kg-1 and 3 mg kg-1. Heart rate increased to 110%, 115% and 118% in patients receiving 1 mg kg-1, 2 mg kg-1 and 3 mg kg-1 respectively. There were no significant effects on systolic and diastolic blood pressures for the two lower dose groups. Patients receiving Org 9487 3 mg kg-1 displayed significant decreases in systolic and diastolic blood pressures (91% and 82% of the control values respectively). Except for heart rate in the group receiving 3 mg kg-1, all measurements returned to baseline after a maximum of 15 min. Six patients experienced a transient increase in airway pressure after administration of Org 9487, which was accompanied by a decrease in oxygen saturation in two out of six subjects, but there was no audible wheezing. These episodes were self-limiting and required no treatment. There were no other adverse reactions to this drug during this study
Time course of action and endotracheal intubating conditions of Org 9487, a new short-acting steroidal muscle relaxant; a comparison with succinylcholine
No full textIn a randomized study, we evaluated lag time (time from the end of injection of muscle relaxant until the first depression of the train-of-four response [TOF]), onset time (time from the end of injection of muscle relaxant until the maximum depression of the first twitch of the TOF [T1]), neuromuscular block, and endotracheal intubating conditions at 1 min after 1 mg/kg succinylcholine (n = 15) and 1.5 mg/kg Org 9487 (n = 30). Two minutes after administration of Org 9487, 15 of the 30 patients received neostigmine for reversal. Recovery of neuromuscular block after succinylcholine, Org 9487 without and Org 9487 with neostigmine were compared using the time until T1 was 90% for the succinylcholine group, and the time until TOF was 70% for the Org 9487 groups. Neuromuscular transmission was monitored mechanomyographically. Onset time was similar (67 [20] and 83 [38] s for succinylcholine and Org 9487, respectively) and endotracheal intubating conditions were also similar after both muscle relaxants. Times until clinically sufficient recovery of neuromuscular block induced by succinylcholine (time until T1 = 90%:10.6 [3.31 min) and Org 9487 with neostigmine (time until TOF = 70%: 11.6 [1.4] min) were not different. In contrast, in the Org 9487 without neostigmine group, more time was required until complete recovery (24.1 [6.2] min) (P <0.05). In conclusion, Org 9487 is a muscle relaxant suitable for endotracheal intubation and short-lasting interventions.</p
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