Continuous sedation during spinal anaesthesia: gamma-hydroxybutyrate vs. propofol

Kleinschmidt, S.; Schellhase, C.; Mertzlufft, F.

doi:10.1097/00003643-199901000-00006

Cited by 32 publications

(10 citation statements)

References 18 publications

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“…The postsynaptic effects of GHB that we characterized occur via GABA B receptors and parallel behavioral effects such as anesthesia and coma elicited by GABA B receptor agonists. Plasma concentrations in the low millimolar range induce moderate anesthesia in humans (Kleinschmidt et al, 1999) and reach several millimolars in abuse situations (Galloway et al, 1997). GHB levels might be especially high in "acquaintance rape" settings where victims lose consciousness after intoxication.…”

Section: Postsynaptic Effects Of Ghbmentioning

confidence: 99%

γ-Hydroxybutyrate Increases a Potassium Current and Decreases the H-Current in Hippocampal Neurons via GABA_B Receptors

Schweitzer

Roberto²,

Madamba³

et al. 2004

J Pharmacol Exp Ther

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␥-Hydroxybutyrate (GHB) is used for the treatment of alcoholism and to induce absence seizures in animals, but it has also recently emerged as a drug of abuse. In hippocampal neurons, GHB may activate its own putative receptor as well as GABA B receptors to affect synaptic transmission. We used voltage-clamp recordings of rat CA1 pyramidal neurons to characterize the postsynaptic conductances affected by GHB and to further clarify the site of GHB action. Low concentrations of GHB (0.1-1 mM) did not affect postsynaptic properties, but 10 mM GHB elicited an outward current at resting potential by augmenting an inwardly rectifying potassium current and concomitantly decreased the hyperpolarization-activated H-current (I h ). Like GHB, the selective GABA Breceptor agonist baclofen (20 M) increased a potassium current and decreased I h . In the presence of 10 mM GHB, the baclofen effects were largely occluded. The selective GABA B receptor antagonist CGP 55845 [3-N[1-(S)-(3,4-dichlorophenyl)ethyl]amino-2-(S)-hydroxypropyl-p-benzyl-phosphinic acid] blocked the effects of both GHB and baclofen, whereas the putative GHB receptor antagonist 7,8,[7]annulen-6-ylidene ethanoic acid] was ineffective. The GHB and baclofen effects were prevented in the presence of 200 M barium, indicating that GHB augments a K ϩ conductance, probably a G protein-coupled inwardly rectifying K ϩ (GIRK) current. The decrease of I h by GHB and baclofen was also prevented by barium, suggesting that the diminution of I h is secondary to GIRK augmentation. Our results indicate that high GHB levels, which can be reached during abuse or intoxication, activate only GABA B receptors and not GHB receptors at the postsynaptic level to augment an inwardly rectifying K ϩ current and decrease I h .

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Section: Postsynaptic Effects Of Ghbmentioning

confidence: 99%

γ-Hydroxybutyrate Increases a Potassium Current and Decreases the H-Current in Hippocampal Neurons via GABA_B Receptors

Schweitzer

Roberto²,

Madamba³

et al. 2004

J Pharmacol Exp Ther

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“…Gamma-hydroxybutyric acid [24,28,30,39,63] Gamma-hydroxybutyric acid (GHB) is an endogenous neurotransmitter that has many similarities with GABA. It was first introduced into clinical anaesthesia in 1960, but was almost completely replaced because of its great variability in recovery time.…”

Section: Sedative-hypnotic Agentsmentioning

confidence: 99%

Sedation and analgesia for brief diagnostic and therapeutic procedures in children

Meyer¹,

Grundmann

Gottschling

et al. 2007

Eur J Pediatr

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The number of diagnostic and therapeutic procedures done outside of the operating room and the intensive care unit has increased substantially in recent years. In parallel, the management of acute pain and anxiety in children undergoing therapeutic and diagnostic procedures has developed considerably in the past two decades. The primary goal of procedural sedation and analgesia is the safe and efficacious control of emotional distress and pain. The availability of non-invasive monitoring, short-acting opioids and sedatives has broadened the possibilities of sedation and analgesia in children in diverse settings. While most of these procedures themselves pose little risk to the child, the administration of sedation or analgesia may add substantial risk to the patient. This article reviews the current status of sedation and analgesia for invasive and non-invasive procedures in children providing an evidence-based approach to several topics of importance, including patient assessment, personnel requirements, equipment, monitoring, and drugs.

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“…SO is approved in a variety of European and American countries as an intravenous anaesthetic [7,8] and as a liquid oral medication for patients with narcolepsycataplexy [9][10][11] or alcohol dependence [12,13].…”

Section: Introductionmentioning

confidence: 99%

“…GHB has a high affinity for GHB receptors which do not recognize GABA. GHB also has an indirect effect on dopaminergic, serotonergic, glutamatergic and opioidergic neural pathways [5,6].SO is approved in a variety of European and American countries as an intravenous anaesthetic [7,8] and as a liquid oral medication for patients with narcolepsycataplexy [9][10][11] or alcohol dependence [12,13].It has been well-demonstrated in animal and human studies that SO reduces alcohol consumption and suppresses alcohol withdrawal syndrome [13,14]. The pharmacological effects of SO present several similarities with those of alcohol [15][16][17].…”

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confidence: 99%

Pharmacodynamic interactions of a solid formulation of sodium oxybate and ethanol in healthy volunteers

Pross¹,

Patat²,

Vivet

et al. 2015

Brit J Clinical Pharma

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AIMThe pharmacologic effects of sodium oxybate (SO) have a number of similarities with those of alcohol. This study evaluated the pharmacodynamic interaction of SMO.IR (a solid immediate release formulation of SO) and alcohol (0.7 (males) or 0.57 (females) g kg -1 alcohol using 40% vodka). METHODSIn a randomized, double-blind, double-dummy, crossover trial, 24 healthy volunteers received randomly a) 2.25 g SMO.IR and placebo alcohol preparation, b) 2.25 g f SMO.IR and alcohol, c) 2.25 g SMO.IR matching placebo and alcohol and d) 2.25 g of SMO.IR matching placebo and placebo alcohol preparation. Objective and subjective cognitive parameters, adverse events and vital signs were assessed before, 15 and 165 min after treatment administration. RESULTSAlcohol produced the expected cognitive impairment and the expected subjective sedation rapidly after intake (from 15 min). The objective effects of SMO.IR were much less pronounced than those of alcohol. The reverse was observed for subjective complaints, which were related to lesser stimulation and greater sedation. Nevertheless, 165 min after administration this sedation feeling was less with SMO.IR than with alcohol. There was a significant interaction between SMO.IR and alcohol at 15 min (i.e. increase in alertness and stimulation and decrease in sedation). In addition, an isolated mild decrease in digit vigilance accuracy occurred at 165 min post-dose after the combination. The co-administration of SMO.IR and alcohol was safe and well-tolerated. CONCLUSIONSMO.IR and alcohol have distinct adverse effect profiles. The objective effects of SMO.IR are much less marked than those of alcohol. No deleterious interaction was observed. WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT• Sodium oxybate (SO) has been approved for the treatment of alcohol dependence in Europe. Post-market surveillance has found no significant safety issues in alcohol relapsing patients taking SO, even though SO and alcohol share several pharmacological targets and effects.• Illicit SO (also called 'street GHB' or 'liquid ecstasy') can lead to abuse, misuse, addiction, criminal use and/or overdosing, and may have long term neurotoxic effects.• SMO.IR, a solid immediate-release formulation of sodium oxybate, is being developed to reduce the risk of criminal or accidental misuse of the drug and to obtain worldwide approval for the treatment of alcohol dependence. WHAT THIS STUDY ADDS• SMO.IR and alcohol have distinct adverse effect profiles. The objective sedative effects of SMO.IR are much less marked than those of alcohol and no interaction was observed.• The dose of SMO.IR used in this study (2.25 g) is in the upper range of the therapeutic interval for alcohol dependence and is 30%-80% higher than commonly prescribed doses.• The low level of interaction between alcohol and SMO.IR may account for the good safety profile of the drug even in the context of alcohol relapses. IntroductionSodium oxybate (SO) is the name of the sodium salt of gamma-hydroxybutyric acid when used as a therapeutic agent. Gamm...

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Continuous sedation during spinal anaesthesia: gamma-hydroxybutyrate vs. propofol

Cited by 32 publications

References 18 publications

γ-Hydroxybutyrate Increases a Potassium Current and Decreases the H-Current in Hippocampal Neurons via GABA_B Receptors

γ-Hydroxybutyrate Increases a Potassium Current and Decreases the H-Current in Hippocampal Neurons via GABA_B Receptors

Sedation and analgesia for brief diagnostic and therapeutic procedures in children

Pharmacodynamic interactions of a solid formulation of sodium oxybate and ethanol in healthy volunteers

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Continuous sedation during spinal anaesthesia: gamma-hydroxybutyrate vs. propofol

Cited by 32 publications

References 18 publications

γ-Hydroxybutyrate Increases a Potassium Current and Decreases the H-Current in Hippocampal Neurons via GABAB Receptors

γ-Hydroxybutyrate Increases a Potassium Current and Decreases the H-Current in Hippocampal Neurons via GABAB Receptors

Sedation and analgesia for brief diagnostic and therapeutic procedures in children

Pharmacodynamic interactions of a solid formulation of sodium oxybate and ethanol in healthy volunteers

Contact Info

Product

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About

γ-Hydroxybutyrate Increases a Potassium Current and Decreases the H-Current in Hippocampal Neurons via GABA_B Receptors

γ-Hydroxybutyrate Increases a Potassium Current and Decreases the H-Current in Hippocampal Neurons via GABA_B Receptors