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pubmed-article:9389257pubmed:abstractTextTen male volunteers received a 1-min i.v. infusion of a new water soluble steroid anaesthetic agent, ORG 21465. Individuals received doses ranging from 0.8 to 1.8 mg kg-1. All subjects experienced venous pain at the site of injection; those receiving 1.0 mg kg-1 or more became anaesthetized. There was no evidence of histamine release and apnoea did not occur. Excitatory phenomena were observed in all subjects and were dose related; no spikes were seen on the EEG. Pharmacokinetic analysis supported a three-compartment (non-weight-related) model with compartmental volumes V1, V2 and V3 of 4.31, 14.2 and 89.4 litre, respectively. Clearance from the central compartment V1 was 1.55 litre min-1. Inter-compartmental clearances Q1 and Q2 were 2.54 and 1.79 litre min-1. We found that ORG 21465 was an effective anaesthetic in humans. The relationship between sedation, anaesthesia and excitation requires further exploration.lld:pubmed
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pubmed-article:9389257pubmed:pagination427-32lld:pubmed
pubmed-article:9389257pubmed:dateRevised2007-11-15lld:pubmed
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pubmed-article:9389257pubmed:articleTitleAdministration to humans of ORG 21465, a water soluble steroid i.v. anaesthetic agent.lld:pubmed
pubmed-article:9389257pubmed:affiliationDepartment of Anaesthesia, Derriford Hospital, Plymouth, UK.lld:pubmed
pubmed-article:9389257pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:9389257pubmed:publicationTypeClinical Triallld:pubmed
pubmed-article:9389257pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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