Administration to humans of ORG 21465, a water soluble steroid i.v. anaesthetic agent

J. R. Sneyd; P. M.C. Wright; M. Cross; P. Thompson; G. Voortman; M. M. Weideman; C. J.H. Andrews; C. J. Daniell

doi:10.1093/bja/79.4.427

Administration to humans of ORG 21465, a water soluble steroid i.v. anaesthetic agent

J. R. Sneyd^*, P. M.C. Wright, M. Cross, P. Thompson, G. Voortman, M. M. Weideman, C. J.H. Andrews, C. J. Daniell

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

Abstract

Ten 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 Q̇₁ and Q̇₂ 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.

Original language	English
Pages (from-to)	427-432
Number of pages	6
Journal	British Journal of Anaesthesia
Volume	79
Issue number	4
DOIs	https://doi.org/10.1093/bja/79.4.427
Publication status	Published - Oct 1997
Externally published	Yes

ASJC Scopus subject areas

Anesthesiology and Pain Medicine

Keywords

Anaesthetics i.v., steroid
Pharmacokinetics, ORG 21465
Pharmacology, ORG 21465
Sedation

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title = "Administration to humans of ORG 21465, a water soluble steroid i.v. anaesthetic agent",

abstract = "Ten 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 {\.Q}1 and {\.Q}2 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.",

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author = "Sneyd, {J. R.} and Wright, {P. M.C.} and M. Cross and P. Thompson and G. Voortman and Weideman, {M. M.} and Andrews, {C. J.H.} and Daniell, {C. J.}",

year = "1997",

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doi = "10.1093/bja/79.4.427",

language = "English",

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AU - Sneyd, J. R.

AU - Wright, P. M.C.

AU - Cross, M.

AU - Thompson, P.

AU - Voortman, G.

AU - Weideman, M. M.

AU - Andrews, C. J.H.

AU - Daniell, C. J.

PY - 1997/10

Y1 - 1997/10

N2 - Ten 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 Q̇1 and Q̇2 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.

AB - Ten 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 Q̇1 and Q̇2 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.

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KW - Pharmacology, ORG 21465

KW - Sedation

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Administration to humans of ORG 21465, a water soluble steroid i.v. anaesthetic agent

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ASJC Scopus subject areas

Keywords

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