Peringatan Keamanan

The oral LD50 is 840 mg/kg in rats and 400 mg/kg in mice.L9722

Overdose from hydroxyzine is most commonly characterized by hypersedation, but may also manifest as convulsions, stupor, nausea, and vomiting.L9677 In cases of overdose, consider the induction of vomiting and the use of gastric lavage. Other treatment should involve general symptomatic and supportive care. Hypotension may be controlled by intravenous fluids and pressors, and caffeine and sodium benzoate injection may be used to counteract any observed CNS depressant effects. Hemodialysis is unlikely to provide any benefit in the treatment hydroxyzine overdose.L9677

Hydroxyzine

DB00557

small molecule approved

Deskripsi

Hydroxyzine is a first-generation histamine H1-receptor antagonist of the dephenylmethane and piperazine classes that exhibits sedative, anxiolytic, and antiemetic properties.A1257,A187589 It was first developed in 1955,A189726 and has since remained a relatively common treatment for allergic conditions such as pruritus, urticaria, dermatoses, and histamine-mediated pruritus.L9677 The active metabolite of hydroxyzine, cetirizine, is also available as an active ingredient in allergic medications, and is responsible for much of its hydroxyzine's antihistaminic effect.A189753 Hydroxyzine is also used for generalized anxiety disorder, tension caused by psychoneurosis, and other conditions with manifestations of anxiety.L9677

Struktur Molekul 2D

Berat 374.904
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of hydroxyzine is reportedly 14-25 hours,[A1257] and appears to be, on average, shorter in children (~7.1 hours) than in adults (~20 hours).[A644] Elimination half-life is prolonged in the elderly, averaging approximately 29 hours,[A187814] and is likely to be similarly prolonged in patients with renal or hepatic impairment.[L9680]
Volume Distribusi The mean volume of distribution is 16.0 ± 3.0 L/kg. Higher concentrations are found in the skin than in the plasma.[A1257]
Klirens (Clearance) Clearance of hydroxyzine has been reported to be 31.1 ± 11.1 mL/min/kg in children and 9.8 ± 3.3 mL/min/kg in adults.[A644]

Absorpsi

The absolute bioavailability of hydroxyzine has not been ascertained, as intravenous formulations are unavailable due to a risk of hemolysis.A1257 Hydroxyzine is rapidly absorbed from the gastrointestinal tract upon oral administration,L9677 reaching its maximum plasma concentration (Tmax) approximately 2 hours following administration.A189705

Metabolisme

Hydroxyzine is metabolized in the liverA1257 by CYP3A4 and CYP3A5.L9677 While the precise metabolic fate of hydroxyzine is unclear, its main and active metabolite (~45 to 60% of an orally administered dose),A189753 generated by oxidation of its alcohol moiety to a carboxylic acid, is the second-generation antihistamine cetirizine.A1257 Hydroxyzine is likely broken down into several other metabolites, though specific structures and pathways have not been elucidated in humans.A189699

Rute Eliminasi

Approximately 70% of hydroxyzine's active metabolite, cetirizine, is excreted unchanged in the urine.A187814 The precise extent of renal and fecal excretion in humans has not been determined.L9677

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Co-administration with alcohol may potentiate the CNS adverse effects of hydroxyzine.
  • 2. Avoid grapefruit products. Co-administration with grapefruit inhibits hydroxyzine metabolism and can result in elevated serum concentrations.

Interaksi Obat

1239 Data
Buprenorphine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Botulinum toxin type B Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Botulinum toxin type B.
Botulinum toxin type A Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Botulinum toxin type A.
Tryptophan Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Tryptophan.
Fluvoxamine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Fluvoxamine.
Baclofen Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
Lorazepam Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Lorazepam.
Ethchlorvynol Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Ethchlorvynol.
Tramadol Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Tramadol.
Succinylcholine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Succinylcholine.
Reserpine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Reserpine.
Eletriptan Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Eletriptan.
Enflurane Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Temazepam Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Temazepam.
Reboxetine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Reboxetine.
Butabarbital Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
Butalbital Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
Methysergide Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Methysergide.
Cabergoline Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Cabergoline.
Phenytoin Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Phenytoin.
Topiramate Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
Etomidate Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Etomidate.
Morphine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Morphine.
Talbutal Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Talbutal.
Pentobarbital Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
Zolmitriptan Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Zolmitriptan.
Codeine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Codeine.
Dihydroergotamine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Dihydroergotamine.
Tolcapone Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Hydromorphone Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
Clobazam Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
Chlorzoxazone Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
Meprobamate Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
Thiethylperazine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Thiethylperazine.
Palonosetron Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Palonosetron.
Carisoprodol Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Carisoprodol.
Eszopiclone Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Eszopiclone.
Alprazolam Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
Loxapine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
Remoxipride Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Remoxipride.
Metocurine iodide Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Metocurine iodide.
Secobarbital Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Secobarbital.
Methocarbamol Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Methocarbamol.
Zolpidem Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Metharbital Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Metharbital.
Dronabinol Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Dronabinol.
Methohexital Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
Chlordiazepoxide Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Chlordiazepoxide.
Duloxetine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Duloxetine.
Gallamine triethiodide Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Gallamine triethiodide.
Nabilone Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Nabilone.
Entacapone Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Entacapone.
Oxycodone Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
Triflupromazine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Triflupromazine.
Dextromethorphan Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Dextromethorphan.
Mephenytoin Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Mephenytoin.
Adinazolam Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Adinazolam.
Carbamazepine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Carbamazepine.
Cisatracurium Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Cisatracurium.
Fenfluramine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Fenfluramine.
Mazindol Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Mazindol.
Fluticasone propionate Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Fluticasone propionate.
Lisuride Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Lisuride.
Thiopental Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Thiopental.
Butorphanol Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
Furazolidone Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Furazolidone.
Paramethadione Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Paramethadione.
Fluphenazine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Fluphenazine.
Clorazepic acid Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Clorazepic acid.
Dexmedetomidine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Dexmedetomidine.
Dyclonine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Dyclonine.
Dextropropoxyphene Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Dextropropoxyphene.
Pentazocine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Pentazocine.
Magnesium sulfate Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Magnesium sulfate.
Metaxalone Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Trimethobenzamide Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Trimethobenzamide.
Sumatriptan Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Sumatriptan.
Midazolam Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Midazolam.
Flurazepam Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Flurazepam.
Ergotamine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Ergotamine.
Sufentanil Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
Paroxetine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Paroxetine.
Procaine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Procaine.
Rocuronium Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Rocuronium.
Atracurium besylate Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Atracurium besylate.
Meclizine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Meclizine.
Riluzole Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Riluzole.
Scopolamine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Scopolamine.
Tranylcypromine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Tranylcypromine.
Ethotoin Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Ethotoin.
Clidinium Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Clidinium.
Oxcarbazepine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Oxcarbazepine.
Propiomazine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Propiomazine.
Phenelzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Phenelzine.
Primidone Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Primidone.
Halazepam Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Halazepam.
Alfentanil Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
Minaprine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Minaprine.
Fentanyl Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Fentanyl.
Acetazolamide Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Acetazolamide.

Target Protein

Histamine H1 receptor HRH1
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2

Referensi & Sumber

Synthesis reference: U.S. Patent 2,899,436.
Artikel (PubMed)
  • PMID: 7103423
    Clark BG, Araki M, Brown HW: Hydroxyzine-associated tardive dyskinesia. Ann Neurol. 1982 Apr;11(4):435.
  • PMID: 23330992
    Altamura AC, Moliterno D, Paletta S, Maffini M, Mauri MC, Bareggi S: Understanding the pharmacokinetics of anxiolytic drugs. Expert Opin Drug Metab Toxicol. 2013 Apr;9(4):423-40. doi: 10.1517/17425255.2013.759209. Epub 2013 Jan 21.
  • PMID: 2562944
    Simons KJ, Watson WT, Chen XY, Simons FE: Pharmacokinetic and pharmacodynamic studies of the H1-receptor antagonist hydroxyzine in the elderly. Clin Pharmacol Ther. 1989 Jan;45(1):9-14. doi: 10.1038/clpt.1989.2.
  • PMID: 21892192
    Lee BH, Lee SH, Chu D, Hyun JW, Choe H, Choi BH, Jo SH: Effects of the histamine H(1) receptor antagonist hydroxyzine on hERG K(+) channels and cardiac action potential duration. Acta Pharmacol Sin. 2011 Sep;32(9):1128-37. doi: 10.1038/aps.2011.66.
  • PMID: 22188412
    Crowe A, Wright C: The impact of P-glycoprotein mediated efflux on absorption of 11 sedating and less-sedating antihistamines using Caco-2 monolayers. Xenobiotica. 2012 Jun;42(6):538-49. doi: 10.3109/00498254.2011.643256. Epub 2011 Dec 22.
  • PMID: 2866055
    Paton DM, Webster DR: Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin Pharmacokinet. 1985 Nov-Dec;10(6):477-97.
  • PMID: 512901
    Fouda HG, Hobbs DC, Stambaugh JE: Sensitive assay for determination of hydroxyzine in plasma and its human pharmacokinetics. J Pharm Sci. 1979 Nov;68(11):1456-8. doi: 10.1002/jps.2600681134.
  • PMID: 17605150
    Martinez-Gomez MA, Villanueva-Camanas RM, Sagrado S, Medina-Hernandez MJ: Evaluation of enantioselective binding of antihistamines to human serum albumin by ACE. Electrophoresis. 2007 Aug;28(15):2635-43. doi: 10.1002/elps.200600742.
Menampilkan 8 dari 13 artikel.
Textbook
  • ISBN: 9780702080609
    How drugs act: General principles. (2020). In Rang and Dale's Pharmacology (9th ed.). Edinburgh: Elsevier.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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