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image/svg+xml Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao Closed Access logo, derived from PLoS Open Access logo. This version with transparent background. http://commons.wikimedia.org/wiki/File:Closed_Access_logo_transparent.svg Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao European Journal of ...arrow_drop_down
image/svg+xml Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao Closed Access logo, derived from PLoS Open Access logo. This version with transparent background. http://commons.wikimedia.org/wiki/File:Closed_Access_logo_transparent.svg Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao
European Journal of Clinical Pharmacology
Article . 1994 . Peer-reviewed
License: Springer TDM
Data sources: Crossref
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Clinical pharmacology of ORG 7617, a short-acting non-depolarizing neuromuscular blocking agent

Authors: van den Broek, L; Wierda, JMKH; PROOST, JH; Hommes, FDM; Agoston, S;

Clinical pharmacology of ORG 7617, a short-acting non-depolarizing neuromuscular blocking agent

Abstract

The dose-response relationship and the time course of action of Org 7617, a short acting non-depolarizing neuromuscular blocking agent, were evaluated during thiopentone, fentanyl, halothane and N2O anaesthesia. Neuromuscular transmission was monitored mechanomyographically. The ED50 and ED90 were calculated after single bolus doses of the drug. Twelve, seven and three patients received 2.5, 3.75 or 5.0 mg.kg-1 Org 7617, respectively. Neuromuscular block was characterized by a short lag time (average 30 s) and rapid development of neuromuscular block (69-84 s). Maximum block approximated to 66%, 91% and 95%, and the duration until clinically adequate recovery (TOF ratio of 0.7) to 7.4, 12.1 and 12.2 min after 2.5, 3.75, 5 mg.kg-1 of Org 7617, respectively. The calculated ED50 and ED90 were 1.8 and 3.4 mg.kg-1. Adverse effects, including a moderate fall in systolic and diastolic arterial blood pressure and a concomitant increase in heart rate appeared to be dose-dependent. Some patients showed flushing. One patient given 5 mg/kg Org 7617 had serious adverse effects suggestive of histamine release, i.e. flushing, urticaria, tachycardia, hypotension and bronchospasm. Therefore further clinical investigations were terminated. Although its low potency and the adverse effects observed will prevent further clinical development of ORG 7617, the results do support the contention that it is feasible to develop short-acting non-depolarizing neuromuscular blocking agents from the steroidal series.

Country
Netherlands
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Keywords

Adult, Male, Time Factors, Adolescent, NEUROMUSCULAR BLOCKADE, Neuromuscular Junction, TIME COURSE OF ACTION, Blood Pressure, SUCCINYLCHOLINE, Synaptic Transmission, INTUBATING CONDITIONS, Heart Rate, DRUGS, Humans, Anesthesia, ORG 7617, SPEED, Aged, Vecuronium Bromide, Dose-Response Relationship, Drug, ANESTHETIZED CAT, Middle Aged, MUSCLE-RELAXANTS, NONDEPOLARIZING, PANCURONIUM, MODEL, ADVERSE EFFECTS, ONSET, POTENCY, DOSE-RESPONSE RELATION, Female, Neuromuscular Nondepolarizing Agents

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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
5
Average
Average
Average
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