Peringatan Keamanan

The oral LD50 in rats is 9690 mg/kg.L42640

There are several cases of GHB overdose in literature where individuals ingested GHB illicitly in conjunction with other drugs and alcohol. These individuals exhibited varying degrees of depressed consciousness that may fluctuate rapidly between a confusional, agitated, combative state with ataxia and coma. Emesis (even when obtunded), diaphoresis, headache, and impaired psychomotor skills have been observed. No typical pupillary changes have been described to assist in diagnosis; pupillary reactivity to light is maintained. Blurred vision has been reported. An increasing depth of coma and acidosis have been observed at higher doses. Myoclonus and tonic-clonic seizures have been reported. Respiration may be unaffected or compromised in rate and depth. Cheyne-Stokes respiration and apnea have been observed. Bradycardia and hypothermia may accompany unconsciousness, as well as muscular hypotonia, but tendon reflexes remain intact.L30598

In clinical trials, two adults experienced sodium oxybate overdose. One patient received an estimated dose of 150 g, which was more than 15 times the maximum recommended dose: this patient became unresponsive with brief periods of apnea and incontinent of urine and feces. The patient recovered without sequelae. The other patient died following a multiple drug overdose consisting of sodium oxybate and numerous other drugs.L30598

There is no known antidote for sodium oxybate; therefore, overdose should be managed with general symptomatic and supportive care, with a consideration of gastric decontamination if co-ingestants are suspected.L30598

Sodium oxybate

DB09072

small molecule approved

Deskripsi

Sodium oxybate (Xyrem) is a central nervous system (CNS) depressant used to treat cataplexy or excessive daytime sleepiness associated with narcolepsy.L30598 It is a sodium salt of gamma-Hydroxybutyric acid, an endogenous cerebral inhibitory neurotransmitter A251445 and a metabolite of the inhibitory neurotransmitter GABA.A251430 Due to its physiological effects, sodium oxybate is associated with a risk for substance misuse and abuse. Sodium oxybate has been misused to stimulate body growth and to induce euphoria, disinhibition, and sexual arousal as a "party drug" or "club drug."A18723 For safety reasons, sodium oxybate is a controlled substance only available through a restricted program in approved countries.L30598

An extended-release oral suspension formulation of sodium oxybate for narcolepsy, marketed under the brand name LUMRYZ, gained tentative FDA approval in July 2022 L42645 and was fully approved in May 2023.L46302 In some countries, sodium oxybate has been investigated and used in alcohol withdrawal syndrome (AWS) to aid abstinence maintenance in alcohol use disorders.A251440, A251445

Struktur Molekul 2D

Berat 126.087
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) GHB has an elimination half-life of 0.5 to 1 hour.[L30598]
Volume Distribusi The apparent volume of distribution of GHB ranges from 190 mL/kg to 384 mL/kg.[L30598]
Klirens (Clearance) In healthy GHB-naïve subjects who received a single oral dose of 25 mg GHB per kg of body weight, the total clearance 1228 ± 233 ?L/min.[A19403]

Absorpsi

Following oral administration of sodium oxybate, GHB is released and rapidly absorbed with an absolute bioavailability of about 88%. The plasma levels of GHB increases more than dose-proportionally, with blood levels increasing 3.7?fold as total daily dose is doubled from 4.5 g to 9 g.L30598 After administration of a single oral dose of 2.25g to 4.5g sodium oxybate, the Cmax was 27–90 ?g/mL and the mean Tmax ranged from 25 to 75 minutes.A187328 A high-fat meal delays absorption (average Tmax increased from 0.75 hr to 2 hr), reduces Cmax of GHB by 59%, and decreases systemic exposure (AUC) by 37%.L30598

Metabolisme

Animal studies suggest that metabolism is the major elimination pathway for GHB, producing carbon dioxide and water via the tricarboxylic acid (Krebs) cycle and secondarily by beta-oxidation. GHB dehydrogenase, a cytosolic NADP+-linked enzyme, converts GHB to succinic semialdehyde, which is then biotransformed to succinic acid by succinic semialdehyde dehydrogenase. Succinic acid enters the Krebs cycle where it is metabolized to carbon dioxide and water. A second mitochondrial oxidoreductase enzyme, a transhydrogenase, also catalyzes the conversion to succinic semialdehyde in the presence of ?-ketoglutarate. GHB can alternatively be converted to carbon dioxide and water via ?-oxidation mediated by 3,4-dihydroxybutyrate. No active metabolites have been identified.L30598

Rute Eliminasi

The clearance of GHB is almost entirely by biotransformation to carbon dioxide, which is then eliminated by expiration. On average, less than 5% of unchanged drug appears in human urine within 6 to 8 hours after dosing. Fecal excretion is negligible.L30598

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Alcohol can potentiate central nervous system (CNS) depression (respiratory depression, hypotension, profound sedation, syncope, and death) caused by sodium oxybate.
  • 2. Take separate from meals. Take the first nightly dose of sodium oxybate at least two hours after eating.

Interaksi Obat

666 Data
Buprenorphine Buprenorphine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Hydrocodone Hydrocodone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Magnesium sulfate Magnesium sulfate may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Methotrimeprazine Methotrimeprazine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Metyrosine Sodium oxybate may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Mirtazapine Mirtazapine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Orphenadrine Orphenadrine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Pramipexole Sodium oxybate may increase the sedative activities of Pramipexole.
Ropinirole Sodium oxybate may increase the sedative activities of Ropinirole.
Rotigotine Sodium oxybate may increase the sedative activities of Rotigotine.
Rufinamide Rufinamide may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Sodium oxybate.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Sodium oxybate.
Tryptophan Tryptophan may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Fluvoxamine Fluvoxamine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Sodium oxybate.
Reserpine Reserpine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Citalopram Citalopram may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Eletriptan Eletriptan may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Enflurane Enflurane may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Reboxetine Reboxetine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Methysergide Methysergide may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Cabergoline Cabergoline may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Phenytoin Phenytoin may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Topiramate Topiramate may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Clemastine Clemastine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Venlafaxine Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Morphine Morphine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Zolmitriptan Zolmitriptan may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Codeine Codeine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Dihydroergotamine Dihydroergotamine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Amitriptyline Amitriptyline may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Tolcapone Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Hydromorphone Hydromorphone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Cetirizine Cetirizine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Protriptyline Protriptyline may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Trimethadione Trimethadione may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Chlorzoxazone Chlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Clozapine Clozapine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Thiethylperazine Thiethylperazine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Palonosetron Palonosetron may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Sulpiride Sulpiride may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Dexbrompheniramine Dexbrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Loxapine Loxapine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Remoxipride Remoxipride may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Metocurine iodide The risk or severity of CNS depression can be increased when Metocurine iodide is combined with Sodium oxybate.
Promazine Promazine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Methocarbamol Methocarbamol may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Triprolidine Triprolidine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Prochlorperazine Prochlorperazine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Cyproheptadine Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Meperidine Meperidine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Imipramine Imipramine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Metharbital Metharbital may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Quinine Quinine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Duloxetine Duloxetine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Chlorpromazine Chlorpromazine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Gallamine triethiodide The risk or severity of CNS depression can be increased when Gallamine triethiodide is combined with Sodium oxybate.
Entacapone Entacapone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Oxycodone Oxycodone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Triflupromazine Triflupromazine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Dextromethorphan Dextromethorphan may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Mephenytoin Mephenytoin may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Nortriptyline Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Amoxapine Amoxapine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Lamotrigine Lamotrigine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Carbamazepine Carbamazepine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Cisatracurium The risk or severity of CNS depression can be increased when Cisatracurium is combined with Sodium oxybate.
Fenfluramine Fenfluramine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Mazindol Mazindol may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Fluticasone propionate Fluticasone propionate may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Lisuride Lisuride may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Ethosuximide Ethosuximide may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Cisapride Cisapride may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Butorphanol The risk or severity of CNS depression can be increased when Butorphanol is combined with Sodium oxybate.
Furazolidone Furazolidone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Paramethadione Paramethadione may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Fluphenazine Fluphenazine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Efavirenz Efavirenz may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Dyclonine Dyclonine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Dextropropoxyphene Dextropropoxyphene may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Pentazocine Pentazocine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Trazodone Trazodone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Metaxalone Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Trimethobenzamide Trimethobenzamide may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Sumatriptan Sumatriptan may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Thioridazine Thioridazine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Moricizine Moricizine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Ergotamine Ergotamine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Tizanidine Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Sufentanil Sufentanil may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Apomorphine The risk or severity of CNS depression can be increased when Apomorphine is combined with Sodium oxybate.

Target Protein

GABA(B) Receptor GABBR1
Solute carrier family 52, riboflavin transporter, member 2 SLC52A2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 16507620
    Lemon MD, Strain JD, Farver DK: Sodium oxybate for cataplexy. Ann Pharmacother. 2006 Mar;40(3):433-40; quiz 581-2. Epub 2006 Feb 28.
  • PMID: 15538955
    Brenneisen R, Elsohly MA, Murphy TP, Passarelli J, Russmann S, Salamone SJ, Watson DE: Pharmacokinetics and excretion of gamma-hydroxybutyrate (GHB) in healthy subjects. J Anal Toxicol. 2004 Nov-Dec;28(8):625-30.
  • PMID: 21447786
    Donjacour CE, Aziz NA, Roelfsema F, Frolich M, Overeem S, Lammers GJ, Pijl H: Effect of sodium oxybate on growth hormone secretion in narcolepsy patients and healthy controls. Am J Physiol Endocrinol Metab. 2011 Jun;300(6):E1069-75. doi: 10.1152/ajpendo.00623.2010. Epub 2011 Mar 29.
  • PMID: 32965954
    Dominguez A, Soca Gallego L, Parmar M: Sodium Oxybate .
  • PMID: 17381187
    Robinson DM, Keating GM: Sodium oxybate: a review of its use in the management of narcolepsy. CNS Drugs. 2007;21(4):337-54. doi: 10.2165/00023210-200721040-00007.
  • PMID: 19520267
    Huang YS, Guilleminault C: Narcolepsy: action of two gamma-aminobutyric acid type B agonists, baclofen and sodium oxybate. Pediatr Neurol. 2009 Jul;41(1):9-16. doi: 10.1016/j.pediatrneurol.2009.02.008.
  • PMID: 30043457
    van den Brink W, Addolorato G, Aubin HJ, Benyamina A, Caputo F, Dematteis M, Gual A, Lesch OM, Mann K, Maremmani I, Nutt D, Paille F, Perney P, Rehm J, Reynaud M, Simon N, Soderpalm B, Sommer WH, Walter H, Spanagel R: Efficacy and safety of sodium oxybate in alcohol-dependent patients with a very high drinking risk level. Addict Biol. 2018 Jul;23(4):969-986. doi: 10.1111/adb.12645.
  • PMID: 29219048
    Mannucci C, Pichini S, Spagnolo EV, Calapai F, Gangemi S, Navarra M, Calapai G: Sodium Oxybate Therapy for Alcohol Withdrawal Syndrome and Keeping of Alcohol Abstinence. Curr Drug Metab. 2018;19(13):1056-1064. doi: 10.2174/1389200219666171207122227.

Contoh Produk & Brand

Produk: 14 • International brands: 0
Produk
  • Lumryz
    For suspension, extended release • 4.5 g/1 • Oral • US • Approved
  • Lumryz
    For suspension, extended release • 6 g/1 • Oral • US • Approved
  • Lumryz
    For suspension, extended release • 7.5 g/1 • Oral • US • Approved
  • Lumryz
    For suspension, extended release • 9 g/1 • Oral • US • Approved
  • Lumryz
    For suspension, extended release; Kit • - • Oral • US • Approved
  • Lumryz
    For suspension, extended release; Kit • - • Oral • US • Approved
  • Lumryz
    For suspension, extended release; Kit • - • Oral • US • Approved
  • Sodium Oxybate
    Solution • .5 g/1mL • Oral • US • Generic • Approved
Menampilkan 8 dari 14 produk.

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