Dose-dependent absorption and elimination of gamma-hydroxybutyric acid in healthy volunteers

Palatini, Pietro; Tedeschi, L.; Frison, Giampietro; Padrini, Roberto; Zordan, Roberta; Orlando, Rocco; Gallimberti, Luigi; Gl, Gessa; Ferrara, Santo Davide

doi:10.1007/bf00265954

Cited by 191 publications

(171 citation statements)

References 14 publications

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“…GHB has an average half-life of around 20-53 min, which seems to increase at higher GHB concentration [7]. This means that after 3-9 hours (10 half-life) only 0.097% of the original drug concentration remains.…”

Section: Introductionmentioning

confidence: 99%

Electrochemical behaviour of gamma hydroxybutyric acid at a platinum electrode in acidic medium

Jiménez‐Pérez

Sevilla

Pineda

et al. 2013

Electrochimica Acta

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Abstract.Gamma Hydroxybutyric Acid (GHB), when studied in a platinum electrode using cyclic voltammetry, presented three oxidation peaks in acid solutions that correspond to the oxidation of the alcohol group to the corresponding aldehyde and carboxylic acid (succinic acid). An anodic scan of GHB yielded two characteristic waves, which indicates an oxidation process dependent on the chemical environment on the surface of the electrode. The cathodic scan presented an inverted oxidation peak with an onset partially overlapping with the tail of the cathodic peak for the reduction of the platinum oxide formed initially during the anodic scan. This inverted peak can be observed at a potential close to +0.2V (vs Ag/AgCl at pH 2) and separated 0.4 and 0.8 V from the two other oxidation peaks obtained during the anodic scan and in such conditions that the surface is particularly activated to favour this electrochemical process. The response obtained in the electronic current for the different peaks when GHB concentration and scan rate were changed allows inferring that these are the result of a potential dependent mechanism.

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Section: Introductionmentioning

confidence: 99%

Electrochemical behaviour of gamma hydroxybutyric acid at a platinum electrode in acidic medium

Jiménez‐Pérez

Sevilla

Pineda

et al. 2013

Electrochimica Acta

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“…Pharmacology SXB is a short-chain fatty acid that is rapidly absorbed after an oral dose. It has a half life of 3060 min and is metabolized by the tricarboxylic acid (Krebs) cycle to water and carbon dioxide [Palatini et al 1993]. Less than 5% of the ingested drug is eliminated unchanged in the urine [Jazz Pharmacuticals, 2005].…”

Section: Treatment Of Fibromyalgiamentioning

confidence: 99%

Sodium Oxybate: A Potential New Pharmacological Option for the Treatment of Fibromyalgia Syndrome

Swick¹

2011

Therapeutic Advances in Musculoskeletal

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Fibromyalgia syndrome (FMS) is a common disorder, characterized by diffuse pain and tenderness, stiffness, fatigue, affective disorders and significant sleep pathology. A new set of diagnostic criteria have been developed which should make it easier for a busy clinician to diagnose the condition. US Food and Drug Administration (FDA) approved medications for the treatment of FMS have, for the most part, been geared to modulate the pain pathways to give the patient some degree of relief. A different kind of pharmacological agent, sodium oxybate (SXB), is described that is currently approved for the treatment of excessive daytime sleepiness and cataplexy in patients with narcolepsy. SXB, an endogenous metabolite of the inhibitory neurotransmitter gamma-hydroxybutyrate, is thought to act independently as a neurotransmitter with a presumed ability to modulate numerous other central nervous system neurotransmitters. In addition SXB has been shown to robustly increase slow wave sleep and decrease sleep fragmentation. Several large clinical trials have demonstrated SXB's ability to statistically improve pain, fatigue and a wide array of quality of life measurements of patients with fibromyalgia. SXB is not FDA approved to treat fibromyalgia.

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“…In the last 15 years GHB (and its related analogues such as gamma-butyrolactone (GBL)) has been linked to cases of drug-facilitated sexual assault (DFSA), more commonly termed "date-rape" (7)(8)(9)(10). In such cases toxicological proof of GHB administration is difficult due to its endogenous nature (0.2 -1 mg/L in urine), and rapid elimination from the body (half-life 20 -45 min), which results in a return to baseline concentrations in urine after only 8 hours post-administration (11)(12)(13)(14)(15)(16)(17)(18).…”

Section: Introductionmentioning

confidence: 99%

Increases in Serum Growth Hormone Concentrations Associated with GHB Administration

et al. 2016

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The administration of gamma-hydroxybutyrate (GHB) has been reported to augment the increase in growth hormone (GH) secretion associated with the onset of sleep. The ability of GHB to stimulate GH production in the absence of sleep in both male and female volunteers was investigated as part of a GHB administration study.Twelve healthy volunteers (6 men and 6 women) were given a small oral dose (25 mg/kg) of GHB (as Xyrem®) at 10:00 h. Basal blood samples (as serum) were taken 10 min prior to GHB administration, with additional samples taken at 10,15,20,25,30, 45, 60, 90, 120, 150, 180, 240, 360 and 480 min post-administration. The serum concentrations of GHB were measured by GC-MS and GH by immunometric assay.Following GHB administration, volunteers exhibited effects consistent with mild sedation, i.e. relaxed with normal responses to verbal stimuli. Despite none being asleep, an increase in serum GH concentration occurred in 11 out of the 12 volunteers (5 women and 6 men). In these volunteers, peak GH concentrations occurred 45 -60 min post-administration compared to a mean serum t max for GHB of 23 min (sd = 5.4 min). The absolute increase in GH was similar for the men and women, averaging 3.4 ng/mL and 3.7 ng/mL respectively. The mean intra-individual increase in GH was much greater in males (29 times) compared with females (2 times), as males had (as expected) lower basal GH concentrations (mean = 0.26 ng/mL) compared to females (mean = 5.4 ng/mL). After maximising, the GH C max decreased rapidly (in agreement with GHB concentrations), returning to basal concentrations at around 90 -120 min post-administration. GHB administration at low therapeutic concentrations results in increases in serum GH concentrations in healthy male and female volunteers in the absence of sleep onset.3

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Dose-dependent absorption and elimination of gamma-hydroxybutyric acid in healthy volunteers

Cited by 191 publications

References 14 publications

Electrochemical behaviour of gamma hydroxybutyric acid at a platinum electrode in acidic medium

Electrochemical behaviour of gamma hydroxybutyric acid at a platinum electrode in acidic medium

Sodium Oxybate: A Potential New Pharmacological Option for the Treatment of Fibromyalgia Syndrome

Increases in Serum Growth Hormone Concentrations Associated with GHB Administration

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